Compound and compositions for weight management and related conditions

Abstract

The present invention relates to a compound or a composition comprising the same for use in the treatment or in the prevention of overweightness, of obesity and / or of the overweightness and the obesity associated metabolic disfunctions or disorders and / or of the overweightness and the obesity associated noncommunicable diseases (NCDs). The present invention also relates to a use, in particular to a non-therapeutic use, of a compound or of a composition comprising the same, for managing / controlling weight, for controlling obesity, for controlling normal weight, for controlling overweightness, for supporting weight loss, for supporting weight maintenance, for suppressing food intake, for reducing appetite, for increasing lipolysis and / or for reducing / controlling weight gain.

Description

[0001] Compound and compositions for weight management and related conditions

[0002] Field of the invention

[0003] The present invention generally relates to the field of weight management and / or control.

[0004] In particular, the present invention relates to the control / maintenance of normal weight, to the control of overweightness, to the control and to the treatment of obesity, to the treatment of the overweightness and the obesity associated metabolic disfunctions or disorders and / or to the treatment of the overweightness and the obesity associated noncommunicable diseases (NCDs) treatment.

[0005] More particularly, the present invention relates to a compound, or a composition comprising the same, for use in the treatment or in the prevention of overweightness, of obesity, and / or of the overweightness and the obesity associated metabolic disfunctions or disorders, and / or of the overweightness and the obesity associated noncommunicable diseases (NCDs).

[0006] The present invention also relates to a use, in particular to a non-therapeutic use, of a compound or of a composition comprising the same, for managing I controlling weight, for controlling obesity, for controlling normal weight, for controlling overweightness, for supporting weight loss, for supporting weight maintenance, for suppressing food intake, for reducing appetite, for increasing lipolysis, for increasing energy expenditure, for reducing fat mass, for maintaining lean mass, for reducing subcutaneous adipose tissue, for increasing brown adipose tissue, and / or for reducing I controlling weight gain.

[0007] Background of the invention

[0008] According to the World Health Organization (WHO), in 2022, 2.5 billion adults aged 18 years and older were overweight, including over 890 million adults who were living with obesity. This corresponds to 43% of adults aged 18 years and over (43% of men and 44% of women) who were overweight; an increase from 1990, when 25% of adults aged 18 years and over were overweight. Inparallel, an estimated 37 million children under the age of 5 years were overweight.

[0009] Generally, overweight and obesity result from an imbalance of energy intake (diet) and energy expenditure (physical activity). In most cases obesity is a multifactorial disease due to obesogenic environments, psycho-social factors and genetic variants. In a subgroup of patients, single major etiological factors can be identified such as medications, diseases, immobilization, iatrogenic procedures, monogenic disease / genetic syndrome.

[0010] Overweight is a condition of excessive fat deposits while obesity is a chronic complex disease defined by excessive fat deposits that can impair health. Obesity can lead to increased risk of type 2 diabetes and heart disease, it can affect bone health and reproduction, it increases the risk of certain cancers and it influences the quality of living, such as sleeping or moving.

[0011] The diagnosis of overweight and obesity is made by measuring people’s weight and height and by calculating the body mass index (BMI): weight (kg) / height2(m2). The body mass index is a surrogate marker of fatness and additional measurements, such as the waist circumference, can help the diagnosis of obesity. The BMI categories for defining obesity vary by age and gender in infants, children and adolescents.

[0012] For adults, WHO defines normal weight, overweight and obesity as follows:

[0013] - normal weight is a BMI between 18.5 and 24.9;

[0014] - overweight is a BMI greater than or equal to 25 (between 25 and 29.9);

[0015] and

[0016] - obesity is a BMI greater than or equal to 30.

[0017] For children, age needs to be considered when defining overweight and obesity:

[0018] - for children under 5 years of age:

[0019] • overweight is weight-for-height greater than 2 standard deviations above WHO Child Growth Standards median; and

[0020] • obesity is weight-for-height greater than 3 standard deviations above the WHO Child Growth Standards median.for children aged between 5-19 years:

[0021] • overweight is BMI-for-age greater than 1 standard deviation above the WHO Growth Reference median; and

[0022] • obesity is greater than 2 standard deviations above the WHO Growth Reference median.

[0023] The health risks caused by overweight and obesity are well known. In 2019, higher-than-optimal BMI caused an estimated 5 million deaths from noncommunicable diseases (NCDs) such as cardiovascular diseases, diabetes, cancers, neurological disorders, chronic respiratory diseases, and digestive disorders (GBD 2019 Risk Factor Collaborators. “Global Burden of 87 Risk Factors in 204 Countries and Territories, 1990-2019: a systematic analysis for the global burden of disease study 2019”. Lancet, 2020, 396:1223-1249). Being overweight in childhood and adolescence affects children’s and adolescents’ immediate health and is associated with greater risk and earlier onset of various NCDs, such as type 2 diabetes and cardiovascular diseases. Children with obesity are very likely to be adults with obesity and are also at a higher risk of developing NCDs in adulthood.

[0024] The economic impacts of the obesity epidemic are also important. If nothing is done, the global costs of overweight and obesity are predicted to reach US$ 3 trillion per year by 2030 and more than US$ 18 trillion by 2060 (Okunogbe et aL, “Economic Impacts of Overweight and Obesity.” 2nd Edition with Estimates for 161 Countries. World Obesity Federation, 2022).

[0025] Overweight and obesity, as well as their related noncommunicable diseases, are preventable and manageable. At the individual level, people may be able to reduce their risk by adopting preventive interventions at each step of the life cycle, starting from pre-conception and continuing during the early years. These include ensuring appropriate weight gain during pregnancy; practicing exclusive breastfeeding in the first 6 months after birth and continued breastfeeding until 24 months or beyond; supporting behaviors of children around healthy eating, physical activity, sedentary behaviors and sleep, regardless of current weight status; limiting screen time; limiting consumption of sugar sweetened beverages and energy-dense foods and promote other healthy eating behaviors; enjoying a healthy life (healthy diet, physical activity, sleep durationand quality, avoid tobacco and alcohol, emotional self-regulation); limiting energy intake from total fats and sugars and increase consumption of fruit and vegetables, as well as legumes, whole grains and nuts; and engaging in regular physical activity. At the same time, health practitioners need to assess the weight and height of people accessing the health facilities; provide counselling on healthy diet and lifestyles; when a diagnosis of obesity is established, provide integrated obesity prevention and management health services including on healthy diet, physical activity and medical and surgical measures; and monitor other NCD risk factors (blood glucose, lipids and blood pressure) and assess the presence of comorbidities and disability, including mental health disorders.

[0026] However, even if all these recommendations are followed, and even if follow-up is carried out with a health practitioner, the fact remains that overweight and obesity remain major issues with a major impact on the world's population in terms of health and cost to society, as indicated above.

[0027] Consequently, there is a real need for providing an effective compound and / or an effective composition comprising the same for use in the treatment or in the prevention of overweightness, of obesity and / or of the overweightness and the obesity associated metabolic disfunctions or disorders and / or of the overweightness and the obesity associated noncommunicable diseases (NCDs). There is also a real need for providing an effective compound and / or an effective composition comprising the same for a use, in particular for a non-therapeutic use, for managing I controlling weight, for controlling obesity, for controlling normal weight, for controlling overweightness, for supporting weight loss, for supporting weight maintenance, for suppressing food intake, for reducing appetite, for increasing lipolysis, for increasing energy expenditure, and / or for reducing I controlling weight gain.

[0028] Summary of the invention

[0029] It is an object of the invention to provide an effective compound, and / or an effective composition comprising the same, for use in the treatment or in the prevention of overweightness, of obesity and / or of the overweightness and the obesity associated metabolic disfunctions or disorders and / or of the overweightness and the obesity associated noncommunicable diseases (NCDs).Another object of the invention is to provide an effective compound, and / or an effective composition comprising the same, for a use, in particular for a non-therapeutic use, for managing / controlling weight, for controlling obesity, for controlling / maintaining normal weight, for controlling overweightness, for supporting weight loss, for supporting weight maintenance, for suppressing food intake, for reducing appetite, for increasing lipolysis, for reducing / controlling weight gain, for reducing fat mass, for maintaining lean mass, for reducing subcutaneous adipose tissue, for increasing energy expenditure, and / or for increasing brown adipose tissue.

[0030] To this end, according to the invention, there is provided a compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same, for use in the treatment or in the prevention of overweightness, of obesity and / or of the overweightness and the obesity associated metabolic disfunctions or disorders and / or of the overweightness and the obesity associated noncommunicable diseases (NCDs),

[0031]

[0032] Formula (I) wherein each of R1 is a C1-4 alkyl, each of R2 is selected from H or COOH, n is an integer equal to 0, 2 or 3, m is an integer equal to 1 or 2, and X is selected from the H or an inorganic cation, wherein the inorganic cation is selected from an alkali metal cation or an alkaline earth metal cation.

[0033] In some embodiments, the present invention provides non-therapeutic use of a compound (C) according to Formula (I), or of stereoisomer thereof, or of a composition comprising the same, for managing / controlling weight, for controlling / maintaining normal weight, for controlling / preventing overweightness, for supporting weight loss, for supporting weight maintenance, for controlling / suppressing food intake, for controlling / reducing appetite, for reducing / controlling / preventing weight gain, for reducing fat mass, maintaining lean mass, reducing subcutaneous adipose tissue, increasing energy expenditure, and / or increasing brown adipose tissue

[0034]

[0035] Formula (I) wherein each of R1 is a C1-4 alkyl, each of R2 is selected from H or COOH, n is an integer equal to 0, 2 or 3, m is an integer equal to 1 or 2, and X is selected from the H or an inorganic cation, wherein the inorganic cation is selected from an alkali metal cation or an alkaline earth metal cation.

[0036] In some embodiments, the present invention provides non-therapeutic use of a compound (C) according to Formula (I), or of stereoisomer thereof, or of a composition comprising the same, for managing / controlling weight, for controlling / maintaining normal weight, for controlling / preventing overweightness, for supporting weight loss, for supporting weight maintenance, for controlling / suppressing food intake, for controlling / reducing appetite, for reducing / controlling / preventing weight gain, for reducing fat mass, maintaining lean mass, reducing subcutaneous adipose tissue, and / or increasing brown adipose tissue

[0037]

[0038] Formula (I) wherein each of R1 is a C1-4 alkyl, each of R2 is selected from H or COOH, n is an integer equal to 0, 2 or 3, m is an integer equal to 1 or 2, and X is selected from the H or an inorganic cation, wherein the inorganic cation is selected from an alkali metal cation or an alkaline earth metal cation.

[0039] In some embodiments, the present invention provides non-therapeutic use of a compound (C) according to Formula (I), or of stereoisomer thereof, or of a composition comprising the same, for increasing energy expenditure

[0040]

[0041] Formula (I)wherein each of R1 is a C1-4 alkyl, each of R2 is selected from H or COOH, n is an integer equal to 0, 2 or 3, m is an integer equal to 1 or 2, and X is selected from the H or an inorganic cation, wherein the inorganic cation is selected from an alkali metal cation or an alkaline earth metal cation.

[0042] In some embodiments, the present invention provides non-therapeutic use of a compound (C) according to Formula (I), or of stereoisomer thereof, or of a composition comprising the same, for enhancing thermogenic capacity for increasing energy expenditure

[0043]

[0044] Formula (I) wherein each of Ri is a C1-4 alkyl, each of R2 is selected from H or COOH, n is an integer equal to 0, 2 or 3, m is an integer equal to 1 or 2, and X is selected from the H or an inorganic cation, wherein the inorganic cation is selected from an alkali metal cation or an alkaline earth metal cation.

[0045] In some embodiments, the present invention provides non-therapeutic use of a compound (C) according to Formula (He), or of stereoisomer thereof, or of a composition comprising the same, for managing / controlling weight, for controlling / maintaining normal weight, for controlling / preventing overweightness, for supporting weight loss, for supporting weight maintenance, for controlling / suppressing food intake, for controlling / reducing appetite, and / or for reducing / controlling / preventing weight gain, for reducing fat mass, maintaining lean mass, reducing subcutaneous adipose tissue, for increasing energy expenditure, and / or increasing brown adipose tissue

[0046]

[0047] Formula (He).

[0048] In some embodiments, the present invention provides non-therapeutic use of a compound (C) according to Formula (He), or of stereoisomer thereof, or of a composition comprising the same, for managing / controlling weight, for controlling / maintaining normal weight, for controlling / preventing overweightness,for supporting weight loss, for supporting weight maintenance, for controlling / suppressing food intake, for controlling / reducing appetite, and / or for reducing / controlling / preventing weight gain, for reducing fat mass, maintaining lean mass, reducing subcutaneous adipose tissue, and / or increasing brown adipose tissue

[0049]

[0050] Formula (He).

[0051] In some embodiments, the present invention provides non-therapeutic use of a compound (C) according to Formula (He), or of stereoisomer thereof, or of a composition comprising the same, for increasing energy expenditure

[0052]

[0053] Formula (He).

