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1. 发明申请

WO2011017296A1 4, 5, 6-TRISUBSTITUTED PYRIMIDINE DERIVATIVES AS FACTOR IXA INHIBITORS 审中-公开
标题翻译：作为因子IXA抑制剂的4,5,6-取代的吡嗪衍生物
公开(公告)号：WO2011017296A1
公开(公告)日：2011-02-10
申请号：PCT/US2010/044208
申请日：2010-08-03
申请人： SCHERING CORPORATION , CHELLIAH, Mariappan, V. , CHACKALAMANNIL, Samuel , GREENLEE, William, J. , EAGEN, Keith, A. , GUO, Zhuyan , CLASBY, Martin, C. , XIA, Yan , JAYNE, Charles, L. , DWYER, Michael , KEERTIKAR, Kartik, M. , CHAN, Tin-Yau , WANG, Li
发明人： CHELLIAH, Mariappan, V. , CHACKALAMANNIL, Samuel , GREENLEE, William, J. , EAGEN, Keith, A. , GUO, Zhuyan , CLASBY, Martin, C. , XIA, Yan , JAYNE, Charles, L. , DWYER, Michael , KEERTIKAR, Kartik, M. , CHAN, Tin-Yau , WANG, Li
IPC分类号： C07D239/34 , C07D239/47 , C07D239/52 , A61K31/505 , A61K31/506 , C07D401/12 , C07D403/04 , C07D403/12 , C07D413/12 , C07D417/12
CPC分类号： C07D239/34 , C07D239/47 , C07D239/52 , C07D401/12 , C07D403/04 , C07D403/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to novel heterocyclic compounds of Formulae (I): (Chemical formula should be inserted here as it appears on abstract in paper form) Formula (I) as disclosed herein, or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.
摘要翻译：本发明涉及式（I）的新型杂环化合物：（化学式应在此插入，如本文摘要中所示）本文公开的式（I），或其药学上可接受的盐，溶剂合物，酯，前药或其立体异构体。还公开了包含所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓栓塞性疾病的方法。

2. 发明申请

WO2008042422A2 BICYCLIC AND TRICYCLIC DERIVATIVES AS THROMBIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为血红蛋白受体拮抗剂的双相和三环衍生物
公开(公告)号：WO2008042422A2
公开(公告)日：2008-04-10
申请号：PCT/US2007021277
申请日：2007-10-02
申请人： SCHERING CORP , CHACKALAMANNIL SAMUEL , CHELLIAH MARIAPPAN V , WANG YUGUGUANG , XIA YAN
发明人： CHACKALAMANNIL SAMUEL , CHELLIAH MARIAPPAN V , WANG YUGUGUANG , XIA YAN
CPC分类号： C07D401/06 , C07D417/06
摘要： Heterocyclic-substituted 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 E, A, G M, Het, B, X, R 3 , R 10 , R 11 , R 32 and R 33 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，如价格要求所允许的，其中E，A，GM，Het，B，X，R 3，R 10，R 11，本文定义了本发明的限制性实施方案，其中R 32，R 32和R 33，并且其余取代基如说明书中所定义，以及含有它们的药物组合物和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。

3. 发明申请

WO2006105217A3 SPIROCYCLIC THROMBIN RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2006105217A3
公开(公告)日：2006-11-23
申请号：PCT/US2006011499
申请日：2006-03-29
申请人： SCHERING CORP , CHACKALAMANNIL SAMUEL , CHELLIAH MARIAPPAN V , XIA YAN
发明人： CHACKALAMANNIL SAMUEL , CHELLIAH MARIAPPAN V , XIA YAN
IPC分类号： C07D263/52 , A61K31/4184 , A61P7/02 , A61P9/00
CPC分类号： C07D263/52 , C07D413/08
摘要： Heterocyclic-substituted tricyclics of the formula 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, En, 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：下式的杂环取代的三环或所述化合物，异构体或外消旋混合物的药学上可接受的盐或溶剂化物，其中代表任选的双键，虚线任选为键或无键，产生双键或单键，如化合价要求所允许的，并且其中An，En，Mn，Un，Gn，Jn，Kn，R9，R10，R11，R32，R33，B和Het在本文中定义且其余取代基如说明书中所定义，公开了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，心力衰竭和癌症有关的疾病的方法。本发明还要求与其他心血管药物组合治疗。

4. 发明申请

WO2006041872A3 THROMBIN RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2006041872A3
公开(公告)日：2006-04-20
申请号：PCT/US2005/035745
申请日：2005-10-05
申请人： SCHERING CORPORATION , CHACKALAMANNIL, Samuel , CHELLIAH, Mariappan, V. , XIA, Yan , EAGEN, Keith, A.
发明人： CHACKALAMANNIL, Samuel , CHELLIAH, Mariappan, V. , XIA, Yan , EAGEN, Keith, A.
IPC分类号： C07D405/06 , C07D409/14 , C07D491/10 , C07D413/14 , C07D405/14 , A61K31/443 , A61P7/00
摘要： Heterocyclic-substituted 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 A, B, G, M, X, J, n, Het, R 3 , R 10 , R 11 , R 32 and R 33 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.

