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41. 发明公开

EP0866708A4 DIHYDROPYRIMIDINES AND USES THEREOF 失效
标题翻译：二氢及其用途
公开(公告)号：EP0866708A4
公开(公告)日：1999-05-06
申请号：EP96941406
申请日：1996-11-15
申请人： SYNAPTIC PHARMA CORP , MERCK & CO INC
发明人： NAGARATHNAM DHANAPALAN , WONG WAI C , MIAO SHOU WU , PATANE MICHAEL A , GLUCHOWSKI CHARLES
IPC分类号： A61K31/00 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/529 , A61P3/00 , A61P3/06 , A61P9/00 , A61P9/06 , A61P9/12 , A61P15/00 , A61P15/10 , A61P27/00 , A61P27/02 , C07D239/22 , C07D401/12 , C07D491/04 , C07D491/048 , C07D487/04
CPC分类号： C07D239/22 , C07D401/12 , C07D491/04

42. 发明公开

EP0885197A1 2-THIOXOTETRAHYDROPYRIMIDIN-4-ONE DERIVATIVES 失效
标题翻译： 2-硫代四氢吡喃嘧啶-4-酮衍生物
公开(公告)号：EP0885197A1
公开(公告)日：1998-12-23
申请号：EP97906583.0
申请日：1997-02-12
申请人： AMERICAN HOME PRODUCTS CORPORATION
发明人： CHAI, Sie-Yearl , ELOKDAH, Hassan, Mahmoud , SULKOWSKI, Theodore, Sylvester
IPC分类号： A61K31 , A61P9 , C07D239
CPC分类号： C07D239/22
摘要： This invention relates to the use of 2-thioxotetrahydropyrimidin-4-one derivatives to increase HDL cholesterol concentration and as therapeutic compositions for treating atherosclerotic conditions such as dyslipoproteinemias and coronary heart disease. The compounds of this invention are represented by formula (a), wherein: R is C1-C6 alkyl or C2-C6 alkenyl; and R?1, R2, and R3¿ are independently hydrogen, halogen or lower alkyl.
摘要翻译：本发明涉及2-硫代四氢嘧啶-4-酮衍生物用于增加HDL胆固醇浓度的用途，以及用作治疗动脉粥样硬化病症如异常脂蛋白血症和冠心病的治疗组合物。本发明化合物由式（a）表示，其中：R为C1-C6烷基或C2-C6链烯基; R 1，R 2和R 3独立地为氢，卤素或低级烷基。

43. 发明公开

EP0882026A1 PROCESS FOR MAKING DIHYDROPYRIMIDINONES 失效
标题翻译：制备二氢嘧啶酮的方法
公开(公告)号：EP0882026A1
公开(公告)日：1998-12-09
申请号：EP96944785.0
申请日：1996-12-12
申请人： Merck & Co., Inc. (a New Jersey corp.)
发明人： HU, Essa, H. , SIDLER, Daniel, R. , DOLLING, Ulf, H. , PATANE, Michael, A.
IPC分类号： C07D239 , C07B61
CPC分类号： C07D239/22
摘要： The present invention provides a process for forming 5-(alkyl or alkoxy)carbonyl-6-alkyl-4-(aryl or alkyl)-3,4-2(1H)-dihydropyrimidinones by combining a β-keto ester or diketone, an aldehyde and urea in the presence of a boron reagent, a metal salt (e.g., Cu2O) and a catalyst (e.g., acid). The reaction is typically run in one pot in a solvent to afford dihydropyrimidinones in higher yields and with easier work up than previously known methods.
摘要翻译：本发明提供了一种通过结合β-酮酯或二酮，形成5-（烷基或烷氧基）羰基-6-烷基-4-（芳基或烷基）-3,4-2（1H） - 二氢嘧啶酮的方法，醛和脲在硼试剂，金属盐（例如Cu 2 O）和催化剂（例如酸）存在下进行。该反应通常在溶剂中在一个罐中进行，以比以前已知的方法更高的收率和更容易的后处理来提供二氢嘧啶酮。

