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1. 发明授权

US5612337A Substituted morpholine derivatives and their use as therapeutic agents 失效
标题翻译：取代的吗啉衍生物及其作为治疗剂的用途
公开(公告)号：US5612337A
公开(公告)日：1997-03-18
申请号：US663201
申请日：1996-06-13
申请人： Raymond Baker , Timothy Harrison , Angus M. MacLeod , Andrew P. Owens , Eileen M. Seward , Christopher J. Swain , Martin R. Teall
发明人： Raymond Baker , Timothy Harrison , Angus M. MacLeod , Andrew P. Owens , Eileen M. Seward , Christopher J. Swain , Martin R. Teall
IPC分类号： C07D487/08 , A61K31/535 , A61K31/5377 , A61K31/541 , A61P1/08 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/28 , A61P29/00 , A61P43/00 , C07D413/06 , C07D413/14 , C07D417/14 , C07F9/6533 , C07F9/6558
CPC分类号： C07D413/06 , C07D413/14 , C07F9/6533 , C07F9/65583
摘要： The present invention relates to compounds of formula (I), wherein R.sup.1 is hydrogen, halogen, C.sub.1-6 C alkyl, C.sub.1-6 alkoxy, CF.sub.3, NO.sub.2, CN, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, CO.sub.2 R.sup.a, CONR.sup.a R.sup.b, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl or C.sub.1-4 alkyl substituted by C.sub.1-4 alkoxy, where R.sup.a and R.sup.b are hydrogen or C.sub.1-4 alkyl; R.sup.2 is hydrogen, halogen, C .sub.1-6 alkyl, C.sub.1-6 alkoxy substituted by C.sub.1-4 alkoxy or CF.sub.3 ; R.sup.3 is hydrogen, halogen or CF.sub.3 ; R.sup.4 is selected from the definitions of R.sup.1 ; R.sup.5 is selected from the definitions of R.sup.2 ; R.sup.6 is a 5-membered or 6-membered heterocyclic ring containing 2 or 3 nitrogen atoms optionally substituted by .dbd.O, .dbd.S or a C.sub.1-4 alkyl group, and optionally substituted by an aminoalkyl group; R.sup.9a and R.sup.9b are hydrogen or C.sub.1-4 alkyl, or R.sup.9a and R.sup.9b are joined to form a C.sub.5-7 ring; X is C.sub.1-4 alkylene optionally substituted by oxo; and Y is a C.sub.1-4 alkyl group optionally substituted by hydroxyl; with the proviso that if Y is C.sub.1-4 alkyl, R.sup.6 is substituted at least by an aminoalkyl group; and pharmaceutically acceptable salts and prodrugs thereof. The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.
摘要翻译： PCT No.PCT / GB94 / 02819 Sec。 371日期：1996年6月13日 102（e）日期1996年6月13日PCT 1994年12月23日PCT公布。公开号WO95 / 18124 日期：1995年7月6日（一）本发明涉及式（I）化合物，其中R 1为氢，卤素，C 1-6烷基，C 1-6烷氧基，CF 3，NO 2，CN，SR a，SOR a ，SO 2 R a，CO 2 R a，CONR a R b，C 2-6烯基，C 2-6炔基或被C 1-4烷氧基取代的C 1-4烷基，其中R a和R b是氢或C 1-4烷基; R2是氢，卤素，C 1-6烷基，被C 1-4烷氧基或CF 3取代的C 1-6烷氧基; R3是氢，卤素或CF3; R4选自R1的定义; R5选自R2的定义; R6是含有2或3个氮原子的5元或6元杂环，任选被= O，= S或C 1-4烷基取代，并且任选被氨基烷基取代; R9a和R9b是氢或C1-4烷基，或R9a和R9b连接形成C5-7环; X是任选被氧代取代的C 1-4亚烷基; Y是任选被羟基取代的C 1-4烷基; 条件是如果Y是C 1-4烷基，则R6至少被氨基烷基取代; 及其药学上可接受的盐和前药。该化合物特别用于治疗疼痛，炎症，偏头痛和呕吐。

