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1. 发明授权

US5232978A 1-(2-arylethyl)-pyrrolidines 失效
标题翻译： 1-（2-芳乙基） - 吡咯烷
公开(公告)号：US5232978A
公开(公告)日：1993-08-03
申请号：US786674
申请日：1991-11-01
申请人： Rudolf Gottschlich , Karl-August Ackermann , Helmut Prucher , Andrew Barbar , Anton Haase , Hartmut Greiner , Gerd Bartoszyk
发明人： Rudolf Gottschlich , Karl-August Ackermann , Helmut Prucher , Andrew Barbar , Anton Haase , Hartmut Greiner , Gerd Bartoszyk
IPC分类号： C07D207/08 , C07D207/12 , C07D217/14 , C07D401/12 , C07D409/06 , C07D409/12
CPC分类号： C07D207/08 , C07D207/12 , C07D217/14 , C07D401/12 , C07D409/06 , C07D409/12
摘要： Novel 1-(2-arylethyl)-pyrrolidines of the formula ##STR1## in which, Ar is a phenyl group which is unsubstituted or monosubstituted by OH, --O--CO--NH.sub.2, --O--CO--NHA, --O--CO--NA.sub.2, NH.sub.2, --NH--CHO, --NH--CO--A, --NH--CO--NH.sub.2, --NH--CO--NHA or NH--SO.sub.2 --A,R.sup.1 is A,R.sup.2 is a phenyl, naphthyl, thienyl, benzothienyl or pyridyl group which is unsubstituted or mono- or disubstituted by A, Hal, CF.sub.3, OH, OA, --O--CO--NH.sub.2, --O--CO--NHA, --O--CO--NA.sub.2, NO.sub.2, NH.sub.2, --NH--CHO, --NH--CO--A, --NH--CO--NH.sub.2, --NH--CO--NHA, --NH--SO.sub.2 A, --CO--A, --CONH.sub.2, --CONHA, --CONA.sub.2, --CH.sub.2 --CONH.sub.2 and/or --O--CH.sub.2 --CONH.sub.2,R.sup.3 is OH or CH.sub.2 OH,A is alkyl with 1-4 C atoms andHal is F, Cl, Br or I,or a pharmaceutically acceptable salt thereof for use as an analgesic in humans and veterinary medicine.
摘要翻译：具有下式的新颖的1-（2-芳基乙基） - 吡咯啉其中，Ar是未被取代或被OH，-O-CO-NH 2，-O-CO-NHA，-O- CO-NA2，NH2，-NH-CHO，-NH-CO-A，-NH-CO-NH2，-NH-CO-NHA或NH-SO2-A，R1是A，R2是苯基，萘基，噻吩基，未取代或被A，Hal，CF 3，OH，OA，-O-CO-NH 2，-O-CO-NHA，-O-CO-NA 2，NO 2，NH 2 - 取代的苯并噻吩基或吡啶基， NH-CHO，-NH-CO-A，-NH-CO-NH2，-NH-CO-NHA，-NH-SO2A，-CO-A，-CONH2，-CONHA，-CONA2，-CH2-CONH2和/ 或-O-CH 2 -CONH 2，R 3是OH或CH 2 OH，A是具有1-4个C原子的烷基，Hal是F，Cl，Br或I，或其药学上可接受的盐，用作人类和兽医学中的止痛剂。