[0054] In some embodiments, the present invention provides non-therapeutic use of a compound (C) according to Formula (He), or of stereoisomer thereof, or of a composition comprising the same, for enhancing thermogenic capacity for increasing energy expenditure

[0055]

[0056] Formula (He).

[0057] In some embodiments, the present invention provides non-therapeutic use of a compound (C) according to Formula (He), or of stereoisomer thereof, or of a composition comprising the same, wherein at least one gene involved in brown adipose tissue thermogenesis, mitochondrial function, lipid metabolism, adipocyte identity, and / or inflammatory modulation is modulated, such as at least one gene from the group consisting of Ucp1, Ppargcla, Cidea, Dio2, and Elovl3 is upregulated, particularly upregulated in brown adipose tissue.In some embodiments, the present invention provides non-therapeutic use of a compound (C) according to Formula (He), or of stereoisomer thereof, or of a composition comprising the same, wherein at least one gene from the group consisting of Ucp1, Ppargcla, Cidea, Dio2, and Elovl3 is upregulated, particularly upregulated in brown adipose tissue.

[0058] In some embodiments, the present invention provides a compound (C) according to Formula (He), or stereoisomer thereof, or a composition comprising the same, for use in increasing lipolysis, reducing LDL cholesterol, increasing HDL cholesterol, reducing triglycerides, and / or reducing free fatty acids

[0059]

[0060] Formula (He).

[0061] In some embodiments, the present invention provides a compound (C) according to Formula (He), or stereoisomer thereof, or a composition comprising the same, for use in the treatment or in the prevention of obesity, obesity associated metabolic disfunctions or disorders, and obesity associated noncommunicable diseases (NCDs),

[0062]

[0063] Formula (He).

[0064] In some embodiments, the present invention provides a compound (C) according to Formula (He), or stereoisomer thereof, or the composition comprising the same, for preventive and / or therapeutic use as described herein, wherein metabolic syndrome includes dyslipidemia.

[0065] In some embodiments, the present invention provides a compound (C) according to Formula (He), or stereoisomer thereof, or a composition comprising the same, for use as described herein, wherein at least one gene involved in brown adipose tissue thermogenesis, mitochondrial function, lipid metabolism, adipocyte identity, and / or inflammatory modulation is modulated, such as at least one gene from the group consisting of Ucp1, Ppargcla, Cidea, Dio2, and Elovl3 is upregulated, particularly upregulated in brown adipose tissue.In some embodiments, the present invention provides a compound (C) according to Formula (He), or stereoisomer thereof, or a composition comprising the same, for use as described herein, wherein at least one gene from the group consisting of Ucp1, Ppargcla, Cidea, Dio2, and Elovl3 is upregulated, particularly upregulated in brown adipose tissue.

[0066] In some embodiments, the present invention provides a compound (C) according to Formula (He), or stereoisomer thereof, or the composition comprising the same, for preventive and / or therapeutic use as described herein, wherein the associated metabolic disfunctions or disorders and / or associated noncommunicable diseases (NCDs) are selected from the group consisting of hypertension, liver cirrhosis, metabolic syndrome, cardiovascular diseases, cancers, neurological disorders, chronic respiratory diseases, digestives disorders, and combinations thereof.

[0067] In some embodiments, the present invention provides non-therapeutic use of a compound (C) according to Formula (I), or of stereoisomer thereof, or of a composition comprising the same, for reducing fat mass, maintaining lean mass, reducing subcutaneous adipose tissue, increasing energy expenditure, and / or increasing brown adipose tissue

[0068]

[0069] Formula (I)

[0070] wherein each of Ri is a C1-4 alkyl, each of R2 is selected from H or COOH, n is an integer equal to 0, 2 or 3, m is an integer equal to 1 or 2, and X is selected from H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

[0071] In some embodiments, the present invention provides non-therapeutic use of a compound (C) according to Formula (I), or of stereoisomer thereof, or of a composition comprising the same, for reducing fat mass, maintaining lean mass, reducing subcutaneous adipose tissue, and / or increasing brown adipose tissue

[0072]

[0073] Formula (I) wherein each of Ri is a C1-4 alkyl, each of R2 is selected from H or COOH, n is an integer equal to 0, 2 or 3, m is an integer equal to 1 or 2, and X is selected from H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

[0074] In some embodiments, the present invention provides non-therapeutic use of a compound (C) according to Formula (I), or of stereoisomer thereof, or of a composition comprising the same, for increasing energy expenditure

[0075]

[0076] Formula (I) wherein each of R1 is a C1-4 alkyl, each of R2 is selected from H or COOH, n is an integer equal to 0, 2 or 3, m is an integer equal to 1 or 2, and X is selected from H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

[0077] In some embodiments, the present invention provides non-therapeutic use of a compound (C) according to Formula (I), or of stereoisomer thereof, or of a composition comprising the same, for enhancing thermogenic capacity for increasing energy expenditure

[0078]

[0079] Formula (I) wherein each of R1 is a C1-4 alkyl, each of R2 is selected from H or COOH, n is an integer equal to 0, 2 or 3, m is an integer equal to 1 or 2, and X is selected from H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.In some embodiments, the present invention provides on-therapeutic use of a compound (C) according to Formula (I), or of stereoisomer thereof, or of a composition comprising the same, as described herein wherein at least one gene involved in brown adipose tissue thermogenesis, mitochondrial function, lipid metabolism, adipocyte identity, and / or inflammatory modulation is modulated, such as at least one gene from the group consisting of Ucp1, Ppargcla, Cidea, Dio2, and Elovl3 is upregulated, particularly upregulated in brown adipose tissue.

[0080] In some embodiments, the present invention provides on-therapeutic use of a compound (C) according to Formula (I), or of stereoisomer thereof, or of a composition comprising the same, as described herein wherein at least one gene from the group consisting of Ucp1, Ppargcla, Cidea, Dio2, and Elovl3 is upregulated, particularly upregulated in brown adipose tissue.

[0081] In some embodiments, the present invention provides a compound (C) according to Formula (I), or stereoisomer thereof, or a composition comprising the same, for use in the treatment or in the prevention of obesity associated metabolic disfunctions or disorders, and obesity associated noncommunicable diseases (NCDs),

[0082]

[0083] Formula (I)

[0084] wherein each of Ri is a C1-4 alkyl, each of R2 is selected from H or COOH, n is an integer equal to 0, 2 or 3, m is an integer equal to 1 or 2, and X is selected from H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

[0085] In some embodiments, the present invention provides a compound (C) according to Formula (I), or stereoisomer thereof, or a composition comprising the same, for use as described herein, wherein the associated metabolic disfunctions or disorders and / or associated noncommunicable diseases (NCDs) are selected from the group consisting of hypertension, liver cirrhosis, metabolic syndrome, cardiovascular diseases, cancers, neurological disorders, chronic respiratory diseases, and combinations thereof.In some embodiments, the present invention provides a compound (C) according to Formula (I), or stereoisomer thereof, or a composition comprising the same, for use as described herein, wherein metabolic syndrome includes dyslipidemia.

[0086] In some embodiments, the present invention provides a compound (C) according to Formula (I), or stereoisomer thereof, or a composition comprising the same, for use in increasing lipolysis, reducing LDL cholesterol, increasing HDL cholesterol, reducing triglycerides, and / or reducing free fatty acids

[0087]

[0088] Formula (I)

[0089] wherein each of Ri is a C1-4 alkyl, each of R2 is selected from H or COOH, n is an integer equal to 0, 2 or 3, m is an integer equal to 1 or 2, and X is selected from H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

[0090] In some embodiments, the present invention provides a compound (C) according to Formula (I), or stereoisomer thereof, or a composition comprising the same, for use as described herein, wherein at least one gene involved in brown adipose tissue thermogenesis, mitochondrial function, lipid metabolism, adipocyte identity, and / or inflammatory modulation is modulated, such as at least one gene from the group consisting of Ucp1, Ppargcla, Cidea, Dio2, and Elovl3 is upregulated, particularly upregulated in brown adipose tissue.

[0091] In some embodiments, the present invention provides a compound (C) according to Formula (I), or stereoisomer thereof, or a composition comprising the same, for use as described herein, wherein at least one gene from the group consisting of Ucp1, Ppargcla, Cidea, Dio2, and Elovl3 is upregulated, particularly upregulated in brown adipose tissue.

[0092] In some embodiments, the present invention provides a method for treating or preventing overweightness, obesity, and / or overweightness and obesity associated metabolic disfunctions or disorders, and / or overweightness and obesity associated noncommunicable diseases (NCDs), or for managing / controlling weight, for controlling obesity, for controlling / maintainingnormal weight, for controlling overweightness, for supporting weight loss, for supporting weight maintenance, for suppressing food intake, for reducing appetite, for increasing lipolysis, for reducing / controlling weight gain, for reducing fat mass, for maintaining lean mass, for reducing subcutaneous adipose tissue, for increasing energy expenditure, and / or for increasing brown adipose tissue, comprising the step of administering an effective amount of a compound (C) according to general Formula (He)

[0093] >

[0094]

[0095] Formula (He).

[0096] In some embodiments, the present invention provides a method for treating or preventing overweightness, obesity, and / or overweightness and obesity associated metabolic disfunctions or disorders, and / or overweightness and obesity associated noncommunicable diseases (NCDs), or for managing / controlling weight, for controlling obesity, for controlling / maintaining normal weight, for controlling overweightness, for supporting weight loss, for supporting weight maintenance, for suppressing food intake, for reducing appetite, for increasing lipolysis, for reducing / controlling weight gain, for reducing fat mass, for maintaining lean mass, for reducing subcutaneous adipose tissue, and / or for increasing brown adipose tissue, comprising the step of administering an effective amount of a compound (C) according to general Formula (He)

[0097] > >

[0098]

[0099] Formula (He).

[0100] In some embodiments, the present invention provides a method for increasing energy expenditure, comprising the step of administering an effective amount of a compound (C) according to general Formula (He)

[0101] >

[0102]

[0103] Formula (He).In some embodiments, the present invention provides a method for enhancing thermogenic capacity for increasing energy expenditure, comprising the step of administering an effective amount of a compound (C) according to general Formula

[0104]

[0105] Formula (He).

[0106] In some embodiments, the present invention provides a method comprising the step of administering an effective amount of a compound (C) according to general Formula (He) as described herein, wherein at least one gene involved in brown adipose tissue thermogenesis, mitochondrial function, lipid metabolism, adipocyte identity, and / or inflammatory modulation is modulated, such as at least one gene from the group consisting of Ucp1, Ppargcla, Cidea, Dio2, and Elovl3 is upregulated, particularly upregulated in brown adipose tissue.

[0107] In some embodiments, the present invention provides a method comprising the step of administering an effective amount of a compound (C) according to general Formula (He) as described herein, wherein at least one gene from the group consisting of Ucp1, Ppargcla, Cidea, Dio2, and Elovl3 is upregulated, particularly upregulated in brown adipose tissue.

[0108] In some embodiments, the present invention provides a method comprising the step of administering an effective amount of a compound (C) according to general Formula (He) as described herein, wherein the associated metabolic disfunctions or disorders and / or associated noncommunicable diseases (NCDs) are selected from the group consisting of hypertension, liver cirrhosis, metabolic syndrome, cardiovascular diseases, cancers, neurological disorders, chronic respiratory diseases, and combinations thereof.

[0109] In some embodiments, the present invention provides a method for reducing LDL cholesterol, increasing HDL cholesterol, reducing triglycerides, and / or reducing free fatty acids, comprising the step of administering an effective amount of a compound (C) according to general Formula (He)

[0110]

[0111] Formula (He).