44. 发明公开

EP0882024A1 RETROVIRAL PROTEASE INHIBITING COMPOUNDS 失效
标题翻译： CONNECTIONS WHICH逆转录病毒蛋白酶INHIBIT
公开(公告)号：EP0882024A1
公开(公告)日：1998-12-09
申请号：EP96944941.0
申请日：1996-12-06
申请人： Abbott Laboratories
发明人： SHAM, Hing, Leung , NORBECK, Daniel, W. , CHEN, Xiaoqi , BETEBENNER, David, A. , KEMPF, Dale, J. , HERRIN, Thomas, R. , KUMAR, Gondi, N. , CONDON, Stephen, L. , COOPER, Arthur, J. , DICKMAN, Daniel, A. , HANNICK, Steven, M. , KOLACZKOWSKI, Lawrence , OLIVER, Patricia, A. , PLATA, Daniel, J. , STENGEL, Peter, J. , STONER, Eric, J. , TIEN, Jieh-Heh, J. , LIU, Jih-Hua , PATEL, Ketan, M.
IPC分类号： C07D , C07D253 , A61K31 , A61K38 , A61K45 , A61P31 , A61P43 , C07C231 , C07C235 , C07C273 , C07C275 , C07D207 , C07D211 , C07D223 , C07D233 , C07D239 , C07D241 , C07D243 , C07D263 , C07D265 , C07D267 , C07D277 , C07D279 , C07D281 , C07D401 , C07D403 , C07D405 , C07D409 , C07D413 , C07D417
CPC分类号： C07D207/27 , C07D207/404 , C07D207/408 , C07D223/10 , C07D233/32 , C07D233/42 , C07D239/10 , C07D239/22 , C07D241/08 , C07D241/18 , C07D253/06 , C07D263/22 , C07D307/20 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D417/12
摘要： A compound of formula (I) is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

45. 发明授权

EP0339596B1 Antibiotics TAN-1057 失效
标题翻译：抗生素TAN-1057。
公开(公告)号：EP0339596B1
公开(公告)日：1994-03-23
申请号：EP89107527.7
申请日：1989-04-26
申请人： Takeda Chemical Industries, Ltd.
发明人： Ono, Hideo , Funabashi, Yasunori , Harada, Setsuo
IPC分类号： C12P13/02 , C07D239/22 , C07D243/08
CPC分类号： C07D239/22 , C07D243/08 , C12P13/02

46. 发明授权

EP0247725B1 Calcium independent camp phosphodiestrerase inhibitor antidepressant 失效
标题翻译：钙独立营磷酸二酯酶抑制剂抗抑郁药
公开(公告)号：EP0247725B1
公开(公告)日：1994-03-02
申请号：EP87303563.8
申请日：1987-04-23
申请人： PFIZER INC.
发明人： Saccomano, Nicholas Alex , Vinick, Frederick James
IPC分类号： C07D233/32 , C07D233/38 , C07D285/06 , C07D233/78 , C07D233/64 , C07D487/04 , C07D207/26 , C07D233/42 , C07D231/12 , C07D239/22 , A61K31/415
CPC分类号： C07D207/26 , C07D231/12 , C07D233/32 , C07D233/38 , C07D233/42 , C07D233/64 , C07D233/78 , C07D239/22 , C07D285/06 , C07D487/04

47. 发明公开

EP0572635A4 NOUVEAUX COMPOSES A STRUCTURE GUANIDIQUE ET COMPOSITION PHARMACEUTIQUE LES CONTENANT. 失效
标题翻译：化合物满足胍结构和含有它们的药物组合物。
公开(公告)号：EP0572635A4
公开(公告)日：1993-09-17
申请号：EP93901791
申请日：1992-11-20
申请人： CENTRE NAT RECH SCIENT
发明人： THAL CLAUDE , QUIROSA-GUILLOU CATHERINE CITE , POTIER PIERRE , RENKO DOLOR , ZANETTA JEAN-PIERRE , PORTIER MARIE-MADELEINE , SENSENBRENNER MONIQUE , KOENIG JANINE , KOENIG HERBERT
IPC分类号： A61K31/155 , A61K31/22 , A61K31/415 , A61K31/4166 , A61K31/505 , A61P25/00 , A61P25/28 , C07C279/02 , C07C279/04 , C07C279/08 , C07D233/60 , C07D233/70 , C07D233/72 , C07D233/88 , C07D233/90 , C07D239/22 , C07D239/28 , C07D239/42
CPC分类号： C07D239/22 , C07C279/08 , C07D233/88 , C07D233/90 , C07D239/42
摘要： Novel compounds having a guanidine structure of formula (I), in which R1 is an isopropyl radical, benzyl optionally substituted by one or more alkoxy (C1-C4) radicals or a radical (a); R2, R3 and R4 are the hydrogen atom or together can form an imidazole, pyrimidine, dihydropyrimidine, pyrimidinium ring. The compounds are especially for use in regenerating neuron axons in diseases such as neuropathies and myopathies.