2. 发明授权

US5472978A Aromatic compounds, pharmaceutical compositions containing them and their use in therapy 失效
标题翻译：芳香族化合物，含有它们的药物组合物及其在治疗中的应用
公开(公告)号：US5472978A
公开(公告)日：1995-12-05
申请号：US162096
申请日：1993-12-10
申请人： Raymond Baker , Angus M. MacLeod , Kevin J. Merchant , Christopher J. Swain
发明人： Raymond Baker , Angus M. MacLeod , Kevin J. Merchant , Christopher J. Swain
IPC分类号： A61K31/135 , A61K31/165 , A61K31/19 , A61K31/215 , A61K31/27 , A61K31/34 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K38/00 , A61P37/00 , C07C211/27 , C07C211/29 , C07C211/30 , C07C217/48 , C07C217/64 , C07C229/12 , C07C229/14 , C07C229/36 , C07C233/18 , C07C233/22 , C07C233/36 , C07C233/47 , C07C233/73 , C07C237/06 , C07C237/08 , C07C237/20 , C07C255/11 , C07C255/13 , C07C255/24 , C07C255/54 , C07C271/08 , C07C271/16 , C07C271/20 , C07C271/22 , C07C275/10 , C07C275/24 , C07C275/28 , C07C311/04 , C07C323/25 , C07C323/39 , C07D207/28 , C07D209/14 , C07D209/20 , C07D231/56 , C07D241/08 , C07D295/084 , C07D295/185 , C07D307/81 , C07D333/58 , C07D333/60 , C07K5/06
CPC分类号： C07D333/58 , C07C211/29 , C07C217/48 , C07C217/64 , C07C229/14 , C07C229/36 , C07C233/18 , C07C233/22 , C07C233/47 , C07C233/73 , C07C237/06 , C07C237/08 , C07C237/20 , C07C255/13 , C07C255/54 , C07C271/16 , C07C271/20 , C07C271/22 , C07C275/10 , C07C275/24 , C07C275/28 , C07C311/04 , C07D207/28 , C07D209/14 , C07D209/20 , C07D231/56 , C07D241/08 , C07D295/092 , C07D295/185 , C07D333/60 , C07K5/06026 , A61K38/00 , C07C2101/02
摘要： Compounds of formula (I), and salts and prodrugs thereof, wherein Q represents optionally substituted phenyl, naphthyl, indolyl, benzothiophenyl, benzofuranyl, benzyl or indazolyl; Z represents O, S or NR.sup.8 ; X and Y are H or are together .dbd.O; R.sup.1 and R.sup.2 are H; optionally substituted C.sub.1-6 alkyl; optionally substituted phenyl(C.sub.1-4 alkyl); COR.sup.c ; CO.sub.2 R.sup.c ; CONR.sup.c R.sup.d ; CONR.sup.c COOR.sup.d ; or SO.sub.2 R.sup.c ; R.sup.3 is H or C.sub.1-6 alkyl, R.sup.4 is H , C.sub.1-6 alkyl or optionally substituted phenyl; and R.sup.5 represents optionally substituted phenyl; are tachykinin antagonists. They and compositions thereof are useful in therapy.
摘要翻译： PCT No.PCT / GB92 / 01214 Sec。 371日期：1993年12月10日 102（e）日期1993年12月10日PCT提交1992年7月3日PCT公布。公开号WO93 / 01169 （I）化合物及其盐和前药，其中Q表示任选取代的苯基，萘基，吲哚基，苯并噻吩基，苯并呋喃基，苄基或吲唑基; Z表示O，S或NR8; X和Y为H或一起= O; R1和R2是H; 任选取代的C 1-6烷基; 任选取代的苯基（C 1-4烷基）; CORC; CO2Rc; CONRcRd; CONRcCOORd; 或SO2Rc; R3是H或C1-6烷基，R4是H，C1-6烷基或任选取代的苯基; 并且R 5表示任选取代的苯基; 速激肽拮抗剂。它们及其组合物可用于治疗。

