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1. 发明申请

WO2008103351A3 HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译：异源ASPARTYL蛋白酶抑制剂
公开(公告)号：WO2008103351A3
公开(公告)日：2009-07-23
申请号：PCT/US2008002182
申请日：2008-02-20
申请人： SCHERING CORP , PHARMACOPEIA INC , ZHU ZHAONING , MCKITTRICK BRIAN , SUN ZHONG-YUE , YE YUANZAN C , VOIGT JOHANNES H , STRICKLAND COREY , SMITH ELIZABETH M , STAMFORD ANDREW , GREENLEE WILLIAM J , MAZZOLA JR ROBERT D , CALDWELL JOHN , CUMMING JARED N , WANG LINGYAN , WU YUSHENG , ISERLOH ULRICH , LIU XIAOXIANG , HUANG YING , LI GUOQING , PAN JIANPING , MISIASZEK JEFFREY A , GUO TAO , LE THUY X H , SAIONZ KURT W , BABU SURESH D , HUNTER RACHAEL C , MORRIS MICHELLE L , GU HUIZHONG , QIAN GANG , TADESSE DAWIT , LAI GAIFA , DUO JINGQI , QU CHUANXING , SHAO YUEFEI
发明人： ZHU ZHAONING , MCKITTRICK BRIAN , SUN ZHONG-YUE , YE YUANZAN C , VOIGT JOHANNES H , STRICKLAND COREY , SMITH ELIZABETH M , STAMFORD ANDREW , GREENLEE WILLIAM J , MAZZOLA JR ROBERT D , CALDWELL JOHN , CUMMING JARED N , WANG LINGYAN , WU YUSHENG , ISERLOH ULRICH , LIU XIAOXIANG , HUANG YING , LI GUOQING , PAN JIANPING , MISIASZEK JEFFREY A , GUO TAO , LE THUY X H , SAIONZ KURT W , BABU SURESH D , HUNTER RACHAEL C , MORRIS MICHELLE L , GU HUIZHONG , QIAN GANG , TADESSE DAWIT , LAI GAIFA , DUO JINGQI , QU CHUANXING , SHAO YUEFEI
IPC分类号： C07D233/88 , A61K31/513 , A61P25/28 , C07D239/22 , C07D401/06 , C07D401/10 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/10 , C07D417/14 , C07D495/10
CPC分类号： C07D233/88 , A61K31/4168 , A61K31/4178 , C07D239/22 , C07D401/06 , C07D401/10 , C07D403/06 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/10 , C07D417/14 , C07D495/10
摘要： Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, -C(=S)-, -S(O)-, -S(O)2-, -C(=O)-, -O-, -C(R6)(R7)-, -N(R5)- or -C(=N(R5))-; X is -O-, -N(R5)- or -C(R6)(R7)-; provided that when X is -O-, U is not -O-, -S(O)-, -S(O)2-, -C(=O)- or -C(=NR5)-; U is a bond, -S(O)-, -S(O)2-, -C(O)-, -O-, -P(O)(OR15)-, -C(=NR5)-, -(C(R6)(R7))b- or -N(R5)-; wherein b is 1 or 2; provided that when W is -S(O)-, -S(O)2-, -O-, or -N(R5)-, U is not -S(O)-, -S(O)2-, -O-, or -N(R5)-; provided that when X is -N(R5)- and W is -S(O)-, -S(O)2-, -O-, or -N(R5)-, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula (I). Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
摘要翻译：公开了式（I）化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂合物，其中W是一个键，-C（= S） - ， - S（O） - ， - S（O） - ， - （= O） - ， - O - ， - C（R6）（R7） - ， - N（R5） - 或-C（= N（R5） X是-O - ， - N（R 5） - 或-C（R 6）（R 7） - ; 条件是当X是-O-时，U不是-O-，-S（O） - ， - S（O）2 - ， - C（= O） - 或-C（= NR5） - ; U是一个键，-S（O） - ， - S（O）2 - ， - C（O） - ， - O - ， - O（OR）（C（R6）（R7））b-或-N（R5） - ; 其中b为1或2; 条件是当W是-S（O） - ， - S（O）2 - ， - O-或-N（R 5） - 时，U不是-S（O） - ， - S（O） -O-或-N（R 5） - ; 条件是当X为-N（R5） - 且W为-S（O） - ， - S（O）2 - ， - O-或-N（R5） - 时，则U不为键; 并且R1，R2，R3，R4，R5，R6和R7如说明书中所定义; 和包含式（I）化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经退行性疾病的方法，以及抑制人类免疫缺陷病毒，plasmepins，组织蛋白酶D和原生动物酶的方法。还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱m1激动剂或m2拮抗剂组合治疗认知或神经变性疾病的方法。