[0112] In some embodiments, the present invention provides a method for treating or preventing overweightness, obesity, and / or overweightness and obesity associated metabolic disfunctions or disorders, and / or overweightness and obesity associated noncommunicable diseases (NCDs), or for managing / controlling weight, for controlling obesity, for controlling / maintaining normal weight, for controlling overweightness, for supporting weight loss, for supporting weight maintenance, for suppressing food intake, for reducing appetite, for increasing lipolysis, for reducing / controlling weight gain, for reducing fat mass, for maintaining lean mass, for reducing subcutaneous adipose tissue, for increasing energy expenditure, and / or for increasing brown adipose tissue, comprising the step of administering an effective amount of a compound (C) according to general Formula (I)

[0113]

[0114] Formula (I) wherein each of R1 is a C1-4 alkyl, each of R2 is selected from H or COOH, n is an integer equal to 0, 2 or 3, m is an integer equal to 1 or 2, and X is selected from H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

[0115] In some embodiments, the present invention provides a method for treating or preventing overweightness, obesity, and / or overweightness and obesity associated metabolic disfunctions or disorders, and / or overweightness and obesity associated noncommunicable diseases (NCDs), or for managing / controlling weight, for controlling obesity, for controlling / maintaining normal weight, for controlling overweightness, for supporting weight loss, for supporting weight maintenance, for suppressing food intake, for reducing appetite, for increasing lipolysis, for reducing / controlling weight gain, for reducing fat mass, for maintaining lean mass, for reducing subcutaneous adipose tissue,and / or for increasing brown adipose tissue, comprising the step of administering an effective amount of a compound (C) according to general Formula (I)

[0116]

[0117] Formula (I) wherein each of R1 is a C1-4 alkyl, each of R2 is selected from H or COOH, n is an integer equal to 0, 2 or 3, m is an integer equal to 1 or 2, and X is selected from H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

[0118] In some embodiments, the present invention provides a method for increasing energy expenditure, comprising the step of administering an effective amount of a compound (C) according to general Formula (I)

[0119]

[0120] Formula (I) wherein each of Ri is a Ci-4 alkyl, each of Fte is selected from H or COOH, n is an integer equal to 0, 2 or 3, m is an integer equal to 1 or 2, and X is selected from H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

[0121] In some embodiments, the present invention provides a method for enhancing thermogenic capacity for increasing energy expenditure, comprising the step of administering an effective amount of a compound (C) according to general Formula (I)

[0122]

[0123] Formula (I) wherein each of R1 is a C1-4 alkyl, each of R2 is selected from H or COOH, n is an integer equal to 0, 2 or 3, m is an integer equal to 1 or 2, and X is selectedfrom H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

[0124] In some embodiments, the present invention provides a method comprising the step of administering an effective amount of a compound (C) according to general Formula (I) as described herein, wherein at least one gene involved in brown adipose tissue thermogenesis, mitochondrial function, lipid metabolism, adipocyte identity, and / or inflammatory modulation is modulated, such as at least one gene from the group consisting of Ucp1, Ppargcla, Cidea, Dio2, and Elovl3 is upregulated, particularly upregulated in brown adipose tissue.

[0125] In some embodiments, the present invention provides a method comprising the step of administering an effective amount of a compound (C) according to general Formula (I) as described herein, wherein at least one gene from the group consisting of Ucp1, Ppargcla, Cidea, Dio2, and Elovl3 is upregulated, particularly upregulated in brown adipose tissue.

[0126] In some embodiments, the present invention provides a method comprising the step of administering an effective amount of a compound (C) according to general Formula (I) as described herein, wherein the associated metabolic disfunctions or disorders and / or associated noncommunicable diseases (NCDs) are selected from the group consisting of hypertension, liver cirrhosis, metabolic syndrome, cardiovascular diseases, cancers, neurological disorders, chronic respiratory diseases, and combinations thereof.

[0127] In some embodiments, the present invention provides a method for reducing LDL cholesterol, increasing HDL cholesterol, reducing triglycerides, and / or reducing free fatty acids, comprising the step of administering an effective amount of a compound (C) according to general Formula (I)

[0128]

[0129] Formula (I) wherein each of Ri is a Ci-4 alkyl, each of Fte is selected from H or COOH, n is an integer equal to 0, 2 or 3, m is an integer equal to 1 or 2, and X is selected from H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.Figures

[0130] Fig 1 : Analysis of body weight gain

[0131] Fig 2: Endpoint analysis of body weight gain

[0132] Fig 3: Analysis of food intake

[0133] Fig 4: Analysis of mean water intake

[0134] Fig 5: Analysis of cumulative water intake

[0135] Fig 6: Analysis of fat mass

[0136] Fig 7: Analysis of lean mass

[0137] Fig 8: Analysis of subcutaneous adipose tissue

[0138] Fig 9: Analysis of brown adipose tissue

[0139] Fig 10: Analysis of HDL cholesterol

[0140] Fig 11 : Analysis of LDL cholesterol

[0141] Fig 12: Analysis of triglycerides

[0142] Fig 13: Analysis of free fatty acids

[0143] Fig 14: Analysis of Ucp-1 gene in BAT

[0144] Fig 15: Analysis of Ppargcla gene in BAT

[0145] Fig 16: Analysis of Dio2 gene in BAT

[0146] Fig 17: Analysis of Cidea gene in BAT

[0147] Fig 18: Analysis of Elovl3 gene in BAT

[0148] Fig 19: Analysis of Tnfa gene in BAT

[0149] Fig 20: Analysis of Ptergene in BAT

[0150] Detailed description

[0151] Definitions

[0152] In the present specification, the following terms have the following meanings:

[0153] “Body mass index" or "BMI" is the ratio of weight in kg divided by the height in metres, squared.

[0154] “Normal weight” is defined for an adult human as having a BMI between 18.5 and 24.9. In the context of the present invention, individuals presenting a normal weight and having a BMI between 18.5 and 24.9 are particularly targeted, in particular for controlling obesity, for controlling I maintaining normal weight, for controlling overweightness, for supporting weight loss, for supporting weightmaintenance, for suppressing food intake, for reducing appetite, for increasing lipolysis, for increasing energy expenditure, and / or for reducing I controlling weight gain. In particular, it may be understood that the increase in energy expenditure can be through different avenues, such as thermogenesis (e.g. via brown adipose tissue), muscle energy expenditure (e.g. via maintenance of lean mass), enhanced thermogenic capacity, etc.

[0155] "Overweight" is defined for an adult human as having a BMI between 25 and 30 and is a condition of excessive fat deposits.

[0156] "Obesity" is a condition in which the natural energy reserve, stored in the fatty tissue of animals (including humans), is increased to a point where it is associated with certain health conditions or increased mortality. Obesity is recognized as being a disease defined by excessive fat deposits that can impair health. “Obese” is defined for an adult human as having a BMI greater than 30.

[0157] “Non communicable diseases (NCDs)” refers to a group of conditions that are not mainly caused by an acute infection, result in long-term health consequences and often create a need for long-term treatment and care. These conditions include cancers, cardiovascular disease, diabetes and chronic lung illnesses.

[0158] “Metabolic syndrome” refers to the co-occurrence of several known cardiovascular risk factors, including insulin resistance, obesity, dyslipidemia, atherogenic dyslipidemia, and hypertension. One way of addressing dyslipidemia and atherogenic dyslipidemia is through increasing lipolysis.

[0159] “Modulation” as used herein refers to a change in the expression level of a specific gene, such that the amount of its RNA transcript and / or corresponding protein product is different under the conditions of interest compared to a reference condition, such as upregulation or downregulation. This change can be, for example, due to change in transcriptional activity, RNA stability, translation efficiency, or change in degradation of the gene product.

[0160] “Upregulated” as used herein refers to an increase in the expression level of a specific gene, such that the amount of its RNA transcript and / or corresponding protein product is higher under the conditions of interest compared to a reference condition. This increase can be, for example, due to enhancedtranscriptional activity, increased RNA stability, improved translation efficiency, or reduced degradation of the gene product.

[0161] "Alkyl" has the broadest meaning generally understood in the art, and may include a moiety which is linear or branched, or a combination thereof.

[0162] “Alkyl” - alone or in combination refers to a straight or branched alkanederived radical, for example, CF-G alkyl defines a straight or branched alkyl radical having from F to G carbon atoms, e.g. Ci-4 alkyl defines a straight or branched alkyl radical having from 1 to 4 carbon atoms such as for example methyl, ethyl, 1 -propyl, 2-propyl (isopropyl), 1 -butyl, 2-butyl, 2-methyl-2-propyl (tert-butyl), 2-methyl-1 -propyl (isobutyl).

[0163] The term "effective amount" as used herein means that amount of active compound that elicits the biological response in a tissue, system, animal or human that is being sought, in the light of the present invention, by a researcher, veterinarian, medical doctor or other clinician such as a nutritionist, which includes alleviation of the symptoms of the disease being treated.

[0164] Compound and compositions

[0165] According to the present invention, the compound (C) is according to general Formula (I)

[0166]

[0167] Formula (I) wherein:

[0168] - each of Ri is a Ci-4 alkyl;

[0169] - each of R2 is selected from H or COOH;

[0170] - n is an integer equal to 0, 2 or 3;

[0171] - m is an integer equal to 1 or 2; and

[0172] - X is selected from H or an inorganic cation, wherein the inorganic cation is selected from an alkali metal cation and an alkaline earth metal cation.It will be understood that when n is equal to 0, S(O)n represents a thiolate (-S-) moiety.

[0173] It will be further understood that when n is equal to 2, S(O)n represents a sulfinate (-S(=O)O-) moiety.

[0174] It will be further understood that when n is equal to 3, S(O)n represents a sulfonate (-S(=O)2O-) moiety.

[0175] It will be understood that the nature of X, as detailed above, determines m. In particular, provided that X of compound (C) of the present invention is H, m is equal to 1.

[0176] In particular, provided that X of compound (C) of the present invention is an alkali metal cation ( / .e. a cation having a charge of +1 , e.g. a lithium cation, a sodium cation or a potassium cation), m is equal to 1.

[0177] In particular, provided that X of compound (C) of the present invention is an alkaline earth metal cation ( / .e. a cation having a charge of +2, e.g. a magnesium cation or a calcium cation), m is equal to 2.

[0178] Preferably, each of Ri is a C1-3 alkyl. More preferably, each of R1 is selected from CH3 or C2H5. Even more preferably each of R1 is CH3.

[0179] Preferably each of R2 is H.

[0180] Preferably, X is an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation. More preferably, X is an inorganic cation selected from the group consisting of a lithium cation, a sodium cation, a potassium cation, a magnesium cation and a calcium cation. More preferably X is selected from the group consisting of a sodium cation, a potassium cation, a magnesium cation and a calcium cation. More preferably, X is selected from a magnesium cation and a calcium cation. Even more preferably, X is a magnesium cation.

[0181] According to certain embodiments of the present invention, the compound (C) according to general Formula (I) is a compound of Formula (II) [compound (C) of class (I), herein after]:

[0182]

[0183] Formula (II)wherein R1, m and X are as defined above for Formula (I).

[0184] According to an embodiment of the present invention, compound (C) of class (I) is a compound of Formula (Ha):

[0185]

[0186] Formula (Ha) wherein:

[0187] - each of R11 is a Ci -4 alkyl;

[0188] - ml is an integer equal to 1 or 2;

[0189] - Xi is an inorganic cation selected from the group consisting of an alkali metal cation and an alkaline earth metal cation;

[0190] Preferably, each of Rn is a C1-3 alkyl; more preferably, each of R11 is selected from CH3 or C2H5; even more preferably each of R11 is CH3.

[0191] Preferably, Xi is an inorganic cation selected from the group consisting of a lithium cation, a sodium cation, a potassium cation, a magnesium cation and a calcium cation; more preferably Xi is selected from the group consisting of a sodium cation, a potassium cation, a magnesium cation and a calcium cation; more preferably, Xi is selected from a magnesium cation and a calcium cation; even more preferably, Xi is a magnesium cation.

[0192] According to a preferred embodiment of the present invention, compound (C) of class (I) is a compound of Formula (lib):

[0193]

[0194] Formula (Hb) wherein ml and Xi have the same meaning as defined above for Formula (Ila).

[0195] According to a preferred embodiment of the present invention, compound (C) of class (I) is a compound of Formula (He):

[0196]

[0197] Formula (He)It will be understood that said compound according to Formula (He) is magnesium n-acetyl taurinate.

[0198] According to another embodiment of the present invention, the compound (C) according to general Formula (I) is a compound of Formula (III) [compound (C) of class (II), hereinafter]:

[0199]

[0200] Formula (III) wherein R1, m and X are as defined above for Formula (I).

[0201] According to a preferred embodiment of the present invention, compound (C) of class (II) is a compound of Formula (Illa):

[0202]

[0203] Formula (Illa) wherein:

[0204] - each of R12 is a C1-4 alkyl;

[0205] - m2 is an integer equal to 1 or 2;

[0206] - X2 is an inorganic cation selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

[0207] Preferably, each of R12 is a C1-3 alkyl; more preferably, each of R12 is selected from CH3 or C2H5; even more preferably each of R12 is CH3.

[0208] Preferably, X2 is an inorganic cation selected from the group consisting of a lithium cation, a sodium cation, a potassium cation, a magnesium cation and a calcium cation; more preferably X2 is selected from the group consisting of a sodium cation, a potassium cation, a magnesium cation and a calcium cation; more preferably, X2 is selected from a magnesium cation and a calcium cation; even more preferably, X2 is a magnesium cation.

[0209] According to a preferred embodiment of the present invention, compound (C) of class (II) is a compound of Formula (I I lb):

[0210]

[0211] Formula (II lb) wherein m2 and X2 have the same meaning as defined above for Formula (Illa).

[0212] According to a preferred embodiment of the present invention, compound (C) of class (II) is a compound of Formula (I I Ic):

[0213]

[0214] Formula (I I Ic) According to another embodiment of the present invention, the compound (C) according to general Formula (I) is a compound of Formula (IV) [compound (C) of class (III), hereinafter]:

[0215]

[0216] Formula (IV) wherein R1, m and X are as defined above for Formula (I).

