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31. 发明公开

EP1484057A1 USE OF 2-AMINO-1-3-PROPANEDIOL DERIVATIVES FOR THE MANUFACTURE OF A MEDICAMENT FOR THE TREATMENT OF VARIOUS TYPES OF PAIN 审中-公开
标题翻译： 2-氨基-1,3- PROPANDIOLDERIVATEN FOR HERSTRLLUNG药物用于某些治疗疼痛的
公开(公告)号：EP1484057A1
公开(公告)日：2004-12-08
申请号：EP03012864.9
申请日：2003-06-06
申请人： Aventis Pharma Deutschland GmbH
发明人： Michaelis, Martin, Dr. , Geisslinger, Gerd, Prof. Dr. , Scholich, Klaus, Dr.
IPC分类号： A61K31/137 , A61P25/04 , A61P25/06
CPC分类号： A61K31/137
摘要： The present invention relates to the use of 2-Amino-1,3-propanediol derivatives of the formula I,
for the preparation of pharmaceuticals for the prophylaxis or treatment of pain.
摘要翻译：本发明涉及使用式I，药品用于预防或治疗疼痛的制备的2-氨基-1,3-丙二醇衍生物。

32. 发明公开

EP1483244A1 CYCLISCHE N-SUBSTITUIERTE ALPHA-IMINOCARBONSÄUREN ZUR SELEKTIVEN INHIBIERUNG VON KOLLAGENASE 有权
标题翻译：环状N-取代的α-亚氨基羧酸胶原酶的选择性抑制
公开(公告)号：EP1483244A1
公开(公告)日：2004-12-08
申请号：EP03709711.0
申请日：2003-02-18
申请人： Aventis Pharma Deutschland GmbH
发明人： STAHL, Petra , KIRSCH, Reinhard , RUF, Sven , WEHNER, Volkmar , WEITHMANN, Klaus-Ulrich
IPC分类号： C07D217/26 , C07D471/04 , A61K31/472 , A61K31/437 , A61P19/00
CPC分类号： C07D471/04 , C07D217/26
摘要： The invention relates to compounds of formula (I), which are suitable for the production of medicaments for the prophylaxis and therapy of diseases in the course of which reinforced activity of matrix metalloproteinase 13 is involved. Said diseases include degenerative arthropathy, for example, spondylosis, chondroporosis after joint trauma or prolonged joint immobilization after meniscus or patella injuries or ruptures of a ligament or a disease of the connective tissue such as collagenosis, periodontal diseases, wound healing disorders or a chronic disease of the locomotor system such as acute or chronic inflammatory, immunological or metabolic arthritis, arthropathy, myalgia or bone metabolism disorders or an ulceration, arteriosclerosis or stenosis or an inflammatory disease or a cancer disease, tumor metastasis formation, cachexia, anorexia or septic shock.

33. 发明授权

EP1051402B1 VERFAHREN ZUR HERSTELLUNG VON S-ALKYL(ARYL)-SUBSTITUIERTEN IMIDAZOL-DERIVATEN 有权
标题翻译：用于生产S-烷基（芳基）取代的咪唑衍生物
公开(公告)号：EP1051402B1
公开(公告)日：2004-12-08
申请号：EP99906156.7
申请日：1999-01-19
申请人： Aventis Pharma Deutschland GmbH
发明人： HOLLA, Wolfgang , NAPIERSKI, Bernd , REBENSTOCK, Heinz-Peter
IPC分类号： C07D233/90
CPC分类号： C07D233/90
摘要： The invention relates to a method for producing compounds of formula (I), wherein R(2) and R(3) independently of each other mean -SR(4) or -COOR(5) and R(1), R(4) and R(5) have the meaning cited in the description. The inventive method is characterized in that compounds of formula (II), wherein R(1), R(2) and R(3) have the meaning defined above, are cyclized in the presence of alkyl phosphonic acid anhydrides to form compounds of formula (I), whereupon said compounds are subsequently purified in a manner known per se involving the formation of salt and optionally recrystallization, and that the residues introduced to protect other functional groups are optionally separated in a manner known per se. The invention also relates to the use of said compounds as an intermediate product for the synthesis of active substances.