2. 发明授权

US5532266A Acrylacetamides 失效
标题翻译：丙烯酰胺
公开(公告)号：US5532266A
公开(公告)日：1996-07-02
申请号：US453811
申请日：1995-05-30
申请人： Rudolf Gottschlich , Karl-August Ackermann , Helmut Prucher , Christoph Seyfried , Hartmut Greiner , Gerd Bartoszyk , Frank Mauler , Manfred Stohrer , Andrew Barber
发明人： Rudolf Gottschlich , Karl-August Ackermann , Helmut Prucher , Christoph Seyfried , Hartmut Greiner , Gerd Bartoszyk , Frank Mauler , Manfred Stohrer , Andrew Barber
IPC分类号： A61K31/435 , A61K31/165 , A61K31/17 , A61K31/35 , A61K31/40 , A61K31/4025 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/535 , A61P7/10 , A61P11/08 , A61P11/14 , A61P25/04 , A61P25/08 , A61P25/28 , A61P29/00 , A61P43/00 , C07C233/00 , C07C233/05 , C07C233/08 , C07D207/08 , C07D207/09 , C07D207/12 , C07D215/00 , C07D217/06 , C07D217/14 , C07D295/12 , C07D295/135 , C07D311/84 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/12 , C07D409/06 , C07D413/06 , C07D207/36 , C07D207/325
CPC分类号： C07D405/06 , C07D207/09 , C07D207/12 , C07D217/14 , C07D311/84 , C07D405/12
摘要： Novel arylacetamides of the formula I ##STR1## in which Q is R.sup.4 --CH(CH.sub.2 Z)--NA--, ##STR2## R.sup.1 is Ar, cycloalkyl with 3-7 C atoms or C.sub.4 -C.sub.8 -cycloalkyl-C.sub.1 -C.sub.7 -alkyl,R.sup.2 is Ar,R.sup.3 is H, OH, OA or A,R.sup.4 is A or phenyl which can optionally be substituted once or twice by F, Cl, Br, I, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A or NA.sub.2,R.sup.5 and R.sup.6 are each, independently of one another, H, F, Cl, Br, I, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or taken together are methylenedioxy,A is alkyl with 1-7 C atoms, and physiologically acceptable salts thereof.
摘要翻译：其中Q为R4-CH（CH2Z）-NA-，R1为Ar，具有3-7个C原子的环烷基或C 4 -C 8 - 环烷基-C 1 -C 4烷基的新的芳基乙酰胺， C7-烷基，R2是Ar，R3是H，OH，OA或A，R4是A或可以被F，Cl，Br，I，OH，OA，CF3，NO2，NH2等任意取代一次或两次的苯基， NHA，NHCOA，NHSO2A或NA2，R5和R6各自独立地为H，F，Cl，Br，I，OH，OA，CF3，NH2，NHA，NA2，NHCOA，NHCONH2，亚甲二氧基，A是具有1-7个C原子的烷基，以及其生理上可接受的盐。

3. 发明授权

US06756370B1 Piperidine alcohols 失效
标题翻译：哌啶醇
公开(公告)号：US06756370B1
公开(公告)日：2004-06-29
申请号：US10069054
申请日：2002-02-21
申请人： Helmut Prücher , Henning Böttcher , Karl-August Ackermann , Rudolf Gottschlich , Christoph van Amsterdam , Christoph Seyfried , Jürgen Harting , Gerd Bartoszyk , Hartmut Greiner
发明人： Helmut Prücher , Henning Böttcher , Karl-August Ackermann , Rudolf Gottschlich , Christoph van Amsterdam , Christoph Seyfried , Jürgen Harting , Gerd Bartoszyk , Hartmut Greiner
IPC分类号： A61K3154
CPC分类号： C07D401/06 , C07D211/22 , C07D405/06 , C07D409/06 , C07D417/06
摘要： The invention relates to compounds of formula (I), wherein R1, R2 and A have the meanings given in claim 1, are potent 5-HT2A antagonists and are suitable for treating psychoses, schizophrenia, depression, neurological disorders, impaired memory, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia and anorexia nervosa, Pre-Menstrual Syndrome and/or for positively influencing obsessive-compulsive disorders, (OCD).
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2和A具有权利要求1中给出的含义，它们是有效的5-HT2A拮抗剂，适用于治疗精神病，精神分裂症，抑郁症，神经障碍记忆障碍，帕金森病，肌萎缩性侧索硬化症，阿尔茨海默氏病，亨廷顿疾病，进食障碍如贪食症和神经性厌食症，前月经综合征和/或积极影响强迫症（OCD）。

4. 发明授权

US5472961A Acetamides 失效
标题翻译：乙酰胺
公开(公告)号：US5472961A
公开(公告)日：1995-12-05
申请号：US397758
申请日：1995-03-02
申请人： Rudolf Gottschlich , Karl-August Ackermann , Christoph Seyfried , Andrew Barber , Gerd Bartoszyk , Hartmut Greiner
发明人： Rudolf Gottschlich , Karl-August Ackermann , Christoph Seyfried , Andrew Barber , Gerd Bartoszyk , Hartmut Greiner
IPC分类号： C07D413/06 , A61K31/42 , A61K31/47 , A61P9/10 , A61P25/00 , A61P25/04 , A61P43/00 , C07D235/26 , C07D263/58 , C07D265/36 , C07D265/38 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14
CPC分类号： C07D263/58 , C07D235/26 , C07D265/36 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14
摘要： Novel acetamides of the formula I ##STR1## in which Q, R, X and Y have the meanings defined herein, have analgesic and neuroprotective properties and bind with high affinity to kappa receptors.
摘要翻译：其中Q，R，X和Y具有本文定义的含义的式I“I”的新型乙酰胺具有止痛和神经保护性质，并以高亲和力结合κ受体。