2. 发明申请

WO2006065277A3 HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译：异源ASPARTYL蛋白酶抑制剂
公开(公告)号：WO2006065277A3
公开(公告)日：2007-01-25
申请号：PCT/US2005020446
申请日：2005-06-09
申请人： SCHERING CORP , PHARMACOPEIA DRUG DISCOVERY , ZHU ZHAONING , MCKITTRICK BRIAN , SUN ZHONG-YUE , YE YUANZAN C , VOIGT JOHANNES H , STRICKLAND COREY , SMITH ELIZABETH M , STAMFORD ANDREW , GREENLEE WILLIAM J , MAZZOLA ROBERT , CALDWELL JOHN , CUMMING JARED , WANG LINGYAN , WU YUSHENG , ISERLOH ULRICH , GUO TAO , LE THUY X H , SAIONZ KURT W , BABU SURESH D , HUNTER RACHAEL C , MORRIS MICHELLE L , GU HUIZHONG , QIAN GANG , TADESSE DAWIT
发明人： ZHU ZHAONING , MCKITTRICK BRIAN , SUN ZHONG-YUE , YE YUANZAN C , VOIGT JOHANNES H , STRICKLAND COREY , SMITH ELIZABETH M , STAMFORD ANDREW , GREENLEE WILLIAM J , MAZZOLA ROBERT , CALDWELL JOHN , CUMMING JARED , WANG LINGYAN , WU YUSHENG , ISERLOH ULRICH , GUO TAO , LE THUY X H , SAIONZ KURT W , BABU SURESH D , HUNTER RACHAEL C , MORRIS MICHELLE L , GU HUIZHONG , QIAN GANG , TADESSE DAWIT
IPC分类号： A61K31/4168 , A61K31/4178 , C07D233/46 , C07D233/88 , C07D239/22 , C07D271/06 , C07D273/00 , C07D401/10 , C07D403/06 , C07D403/12 , C07D407/10 , C07D409/04 , C07D409/14 , C07D413/10 , C07D413/12
CPC分类号： C07D233/88 , A61K31/4168 , A61K31/4178 , A61K31/4184 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/5377 , A61K31/655 , A61K45/06 , C07D233/46 , C07D233/70 , C07D235/02 , C07D239/22 , C07D239/70 , C07D271/07 , C07D273/00 , C07D295/15 , C07D401/04 , C07D401/06 , C07D401/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/10 , C07D403/12 , C07D405/06 , C07D405/10 , C07D405/14 , C07D407/06 , C07D409/04 , C07D409/06 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/06
摘要： Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, and pharmaceutical compositions comprising the compounds of formula (I). Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula (I) in combination with a cholinesterase inhibitor or a muscarinic m 1 agonist or m 2 antagonist.
摘要翻译：公开了式（I）的化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂合物，以及包含式（I）化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经变性疾病的方法，以及抑制人类免疫缺陷病毒，plasmepins，组织蛋白酶D和原生动物酶的方法。还公开了使用式（I）化合物与胆碱酯酶抑制剂或毒蕈碱m 1激动剂或m 2 H 2拮抗剂组合来治疗认知或神经退行性疾病的方法。