3. 发明授权

US5288730A Azabicyclic compounds, pharmaceutical compositions containing them and their use in therapy 失效
标题翻译：氮杂双环化合物，含有它们的药物组合物及其在治疗中的用途
公开(公告)号：US5288730A
公开(公告)日：1994-02-22
申请号：US899205
申请日：1992-06-16
申请人： Raymond Baker , Christopher J. Swain , Martin R. Teall , Brian J. Williams
发明人： Raymond Baker , Christopher J. Swain , Martin R. Teall , Brian J. Williams
IPC分类号： A61K31/40 , A61K31/435 , A61K31/55 , A61P1/00 , A61P11/00 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P29/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D453/02 , C07D471/08 , C07D487/08 , C07F7/08 , C07D453/00
CPC分类号： C07D453/02
摘要： Compounds of formula (I), and salts and prodrugs thereof: ##STR1## wherein Q is the residue of an optionally substituted azabicyclic ring system;X represents oxa or thia;Y represents H or hydroxy;R.sup.1 represents phenyl or thienyl, either of which groups may be optionally substituted by halo, trifluoromethyl or C.sub.1-3 alkoxy, or C.sub.5-7 cycloalkyl;R.sup.2 represents benzyl which may be substituted in the benzyl ring by halo, trifluoromethyl or C.sub.1-3 alkoxy, or C.sub.5-7 cycloalkyl; andR.sup.3, R.sup.4 and R.sup.5 independently represent H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, --OR.sup.a, SCH.sub.3, SOCH.sub.3, S0.sub.2 CH.sub.3, --NR.sup.a R.sup.b, --NR.sup.a COR.sup.b, --NR.sup.a C0.sub.2 R.sup.b, --C0.sub.2 R.sup.a or --CONR.sup.a R.sup.b ; andR.sup.a and R.sup.b independently represent H, C.sub.1-6 alkyl, phenyl or trifluoromethyl, are tachykinin receptor antagonists. They and compositions thereof are useful in therapy.
摘要翻译：式（I）化合物及其盐和前药：（*化学结构*）（I）其中Q是任选取代的氮杂双环体系的残基; X表示氧杂或硫杂; Y表示H或羟基; R 1表示苯基或噻吩基，其中任一个可以任选被卤素，三氟甲基或C 1-3烷氧基或C 5-7环烷基取代; R 2表示可以在苄基环中被卤素，三氟甲基或C 1-3烷氧基取代的苄基或C 5-7环烷基; 并且R 3，R 4和R 5独立地表示H，C 1-6烷基，C 2-6烯基，C 2-6炔基，卤素，氰基，硝基，三氟甲基，三甲基甲硅烷基，-OR a，SCH 3，SOCH 3，SO 2 CH 3，-NR a R b，-NR a COR b， -NR a CO 2 R b，-CO 2 R a或-CONR a R b; 并且R a和R b独立地表示H，C 1-6烷基，苯基或三氟甲基，是速激肽受体拮抗剂。它们及其组合物可用于治疗。

4. 发明授权

US5459270A Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them 失效
标题翻译：氮环化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US5459270A
公开(公告)日：1995-10-17
申请号：US196269
申请日：1994-02-16
申请人： Brian Williams , Raymond Baker , Timothy Harrison , Christopher J. Swain
发明人： Brian Williams , Raymond Baker , Timothy Harrison , Christopher J. Swain
IPC分类号： A61K31/395 , A61K31/397 , A61K31/40 , A61K31/4433 , A61K31/445 , A61K31/451 , A61P25/00 , A61P25/02 , A61P29/00 , A61P43/00 , C07D205/04 , C07D205/08 , C07D207/12 , C07D211/42 , C07D211/54 , C07D211/74 , C07D211/76 , C07D401/04 , C07D409/04
CPC分类号： C07D401/04 , C07D205/04 , C07D207/12 , C07D211/42 , C07D211/76 , C07D409/04
摘要： ##STR1## Compounds of formula (I), and salts and prodrugs thereof wherein n is 1, 2 or 3; X represents O or S; R
1 represents optionally substituted phenyl; R
2 represents aryl, heteroaryl, benzhydryl, or benzyl; R
4 and R
5 each independently represent H, halo, CH
2 OR
9 , C
1-6 alkyl, oxo, CO
2 R
10 or CONR
10 R
11 ; R
8 represents H, COR
9 , CO
2 R
10 or optionally substituted C
1-6 alkyl; R
9 represents H, C
1-6 alkyl or phenyl; and R
10 and R
11 each independently represent H or C
1-6 alkyl; are tachykinin antagonists. They and compositions thereof are useful in medicine.
摘要翻译： PCT No.PCT / GB92 / 01503 Sec。 371日期：1994年2月16日 102（e）日期1994年2月16日PCT提交1992年8月13日PCT公布。出版物WO93 / 04040 （I）式（I）化合物及其盐和前药，其中n为1,2或3; X表示O或S; R 1表示任选取代的苯基; R2代表芳基，杂芳基，二苯甲基或苄基; R 4和R 5各自独立地表示H，卤素，CH 2 OR 9，C 1-6烷基，氧代，CO 2 R 10或CONR 10 R 11; R8表示H，COR9，CO2R10或任选取代的C 1-6烷基; R9表示H，C1-6烷基或苯基; R 10和R 11各自独立地表示H或C 1-6烷基; 速激肽拮抗剂。它们及其组合物可用于医药。