5. 发明授权

US5561145A 4-aryloxy- and 4-arylthiopiperidine derivatives 失效
标题翻译： 4-芳氧基和4-芳硫基哌啶衍生物
公开(公告)号：US5561145A
公开(公告)日：1996-10-01
申请号：US278210
申请日：1994-07-21
申请人： Helmut Prucher , Rudolf Gottschlich , Gerd Bartoszyk , Christoph Seyfried
发明人： Helmut Prucher , Rudolf Gottschlich , Gerd Bartoszyk , Christoph Seyfried
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
CPC分类号： C07D413/06
摘要： Novel 4-aryloxy- or 4-arylthiopiperidine derivatives of the formula I ##STR1## in which R.sup.1 and R.sup.2 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, --0--(CH.sub.2).sub.n --0--, Hal, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NA.sub.2, NHAc, NAAc, NHSO.sub.2 A and/or NASO.sub.2 A,X is O, S, SO or SO.sub.2,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 landAc 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.
摘要翻译：式I的新型4-芳氧基 - 或4-芳硫基哌啶衍生物，其中R 1和R 2各自彼此独立地是未被取代的，被A，OH，OA，芳氧基与6- 10 C原子，具有7-11个碳原子的芳烷氧基，-O-（CH2）n-O-，Hal，CF3，NO2，NH2，NHA，NA2，NHAc，NAAc，NHSO2A和/或NASO2A，X是O，S ，SO或SO 2，m为1,2或3，n为1或2，A为具有1-6个C原子的烷基，Hal为F，Cl，Br或l，Ac为具有1-8个C原子的烷酰基具有1-10个C原子的芳烷酰基或具有7-11个C原子的芳酰基及其生理上可接受的盐显示出影响中枢神经系统的作用，特别是抗精神病药效应，具有可忽略的催眠作用。

6. 发明授权

US06413989B1 Piperidinylmethyloxazolidinone derivative 失效
标题翻译：哌啶基甲基恶唑烷酮衍生物
公开(公告)号：US06413989B1
公开(公告)日：2002-07-02
申请号：US09508059
申请日：2000-05-17
申请人： Helmut Prucher , Gerd Bartoszyk , Christoph Seyfried , Rudolf Gottschlich , Joachim Leibrock
发明人： Helmut Prucher , Gerd Bartoszyk , Christoph Seyfried , Rudolf Gottschlich , Joachim Leibrock
IPC分类号： A61K3145
CPC分类号： C07D413/06
摘要： The invention relates to the compound 5-[4-(4-fluorobenzyl) piperidin-1-ylmethyl]-3-(4-hydroxy-phenyl)oxazolidin-2-one of the formula I and to physiologically acceptable salts thereof. The compound acts as a neuroleptic.
摘要翻译：本发明涉及式I的化合物5- [4-（4-氟苄基）哌啶-1-基甲基] -3-（4-羟基 - 苯基）恶唑烷-2-酮及其生理上可接受的盐。化合物作为精神安定药物。

7. 发明申请

US20060264419A1 Substituted pyrazoles 审中-公开
标题翻译：取代的吡唑
公开(公告)号：US20060264419A1
公开(公告)日：2006-11-23
申请号：US10552065
申请日：2004-03-08
申请人： Kai Schiemann , Karl-August Ackermann , Michael Arlt , Dirk Finsinger , Christoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried , Oliver Schadt
发明人： Kai Schiemann , Karl-August Ackermann , Michael Arlt , Dirk Finsinger , Christoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried , Oliver Schadt
IPC分类号： A61K31/551 , A61K31/5377 , A61K31/496 , A61K31/4439 , A61K31/416
CPC分类号： C07D231/12 , A61K31/415 , C07D231/14 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D409/06 , C07D409/10 , C07D413/12 , C07D451/06 , C07D453/06 , C07D471/04 , C07D471/10 , C07D487/08 , C07D491/08
摘要： The compounds of the formula (I) and salts and solvates thereof, in which X, R1, R2, R3, R4 and R5 have the meanings indicated in Claim (1), are suitable as ligands of 5 HT receptors.
摘要翻译：式（I）化合物及其盐和溶剂合物，其中X，R 1，R 2，R 3，R 3， SUP> 4和R 5具有权利要求（1）所示的含义，适合作为5HT受体的配体。

