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1. 发明专利

JPS62155280A 4-THIENYL-DIHYDROPYRIDINES 失效
公开(公告)号：JPS62155280A
公开(公告)日：1987-07-10
申请号：JP30017386
申请日：1986-12-18
申请人： BAYER AG
发明人： GOLDMANN SIEGFRIED , BISCHOFF HILMAR , PULS WALTER , BENDER JOACHIM , PETZINNA DIETER , SCHLOSSMANN KLAUS
IPC分类号： A61K31/435 , A61P3/08 , A61P3/10 , C07D491/04 , C07D491/048
摘要： Blood sugar levels are reduced by administration of novel 4-thienyl-dihydropyridines of the formula in which R1 represents 1 or 2 halogen atoms, or represents straight-chain, branched or cyclic alkyl with up to 8 carbon atoms, R2 represents a straight-chain, branched or cyclic, saturated or unsaturated hydrocarbon radical which has up to 15 carbon atoms, is optionally interrupted by one or two oxygen atoms, -N-phenyl or -SOn-(n=0, 1 or 2) and is optionally substituted by halogen, phenyl, hydroxyl, cyano, amino, C1-C6-alkylamino, di-C1-C6-alkylamino, pyridyl, piperidino, N-phenylpiperazino, N-methylpiperazino, morpholino or N-benzyl-N-benzyl-N-methyl-amino, R3 represents hydrogen, or represents straight-chain, branched or cyclic alkyl which has up to 6 carbon atoms and is optionally substituted by halogen, hydroxyl, amino or amino-C1-C6-alkoxy, or represents cyano or formyl and R4 represents hydrogen or a straight-chain, branched or cyclic alkyl radical which has up to 10 carbon atoms, is optionally interrupted by one or two oxygen atoms in the chain and is optionally substituted by halogen, cyano, hydroxyl, phenyl, carboxyl, C1-C6-alkoxycarbonyl, amino, C1-C6-alkylamino, di-C1-C6-alkylamino, formyl, piperidino, morpholino or thiomorpholino, or physiologically acceptable salts thereof.

2. 发明专利

JPH1036372A NEW PYRIDAZINO-, PYRIMIDO-, PYRAZINO-AND TRIAZINO-INDOLES 失效
公开(公告)号：JPH1036372A
公开(公告)日：1998-02-10
申请号：JP10681497
申请日：1997-04-10
申请人： BAYER AG
发明人： MUELLER ULRICH , ECKENBERG PETER , GRUETZMANN RUDI , BISCHOFF HILMAR , DENZER DIRK , NIELSCH ULRICH
IPC分类号： A61K31/435 , A61K31/495 , A61K31/50 , A61K31/505 , A61K31/53 , A61P9/00 , A61P9/10 , C07D471/14 , C07D487/04
摘要： PROBLEM TO BE SOLVED: To obtain new pyridazino-, pyrimido-, pyrazino- and triazino-indoles, having characteristics effective in control, etc., of atheroselerosis and coronary heart diseases and useful as a medicine, etc. SOLUTION: The new compounds are represented by formula I [R and R form a (substituted) phenyl ring, a 5-8 membered (substituted) (oxo) cycloalkene ring, a (substituted) pyridyl ring, etc., together with double bond which bonds these groups; R and R form a group of formula II (R and R are each H, a group of carboxyl, a 1-6C alkoxy, a 1-6C alkyl, etc., a (substituted) pyridyl ring, etc., together with double bond; A and D is each H, a halogen, CF3 , OH, a 1-5C alkyl, a 1-5C alkoxy; E and L are each H, a 3-8C cycloalkyl, a (substituted) alkyl, a (substituted) phenyl, etc.; R is (substituted) phenyl, a (substituted) hetero ring, etc.; R is H, carboxyl, a 1-5C alkoxycarbonyl, a 1-6C (substituted) alkyl, etc.]. The compounds are useful as medicines, etc., for treating atherosclerosis, heart diseases, etc.

