摘要:
The present invention relates to pharmaceutical compositions comprising therapeutic combinations comprising: one or more H3 antagonists/inverse agonists; one or more appetite suppressants selected from the group consisting of CB1 antagonists/inverse agonists, sibutramine, phentermine and topiramate; and optionally one or more HMG-CoA reductase inhibitors. The invention also relates to medicaments and kits comprising the pharmaceutical compositions of the present invention, and methods of treating obesity, obesity related disorders and diabetes using the pharmaceutical compositions of the present invention.
摘要:
Disclosed are compounds of the formula or a pharmaceutically acceptable salt thereof, wherein M1 is M2 is N; X is a bond, optionally substituted alkylene, alkenylene, —O—, —CH2N(R12)—, —N(R12)CH2—, —N(R12)—, —NHC(O)—, —OCH2—, —CH2O—, or —S(O)0-2—; and Y is —(CH2)1-2—, —C(═O)—, —C(═NOR13)— or —SO0-2—; or M1 is N; M2 is N or CH; X is a bond, alkylene, alkenylene, —C(O)—, —NHC(O)—, —OC(O)— or —S(O)1-2—; Y is —(CH2)1-2—, —C(═O)— or —SO0-2—; and when M2 is CH, Y is also Y is —O— or —C(═NOR13)—; Z is a bond or optionally substituted alkylene or alkenylene; U and W are CH, or one is CH and one is N; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; and compositions and methods of treating obesity, metabolic syndrome and a cognition deficit disorder, alone or in combination with other agents.
摘要:
Disclosed are compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is —C(═O)—, —C(═S)—, —(CH2)q—, —C(═NOR7)— or —SO1-2—; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, alkyl, alkenyl, or optionally substituted cycloalkyl, aryl, heteroaryl, heterocycloalkyl or a group of the formula: where ring A is a monoheteroaryl ring; R1 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome nonalcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma or cognition deficit disorders using said compounds, alone or in combination with other agents.
摘要翻译:公开了下式的化合物或其药学上可接受的盐,其中:M 1和M 3是CH或N; M 2是CH,CF或N; Y是-C(-O) - , - C(-S) - , - (CH 2 CH 2)q - , - C(-NOR 7) / SO 2 - ) - 或-SO 2 1-2。 Z是键或任选取代的亚烷基或亚烯基; R 1是H,烷基,烯基或任选取代的环烷基,芳基,杂芳基,杂环烷基或下式的基团:其中环A是单杂芳基环; R 1是任选取代的烷基,烯基,芳基,杂芳基,环烷基或杂环烷基; 剩余的变量如规范中所定义; 使用所述化合物单独或与其它试剂组合治疗过敏引起的气道反应,充血,肥胖,代谢综合征非酒精性脂肪性肝病,肝脂肪变性,非酒精性脂肪性肝炎,肝硬化,肝细胞癌或认知缺陷障碍的组合物和方法。
摘要:
The present invention discloses the compound of Formula I and pharmaceutically acceptable salts and solvates thereof. The invention also relates to pharmaceutical compositions comprising the Compound of Formula I and its use in treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease. The invention also relates to the use of a combination of the Compound of Formula I with additional therapeutic agents for treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease.
摘要:
The present invention discloses the compound of Formula I and pharmaceutically acceptable salts and solvates thereof. The invention also relates to pharmaceutical compositions comprising the Compound of Formula I and its use in treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease. The invention also relates to the use of a combination of the Compound of Formula I with additional therapeutic agents for treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease.
摘要:
Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: M is CH or N; U and W are each CH, or one of U and W is CH and the other is N; X is a bond, alkylene, —C(O)—, —C(N—OR5)—, —C(N—OR5)—CH(R6)—, —CH(R6)—C(N—OR5)—, —O—, —OCH2—, —CH2O— or —S(O)0-2—; Y is —O—, —(CH2)2—, —C(═O)—, —C(═NOR7)— or —SO0-2—; Z is a bond, optionally substituted alkylene or alkylene interrupted by a heteroatom or heterocyclic group; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl, or benzimidazolyl or a derivative thereof; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods for treating an allergy-induced airway response, congestion, diabetes, obesity, an obesity-related disorder, metabolic syndrome and a cognition deficit disorder using said compounds, alone or in combination with other agents.
摘要:
Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is —C(═O)—, —C(═S)—, —(CH2)q—, —C(═NOR7)— or —SO1-2—; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, or alkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, all optionally substituted, or a group of the formula: where ring A is a heteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R3 is H, —C(O)NH2, or alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl, all optionally substituted; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome, alcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma and cognition deficit disorders using said compounds, alone or in combination with other agents.
摘要翻译:公开了下式的新化合物或其药学上可接受的盐,其中:M 1和M 3是CH或N; M 2是CH,CF或N; Y是-C(-O) - , - C(-S) - , - (CH 2 CH 2)q - , - C(-NOR 7) / SO 2 - ) - 或-SO 2 1-2。 Z是键或任选取代的亚烷基或亚烯基; R 1是H或烷基,环烷基,芳基,杂芳基,杂环烷基,全部是任选取代的,或下式的基团:其中环A是杂芳基环; R 2是任选取代的烷基,烯基,芳基,杂芳基,环烷基或杂环烷基; R 3是H,-C(O)NH 2或烷基,芳基,环烷基,杂环烷基或杂芳基,全部任选被取代; 剩余的变量如规范中所定义; 使用所述化合物单独或与其它试剂组合治疗过敏引起的气道反应,充血,肥胖,代谢综合征,酒精性脂肪肝疾病,肝脂肪变性,非酒精性脂肪性肝炎,肝硬化,肝细胞癌和认知缺陷障碍的组合物和方法。
摘要:
Disclosed are compounds of Formula A: (structurally represented) where “RG1”, “RG2a”, “RG4”, “RG5”, “MG1”, “n” and “m” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
摘要:
Methods and systems are disclosed for creating an aqueous flow pathway in the trabecular meshwork, juxtacanalicular trabecular meshwork and Schlemm's canal of an eye for reducing elevated intraocular pressure. Some embodiments described apparatus and methods useful in photoablation of tissues. In some embodiments, a photoablation apparatus is used to perforate a tissue, forming an aperture into a space behind the tissue. Gases formed during a photoablation process can be used to pressurize the space behind the tissue to enhance patency of the space. In some embodiments the tissue is the trabecular meshwork of the eye and a wall of Schlemm's canal, and the space behind the tissue is a portion of the lumen of Schlemm's canal. In some embodiments, the method is useful in the treatment of glaucoma by improving outflow from the anterior chamber of the eye into Schlemm's canal, reducing intraocular pressure.
摘要:
Methods and systems are disclosed for creating an aqueous flow pathway in the trabecular meshwork, juxtacanalicular trabecular meshwork and Schlemm's canal of an eye for reducing elevated intraocular pressure. Some embodiments described apparatus and methods useful in photoablation of tissues. In some embodiments, a photoablation apparatus is used to perforate a tissue, forming an aperture into a space behind the tissue. Gases formed during a photoablation process can be used to pressurize the space behind the tissue to enhance patency of the space. In some embodiments the tissue is the trabecular meshwork of the eye and a wall of Schlemm's canal, and the space behind the tissue is a portion of the lumen of Schlemm's canal. In some embodiments, the method is useful in the treatment of glaucoma by improving outflow from the anterior chamber of the eye into Schlemm's canal, reducing intraocular pressure.