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1. 发明申请

WO0222569A8 METHOD FOR PRODUCING CHIRAL COMPOUNDS 审中-公开
标题翻译：用于生产手性化合物
公开(公告)号：WO0222569A8
公开(公告)日：2002-06-13
申请号：PCT/EP0110626
申请日：2001-09-14
申请人： GRUENENTHAL GMBH , GERLACH MATTHIAS , PUETZ CLAUDIA , ENDERS D , GAUBE GERO
发明人： GERLACH MATTHIAS , PUETZ CLAUDIA , ENDERS D , GAUBE GERO
IPC分类号： C07C319/18 , A61P25/04 , C07B53/00 , C07B61/00 , C07C323/59 , C07C323/60 , A61K31/10
CPC分类号： C07C323/59 , C07B2200/07
摘要： The invention relates to a method for producing chiral compounds according to the condition of a 1.4 Michael reaction in addition to a compound of general formula (31) and the use thereof as an antalgic.
摘要翻译：本发明涉及用于制备通式（31）和它们作为止痛药使用的1,4-迈克尔加成和化合物的条件下的手性化合物。

2. 发明申请

WO0158875A3 SUBSTITUTED 1,2,3,4- TETRAHYDROQUINOLINE-2-CARBOXYLIC ACID DERIVATIVES 审中-公开
标题翻译：取代的1,2,3,4-四氢喹啉-2-羧酸衍生物
公开(公告)号：WO0158875A3
公开(公告)日：2002-01-24
申请号：PCT/EP0100588
申请日：2001-01-19
申请人： GRUENENTHAL GMBH , GERLACH MATTHIAS , PRZEWOSNY MICHAEL , ENGLBERGER WERNER , REISSMUELLER ELKE , BLOMS FUNKE PETRA , MAUL CORINNA , JAGUSCH UTZ PETER
发明人： GERLACH MATTHIAS , PRZEWOSNY MICHAEL , ENGLBERGER WERNER , REISSMUELLER ELKE , BLOMS-FUNKE PETRA , MAUL CORINNA , JAGUSCH UTZ-PETER
IPC分类号： A61K31/47 , A61K31/4709 , A61K31/473 , A61K31/4741 , A61K31/4743 , A61P1/04 , A61P1/12 , A61P3/10 , A61P9/00 , A61P11/00 , A61P11/14 , A61P13/02 , A61P19/10 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P25/32 , A61P25/34 , A61P25/36 , A61P27/06 , A61P27/16 , A61P29/00 , A61P37/08 , C07D215/48 , C07D221/16 , C07D221/18 , C07D221/22 , C07D405/04 , C07D491/04 , C07D491/048 , C07D495/04
CPC分类号： C07D221/22 , C07D215/48 , C07D221/16 , C07D221/18 , C07D405/04 , C07D491/04 , C07D495/04
摘要： The invention concerns substituted 1,2,3,4- tetrahydroquinoline-2-carboxylic acid derivatives, a method for the production of said derivatives, their use in the production of medicaments and medicaments containing said compounds.
摘要翻译：本发明涉及取代的1,2,3,4-四氢喹啉-2-羧酸衍生物，以及它们的制备方法，其用于制备医药品，含有这些化合物的药物组合物的用途。

3. 发明申请

WO0147866A9 SUBSTITUTED 1 AND 2 NAPHTHOL MANNICH BASES 审中-公开
标题翻译：取代的1-和2-萘酚的曼尼希碱
公开(公告)号：WO0147866A9
公开(公告)日：2002-11-07
申请号：PCT/EP0012972
申请日：2000-12-20
申请人： GRUENENTHAL GMBH , GERLACH MATTHIAS , MAUL CORINNA
发明人： GERLACH MATTHIAS , MAUL CORINNA
IPC分类号： C07D295/08 , A61K31/137 , A61K31/166 , A61K31/167 , A61K31/18 , A61K31/195 , A61K31/24 , A61K31/4453 , A61K31/5375 , A61P1/04 , A61P1/12 , A61P3/04 , A61P9/00 , A61P11/06 , A61P13/00 , A61P25/00 , A61P25/06 , A61P25/24 , A61P25/30 , A61P25/32 , A61P27/06 , A61P29/00 , A61P37/08 , C07B61/00 , C07C213/02 , C07C213/10 , C07C215/50 , C07C215/86 , C07C217/58 , C07C219/28 , C07C221/00 , C07C225/16 , C07C227/10 , C07C227/40 , C07C229/38 , C07C237/48 , C07C243/38 , C07C303/40 , C07C303/44 , C07C311/37 , C07D295/096 , C07D295/135 , C07D295/155 , A61K31/136 , A61K31/16 , A61K31/165 , A61P25/04 , C07D295/12 , C07D295/14
CPC分类号： C07D295/096 , C07C215/50 , C07C217/58 , C07C219/28 , C07C225/16 , C07C229/38 , C07C237/48 , C07C243/38 , C07C311/37 , C07D295/135 , C07D295/155
摘要： The invention relates to substituted 1 and 2 naphthol Mannich bases, a method for the production thereof, medicaments containing said compounds and the use of said compounds in the production of medicaments.
摘要翻译：本发明涉及取代的1-和2-萘酚的曼尼希碱，其制备方法，包含这些化合物和用于生产药物的用途，这些化合物的药物组合物。