3. 发明专利

JPS62169790A DIHYDROPYRIDINE LACTOLS 失效
公开(公告)号：JPS62169790A
公开(公告)日：1987-07-25
申请号：JP19570486
申请日：1986-08-22
申请人： BAYER AG
发明人： GOLDMANN SIEGFRIED , BOSSERT FRIEDRICH , AHR HANS J , BISCHOFF HILMAR , PULS WALTER , PETZINNA DIETER , SCHLOSSMANN KLAUS , BENDER JOACHIM
IPC分类号： C07D307/33 , A61K31/435 , A61K31/4355 , A61K31/44 , A61P3/08 , A61P3/10 , C07D491/04 , C07D491/048

4. 发明申请

WO9804528A3 SUBSTITUTED PYRIDINES AND BIPHENYLS AS ANTI-HYPERCHOLESTERINEMIC, ANTI-HYPERLIPOPROTEINEMIC AND ANTI-HYPERGLYCEMIC AGENTS 审中-公开
标题翻译：作为抗高血压药物，抗高血压药物和抗高血压药物的替代吡啶和二苯醚
公开(公告)号：WO9804528A3
公开(公告)日：1999-11-11
申请号：PCT/US9713248
申请日：1997-07-29
申请人： BAYER AG , BAYER AG
发明人： SCHMIDT GUNTER , ANGERBAUER ROLF , BRANDES ARNDT , MULLER-GLIEMANN MATTHIAS , BISCHOFF HILMAR , SCHMIDT DELF , WOHLFEIL STEFAN , SCHOEN WILLIAM R , LADOUCEUR GAETAN H , COOK JAMES H II , LEASE TIMOTHY G , WOLANIN DONALD J , KRAMSS RICHARD H , HERTZOG DONALD L , OSTERHOUT MARTIN H
IPC分类号： C07C33/24 , A61K31/045 , A61K31/055 , A61K31/075 , A61K31/10 , A61K31/425 , A61K31/426 , A61K31/435 , A61K31/44 , A61K31/4409 , A61K31/4427 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/451 , A61K31/4545 , A61K31/47 , A61K31/496 , A61K31/5377 , A61P3/10 , C07C33/46 , C07C39/12 , C07C39/205 , C07C39/367 , C07C43/178 , C07C323/16 , C07C323/20 , C07D211/26 , C07D213/24 , C07D213/30 , C07D213/32 , C07D213/34 , C07D213/36 , C07D213/38 , C07D213/50 , C07D213/55 , C07D213/64 , C07D213/70 , C07D213/74 , C07D213/80 , C07D215/14 , C07D221/04 , C07D275/02 , C07D277/22 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/06 , C07D405/12 , C07D407/04 , C07D409/04 , C07D411/12 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/04 , C07D417/12 , C07D419/04 , C07D487/04 , C07D521/00 , C07F7/18
CPC分类号： C07D213/30 , C07D213/32 , C07D213/34 , C07D213/38 , C07D213/50 , C07D213/55 , C07D213/64 , C07D213/70 , C07D213/74 , C07D213/80 , C07D215/14 , C07D221/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D411/12 , C07D413/06 , C07D413/12 , C07D417/12 , C07D487/04 , C07F7/1856
摘要： Substituted pyridines of formula (IA) are produced by reaction of suitably substituted pyridylaldehydes with Grignard or Witting reagents, and the resulting products are appropriately reduced. The pyridines of formula (IA) are suitable as active compounds in pharmaceutical products, particularly in pharmaceutical products for the inhibition of cholesterol ester transfer proteins. 3-Heteroalkyl-aryl-substituted pyridines of formula (IB) are produced from pyridines which are correspondingly protected at the hydroxy group and correspondingly substituted. The compounds of formula (IB) according to the invention are suitable as active compounds in pharmaceutical products, particularly pharmaceutical products for the treatment of hyperlipoproteinemia. Substituted pyridines and benzenes of formula (IC) are produced by procedures disclosed herein, and are useful as active ingredients in pharmaceutical products, particularly pharmaceutical products for inhibition of the glucagon receptor, leading to treatment of glucagon-mediated conditions such as diabetes.
摘要翻译：式（IA）的取代的吡啶通过适当取代的吡啶基醛与格氏试剂或Witting试剂的反应制备，所得产物适当地还原。式（IA）的吡啶适合作为药物产品中的活性化合物，特别是用于抑制胆固醇酯转移蛋白的药物。式（IB）的3-杂芳烷基 - 芳基取代的吡啶由吡啶制备，其相应地被羟基保护并相应地被取代。根据本发明的式（IB）化合物适合作为药物产品中的活性化合物，特别是用于治疗高脂蛋白血症的药物。通过本文公开的方法制备式（IC）的取代的吡啶和苯，并且可用作药物产品中的活性成分，特别是用于抑制胰高血糖素受体的药物产品，导致治疗胰高血糖素介导的病症如糖尿病。

