36 results about "Inverse agonist" patented technology

The invention belongs to the field of medicines, and discloses a GPR6 inverse agonist as shown in the following formula (I), a preparation method, a pharmaceutical composition and application of the compound in preparation of medicines for treating GPR6-mediated related diseases.

The present invention relates to the use of an ROR inverse agonist or a pharmaceutically acceptable salt thereof for the preparation of a medicament for modulating ROR in a patient and / or for controlling autoimmune diseases and antibody-mediated rejection in a patient. The ROR-mediated diseases or autoimmune diseases include HIV, cancer, celiac disease, type 1 diabetes, Graves' disease (Graves' disease), inflammatory bowel disease, multiple sclerosis, psoriasis, rheumatoid arthritis, systemic lupus erythematosus, asthma, dermatitis, fatty liver disease, Crohn's disease (Crohn's disease), cardiovascular disease, inflammatory disease, nervous system disorders, multiple sclerosis, and the like. Acute respiratory distress syndrome and arteriosclerosis.

Provided are a compound having serotonin 5-HT2A receptor antagonism and / or inverse agonism, a pharmaceutically acceptable salt thereof, and a composition for serotonin 5-HT2A receptor antagonism and / or inverse agonism comprising them.A compound represented by Formula (I):wherein R1 is substituted or unsubstituted aromatic heterocyclyl or the like; R2 is each independently a hydrogen atom or the like; R3 is each independently a hydrogen atom or the like; n is 1 or the like; a combination of (L1, L2) is (NH, N) or the like; R4 is a group represented by Formula:wherein p and q are each independently 2 or the like; Ra is substituted or unsubstituted alkyl or the like; Xb is each independently CRbRb′; Rb is each independently a hydrogen atom or the like; Rb′ is each independently a hydrogen atom or the like; Xc is each independently CRcRc′; Rc is each independently a hydrogen atom or the like; Rc′ is each independently a hydrogen atom or the like; Xd is CRd or the like; and Rd is a hydrogen atom or the like; R5 and R6 are each independently a hydrogen atom or the like; and R7 is a group represented by Formula:wherein A is CR11 or the like; R9 is substituted or unsubstituted alkyloxy or the like; R10 is a hydrogen atom or the like; and R11 is each independently a hydrogen atom or the like; or a pharmaceutically acceptable salt thereof.

The invention relates to a novel compound as a 5-HT2A receptor inverse agonist, and a preparation method and a pharmaceutical composition thereof. The invention also relates to application of the compound or the pharmaceutical composition in preparation of drugs for treating 5-HT2A receptor related diseases, wherein the diseases comprise non-motor symptoms caused by Parkinson's disease, such as delusional disorder, hallusion, depression, anxiety, cognitive disorder and sleep disorder; dementia-related mental disorders; major depression; or negative symptoms of schizophrenia and the like.

The present invention relates to a novel compound as a 5-HT 2A receptor inverse agonist, a method for preparing the same and a pharmaceutical composition. It also relates to the use of the compound or the pharmaceutical composition in the manufacture of a medicament for treating 5-HT 2A receptor related diseases, including non-motor symptoms of Parkinson's disease: delusions, hallucinations, depression, anxiety, cognitive impairment, sleep disorders; dementia-related psychiatric disorders; major depressive disorder; or negative symptoms of schizophrenia, etc.

A salt form of a 5-HT 2A receptor inverse agonist, its preparation method and use. Specifically, provided are a pharmaceutically acceptable salt of a compound of formula (I), a crystal form of a fumarate salt thereof, a preparation method thereof, and use in treating a 5-HT2A receptor-related disease.

Disclosed herein are compounds suitable for use in the treatment of disorders, e.g., diabetic disorder, a dyslipidemia disorder, a cardiovascular disorder, an inflammatory disorder, a hepatic disorder, cancer, or obesity or co-morbidities thereof. Also disclosed are compositions containing one or more of the compounds and uses of the compounds in the treatment of disorders in a subject.

This invention provides compounds having serotonin 5-HT2A receptor inverse agonist activity or pharmaceutically permissible salts thereof, and compositions for serotonin 5-HT2A receptor inverse agonist containing the like. The compositions for serotonin 5-HT2A receptor inverse agonist contain a compound represented by formula (I) or a pharmaceutically permissible salt thereof, wherein in formula (I), R... 1 It is a substituted or unsubstituted aromatic heterocyclic group, etc., R 2 Each is independently a hydrogen atom, etc., R 3 Each is independently a hydrogen atom, etc., n is 1 or 2, R 4 It is a substituted or unsubstituted non-aromatic nitrogen-containing heterocyclic group, and L is -NR. 8 - etc., R 8 It is a hydrogen atom, etc., R 5 Each is independently a hydrogen atom, etc., R 6 Each is independently a hydrogen atom, etc., p is 1 or 2, R 7 It is a basis expressed by the following formula, where R 9 It is a substituted or unsubstituted alkoxy group, etc., R 10 It is a hydrogen atom, etc., R 11 It is a halogen, etc., where m is 0 or 1.

