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1. 发明申请

WO0047568A3 1,2-BENZOTHIAZEPINES FOR THE TREATMENT OF HYPERLIPIDEMIC DISEASES 审中-公开
标题翻译：用于治疗高致病性疾病的1,2-苯二氮
公开(公告)号：WO0047568A3
公开(公告)日：2000-12-14
申请号：PCT/US0002503
申请日：2000-02-10
申请人： SEARLE & CO , TOLLEFSON MICHAEL B , KOLODZIEJ STEVE A , REITZ DAVID B
发明人： TOLLEFSON MICHAEL B , KOLODZIEJ STEVE A , REITZ DAVID B
IPC分类号： A61K31/554 , A61P3/06 , A61P9/10 , C07D281/02 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D521/00 , C07F9/36 , C07F9/38 , C07F9/54 , A61K31/55
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D281/02 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07F9/36 , C07F9/3808 , C07F9/5407
摘要： Novel 1,1-dioxido-1,2-benzothiazepines, derivatives and analogs thereof, pharmaceutical compositions containing them, and their use in medicine, particularly in the prophylaxis and/or treatment of hyperlipidemic diseases, conditions and/or disorders, such as those associated with atherosclerosis and/or hypercholesterolemia.
摘要翻译：新的1,1-二氧化-1,2-苯并硫氮杂，其衍生物和类似物，含有它们的药物组合物及其在药物中的用途，特别是用于预防和/或治疗高脂血症，病症和/或病症，例如与动脉粥样硬化和/或高胆固醇血症相关。

2. 发明申请

WO0001687A9 BENZOTHIEPINES HAVING ACTIVITY AS INHIBITORS OF ILEAL BILE ACID TRANSPORT AND TAUROCHOLATE UPTAKE 审中-公开
标题翻译：具有作为ILEAL BILE ACID TRACSPORT和TAUROCHOLATE摄取的抑制剂的活性的BENZOTHIEPINES
公开(公告)号：WO0001687A9
公开(公告)日：2000-07-20
申请号：PCT/US9912828
申请日：1999-06-29
申请人： SEARLE & CO , LEE LEN F , BANERJEE SHYAMAL C , HUANG HORNG CHIH , LI JINGLIN J , MILLER RAYMOND E , REITZ DAVID B , TREMONT SAMUEL J
发明人： LEE LEN F , BANERJEE SHYAMAL C , HUANG HORNG-CHIH , LI JINGLIN J , MILLER RAYMOND E , REITZ DAVID B , TREMONT SAMUEL J
IPC分类号： A61K31/00 , A61K31/38 , A61K31/4035 , A61K31/41 , A61K31/4178 , A61K31/4433 , A61K31/4436 , A61K31/4709 , A61K31/4995 , A61K31/662 , A61K31/67 , A61P1/16 , A61P3/06 , A61P9/10 , A61P43/00 , C07B53/00 , C07C319/14 , C07C323/12 , C07C323/18 , C07C323/19 , C07D337/06 , C07D337/08 , C07D409/10 , C07D409/12 , C07D487/08 , C07D495/04 , C07D495/10 , C07F9/653 , C07F9/6553 , C07K5/06 , C07K5/068 , C08G65/329
CPC分类号： A61K31/38 , C07C319/14 , C07D337/06 , C07D337/08 , C07D409/10 , C07D409/12 , C07D487/08 , C07D495/04 , C07D495/10 , C07F9/65539 , C07K5/06086 , C08G65/329 , C07C323/12 , C07C323/18
摘要： Novel benzothiepines, derivatives, and analogs thereof; methods of preparing such compounds; pharmaceutical compositions containing such compounds; and methods of using these compounds and compositions in the preparation of a medicament, particularly medicaments for use in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.
摘要翻译：新的苯并噻庚因衍生物及其类似物; 制备这些化合物的方法; 含有这些化合物的药物组合物; 以及使用这些化合物和组合物制备药物，特别是用于预防和治疗哺乳动物中与高血脂症状相关的高脂血症或与高胆固醇血症有关的药物的方法。

