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11. 发明申请

WO2009055331A3 BICYCLIC HETEROCYCLE DERIVATIVES AND THEIR USE AS MODULATORS OF THE ACTIVITY OF GPR119 审中-公开
标题翻译：双相异构体衍生物及其作为GPR119活性调节剂的用途
公开(公告)号：WO2009055331A3
公开(公告)日：2009-07-30
申请号：PCT/US2008080462
申请日：2008-10-20
申请人： SCHERING CORP , XIA YAN , BOYLE CRAIG D , GREENLEE WILLIAM J , CHACKALAMANNIL SAMUEL , JAYNE CHARLES LEE , STAMFORD ANDREW W , DAI XING , HARRIS JOEL M , NEUSTADT BERNARD R , NEELAMKAVIL SANTHOSH FRANCIS , SHAH UNMESH G , LANKIN CLAIRE M , LIU HONG
发明人： XIA YAN , BOYLE CRAIG D , GREENLEE WILLIAM J , CHACKALAMANNIL SAMUEL , JAYNE CHARLES LEE , STAMFORD ANDREW W , DAI XING , HARRIS JOEL M , NEUSTADT BERNARD R , NEELAMKAVIL SANTHOSH FRANCIS , SHAH UNMESH G , LANKIN CLAIRE M , LIU HONG
IPC分类号： C07D401/14 , A61K31/439 , A61K31/506 , A61K31/537 , A61P3/00 , C07D451/06 , C07D471/08 , C07D487/08 , C07D491/08 , C07D495/08 , C07D498/08
CPC分类号： C07D451/06 , A61K31/439 , C07D401/14 , C07D451/14 , C07D471/08 , C07D487/08 , C07D491/08 , C07D495/08 , C07D498/08
摘要： The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
摘要翻译：本发明涉及双环杂环衍生物，包含双环杂环衍生物的组合物，以及使用双环杂环衍生物治疗或预防肥胖症，糖尿病，代谢紊乱，心血管疾病或与GPR119活性相关的病症的方法患者。

12. 发明申请

WO2009124103A3 COMBINATION THERAPIES COMPRISING PAR1 ANTAGONISTS WITH PAR4 ANTAGONISTS 审中-公开
标题翻译：包含PAR1拮抗剂与PAR4拮抗剂的组合治疗
公开(公告)号：WO2009124103A3
公开(公告)日：2010-01-14
申请号：PCT/US2009039070
申请日：2009-04-01
申请人： SCHERING CORP , XIA YAN , CHACKALAMANNIL SAMUEL
发明人： XIA YAN , CHACKALAMANNIL SAMUEL
IPC分类号： A61K31/416 , A61K31/443 , A61K31/5377 , A61K45/06 , A61P7/02 , A61P9/00 , A61P25/28 , A61P35/00
CPC分类号： A61K31/443 , A61K31/416 , A61K31/5377 , A61K45/06 , A61K2300/00
摘要： The present invention is directed to a pharmaceutical composition comprising an effective amount of at least one PAR1 antagonist, at least one PAR4 antagonist, optionally, an effective amount of at least one cardiovascular agent, and, optionally, a pharmaceutically acceptable carrier. The present invention also provides for the use of theses pharmaceutical compositions to treat various diseases associated with thrombosis.
摘要翻译：本发明涉及包含有效量的至少一种PAR1拮抗剂，至少一种PAR4拮抗剂，任选的有效量的至少一种心血管药物和任选的药学上可接受的载体的药物组合物。本发明还提供了这些药物组合物用于治疗与血栓形成相关的各种疾病的用途。