5. 发明申请

WO03028727A9 3-`HYDROXY-(-4-TRIFLUOROMETHYLPHENYL)-METHYL-7-SPIROCYCLOBUTYL-5,6,7,8-TETRAHYDROQUINOLIN-5-OL DERIVATIVES AND THE USE OF THE SAME AS CHOLESTEROL ESTER TRANSFER PROTEIN (CETP) INHIBITORS 审中-公开
标题翻译： 3- `HYDROXY-（4-三氟甲基苯基）-7-甲基SPIROCYCLOBUTYL -5,6,7,8-四氢喹啉-5-醇衍生物及其作为胆固醇酯转移蛋白（CETP） - 抑制剂
公开(公告)号：WO03028727A9
公开(公告)日：2003-11-13
申请号：PCT/EP0210444
申请日：2002-09-18
申请人： BAYER AG , GIELEN HEIKE , GOLDMANN SIEGFRIED , KELDENICH JOERG , PAULSEN HOLGER , SCHMECK CARSTEN , SIEGEL STEPHAN , BISCHOFF HILMAR , RAABE MARTIN , SCHMIDT DELF , FAESTE CHRISTIANE
发明人： GIELEN HEIKE , GOLDMANN SIEGFRIED , KELDENICH JOERG , PAULSEN HOLGER , SCHMECK CARSTEN , SIEGEL STEPHAN , BISCHOFF HILMAR , RAABE MARTIN , SCHMIDT DELF , FAESTE CHRISTIANE
IPC分类号： C07D215/20 , A61K31/47 , A61K31/4709 , A61P3/04 , A61P3/06 , A61P9/00 , A61P9/10 , A61P25/28 , A61P43/00 , C07D221/20 , C07D409/04 , A61K31/4747
CPC分类号： C07D221/20 , C07D409/04
摘要： The invention relates to substituted tetrahydroquinoline derivatives of formula (I), wherein A represents a radical (a), (b), (c), (d), (e), (f), (g), (h) or -(CH2)2CH3 and B represents a radical (f) or (h), and to the salts of the same. The invention also relates to a method for producing said substances and to the use thereof in pharmaceuticals.
摘要翻译：所需的登记涉及其中A代表基团或取代的四氢喹啉衍生物（I） - （CH 2）2 CH 3，B表示其制备方法和其医药用途的基团和它们的盐，流程。

6. 发明申请

WO0228821A3 PROPIONIC ACID DERIVATIVES WITH PPAR-ALPHA ACTIVATING PROPERTIES 审中-公开
标题翻译：具有PPAR-α活化性能的丙酸衍生物。
公开(公告)号：WO0228821A3
公开(公告)日：2002-08-15
申请号：PCT/EP0111005
申请日：2001-09-24
申请人： BAYER AG , URBAHNS KLAUS , WOLTERING MICHAEL , NIKOLIC SUSANNE , PERNERSTORFER JOSEF , HINZEN BERTHOLD , DITTRICH-WENGENROTH ELKE , BISCHOFF HILMAR , HIRTH-DIETRICH CLAUDIA , LUSTIG KLEMENS
发明人： URBAHNS KLAUS , WOLTERING MICHAEL , NIKOLIC SUSANNE , PERNERSTORFER JOSEF , HINZEN BERTHOLD , DITTRICH-WENGENROTH ELKE , BISCHOFF HILMAR , HIRTH-DIETRICH CLAUDIA , LUSTIG KLEMENS
IPC分类号： C07C237/00 , A61K31/192 , A61K31/196 , A61K31/216 , A61K31/341 , A61K31/381 , A61K31/421 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P9/12 , A61P35/00 , C07C229/18 , C07C229/34 , C07C237/04 , C07C237/08 , C07C237/20 , C07C317/10 , C07C317/28 , C07C323/32 , C07C323/52 , C07C323/58 , C07D263/32 , C07D307/52 , C07D333/20 , A61K31/165 , C07C229/14 , C07C229/36 , C07C317/18 , C07C333/20
CPC分类号： C07D263/32 , C07C229/18 , C07C229/34 , C07C237/04 , C07C317/28 , C07C323/52 , C07C2601/14 , C07D307/52 , C07D333/20
摘要： The invention relates to the PPAR-alpha activating compounds of general formula (I), for treating for example coronary heart diseases, and to a method for producing said compounds, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, A and X are defined as in claim 1.
摘要翻译：本申请涉及PPAR-α活化通式（I）的化合物用于治疗例如冠状心脏疾病，以及它们的制备，其中变量R 1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R11 ，R13，R12 A和X具有权利要求中给出的含义。1

