30 results about "Cannabinoid Receptor Modulators" patented technology

Pharmaceutical compositions in which isolated cannabinoid receptor modulators are optionally combined with terpene blends in a pharmaceutically acceptable carrier. Methods for treating or preventing a disease, disorder, dysfunction or condition caused by exposure to an organophosphate or carbamate acetylcholineesterase inhibitor with the inventive compositions are also disclosed.

The present disclosure provides Diels-Alder adducts of chalcone and prenylphenyl moieties capable of modulating the activity of cannabinoid receptors, and to oligomers of flavan-3-ol capable of modulating fat absorption and storage. Such Diels-Alder adducts of chalcone and prenylphenyl moieties or oligomers of flavan-3-ol can optionally be used in combination with other weight management agents, such as anorectic agents, a lipase inhibitors, other cannabinoid receptor modulators, psychotropic agents, insulin sensitizers, stimulants, or satiety agents, as well as to methods of use thereof such as treating or preventing weight gain or obesity, promoting weight loss, appetite suppression, modifying satiety, or the like.

Described herein are substituted 2-(azetidin-2-on-1-yl)alkanoic acids, alkanedioic acids and 2-hydroxyalkyl alkanoic acids, and 2-acyl alkanoic acids, and derivatives thereof, that are capable of modulating activity at the cannabinoid-1 (CB1) and/or cannabinoid-2 (CB2) receptor. Also described herein are methods for treating mammals in need of relief from disease states associated with and responsive to modulation of the CB1 and/or CB2 receptor activity.

Novel compounds of structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as psychotropic drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinsons disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as, the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

Compounds of formula (I) are modulators of cannabinoid receptor CB1, useful inter alia for treatment of obesity: Formula (I). Wherein: X is a bond, or a divalent radical selected from —C(R₁₀)(R₁₁)—*, —C(R₁₀)(R₁₁)—O—*, —C(R₁₀)(R₁₁)CH₂—*, —C(R₁₀)(R₁₁)CH₂—O—*, —CH₂C(R₁₀)(R₁₁)—*, —CH₂C(R₁₀)(R₁₁)—O—*. and —CH₂—O—C(R₁₀)(R₁₁)—*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; Z is a carboxyl isostere radical selected from the group specified; R₃ is hydrogen, (C₁-C)alkyl or (C₁C₃)fluoroalkyl; R₄ is a radical of formula -(Alk₁)_p-(Q₁)_r (L)_s-Q₂ wherein p, r, s, Alk₁, L, Q₁ and Q₂ are as specified; or R₃and R₄ taken together with the nitrogen to which they are attached form a cyclic amino ring of 4 to 7 ring atoms which is optionally substituted by a radical of formula -(L)_s-Q₂ wherein s, L and Q₂ are as defined above, or by an optional substituent selected from hydroxy, methoxy, —NH₂—, or mono- or di-(C₁C₃)alkylamino; R₅, R₆, R₇ and R₈ are each independently selected from hydrogen —F, —Cl, —Br, —CN, (C₁-C₃)alkyl, (C₁C₃)fluoroalkyl, cyclopropyl, and —OR₉; R₁₀ is hydrogen, (C₁C₃)alkyl, hydroxyl or NH₂, and R₁₁ is hydrogen or (C₁-C₃)alkyl; or R₁₀ and R₁₁ taken together with the carbon atom to which they are attached form a (C₃-C₅)cycloalkyl ring.

The invention is directed to the use of at least one CBx modulator wherein the CBx modulator is selected from the group consisting of CB1 agonists; CB2 agonists; CB2 partial agonists; CB2 antagonists; CB2 inverse agonists; and dually acting compounds which are both a CB1 agonist and a CB2 agonist; and mixtures thereof, as KATP channel modulator for the prophylaxis, treatment, delayed progression, delayed onset and/or inhibition of a variety of disease conditions including obesity, diabetes mellitus, metabolic syndrome, syndrome X, insulinoma, familial hyperinsulemic hypoglycemia, male pattern baldness, detrusor hyperreactivity, asthma, neuroprotection, epilepsy, analgesia, cardioprotection, angina, cardioplegia, arrhythmia, coronary spasm, peripheral vascular disease, cerebral vasospasm, appetite regulation, neurodegeneration, pain - including neuropathic pain and chronic pain - and impotence in mammals and humans. The invention further relates to methods of treating, preventing, delaying progression of, delaying onset of and/or inhibiting a variety of disease conditions including obesity, diabetes mellitus, metabolic syndrome, syndrome X, insulinoma, familial hyperinsulemic hypoglycemia, male pattern baldness, detrusor hyperreactivity, asthma, neuroprotection, epilepsy, analgesia, cardioprotection, angina, cardioplegia, arrhythmia, coronary spasm, peripheral vascular disease, cerebral vasospasm, appetite regulation, neurodegeneration, pain - including neuropathic pain and chronic pain - and impotence in mammals and humans comprising administering to a subject in need thereof an effective amount of at least one CBx modulator having KATP channel modulating properties.

The present invention relates to novel cannabinoid receptor modulators, in particular cannabinoid 1 (CB1) or cannabinoid 2 (CB2) receptor modulators, and uses thereof for treating diseases, conditions and/or disorders modulated by a cannabinoid receptor (such as pain, neurodegenative disorders, eating disorders, weight loss or control, and obesity).

The present invention relates to novel cannabinoid receptor modulators, in particular cannabinoid 1 (CB1) or cannabinoid 2 (CB2) receptor modulators, and uses thereof for treating diseases, conditions and/or disorders modulated by a cannabinoid receptor (such as pain, neurodegenative disorders, eating disorders, weight loss or control, and obesity).