[0217] According to a preferred embodiment of the present invention, compound (C) of class (III) is a compound of Formula (IVa):

[0218]

[0219] Formula (IVa) wherein:

[0220] - each of R13 is a C1-4 alkyl;

[0221] - m3 is an integer equal to 1 or 2;

[0222] - X3 is an inorganic cation selected from the group consisting of an alkali metal cation and an alkaline earth metal cation;

[0223] Preferably, each of R13 is a C1-3 alkyl; more preferably, each of each of R13 is selected from CH3 or C2H5; even more preferably each of R13 is CH3.Preferably, X3 is an inorganic cation selected from the group consisting of a lithium cation, a sodium cation, a potassium cation, a magnesium cation and a calcium cation; more preferably X3 is selected from the group consisting of a sodium cation, a potassium cation, a magnesium cation and a calcium cation; more preferably, X3 is selected from a magnesium cation and a calcium cation; even more preferably, X3 is a magnesium cation.

[0224] According to a preferred embodiment of the present invention, compound (C) of class (III) is a compound of Formula (IVb):

[0225]

[0226] Formula (I Vb) wherein m3 and X3 have the same meaning as defined above for Formula (Va).

[0227] According to a preferred embodiment of the present invention, compound (C) of class (III) is a compound of Formula (IVc):

[0228] >

[0229]

[0230] Formula (IVc) According to another embodiment of the present invention, the compound (C) according to general Formula (I) is a compound of Formula (V) [compound (C) of class (IV), herein after]:

[0231]

[0232] Formula (V) wherein R1, m and X are as defined above for Formula (I).

[0233] According to a preferred embodiment of the present invention, compound (C) of class (IV) is a compound of Formula (Va):

[0234]

[0235] Formula (Va)wherein:

[0236] - Ri4 is a C1-4 alkyl;

[0237] - m4 is an integer equal to 1 or 2;

[0238] - X4 is an inorganic cation selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

[0239] Preferably, each of R14 is a C1-3 alkyl; more preferably, each of each of R14 is selected from CH3 or C2H5; even more preferably each of R14 is CH3.

[0240] Preferably, X4 is an inorganic cation selected from the group consisting of a lithium cation, a sodium cation, a potassium cation, a magnesium cation and a calcium cation; more preferably X4 is selected from the group consisting of a sodium cation, a potassium cation, a magnesium cation and a calcium cation; more preferably, X4 is selected from a magnesium cation and a calcium cation; even more preferably, X4 is a magnesium cation.

[0241] According to a preferred embodiment of the present invention, compound (C) of class (IV) is a compound of Formula (Vb):

[0242] >

[0243]

[0244] Formula (Vb) wherein m4 and X4 have the same meaning as defined above for Formula (IVa).

[0245] According to a preferred embodiment of the present invention, compound (C) of class (IV) is a compound of Formula (Vc):

[0246]

[0247] Formula (Vc) When any variable occurs more than one time in any constituent, each definition is independent. Whenever used hereinafter, the term ‘compounds (C) of Formula (I)”, or “the present compounds” or similar terms, it is meant to include all the compounds (C) of Formula (I), and stereochemically isomeric forms. One embodiment comprises the compounds (C) of Formula (I) or any subgroups of compounds of Formula (II), (lla)-(llc), (III), (llla)-(lllc), (IV), (IVa)-(IVc), (V), (Va)-(Vc) specified herein, as well as the possible stereoisomeric forms thereof.The compound (C) of Formula (I) as specified herein, or a compound of any of subgroups of compounds of Formula (II), (lla)-(llc), (III), (llla)-(lllc), (IV), (IVa)-(IVc), (V), (Va)-(Vc) specified herein, have several centers of chirality and exist as stereochemically isomeric forms. The term "stereochemically isomeric forms" as used herein defines all the possible compounds made up of the same atoms bonded by the same sequence of bonds but having different three-dimensional structures which are not interchangeable, which the compound (C) of Formulae (I) as specified herein, or a compound of any of subgroups of compounds of Formula (II), (lla)-(llc), (III), (llla)-(lllc), (IV), (IVa)-(IVc), (V), (Va)-(Vc) as specified herein, may possess.

[0248] Unless otherwise mentioned or indicated, the chemical designation of a compound (C) of Formulae (I) as specified herein, or a compound of any of subgroups of compounds of Formula (II), (lla)-(llc), (III), (llla)-(lllc), (IV), (IVa)-(IVc), (V), (Va)-(Vc) as specified herein, encompasses the mixture of all possible stereochemically isomeric forms, which said compound may possess. Said mixture may contain all enantiomers of the basic molecular structure of said compound. All stereochemically isomeric forms of the compounds of the present invention both in pure form or mixed with each other are intended to be embraced within the scope of the present invention.

[0249] Pure stereoisomeric forms of compound (C) of Formulae (I) as specified herein, or a compound of any of subgroups of compounds of Formula (II), (lla)-(llc), (III), (llla)-(lllc), (IV), (IVa)-(IVc), (V), (Va)-(Vc) as specified herein, and intermediates as mentioned herein are defined as isomers substantially free of other enantiomeric of the same basic molecular structure of said compounds or intermediates. In particular, the term “stereoisomerically pure” concerns compounds or intermediates having a stereoisomeric excess of at least 80% (i.e. minimum 90% of one isomer and maximum 10% of the other possible isomers) up to a stereoisomeric excess of 100% (i.e. 100% of one isomer and none of the other), more in particular, compounds or intermediates having a stereoisomeric excess of 90% up to 100%, even more in particular having a stereoisomeric excess of 94% up to 100% and most in particular having a stereoisomeric excess of 97% up to 100%. The terms “enantiomerically pure” and should be understoodin a similar way, but then having regard to the enantiomeric excess of the mixture in question.

[0250] Pure stereoisomeric forms of the compounds and intermediates of this invention may be obtained by the application procedures known in the art.

[0251] A person skilled in the art is able to determine the absolute configuration of such compounds using art-known methods such as, for example, X-ray diffraction.

[0252] The present invention is also intended to include all isotopes of atoms occurring on the present to a compound (C) of compound (C) of Formulae (I) as specified herein, or a compound of any of subgroups of compounds of Formula (II), (lla)-(llc), (III), (llla)-(lllc), (IV), (IVa)-(IVc), (V), (Va)-(Vc), as specified herein. Isotopes include those atoms having the same atomic number but different mass numbers. By way of general example and without limitation, isotopes of hydrogen include tritium and deuterium. Isotopes of carbon include C-13 and C-14.

[0253] The present invention also contemplates compositions comprising any one of the compounds described herein.

[0254] In some embodiments, the composition of the present invention comprises compound (C) according to Formula (He), or stereoisomers thereof, as the only active component for managing weight, particularly via a non-therapeutic use of a composition according to the invention. It has been surprisingly found by the inventors that the compound according to Formula (He), or stereoisomers thereof, is particularly effective on its own as the active component in managing / controlling weight, for controlling / maintaining normal weight, for controlling / preventing overweightness, for supporting weight loss, for supporting weight maintenance, for controlling / suppressing food intake, for controlling / reducing appetite, for reducing / controlling / preventing weight gain, for reducing fat mass, maintaining lean mass, reducing subcutaneous adipose tissue, increasing energy expenditure, and / or increasing brown adipose tissue.

[0255] In some embodiments, the composition of the present invention comprises compound (C) according to Formula (He), or stereoisomers thereof, as the only active component for managing weight, particularly via a non-therapeutic use of a composition according to the invention. It has been surprisingly found by the inventors that the compound according to Formula (He), or stereoisomers thereof,is particularly effective on its own as the active component in managing / controlling weight, for controlling / maintaining normal weight, for controlling / preventing overweightness, for supporting weight loss, for supporting weight maintenance, for controlling / suppressing food intake, for controlling / reducing appetite, for reducing / controlling / preventing weight gain, for reducing fat mass, maintaining lean mass, reducing subcutaneous adipose tissue, enhancing thermogenic capacity for increasing energy expenditure, and / or increasing brown adipose tissue.

[0256] In some embodiments, the composition of the present invention comprises compound (C) according to Formula (He) , or stereoisomers thereof, as the only active component for treatment or prevention of obesity, obesity associated metabolic disfunctions or disorders, and obesity associated noncommunicable diseases (NCDs), particularly via a therapeutic use of a composition according to the invention. In some embodiments, the composition of the present invention comprises compound (C) according to Formula (He) , or stereoisomers thereof, as the only active component for increasing lipolysis. It has been surprisingly found by the inventors that the compound according to Formula (He), or stereoisomers thereof, is particularly effective on its own as the active component in treating or preventing obesity, obesity associated metabolic disfunctions or disorders, and obesity associated noncommunicable diseases (NCDs), and for increasing lipolysis.

[0257] Formulations and administration

[0258] To prepare the compositions of the present invention, an effective amount of the particular compound (C) as the active ingredient is combined in intimate admixture with a carrier, in particular with a pharmaceutically acceptable carrier or nutraceutically acceptable carrier, which carrier may take a wide variety of forms depending on the form of preparation desired for administration. These compositions are desirable in unitary dosage form suitable, particularly, for administration orally, for enteral administration or for parenteral injection. For example, in preparing the compositions in oral dosage form, any of the usual media may be employed such as, for example, water, glycols, oils, alcohols and the like in the case of oral liquid preparations such as suspensions, syrups, elixirs,emulsions and solutions; or solid carriers such as starches, sugars, kaolin, lubricants, binders, disintegrating agents and the like in the case of powders, pills, capsules, and tablets. In the case of capsules, a compound (C) of formula (I), or the particular compound of any of the subgroups of compounds of formula (II), (lla)-(llc), (III), (llla)-(lllc), (IV), (IVa)-(IVc), (V), (Va)-(Vc), may be present alone.

[0259] Because of their ease in administration, tablets and capsules represent the most advantageous oral dosage unit forms, in which case solid carriers may be employed. For enteral compositions, the carrier will usually comprise sterile water, at least in large part, though other ingredients, for example, to aid solubility, may be included. Injectable solutions, for example, may be prepared in which the carrier comprises saline solution, glucose solution or a mixture of saline and glucose solution. For example, saline solution may be phosphate-buffered saline (PBS). Injectable suspensions may also be prepared in which case appropriate liquid carriers, suspending agents and the like may be employed. All these forms of administration may also comprise bioavailability enhancers such as cyclodextrins, PEG, emulsions, micronized powder, liposomes, niosomes, phytosomes, exosomes, and combinations thereof.

[0260] It is especially advantageous to formulate the compositions according to the present invention in unit dosage form for ease of administration and uniformity of dosage. Unit dosage form as used herein refers to physically discrete units suitable as unitary dosages, each unit containing a predetermined quantity of active ingredient calculated to produce the desired effect in association with the required pharmaceutical carrier. Examples of such unit dosage forms are tablets (including scored or coated tablets), capsules, pills, powder packets, wafers, injectable solutions or suspensions and the like, and segregated multiples thereof.

[0261] In some embodiments, the compound or the composition comprising the same according to the present invention is intended for infants, children, and / or adults.

[0262] For example, the compound or the composition comprising the same according to the present invention is in an orally administrable form or in a enteral administrable form or in a parenteral administrable form, in particular in the form of a tablet, a pill, a capsule, a soluble powder, an oily solution, an effervescenttablet, a soft capsule, a solution including a beverage, a shot, or a in a medical food format.

[0263] Preferably, the composition according to the present invention may comprise protective hydrocolloids, excipients, diluents binders, film forming agents, flavouring agents, preservatives, stabilizers, buffers, lubricants, colorants, wetting agents, fillers, encapsulating agents, coatings, emulsifiers, surface active agents, solubilizing agents, adsorbents, carriers, dispersing agents, taste masking agents, gel forming agents, antioxidants and / or antimicrobials, and combinations thereof.

[0264] Advantageously, the composition according to the present invention may also comprise bioavailability enhancers, for example cyclodextrins, PEG, emulsions, micronized powder, liposomes, niosomes, phytosomes, exosomes, and combinations thereof.

[0265] Advantageously, the composition according to the present invention may also comprise minerals and micronutrients, for example calcium, magnesium, phosphorus, iron, zinc, copper, iodine, selenium, beta carotene, vitamin C, vitamin B1 , vitamin B6, vitamin B2, niacin, vitamin B12, folic acid, biotin, 1 to 5 pg vitamin D and / or vitamin E, docosahexaenoic acid, eicosapentaenoic acid, and combinations thereof.

[0266] Advantageously, the composition according to the present invention may also comprise other natural ingredients for weight management support such as for example green tea extract, caffeine, glucomannan, chromium picolinate, chitosan, berberine, conjugated linoleic acid, prebiotic fibers (GOS, XOS, FOS, inulin, XOS), green kiwi fruit extract, yellow kiwi fruit extract, pineapple guava extract, cinnamon extract, and combinations thereof. Preferably, the composition according to the present invention does not comprise glutamine.