5. 发明申请

WO2005046688A2 METHODS OF USE OF THROMBIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：使用凝血酶受体拮抗剂的方法
公开(公告)号：WO2005046688A2
公开(公告)日：2005-05-26
申请号：PCT/US2004/037519
申请日：2004-11-09
申请人： SCHERING CORPORATION , CHACKALAMANNIL, Samuel , CLASBY, Martin, C. , GREENLEE, William, J. , WANG, Yuguang , XIA, Yan , VELTRI, Enrico, P. , CHELLIAH, Mariappan, V. , WU, Wenxue , GRAZIANO, Michael, P. , KOSOGLOU, Teddy , CHINTALA, Madhu
发明人： CHACKALAMANNIL, Samuel , CLASBY, Martin, C. , GREENLEE, William, J. , WANG, Yuguang , XIA, Yan , VELTRI, Enrico, P. , CHELLIAH, Mariappan, V. , WU, Wenxue , GRAZIANO, Michael, P. , KOSOGLOU, Teddy , CHINTALA, Madhu
IPC分类号： A61K31/4525
CPC分类号： A61K31/4525 , A61K31/343 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/06 , C07D405/14 , C07D413/14 , C07D417/14
摘要： A method of treating a therapeutic condition comprising administering to a mammal in need of such treatment an effective amount of at least one compound of the formulas (I) and (II) or a pharmaceutically acceptable isomer, salt, solvate or co-crystal form thereof, wherein the substituents are as defined in the specification, wherein said therapeutic condition is a cardiovascular or circulatory disease or condition, an inflammatory disease or condition, a respiratory tract or disease or condition, cancer, acute renal failure, astrogliosis, a fibrotic disorder of the liver, kidney, lung or intestinal tract, Alzheimer’s disease, diabetes, diabetic neuropathy, rheumatoid arthritis, neurodegenerative disease, neurotoxic disease, systemic lupus erythematosus, multiple sclerosis, osteoporosis, glaucoma, macular degeneration, psoriasis, radiation fibrosis, endothelial dysfunction, a wound or a spinal cord injury, or a symptom or result thereof. Combination therapy with other therapeutically effective agents is also disclosed.
摘要翻译：治疗疾病的方法包括给予需要这种治疗的哺乳动物有效量的至少一种式（I）和（II）化合物或其药学上可接受的异构体，盐其溶剂化物或共晶形式，其中所述取代基如说明书中所定义，其中所述治疗性病症为心血管或循环系统疾病或病症，炎性疾病或病症，呼吸道或疾病或病症，癌症，急性肾病肝，肾，肺或肠道的纤维化病症，阿尔茨海默氏病，糖尿病，糖尿病性神经病，类风湿性关节炎，神经退行性疾病，神经毒性疾病，系统性红斑狼疮，多发性硬化症，骨质疏松症，青光眼，黄斑变性，银屑病，辐射纤维化，内皮功能障碍，伤口或脊髓损伤，或其症状或结果。还公开了与其他治疗有效药剂的联合疗法。

6. 发明申请

WO2007120730A3 FUSED RING THROMBIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：融合环硫蛋白受体拮抗剂
公开(公告)号：WO2007120730A3
公开(公告)日：2008-02-28
申请号：PCT/US2007008978
申请日：2007-04-11
申请人： SCHERING CORP , XIA YAN , CHELLIAH MARIAPPAN V , CHACKALAMANNIL SAMUEL
发明人： XIA YAN , CHELLIAH MARIAPPAN V , CHACKALAMANNIL SAMUEL
IPC分类号： C07D405/06 , A61K31/443 , A61P7/02
CPC分类号： C07D405/06 , C07D498/04
摘要： Fused-ring, heterocyclic-substituted tricyclics of the Formula (I) or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein Formula (II) represents an optional double bond, and wherein A n , E n , M n , G n , J n , R 3 , n 7 , R 8 , R 9 , R 10 , R 11 , R 32 , R 33 , X, Y, 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）的稠环，杂环取代三环或所述化合物的药学上可接受的盐或溶剂合物，异构体或外消旋混合物，其中式（II）表示任选的双键，并且其中A n N，N，N，N，N，N，N，N，N， >，n 7，R 8，R 9，R 10，R 11， >，R 32，R 33，X，Y，B和Het在本文中定义，并且其余取代基如说明书中所定义，以及药物含有它们的组合物和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。