Compounds of formula (I), are cannabinoid CB1 receptors, useful, inter alia in the treatment of obesity:

wherein A₁ is hydrogen, —COOH, or tetrazolyl, and A₂ is hydrogen, —COOH, tetrazolyl, —CN, —CF₃, —COR₆, —SO₂R₆, —OR₇, —NR₇R₈, —NHCOR₆, and —NR₇SO₂R₈ provided that one of A₁ and A₂ is either —COOH or tetrazolyl; p is 0 or 1 and A₃ is phenyl or cycloalkyl, either of which is optionally substituted with R₄ and/or R₅; q is 0 or 1; R₁ is a bond, or —(CH₂)_aB₁(CH₂)_b— wherein a and b are independently 0, 1, 2 or 3 provided that a+b is not greater than 4, and B₁ is —CO—, —O—, —S—, —SO—, —SO₂—, —CH₂—, —CHOH— or —NR₇—; R₂ is a bond, —CH₂)_aB₁(CH₂)_b— or —[(CH₂)_aB₁(CH₂)_b]_n-A₄-[(CH₂)_cB₂(CH₂)_d]_m— wherein a, b, and B₁ are as defined for R₁; B₂ is as defined for B₁, c and d are independently 0, 1, 2 or 3; with the proviso that a+b+c+d is not greater than 6, n and m are independently 0 or 1 and A₄ is a monocarbocyclic or monoheterocyclic ring, having 3 to 8 ring atoms, optionally substituted with one or more of —F, —Cl, —Br, —CN, —CF₃, C₁-C₄ alkyl, cycloalkyl, —OR₉, oxo or —NR₇R₈; R₃ is hydrogen, C₁-C₄ alkyl, cycloalkyl, —CF₃, —OR₉, —NR₇R₈, —(CH₂)_sCOR₆, —(CH₂)_sSO₂R₆, —(CH₂)_sNR₇COR₆, —(CH₂)_sNR₇COOR₈, —(CH₂)_sNR₇SO₂R₆, wherein s is 1, 2, 3 or 4; R₄ and R₅ independently —R₉, —CN, —F, —Cl, —Br, —OR₉, —NR₇R₈, —NR₇COR₆, —NR₇SO₂R₆, —COR₆, —SR₉, —SOR₉, —SO₂R₆, (C₁-C₄ alkyl)OR₉, —(C₁-C₄ alkyl)NR₇R₈, —(C₁-C₄ alkyl)NR₇COR₆, C₁-C₄ alkyl)NR₇COOR₈, —(C₁-C₄ alkyl)NR₇SO₂R₆, —(C₁-C₄ alkyl)COR₆, —(C₁-C₄ alkyl)SO₂R₆, —NR₇COOR₈, or [N—(C₁-C₄ alkyl)]-tetrazolyl; R₆ is C₁-C₄ alkyl, cycloalkyl, —CF₃ or —NR₇R₈; R₇ and R₈ are independently hydrogen, C₁-C₄ alkyl or cycloalkyl; and R₉ is hydrogen, C₁-C₄ alkyl, cycloalkyl, fully or partially fluorinated C₁-C₄ alkyl.

The present invention relates to novel cannabinoid receptor modulators, in particular cannahinoid I (CB1) or cannabinoid 2 (CH2) receptor modulators, and uses thereof for treating diseases, conditions and/or disorders modulated by a cannabinoid receptor (such as pain, neurodegenerative disorders, eating disorders, weight loss or control, and obesity).

The invention relates to the preparation of a curcumin derivative and application of the curcumin derivative as a cannabinoid receptor modulator. In the synthetic route of the curcumin derivative, 10% of Pd-C is used for reducing the curcumin; for protecting a phenolic hydroxyl group, only 2.0% mol of DMAP (Dimethylaminopyridine) is used for catalysis and (Boc)2O of which the mole amount is 2.05 times as much as that of the curcumin is used so that reaction is completely realized; during a Mannich reaction, Mannich reagents such as N,N,N',N'-tetramethyldiaminomethane prepared in advance are used so as to avoid that an acid component reacts with formaldehyde to generate by-products at first. In the whole route, the target compound is obtained through reducing, protection, alkylation, deprotection and the Mannich reaction with the curcumin as the raw material. The route has the characteristics of cheap and available raw material, high yield and easy operation. The curcumin derivative is capable of inhibiting the hepatic stellate cells of a hepatic fibrosis rat from synthesizing and secreting extracellular matrix through a cannabinoid receptor, promoting the degradation of the extracellular matrix, reducing the deposition of the extracellular matrix in the liver and further developing the effect of treating the hepatic fibrosis.

The invention is directed to pharmaceutical compositions comprising pharmacologically effective quantities of each of a) at least one KATP channel modulator as a first active agent and b) at least one CBx modulator as a second active agent. The invention further relates to the use of such compositions and to methods of treating, preventing, delaying progression of, delaying onset of and/or inhibiting a variety of disease conditions including obesity, diabetes mellitus, metabolic syndrome, syndrome X, insulinoma, familial hyperinsulemic hypoglycemia, male pattern baldness, detrusor hyperreactivity, asthma, neuroprotection, epilepsy, analgesia, cardioprotection, angina, cardioplegia, arrhythmia, coronary spasm, peripheral vascular disease, cerebral vasospasm, appetite regulation, neurodegeneration, pain - including neuropathic pain and chronic pain - and impotence in mammals and humans by administering such compositions to subjects in need thereof. The invention also is directed to processes of manufacturing such compositions.

Oral formulations of benzofuran compounds which modulate cannabinoid receptors are presented. Methods of using these formulations for treatment of cannabinoid receptor-mediated disease, including neuropathic pain and addition, are also described.