13. 发明申请

WO2005016876A3 CYCLIC AMINE BACE-1 INHIBITORS HAVING A BENZAMIDE SUBSTITUENT 审中-公开
标题翻译：具有苯甲酸替代物的循环胺BACE-1抑制剂
公开(公告)号：WO2005016876A3
公开(公告)日：2005-09-22
申请号：PCT/US2004025018
申请日：2004-08-04
申请人： SCHERING CORP , PHARMACOPEIA DRUG DISCOVERY , CUMMING JARED N , ISERLOH ULRICH , STAMFORD ANDREW , STRICKLAND COREY , VOIGT JOHANNES H , WU YUSHENG , HUANG YING , XIA YAN , CHACKALAMANNIL SAMUEL , GUO TAO , HOBBS DOUGLAS W , LE THUY X H , LOWRIE JEFFREY F , SAIONZ KURT W , BABU SURESH D
发明人： CUMMING JARED N , ISERLOH ULRICH , STAMFORD ANDREW , STRICKLAND COREY , VOIGT JOHANNES H , WU YUSHENG , HUANG YING , XIA YAN , CHACKALAMANNIL SAMUEL , GUO TAO , HOBBS DOUGLAS W , LE THUY X H , LOWRIE JEFFREY F , SAIONZ KURT W , BABU SURESH D
IPC分类号： A61K31/55 , A61K31/553 , A61K31/554 , A61K31/675 , C07D207/09 , C07D211/26 , C07D217/18 , C07D241/04 , C07D243/08 , C07D401/06 , C07D403/12 , C07D403/14 , C07D413/06 , C07F9/38 , A61K31/40 , A61K31/47 , A61K31/495 , A61K31/5355 , A61K33/42
CPC分类号： C07D243/08 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/26 , C07D209/52 , C07D211/26 , C07D211/46 , C07D217/18 , C07D233/32 , C07D241/04 , C07D241/08 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/12 , C07D403/14 , C07D409/06 , C07D409/12 , C07D413/06
摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R is-C(O)-N(R )(R ) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a beta-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, and N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
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R是-C（O）-N（R 27）（R 28）），其余的变量如说明书中所定义。还公开了包含式I化合物的药物组合物。还公开了治疗认知或神经变性疾病如阿尔茨海默病的方法。还公开了治疗认知或神经变性疾病的药物组合物和方法，其包含式I化合物与除式I以外的β-分泌酶抑制剂，HMG-CoA还原酶抑制剂，γ-分泌酶抑制剂，甾族抗炎剂和N-甲基-D-天冬氨酸受体拮抗剂，胆碱酯酶抑制剂或抗淀粉样蛋白抗体。

14. 发明申请

WO2008002596A3 ADENOSINE A2A RECEPTOR ANTAGONISTS 审中-公开
标题翻译：腺苷A2A受体拮抗剂
公开(公告)号：WO2008002596A3
公开(公告)日：2008-07-03
申请号：PCT/US2007014886
申请日：2007-06-25
申请人： SCHERING CORP , CLASBY MARTIN C , CHACKALAMANNIL SAMUEL , STAMFORD ANDREW
发明人： CLASBY MARTIN C , CHACKALAMANNIL SAMUEL , STAMFORD ANDREW
IPC分类号： C07D487/04 , A61K31/522 , A61P25/16
CPC分类号： C07D487/04
摘要： Compounds having the structural formula (I) or a pharmaceutically acceptable salt thereof, wherein: X 1 and X 2 are 1-3 substituents independently selected from the group consisting of H, alkyl, halo, -CF 3 , -OCF 3 , alkoxy, -OH and -CN; n is 0, 1 or 2; and R and R 1 are H or alkyl; also disclosed is the use of the compounds in the treatment of CNS diseases such as Parkinson's disease, alone or in combination with other agents for treating CNS diseases, pharmaceutical compositions comprising them and kits comprising the components of the combinations.
摘要翻译：具有结构式（I）的化合物或其药学上可接受的盐，其中：X 1和X 2是1-3个取代基，独立地选自H，烷基，卤素，-CF 3，-OCF 3，烷氧基，-OH和-CN; n是0,1或2; 并且R和R 1是H或烷基; 还公开了这些化合物单独或与其它治疗CNS疾病的药物一起用于治疗CNS疾病如帕金森氏病的用途，包含它们的药物组合物和包含所述组合的组分的试剂盒。