[0267] Advantageously, the compound or the composition comprising the same according to the present invention is a medicament, a food or a beverage product, a pet food product, a food additive or a nutraceutical or a dietary supplement. Preferably, according to the method following the present invention, the administration consists in the administration of a medicament, a food or beverage product, a pet food product, a food additive or a nutraceutical or a dietary supplement.Preferably, according to the method following the present invention, the administration is intended for infants, children, and / or adults.

[0268] Advantageously, according to the method following the present invention, the administration is performed through an orally or a enteral administrable form or a parenteral administrable form, for example via a tablet, a pill, a capsule, a soluble powder, an oily solution, an effervescent tablet or a soft capsule, a solution including a beverage, a shot, or a medical food format.

[0269] Treatment and prevention of disorders

[0270] In the context of the present invention, it has been determined that a compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same has positive effects when used in the treatment or in the prevention of overweightness, of obesity and / or of the overweightness and the obesity associated metabolic disfunctions or disorders and / or of the overweightness and the obesity associated noncommunicable diseases (NCDs).

[0271] In some embodiments, the compound (C) according to general Formula (I) is a compound according to Formula (He), or stereoisomer thereof, or a composition comprising the same, and has positive effects when used in the treatment or in the prevention of overweightness, of obesity and / or of the overweightness and the obesity associated metabolic disfunctions or disorders and / or of the overweightness and the obesity associated noncommunicable diseases (NCDs).

[0272] Preferably, according to the present invention, the associated metabolic disfunctions or disorders and / or associated noncommunicable diseases (NCDs) are selected from the group consisting of diabetes, hypertension, liver cirrhosis, metabolic syndrome, cardiovascular diseases, cancers, neurological disorders, chronic respiratory diseases, digestives disorders, and combinations thereof.

[0273] Another object of the present invention is a method for (therapeutically) treating or preventing overweightness, obesity and / or the overweightness and the obesity associated metabolic disfunctions or disorders and / or the overweightness and the obesity associated noncommunicable diseases (NCDs) or for (non-therapeutically) managing / controlling weight, controlling obesity, controlling / maintaining normal weight, controlling overweightness, supporting weight loss, supporting weight maintenance, suppressing food intake, reducing appetite, increasing lipolysis, for reducing fat mass, for maintaining lean mass, for reducing subcutaneous adipose tissue, for increasing brown adipose tissue, for increasing energy expenditure, and / or reducing I controlling weight gain, comprising the step of administering an effective amount of a compound according to the general Formula (I), or stereoisomer thereof, or a compound of any of the subgroups of compounds of Formula (II), (lla)-(llc), (III), (llla)-(lllc), (IV), (IVa)-(IVc), (V), (Va)-(Vc), as specified herein, and according to any one of the embodiments presented hereinto, to an individual. In a preferred embodiment, the compound (C) is according to formula (He). In a further preferred embodiment, the compound (C) according to formula (He) is the only active component in the composition.

[0274] In some embodiments, the present invention is a method for (therapeutically) treating or preventing overweightness, obesity and / or the overweightness and the obesity associated metabolic disfunctions or disorders and / or the overweightness and the obesity associated noncommunicable diseases (NCDs) or for (non-therapeutically) managing I controlling weight, controlling obesity, controlling I maintaining normal weight, controlling overweightness, supporting weight loss, supporting weight maintenance, suppressing food intake, reducing appetite, increasing lipolysis, for reducing fat mass, for maintaining lean mass, for reducing subcutaneous adipose tissue, for increasing brown adipose tissue, enhancing thermogenic capacity for increasing energy expenditure, and / or reducing I controlling weight gain, comprising the step of administering an effective amount of a compound according to the general Formula (I), or stereoisomer thereof, or a compound of any of the subgroups of compounds of Formula (II), (lla)-(llc), (HI), (llla)-(lllc), (IV), (IVa)-(IVc), (V), (Va)-(Vc), as specified herein, and according to any one of the embodiments presented hereinto, to an individual. In a preferred embodiment, the compound (C) is according to formula (He). In a further preferred embodiment, the compound (C) according to formula (He) is the only active component in the composition.

[0275] Advantageously, according to the method following the present invention, the associated metabolic disfunctions or disorders and / or associated noncommunicable diseases (NCDs) are selected from the group consisting ofdiabetes, hypertension, liver cirrhosis, metabolic syndrome, cardiovascular diseases, cancers, neurological disorders, chronic respiratory diseases, digestives disorders, and combinations thereof.

[0276] As will be understood from the disclosures herein, the present invention also provides the use of a compound (C) of formula (I), or the particular compound of any of the subgroups of compounds of formula (II), (lla)-(l Ic), (III), (llla)-(l I Ic), (IV), (IVa)-(IVc), (V), (Va)-(Vc), as specified herein, or compositions of the invention for the manufacture of a medicament, in particular a medicament for the treatment of overweightness, of obesity and / or of the overweightness and the obesity associated metabolic disfunctions or disorders and / or of the overweightness and the obesity associated noncommunicable diseases (NCDs).

[0277] The compound, the compositions and the combinations of the present invention may be used as medicaments. Said use as a medicine or method of treatment comprises the systemic administration to subjects to be treated of an amount effective to combat the conditions. Consequently, the compound, the compositions and the combinations of the present invention can be used in the manufacture of a medicament useful for treating or preventing overweightness, obesity and / or the overweightness and the obesity associated metabolic disfunctions or disorders and / or the overweightness and the obesity associated noncommunicable diseases (NCDs) consisting notably of diabetes, hypertension, liver cirrhosis, metabolic syndrome, cardiovascular diseases, cancers, neurological disorders, chronic respiratory diseases, digestives disorders, and combinations thereof.

[0278] The compound, the compositions and the combinations of the present invention may be used as non-medicaments, for example as a food or a beverage product, a pet food product, a food additive or a nutraceutical or a dietary supplement.

[0279] The exact dosage and frequency of administration depends on the particular compound (C) of formula (I), or the particular compound of any of the subgroups of compounds of formula (II), (lla)-(llc), (III), (llla)-(lllc), (IV), (IVa)-(IVc), (V), (Va)-(Vc), as specified herein, used, the particular condition being treated, the severity of the condition being treated, the age, weight, sex, extent of disorder and general physical condition of the particular patient as well as othermedication the individual may be taking, as is well known to those skilled in the art. Furthermore, it is evident that said effective daily amount may be lowered or increased depending on the response of the treated subject and / or depending on the evaluation of the physician prescribing the compounds of the instant invention.

[0280] In some embodiments, the present invention provides a compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same, for use in the treatment or prevention of obesity, obesity associated metabolic disfunctions or disorders, and obesity associated noncommunicable diseases (NCDs). In some embodiments, the present invention provides a compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same, for use in increasing lipolysis. In a preferred embodiment, the compound (C) is according to formula (He). In a further preferred embodiment, the compound (C) according to formula (He) is the only active component in the composition.

[0281] In some embodiments, the present invention provides a compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same, for use as a medicament in the treatment or prevention of obesity, obesity associated metabolic disfunctions or disorders, and obesity associated noncommunicable diseases (NCDs). In some embodiments, the present invention provides a compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same, for use as a medicament in increasing lipolysis. In a preferred embodiment, the compound (C) is according to formula (He). In a further preferred embodiment, the compound (C) according to formula (He) is the only active component in the composition.

[0282] In some embodiments, the present invention provides a compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same, for use in the manufacture of a medicament for treatment or prevention of obesity, obesity associated metabolic disfunctions or disorders, and obesity associated noncommunicable diseases (NCDs). In some embodiments, the present invention provides a compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising thesame, for use in the manufacture of a medicament for increasing lipolysis. In a preferred embodiment, the compound (C) is according to formula (He). In a further preferred embodiment, the compound (C) according to formula (He) is the only active component in the composition.

[0283] In some embodiments, the present invention provides a pharmaceutical composition comprising compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same, for use in the treatment or prevention of obesity, obesity associated metabolic disfunctions or disorders, and obesity associated noncommunicable diseases (NCDs). In some embodiments, the present invention provides a pharmaceutical composition comprising compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same, for use in increasing lipolysis. In a preferred embodiment, the compound (C) is according to formula (He). In a further preferred embodiment, the compound (C) according to formula (He) is the only active component in the composition.

[0284] In some embodiments, the present invention provides use of a compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same, for treatment or prevention of obesity, obesity associated metabolic disfunctions or disorders, and obesity associated noncommunicable diseases (NCDs). In a preferred embodiment, the compound (C) is according to formula (He). In a further preferred embodiment, the compound (C) according to formula (He) is the only active component in the composition.

[0285] In some embodiments, the present invention provides use of a compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same, in the preparation of a medicament for treatment or prevention of obesity, obesity associated metabolic disfunctions or disorders, and obesity associated noncommunicable diseases (NCDs). In some embodiments, the present invention provides use of a compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same, in the preparation of a medicament for increasing lipolysis. In a preferred embodiment, the compound (C) is according to formula (He). In a further preferred embodiment, the compound (C) according to formula (He) is the only active component in the composition.In some embodiments, the present invention provides a method of treating or preventing obesity, obesity associated metabolic disfunctions or disorders, and obesity associated noncommunicable diseases (NCDs), comprising administering a compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same, to a subject in need thereof. In some embodiments, the present invention provides a method of increasing lipolysis, comprising administering a compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same, to a subject in need thereof. In a preferred embodiment, the compound (C) is according to formula (He). In a further preferred embodiment, the compound (C) according to formula (He) is the only active component in the composition.

[0286] In some embodiments, the present invention provides a method of treating or preventing obesity, obesity associated metabolic disfunctions or disorders, and obesity associated noncommunicable diseases (NCDs) in a patient, comprising administering a compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same. In some embodiments, the present invention provides a method of increasing lipolysis in a patient, comprising administering a compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same. In a preferred embodiment, the compound (C) is according to formula (He). In a further preferred embodiment, the compound (C) according to formula (He) is the only active component in the composition.

[0287] The inventors have surprisingly found that said compound (C) demonstrates strong and consistent positive effects in addressing low HDL cholesterol. These findings are even more surprising as they are contrary to what is expected from other similar compounds.

[0288] In some embodiments, the present invention provides compound (C), or a composition comprising the same, as described in any of the embodiments herein, for use in increasing HDL cholesterol. In some embodiments, the present invention provides compound (C), or a composition comprising the same, as described in any of the embodiments herein, for use in treatment of low HDL cholesterol. In some embodiments, the present invention provides compound (C), or a composition comprising the same, as described in any of the embodimentsherein, for use in the manufacture of a medicament for treatment of low HDL cholesterol. In some embodiments, the present invention provides compound (C), or a composition comprising the same, as described in any of the embodiments herein, for use as a medicament in treatment of low HDL cholesterol. In some embodiments, the present invention provides the use of compound (C), or a composition comprising the same, as described in any of the embodiments herein, for treatment of low HDL cholesterol. In some embodiments, the present invention provides the use of compound (C), or a composition comprising the same, as described in any of the embodiments herein, in the preparation of a medicament for treatment of low HDL cholesterol. In some embodiments, the present invention provides a method of treating or preventing low HDL, comprising administering a compound (C), or a composition comprising the same, as described in any of the embodiments herein, to a subject in need thereof. In a preferred embodiment, the compound (C), or a composition comprising the same, as described hereinabove is according to formula (He). In a further preferred embodiment, the compound (C) according to formula (He) is the only active component in the composition.

[0289] The inventors have surprisingly found that said compound (C) demonstrates strong and consistent positive effects in addressing high triglycerides and / or free fatty acids. These findings are even more surprising as they are contrary to what is expected from other similar compounds.

[0290] Therefore, in some embodiments, the present invention provides compound (C), or a composition comprising the same, as described in any of the embodiments herein, for use in reducing triglycerides and / or free fatty acids. In some embodiments, the present invention provides compound (C), or a composition comprising the same, as described in any of the embodiments herein, for use in treatment of high triglycerides and / or free fatty acids. In some embodiments, the present invention provides compound (C), or a composition comprising the same, as described in any of the embodiments herein, for use in the manufacture of a medicament for treatment of high triglycerides and / or free fatty acids. In some embodiments, the present invention provides compound (C), or a composition comprising the same, as described in any of the embodiments herein, for use as a medicament in treatment of high triglycerides and / or free fattyacids. In some embodiments, the present invention provides the use of compound (C), or a composition comprising the same, as described in any of the embodiments herein, for treatment of high triglycerides and / or free fatty acids. In some embodiments, the present invention provides the use of compound (C), or a composition comprising the same, as described in any of the embodiments herein, in the preparation of a medicament for treatment of high triglycerides and / or free fatty acids. In some embodiments, the present invention provides a method of treating or preventing high triglycerides and / or free fatty acids, comprising administering a compound (C), or a composition comprising the same, as described in any of the embodiments herein, to a subject in need thereof. In a preferred embodiment, the compound (C), or a composition comprising the same, as described hereinabove is according to formula (He). In a further preferred embodiment, the compound (C) according to formula (He) is the only active component in the composition.