3. 发明申请

WO9840375A2 COMBINATION THERAPY EMPLOYING ILEAL BILE ACID TRANSPORT INHIBITING BENZOTHIEPINES AND HMG Co-A REDUCTASE INHIBITORS 审中-公开
标题翻译：联合治疗使用ILEAL BILE ACID运输抑制苯扎硫酯和HMG联合还原酶抑制剂
公开(公告)号：WO9840375A2
公开(公告)日：1998-09-17
申请号：PCT/US9803792
申请日：1998-03-10
申请人： SEARLE & CO , REITZ DAVID B , LEE LEN F , LI JINGLIN J , HUANG HORNG CHIH , TREMONT SAMUEL J , MILLER RAYMOND E , BANERIEE SHYAMAL C , MANNING ROBERT E , GLENN KEVIN C , KELLER BRADLEY T
发明人： REITZ DAVID B , LEE LEN F , LI JINGLIN J , HUANG HORNG-CHIH , TREMONT SAMUEL J , MILLER RAYMOND E , BANERIEE SHYAMAL C , MANNING ROBERT E , GLENN KEVIN C , KELLER BRADLEY T
IPC分类号： C07D337/08 , A61K31/19 , A61K31/22 , A61K31/366 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/4025 , A61K31/4035 , A61K31/405 , A61K31/4178 , A61K31/437 , A61K31/4375 , A61K31/4436 , A61K31/4709 , A61K31/4725 , A61K31/473 , A61K31/496 , A61K31/498 , A61K31/4995 , A61K31/502 , A61K31/5377 , A61K31/55 , A61K31/67 , A61K45/06 , A61P3/06 , C07D409/04 , C07D409/10 , C07D409/12 , C07D409/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D337/00
CPC分类号： A61K45/06 , A61K31/22 , A61K31/366 , A61K31/405 , A61K2300/00
摘要： Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals. Also provided are compositions and methods for combination therapy employing ileal bile acid transport inhibitors and HMG Co-A reductase inhibitors for the treatment of hyperlipidemic conditions.
摘要翻译：提供了新的苯并噻庚因，衍生物和类似物; 含有它们的药物组合物; 以及在医学中使用这些化合物和组合物的方法，特别是用于预防和治疗哺乳动物中高脂血症的疾病，例如与动脉粥样硬化或高胆固醇血症有关的那些。还提供了使用回肠胆汁酸转运抑制剂和HMG Co-A还原酶抑制剂联合治疗高脂血症的组合物和方法。

4. 发明申请

WO9218092A3 I-arylheteroarylalkyl substituted-1h-1,2,4-triazo le compounds for treatment of circulatory disorders 审中-公开
标题翻译：用于治疗循环系统疾病的1-芳基杂芳基烷基取代的-1h-1,2,4-三唑类化合物
公开(公告)号：WO9218092A3
公开(公告)日：1992-12-10
申请号：PCT/US9202801
申请日：1992-04-10
申请人： SEARLE & CO , REITZ DAVID B
发明人： REITZ DAVID B
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/4439 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P9/12 , C07D401/06 , C07D401/10 , C07D401/14 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/10 , C07D401/14
摘要： A class of 1-arylheteroarylalkyl substituted-1H-1,2,4-triazole compounds is described for use in treatment of circulatory disorders such as hypertension. Compounds of particular interest are angiotensin II antagonists of the formula (I) wherein A is selected from (1, 2, 3, 4, 5 and 6), wherein m is one; wherein R1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, phenyl, benzyl, phenethyl, 2-ethylbutyl, 1,1-difluorobutyl, N-methylamido, N-methyl-N-tertbutylamido, 2-methylphenyl, 2-isopropylphenyl, 2-methoxyphenyl, 2-chlorophenyl, 2,6-difluorophenyl, cyclohexyl, cyclohexylmethyl, 2-butenyl, 3-butenyl, 2-butynyl, 3-butynyl and 2-hydroxybutyl; wherein R2 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, ethylbutyl, n-pentyl, 1-oxo-2-phenylethyl, 1-oxo-2-cyclohexylethyl, 1,1-difluoro-2-phenylethyl, 1,1-difluoro-2-cyclohexylethyl, 2-cyclohexylethyl, 1,1-difluoro-3-cyclohexylpropyl, 1,1-dimethoxybutyl, 1,1-difluoroethyl, 1,1-difluoropropyl, 1,1-difluorobutyl, 1,1-difluoropentyl, phenyl, benzyl, 2-phenylethyl, 1,1-difluoro-3-phenylpropyl, cyclohexylmethyl, cyclohexanoyl, N-methylamido, N-methyl-N-tertbutylamido, 2-methylphenyl, 2-isopropylphenyl, 2-methoxyphenyl, 2-chlorophenyl, 2,6-difluorophenyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-butynyl, 2-butynyl, 3-butynyl, propylthio and buthylthio; wherein R5 is an acidic group selected from CO¿2?H and tetrazole radicals; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.

