专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20070142394A1 Substituted aniline derivatives useful as histamine H3 antagonists 失效
标题翻译：用作组胺H3拮抗剂的取代苯胺衍生物
公开(公告)号：US20070142394A1
公开(公告)日：2007-06-21
申请号：US11641153
申请日：2006-12-19
申请人： Daniel Solomon , Robert Aslanian , Michael Berlin , Manuel de Lera Ruiz , Kevin McCormick , Mwangi Mutahi , Wing Tom
发明人： Daniel Solomon , Robert Aslanian , Michael Berlin , Manuel de Lera Ruiz , Kevin McCormick , Mwangi Mutahi , Wing Tom
IPC分类号： A61K31/496 , A61K31/4545 , C07D403/14 , C07D401/14
CPC分类号： C07D401/12 , C07D213/73 , C07D213/74 , C07D401/14 , C07D471/04
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是M 2是N; X是一个键，任选取代的亚烷基，亚烯基，-O - ， - CH 2 N（R 12） - ， - N（R 12） CH 2 - ， - N（R 12） - ， - NHC（O） - ， - OCH 2 - ， - O 2或-S（O）0-2 - ; 并且Y是 - （CH 2）2 - ， - C（ - ） - ， - C（-NOR 13） - 或-SO <0-2 < - >。或M 1是N; M 2是N或CH; X是键，亚烷基，亚烯基，-C（O） - ， - NHC（O） - ， - OC（O） - 或-S（O） Y是 - （CH 2）2 - ， - C - （ - O） - 或-SO 0-2 - 。当M 2是CH时，Y也是Y是-O-或-C（-NOR 13） - ; Z是键或任选取代的亚烷基或亚烯基; U和W是CH，或一个是CH，一个是N; R 1是任选取代的烷基，环烷基，芳基，芳烷基，杂芳基，杂环烷基; R 2是任选取代的烷基，烯基，芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基或杂环烷基; 剩余的变量如规范中所定义; 以及单独或与其他药物组合治疗肥胖症，代谢综合征和认知缺陷障碍的组合物和方法。

2. 发明申请

US20070015807A1 Heteroatom-linked substituted piperidines and derivatives thereof useful as histamine H3 antagonists 失效
标题翻译：杂原子取代的哌啶及其衍生物可用作组胺H3拮抗剂
公开(公告)号：US20070015807A1
公开(公告)日：2007-01-18
申请号：US11455625
申请日：2006-06-19
申请人： Robert Aslanian , Michael Berlin , Christopher Boyce , Jianhua Chao , Manuel de Lera Ruiz , Pietro Mangiaracina , Kevin McCormick , Mwangi Mutahi , Stuart Rosenblum , Neng-Yang Shih , Daniel Solomon , Wing Tom , Henry Vaccaro , Junying Zheng , Xiaohong Zhu
发明人： Robert Aslanian , Michael Berlin , Christopher Boyce , Jianhua Chao , Manuel de Lera Ruiz , Pietro Mangiaracina , Kevin McCormick , Mwangi Mutahi , Stuart Rosenblum , Neng-Yang Shih , Daniel Solomon , Wing Tom , Henry Vaccaro , Junying Zheng , Xiaohong Zhu
IPC分类号： C07D403/02 , A61K31/4178 , A61K31/4025
CPC分类号： C07D295/185 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , Y02P20/582
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。

3. 发明申请

US20070167435A1 Phenoxypiperidines and analogs thereof useful as histamine H3 antagonists 失效
标题翻译：苯氧基哌啶及其类似物可用作组胺H3拮抗剂
公开(公告)号：US20070167435A1
公开(公告)日：2007-07-19
申请号：US11641175
申请日：2006-12-19
申请人： Mwangi Mutahi , Robert Aslanian , Michael Berlin , Christopher Boyce , Manuel de Lera Ruiz , Kevin McCormick , Daniel Solomon , Henry Vaccaro , Junying Zheng , Purakkattle Biju , Younong Yu , Wei Zhou , Xiaohong Zhu
发明人： Mwangi Mutahi , Robert Aslanian , Michael Berlin , Christopher Boyce , Manuel de Lera Ruiz , Kevin McCormick , Daniel Solomon , Henry Vaccaro , Junying Zheng , Purakkattle Biju , Younong Yu , Wei Zhou , Xiaohong Zhu
IPC分类号： A61K31/551 , A61K31/501 , A61K31/506 , A61K31/4745 , C07D471/02
CPC分类号： C07D471/04 , C07D213/38 , C07D213/73 , C07D277/40 , C07D401/06 , C07D401/12 , C07D401/14 , C07D409/12 , C07D417/06 , C07D417/14 , C07D473/00
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.
摘要翻译：公开了下式的化合物或其药学上可接受的盐或溶剂化物，其中：M是CH或N; U和W各自为CH，或U和W中的一个为CH，另一个为N; X是键，亚烷基，-C（O） - ， - C（N-OR 5） - ， - （N -OR 5）-CH（R - （CH 3） - ， - CH（R 6） - ， - （N-OR 5） - ， - O - ， - 2 - ， - CH 2 O-或-S（O）0-2 - 。 Y是-O-， - （CH 2）2 - ， - C（-O） - ， - C（-NOR 7） - 或-SO <0-2 - ; - Z是一个键，任选取代的被杂原子或杂环基中断的亚烷基或亚烷基; R 1是任选取代的烷基，环烷基，芳基，芳基烷基，杂芳基，杂环烷基或苯并咪唑基或其衍生物; R 2是任选取代的烷基，烯基，芳基，芳基烷基，杂芳基，杂芳基烷基，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，糖尿病，肥胖，肥胖相关病症，代谢综合征和认知缺陷障碍的组合物和方法。