[0291] In some embodiments, the present invention provides methods as described herein, comprising administering the compound (C) in an amount ranging from 50 mg per day (in one or more doses) to 4000 mg per day. In some preferred embodiments, the compound (C) is administered in an amount of 100, 200, 300, 400, 500, 600, 700, 800, 900, 1000, 1100, 1200, 1300, 1400, 1600, 1700, 1800, 1900, 2000, 2100, 2200, 2300, 2400, 2500, 2600, 2700, 2800, 2900, 3000, 3100, 3200, 3300, 3400, 3500, 3600, 3700, 3800, 3900, or 4000 mg per day (in one or more doses). Preferably, the compound (C) is administered in an amount ranging from 500 to 2000 mg per day. More preferably, the compound (C) is administered in an amount ranging from 600 to 1800 mg per day. Most preferably, the compound (C) is administered in an amount ranging from 700 to 1400 mg per day. It is to be understood that compound (C) is according to any of the formulas as described herein. In a particular embodiment, compound (C) is according to Formula (I). In yet another particular embodiment, compound (C) is according to formula (He).

[0292] Non-therapeutic use

[0293] Another object of the present invention is a use, in particular a non-therapeutic use, of a compound (C) according to general Formula (I), or ofstereoisomer thereof, or of a compound of any of the subgroups of compounds of Formula (II), (lla)-(llc), (III), (llla)-(lllc), (IV), (IVa)-(IVc), (V), (Va)-(Vc), as specified herein, and according to any one of the embodiments presented hereinto, or of a composition comprising the same, for controlling obesity, for controlling / maintaining normal weight, for controlling overweightness, for supporting weight loss, for supporting weight maintenance, for suppressing food intake, for reducing appetite, for increasing lipolysis, for reducing fat mass, maintaining lean mass, reducing subcutaneous adipose tissue, increasing brown adipose tissue, for increasing energy expenditure, and / or for reducing I controlling weight gain.

[0294] In some embodiments, the present invention is a use, in particular a non-therapeutic use, of a compound (C) according to general Formula (I), or of stereoisomer thereof, or of a compound of any of the subgroups of compounds of Formula (II), (lla)-(llc), (III), (llla)-(lllc), (IV), (IVa)-(IVc), (V), (Va)-(Vc), as specified herein, and according to any one of the embodiments presented hereinto, or of a composition comprising the same, for controlling obesity, for controlling / maintaining normal weight, for controlling overweightness, for supporting weight loss, for supporting weight maintenance, for suppressing food intake, for reducing appetite, for increasing lipolysis, for reducing fat mass, maintaining lean mass, reducing subcutaneous adipose tissue, increasing brown adipose tissue, for enhancing thermogenic capacity for increasing energy expenditure, and / or for reducing I controlling weight gain.

[0295] In particular, the composition according to the present invention may be used to reduce weight gain or as a suppressor of food intake. More particularly, the composition according to the present invention may be used to treat or prevent overweightness and / or obesity resulting from a high-fat-diet. Even more particularly, the composition according to the present invention may be used to treat or prevent overweightness resulting from a high-fat-diet.

[0296] Use, in particular non-therapeutic use, according to the invention, may consist in a dietary supplementation to support / to maintain a normal healthy weight and metabolism. Preferably, the use is a non-therapeutic use. In the context of the present invention, it has been determined that a compound (C) according to general Formula (I), or stereoisomer thereof, or a compositioncomprising the same has positive effects when used, in particular when non-therapeutically used, for controlling obesity, for controlling I maintaining normal weight, for controlling overweightness, for supporting weight loss, for supporting weight maintenance, for suppressing food intake, for reducing appetite, for increasing lipolysis, for reducing fat mass, maintaining lean mass, reducing subcutaneous adipose tissue, increasing brown adipose tissue, for increasing energy expenditure, and / or for reducing I controlling weight gain.

[0297] In the context of the present invention, it has also been determined that a compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same has positive effects when used, in particular when non-therapeutically used, for controlling obesity, for controlling I maintaining normal weight, for controlling overweightness, for supporting weight loss, for supporting weight loss, for supporting weight maintenance, for suppressing food intake, for reducing appetite, for increasing lipolysis, for reducing fat mass, maintaining lean mass, reducing subcutaneous adipose tissue, increasing brown adipose tissue, for enhancing thermogenic capacity for increasing energy expenditure, and / or for reducing I controlling weight gain.

[0298] In the context of the present invention, it has been determined that a compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same has positive effects when used non-therapeutically for controlling I maintaining normal weight, for controlling overweightness, for supporting weight loss, for supporting weight maintenance, for suppressing food intake, for reducing appetite, and / or for reducing I controlling weight gain.

[0299] In a preferred embodiment, the present invention provides non-therapeutic use of compound (C) according to formula (He) or stereoisomer thereof, or a composition comprising the same, for controlling I maintaining normal weight, for controlling overweightness, for supporting weight loss, for supporting weight maintenance, for suppressing food intake, for reducing appetite, and / or for reducing / controlling weight gain. In some embodiments, the present invention also provides for non-therapeutic use of a composition comprising compound (C) according to formula (He) or stereoisomer thereof, for controlling I maintaining normal weight, for controlling overweightness, for supporting weight loss, forsupporting weight maintenance, for suppressing food intake, for reducing appetite, and / or for reducing / controlling weight gain, wherein compound (C) according to formula (He) or stereoisomer thereof is the only active component in the composition.

[0300] It has surprisingly been found that said compound (C) has a strong and consistent positive effect on controlling weight gain and reducing food intake, without affecting water intake. These findings are even more surprising as they are contrary to what is expected from other similar compounds.

[0301] In a preferred embodiment, the present invention provides non-therapeutic use of compound (C) according to formula (He) or stereoisomer thereof, or a composition comprising the same, for reducing fat mass, maintaining lean mass, reducing subcutaneous adipose tissue, increasing energy expenditure, and / or increasing brown adipose tissue. In some embodiments, the present invention also provides for non-therapeutic use of a composition comprising compound (C) according to formula (He) or stereoisomer thereof, for reducing fat mass, maintaining lean mass, reducing subcutaneous adipose tissue, increasing energy expenditure, and / or increasing brown adipose tissue, wherein compound (C) according to formula (He) or stereoisomer thereof is the only active component in the composition.

[0302] In a preferred embodiment, the present invention provides non-therapeutic use of compound (C) according to formula (He) or stereoisomer thereof, or a composition comprising the same, for reducing fat mass, maintaining lean mass, reducing subcutaneous adipose tissue, enhancing thermogenic capacity for increasing energy expenditure, and / or increasing brown adipose tissue. In some embodiments, the present invention also provides for non-therapeutic use of a composition comprising compound (C) according to formula (He) or stereoisomer thereof, for reducing fat mass, maintaining lean mass, reducing subcutaneous adipose tissue, enhancing thermogenic for increasing energy expenditure, and / or increasing brown adipose tissue, wherein compound (C) according to formula (He) or stereoisomer thereof is the only active component in the composition.

[0303] It was surprisingly observed that the present invention showed these specific positive effects, whilst not affecting other adipose tissues in a nonspecific manner, such as visceral and / or epididymal adipose tissue. The non-therapeutic use according to the present invention also did not have an impact on the free body fluid, further supporting its specific positive effect. These findings are even more surprising as they are contrary to what is expected from other similar compounds.

[0304] In some embodiments, the present invention provides uses as described herein, comprising administering the compound (C) in an amount ranging from 50 mg per day (in one or more doses) to 4000 mg per day. In some preferred embodiments, the compound (C) is administered in an amount of 100, 200, 300, 400, 500, 600, 700, 800, 900, 1000, 1100, 1200, 1300, 1400, 1600, 1700, 1800, 1900, 2000, 2100, 2200, 2300, 2400, 2500, 2600, 2700, 2800, 2900, 3000, 3100, 3200, 3300, 3400, 3500, 3600, 3700, 3800, 3900, or 4000 mg per day (in one or more doses). Preferably, the compound (C) is administered in an amount ranging from 500 to 2000 mg per day. More preferably, the compound (C) is administered in an amount ranging from 600 to 1800 mg per day. Most preferably, the compound (C) is administered in an amount ranging from 700 to 1400 mg per day. It is to be understood that compound (C) is according to any of the formulas as described herein. In a particular embodiment, compound (C) is according to Formula (I). In yet another particular embodiment, compound (C) is according to formula (He).

[0305] Mechanism of action

[0306] Although it is not necessary to understand the mechanism of action of the invention, an explanation is provided to supplement understanding of the invention for a skilled person. The inventors have surprisingly found that compound (C) according to the present invention, in particular according to Formula (He), acts on metabolic syndrome via both central and peripheral pathways. The present invention acts on various metabolic syndrome parameters, including reducing body weight gain and fat mass, improving plasma lipid parameters, and selectively increasing brown adipose tissue (BAT) mass, while preserving lean mass.

[0307] For example, on one hand, the present invention exerts central regulation of energy balance and feeding behavior, as supported by experimental data showing an effect on satiety (e.g. Example 6, Fig. 3).On the other hand, the present invention induces peripheral metabolic improvements, notably through modulation of brown adipose tissue (BAT) function and lipid metabolism, whilst preventing loss of lean body mass. It is understood that the mechanism of peripheral metabolic improvement is mediated through changes in BAT-relevant genes supporting BAT identity, mitochondrial function, lipid handling, and inflammatory modulation, such as Prdm16 (master regulator of BAT / beige adipocyte identity), Zic1 (BAT-specific identity marker), Tbx1 (beige / brown adipocyte program marker), Cox7a1 (mitochondrial electron transport chain subunit enriched in BAT), Cox8b (BAT-enriched mitochondrial ETC subunit), Tfam (mitochondrial DNA replication and maintenance), Nrf1 (transcriptional regulator of mitochondrial biogenesis), Esrra / ERRa (regulator of oxidative metabolism and thermogenic programming), Pnpla2 / ATGL (key regulator of lipolysis), Lipe / HSL (complementary lipolytic enzyme), Slc27a1 / FATP1 (fatty-acid uptake in brown adipocytes), Cd36 (fatty-acid transporter involved in BAT lipid utilization), Ppara (driver of fatty-acid oxidation programs in brown adipocytes), Tnf (inflammatory cytokine linked to metabolic stress), 116 (cytokine associated with local metabolic inflammation), Arg1 (marker of M2, pro-thermogenic macrophages), Mrc1 / CD206 (alternative macrophage activation marker), PGC-1a (master transcriptional co-activator of BAT thermogenesis), UCP1 (obligate effector of non-shivering thermogenesis), DIO2 (amplifier of thyroid hormone signalling by converting T4 to T3), Cidea (BAT / beige marker involved in lipid droplet dynamics), TNF-alpha (inflammation marker), and Elovl3 (BAT-enriched, thermogenesis-dependent).

[0308] The inventors have surprisingly observed that the present invention results in a selective induction of Ppargcla (PGC-1a) in BAT (Fig 14). PGC-1a is the master transcriptional co-activator of BsAT thermogenesis, integrating mitochondrial biogenesis, oxidative metabolism, and adaptive heat production through coordinated regulation of large thermogenic gene networks. Activation of this node reflects a commitment to functional BAT engagement rather than isolated marker expression in mice treated with the present invention.

[0309] Consistent with this framework, the inventors also surprisingly observed that the administration of a compound according to the present invention was also associated with coordinated upward trends in Ucp1, Dio2, Cidea, and Elovl3a gene ensemble that defines thermogenically competent BAT. UCP1 is the obligate effector of non-shivering thermogenesis, while DIO2 locally amplifies thyroid hormone signalling by converting T4 to T3, a prerequisite for full adrenergic responsiveness and L / CPZ-driven heat production. This intracellular thyroid hormone amplification explains how BAT can markedly increase energy expenditure without changes in circulating thyroid hormones and represents a defining feature of active BAT. In parallel, increased Elovl3 expression is consistent with BAT-specific lipid remodelling required to support efficient mitochondrial oxidation and controlled lipid droplet dynamics during thermogenesis.

[0310] Importantly, it is understood that lean mass preservation and the selective induction of BAT-exclusive markers indicate a different mechanism than generalized muscle catabolism or fasting-like metabolic stress, as often seen in GLP-1 treatment . The expression of PGC-1a in skeletal muscle, its activation in BAT drives energy dissipation rather than enhanced oxidative capacity alone, which points to tissue-specific metabolic engagement. It is further understood that the present invention exerts superior metabolic efficacy by activating a PGC-1a-centered thermogenic network, encompassing mitochondrial biogenesis, thyroid hormone amplification, and UCP1 -mediated energy dissipation. Therefore, the present invention surprisingly acts, at least in part, by increasing energy expenditure, for example, through enhanced thermogenic capacity.