3. 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。

4. 发明申请

WO2006138264A3 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2006138264A3
公开(公告)日：2007-03-01
申请号：PCT/US2006022918
申请日：2006-06-12
申请人： SCHERING CORP , ZHU ZHAONING , MCKITTRICK BRIAN , STAMFORD ANDREW , GREENLEE WILLIAM J , LIU XIAOXIANG , MANDAL MIHIRBARAN , VOIGT JOHANNES H , STRICKLAND COREY
发明人： ZHU ZHAONING , MCKITTRICK BRIAN , STAMFORD ANDREW , GREENLEE WILLIAM J , LIU XIAOXIANG , MANDAL MIHIRBARAN , VOIGT JOHANNES H , STRICKLAND COREY
IPC分类号： C07D487/04 , A61K31/519 , A61P25/28
CPC分类号： C07D487/04
摘要： Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein j, k, U, W, R, R 1 , R 2 , R 3 , R 4 , R 6 , R 7 and R 7a are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula (I) in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m 2 antagonist.
摘要翻译：公开了式（I）化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂化物，其中j，k，U，W，R，R 1，R 2， R 3，R 4，R 4，R 6，R 7和R 7， / SUP>如上文在说明书中所述。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经变性疾病的方法。还公开了使用式（I）化合物与胆碱酯酶抑制剂或毒蕈碱m1激动剂或m 2拮抗剂组合治疗认知或神经变性疾病的方法。

5. 发明申请

WO2010056630A8 TRIAZOLOPYRIMIDINONES AND METHODS OF USE THEREOF 审中-公开
标题翻译：三唑并嘧啶酮及其使用方法
公开(公告)号：WO2010056630A8
公开(公告)日：2011-01-27
申请号：PCT/US2009063786
申请日：2009-11-10
申请人： SCHERING CORP , SHIPPS GERALD W JR , ORTH PETER , VOIGT JOHANNES H
发明人： SHIPPS GERALD W JR , ORTH PETER , VOIGT JOHANNES H
IPC分类号： A61K31/522 , A61P3/04 , A61P9/00
CPC分类号： A61K31/522
摘要： The present invention discloses a method of treating a cardiovascular disease or condition comprising administering therapeutically effective amounts of certain triazolopyrimidinones as Fatty Acid Binding Protein ("FABP") inhibitors. Examples of such disease or condition include metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative inventive method to treat the above-noted conditions uses the administration of the compound shown below: (I)
摘要翻译：本发明公开了一种治疗心血管疾病或病症的方法，包括给予治疗有效量的某些三唑并嘧啶酮作为脂肪酸结合蛋白（“FABP”）抑制剂。这种疾病或病症的实例包括代谢紊乱，肥胖或肥胖相关疾病，糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。用于治疗上述病症的说明性发明方法使用下列化合物的施用：（I）

6. 发明申请

WO2004003005A3 SH2 DOMAIN BINDING INHIBITORS 审中-公开
标题翻译： SH2域绑定抑制剂
公开(公告)号：WO2004003005A3
公开(公告)日：2007-02-01
申请号：PCT/US0319987
申请日：2003-06-26
申请人： US GOV HEALTH & HUMAN SERV , BURKE TERRENCE R JR , WEI CHANG-QING , VOIGT JOHANNES H , SHI ZHEN-DAN , GAO YANG
发明人： BURKE TERRENCE R JR , WEI CHANG-QING , VOIGT JOHANNES H , SHI ZHEN-DAN , GAO YANG
IPC分类号： A61K38/12 , A61K38/00 , A61K38/02 , A61K38/05 , A61K38/06 , A61K38/08 , A61P35/00 , C07C211/30 , C07F9/40 , C07K1/00 , C07K1/04 , C07K1/06 , C07K1/14 , C07K5/06 , C07K5/08 , C07K5/12 , C07K7/04 , C07K7/56 , G01N33/68
CPC分类号： C07K5/06191 , A61K38/00 , C07K5/0827 , C07K5/123 , C07K5/126 , C07K7/56
摘要： Disclosed are compounds for SH2 domain binding inhibition, for example, a compound of formula (I), wherein R 1 is a lipophile; R 2 , in combination with the phenyl ring, is a phenylphosphate mimic group or a protected phenylphosphate mimic group; R 3 is hydrogen, azido, amino, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, or alkylcarbonylamino, wherein the alkyl portion of R 3 may be optionally substituted with a substituent selected from the group consisting of halo, hydroxy, carboxyl, amino, aminoalkyl, alkyl, alkoxy, and keto; R 6 is a linker; AA is an amino acid; and n is 1 to 6; or a salt thereof. The conformationally compounds provide enhanced binding affinity with SH2 domain protein. Also disclosed are a pharmaceutical compositions and a method for inhibiting an SH2 domain from binding with a phosphoprotein.
摘要翻译：公开了用于SH2结构域结合抑制的化合物，例如式（I）的化合物，其中R 1是亲脂体; R 2与苯环组合是苯基磷酸酯模拟基团或被保护的苯基磷酸酯模拟基团; R 3是氢，叠氮基，氨基，羧基烷基，烷氧基羰基烷基，氨基羰基烷基或烷基羰基氨基，其中R 3的烷基部分可以任选地被选自由卤素，羟基，羧基，氨基，氨基烷基，烷基，烷氧基和酮基组成; R 6是连接体; AA是氨基酸; n为1〜6; 或其盐。构象化合物提供与SH2结构域蛋白质增强的结合亲和力。还公开了用于抑制SH2结构域与磷蛋白结合的药物组合物和方法。