5. 发明授权

US5242930A Azabicyclic compounds, pharmaceutical compositions containing them and their use in therapy 失效
标题翻译：化学化合物，含有它们的药物组合物及其在治疗中的使用
公开(公告)号：US5242930A
公开(公告)日：1993-09-07
申请号：US830822
申请日：1992-02-04
申请人： Raymond Baker , Eileen M. Seward , Christopher Swain
发明人： Raymond Baker , Eileen M. Seward , Christopher Swain
IPC分类号： A61K31/40 , A61K31/435 , A61P1/00 , A61P11/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/28 , A61P29/00 , A61P37/06 , C07D453/02 , C07D487/08
CPC分类号： C07D487/08 , C07D453/02
摘要： Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein Q is the residue of an optionally substituted azabicyclic ring system;X represents oxa or thia;Y represents H or hydroxy;R.sup.1 and R.sup.2 independently represent phenyl or thienyl, either of which groups may be optionally substituted by halo or trifluoromethyl;R.sup.3, R.sup.4 and R.sup.5 independently represent H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, --OR.sup.a, SCH.sub.3, SOCH.sub.3, SO.sub.2 CH.sub.3, --NR.sup.a R.sup.b, --NR.sup.a COR.sup.b, --NR.sup.a CO.sub.2 R.sup.b, --CO.sub.2 R.sup.a or --CONR.sup.a R.sup.b ;R.sup.a and R.sup.b independently represent H, C.sub.1-6 alkyl, phenyl or trifluoromethyl,are tachykinin antagonists. They and compositions thereof are therefore useful in therapy.

6. 发明授权

US5405853A Thiadiazoles useful in the treatment of senile dementia 失效
标题翻译：噻二唑可用于治疗老年痴呆症
公开(公告)号：US5405853A
公开(公告)日：1995-04-11
申请号：US166656
申请日：1993-12-13
申请人： Raymond Baker , Angus M. MacLeod , John Saunders , Kevin Merchant
发明人： Raymond Baker , Angus M. MacLeod , John Saunders , Kevin Merchant
IPC分类号： C07D417/04 , C07D453/02 , C07D453/06 , C07D471/08 , C07D487/08 , C07D413/14 , A61K31/33
CPC分类号： C07D417/04 , C07D453/02 , C07D453/06 , C07D471/08 , C07D487/08
摘要： A class of novel thiadiazoles, substituted on one of the ring carbon atoms with a non-aromatic azacyclic or azabicyclic ring system, and substituted on the other ring carbon atom with a substituent of low lipophilicity, or a hydrocarbon substituent; are potent muscarinic agonists, and have good CNS penetrability. The compounds are therefore useful in the treatment of neurological and mental illnesses, and are also of benefit in the treatment of severe painful conditions.
摘要翻译：一类新的噻二唑，其中一个环碳原子上被非芳族氮杂环或氮杂双环系取代，并在另一个环碳原子上被低亲油性的取代基或烃取代基取代; 是有效的毒蕈碱激动剂，具有良好的CNS渗透性。因此，这些化合物可用于治疗神经和精神疾病，并且在治疗严重的疼痛病症中也是有益的。

