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1. 发明授权

US06166040A Indole compounds 失效
标题翻译：吲哚化合物
公开(公告)号：US06166040A
公开(公告)日：2000-12-26
申请号：US309420
申请日：1999-05-11
申请人： John Fairhurst , Peter Thaddeus Gallagher , Martin Victor Miles , William Martin Owton , Colin William Smith
发明人： John Fairhurst , Peter Thaddeus Gallagher , Martin Victor Miles , William Martin Owton , Colin William Smith
IPC分类号： A61K31/4427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61P1/00 , A61P1/08 , A61P3/04 , A61P9/00 , A61P9/12 , A61P15/10 , A61P25/04 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P43/00 , C07D401/14 , A61K31/40 , A61K31/435 , C07D209/36 , C07D401/00
CPC分类号： C07D401/14
摘要： Pharmaceutical compounds of the formula: ##STR1## in which n is 1 to 6, m is 1 or 2 and p is 1 or 2, R.sup.1 and R.sup.2 are each hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, HO--C.sub.1-4 alkyl, C.sub.1-4 alkoxy-C.sub.1-4 alkyl, C.sub.1-4 alkylthio, halo, optionally substituted phenyl, optionally substituted phenyl-C.sub.1-4 alkyl, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a C.sub.3-6 cycloalkyl group, >C.dbd.O, C.dbd.NOR' where R' is hydrogen or C.sub.1-4 alkyl,R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, halo, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkyl-CO--, where m is 0, 1 or 2, R'R"N--SO.sub.2 --, --COOR', --CONR'R", --NR'R", --N(OR')COOR", --COR', --NHSO.sub.2 R', where R' and R' are each hydrogen or C.sub.1-4 alkyl,R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl,X is oxygen or sulphur,the dotted line represents an optional double bond, and the fluorine atom is attached at the 6- or 7-position; and salts thereof.
摘要翻译：下式的药物化合物：其中n为1至6，m为1或2，p为1或2，R 1和R 2各自为氢，C 1-4烷基，C 1-4烷氧基，HO-C 1-4烷基， C 1-4烷氧基-C 1-4烷基，C 1-4烷硫基，卤素，任选取代的苯基，任选取代的苯基-C 1-4烷基，或R 1和R 2与它们所连接的碳原子一起形成C 3-6环烷基基团，C = O，C = NOR，其中R'是氢或C 1-4烷基，R 3，R 4和R 5各自是氢，卤素，硝基，C 1-4烷基，C 1-4烷氧基，C 1-4烷基 - CO-，其中m是0,1或2，R'R''N-SO2-，-COOR'，-CONR'R“，-NR'R”，-N（OR'）COOR“ -COR'，-NHSO 2 R'，其中R'和R'各自为氢或C 1-4烷基，R 6和R 7各自为氢或C 1-4烷基，X为氧或硫，虚线为任选的双键，并且氟原子连接在6-或7-位; 及其盐。

2. 发明授权

US6075039A 5HT receptor binding benzimidazolylpiperidines 失效
标题翻译： 5HT受体结合苯并咪唑基哌啶
公开(公告)号：US6075039A
公开(公告)日：2000-06-13
申请号：US880450
申请日：1997-06-24
申请人： Peter Thaddeus Gallagher , Martin Victor Miles , William Martin Owton , Colin William Smith
发明人： Peter Thaddeus Gallagher , Martin Victor Miles , William Martin Owton , Colin William Smith
IPC分类号： A61K31/4427 , A61K31/445 , A61P25/00 , C07D401/06 , C07D407/14 , C07D413/14
CPC分类号： C07D401/06 , C07D407/14 , C07D413/14
摘要： A pharmaceutical compound of the formula ##STR1## in which X is --CR'R"-- or --C(O)-- where R' and R" are each hydrogen, C.sub.1-6 alkyl or optionally substituted phenyl, Y is oxygen or sulphur, R.sup.1, R.sup.2 and R.sup.7 are each selected from halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, nitro, cyano, amino, phenyl, phenoxy, benzyl, benzyloxy, acylamino, C.sub.1-4 alkylsulphonylamino, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphonyl, carboxamido, sulphonamido, hydroxy, methylenedioxy, carboxy, and heteroaryl, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each hydrogen, C.sub.1-6 alkyl or optionally substituted phenyl, n, m and p are each 0, 1, 2 or 3;or a salt or ester thereof.
摘要翻译：其中X为-CR'R“ - 或-C（O） - 的式的药物化合物，其中R'和R”各自为氢，C 1-6烷基或任选取代的苯基，Y为氧或硫， R1，R2和R7各自选自卤素，C1-4烷基，C1-4烷氧基，三氟甲基，硝基，氰基，氨基，苯基，苯氧基，苄基，苄氧基，酰氨基，C1-4烷基磺酰氨基，C1-4烷硫基，C1 -4-烷基磺酰基，甲酰氨基，磺酰氨基，羟基，亚甲二氧基，羧基和杂芳基，R 3，R 4，R 5和R 6各自为氢，C 1-6烷基或任选取代的苯基，n，m和p各自为0,1,2或 3; 或其盐或酯。