[0311] It is further believed that the effects of the present invention are not driven by local changes in taurine / N-acetyltaurine enzymatic regulation, but rather by downstream metabolic or systemic signals converging on mitochondrial and thermogenic pathways.

[0312] Additionally, the inventors have also surprisingly noted that the present invention modulates low-grade chronic inflammation, as seen through a tendency towards a decrease in TNF-alpha. Inflammation is implicated in metabolic syndrome.

[0313] The present invention is further surprising since other similar compounds are not known to provide similar effects. For example, other similar compounds do not engage this network and therefore lack the capacity to induce functionalBAT thermogenesis under high-fat diet conditions. This strongly demonstrates a link of the present invention with a new clinical situation not known so far.

[0314] The present invention has been described in terms of specific embodiments, which are illustrative of the invention and not to be construed as limiting. More generally, it will be appreciated by persons skilled in the art that the present invention is not limited by what has been particularly shown and / or described hereinabove. It is to be understood that any of the embodiments described herein can be combined in any manner to achieve the aims of the present invention.

[0315] Use of the verbs "to comprise", "to include", "to be composed of", or any other variant, as well as their respective conjugations, does not exclude the presence of elements other than those stated.

[0316] Use of the article "a", "an" or "the" preceding an element does not exclude the presence of a plurality of such elements.

[0317] Embodiments

[0318] In some embodiments, the present invention provides a compound (C) according to general Formula (I), or stereoisomer thereof, or a composition comprising the same, for use in the treatment or in the prevention of overweightness, of obesity and / or of the overweightness and the obesity associated metabolic disfunctions or disorders and / or of the overweightness and the obesity associated noncommunicable diseases (NCDs),

[0319]

[0320] Formula (I) wherein:

[0321] - each of Ri is a Ci-4 alkyl;

[0322] - each of R2 is selected from H or COOH;

[0323] - n is an integer equal to 0, 2 or 3;

[0324] - m is an integer equal to 1 or 2;- X is selected from H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

[0325] In some embodiments, the present invention provides a compound (C), or stereoisomer thereof, or the composition comprising the same, for use as described herein, wherein the associated metabolic disfunctions or disorders and / or associated noncommunicable diseases (NCDs) are selected from the group consisting of diabetes, hypertension, liver cirrhosis, metabolic syndrome, cardiovascular diseases, cancers, neurological disorders, chronic respiratory diseases, digestives disorders, and combinations thereof.

[0326] In some embodiments, the present invention provides a compound (C), or stereoisomer thereof, or the composition comprising the same, for use as described herein, wherein the compound (C) is selected from those of Formula (Ila), (Illa), (IVa) or (Va) hereinbelow:

[0327]

[0328] wherein:

[0329] - each of R11 is a Ci -4 alkyl;

[0330] - ml is an integer equal to 1 or 2;- Xi is an inorganic cation selected from the group consisting of an alkali metal cation and an alkaline earth metal cation;

[0331] - each of R12 is a C1-4 alkyl;

[0332] - m2 is an integer equal to 1 or 2;

[0333] - X2 is an inorganic cation selected from the group consisting of an alkali metal cation and an alkaline earth metal cation;

[0334] - each of R13 is a C1-4 alkyl;

[0335] - m3 is an integer equal to 1 or 2;

[0336] - X3 is an inorganic cation selected from the group consisting of an alkali metal cation and an alkaline earth metal cation;

[0337] - each of R14 is a C1-4 alkyl;

[0338] - m4 is an integer equal to 1 or 2;

[0339] - X4 is an inorganic cation selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

[0340] In some embodiments, the present invention provides a compound (C), or stereoisomer thereof, or the composition comprising the same, for use as described herein, wherein the compound (C) is selected from those of Formula (He), (I I Ic), (IVc) or (Vc) hereinbelow:

[0341]

[0342] )

[0343]

[0344] Formula (Vc) In some embodiments, the present invention provides a use, in particular non-therapeutic use, of a compound (C) according to general Formula (I), or of stereoisomer thereof, or of a composition comprising the same, for managing I controlling weight, for controlling obesity, for controlling I maintaining normal weight, for controlling overweightness, for supporting weight loss, for supporting weight maintenance, for suppressing food intake, for reducing appetite, for increasing lipolysis, for increasing energy expenditure, and / or for reducing I controlling weight gain,

[0345]

[0346] Formula (I) wherein:

[0347] - each of Ri is a C1-4 alkyl;

[0348] - each of R2 is selected from H or COOH;

[0349] - n is an integer equal to 0, 2 or 3;

[0350] - m is an integer equal to 1 or 2;

[0351] - X is selected from H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

[0352] In some embodiments, the present invention provides a use, in particular non-therapeutic use, of a compound (C) according to general Formula (I), or of stereoisomer thereof, or of a composition comprising the same, as described herein, wherein the compound (C) is selected from those of Formula (Ila), (Illa), (IVa) or (Va) hereinbelow:

[0353] >

[0354]

[0355] wherein:

[0356] - each of R11 is a Ci -4 alkyl;

[0357] - ml is an integer equal to 1 or 2;

[0358] - Xi is an inorganic cation selected from the group consisting of an alkali metal cation and an alkaline earth metal cation;

[0359] - each of R12 is a C1-4 alkyl;

[0360] - m2 is an integer equal to 1 or 2;

[0361] - X2 is an inorganic cation selected from the group consisting of an alkali metal cation and an alkaline earth metal cation;

[0362] - each of R13 is a C1-4 alkyl;

[0363] - m3 is an integer equal to 1 or 2;

[0364] - X3 is an inorganic cation selected from the group consisting of an alkali metal cation and an alkaline earth metal cation;

[0365] - each of R14 is a C1-4 alkyl;

[0366] - m4 is an integer equal to 1 or 2;- X4 is an inorganic cation selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

[0367] In some embodiments, the present invention provides a use, in particular non-therapeutic use, of a compound (C) according to general Formula (I), or of stereoisomer thereof, or of a composition comprising the same, as described herein, wherein the compound (C) is selected from those of Formula (He), (lllc), (IVc) or (Vc) hereinbelow:

[0368] >

[0369]

[0370] In some embodiments, the present invention provides a method for treating or preventing overweightness, obesity and / or the overweightness and the obesity associated metabolic disfunctions or disorders and / or the overweightness and the obesity associated noncommunicable diseases (NCDs) or for managing I controlling weight, for controlling obesity, for controlling I maintaining normal weight, for controlling overweightness, for supporting weight loss, for supporting weight maintenance, for suppressing food intake, for reducing appetite, for increasing lipolysis, for increasing energy expenditure, and / or for reducing I controlling weight gain, comprising the step of administering an effective amountof a compound (C) according to general Formula (I), or stereoisomer thereof, to an individual:

[0371] >

[0372]

[0373] Formula (I) wherein:

[0374] - each of Ri is a C1-4 alkyl;

[0375] - each of R2 is selected from H or COOH;

[0376] - n is an integer equal to 0, 2 or 3;

[0377] - m is an integer equal to 1 or 2;

[0378] - X is selected from H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

[0379] In some embodiments, the present invention provides a method as described herein, wherein the associated metabolic disfunctions or disorders and / or associated noncommunicable diseases (NCDs) are selected from the group consisting of diabetes, hypertension, liver cirrhosis, metabolic syndrome, cardiovascular diseases, cancers, neurological disorders, chronic respiratory diseases, digestives disorders, and combinations thereof.

[0380] In some embodiments, the present invention provides a method as described herein, wherein the compound (C) according to general Formula (I), or stereoisomer thereof is selected from those of Formula (Ila), (Illa), (IVa) or (Va) hereinbelow:

[0381]

[0382] )

[0383]

[0384] wherein:

[0385] - each of R11 is a Ci -4 alkyl;

[0386] - ml is an integer equal to 1 or 2;

[0387] - Xi is an inorganic cation selected from the group consisting of an alkali metal cation and an alkaline earth metal cation;

[0388] - each of R12 is a C1-4 alkyl;

[0389] - m2 is an integer equal to 1 or 2;

[0390] - X2 is an inorganic cation selected from the group consisting of an alkali metal cation and an alkaline earth metal cation;

[0391] - each of R13 is a C1-4 alkyl;

[0392] - m3 is an integer equal to 1 or 2;

[0393] - X3 is an inorganic cation selected from the group consisting of an alkali metal cation and an alkaline earth metal cation;

[0394] - each of R14 is a C1-4 alkyl;

[0395] - m4 is an integer equal to 1 or 2

[0396] - X4 is an inorganic cation selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

[0397] In some embodiments, the present invention provides a method as described herein, wherein the compound (C) according to general Formula (I), or stereoisomer thereof, is selected from those of Formula (He), (I I Ic), (IVc) or (Vc) hereinbelow:

[0398]

[0399] Examples

[0400] Example 1 : Preparation of formulations

[0401] A test compound according to the invention (Magnesium N-acetylaurinate, ATAMg hereinafter) was diluted in sterile PBS vehicle according to the required dose for the ATAMg test group. After homogenization, 180 pl of the solution was administered as described hereafter.

[0402] Two doses of ATAMg were evaluated: 59 mg / kg / day of treatment (ATAMg_L) and 176 mg / kg / day of treatment (ATAMgJH).

[0403] Sterile PBS alone was used as a control Vehicle.

[0404] Example 2: Animal models

[0405] C57BI6J DIO (diet induced obese) mice, aged 5 month old at arrival, were purchased from Charles River Laboratories, Saint Germain sur I’Arbresle, France.The animals were housed in ventilated and enriched cages (48 x 37.5 x 21 cm3). Animals’ cages litters were changed once weekly. Animals were housed in groups of 5 animals on a normal light cycle (lights off at 7 pm), 22 ± 2 °C and 50 ± 10% relative humidity. Housing parameters were recorded daily.

[0406] Animals were allowed to acclimatize to new facility and maintained on high-fat diet for 2 weeks. Body weight was taken daily to determine normalization of weight following transportation. During the acclimatation and experimental phase, high fat diet (HFD) (ResearchDiet # D12492i) and tap water were provided ad libitum.

[0407] After the 2-week acclimatation period, daily oral gavage of saline was performed for 5-days to account for stress-dependent food intake effects.

[0408] Example 3: in vivo protocol for treatment of animals

[0409] Mice were kept in a controlled environment with free access to food and water. For 6 weeks, mice were fed on a high-fat diet containing 20% protein, 35% carbohydrate, and 60% fat (Research diet, New Brunswick, NJ, USA).

[0410] Mice were treated daily with oral gavage of sterile PBS (control), ATAMg_L, or ATAMgJH, depending on the assessment, in a volume of 180pL. This was done for the 6 weeks of the HFD study. Each day, the experimental groups were force-fed in random order. The oral gavage was performed each day at the very end of the morning (between 11am and 12pm). The force-feeding dose was adjusted every week after the animals had been weighed, and the adjusted dose was used for 7 days.

[0411]

[0412] The data was expressed as the mean ± SEM. Differences between the experimental groups were assessed, where appropriate, using unpaired Student’s, one- or two-way ANOVA, followed by post-hoc test. Data was analysed using GraphPad Prism version 10 for Windows (GraphPad Software, San Diego, CA, USA). The results were considered statistically significant at p< 0.05.Example 5: Effect of ATAMq on body weight

[0413] Animals on HFD, being treated with ATAMg_L, ATAMg_H, and control, as described above, were used for body weight analysis. Body weight was recorded weekly.

[0414] Analysis of body weight gain (Fig 1) revealed that ATAMg_L (labelled HFD+ATAMg_L) and ATAMg_H (labelled HFD+ATAMg_H) treated group gained significantly less weight over time compared to the vehicle group (labelled HFD+Vehicle). Significant differences emerged from week 4 onward, notably ATAMg_H group differed significantly from control Vehicle at week 4, 5, and 6, and ATAMg_L group also differed significantly from control Vehicle at week 6.

[0415] At the end of the study (week 6), analysis of total body weight gain (Fig 2) revealed a reduction in both the ATAMg_L and ATAMg_H groups compared to the vehicle, with statistical significance as indicated by the superscripts on the bars.

[0416] Together, these data indicate that ATAMg supplementation limited body weight gain in mice fed with HFD.

[0417] Example 6: Effect of ATAMg on food and water intake

[0418] Animals on HFD, being treated with Vehicle, ATAMg_L, and ATAMg_H as described above, were used for assessing the effect of ATAMg on food and water intake. Food and water intake was recorded daily throughout the study.

[0419] Mean and cumulative intakes were analyzed at the end of the study. Mean food intake (Figure 3) was reduced in ATAMg treated groups compared with vehicle.

[0420] Alternatively, mean (Fig 4) and cumulative (Fig 5) water intake did not differ significantly among groups, confirming that the observed effects were specific to food consumption.

[0421] These findings reinforce that ATAMg treatment reduce energy intake under HFD conditions without altering hydration behavior.

