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1. 发明专利

JPH08225569A BENZYL PIPERIDINE DERIVATIVE 失效
公开(公告)号：JPH08225569A
公开(公告)日：1996-09-03
申请号：JP28344695
申请日：1995-10-31
申请人： MERCK PATENT GMBH
发明人： PRUECHER HELMUT , GOTTSCHLICH RUDOLF , LEIBROCK JOACHIM , SCHWARTZ HARRY
IPC分类号： C07D413/12 , A61K31/4427 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/55 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/28 , A61P43/00 , C07D401/06 , C07D401/12 , C07D403/12 , C07D413/06 , C07D417/06
摘要： Benzyl substd. piperidinoalkyl heterobicyclyl ketones and alcohols and their salts are new: R = H; halo; or NO2; R = 2-, 3- or 4-benzyl opt. ring substd. by halo; R = H or A; A = 1-6C alkyl; B = O or (H)(OH); halo = F, Cl, Br or I; n = 0-2; X = CO or SO2; Y = CH2; NH; O; S; or CO when X = CO and Z = NH or NA; and Z = CH2; C(A)2; CH2-CH2; CH=CH; CO; NH; O; or a bond; and 1 of X, Y and Z can be O, S or NH; cpds. are excluded when R = 4-benzyl, X = CO, Y = Z = CH2 and R =H; and when X-Y or Y-Z = -O-O-, -S-S-, -NH-O-, -O-NH-, -NH-NH-, -O-S- or -S-O.

2. 发明申请

WO0158893A2 INDOL-3-YL DERIVATIVES 审中-公开
标题翻译：吲哚-3-基衍生物
公开(公告)号：WO0158893A2
公开(公告)日：2001-08-16
申请号：PCT/EP0100084
申请日：2001-01-05
申请人： MERCK PATENT GMBH , GOODMAN SIMON , GOTTSCHLICH RUDOLF , WIESNER MATTHIAS
发明人： GOODMAN SIMON , GOTTSCHLICH RUDOLF , WIESNER MATTHIAS
IPC分类号： C07D401/06 , A61K31/405 , A61K31/4178 , A61K31/4184 , A61K31/4439 , A61K31/506 , A61P7/02 , A61P9/00 , A61P9/10 , A61P19/02 , A61P19/10 , A61P25/00 , A61P27/02 , A61P29/00 , A61P31/00 , A61P35/00 , A61P43/00 , C07D209/18 , C07D209/20 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D409/06 , C07D417/06 , C07D417/14
CPC分类号： C07D401/12 , C07D209/18 , C07D403/12 , C07D417/14
摘要： Indol-3-yl derivatives of general formula (I), wherein A, B, X, R , R , R , R , R , n or m have the meanings given in Claim 1, and the physiologically unobjectionable salts or solvates thereof are integrin inhibitors and can be used for combating thrombosis, myocardial infarcts, coronary heart diseases, arteriosclerosis, inflammations, tumours, osteoporosis, rheumatic arthritis, macular degenerative diseases, diabetic retinopathy, infections and restenosis after angioplasty or in the event of pathological actions which are maintained or propagated by angiogenesis.
摘要翻译：通式（I）其中A，B，X，R <1>，R <2>，R <3>，R <4>，R <5>，N或者M的吲哚-3-基衍生物在根据权利要求1名的含义已经描述，以及它们的生理学可接受的盐或溶剂化物是整联蛋白抑制剂，并且可以用于防治血栓形成，心肌梗死，冠状动脉心脏疾病，动脉硬化，炎症，肿瘤，骨质疏松症，风湿性关节炎，黄斑变性疾病，糖尿病性视网膜病，感染和术后再狭窄用于血管成形术或在其通过血管发生维持或繁殖的病理过程。

3. 发明专利

CA2399813C INDOL-3-YL DERIVATIVES 未知
公开(公告)号：CA2399813C
公开(公告)日：2010-03-09
申请号：CA2399813
申请日：2001-01-05
申请人： MERCK PATENT GMBH
发明人： WIESNER MATTHIAS , GOODMAN SIMON , GOTTSCHLICH RUDOLF
IPC分类号： C07D401/06 , C07D401/12 , A61K31/404 , A61K31/405 , A61K31/4178 , A61K31/4184 , A61K31/4439 , A61K31/506 , A61P7/02 , A61P9/00 , A61P9/10 , A61P19/02 , A61P19/10 , A61P25/00 , A61P27/02 , A61P29/00 , A61P31/00 , A61P35/00 , A61P43/00 , C07D209/18 , C07D209/20 , C07D401/14 , C07D403/06 , C07D403/12 , C07D409/06 , C07D417/06 , C07D417/14
摘要： Indol-3-yl derivatives of the general formula I (see formula I) in which A, B, X, R1, R2, R3, R4, R5, n and m are as defined in Patent Claim 1, and their physiologically acceptable salts or solvates are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart diseases, arteriosclerosis, inflammations, tumours, osteoporosis, rheumatic arthritis, macular degenerative disease, diabetic retinopathy, infections and restenosis after angioplasty or in pathological processes maintained or propagated by angiogenesis.