4. 发明申请

US20070010513A1 Carbon-linked substituted piperidines and derivatives thereof useful as histamine H3 antagonists 失效
标题翻译：碳链取代的哌啶及其衍生物可用作组胺H3拮抗剂
公开(公告)号：US20070010513A1
公开(公告)日：2007-01-11
申请号：US11455873
申请日：2006-06-19
申请人： Robert Aslanian , Michael Berlin , Ying Huang , Kevin McCormick , Mwangi Mutahi , Neng-Yang Shih , Pauline Ting , Wing Tom , Junying Zheng
发明人： Robert Aslanian , Michael Berlin , Ying Huang , Kevin McCormick , Mwangi Mutahi , Neng-Yang Shih , Pauline Ting , Wing Tom , Junying Zheng
IPC分类号： A61K31/538 , A61K31/4709 , A61K31/4704 , C07D265/12
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14
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。

5. 发明申请

US20080058370A1 1-[[1-[(2-Amino-6-methyl-4-pyridinyl)methyl]-4-fluoro-4-piperidinyl]carbonyl]-4-[2-(2-pyridinyl)-3H-imidazo[4,5-b]pyridin-3-yl]piperidine and Methods of Use Thereof 失效
标题翻译： 1 - [[1 - [（2-氨基-6-甲基-4-吡啶基）甲基] -4-氟-4-哌啶基]羰基] -4- [2-（2-吡啶基）-3H-咪唑并[4 ，5-b]吡啶-3-基]哌啶及其使用方法
公开(公告)号：US20080058370A1
公开(公告)日：2008-03-06
申请号：US11837248
申请日：2007-08-10
申请人： Manuel de Lera Ruiz , Robert Aslanian , Michael Berlin , Kevin McCormick , Chander Celly
发明人： Manuel de Lera Ruiz , Robert Aslanian , Michael Berlin , Kevin McCormick , Chander Celly
IPC分类号： A61K31/437 , A61P1/00 , A61P3/00 , A61P3/04 , A61P3/10
CPC分类号： C07D471/04
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.
摘要翻译：本发明公开了式I化合物及其药学上可接受的盐和溶剂化物。本发明还涉及包含式I化合物及其在治疗肥胖，代谢综合征，糖尿病，肝脏脂质沉积或非酒精性脂肪性肝病中的用途的药物组合物。本发明还涉及式I化合物与用于治疗肥胖，代谢综合征，糖尿病，肝脏脂质沉积或非酒精性脂肪性肝病的其它治疗剂的组合的用途。

6. 发明申请

US20070066644A1 1-[[1-[(2-Amino-6-methyl-4-pyridinyl)methyl]-4-fluoro-4-piperidinyl]carbonyl]-4-[2-(2-pyridinyl)-3H-imidazo[4,5-b]pyridin-3-yl]piperidine 失效
标题翻译： 1 - [[1 - [（2-氨基-6-甲基-4-吡啶基）甲基] -4-氟-4-哌啶基]羰基] -4- [2-（2-吡啶基）-3H-咪唑并[4 ，5-b]吡啶-3-基]哌啶
公开(公告)号：US20070066644A1
公开(公告)日：2007-03-22
申请号：US11523489
申请日：2006-09-19
申请人： Manuel de Lera Ruiz , Robert Aslanian , Michael Berlin , Kevin McCormick , Chander Celly
发明人： Manuel de Lera Ruiz , Robert Aslanian , Michael Berlin , Kevin McCormick , Chander Celly
IPC分类号： A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
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.
摘要翻译：本发明公开了式I化合物及其药学上可接受的盐和溶剂化物。本发明还涉及包含式I化合物及其在治疗肥胖，代谢综合征，糖尿病，肝脏脂质沉积或非酒精性脂肪性肝病中的用途的药物组合物。本发明还涉及式I化合物与用于治疗肥胖，代谢综合征，糖尿病，肝脏脂质沉积或非酒精性脂肪性肝病的其它治疗剂的组合的用途。