7. 发明申请

WO0119357A3 COMBINATION PREPARATION FOR THE TREATMENT OF SEXUAL DYSFUNCTION 审中-公开
标题翻译：复合制剂，性功能障碍的治疗
公开(公告)号：WO0119357A3
公开(公告)日：2001-09-27
申请号：PCT/EP0008836
申请日：2000-09-11
申请人： BAYER AG , BISCHOFF ERWIN , BISCHOFF HILMAR , GIULIANO FRANCOIS
发明人： BISCHOFF ERWIN , BISCHOFF HILMAR , GIULIANO FRANCOIS
IPC分类号： A61K45/06 , A61K31/00 , A61P15/10
CPC分类号： A61K45/06
摘要： Disclosed is a combination preparation for the treatment of sexual dysfunction in men or women containing at least one active ingredient A and one active ingredient B as pharmaceutically active ingredients, whereby the active ingredient A is a PDE inhibitor, preferably a cGMP PDE inhibitor and the active ingredient B a lipid-reducing agent. Both the active ingredients A and B can be administered simultaneously or at alternate intervals, that is, as a functional unit or separated from each other.
摘要翻译：我们将描述用于在人或含有妇女，作为药物活性成分的至少一种活性化合物组分A和至少一种活性化合物组分B，其中，所述活性化合物组分A是PDE抑制剂，优选的cGMP PDE抑制剂和活性组分的治疗性功能障碍的组合制剂 B是降脂剂。两种活性化合物的组分A和B可以同时或依次但是被施加，即功能单元或彼此独立地存在。

8. 发明申请

WO0197787A3 USE OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN (MTP) INHIBITORS FOR REDUCING THE NUMBER OF POSTPRANDIAL TRIGLYCERIDE-RICH LIPOPROTEIN PARTICLES (PPTRL) 审中-公开
标题翻译： MTP抑制剂的减少PPTRL的使用
公开(公告)号：WO0197787A3
公开(公告)日：2002-11-14
申请号：PCT/EP0106526
申请日：2001-06-08
申请人： BAYER AG , GRUETZMANN RUDI , MUELLER ULRICH , BISCHOFF HILMAR , ZAISS SIEGFRIED
发明人： GRUETZMANN RUDI , MUELLER ULRICH , BISCHOFF HILMAR , ZAISS SIEGFRIED
IPC分类号： C07D275/06 , A61K31/4035 , A61K31/404 , A61K31/4164 , A61K31/4184 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/5025 , A61K31/519 , A61K31/522 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/50 , A61P7/00 , A61P9/00 , A61P25/28 , A61P43/00 , C07D209/08 , C07D209/48 , C07D235/08 , C07D235/18 , C07D235/28 , C07D401/04 , C07D417/04 , C07D471/04 , C07D473/08 , C07D487/04 , A61K31/435
CPC分类号： A61K31/437
摘要： The invention relates to the use of inhibitors of the microsomal triglyceride transfer protein (MTP) for reducing the number of postprandial triglyceride-rich lipoprotein particles (ppTRL) or for reducing their decomposition products i.e. the cholesterol-rich "small remnant particle" (remnants). Said particles are associated with apolipoprotein B-48 (ApoB-48) and are designated as "ppTRL" in the further course of events.
摘要翻译：本发明涉及使用该微粒体甘油三酯转移蛋白（MTP）抑制剂，以降低餐后富含甘油三酯的脂蛋白颗粒（ppTRL）或降低胆固醇更丰富的“小残余颗粒”的它们的降解产物（遗留）。表示，与载脂蛋白B-48（载脂蛋白B-48）相关联，并且颗粒被进一步称为“ppTRL”。