5. 发明申请

WO0242272A8 SUBSTITUTED POLYCYCLIC ARYL AND HETEROARYL PYRIDINES USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开
标题翻译：用于选择性抑制凝聚剂CASCADE的取代的多环芳烃和异丁基吡啶
公开(公告)号：WO0242272A8
公开(公告)日：2003-10-23
申请号：PCT/US0143280
申请日：2001-11-20
申请人： PHARMACIA CORP , SOUTH MICHAEL S , CASE BRENDA , GARLAND DANNY J , HAYES MICHAEL J , HUANG HORNG-CHIH , HUANG WEI , JONES DARIN E , NEUMANN WILLIAM L , PARLOW JOHN J , REITZ DAVID B , RUEPPEL MELVIN L , WEBBER RONALD K
发明人： SOUTH MICHAEL S , CASE BRENDA , GARLAND DANNY J , HAYES MICHAEL J , HUANG HORNG-CHIH , HUANG WEI , JONES DARIN E , NEUMANN WILLIAM L , PARLOW JOHN J , REITZ DAVID B , RUEPPEL MELVIN L , WEBBER RONALD K
IPC分类号： A61K31/44 , A61K31/4418 , A61K31/4436 , A61K31/4439 , A61K45/00 , A61P7/02 , A61P9/10 , A61P11/00 , A61P35/00 , A61P43/00 , C07D213/74 , C07D213/89 , C07D401/10 , C07D409/04 , C07D213/77 , C07D213/90 , C07D237/20 , C07D239/36 , C07D239/42 , C07D241/20 , C07D253/04 , C07D253/06 , C07D265/02 , C07D417/12
CPC分类号： C07D213/74 , C07D213/89
摘要： The present invention relates to compounds, and prodrugs thereof, composition and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.
摘要翻译：本发明涉及化合物及其前药，可用于预防和治疗哺乳动物血栓形成病症的组合物和方法。本发明的化合物及其前药选择性地抑制凝血级联的某些蛋白酶。