4. 发明申请

WO0147882A3 SUBSTANCE LIBRARY WHICH CAN BE OBTAINED BY REACTING ALDEHYDES WITH SECONDARY AMINES, ACID CHLORIDES AND NAPHTHOL, PYRROLE AND/OR INDOLE COMPOUNDS 审中-公开
标题翻译：物质LIBRARY可通过醛与仲胺的执行，和酰基氯萘酚，吡咯和/或吲哚化合物
公开(公告)号：WO0147882A3
公开(公告)日：2002-05-30
申请号：PCT/EP0012973
申请日：2000-12-20
申请人： GRUENENTHAL GMBH , GERLACH MATTHIAS , MAUL CORINNA
发明人： GERLACH MATTHIAS , MAUL CORINNA
IPC分类号： B01J19/00 , C07D209/00 , C07D209/14 , C07C217/58 , C07C219/28 , C07D207/32 , C07D209/42 , C07D295/08 , C07D401/06
CPC分类号： C07D209/00 , B01J19/0046 , B01J2219/00691 , B01J2219/0072
摘要： The invention relates to a substance library which can be obtained by reaction of aromatic aldehyde compounds and/or heteroaromatic aldehyde compounds and/or aliphatic aldehyde compounds without an acid proton in a-position in a solution in the presence of a base with secondary amines to produce aminal compounds; reaction of said aminal compounds without any further purification with acid chlorides in an absolute solvent to produce iminium salts; reaction thereof without any further purification in an organic solvent with unsubstituted or substituted naphthol, pyrrole and/or indole compounds; purification and isolation of the compounds thus obtained according to the usual methods and optionally, reaction of the naphthol and/or indol compounds thus obtained in a solution with organic halogen compounds in the presence of a base and optionally, purification by filtration and isolation of the naphthol and/or indol compounds thus obtained according to the usual methods. The invention also relates to the use of said substance library for the detection of active ingredients.
摘要翻译：本发明涉及一种可用的由芳族醛化合物和/或杂芳族醛化合物和/或脂族醛化合物而无需在一个位置酸性质子的反应的物质库，在溶液中，在与仲胺碱的存在下反应得到缩醛胺化合物，Umsetzsung而不进一步纯化这些缩醛胺化合物在绝对溶剂，得到亚胺盐和它们的不经进一步纯化在有机溶剂中反应的酰氯具有未取代的或取代的萘酚，吡咯，和/或由此获得的萘酚吲哚化合物，纯化并由此通过常规方法得到的化合物的分离，和任选地反应 - 和/或吲哚在通过过滤与有机卤素化合物的溶液中，在碱的存在下，并且如果合适的纯化的萘酚化合物，和分离因此，根据通常的甲基获得和/或吲哚化合物关东煮，以及使用这种物质库来筛选药物。

5. 发明申请

WO0127118A3 BICYCLIC IMIDAZO-5-YL-AMINE DERIVATIVES 审中-公开
标题翻译：双环咪唑-5-基阿明衍生物
公开(公告)号：WO0127118A3
公开(公告)日：2001-09-20
申请号：PCT/EP0009097
申请日：2000-09-18
申请人： GRUENENTHAL GMBH , GERLACH MATTHIAS , MAUL CORINNA
发明人： GERLACH MATTHIAS , MAUL CORINNA
IPC分类号： C07D513/00 , A61K31/4188 , A61K31/4196 , A61K31/429 , A61P25/02 , C07B61/00 , C07D471/04 , C07D487/04 , C07D513/04 , C07F9/6561 , A61K31/41 , A61P25/00 , A61P43/00 , C07D285/00
CPC分类号： C07D471/04 , C07D487/04 , C07D513/04 , C07F9/6561 , C40B40/00
摘要： The invention relates to novel bicyclic imidazo-5-yl-amine derivatives of general formula (I), whereby X represents CR , N or S, and; Y represents CR or N, in the case that X represents S, and in all other cases, Y represents N.
摘要翻译：新的双环咪唑-5-基胺的通式（I），其中X为CR <5>，N或S，且Y为X为S，CR的情况下<6>或N，并且在所有其它情况下表示N ，