9. 发明申请

WO0100183A3 COMBINATION OF MTP INHIBITORS AND HMG-CoA REDUCTASE INHIBITORS AND THE USE THEREOF IN MEDICAMENTS 审中-公开
标题翻译：组合MTP抑制剂和HMG-CoA还原酶抑制剂和它们在药物的
公开(公告)号：WO0100183A3
公开(公告)日：2001-05-10
申请号：PCT/EP0005410
申请日：2000-06-13
申请人： BAYER AG , GRUETZMANN RUDI , MUELLER ULRICH , BISCHOFF HILMAR
发明人： GRUETZMANN RUDI , MUELLER ULRICH , BISCHOFF HILMAR
IPC分类号： A61K31/437 , A61K31/22 , A61K31/366 , A61K31/40 , A61K31/405 , A61K31/44 , A61K31/519 , A61K45/06 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/04 , A61P9/10 , A61P13/12 , A61P43/00 , A61P9/00
CPC分类号： A61K45/06
摘要： The invention relates to the use of a combination consisting of at least one selected MTP inhibitor (constituent A) and of at least one HMG-CoA reductase inhibitor (constituent B) for fighting cardiovascular diseases. The invention also relates to medicaments containing this combination and to the production thereof.
摘要翻译：本发明涉及一种使用至少一个所选择的MTP抑制剂（组分A）和心血管障碍，包括这些的组合和它们的制备药物组合物的控制的HMG-CoA还原酶抑制剂（组分B）的组合。

10. 发明专利

BG103200A SUBSTITUTED PYRIDINES AND BIPHENYLS AS ANTIHYPERCHOLESTERINEMIC, ANTIHYPERLIPOPROTEINEMIC AND ANTIHYPERGLYCEMIC FORMULATIONS 未知
公开(公告)号：BG103200A
公开(公告)日：1999-11-30
申请号：BG10320099
申请日：1999-02-23
申请人： BAYER AG , BAYER AG
发明人： SCHMIDT GUNTER , ANGERBAUER ROLF , BRANDES ARNDT , MULLER-GLIEMAN MATTHIAS , BISCHOFF HILMAR , SCHMIDT DELF , WOHLFEIL STEFAN , SCHOEN WILLIAM R , LADOUCEUR GAETAN H , COOK JAMES , LEASE TIMOTHY G , OWLANIN DONALD J , KRAMSS RICHARD H , HERTZOG DONALD L , OSTERHOUT MARTIN H
IPC分类号： C07C33/24 , A61K31/045 , A61K31/055 , A61K31/075 , A61K31/10 , A61K31/425 , A61K31/426 , A61K31/435 , A61K31/44 , A61K31/4409 , A61K31/4427 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/451 , A61K31/4545 , A61K31/47 , A61K31/496 , A61K31/5377 , A61P3/10 , C07C33/46 , C07C39/12 , C07C39/205 , C07C39/367 , C07C43/178 , C07C323/16 , C07C323/20 , C07D211/26 , C07D213/24 , C07D213/30 , C07D213/32 , C07D213/34 , C07D213/36 , C07D213/38 , C07D213/50 , C07D213/55 , C07D213/64 , C07D213/70 , C07D213/74 , C07D213/80 , C07D215/14 , C07D221/04 , C07D275/02 , C07D277/22 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/06 , C07D405/12 , C07D407/04 , C07D409/04 , C07D411/12 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/04 , C07D417/12 , C07D419/04 , C07D487/04 , C07D521/00 , C07F7/18 , C07D213/20
摘要： The substituted pyridines with formula (IA) are produced inthe reaction between suitably substituted pyridylaldehydes andGrignar or Wittig reagents and respective reduction of theresulting products. Pyridines with formula (IA) can be applied asactive ingredients in pharmaceutical compositions and inparticular for the inhibition of the proteins transferring thecholesterol ester. The 3-heteroalkyl-aryl-substituted pyridineswith the formula (IB) are produced from pyridines which are dulyprotected in the hydroxy group and are duly substituted. They aresuitable as active ingredients in pharmaceutical compositions, inparticular for the treatment of hyperlipoproteinemia. Substitutedpyridines or benzenes with formula (IC) are produced by themethods revealed in the description and are suitable as activeingredients, in particular for the inhibition of glucagon receptorwhich on its turn results in the treatment of conditions resultingfrom the glucagon, such as diabetes. The compounds have generalformulae revealed in detail in the description.47 claims

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