34. 发明公开

EP1480960A1 SUBSTITUIERTE 3-PHENYL-5-ALKOXY-1,3,4-OXADIAZOL-2-ONE SOWIE IHRE HERSTELLUNG UND VERWENDUNG IN ARZNEISTOFFEN 有权
标题翻译：取代的3-苯基-5-烷氧基-1,3,4-恶二唑-2-酮以及它们的制备和在药物中使用
公开(公告)号：EP1480960A1
公开(公告)日：2004-12-01
申请号：EP03742936.2
申请日：2003-02-14
申请人： Aventis Pharma Deutschland GmbH
发明人： SCHOENAFINGER, Karl , PETRY, Stefan , MÜLLER, Günter , BAUER, Armin , HEUER, Hubert, Otto
IPC分类号： C07D271/113 , A61K31/4245 , A61P3/04
CPC分类号： C07D271/113
摘要： The invention relates to substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones, of general formula (I), wherein R1 represents C7-C22 alkyl, C2-C4 alkyl that is substituted by C4-C20 alkoxy, C6-C10 aryl, C6-C10 aryloxy or C4-C12-alkoxy-C2-C4-alkoxy, and represents C7-C20 alkenyl, 3β-cholestan-3-yl or substituted phenyl; R2, R3, R4 and R5 represent hydrogen, halogen, nitro, C1-C4 alkyl, C1-C9 alkyloxy, trifluoromethyl, trifluoromethoxy or C6-C10-aryl-C1-C4-alkyloxy, C6-C10 aryloxy, C6-C10 aryl, C3-C8 cycloalkyl or O-C3-C8-cycloalkyl, whereby all of these can be substituted. The invention also relates to methods for producing these compounds. The compounds of formula (I) have an inhibiting effect on the pancreatic lipase and can be used as active substances for treating obesity.

35. 发明公开

EP1480628A1 VERWENDUNG VON INHIBITOREN DES NATRIUM-WASSERSTOFF-AUSTAUSCHERS ZUR BEHANDLUNG VON THROMBOTISCHER UND INFLAMMATORISCHER ERKRANKUNGEN 审中-公开
标题翻译：钠 - 氢交换抑制剂的用于治疗血栓形成和炎症性疾病USE
公开(公告)号：EP1480628A1
公开(公告)日：2004-12-01
申请号：EP03706415.1
申请日：2003-02-03
申请人： Aventis Pharma Deutschland GmbH
发明人： LANG, Hans-Jochen , SCHNEIDER, Stefan, Werner , OBERLEITHNER, Hans , NIEMEYER, André
IPC分类号： A61K31/185 , A61K31/47 , A61K31/255 , A61K31/417 , A61K31/404 , A61K31/4418 , A61K7/02 , A61P9/10
CPC分类号： A61K45/06 , A61K31/165 , A61K31/185 , A61K31/255 , A61K31/403 , A61K31/404 , A61K31/417 , A61K31/435 , A61K31/4418 , A61K31/454 , A61K31/47 , A61K31/496
摘要： Inhibitors of cellular sodium/hydrogen exchangers display an inhibiting effect on the secretion of von-Willebrand factor and/or increased expression of P-selektin. Said inhibitors can thus be used for the treatment of thrombotic and inflammatory diseases.

36. 发明公开

EP1479677A1 New indole derivatives as factor xa inhibitors 审中-公开
标题翻译： Neue Indolderivate als Faktor Xa-Inhibitoren
公开(公告)号：EP1479677A1
公开(公告)日：2004-11-24
申请号：EP03011306.2
申请日：2003-05-19
申请人： Aventis Pharma Deutschland GmbH
发明人： Nazaré, Marc, Dr. , Wehner, Volkmar, Dr. , Ritter, Kurt, Dr. , Laux, Volker, Dr.
IPC分类号： C07D413/14 , C07D401/04 , C07D401/14 , A61K31/404 , A61P7/02
CPC分类号： C07D413/14
摘要： The present invention relates to compounds of the formula I,
in which R 0 ; R 1 ; R 2 ; R 3 ; R 4 ; R 5 ; R 6 ; R 7 ; Q; V, G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式I化合物，其中R 0为CHEM; R 1; R 2; R 3; R 4; R 5; R 6; R 7; Q; V，G和M具有权利要求中所示的含义。式I的化合物是有价值的药理活性化合物。它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。它们是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可以在其中存在因子Xa和/或因子VIIa的不期望活性或用于治愈或预防因子Xa和/或因子VIIa的抑制。本发明还涉及式I化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