7. 发明申请

WO2005030712A8 THROMBIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：硫蛋白受体拮抗剂
公开(公告)号：WO2005030712A8
公开(公告)日：2007-12-21
申请号：PCT/US2004031495
申请日：2004-09-23
申请人： SCHERING CORP , CHACKALAMANNIL SAMUEL , CHELLIAH MARIAPPAN V , XIA YAN
发明人： CHACKALAMANNIL SAMUEL , CHELLIAH MARIAPPAN V , XIA YAN
IPC分类号： C07D405/06 , C07D405/14 , C07D413/14 , C07D417/14 , C07D521/00
CPC分类号： C07D417/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/06 , C07D405/14 , C07D413/14
摘要： A series of compounds represented by the structural formulas and pharmaceutically acceptable isomers, salts, solvates and polymorphs thereof are disclosed. Also disclosed are pharmaceutical compositions containing said compounds and their use as thrombin receptor antagonists and binders to cannabinoid receptors.
摘要翻译：公开了一系列由结构式表示的化合物及其药学上可接受的异构体，盐，溶剂化物和多晶型物。还公开了含有所述化合物的药物组合物及其作为大麻素受体的凝血酶受体拮抗剂和粘合剂的用途。

8. 发明申请

WO2005118576A1 CONSTRAINED HIMBACINE ANALOGS AS THROMBIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：受约束的肝素模拟物作为血红蛋白受体拮抗剂
公开(公告)号：WO2005118576A1
公开(公告)日：2005-12-15
申请号：PCT/US2005/018372
申请日：2005-05-25
申请人： SCHERING CORPORATION , CHELLIAH, Mariappan, V. , CHACKALAMANNIL, Samuel , XIA, Yan , CLASBY, Martin, C. , GREENLEE, William, J. , WANG, Yuguang , VELTRI, Enrico, P. , WU, Wenxue , GRAZIANO, Michael, P. , KOSOGLOU, Teddy , CHINTALA, Madhu
发明人： CHELLIAH, Mariappan, V. , CHACKALAMANNIL, Samuel , XIA, Yan , CLASBY, Martin, C. , GREENLEE, William, J. , WANG, Yuguang , VELTRI, Enrico, P. , WU, Wenxue , GRAZIANO, Michael, P. , KOSOGLOU, Teddy , CHINTALA, Madhu
IPC分类号： C07D405/08
CPC分类号： C07D493/04 , C07D405/06
摘要： A compound represented by the structural formula (Chemical formula should be inserted here as it appears on abstract in paper form) and pharmaceutically acceptable salts and solvents thereof is disclosed, wherein: the single-dashed line between the ring carbons to which R10 and R34 are attached represents either a single bond or a double bond; the double-dashed line between X and the carbon to which Y is attached represents either a single bond or an absent bond; X is -O- or -NR6- when the double-dashed line represents a single bond; X is H, -OH or -NHR20 when the double-dashed line represents an absent bond; and other parameters are as defined herein. Also disclosed are pharmaceutical compositions and combinations containing said compounds and their uses as thrombin receptor antagonists and binders to cannabinoid receptors.
摘要翻译：公开了由结构式表示的化合物（化学式在此插入，以纸张形式摘录）及其药学上可接受的盐和溶剂，其中：R10和R34之间的环碳上的单点划线附表示单键或双键; X与Y所连接的碳之间的双点划线表示单键或不存在键; 当双点划线表示单键时，X是-O-或-NR6-; 当双点划线表示不存在的键时，X是H，-OH或-NHR 20; 和其他参数如本文所定义。还公开了含有所述化合物及其作为凝血酶受体拮抗剂和大麻素受体的结合物的药物组合物和组合。