15. 发明申请

WO2009023664A3 SUBSTITUTED AZEPINE- AND DIAZEPINE-SULFONAMIDES USEFUL TO INHIBIT 11BETA-HYDROXYSTEROID DEHYDROGENASE TYPE-1 审中-公开
标题翻译：用于抑制11BetaA-羟基类固醇脱氢酶-1型的取代的氮杂环庚烯 - 和二氮嗪 - 磺酰胺
公开(公告)号：WO2009023664A3
公开(公告)日：2009-07-23
申请号：PCT/US2008072889
申请日：2008-08-12
申请人： SCHERING CORP , NEELAMKAVIL SANTHOSH , BOYLE CRAIG D , CHACKALAMANNIL SAMUEL
发明人： NEELAMKAVIL SANTHOSH , BOYLE CRAIG D , CHACKALAMANNIL SAMUEL
IPC分类号： C07D223/08 , A61K31/55 , A61K31/551 , A61P3/00 , C07D223/12 , C07D243/08 , C07D401/12 , C07D409/04
CPC分类号： C07D223/08 , C07D223/04 , C07D223/12 , C07D223/30 , C07D243/08 , C07D401/12 , C07D409/04
摘要： In its many embodiments, the present invention relates to a novel class of substituted azepine- and diazepine-sulfonamide compounds useful to inhibit 11BETA-hydroxysteroid dehydrogenase type-1, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11BETA-hydroxysteroid dehydrogenase type-1 using such compounds or pharmaceutical compositions.
摘要翻译：在其许多实施方案中，本发明涉及可用于抑制11BETA-羟基类固醇脱氢酶-1型的新类别的取代的氮杂 - 和二氮杂 - 磺酰胺化合物，含有该化合物的药物组合物，以及治疗，预防，抑制或改善与使用此类化合物或药物组合物的11BETA-羟基类固醇脱氢酶1型的表达相关的一种或多种病症。

16. 发明申请

WO2007075809A2 OXAZOLOISOQUINOLINE DERIVATIVES AS THROMBIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：氧杂氮杂环丁酮衍生物作为硫蛋白受体拮抗剂
公开(公告)号：WO2007075809A2
公开(公告)日：2007-07-05
申请号：PCT/US2006048646
申请日：2006-12-20
申请人： SCHERING CORP , CHACKALAMANNIL SAMUEL , WANG YUGUANG
发明人： CHACKALAMANNIL SAMUEL , WANG YUGUANG
CPC分类号： C07D487/04 , C07D471/04
摘要： Heterocyclic-substituted bi or tricyclics of the formula (I) or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein An, Mn, Un, Gn, Jn, Kn, R9, R10, R11, R32, R33, B and Het are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
摘要翻译：式（I）的杂环取代的二环或三环或所述化合物，异构体或外消旋混合物的药学上可接受的盐或溶剂合物，其中代表任选的双键，虚线任选是键或无键，得到双键或单价键，如价格要求所允许的，其中An，Mn，Un，Gn，Jn，Kn，R9，R10，R11，R32，R33，B和Het在本文中定义，其余取代基如说明书以及含有它们的药物组合物以及通过施用所述化合物治疗与血栓形成，动脉粥样硬化，再狭窄，高血压，心绞痛，心律失常，心力衰竭和癌症相关的疾病的方法。还要求与其它心血管药物联合治疗。