3. 发明授权

US5773448A Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US5773448A
公开(公告)日：1998-06-30
申请号：US833239
申请日：1997-04-14
申请人： Peter Thaddeus Gallagher , William Martin Owton , Colin William Smith
发明人： Peter Thaddeus Gallagher , William Martin Owton , Colin William Smith
IPC分类号： A61K31/40 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/55 , A61P1/00 , A61P1/08 , A61P3/04 , A61P9/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D209/30 , C07D209/34 , C07D209/38 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14
CPC分类号： C07D401/06
摘要： A pharmaceutical compound of the formula ##STR1## and salts and esters thereof.
摘要翻译：式（I）的药物化合物及其盐和酯。

4. 发明授权

US5663375A Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US5663375A
公开(公告)日：1997-09-02
申请号：US293786
申请日：1994-08-22
申请人： Michael Brunavs , Colin Peter Dell , Peter Thaddeus Gallagher , William Martin Owton , Colin William Smith
发明人： Michael Brunavs , Colin Peter Dell , Peter Thaddeus Gallagher , William Martin Owton , Colin William Smith
IPC分类号： A61K31/35 , A61K31/352 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/44 , A61K31/443 , A61K31/4433 , A61P1/16 , A61P3/10 , A61P9/10 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/06 , A61P43/00 , C07D311/92 , C07D405/04 , C07D407/04 , C07D409/04 , C07D215/00 , C07D333/62 , C07D409/00
CPC分类号： C07D405/04 , A61K31/35 , A61K31/36 , A61K31/38 , A61K31/40 , A61K31/44 , C07D311/92 , C07D407/04 , C07D409/04
摘要： Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 7, 8, 9 or 10, and each R.sup.1 is halo, carboxy, trifluoromethyl, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, nitrogen-containing heterocyclyl, nitro, trifluoromethoxy, --COOR.sup.5 where R.sup.5 is an ester group, --COR.sup.6, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl;R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl;R.sup.3 is nitrile, carboxy, --COOR.sup.8 where R.sup.8 is an ester group, or --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl; andR.sup.4 is --NR.sup.11 R.sup.12, --NR.sup.11 COR.sup.12, --N(COR.sup.11).sub.2 or --N.dbd.CHOCH.sub.2 R.sup.11 where R.sup.11 and R.sup.12 are each hydrogen or C.sub.1-4 alkyl optionally substituted with carboxy, --N.dbd.CH--NR.sup.13 R.sup.14 where R.sup.13 is hydrogen or C.sub.1-4 alkyl and R.sup.14 is C.sub.1-4 alkyl, optionally substituted phenyl or optionally substituted heteroaryl, ##STR2## where X is C.sub.2-4 alkylene, or --NHSO.sub.2 R.sup.15 where R.sup.15 is C.sub.1-4 alkyl, trifluoromethyl or optionally substituted phenyl; and salts thereof.
摘要翻译：其中n为0,1或2并且R 1连接在7,8,9或10位的任何位置的式“IMAGE”的药物化合物，并且每个R 1为卤素，羧基，三氟甲基，羟基，C 1-4烷基 C 1-4烷氧基，C 1-4烷硫基，羟基-C 1-4烷基，羟基-C 1-4烷氧基，含氮杂环基，硝基，三氟甲氧基，-COOR 5，其中R5是酯基，-COR6，-CONR6R7或 - NR 6 R 7，其中R 6和R 7各自为氢或C 1-4烷基; R 2是选自噻吩基，吡啶基，苯并噻吩基，喹啉基，苯并呋喃基或苯并咪唑基的苯基，萘基或杂芳基，所述苯基，萘基和杂芳基任选被取代，或R 2是任选被C 1-4烷基取代的呋喃基; R3是腈，羧基，-COOR8，其中R8是酯基，或-CONR9R10，其中R9和R10各自是氢或C1-4烷基; 并且R 4为-NR 11 R 12，-NR 11 COR 12，-N（COR 11）2或-N = CHOCH 2 R 11，其中R 11和R 12各自为氢或任选被羧基取代的C 1-4烷基，-N = CH-NR 13 R 14，其中R 13为氢或C1- 4烷基和R 14是C 1-4烷基，任选取代的苯基或任选取代的杂芳基，其中X是C 2-4亚烷基或-NHSO 2 R 15，其中R 15是C 1-4烷基，三氟甲基或任选取代的苯基; 及其盐。