9. 发明申请

WO2005046688A3 METHODS OF USE OF THROMBIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：使用硫蛋白受体拮抗剂的方法
公开(公告)号：WO2005046688A3
公开(公告)日：2005-09-29
申请号：PCT/US2004037519
申请日：2004-11-09
申请人： SCHERING CORP , CHACKALAMANNIL SAMUEL , CLASBY MARTIN C , GREENLEE WILLIAM J , WANG YUGUANG , XIA YAN , VELTRI ENRICO P , CHELLIAH MARIAPPAN V , WU WENXUE , GRAZIANO MICHAEL P , KOSOGLOU TEDDY , CHINTALA MADHU
发明人： CHACKALAMANNIL SAMUEL , CLASBY MARTIN C , GREENLEE WILLIAM J , WANG YUGUANG , XIA YAN , VELTRI ENRICO P , CHELLIAH MARIAPPAN V , WU WENXUE , GRAZIANO MICHAEL P , KOSOGLOU TEDDY , CHINTALA MADHU
IPC分类号： A61K31/343 , A61K31/4525 , C07D405/06 , C07D405/14 , C07D413/14 , C07D417/14 , C07D521/00 , A61P9/00 , A61P11/00 , A61P13/12 , A61P25/28 , A61P29/00 , A61P35/00
CPC分类号： A61K31/4525 , A61K31/343 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/06 , C07D405/14 , C07D413/14 , C07D417/14
摘要： A method of treating a therapeutic condition comprising administering to a mammal in need of such treatment an effective amount of at least one compound of the formulas (I) and (II) or a pharmaceutically acceptable isomer, salt, solvate or co-crystal form thereof, wherein the substituents are as defined in the specification, wherein said therapeutic condition is a cardiovascular or circulatory disease or condition, an inflammatory disease or condition, a respiratory tract or disease or condition, cancer, acute renal failure, astrogliosis, a fibrotic disorder of the liver, kidney, lung or intestinal tract, Alzheimer's disease, diabetes, diabetic neuropathy, rheumatoid arthritis, neurodegenerative disease, neurotoxic disease, systemic lupus erythematosus, multiple sclerosis, osteoporosis, glaucoma, macular degeneration, psoriasis, radiation fibrosis, endothelial dysfunction, a wound or a spinal cord injury, or a symptom or result thereof. Combination therapy with other therapeutically effective agents is also disclosed.
摘要翻译：治疗治疗条件的方法包括向需要这种治疗的哺乳动物施用有效量的至少一种式（I）和（II）化合物或其药学上可接受的异构体，盐，溶剂合物或共晶体形式其中所述取代基如说明书中所定义，其中所述治疗条件是心血管或循环系统疾病或病症，炎性疾病或病症，呼吸道或疾病或病症，癌症，急性肾功能衰竭，星形胶质细胞增生症，纤维化疾病肝，肾，肺或肠道，阿尔茨海默病，糖尿病，糖尿病性神经病，类风湿性关节炎，神经变性疾病，神经毒性疾病，系统性红斑狼疮，多发性硬化症，骨质疏松症，青光眼，黄斑变性，牛皮癣，放射纤维化，内皮功能障碍伤口或脊髓损伤，或其症状或结果。还公开了与其它治疗有效药物的联合治疗。

10. 发明申请

WO2011025565A1 MORPHOLINONE COMPOUNDS AS FACTOR IXA INHIBITORS 审中-公开
标题翻译：吗啉酮化合物作为因子IXA抑制剂
公开(公告)号：WO2011025565A1
公开(公告)日：2011-03-03
申请号：PCT/US2010/036853
申请日：2010-06-01
申请人： MOCHIDA PHARMACEUTICAL CO., LTD. , SCHERING CORPORATION , NISHIDA, Hidemitsu , SAITOH, Fumihiko , HIRABAYASHI, Tomokazu , CHACKALAMANNIL, Samuel , CHAN, Tin-Yau , CHELLIAH, Mariappan, V. , CLASBY, Martin, C. , DWYER, Michael, P. , GREENLEE, William, J. , XIA, Yan , NEELAMKAVIL, Santhosh , SHAH, Unmesh, G.
发明人： NISHIDA, Hidemitsu , SAITOH, Fumihiko , HIRABAYASHI, Tomokazu , CHACKALAMANNIL, Samuel , CHAN, Tin-Yau , CHELLIAH, Mariappan, V. , CLASBY, Martin, C. , DWYER, Michael, P. , GREENLEE, William, J. , XIA, Yan , NEELAMKAVIL, Santhosh , SHAH, Unmesh, G.
IPC分类号： C07D265/32 , C07D413/04 , C07D413/12 , C07D413/14 , A61K31/5377 , A61P7/02
CPC分类号： C07D413/12 , C07D265/32 , C07D413/04 , C07D413/14
摘要： The present invention provides compounds having the formula (I) or a pharmaceutically acceptable salt or a solvate thereof, pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.
摘要翻译：本发明提供具有式（I）化合物或其药学上可接受的盐或溶剂合物，包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝状态或纤维化改变的方法。

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