48. 发明授权

EP0234830B1 2-(Substituted imino)-6-aryl-3,6-dihydro-4-substituted-1,5(2H)-pyrimidinecarboxylic acids and analogs 失效
标题翻译： 2-（取代的亚氨基）-6-亚芳基-3,6-二氢-4-取代的-1,5（2H） - 嘧啶甲酰氧基和类似物
公开(公告)号：EP0234830B1
公开(公告)日：1991-04-24
申请号：EP87301307.2
申请日：1987-02-16
申请人： E.R. Squibb & Sons, Inc.
发明人： Atwal, Karnail
IPC分类号： C07D239/22 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14
CPC分类号： C07D239/22

49. 发明公开

EP0339596A2 Antibiotics TAN-1057 失效
标题翻译：抗生素TAN-1057。
公开(公告)号：EP0339596A2
公开(公告)日：1989-11-02
申请号：EP89107527.7
申请日：1989-04-26
申请人： Takeda Chemical Industries, Ltd.
发明人： Ono, Hideo , Funabashi, Yasunori , Harada, Setsuo
IPC分类号： C12P13/02 , C07D239/22 , C07D243/08
CPC分类号： C07D239/22 , C07D243/08 , C12P13/02
摘要： Novel antibiotics TAN-1057 represented by the formula:
wherein, the absolute configuration in (A) is R or S, each R₁ and R₃ is a bonding hand or hydrogen, and R₂ is a bonding hand, provided that when R₂ binds with R₁ or R₃ the other is hydrogen, were produced by microorganisms belonging to the genus Flexibacter . TAN-1057 strongly inhibit the growth of pathogenic microorganisms and malignant tumors, thus being useful as therapeutic agents of infectious diseases or antitumor agents.
摘要翻译：新型抗生素TAN-1057由下式表示：其中，（A）中的绝对构型为R或S，每个R 1和R 3为键合键或氢，R2为键合键，条件是当R 2结合时其中R1或R3是另一个是氢，由属于柔毛菌属的微生物产生。 TAN-1057强烈抑制致病微生物和恶性肿瘤的生长，因此可用作感染性疾病或抗肿瘤剂的治疗剂。

50. 发明公开

EP0168262A3 Pyrimidine derivatives, processes for preparation thereof and use thereof 失效
标题翻译：吡嗪衍生物，其制备方法及其用途
公开(公告)号：EP0168262A3
公开(公告)日：1987-05-13
申请号：EP85305004
申请日：1985-07-12
申请人： FUJISAWA PHARMACEUTICAL CO., LTD.
发明人： Takaya, Takao , Murata, Masayoshi , Ito, Kiyotaka
IPC分类号： C07D239/42 , C07D239/48 , C07D239/46 , C07D487/04 , C07D403/04 , C07D239/22 , C07D471/04 , C07D401/04 , A61K31/505
CPC分类号： C07D239/22 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D403/04 , C07D471/04 , C07D487/04
摘要： A pyrimidine derivative of the formula :

wherein
R' is hydrogen, aryl optionally having substituent(s) selected from lower alkoxy, lower alkyl, halogen and lower
+alkylthio or , in which N D is a N-containing heterocyclic group; R 2 is a) =N-R 2 or

in which R 2 is aryl optionally substituted with lower alkyl, lower alkoxy, amino and/or acylamino and is hydrogen or lower alkyl, -N B is a N-containing heterocyclic group optionally substituted with acyl and/or ar(lower) alkyl; R 3 is hydrogen or lower alkyl; R 4 is a) imino optionally substituted with lower alkyl, aryl or ar(lower)alkyl, or b) lower alkyl, hydrogen, halogen, lower alkylthio, amino optionally substituted with lower alkyl, aryl, ar(lower)alkyl and/or acyl,
or hydrazino optionally substituted with acyl, in which
is a N-containing heterocyclic goup optionally substituted with acyl, and/or ar(lower)alkyl; R 5 is hydrogen, lower alkyl, lower alkanoyl optionally substituted with lower alkylamino or no significance; or R 3 and R 4 or R 4 and R 5 are taken together with the adjacent nitrogen atom and carbon atom to form a N-containing heterocyclic ring; R 6 is hydrogen, lower alkyl, halogen or aryl optionally having substituent(s) selected from lower alkoxy, lower alkyl, halogen and lower alkylthio substituents; the bond represents single bond or double bond; and the dotted line in the ring A represents one, two or three additional C-C and/or C-N bond(s) in the ring system, provided that R' and R 6 are not both hydrogen; and pharmaceutically acceptable salt thereof. These compounds are useful in the treatment of heart disease, hypertension, cerebrovascular disease and thrombosis. Processes for the preparation of these compounds are also described, together with novel starting compounds for use in such processes and pharmaceutical compositions comprising pyrimidine derivatives of the above formula.

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