6. 发明申请

WO02072585A3 SUBSTITUTED PYRAZOLOPYRIMIDINES AND THIAZOLOPYRIMIDINES USED AS ANALGESICS 审中-公开
标题翻译：取代的吡唑和噻唑并嘧啶镇痛
公开(公告)号：WO02072585A3
公开(公告)日：2003-02-20
申请号：PCT/EP0202722
申请日：2002-03-13
申请人： GRUENENTHAL GMBH , GERLACH MATTHIAS , MAUL CORINNA , JAGUSCH UTZ-PETER , SUNDERMANN BERND , FUHR MARTIN , IJZERMAN ADRIAAN P , DISSEN-DE GROOTE MIRIAM , UNIV LEIDEN
发明人： GERLACH MATTHIAS , MAUL CORINNA , JAGUSCH UTZ-PETER , SUNDERMANN BERND , FUHR MARTIN , IJZERMAN ADRIAAN P , DISSEN-DE GROOTE MIRIAM
IPC分类号： A61K31/4745 , A61K31/4985 , A61K31/519 , A61P9/00 , A61P9/06 , A61P11/00 , A61P13/02 , A61P13/12 , A61P17/06 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/20 , A61P25/28 , A61P27/06 , A61P29/00 , A61P35/00 , A61P37/00 , C07D471/14 , C07D487/04 , C07D495/04 , C07D513/04 , A61K31/505
CPC分类号： C07D487/04 , C07D513/04
摘要： The invention relates to substituted pyrazolopyrimidines and thiazolopyrimidines with the general structures (I A), (I B) and (II), to a method for their production, to substance libraries containing the same, to medicaments containing said compounds, to the use of said compounds in the production of medicaments for treating pain, epilepsy, schizophrenia, neurodegenerative diseases, in particular Alzheimer's disease, Huntington's disease and Parkinson's disease, for treating cerebral ischaemia and infarcts, psychosis caused by increased amino acid levels, cerebral oedema, conditions caused by an under-supply of the central nervous system, in particular in hypoxia, especially newborn hypoxia and anoxia, for treating AIDS-related dementia, encephalomyelitis, Tourette's syndrome, perinatal asphyxia, tinnitus, neuropathic pain, diseases of the respiratory tract, cancer, cardiac arrythmia, immune disorders and diseases, inflammatory conditions and diseases, renal shutdown, dyssomnia, strokes, thromboses, urinary incontinence, diabetes, psoriasis, septicaemic shock, cerebral traumas, glaucoma and/or congestive heart failure. The invention further relates to pharmaceutical compositions containing said compounds.
摘要翻译：本发明涉及取代的吡唑噻唑并嘧啶和一般结构式（I A），（I B）和（II）。用于容纳物质库其制备方法，组合物的方法，含有这些化合物的药物组合物中，使用这些化合物用于制备药物的疼痛，癫痫，精神分裂症，神经变性疾病，特别是阿尔茨海默氏病，亨廷顿氏病和帕金森氏病，脑局部缺血的治疗和梗塞，通过升高的氨基酸水平，脑水肿，中枢神经系统的机能不全状态，特别是在hypoxias，特别是新生儿缺氧和缺氧，AIDS痴呆，脑脊髓炎，图雷特综合征的，围产期窒息，耳鸣，neurophathischem疼痛带来精神病，呼吸系统疾病，癌症，心律失常，免疫紊乱和疾病，炎症性的病症，神经变性疾病，帕金森氏病，肾功能衰竭，精神分裂症，睡眠障碍，中风，血栓形成，尿失禁，Diabeter，诗 oriasis，脓毒性休克，脑外伤，青光眼和/或充血性心脏衰竭，以及含有它们的这些药物组合物。

7. 发明申请

WO0127109A3 TERT.-BUTYL-(7-METHYL-IMIDAZO[1,2-A]PYRIDINE-3-YL)-AMINE DERIVATIVES 审中-公开
标题翻译： TERT。丁基（7-甲基咪唑并[1,2-a]吡啶-3-基） - 胺衍生物