4. 发明专利

CA2302669C PIPERIDINYLMETHYLOXAZOLIDINONE DERIVATIVE 未知
公开(公告)号：CA2302669C
公开(公告)日：2008-04-22
申请号：CA2302669
申请日：1998-08-26
申请人： MERCK PATENT GMBH
发明人： GOTTSCHLICH RUDOLF , SEYFRIED CHRISTOPH , BARTOSZYK GERD , LEIBROCK JOACHIM , PRUCHER HELMUT
IPC分类号： C07D413/06 , A61K31/42 , A61K31/4453 , A61K31/454 , A61P9/10 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/28 , C07D211/00 , C07D263/00
摘要： The invention relates to the compound 5-[4-(4-fluorobenzyl)-piperidin-1- ylmethyl] -3-(4-hydroxyphenyl)-oxazolidin-2-one of formula (I), and to its physiologically suitable salts. The Inventive compou nd acts as a neuroleptic.

5. 发明专利

AU2001278457B2 Heterocyclic aminoalkyl pyridine derivatives as psychopharmaceuticals 未知
公开(公告)号：AU2001278457B2
公开(公告)日：2006-10-19
申请号：AU2001278457
申请日：2001-06-19
申请人： MERCK PATENT GMBH
发明人： BARTOSZYK GERD , ARLT MICHAEL , SEYFRIED CHRISTOPH , HARTING JURGEN , BOTTCHER HENNING DR , GOTTSCHLICH RUDOLF , DORSCH DIETER
IPC分类号： C07D401/12 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61P5/00 , A61P5/06 , A61P9/00 , A61P9/10 , A61P9/12 , A61P15/08 , A61P15/10 , A61P15/12 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D213/38 , C07D213/64 , C07D405/12 , C07D417/12
摘要： The invention relates to heterocyclic aminoalkylpyridine derivatives of the formula I: where R 1 is the radical of a heterocycle having 1 to 3 ring structures, where each ring structure is saturated, unsaturated or aromatic and optionally fused to other ring structures to give a fused ring system and the heterocycle has a total of 1 to 4 N, O and/or S atoms in the ring structures and is optionally monosubstituted, disubstituted or trisubstituted by one or more of the groups -A, -OR 4 , -N(R 4 ) 2 , -NO 2 , -CN, Hal, -COOR 4 , -CON(R 4 ) 2 , -COR 4 , -O; R 2 is a phenyl group which is optionally monosubstituted, disubstituted, trisubstituted, tetrasubstituted or pentasubstituted by one or more of the groups Hal, -A, -O-A, -NO 2 or -CN, or is a thienyl group which is optionally monosubstituted or disubstituted by one or more of the groups Hal, -A, -O-A, -NO 2 , -CN or thienyl; R 3 is H, -A, -CO-A, -C(R 4 ) 2 R 2 , -C(R 4 ) 2 -pyridinediyl-R 2 ; R 4 is H or -A; A is C 1 -C 6 -alkyl, where 1 to 7 hydrogen atoms are optionally replaced by fluorine; -X- is -O-, -S-, sulfinyl, sulfonyl, -C(R 4 ) 2 -; -Y- is -[C(R 4 ) 2 ] n -; -Z- is -C(R 4 ) 2 -; Hal is F, Cl, Br or I; n is 1, 2, 3 or 4; and their tolerable salts and solvates and their use as medicaments.

6. 发明专利

AU2001231664C1 Indol-3-yl derivatives 未知
公开(公告)号：AU2001231664C1
公开(公告)日：2006-10-05
申请号：AU2001231664
申请日：2001-01-05
申请人： MERCK PATENT GMBH
发明人： GOTTSCHLICH RUDOLF , WIESNER MATTHIAS , GOODMAN SIMON
IPC分类号： C07D401/06 , C07D401/12 , A61K31/404 , A61K31/405 , A61K31/4178 , A61K31/4184 , A61K31/4439 , A61K31/506 , A61P7/02 , A61P9/00 , A61P9/10 , A61P19/02 , A61P19/10 , A61P25/00 , A61P27/02 , A61P29/00 , A61P31/00 , A61P35/00 , A61P43/00 , C07D209/18 , C07D209/20 , C07D401/14 , C07D403/06 , C07D403/12 , C07D409/06 , C07D417/06 , C07D417/14
摘要： Indol-3-yl derivatives of the general formula I in which A, B, X, R1, R2, R3, R4, R5, n and m are as defined in Patent claim 1, and their physiologically acceptable salts or solvates are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart diseases, arteriosclerosis, inflammations, tumours, osteoporosis, rheumatic arthritis, macular degenerative disease, diabetic retinopathy, infections and restenosis after angioplasty or in pathological processes maintained or propagated by angiogenesis.

7. 发明专利

BRPI0412451A 未知
公开(公告)号：BRPI0412451A
公开(公告)日：2006-09-19
申请号：BRPI0412451
申请日：2004-06-18
申请人： MERCK PATENT GMBH
发明人： STOHLE WOLFGANG , GOTTSCHLICH RUDOLF , HARTING JUERGEN , SEYFRIED CHRISTOPH
IPC分类号： A61P1/00 , C07D207/12 , A61K31/40
摘要： Compound of the formula (I), in which A, R 1 , R 2 , R 3 , X, Y, m and n have the meaning indicated, are suitable as for the treatment of irritable bowel syndrome.