8. 发明授权

US5977161A Kappa-opiate agonists effective in the treatment of postoperative ileus 失效
标题翻译：卡帕阿片激动剂有效治疗术后肠梗阻
公开(公告)号：US5977161A
公开(公告)日：1999-11-02
申请号：US27228
申请日：1998-02-20
申请人： Andrew Barber , Christoph Seyfried , Gerd Bartoszyk , Rudolf Gottschlich
发明人： Andrew Barber , Christoph Seyfried , Gerd Bartoszyk , Rudolf Gottschlich
IPC分类号： C07D207/08 , A61K31/135 , A61K31/165 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61P1/00 , A61P1/04 , A61P29/00 , A61P43/00 , C07D207/12
CPC分类号： A61K31/4025
摘要： Disclosed herein are pharmaceutical preparations which are suitable for the treatment of postoperative ileus and contain at least one compound of the formula I ##STR1## in which R.sup.1 is Ar, cycloalkyl having 3-7 C atoms or cycloalkylalkyl having 4-8 C atoms,R.sup.2 is Ar, orR.sub.1 and R.sup.2 together are ##STR2## R.sup.3 is H, OH, OA or A, R.sup.4 is A or phenyl which can optionally be mono- or disubstituted by Hal, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A and/or NA.sub.2,R.sup.5 is OH, CH.sub.2 OH,R.sup.6 and R.sup.7 in each case independently of one another are H, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or methylenedioxy, with the oxy groups bonded to adjacent carbons on the ring,A is alkyl having 1-7 C atoms,Ar is a mono- or bicyclic aromatic radical which can optionally contain an N, O or S atom in the ring and can be mono-, di- or trisubstituted by A, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA and/or NHCONH.sub.2,D is CH.sub.2, O, S, NH, NA, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 NH--, --CH.sub.2 --NA-- or a bondandHal is F, Cl, Br or I.
摘要翻译：本文公开了适用于治疗术后肠梗阻并含有至少一种其中R 1为Ar的式I化合物或具有3-7个C原子的环烷基或具有4-8个C原子的环烷基烷基，R2为Ar，或R 1和R 2一起为R 3为H，OH，OA或A，R 4为A或可任选被Hal，OH，OA，CF 3，NO 2，NH 2，NHA，NHCOA，NHSO 2 A单取代或二取代的苯基和/或 NA2，R5分别为H，Hal，OH，OA，CF3，NH2，NHA，NA2，NHCOA，NHCONH2，NO2或亚甲二氧基的OH，CH2OH，R6和R7彼此独立地键合， A是具有1-7个C原子的烷基，Ar是可以在环中任选含有N，O或S原子的单环或双环芳族基团，并且可以被A，，Hal，OH，OA，CF 3，NH 2，NHA，NA 2，NHCOA和/或NHCONH 2，D是CH 2，O，S，NH，NA，-CH 2 -CH 2 - ， - CH = CH-， - CH 2 NH-， CH2-NA-或键，Hal为F，Cl，Br或I.

9. 发明授权

US5714502A Piperidinylmethyloxazolidinones 失效
标题翻译：哌啶基甲基恶唑烷酮
公开(公告)号：US5714502A
公开(公告)日：1998-02-03
申请号：US701852
申请日：1996-08-23
申请人： Helmut Prucher , Gerd Bartoszyk
发明人： Helmut Prucher , Gerd Bartoszyk
IPC分类号： A61K31/422 , A61K31/435 , A61K31/445 , A61K31/4523 , A61P9/12 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , C07D263/18 , C07D295/00 , C07D413/06
CPC分类号： C07D413/06
摘要： The invention relates to novel piperidinylmethyloxazolidin-2-one derivatives of the formula I ##STR1## in which R.sup.1 and R.sup.2 in each case independently of one another are unsubstituted or mono- to disubstituted phenyl radicals whose substituents can be A, OA, aryloxy having 6-10 C atoms, aralkyloxy having 7-11 C atoms, --O--(CH.sub.2).sub.n --O-- (bonded in directly adjacent positions or in the meta- or para-position to one another on the phenyl ring), --O--(CH.sub.2).sub.n --OH, Hal, CF.sub.3, OH, NO.sub.2, NH.sub.2, NHA, NA.sub.2, NHR.sup.3, NAR.sup.3, SO.sub.2 NH.sub.2, SO.sub.2 NHA, SO.sub.2 NA.sub.2, SO.sub.2 NHR.sup.3 (excluding R.sup.3 =SO.sub.2 A) , SO.sub.2 N (R.sup.3).sub.2 (excluding R.sup.3 =SO.sub.2 A) or R.sup.3, R.sup.3 is COH, CO-alkyl having 1-7 C atoms in the alkyl, CO-alkyl-Ar having 8-12 C atoms, CO-Ar having 7-13 C atoms, SO.sub.2 A A is an alkyl radical having 1-6 C atoms n is 1 or 2 Hal is F, Cl, Br or I and their physiologically acceptable salts.
摘要翻译：本发明涉及式I（I）的新颖的哌啶基甲基恶唑烷-2-酮衍生物，其中R 1和R 2各自独立地是未取代的或被单取代或被取代的苯基，其取代基可以是A，OA，具有6-10个碳原子的芳氧基，具有7-11个碳原子的芳烷氧基，-O-（CH 2）n O-（在苯环的直接相邻位置或彼此间位置或对位键合），-O - （CH2）n-OH，Hal，CF3，OH，NO2，NH2，NHA，NA2，NHR3，NAR3，SO2NH2，SO2NHA，SO2NA2，SO2NHR3（不包括R3 = SO2A），SO2N（R3）2（不包括R3 = ）或R3，R3是COH，在烷基中具有1-7个C原子的CO-烷基，具有8-12个C原子的CO-烷基-Ar，具有7-13个C原子的CO-Ar，SO2A A是具有 1-6个碳原子，n为1或2个Hal为F，Cl，Br或I及其生理上可接受的盐。