6. 发明申请

WO2005009370A3 BETA-CARBOLINE COMPOUNDS AND ANALOGUES THEREOF AND THEIR USE AS MITOGEN-ACTIVATED PROTEIN KINASE-ACTIVATED PROTEIN KINASE-2 INHIBITORS 审中-公开
标题翻译： β-环糊精化合物及其类似物及其用作活化蛋白激酶的蛋白激酶蛋白激酶-2抑制剂
公开(公告)号：WO2005009370A3
公开(公告)日：2005-10-20
申请号：PCT/US2004023350
申请日：2004-07-22
申请人： PHARMACIA CORP , MEYERS MARVIN J , TRUJILLO JOHN I , VERNIER WILLIAM F , ANDERSON DAVID R , REITZ DAVID B , BUCHLER INGRID P , HEGDE SHRIDHAR G , MAHONEY MATTHEW W , WU KUN K
发明人： MEYERS MARVIN J , TRUJILLO JOHN I , VERNIER WILLIAM F , ANDERSON DAVID R , REITZ DAVID B , BUCHLER INGRID P , HEGDE SHRIDHAR G , MAHONEY MATTHEW W , WU KUN K
IPC分类号： A61K20060101 , A61K31/40 , A61K31/403 , A61K31/407 , A61K31/4745 , A61K31/55 , C07D209/82 , C07D209/94 , C07D471/02 , C07D471/14
CPC分类号： A61K31/40 , C07D471/04 , C07D471/14 , C07D471/18
摘要： Novel methods and compositions are described for inhibiting mitogen activated protein kinase-activated protein kinase-2 in a subject. The method involves administering to the subject a beta-carboline MK-2 inhibiting compound, or a pharmaceutically acceptable salt, or isomer thereof. The novel compositions are capable of inhibiting mitogen activated protein kinase-activated protein kinase-2 and analogues thereof. Pharmaceutical compositions and kits that include these compounds are also described.
摘要翻译：描述了用于抑制受试者中丝裂原活化蛋白激酶激活蛋白激酶-2的新方法和组合物。该方法包括给受试者施用β-咔啉MK-2抑制化合物或其药学上可接受的盐或其异构体。新型组合物能够抑制丝裂原活化蛋白激酶活化蛋白激酶-2及其类似物。还描述了包括这些化合物的药物组合物和试剂盒。

7. 发明申请

WO0242272A2 SUBSTITUTED POLYCYCLIC ARYL AND HETEROARYL PYRIDINES USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开
标题翻译：用于选择性抑制凝聚剂CASCADE的取代的多环芳烃和异丁基吡啶
公开(公告)号：WO0242272A2
公开(公告)日：2002-05-30
申请号：PCT/US0143280
申请日：2001-11-20
申请人： PHARMACIA CORP , SOUTH MICHAEL S , CASE BRENDA , GARLAND DANNY J , HAYES MICHAEL J , HUANG HORNG CHIH , HUANG WEI , JONES DARIN E , NEUMANN WILLIAM L , PARLOW JOHN J , REITZ DAVID B , RUEPPEL MELVIN L , WEBBER RONALD K
发明人： SOUTH MICHAEL S , CASE BRENDA , GARLAND DANNY J , HAYES MICHAEL J , HUANG HORNG-CHIH , HUANG WEI , JONES DARIN E , NEUMANN WILLIAM L , PARLOW JOHN J , REITZ DAVID B , RUEPPEL MELVIN L , WEBBER RONALD K
IPC分类号： A61K31/44 , A61K31/4418 , A61K31/4436 , A61K31/4439 , A61K45/00 , A61P7/02 , A61P9/10 , A61P11/00 , A61P35/00 , A61P43/00 , C07D213/74 , C07D213/89 , C07D401/10 , C07D409/04 , C07D213/00
CPC分类号： C07D213/74 , C07D213/89
摘要： The present invention relates to compounds, and prodrugs thereof, composition and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.
摘要翻译：本发明涉及化合物及其前药，可用于预防和治疗哺乳动物血栓形成病症的组合物和方法。本发明的化合物及其前药选择性地抑制凝血级联的某些蛋白酶。