8. 发明专利

AT303361T 未知
公开(公告)号：AT303361T
公开(公告)日：2005-09-15
申请号：AT99923421
申请日：1999-04-16
申请人： MERCK PATENT GMBH
发明人： BATHE ANDREAS , HELFERT BERND , ACKERMANN KARL-AUGUST , GOTTSCHLICH RUDOLF , STEIN INGEBORG , BUDAK JENS
IPC分类号： C07D207/12 , A61K31/40 , A61P1/00 , A61P7/10 , A61P29/00 , C07B35/02 , C07B43/06
摘要： Production of N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidino)ethyl]-2,2-diphenylacetamide (Ia) or N-methyl-N-[(1R)-1-phenyl-2-((3R)-3-hydroxypyrrolidino)ethyl]-2,2-diphenylacetamide (Ib) comprises (a) reacting the corresponding enantiomer of an N-substituted phenylglycine derivative with an optionally O-protected 3-hydroxypyrrolidine derivative, (b) reducing the product to convert the N-substituent to methyl and remove any protecting group, and (c) reacting with an activated diphenylacetic acid derivative. Production of N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidino)ethyl]-2,2-diphenylacetamide (Ia) or N-methyl-N-[(1R)-1-phenyl-2-((3R)-3-hydroxypyrrolidino)ethyl]-2,2-diphenylacetamide (Ib) comprises (a) reacting the corresponding enantiomer of an N-substituted phenylglycine derivative of formula (II) with an optionally O-protected 3-hydroxypyrrolidine derivative of formula (III), (b) reducing the product of formula (IV), and (c) reacting the product of formula (V) with an activated diphenylacetic acid derivative of formula (VI) to give a product of formula (Ia/Ib): [Image] [Image] [Image] [Image] R : H, OR 1> or SR 1>; R 1>A, aryl, heteroaryl, Si(R 3>) 3 or COR 3>; R 3>H, A, aryl or heteroaryl; A : 1-6C alkyl; M : H, alkali(ne earth) metal, NH 4 or alkylammonium; R 2>H, A, aryl, heteroaryl, Si(R 3>) 3 or COR 3>; R 4>halogen, OA or OCOA. An independent claim is also included for compounds referred to as N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidino)ethane] and N-methyl-N-[(1R)-1-phenyl-2-((3R)-3-hydroxypyrrolidino)ethane] useful as intermediates for (Ia) and (Ib). ACTIVITY : Antiinflammatory; analgesic; diuretic. MECHANISM OF ACTION : None given.

9. 发明专利

CA2128380C 4-ARYLOXY- AND 4-ARYLTHIOPIPERIDINE DERIVATIVES 未知
公开(公告)号：CA2128380C
公开(公告)日：2005-04-12
申请号：CA2128380
申请日：1994-07-19
申请人： MERCK PATENT GMBH
发明人： PRUCHER HELMUT , GOTTSCHLICH RUDOLF , BARTOSZYK GERD , SEYFRIED CHRISTOPH
IPC分类号： A61K31/445 , A61K31/42 , A61K31/4465 , A61K31/4523 , A61P9/12 , A61P25/04 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/26 , C07D211/54 , C07D263/20 , C07D413/06 , C07D413/14
摘要： Novel 4-aryloxy- or 4-arylthiopiperidine derivatives of the formula I (see formula I) in which R1 and R2 are each, independently of one another phenyl radicals which are unsubstituted or mono- or disubstituted by A, OH, OA, aryloxy with 6-10 C atoms, aralkyloxy with 7-11 C atoms, -O,- (CH2)n-O-, Hal, CF3, NO2, NH2, NHA, NA2, NHY, NAY, NHSO2A and/or NASO2A, X is O, S, SO or SO2, m is 1, 2 or 3, n is 1 or 2, A is an alkyl radical with 1-6 C atoms, Hal is F, Cl, Br or I and y is alkanoyl with 1-8 C atoms, aralkanoyl with 1-10 C atoms or aroyl with 7-11 C atoms, and the physiologically acceptable salts thereof, show an effect influencing the central nervous system, in particular neuroleptic effect, with a negligible cataleptic effect.

10. 发明专利

PL360289A1 ARYLPIPERAZINE DERIVATIVES AND THEIR USE AS PSYCHOTROPIC AGENTS 未知
公开(公告)号：PL360289A1
公开(公告)日：2004-09-06
申请号：PL36028901
申请日：2001-08-07
申请人： MERCK PATENT GMBH
发明人： GOTTSCHLICH RUDOLF , DORSCH DIETER , BARTOSZYK GERD , HARTING JUERGEN , SEYFRIED CHRISTOPH , VAN AMSTERDAM CHRISTOPH
IPC分类号： A61K31/496 , C07D209/08 , C07D215/40 , A61P25/18
摘要： The invention relates to arylpiperazine derivatives of formula (I), wherein R , R , A, B, Ar and n have the given meanings.

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