7. 发明授权

US5242927A Prodrugs for oxadiazole muscarinic agonists 失效
标题翻译：用于奥沙利霉素促性腺激素的药物
公开(公告)号：US5242927A
公开(公告)日：1993-09-07
申请号：US220209
申请日：1988-07-18
申请人： Raymond Baker , John Saunders , Angus M. MaCleod , Graham A. Showell
发明人： Raymond Baker , John Saunders , Angus M. MaCleod , Graham A. Showell
IPC分类号： C07D487/04 , A61K31/41 , A61K31/44 , A61P25/04 , A61P25/18 , C07D413/04 , C07D453/02 , C07D453/06 , C07D471/08 , C07D487/08
CPC分类号： C07D413/04 , C07D453/02 , C07D487/08
摘要： A class of novel oxadiazoles, substituted on one of the ring carbon atoms with a non-aromatic azacyclic or azabicyclic ring and on the other ring carbon atom with a substituent which is convertible in vivo to an amino group, are potent muscarinic agonists, and exhibit improved CNS penetrability and duration of action compared with the corresponding amino compounds. The compounds are therefore useful in the treatment of neurological and mental illnesses.

8. 发明授权

US5633266A Azacyclic compounds compositions containing them and their use as tachykinin antagonists 失效
标题翻译：含有它们的氮环化合物组合物及其作为速激肽拮抗剂的用途
公开(公告)号：US5633266A
公开(公告)日：1997-05-27
申请号：US495429
申请日：1995-07-26
申请人： Raymond Baker , Christopher J. Swain , Brian J. Williams
发明人： Raymond Baker , Christopher J. Swain , Brian J. Williams
IPC分类号： A61K31/4427 , A61K31/445 , A61K31/451 , A61P1/08 , A61P25/20 , A61P29/00 , A61P43/00 , C07D207/00 , C07D211/42 , C07D211/54 , C07D401/06
CPC分类号： C07D401/06 , C07D211/42
摘要： The present invention relates to compounds of formula (I), and salts and prodrugs thereof, wherein n is 1 , 2 or 3 and where any carbon atom of (CH.sub.2).sub.n may be substituted by R.sup.4 and/or R.sup.5 ; X represents O or S; R.sup.1 represents optionally substituted (CH.sub.2).sub.q phenyl, wherein q is 0, 1, 2 or 3; R.sup.2 represents optionally substituted aryl, heteroaryl, benzhydryl or benzyl; R.sup.4 and R.sup.5 each independently represent H, halo, C.sub.1-6 alkyl, oxo, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b ; R.sup.6 represents H or C.sub.1-6 alkyl; R.sup.7 represents C.sub.1-6 alkyl or optionally substituted phenyl; R.sup.8 represents H, COR.sup.a, CO.sub.2 R.sup.a, COCONR.sup.a R.sup.b, COCO.sub.2 R.sup.a, C.sub.1-6 alkyl optionally substituted by a variety of substituents, or C.sub.1-6 alkyl, optionally substituted by oxo, substituted by an optionally substituted aromatic heterocycle. The compounds are tachykinin antagonists useful for treating pain or inflammation, migraine or emesis.
摘要翻译： PCT No.PCT / EP94 / 00412 Sec。 371日期：1995年7月26日 102（e）日期1995年7月26日PCT 1994年2月10日PCT PCT。 WO94 / 19323 PCT出版物（I）的化合物本发明涉及式（I）化合物及其盐和前药，其中n为1,2或3，并且其中（CH 2）n的任何碳原子可以是被R4和/或R5取代; X表示O或S; R 1表示任选取代的（CH 2）q苯基，其中q是0,1,2或3; R 2表示任选取代的芳基，杂芳基，二苯甲基或苄基; R 4和R 5各自独立地表示H，卤素，C 1-6烷基，氧代，CO 2 R a或CONR a R b; R 6表示H或C 1-6烷基; R 7表示C 1-6烷基或任选取代的苯基; R8表示H，CORa，CO 2 R a，COCONR a R b，COCO 2 R a，任选被各种取代基取代的C 1-6烷基，或任选被氧代取代的被任选取代的芳族杂环取代的C 1-6烷基。这些化合物是可用于治疗疼痛或炎症，偏头痛或呕吐的速激肽拮抗剂。