37. 发明公开

EP1479676A1 Benzimidazole-derivatives as factor xa inhibitors 审中-公开
标题翻译： Benzimidazolderivate als Faktor Xa-Inhibitoren
公开(公告)号：EP1479676A1
公开(公告)日：2004-11-24
申请号：EP03011305.4
申请日：2003-05-19
申请人： Aventis Pharma Deutschland GmbH
发明人： Nazaré, Marc, Dr. , Wagner, Michael, Dr. , Wehner, Volkmar, Dr. , Matter, Hans, Dr. , Urmann, Matthias, Dr. , Ritter, Kurt, Dr.
IPC分类号： C07D413/14 , C07D401/04 , C07D401/14 , C07D417/14 , C07D471/04 , A61K31/4184 , A61P7/02
CPC分类号： C07D235/24 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/08 , C07D495/04
摘要： Benzimidazole-derivatives as factor Xa inhibitors

The present invention relates to compounds of the formula I,
wherein R 0 ; R 1 ; R 2 ; R 3 ; R 4 ; Q; V, G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译：作为因子Xa抑制剂的苯并咪唑衍生物本发明涉及式I化合物，其中R 0; R 1; R 2; R 3; [R <4>; Q; V，G和M具有权利要求中所示的含义。式I的化合物是有价值的药理活性化合物。它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。它们是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可以在其中存在因子Xa和/或因子VIIa的不期望活性或用于治愈或预防因子Xa和/或因子VIIa的抑制。本发明还涉及式I化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

38. 发明公开

EP1479675A1 Indazole-derivatives as factor Xa inhibitors 审中-公开
标题翻译： Indazolderivate als Faktor Xa-Inhibitoren
公开(公告)号：EP1479675A1
公开(公告)日：2004-11-24
申请号：EP03011303.9
申请日：2003-05-19
申请人： Aventis Pharma Deutschland GmbH
发明人： Nazaré, Marc, Dr. , Wehner, Volkmar, Dr. , Laux, Volker, Dr. , Urmann, Matthias, Dr. , Bauer, Armin, Dr. , Matter, Hans, Dr.
IPC分类号： C07D413/14 , C07D401/14 , C07D401/12 , C07D413/04 , A61K31/416 , A61P7/02
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14
摘要： The present invention relates to compounds of the formulae I and Ib

wherein R 0 ; R 1 ; R 2 ;Q; V, G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formulae I and Ib, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式I和Ib化合物 CHEM>其中R 0; R 1; R 2; Q; V，G和M具有权利要求中所示的含义。式I的化合物是有价值的药理活性化合物。它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。它们是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可以在其中存在因子Xa和/或因子VIIa的不期望活性或用于治愈或预防因子Xa和/或因子VIIa的抑制。本发明还涉及制备式I和Ib化合物的方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