公开(公告)号：WO0127109A3

公开(公告)日：2001-09-20

申请号：PCT/EP0009791

申请日：2000-10-06

申请人： GRUENENTHAL GMBH , MAUL CORINNA , SUNDERMANN BERND , HENNIES HAGEN HEINRICH , SCHNEIDER JOHANNES , GERLACH MATTHIAS

发明人： MAUL CORINNA , SUNDERMANN BERND , HENNIES HAGEN-HEINRICH , SCHNEIDER JOHANNES , GERLACH MATTHIAS

IPC分类号： C07D471/00 , A61K31/437 , A61P3/10 , A61P9/10 , A61P17/02 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/04 , A61P43/00 , C07B61/00 , C07D471/04 , C07D487/04 , C07D513/04 , C07F9/6561 , A61K31/435

CPC分类号： C07D471/04 , C07D487/04 , C07D513/04 , C07F9/6561 , C40B40/00

摘要： The invention relates to tert. -butyl-(7-methyl-imidazo[1,2-a]pyridine-3-yl)-amine derivatives of the general structure (I), to a method for the preparation thereof and to medicaments that contain said compounds. The invention further relates to the use of the inventive tert. -butyl-(7-methyl-imidazo[1,2-a]pyridine-3-yl)-amine derivatives in the production of a medicament for the inhibition of the NO synthase and for the treatment of inter alia migraine and to pharmaceutical compositions that contain tert. -butyl-(7-methyl-imidazo[1,2-a]pyridine-3-yl)-amine derivatives.

摘要翻译：本发明涉及的叔丁基（7-甲基咪唑并[1,2-a]吡啶-3-基）通式结构（I），它们的制备方法的胺衍生物，含有这些化合物中，使用本发明的叔的丁基的（7-甲基咪唑并[1,2-a]吡啶-3-基） - 胺衍生物用于制造药物组合物药物中的NO合成酶抑制和治疗，特别是偏头痛以及含有的叔丁基（7-甲基咪唑并[1,2-a]吡啶-3-基） - 胺衍生物的药物组合物。

8. 发明申请

WO0127119A3 SUBSTANCE LIBRARY CONTAINING BICYCLIC IMIDAZO-5-YL-AMINES AND/OR BICYCLIC IMIDAZO-3-YL-AMINES 审中-公开
标题翻译：含双环咪唑-5-基 - 胺和/或双环咪唑-3-基 - 胺的亚麻三嗪类
公开(公告)号：WO0127119A3
公开(公告)日：2001-10-11
申请号：PCT/EP0009098
申请日：2000-09-18
申请人： GRUENENTHAL GMBH , GERLACH MATTHIAS , MAUL CORINNA
发明人： GERLACH MATTHIAS , MAUL CORINNA
IPC分类号： C07D471/00 , A61K31/437 , A61P3/10 , A61P9/10 , A61P17/02 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/04 , A61P43/00 , C07B61/00 , C07D471/04 , C07D487/04 , C07D513/04 , C07F9/6561 , A61K31/435
CPC分类号： C07D471/04 , C07D487/04 , C07D513/04 , C07F9/6561 , C40B40/00
摘要： The invention relates to a substance library containing bicyclic imidazo-5-yl-amines and/or bicyclic imidazo-3-yl-amines of general formula (I) or (II), to a method for producing this substance library, and to the use of substances from this substance library for producing a medicament used to treat pain.
摘要翻译：含有双环咪唑-5-基胺和/或双环通式（I）或（II）中，用于生产这种物质库和使用的物质从该物质库制造过程的咪唑-3-基 - 胺物质库用于治疗疼痛的药物。