8. 发明申请

WO9217469A3 N-ARYLHETEROARYLALKYL IMIDAZOL-2-ONE COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS 审中-公开
标题翻译： N-ARYLHETEROARYLALKYL咪唑啉-2-酮化合物治疗循环系统疾病
公开(公告)号：WO9217469A3
公开(公告)日：1992-11-12
申请号：PCT/US9202439
申请日：1992-04-01
申请人： SEARLE & CO
发明人： REITZ DAVID B , MANNING ROBERT E
IPC分类号： A61K31/4439 , C07D401/06 , C07D401/10 , C07D401/14 , C07D409/14
CPC分类号： C07D401/06 , A61K31/4439 , C07D401/10 , C07D401/14
摘要： A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of circulatory disorders such as hypertension and congestive heart failure. Compounds of particular interest are angiotensin II antagonists of formula (I) wherein A is selected from (a), (b), (c), (d), (e) and (f), wherein m is one; R1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, 2-ethylbutyl, n-pentyl, neopentyl, phenyl, methylphenyl, difluorophenyl, benzyl, phenetyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; wherein R0 is hydrido; wherein R2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R?3, R4, R6, R7, R8, R9, R10 and R11¿ is hydrido and R5 must be seleted from COOH, SH, PO¿3?H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, (g), (h) and (i) wherein each of R?42 and R43¿ is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类N-芳基杂芳基烷基咪唑-2-酮化合物用于治疗循环障碍如高血压和充血性心力衰竭。特别感兴趣的化合物是式（I）的血管紧张素II拮抗剂，其中A选自（a），（b），（c），（d），（e）和（f），其中m是1; R1选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，4-甲基丁基，2-乙基丁基，正戊基，新戊基，苯基，甲基苯基，苯乙基，1-环氧乙基，1-氧代丙基，1-氧代丁基，1-氧代戊基和2-羟基丁基; 其中R0是氢; 其中R2选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，正戊基，异戊基，新戊基，苯基，苄基，苯乙基，环己基，环己基甲基，丙硫基，丁硫基和羟烷基; 其中每个R 3，R 4，R 6，R 7，R 8，R 9，R 10和R 11' （g），（h）和（i）其中R142和R43各自是氢，R5必须选自COOH，SH，PO和Iquest; 氰基，硝基，三氟甲基，甲氧基羰基和三氟甲基磺酰基; 或其互变异构体或其药学上可接受的盐。

9. 发明申请

WO9204335A3 RENAL-SELECTIVE BIPHENYLALKYL 1H-SUBSTITUTED-1,2,4-TRIAZOLE ANGIOTENSIN II ANTAGONISTS FOR TREATMENT OF HYPERTENSION 审中-公开
标题翻译：肾上腺素选择性联苯胺1 H-取代的1,2,4-三唑血管生成素II治疗高血压的拮抗剂
公开(公告)号：WO9204335A3
公开(公告)日：1992-04-16
申请号：PCT/US9105897
申请日：1991-08-26
申请人： SEARLE & CO
发明人： REITZ DAVID B , MANNING ROBERT E
IPC分类号： C07D249/08 , C07D249/10 , C07D403/10 , C07D521/00 , H04B1/38 , A61K31/41
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D249/10 , C07D403/10 , H04B1/3883
摘要： Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney. Conjugates of particular interest are glutamyl derivatives of biphenylmethyl 1H-substituted-1,2,4-triazole compounds, of which N-acetylglutamic acid, 5-[[4'-[(3,5-dibutyl-1H-1,2,4-triazol-1-yl)methyl][1,1'-biphenyl]-2-yl]]carbonylhydrazide is an example.

10. 发明申请

WO9202257A3 RENAL-SELECTIVE ANGIOTENSIN II ANTAGONISTS FOR TREATMENT OF HYPERTENSION 审中-公开
标题翻译：选择性血管紧张素II治疗高血压的拮抗剂
公开(公告)号：WO9202257A3
公开(公告)日：1992-04-02
申请号：PCT/US9105476
申请日：1991-08-06
申请人： SEARLE & CO
发明人： MANNING ROBERT E , REITZ DAVID B
IPC分类号： A61K47/48 , C07D233/68 , C07D403/10
CPC分类号： C07D403/10 , A61K47/54 , A61K47/545 , C07D233/68
摘要： Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney. Conjugates of particular interest are glutamyl derivatives of biphenylmethyl 1H-substituted imidazole compounds, of which N-acetyl-L-glutamic acid, 5-[[4'-[2-butyl-4-chloro-5-(hydroxymethyl)-1H-imidazol-1-ylmethyl] [1,1'-biphenyl]-2-yl]carbonyl]hydrazide shown above is an example.

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