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公开(公告)号：EP1194425B1
公开(公告)日：2005-08-10
申请号：EP00938780.4
申请日：2000-06-09
发明人： RITZELER, Olaf , STILZ, Hans, Ulrich , NEISES, Bernhard , BOCK, William, Jerome, Jr. , WALSER, Armin , FLYNN, Gary, A. , HABERMANN, Jörg , JAHNE, Gerhard
IPC分类号： C07D401/04 , A61K31/415 , A61P29/00 , C07D401/14 , C07D413/14 , C07D471/04
CPC分类号： C07D401/04 , C07D401/14 , C07D409/14 , C07D471/04
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公开(公告)号：EP1361882A1
公开(公告)日：2003-11-19
申请号：EP02722066.4
申请日：2002-02-12
发明人： WOHLFART, Paulus , SUZUKI, Teri , DHARANIPRAGADA, Ramalinga, M. , SAFAROVA, Alena , WALSER, Armin , STROBEL, Hartmut
IPC分类号： A61K31/66 , C07C233/65 , A61P1/16 , A61P5/48 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/12 , A61P15/10 , A61P19/10 , A61P25/28
CPC分类号： C07C233/65 , A61K31/166 , C07C2602/08
摘要： The present invention relates to 4-fluoro-N-indan-2-yl benzamide according to the formula (I), and its use as pharmaceutical. The compound (I) can be used for the therapy and prophylaxis of cardiovascular diseases like stable and unstable angina pectoris, Prinzmetal angina (spasm), acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease PAOD, atherosclerosis, restenosis, endothel damage after PTCA, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, and the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptiva, the therapy and propylaxis of diabetes and diabetes complications (nephropathy, retinopathy), angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, restricted memory performance or a restricted ability to learn.
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公开(公告)号：EP1042287B1
公开(公告)日：2005-04-20
申请号：EP98965244.1
申请日：1998-12-10
发明人： DEFOSSA, Elisabeth , HEINELT, Uwe , KLINGLER, Otmar , ZOLLER, Gerhard , AL-OBEIDI, Fahad , WALSER, Armin , WILDGOOSE, Peter , MATTER, Hans
IPC分类号： C07D209/42 , A61K31/40 , C07D401/12 , C07D403/10 , C07D401/06 , C07D471/04
CPC分类号： C07D401/06 , C07D209/42 , C07D401/12 , C07D403/10 , C07D471/04
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4.发明授权ARYLALKANOYL DERIVATIVES, PROCESSES FOR THEIR PREPARATION, THEIR USE AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 有权ARYLALKANOYLDERIVATE，PROCESS FOR THEIR，它们的使用和药物制剂含有它们的
公开(公告)号：EP1150946B1
公开(公告)日：2005-03-30
申请号：EP99967001.1
申请日：1999-12-23
发明人： DEFOSSA, Elisabeth , HEINELT, Uwe , KLINGLER, Otmar , ZOLLER, Gerhard , MATTER, Hans , AL-OBEIDI, Fahad, D. , WALSER, Armin , WILDGOOSE, Peter
IPC分类号： C07C279/00 , C07C279/10 , A61K31/325
CPC分类号： C07D213/40 , A61K38/00 , C07C257/18 , C07C279/14 , C07C2601/14 , C07D211/26 , C07D213/56 , C07D233/20 , C07D233/74 , C07D271/07 , C07D413/12 , C07K5/0205 , C07K5/06078
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公开(公告)号：EP1373191A1
公开(公告)日：2004-01-02
申请号：EP02722067.2
申请日：2002-02-12
发明人： STROBEL, Hartmut , WOHLFART, Paulus , SAFAROVA, Alena , WALSER, Armin , SUZUKI, Teri , DHARANIPRAGADA, Ramalinga, M. , SCHOENAFINGER, Karl
IPC分类号： C07C233/64 , C07C235/44 , C07D213/56 , C07D307/78 , C07D317/60 , C07D333/24 , A61K31/165 , A61K31/36 , A61K31/38 , A61K31/435 , A61P9/00
CPC分类号： C07D213/81 , C07C233/58 , C07C233/65 , C07C233/66 , C07C233/74 , C07C233/76 , C07C235/42 , C07C235/54 , C07C235/84 , C07C237/38 , C07C237/42 , C07C255/57 , C07C255/60 , C07C309/66 , C07C309/73 , C07C311/08 , C07C311/16 , C07C311/21 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2602/08 , C07D207/34 , C07D213/56 , C07D213/82 , C07D215/48 , C07D235/08 , C07D241/24 , C07D249/04 , C07D261/18 , C07D295/185 , C07D307/78 , C07D307/84 , C07D317/60 , C07D333/24 , C07D401/06
摘要： The present invention relates to acylated indanyl amines according to the general formula (I) where R1-R4 have the meanings given in the description, A is CH¿2? CHOH or CH-(C1-C3-alkyl), B is CH2 or CH-(C1-C3-alkyl), and R?5¿ is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description. These compounds are useful in the upregulation of endothelial nitric oxide synthase (eNOS), and may therefore be useful for the manufacture of medicaments for the treatment of cardiovascular diseases, stable or unstable angina pectoris, coronary heart disease, Prinymetal angina, actue coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease, endothelial dysfunction, atherosclerosis, restenosis, endothel damage after PTCA, hypertension, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular hypertension, chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, diabetes or diabetes complications, nephropathy or retinopathy, angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, osteoporosis, restricted memory performance, a restricted ability to learn, or for the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives.