[0422] Example 7: Effect of ATAMg on body composition

[0423] Animals on HFD, being treated with ATAMg_L, ATAMgJH, and vehicle as described above, were used for assessing effect of ATAMg on body composition. Fat mass, lean mass, and fluid content were measured by NMR at the end of thestudy. Briefly, awake animals were weighed and then placed in the Minispec chamber, according to the manufacturer instructions.

[0424] Analysis revealed that ATAMg treated groups significantly reduced fat mass compared with the vehicle group (Fig 6).

[0425] Analysis of the lean mass further provided useful insights. Lean mass did not differ significantly across groups, indicating that the treatments selectively influenced adiposity, rather than muscle or protein compartments (Fig 7).

[0426] At the end of the protocol, after euthanasia, adipose deposits were dissected and expressed as a percentage of body weight. Subcutaneous adipose tissue weight was significantly reduced in ATAMg treated groups as compared with vehicle (Fig 8).

[0427] Furthermore, brown adipose tissue weight was significantly higher in ATAMg-treated animals compared with vehicle (Figure 9).

[0428] Example 8: Effect of ATAMg on lipid profile

[0429] Animals on HFD, being treated with ATAMg_L, ATAMg_H, and vehicle as described above, were used for assessing effect of ATAMg on lipid profile. After euthanasia, blood was collected in K2EDTA tubes and centrifuged at 10,000 rpm for 5 min at 4°C. The plasma was collected, aliquoted, and snap frozen in liquid nitrogen and stored at -80°C for further analysis. Free fatty acids, triglycerides, HDL, and LDL cholesterol were analyzed in plasma using Pentra 400.

[0430] HDL cholesterol was significantly higher in ATAMg treated animals compared with vehicle (Fig 10).

[0431] In contrast, LDL cholesterol did not differ significantly between groups, indicating that ATAMg supplementation has a stabilizing effect on LDL particularly under HFD conditions (Fig 11 ).

[0432] Moreover, triglyceride levels were significantly reduced in the ATAMg group compared with vehicle (Fig 12).

[0433] Free fatty acid concentrations were also significantly decreased in the ATAMg group compared with vehicle, further indicating a positive impact of ATAMg supplementation particularly in HFD conditions (Fig 13).Example 9: Gene expression in brown adipose tissue

[0434] Brown adipose tissue samples were collected from the mice in ATAMg_H (1 sample per mouse) and control HFD+Vehicle (1 sample per mouse) groups following standard procedures. RNA of brown adipose tissues was extracted individually using TriReagent (Sigma Aldrich, France), according to the manufacturer’s instructions. Quantification analysis of total RNA was performed by analyzing 1 pl of each sample in Nanodrop. cDNA was prepared by reverse transcription of 500 ng total RNA using a RT iScript kit (Bio-rad, France).

[0435] Real-time PCR was performed with the Quantstudio real-time PCR system and software (Applied biotechnology) using SYBR Green Real-Time PCR Master Mixes (Bio-rad, France) for detection, according to the manufacturer’s instructions. B2m was chosen as the housekeeping gene. Gene expression of the following genes was analyzed: Ucp1, Ppargcla, Cidea, Dio2, Elovl3, Tnfa, and Pter. All samples were performed in duplicate, and data was analyzed according to the 2AACT method. The identity and purity of the amplified product was assessed by melting curve analysis at the end of amplification.

[0436] The data was expressed as the mean ± SEM. Data were analysed using GraphPad Prism version 10.00 for Windows (GraphPad Software, San Diego, CA, USA).

[0437] A selective induction of Ppargcla (PGC-1a) in BAT following ATAMg_H supplementation was observed (Fig 14). This reflects a commitment to functional BAT engagement rather than isolated marker expression in ATAMg-treated group.

[0438] Upward trends were also observed in Ucp1 (Fig 15), D / o2 (Fig 16), Cidea (Fig 17), and Elovl3 (Fig 18), a gene ensemble that defines thermogenically competent BAT.

[0439] In contrast, an absence of Pter modulation in BAT was observed (Fig 19). This indicates that ATAMg effects in BAT are not driven by local changes in taurine / N-acetyltaurine enzymatic regulation. Instead, involvement of downstream metabolic or systemic signals converging on mitochondrial and thermogenic pathways is the more reasonable explanation.

[0440] Additionally, a nominal anti-inflammatory trend was also observed, indicated by the tendency toward reduced Tnfa expression (Fig 20).

Claims

Claims1. Non-therapeutic use of a compound (C) according to Formula (He), or of stereoisomer thereof, or of a composition comprising the same, for managing / controlling weight, for controlling / maintaining normal weight, for controlling / preventing overweightness, for supporting weight loss, for supporting weight maintenance, for controlling / suppressing food intake, for controlling / reducing appetite, for reducing / controlling / preventing weight gain, for reducing fat mass, maintaining lean mass, reducing subcutaneous adipose tissue, increasing energy expenditure, and / or increasing brown adipose tissueFormula (He).

2. The non-therapeutic use according to claim 1 , wherein at least one gene involved in brown adipose tissue thermogenesis, mitochondrial function, lipid metabolism, adipocyte identity, and / or inflammatory modulation is modulated, such as at least one gene from the group consisting of Ucp1, Ppargcla, Cidea, Dio2, and Elovl3 is upregulated, particularly upregulated in brown adipose tissue.

3. A compound (C) according to Formula (He), or stereoisomer thereof, or a composition comprising the same, for use in the treatment or in the prevention of obesity, obesity associated metabolic disfunctions or disorders, and obesity associated noncommunicable diseases (NCDs),Formula (He).

4. The compound (C), or stereoisomer thereof, or the composition comprising the same, for use according to claim 3, wherein the associated metabolic disfunctions or disorders and / or associated noncommunicable diseases (NCDs) are selected from the group consisting of hypertension, liver cirrhosis, metabolic syndrome, cardiovascular diseases, cancers, neurological disorders, chronic respiratory diseases, and combinations thereof.

5. The compound (C), or stereoisomer thereof, or the composition comprising the same, for use according to claims 4, wherein metabolic syndrome includes dyslipidemia.

6. A compound (C) according to Formula (He), or stereoisomer thereof, or a composition comprising the same, for use in increasing lipolysis, reducing LDL cholesterol, increasing HDL cholesterol, reducing triglycerides, and / or reducing free fatty acidsFormula (He).

7. A compound (C) according to Formula (He), or stereoisomer thereof, or a composition comprising the same, for use according to any one of claims 3- 6, wherein at least one gene involved in brown adipose tissue thermogenesis, mitochondrial function, lipid metabolism, adipocyte identity, and / or inflammatory modulation is modulated, such as at least one gene from the group consisting of Ucp1, Ppargcla, Cidea, Dio2, and Elovl3 is upregulated, particularly upregulated in brown adipose tissue.

8. Non-therapeutic use of a compound (C) according to Formula (I), or of stereoisomer thereof, or of a composition comprising the same, for reducing fat mass, maintaining lean mass, reducing subcutaneous adipose tissue, increasing energy expenditure, and / or increasing brown adipose tissueFormula (I) wherein:- each of Ri is a C1-4 alkyl;- each of R2 is selected from H or COOH;- n is an integer equal to 0, 2 or 3;- m is an integer equal to 1 or 2;- X is selected from H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

9. The non-therapeutic use according to claim 8, wherein at least one gene involved in brown adipose tissue thermogenesis, mitochondrial function, lipid metabolism, adipocyte identity, and / or inflammatory modulation is modulated, such as at least one gene from the group consisting of Ucp1, Ppargcla, Cidea, Dio2, and Elovl3 is upregulated, particularly upregulated in brown adipose tissue.

10. A compound (C) according to Formula (I), or stereoisomer thereof, or a composition comprising the same, for use in the treatment or in the prevention of obesity associated metabolic disfunctions or disorders, and obesity associated noncommunicable diseases (NCDs),Formula (I) wherein:- each of Ri is a C1-4 alkyl;- each of R2 is selected from H or COOH;- n is an integer equal to 0, 2 or 3;- m is an integer equal to 1 or 2;- X is selected from H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

11. The compound (C), or stereoisomer thereof, or the composition comprising the same, for use according to claim 10, wherein the associated metabolic disfunctions or disorders and / or associated noncommunicable diseases (NCDs) are selected from the group consisting of hypertension, liver cirrhosis, metabolic syndrome, cardiovascular diseases, cancers, neurological disorders, chronic respiratory diseases, and combinations thereof.

12. The compound (C), or stereoisomer thereof, or the composition comprising the same, for use according to claim 11 , wherein metabolic syndrome includes dyslipidemia.

13. A compound (C) according to Formula (I), or stereoisomer thereof, or a composition comprising the same, for use in increasing lipolysis, reducing LDL cholesterol, increasing HDL cholesterol, reducing triglycerides, and / or reducing free fatty acidsFormula (I) wherein:- each of R1 is a C1-4 alkyl;- each of R2 is selected from H or COOH;- n is an integer equal to 0, 2 or 3;- m is an integer equal to 1 or 2;- X is selected from H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

14. A compound (C) according to Formula (I), or stereoisomer thereof, or a composition comprising the same, for use according to any one of claims 10- 13, wherein at least one gene involved in brown adipose tissue thermogenesis, mitochondrial function, lipid metabolism, adipocyte identity, and / or inflammatory modulation is modulated, such as at least one gene from the group consisting of Ucp1, Ppargcla, Cidea, Dio2, and Elovl3 is upregulated, particularly upregulated in brown adipose tissue.

15. A method for treating or preventing overweightness, obesity, and / or overweightness and obesity associated metabolic disfunctions or disorders, and / or overweightness and obesity associated noncommunicable diseases (NCDs), or for managing / controlling weight, for controlling obesity, for controlling / maintaining normal weight, for controlling overweightness, for supporting weight loss, for supporting weight maintenance, for suppressing food intake, for reducing appetite, for increasing lipolysis, for reducing / controlling weight gain, for reducing fat mass, for maintaining lean mass, for reducing subcutaneous adipose tissue, for increasing energy expenditure, and / or for increasing brown adipose tissue, comprising the step of administering an effective amount of a compound (C) according to general Formula (He)Formula (He).

16. The method according to claim 15, wherein at least one gene involved in brown adipose tissue thermogenesis, mitochondrial function, lipid metabolism, adipocyte identity, and / or inflammatory modulation is modulated, such as at least one gene from the group consisting of Ucp1, Ppargcla, Cidea, Dio2, and Elovl3 is upregulated, particularly upregulated in brown adipose tissue.

17. The method according to any one of claims 15-16, wherein the associated metabolic disfunctions or disorders and / or associated noncommunicable diseases (NCDs) are selected from the group consisting of hypertension, liver cirrhosis, metabolic syndrome, cardiovascular diseases, cancers, neurological disorders, chronic respiratory diseases, and combinations thereof.

18. A method for reducing LDL cholesterol, increasing HDL cholesterol, reducing triglycerides, and / or reducing free fatty acids, comprising the step of administering an effective amount of a compound (C) according to general Formula (He)>Formula (He).

19. A method for treating or preventing overweightness, obesity, and / or overweightness and obesity associated metabolic disfunctions or disorders, and / or overweightness and obesity associated noncommunicable diseases (NCDs), or for managing / controlling weight, for controlling obesity, for controlling / maintaining normal weight, for controlling overweightness, for supporting weight loss, for supporting weight maintenance, for suppressing food intake, for reducing appetite, for increasing lipolysis, for reducing / controlling weight gain, for reducing fat mass, for maintaining lean mass, for reducing subcutaneous adipose tissue, for increasing energy expenditure, and / or for increasing brown adipose tissue, comprising the step of administering an effective amount of a compound (C) according to general Formula (I)Formula (I)wherein:- each of Ri is a Ci-4 alkyl;- each of R2 is selected from H or COOH;- n is an integer equal to 0, 2 or 3;- m is an integer equal to 1 or 2;- X is selected from H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

20. The method according to claim 19, wherein at least one gene involved in brown adipose tissue thermogenesis, mitochondrial function, lipid metabolism, adipocyte identity, and / or inflammatory modulation is modulated, such as at least one gene from the group consisting of Ucp1, Ppargcla, Cidea, Dio2, and Elovl3 is upregulated, particularly upregulated in brown adipose tissue.

21. The method according to any one of claims 19-20, wherein the associated metabolic disfunctions or disorders and / or associated noncommunicable diseases (NCDs) are selected from the group consisting of hypertension, liver cirrhosis, metabolic syndrome, cardiovascular diseases, cancers, neurological disorders, chronic respiratory diseases, and combinations thereof.

22. A method for reducing LDL cholesterol, increasing HDL cholesterol, reducing triglycerides, and / or reducing free fatty acids, comprising the step of administering an effective amount of a compound (C) according to general Formula (I)Formula (I) wherein:each of R1 is a C1-4 alkyl;- each of R2 is selected from H or COOH;- n is an integer equal to 0, 2 or 3;- m is an integer equal to 1 or 2;- X is selected from H or an inorganic cation, wherein the inorganic cation is selected from the group consisting of an alkali metal cation and an alkaline earth metal cation.

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