The invention relates to a novel compound as a 5-HT2A receptor inverse agonist, and a preparation method and a pharmaceutical composition thereof. The invention also relates to application of the compound or the pharmaceutical composition in preparation of drugs for treating 5-HT2A receptor related diseases, wherein the diseases comprise non-motor symptoms caused by Parkinson's disease, such as delusional disorder, hallusion, depression, anxiety, cognitive disorder and sleep disorder; dementia-related mental disorders; major depression; or negative symptoms of schizophrenia and the like.

The present invention relates to a compounds according to general formula (I), which acts as an inverse agonist of PqsR (the currently only known receptor for the Pseudomonas Quinolone Signal (PQS), sometimes also referred to as MvfR); to a pharmaceutical composition containing one or more of the compound(s) of the invention; to a combination preparation containing at least one compound of the invention and at least one further active pharmaceutical ingredient; and to uses of said compound(s), including the use as a medicament, e.g. the use in the treatment or prophylaxis of a bacterial infection, especially a Pseudomonas aeruginosa or Burkholderia infection.

The present disclosure relates to an antiviral pharmaceutical composition including an estrogen-related receptor γ (ERRγ) inhibitor as an active ingredient. According to embodiments of the present disclosure, an antiviral pharmaceutical composition containing an ERRγ inhibitor as an active ingredient has antiviral effects. In particular, the antiviral pharmaceutical composition is effective in preventing or treating RNA virus infections. Specifically, the ERRγ inhibitor, especially an ERRγ inverse agonist, may exhibit broad-spectrum antiviral effects by inhibiting ERRγ activity in RNA virus-infected cells, thereby blocking fatty acid biosynthesis mediated by sterol regulatory element-binding protein 1c (SREBP1c).

Disclosed herein are compounds suitable for use in the treatment of disorders, e.g., diabetic disorder, a dyslipidemia disorder, a cardiovascular disorder, an inflammatory disorder, a hepatic disorder, cancer, or obesity or co-morbidities thereof. Also disclosed are compositions containing one or more of the compounds and uses of the compounds in the treatment of disorders in a subject.

Disclosed herein are compounds suitable for use in the treatment of disorders, e.g., diabetic disorder, a dyslipidemia disorder, a cardiovascular disorder, an inflammatory disorder, a hepatic disorder, cancer, or obesity or co-morbidities thereof. Also disclosed are compositions containing one or more of the compounds and uses of the compounds in the treatment of disorders in a subject.

Methods and compositions for the treatment of conditions associated with pharyngeal airway muscle collapse while the subject is in a non-fully conscious state, e.g., sleep apnea and snoring, comprising administration of (i) a norepinephrine reuptake inhibitor (NRI) and (ii) a non myorelaxing hypnotic and / or 5-HT2A inverse agonist or antagonist.

The invention relates to a novel compound as a 5-HT2A receptor inverse agonist, and a preparation method and a pharmaceutical composition thereof. The invention also relates to application of the compound or the pharmaceutical composition in preparation of drugs for treating 5-HT2A receptor related diseases, wherein the diseases comprise non-motor symptoms caused by Parkinson's disease, such as delusional disorder, hallusion, depression, anxiety, cognitive disorder and sleep disorder; dementia-related mental disorders; major depression; or negative symptoms of schizophrenia and the like.

The present application relates to an antiviral pharmaceutical composition comprising an estrogen-related receptor γ (ERRγ) inhibitor as an active ingredient. The antiviral pharmaceutical composition comprising an ERRγ inhibitor as an active ingredient, according to embodiments of the present application, has an antiviral effect, and in particular, can exhibit the effect of preventing or treating RNA viral infection. Specifically, the ERRγ inhibitor, particularly an ERRγ inverse agonist, inhibits ERRγ activity in cells infected with RNA virus, thereby blocking SREBP1c-mediated fatty acid biosynthesis, and thus can exhibit broad-spectrum antiviral efficacy.

The invention provides a compound as shown in a formula (I), and a stereoisomer or pharmaceutically acceptable salt thereof. The compound provided by the invention is used as a CB1 receptor antagonist or inverse agonist, and the compound and the pharmaceutical composition thereof can be used for preparing drugs for treating and / or preventing CB1 receptor mediated diseases.