7. 发明申请

WO0216407A3 SH2 DOMAIN BINDING INHIBITORS 审中-公开
标题翻译： SH2域绑定抑制剂
公开(公告)号：WO0216407A3
公开(公告)日：2003-11-20
申请号：PCT/US0126078
申请日：2001-08-22
申请人： US GOV HEALTH & HUMAN SERV , BURKE TERRENCE R JR , WEI CHANG-QING , VOIGT JOHANNES H , GAO YANG
发明人： BURKE TERRENCE R JR , WEI CHANG-QING , VOIGT JOHANNES H , GAO YANG
IPC分类号： A61K38/00 , A61P35/00 , C07K5/06 , C07K5/065 , C07K5/08 , A61K38/05 , A61K38/06 , C07C211/30 , C07F9/40 , C07K5/087 , G01N33/68
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/06191 , C07K5/0827
摘要： Disclosed are compounds for SH2 domain binding inhibition. For example, disclosed is a compound of formula (I) wherein R1 is a lipophile; R2, in combination with the phenyl ring, is a phenylphosphate mimic group or a protected phenylphosphate mimic group; R3 is hydrogen, azido, amino, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, or alkylcarbonylamino, wherein the alkyl portion of R3 may be optionally substituted with a substituent selected from the group consisting of halo, hydroxy, carboxyl, amino, aminoalkyl, alkyl, alkoxy, and keto; R6 is a linker; AA is an amino acid; and n is 1 to 6; or a salt thereof. The compounds of the present invention have the advantage that their conformation is constrained to provide enhanced binding affinity with SH2 domain protein. Also disclosed are a pharmaceutical composition comprising a pharmaceutically or pharmacologically acceptable carrier and a compound of the present invention, a method for inhibiting an SH2 domain from binding with a phosphoprotein comprising contacting an SH2 domain with a compound of the present invention, a method of preventing or treating a disease, state, or condition by the use of one or more of these compounds, and a method for preparing the compounds of the present invention. The present invention further provides intermediates useful in the preparation of the compounds.
摘要翻译：公开了用于SH2结构域结合抑制的化合物。例如，公开了式（I）的化合物，其中R 1是亲油体; R2与苯环组合是苯基磷酸酯模拟基团或被保护的苯基磷酸酯模拟基团; R 3是氢，叠氮基，氨基，羧基烷基，烷氧基羰基烷基，氨基羰基烷基或烷基羰基氨基，其中R3的烷基部分可以任选地被选自卤素，羟基，羧基，氨基，氨基烷基，烷基，烷氧基，和酮 R6是连接体; AA是氨基酸; n为1〜6; 或其盐。本发明的化合物具有这样的优点：它们的构象被限制以提供与SH2结构域蛋白质的增强的结合亲和力。还公开了包含药学上可接受的载体和本发明化合物的药物组合物，一种抑制SH2结构域与磷蛋白结合的方法，包括使SH2结构域与本发明的化合物接触，一种预防或通过使用一种或多种这些化合物治疗疾病，状态或病症，以及制备本发明化合物的方法。本发明还提供可用于制备化合物的中间体。

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