17. 发明申请

WO2006068954A3 PYRAZOLO[1,5-A]PYRIMIDINE ADENOSINE A2a RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯并[1,5-A]吡嗪酮腺苷A2a受体拮抗剂
公开(公告)号：WO2006068954A3
公开(公告)日：2006-12-07
申请号：PCT/US2005045658
申请日：2005-12-19
申请人： SCHERING CORP , CLASBY MARTIN C , CHACKALAMANNIL SAMUEL , NEUSTADT BERNARD R , GAO XIAOBANG
发明人： CLASBY MARTIN C , CHACKALAMANNIL SAMUEL , NEUSTADT BERNARD R , GAO XIAOBANG
IPC分类号： C07D487/04 , A61K31/519 , A61P25/00 , A61P25/16 , A61P25/18
CPC分类号： C07D487/04
摘要： Compounds having the structural formula (I) are disclosed, wherein A is alkylene, or optionally substituted arylene, cycloalkylene or heteroaryldiyl; X is -C(O)- or -S(O) 2 -; R 1 is alkyl or cycloalkyl; R 2 is hydrogen, halo or -CN; R 3 is hydrogen or alkyl; R 4 is hydrogen, alkyl, alkoxy, hydroxyalkyl, aminoalkyl-, cycloalkyl, heterocycloalkyl, heterocycloalkyl substituted by alkyl, optionally substituted arylalkyl or optionally substituted heteroarylalkyl; or R 3 and R 4 , form an optionally substituted 5-7 membered ring, said ring optionally comprising an additional heteroatom ring member; R 7 is alkyl, optionally substituted phenyl, optionally substituted heteroaryl, cycloalkyl, halo, morpholinyl, optionally substituted piperazinyl, or optionally substituted azacycloalkyl. Also disclosed is the use of the compounds in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations.
摘要翻译：公开了具有结构式（I）的化合物，其中A是亚烷基或任选取代的亚芳基，亚环烷基或杂芳基二基; X是-C（O） - 或-S（O）2 - 。 R 1是烷基或环烷基; R 2是氢，卤素或-CN; R 3是氢或烷基; R 4是氢，烷基，烷氧基，羟基烷基，氨基烷基 - ，环烷基，杂环烷基，被烷基，任选取代的芳基烷基或任选取代的杂芳基烷基取代的杂环烷基; 或R 3和R 4，形成任选取代的5-7元环，所述环任选地包含另外的杂原子环成员; R 7是烷基，任选取代的苯基，任选取代的杂芳基，环烷基，卤素，吗啉基，任选取代的哌嗪基或任选取代的氮杂环烷基。还公开了化合物在治疗帕金森病中的用途，单独或与其他治疗帕金森病的药物组合，包含它们的药物组合物和包含组合组分的试剂盒的用途。

18. 发明申请

WO2008060372A3 THROMBIN RECEPTOR ANTAGONISTS BASED ON THE MODIFIED TRICYCLIC UNIT OF HIMBACINE 审中-公开
标题翻译：基于改性三聚体单元的血红蛋白受体拮抗剂
公开(公告)号：WO2008060372A3
公开(公告)日：2008-12-24
申请号：PCT/US2007021259
申请日：2007-10-02
申请人： SCHERING CORP , CHACKALAMANNIL SAMUEL , WANG YUGUANG , THIRUVENGADAM TIRUVETTIPURAM K , ZAVIALOV ILIA A , LI TAO
发明人： CHACKALAMANNIL SAMUEL , WANG YUGUANG , THIRUVENGADAM TIRUVETTIPURAM K , ZAVIALOV ILIA A , LI TAO
IPC分类号： C07D405/06 , A61K31/443 , A61P9/00 , A61P11/00 , A61P25/00 , A61P29/00 , A61P35/00
CPC分类号： C07D405/06
摘要： Multiple stereoisomers of the heterocyclic-substituted tricyclics of the formula: or a pharmaceutically acceptable salt, solvate, or ester of said compound wherein R and the stereochemistry are illustrated in the structural formulas herein are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
摘要翻译：公开了下式结构式中R和立体化学结构式所示的化合物或其药学上可接受的盐，溶剂化物或酯的立体异构体：以及含有它们的药物组合物和方法通过施用所述化合物治疗与血栓形成，动脉粥样硬化，再狭窄，高血压，心绞痛，心律失常，心力衰竭和癌症相关的疾病。还要求与其它心血管药物联合治疗。