7. 发明申请

US20070142369A1 Combination of an H3 antagonist/inverse agonist and an appetite suppressant 审中-公开
标题翻译： H3拮抗剂/反向激动剂与食欲抑制剂的组合
公开(公告)号：US20070142369A1
公开(公告)日：2007-06-21
申请号：US11640729
申请日：2006-12-18
申请人： Margaret van Heek , Joyce Hwa , Michael Graziano , Jean Lachowicz , Timothy Kowalski , Enrico Veltri , Kevin McCormick , Michael Berlin , Robert Aslanian
发明人： Margaret van Heek , Joyce Hwa , Michael Graziano , Jean Lachowicz , Timothy Kowalski , Enrico Veltri , Kevin McCormick , Michael Berlin , Robert Aslanian
IPC分类号： A61K31/541 , A61K31/517 , A61K31/4745 , A61K31/4192 , A61K31/428 , A61K31/496 , A61K31/5377 , A61K31/423 , A61K31/4184 , A61K31/4178
CPC分类号： A61K45/06 , A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4192 , A61K31/423 , A61K31/428 , A61K31/4745 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K2300/00
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.
摘要翻译：本发明涉及包含治疗组合的药物组合物，其包含：一种或多种H 3拮抗剂/反向激动剂; 一种或多种选自CB 1拮抗剂/反向激动剂，西布曲明，苯丁胺和托吡酯的食欲抑制剂; 和任选的一种或多种HMG-CoA还原酶抑制剂。本发明还涉及包含本发明的药物组合物的药物和试剂盒，以及使用本发明的药物组合物治疗肥胖，肥胖相关疾病和糖尿病的方法。

8. 发明授权

US09676780B2 Piperazine-substituted [1,2,4]triazolo[1,5-C]quinazolin-5-amine compounds with A2A antagonist properties 有权
公开(公告)号：US09676780B2
公开(公告)日：2017-06-13
申请号：US14655572
申请日：2013-12-20
申请人： MERCK SHARP & DOHME CORP. , Amjad Ali , Michael Man-Chu Lo , Yeon-Hee Lim , Andrew Stamford , Rongze Kuang , Paul Tempest , Younong Yu , Michael Berlin , Pauline Ting , Gang Zhou , Tao Yu , Christopher Boyce , Joseph Michael Kelly , Jayaram R. Tagat , Junying Zheng , Xianhai Huang , Wei Zhou , Jae-Hun Kim , Nicolas Zorn , Dong Xiao , Gioconda V. Gallo , Walter Won , Heping Wu , Rajan Anand , Qiaolin Deng
发明人： Amjad Ali , Michael Man-Chu Lo , Yeon-Hee Lim , Andrew Stamford , Rongze Kuang , Paul Tempest , Younong Yu , Michael Berlin , Pauline Ting , Gang Zhou , Tao Yu , Christopher Boyce , Joseph Michael Kelly , Jayaram R. Tagat , Junying Zheng , Xianhai Huang , Wei Zhou , Jae-Hun Kim , Nicolas Zorn , Dong Xiao , Gioconda V. Gallo , Walter Won , Heping Wu , Rajan Anand , Qiaolin Deng
IPC分类号： C07D487/04 , A61K31/519 , C07D487/08 , C07D487/18 , C07D513/04
CPC分类号： C07D487/04 , C07D487/08 , C07D487/18 , C07D513/04
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.

9. 发明授权

US09642746B2 Glaucoma surgery methods and systems 有权
公开(公告)号：US09642746B2
公开(公告)日：2017-05-09
申请号：US14191277
申请日：2014-02-26
申请人： Michael Berlin
发明人： Michael Berlin
IPC分类号： A61F9/007 , A61F9/008 , A61F9/00
CPC分类号： A61F9/00781 , A61F9/0017 , A61F9/00802 , A61F2009/00844 , A61F2009/00868 , A61F2009/00891
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.

10. 发明申请

US20170119579A9 Glaucoma Surgery Methods and Systems 审中-公开
公开(公告)号：US20170119579A9
公开(公告)日：2017-05-04
申请号：US14191277
申请日：2014-02-26
申请人： Michael Berlin
发明人： Michael Berlin
IPC分类号： A61F9/007 , A61F9/008 , A61F9/00
CPC分类号： A61F9/00781 , A61F9/0017 , A61F9/00802 , A61F2009/00844 , A61F2009/00868 , A61F2009/00891
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.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式