The invention relates to a novel compound as a 5-HT2A receptor inverse agonist, and a preparation method and a pharmaceutical composition thereof. The invention also relates to application of the compound or the pharmaceutical composition in preparation of drugs for treating 5-HT2A receptor related diseases, wherein the diseases comprise non-motor symptoms caused by Parkinson's disease, such as delusional disorder, hallusion, depression, anxiety, cognitive disorder and sleep disorder; dementia-related mental disorders; major depression; or negative symptoms of schizophrenia and the like.

Methods and compositions for the treatment of conditions associated with pharyngeal airway muscle collapse while the subject is in a non-fully conscious state, e.g., sleep apnea and snoring, comprising administration of (i) a norepinephrine reuptake inhibitor (NRI) and (ii) a non myorelaxing hypnotic and / or 5-HT2A inverse agonist or antagonist.

The invention provides a compound as shown in a formula (I). The compound as a medicine has a good inverse agonistic effect on a CB1 receptor. Compared with the existing known CB1 receptor inverse agonist, the CB1 receptor inverse agonist has the following advantages: 1) the CB1 receptor inverse agonist has lower brain penetration capability, so that the CB1 receptor inverse agonist has better safety and can avoid or relieve neuropsychiatric side effects; and 2) the oral bioavailability is better.

Administration of receptor antagonists, inverse agonists, allosteric modulators or signaling specific inhibitors of cannabinoid receptor 1 (CB1) prevents and treats conditions and complications in patients, including conditions and complications associated with treatment of various cardiovascular diseases. Patients with the history of use of cannabis have the risk of severe complications. Administration of inhibitors or modulators of CB1 during perioperative, intraoperative and / or postoperative periods results in an improvement in the outcome of a patient for methods involving the treatment of cardiovascular diseases, such as percutaneous coronary intervention, coronary artery bypass surgery or stenting.

The present invention provides a compound. Specifically, the present invention provides a compound having a structure as shown in the following formula (I), or an optical isomer, a pharmaceutically acceptable salt, a prodrug, a deuterated derivative, a hydrate, and a solvate thereof. The compound can effectively inhibit PPARG, and is used for treating or preventing diseases or disorders related to PPARG activity or expression level.

Disclosed herein are compounds suitable for use in the treatment of disorders, e.g., diabetic disorder, a dyslipidemia disorder, a cardiovascular disorder, an inflammatory disorder, a hepatic disorder, cancer, or obesity or co-morbidities thereof. Also disclosed are compositions containing one or more of the compounds and uses of the compounds in the treatment of disorders in a subject.

Certain serotonin type 4 receptor (5-HT4Rs) inverse agonists or antagonists are protective against stress-induced behavior and can treat stress-induced behavior. These 5-HT4R inverse agonists or antagonists can be administered to subjects in need, to help prevent and treat stress-induced behavior psychiatric disorders.

The present invention relates to a compound according to general formula (I), which acts as an inverse agonist of PqsR (the currently only known receptor for the Pseudomonas Quinolone Signal (PQS), sometimes also referred to as MvfR); to a pharmaceutical composition containing one or more of the compound(s) of the invention: to a combination preparation containing at least one compound of the invention and at least one further active pharmaceutical ingredient; and to uses of said compound(s), including the use as a medicament, e.g. the use in the treatment or prophylaxis of a bacterial infection, especially a Pseudomonas aeruginosa or Burkholderia infection.

Provided are methods of treating neuropsychiatric disorders including obsessive-compulsive related disorders, tic disorders, glutamate excitotoxicity related disorders, autism spectrum disorders, and other medical conditions in patients with a mutation in genes involving function, structure, or plasticity, including but not limited to SHANK3, SAPAP3, NLGN3, NLGN4, NRXN1, CNTNAP2, or MECP2. The methods include administering an effective amount of a histamine type 1 receptor agonist and / or histamine type 3 receptor antagonist or inverse agonist, their pharmaceutically acceptable salts, analogs, metabolites, and prodrugs, including prodrugs of its metabolites, to patients in need of such treatment.

Described herein are methods of treating polycystic kidney disease (PKD) in a patient in need thereof comprising administering to said patient an effective amount of a PPAR-γ modulator wherein the PPAR-γ modulator is a non-activating (non-agonist) modulator of PPAR-γ. The PKD can be autosomal dominant polycystic kidney disease (ADPKD) or autosomal recessive polycystic kidney disease (ARPKD). The PPAR-γ modulator can, for example, be an inverse agonist of PPAR-γ.

The present invention relates to the field of medicine. Disclosed are a monocyclic GPR6 inverse agonist and a use thereof. Specifically, provided are a GPR6 inverse agonist as shown in formula (I), a preparation method, a pharmaceutical composition, and a use of the compound in the treatment of GPR6-mediated related diseases.