9. 发明申请

WO0147878A8 SUBSTITUTED PYRROLE MANNICH BASES TO COMBAT PAIN AND ALLERGIC REACTIONS 审中-公开
标题翻译：取代吡咯曼尼期碱进行战斗疼痛和过敏反应
公开(公告)号：WO0147878A8
公开(公告)日：2001-10-04
申请号：PCT/EP0012976
申请日：2000-12-20
申请人： GRUENENTHAL GMBH , GERLACH MATTHIAS , MAUL CORINNA
发明人： GERLACH MATTHIAS , MAUL CORINNA
IPC分类号： A61K31/401 , A61K31/4453 , A61K31/5377 , A61P1/04 , A61P1/12 , A61P3/04 , A61P9/00 , A61P11/06 , A61P13/02 , A61P25/04 , A61P25/06 , A61P25/14 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/32 , A61P27/06 , A61P29/00 , A61P37/08 , C07D207/32 , C07D207/335 , C07D401/06 , C07D405/04 , C07D407/04 , C07D207/00
CPC分类号： C07D207/335 , C07D401/06 , C07D407/04
摘要： The invention relates to substituted pyrrole Mannich bases of general formula (I), wherein R =H, a C 1-10-alkyl-, aryl, a heteroaryl- or an aryl, heteroaryl-, CN, Br-, C1 or OH radical bound by a C 1-6 alkylene group, R =CH(R )N(R )(R ), R3, R3', R3'' identically or individually represent H, F, C1, Br, CF3, CN, NO2, SO2NH2, NHR ,SR , OR , CO(OR ), CH CO(OR ), COR , a C 1-10-alkyl-, aryl-, heteroaryl- aryl radical or a heteroalkyl radical bound by a C 1-6 alkylene group, R = an unsubstituted phenyl radical or a phenyl radical substituted at least with C 1-4 alkyl, C 1-3-alkoxy-, halogen-, a method for the production of the above-mentioned compounds, medicaments containing said compounds, and the use of said compounds in the production of medicaments. Said active ingredients are particularly suitable for pain therapy, and for treating inflammatory and allergic reactions, drug or alcohol abuse, diarrhoea, gastritis, ulcers, cardiovascular diseases, urinary incontinence, depressions, states of shock, migranes, narcolepsy, overweight, asthma, glaucoma, hyperkinetic syndrome, lack of drive, bulimia, anorexia, catalepsia, anxiolysis, increasing vigilance and/or increasing libido.
摘要翻译：本发明涉及通式（I）取代的吡咯曼尼希碱，其中R <1> = H，C1-10的烷基，芳基，杂芳基或通过一个C 1-6 - 亚烷基键合的芳基指杂芳基，CN，Br，Cl或OH基团，R <2> = CH（R <4>）N（R <5>）的装置（R <6>），R <3>， [R <3 '>，R <3'>，相同或不同，是H，F，氯，溴，CF 3，CN，NO 2，SO 2 NH 2，NHR <7>，SR <8>或<9>，CO（或<10>），CH 2 CO（或<11>）COR <15>，一个C 1-10烷基，芳基，杂芳基或通过一个C 1-6亚烷基芳基或杂芳基键合的基，R <4> =未取代的苯基残基或可选地至少单取代的C 1-4 - 烷基，C 1-3 - 烷氧基，卤素，CF 3，CN，O-苯基或OH苯基激进。它们的制备方法，包含这些化合物和用于生产药物的用途，这些化合物的药物组合物。这些活性成分特别适用于治疗疼痛和炎症和过敏性反应，药物和/或酒精滥用，腹泻，胃炎，溃疡，心血管疾病，尿失禁，抑郁症，休克，偏头痛，发作性睡病，肥胖症，哮喘，青光眼，运动机能亢进综合症的状态的治疗，缺乏驱动，贪食症，厌食症，强直性昏厥，适合抗焦虑，用于提高警觉和/或用于增加性欲。

10. 发明申请

WO0127110A3 BICYCLIC IMIDAZO-3-YL-AMINE DERIVATIVES WHICH ARE SUBSTITUTED ON THE SIXTH RING 审中-公开
标题翻译：六环取代，双环咪唑并-3-基阿明衍生物
公开(公告)号：WO0127110A3
公开(公告)日：2001-09-20
申请号：PCT/EP0009095
申请日：2000-09-18
申请人： GRUENENTHAL GMBH , GERLACH MATTHIAS , MAUL CORINNA
发明人： GERLACH MATTHIAS , MAUL CORINNA
IPC分类号： C07D487/00 , A61K31/437 , A61K31/4745 , A61K31/519 , A61P25/04 , A61P43/00 , C07B61/00 , C07D471/04 , C07D487/04 , C07D513/04 , C07F9/6561 , A61K31/435 , A61K31/495 , A61K31/505 , A61K31/53 , A61P25/00
CPC分类号： C07D471/04 , C07D487/04 , C07D513/04 , C07F9/6561 , C40B40/00
摘要： The invention relates to bicyclic imidazo-3-yl-amines of general formula (I) which are provided in the form of bases or of pharmaceutically acceptable salts thereof. The invention also relates to methods for producing the bicyclic imidazo-3-yl-amines and to medicaments containing, as an active ingredient, at least one bicyclic imidazo-3-yl-amine of general formula (I) provided in the form of the base or of a pharmaceutically acceptable salt.
摘要翻译：双环咪唑-3-基 - 胺的通式（I）的，在碱或其药学上可接受的盐的形式，它们的制备方法和含有作为Wikstoff至少一个双环通式咪唑-3-基 - 胺的药物（I）以碱或可药用盐的形式。

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