10. 发明授权

US06960599B2 Heterocyclic aminoalkylpyridine derivatives as psychopharmaceuticals 失效
标题翻译：杂环氨基烷基吡啶衍生物作为心理药物
公开(公告)号：US06960599B2
公开(公告)日：2005-11-01
申请号：US10311286
申请日：2001-06-19
申请人： Dieter Dorsch , Henning Boettcher , Michael Arlt , Christoph Seyfried , Gerd Bartoszyk , Juergen Harting , Rudolf Gottschlich
发明人： Dieter Dorsch , Henning Boettcher , Michael Arlt , Christoph Seyfried , Gerd Bartoszyk , Juergen Harting , Rudolf Gottschlich
IPC分类号： 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 , C07D401/12 , C07D405/12 , C07D417/12 , C07D401/02 , A61K31/44 , A61K31/47
CPC分类号： C07D213/64 , C07D213/38 , C07D401/12 , C07D405/12 , C07D417/12
摘要： The invention relates to heterocyclic aminoalkylpyridine derivatives of the formula I: where R1 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, —OR4, —N(R4)2, —NO2, —CN, Hal, —COOR4, —CON(R4)2, —COR4, ═O; R2 is a phenyl group which is optionally monosubstituted, disubstituted, trisubstituted, tetrasubstituted or pentasubstituted by one or more of the groups Hal, -A, —O-A, —NO2 or —CN, or is a thienyl group which is optionally monosubstituted or disubstituted by one or more of the groups Hal, -A, —O-A, -NO2, —CN or thienyl; R3 is H, -A, —CO-A, —C(R4)2R2, —C(R4)2-pyridinediyl-R2; R4 is H or -A; A is C1-C6-alkyl, where 1 to 7 hydrogen atoms are optionally replaced by fluorine; —X— is —O—, —S—, sulfinyl, sulfonyl, —C(R4)2—; —Y— is —[C(R4)2]n—; —Z— is —C(R4)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.
摘要翻译：本发明涉及式I的杂环氨基烷基吡啶衍生物：其中R 1是具有1至3个环结构的杂环的基团，其中每个环结构是饱和的，不饱和的或芳族的并且任选地与其它环结构以得到稠环体系，并且杂环在环结构中总共具有1至4个N，O和/或S原子，并且任选被一个或多个基团-A，-OR单取代，二取代或三取代 -N（R 4）2，-NO 2，-CN，Hal，-COOR 2， -CON（R 4）2，-SOR 4，-O; R 2是一个苯基，其任选被一个或多个Hal，-A，-OA，-NO 2基团单取代，二取代，三取代，四取代或五取代。或-CN，或者是任选被一个或多个Hal，-A，-OA，-NO 2，-CN或噻吩基团单取代或二取代的噻吩基; R 3是H，-A，-CO-A，-C（R 4）2 R 2，，-C（R 4）2 - 吡啶二基-R 2; R 4是H或-A; A为C 1 -C 6 - 烷基，其中1至7个氢原子任选被氟取代; -X-是-O - ， - S-，亚磺酰基，磺酰基，-C（R 4）2 - 。 -Y-是 - [C（R 4）2）n - -Z-是-C（R 4）2 - ; - Hal是F，Cl，Br或I; n为1,2,3或4; 及其可耐受的盐和溶剂合物及其作为药物的用途。

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