39. 发明公开

EP1471066A1 Triaza- and tetraaza-anthracenedione derivates, their preparation and their use as pharmaceuticals 审中-公开
标题翻译： Triaza- und Tetraaza-anthrazendionderivate，ihre Herstellung und Verwendung als Pharmazeutika
公开(公告)号：EP1471066A1
公开(公告)日：2004-10-27
申请号：EP03009286.0
申请日：2003-04-24
申请人： Aventis Pharma Deutschland GmbH
发明人： Weichert, Andreas , Strobel, Hartmut , Wohlfart, Paulus , Patek, Marcel , Smrcina, Martin , Weichsel, Aleksandra
IPC分类号： C07D471/14 , C07D487/04 , A61K31/519 , A61P9/00
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention relates to triaza- and tetraaza-anthracenedione derivatives of the formula I,
in which A, B and R 1 to R 5 have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They are useful in the treatment of various disease states including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency. They upregulate the expression of the enzyme endothelial nitric oxide
(NO) synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译：三氮杂和四氮杂蒽并二酮衍生物，其立体异构形式或混合物或盐是新的。式（I）的三氮杂和四氮杂蒽并二酮衍生物，其立体异构形式或混合物或盐是新的。 [图] A：CR 6或N; B：CR 7或N; R 11-10C烷基，3-8C环烷基，2-10C烯基或2-10C炔基（全部被卤素取代，CN，3-8C环烷基，苯基，联苯基，萘基，茚满基或杂芳基）。（CH 2）a-苯基， - （CH 2）a-咪唑基或 - （CH 2）a-吡啶基; R 1，R 2， a：0 - 2; R 3 - （CH 2）b-苯基， - （CH 2）b-咪唑基， - （CH-2）b-三唑基， - （CH 2）b-Het或 - （CH 2） b：1 - 4; R 4 -R 7，1-4C烷基，CF 3，1-4C烷氧基，OCF 3，卤素，硝基，CN，-CO-R 10，-NR 8 R 9，-NH-CO-1-4C烷基， -SO 2 - NR 8 R 9，-SO 2-1-4C烷基或-SO 2 - （CH 2）c-苯基; c：0 - 2; R 8和R 9H或1-4C烷基; R 10 OH，1-4C烷氧基或-NR 8 R 9; Het：饱和的5-或6-元单环杂环的残基（含有氮键，通过它与之键合，并另外含有另外的选自N，O和S的环杂原子，并且任选被1-4C烷基或 - （CH 2）d-苯基）; d：0 - 2; 杂芳基：芳族5-10元，单环或双环杂环（含1-4个N，O和S）的残基。残基苯基，联苯基，萘基，茚满基，杂芳基，吡啶基，咪唑基和三唑基任选被卤素，CN，1-6C烷基，CF 3，1-6C烷氧基或OCF 3取代.A和B不同时为N. 包括（I）的独立索赔。活动：心血管病。抗心绞痛; Cardiant; 脑保护; Vasotropic; 溶栓; 抗动脉硬化; 低血压; 呼吸根; Nephrotropic; 抗心律不整; 降血糖; 眼科; 平喘; 抗血管生成; 嗜肝; 骨科。作用机制：内皮一氧化氮（NO）合酶（eNOS）表达刺激因子。（4S）-9-（3-（咪唑并）-1-基）丙基）-4-异丙基-6-硝基-2-（4-苯基丁基）-1,2,9,9a四氢2,4a，如Li等人，激活蛋白激酶Cα和/或ε增加人内皮细胞的转录，测试了9-三氮杂 - 蒽-3,10（4H） - 二酮三氟乙酸（Ia）的eNOS转录活化一氧化氮合酶基因药理学。 53（1998）630.（Ia）显示2.2mM的EC 5 0。

40. 发明公开

EP1465870A2 SUBSTITUIERTE 4-PHENYLTETRAHYDROISOCHINOLINIUM-SALZE, VERFAHREN ZU IHRER HERSTELLUNG, IHRER VERWENDUNG ALS MEDIKAMENT, SOWIE SIE ENTHALTENDES MEDIKAMENT 有权
标题翻译：取代的4- PHENYLTETRAHYDROISOCHINOLINIUM盐，PROCESS所周之，它们作为药品和含药
公开(公告)号：EP1465870A2
公开(公告)日：2004-10-13
申请号：EP02795126.8
申请日：2002-12-09
申请人： Aventis Pharma Deutschland GmbH
发明人： HOFMEISTER, Armin , LANG, Hans-Jochen , HEINELT, Uwe , BLEICH, Markus , WIRTH, Klaus
IPC分类号： C07D217/10 , C07D217/14 , A61K31/472 , A61P9/06
CPC分类号： C07D217/14 , C07D217/10
摘要： Compounds of formula (I), where R1 to R10 have the meanings given in the claims are particularly suitable as anti-hypertensives, for the reduction or prevention of ischaemic induced injury, as medicament for operative intervention in the treatment of ischaemia of the nervous system, stroke, cerebral oedema, shock, disrupted respiration, treatment of snoring, as laxative, as agent against ectoparasites, for prevention of gallstone formation, as antiatherosclerotic, as agent against late diabetic complications, carcinogenic disease states, fibrotic diseases, endothelial dysfunctions, organ hypertrophias and hyperplasias. Said compounds are inhibitors of cellular sodium/proton antiporters, influence serum lipoproteins, and can be used for prophylaxis and regression of atherosclerotic changes.

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