19. 发明申请

WO2007123949A2 CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译： CANNABINOID受体调节剂
公开(公告)号：WO2007123949A2
公开(公告)日：2007-11-01
申请号：PCT/US2007009473
申请日：2007-04-18
申请人： SCHERING CORP , WANG YUGUANG , CHACKALAMANNIL SAMUEL , ROOT YURIKO Y
发明人： WANG YUGUANG , CHACKALAMANNIL SAMUEL , ROOT YURIKO Y
IPC分类号： C07C43/225 , C07C255/54 , C07C255/58
CPC分类号： A61K31/03 , A61K31/10 , C07C43/225 , C07C255/54 , C07C255/58 , C07C2601/08
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable salts or solvates thereof, wherein: Ar 1 is a chlorophenyl group, Ar 2 is a dichlorophenyl group, R 1 is a -(CH 2 )m-X-(CH 2 )n-R 2 group, X is a -NH-, -O-, -C(O)- or -S(O) 2 - group, and R 2 is a substituted phenyl group. These compounds are CB1 receptor modulators. Also disclosed are methods of treating CB1 modulated diseases or conditions such as the metabolic syndrome.
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：Ar 1是氯苯基，Ar 2是二氯苯基， 1是 - （CH 2）2 mX-（CH 2）nR 2 O 2基团，X是-NH-， -O - ， - C（O） - 或-S（O）2 - 基，R 2是取代的苯基。这些化合物是CB1受体调节剂。还公开了治疗CB1调节的疾病或诸如代谢综合征的病症的方法。

20. 发明申请

WO2004094431A3 2-ALKYNYL-AND 2-ALKENYL-PYRAZOLO-[4,3-E]-1,2,4-TRIAZOLO-[1,5-C]-PYRIMIDINE ADENOSINE A2A RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 2-炔基 - 和2-烷基 - 吡唑并[4,3-E] -1,2,4-三氮唑 - [1,5-C] - 嘧啶腺苷A2A受体拮抗剂
公开(公告)号：WO2004094431A3
公开(公告)日：2004-12-02
申请号：PCT/US2004012471
申请日：2004-04-21
申请人： SCHERING CORP , NEUSTADT BERNARD R , HAO JINSONG , LIU HONG , BOYLE CRAIG D , CHACKALAMANNIL SAMUEL , SHAH UNMESH G , STAMFORD ANDREW
发明人： NEUSTADT BERNARD R , HAO JINSONG , LIU HONG , BOYLE CRAIG D , CHACKALAMANNIL SAMUEL , SHAH UNMESH G , STAMFORD ANDREW
IPC分类号： A61P25/16 , C07D487/14 , A61K31/519
CPC分类号： C07D487/14
摘要： Compounds having the structural formula (I) or a pharmaceutically acceptable salt thereof, wherein R is R R , R , R and R are H, alkyl or alkoxyalkyl; R is H, alkyl, hydroxyalkyl or -CH2F; R , R and R are H, alkyl, alkoxy, alkylthio, alkoxyalkyl, halo or -CF3; and Z is optionally substituted aryl, heteroaryl or heteroaryl-alkyl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
摘要翻译：具有结构式（I）的化合物或其药学上可接受的盐，其中R为R 1，R 2，R 3，R 4和R 5为H，烷基或烷氧基烷基; R 6是H，烷基，羟烷基或-CH 2 F; R 7，R 8和R 9为H，烷基，烷氧基，烷硫基，烷氧基烷基，卤素或-CF 3; Z是任选取代的芳基，杂芳基或杂芳基 - 烷基。还公开了式I化合物在治疗中枢神经系统疾病，特别是帕金森病中的用途，其单独或与用于治疗帕金森病的其他药剂组合使用，以及包含它们的药物组合物。

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