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6.发明公开NOVEL MALONIC ACID DERIVATES, PROCESSES FOR THEIR PREPARATION, THEIR USE AS INHIBITOR OF FACTOR XA ACTIVITY AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 有权丙二酸衍生物，工艺所周之，及其作为因子Xa活性和药物组合物含有这种抑制剂的
公开(公告)号：EP1265867A1
公开(公告)日：2002-12-18
申请号：EP01907546.4
申请日：2001-02-21
IPC分类号： C07D217/14 , A61K31/40 , A61K31/435 , C07D207/08 , C07K5/08 , A61K31/06
CPC分类号： C07D213/56 , A61K38/00 , C07C257/18 , C07C279/14 , C07C2601/14 , C07K5/0202 , C07K5/06026 , C07K5/06034
摘要： The present invention relates to new compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula (I), wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of the formula (I) are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula (I), to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to the use of the compounds of formula (I) in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (I), in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (I) together with pharmaceutically acceptable carrier substances and auxiliary substances.
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7.发明公开DIARYLSUBSTITUIERTE CYCLISCHE HARNSTOFFDERIVATE MIT MCH-MODULATORISCHER WIRKUNG 有权与MCH-调节作用二芳基环脲衍生物
公开(公告)号：EP1551810A1
公开(公告)日：2005-07-13
申请号：EP03771060.5
申请日：2003-07-18
发明人： SCHWINK, Lothar , STENGELIN, Siegfried , GOSSEL, Matthias , BOEHME, Thomas , HESSLER, Gerhard , ROSSE, Gerard , WALSER, Armin
IPC分类号： C07D233/70 , C07D233/32 , C07D243/04 , C07D249/12 , A61K31/4166 , A61P3/04 , A61P3/10 , C07D401/12 , C07D209/02 , C07D491/10 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D487/08
CPC分类号： C07D233/92 , C07D209/02 , C07D233/32 , C07D233/70 , C07D233/74 , C07D233/94 , C07D243/04 , C07D249/12 , C07D401/12 , C07D403/12 , C07D405/10 , C07D405/12 , C07D409/10 , C07D409/12 , C07D417/12 , C07D487/08 , C07D491/10
摘要： The invention relates to substituted diaryl heterocycles and the physiologically compatible salts and physiologically functional derivatives thereof. The invention also relates to compounds of formula (I) wherein the radicals have the cited designations, to the physiologically compatible salts thereof, and to methods for producing the same. Said compounds are suitable, for example, as anorexiants.
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8.发明公开AMINOALKYL SUBSTITUIERTE AROMATISCHE BICYCLEN, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ALS ARZNEIMITTEL 审中-公开氨基取代芳烃自行车，其制造方法相同，它们作为药物
公开(公告)号：EP1418906A1
公开(公告)日：2004-05-19
申请号：EP02774498.6
申请日：2002-08-03
IPC分类号： A61K31/4045 , A61K31/4184 , C07D209/08 , C07D403/06 , C07D235/06 , C07D235/08 , C07D401/06 , C07D413/06 , C07D403/12 , C07D401/12 , C07D413/12 , C07D417/12 , C07D409/12 , C07D405/06 , C07D409/06
CPC分类号： C07D235/06 , C07D209/08 , C07D235/08 , C07D401/12 , C07D403/06 , C07D403/12 , C07D409/12
摘要： The invention relates to aminoalkyl-substituted aromatic bicyclic compounds and to their physiologically acceptable salts and physiologically functional derivatives. Disclosed are compounds of formula (I), wherein the radicals have the meaning cited in the description. Further disclosed are the physiologically acceptable salts of said compounds and to a method for the production thereof. Said compounds can be suitably used as anorectic drugs.
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公开(公告)号：EP1194425A1
公开(公告)日：2002-04-10
申请号：EP00938780.4
申请日：2000-06-09
发明人： RITZELER, Olaf , STILZ, Hans, Ulrich , NEISES, Bernhard , BOCK, William, Jerome, Jr. , WALSER, Armin , FLYNN, Gary, A. , HABERMANN, Jörg , JAHNE, Gerhard
IPC分类号： C07D401/04 , A61K31/415 , A61P29/00 , C07D401/14 , C07D413/14 , C07D471/04
CPC分类号： C07D401/04 , C07D401/14 , C07D409/14 , C07D471/04
摘要： The invention relates to compounds of formula (I) which are suitable for producing medicaments. Said medicaments are used in the prophylaxis and treatment of diseases, in the course of which there is increased activity of NFkB.
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公开(公告)号：EP1042287A1
公开(公告)日：2000-10-11
申请号：EP98965244.1
申请日：1998-12-10
发明人： DEFOSSA, Elisabeth , HEINELT, Uwe , KLINGLER, Otmar , ZOLLER, Gerhard , AL-OBEIDI, Fahad , WALSER, Armin , WILDGOOSE, Peter , MATTER, Hans
IPC分类号： C07D209/42 , A61K31/40 , C07D401/12 , C07D403/10 , C07D401/06 , C07D471/04
CPC分类号： C07D401/06 , C07D209/42 , C07D401/12 , C07D403/10 , C07D471/04
摘要： The present invention relates to the inhibition of blood clotting proteins, and more particularly, to indole derivatives of formula (I), in which R?1a, R1b, R1c R1d, R2, R3, R4¿ and A are defined as indicated in the claims. The compounds of formula (I) are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula (I), to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to use of the compounds of formula (I) in the treatment and prophylaxis of diseases which can be cured or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (I) in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (I) together with pharmaceutically acceptable carrier substances and/or auxiliary substances.
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