9. 发明授权

US6087348A Use of NK-1 receptor antagonists for treating stress disorders 有权
标题翻译：使用NK-1受体拮抗剂治疗应激障碍
公开(公告)号：US6087348A
公开(公告)日：2000-07-11
申请号：US328743
申请日：1999-06-09
申请人： Raymond Baker , Neil Roy Curtis , Jason Matthew Elliott , Timothy Harrison , Gregory John Hollingworth , Philip Stephen Jackson , Janusz Jozef Kulagowski , Nadia Melanie Rupniak , Eileen Mary Seward , Christopher John Swain , Brian John Williams
发明人： Raymond Baker , Neil Roy Curtis , Jason Matthew Elliott , Timothy Harrison , Gregory John Hollingworth , Philip Stephen Jackson , Janusz Jozef Kulagowski , Nadia Melanie Rupniak , Eileen Mary Seward , Christopher John Swain , Brian John Williams
IPC分类号： A61K31/44 , A61K31/535 , A61K31/675 , A61K31/4445
CPC分类号： A61K31/44 , A61K31/535 , A61K31/675
摘要： The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist for the manufacture of a medicament adapted for oral administration for the treatment or prevention of stress disorders without concomitant therapy with other anti-stress agents, methods of treatment using such a NK-1 receptor antagonist and pharmaceutical compositions comprising it.
摘要翻译：本发明提供口服活性的长效CNS渗透剂NK-1受体拮抗剂在制备适于口服给药以治疗或预防应激障碍的药物中的用途，而不与其它抗应激剂同时治疗，使用这样的NK-1受体拮抗剂的药物组合物的方法和包含它的药物组合物。

10. 发明授权

US6060469A Spiro-piperidine derivatives and their use as tachykinin antagonists 失效
标题翻译：螺哌啶衍生物及其作为速激肽拮抗剂的用途
公开(公告)号：US6060469A
公开(公告)日：2000-05-09
申请号：US77063
申请日：1998-05-18
申请人： Raymond Baker , Timothy Harrison , Christopher John Swain , Brian John Williams
发明人： Raymond Baker , Timothy Harrison , Christopher John Swain , Brian John Williams
IPC分类号： A61K31/00 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4525 , A61K31/454 , A61K31/505 , A61K31/506 , A61P1/00 , A61P1/08 , A61P25/06 , A61P29/00 , A61P43/00 , C07D491/10 , C07D491/107 , C07D471/10
CPC分类号： C07D491/10
摘要： The present invention relates to compounds of formula (I), ##STR1## wherein R.sup.1 represents halogen, hydroxy, C.sub.1-6 alkyl group optionally substituted by one or three fluorine atoms, C.sub.1-6 alkoxy group optionally substituted by one to three fluorine atoms, or C.sub.1-6 alkylthio optionally substituted by one to three fluorine atoms; R.sup.2 represents hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or when R.sup.2 is adjacent to R.sup.1, they may be joined together such that there is formed a 5- or 6-membered saturated or unsaturated ring containing one or two oxygen atoms; R.sup.3 represents an optionally substituted 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur; m is 0-3 and n is 0-3, with the proviso that the sum total of m+n is 2 or 3; p is zero or 1; q is 1 or 2; and when m is 1 and n is 1 or 2, the broken line represents an optional double bond; R.sup.4, R.sup.5, R.sup.6, R.sup.9 and R.sup.10 are a variety of substituents defined in the specification; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, emesis and postherpetic neuralgia.
摘要翻译： PCT No.PCT / GB96 / 02853 Sec。 371日期1998年5月18日 102（e）日期1998年5月18日PCT提交1996年11月20日PCT公布。公开号WO97 / 19084 日期：1997年5月29日本发明涉及式（I）化合物，其中R 1表示卤素，羟基，任选被一个或三个氟原子取代的C 1-6烷基，任选被一至三个氟原子取代的C 1-6烷氧基，或任选被一至三个氟原子取代的C 1-6烷硫基; R 2表示氢，卤素，C 1-6烷基或C 1-6烷氧基; 或者当R 2与R 1相邻时，它们可以连接在一起，使得形成含有一个或两个氧原子的5-或6-元饱和或不饱和环; R3表示含有1,2,3或4个选自氮，氧和硫的杂原子的任选取代的5-或6-元芳族杂环基; m为0-3，n为0-3，条件是m + n的总和为2或3; p为零或1; q为1或2; 当m为1且n为1或2时，虚线表示任选的双键; R4，R5，R6，R9和R10是说明书中定义的各种取代基; 或其药学上可接受的盐。该化合物特别用于治疗或预防疼痛，炎症，呕吐和带状疱疹后神经痛。

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