5. 发明授权

US4027036A 3-Substituted propanoic acid derivatives and pharmaceutical composition 失效
标题翻译： 3-取代的丙酸衍生物和药物组合物
公开(公告)号：US4027036A
公开(公告)日：1977-05-31
申请号：US459829
申请日：1974-04-10
申请人： William Dawson , Michael John Foulis , Norman James Albert Gutteridge , Colin William Smith
发明人： William Dawson , Michael John Foulis , Norman James Albert Gutteridge , Colin William Smith
IPC分类号： A01N37/42 , A01N9/24 , C07C61/38
CPC分类号： A01N37/42
摘要： The invention provides 3-(2-formyl-3-hydroxy-5-oxocyclopent-1-enyl)-propanoic acid and derivatives thereof having anti-thrombotic activity coupled with low toxicity. Also provided is a method for preparing such compounds by subjecting a 3-[3-hydroxy-5-oxo-2-(.beta.-styryl)cyclopent-1-enyl]-propanoic acid or derivative thereof to oxidative cleavage.
摘要翻译：本发明提供具有抗血栓形成活性和低毒性的3-（2-甲酰基-3-羟基-5-氧代环戊-1-烯基） - 丙酸及其衍生物。还提供了通过使3- [3-羟基-5-氧代-2-（β-苯乙烯基）环戊-1-烯基] - 丙酸或其衍生物进行氧化裂解来制备此类化合物的方法。

6. 发明授权

US07148236B2 Modulators of acetylcholine receptors 失效
标题翻译：乙酰胆碱受体的调节剂
公开(公告)号：US07148236B2
公开(公告)日：2006-12-12
申请号：US10500516
申请日：2002-07-29
申请人： Peter Charles Astles , Stephen Richard Baker , Rowena Villanueva Cube , Jose Antonio Martinez-Perez , Ana Isabel Mateo Herranz , Jean Michel Vernier , Colin Peter Dell , Sonia Gutierrez , Lourdes Prieto , Martine Keenan , Adam Jan Sanderson , Colin William Smith
发明人： Peter Charles Astles , Stephen Richard Baker , Rowena Villanueva Cube , Jose Antonio Martinez-Perez , Ana Isabel Mateo Herranz , Jean Michel Vernier , Colin Peter Dell , Sonia Gutierrez , Lourdes Prieto , Martine Keenan , Adam Jan Sanderson , Colin William Smith
IPC分类号： A01N43/42 , A61K31/44 , C07D451/02 , C07D451/04 , C07D451/06
CPC分类号： A61K31/46 , A61K31/55 , C07D451/04 , C07D451/14
摘要： The present invention relates to compounds that modulate neurotransmission by promoting the release of neurotransmitters such as acetylcholine, dopamine and norepinephrine. More particularly, the present invention relates to thio-bridged aryl compounds that are capable of modulating acetylcholine receptors and pharmaceutical compositions comprising such compounds. The compounds disclosed are useful for the treatment of dysfunctions of the central and autonomic nervous systems.
摘要翻译：本发明涉及通过促进神经递质如乙酰胆碱，多巴胺和去甲肾上腺素的释放来调节神经传递的化合物。更具体地，本发明涉及能够调节乙酰胆碱受体的硫代桥连芳基化合物和包含这些化合物的药物组合物。所公开的化合物可用于治疗中枢神经系统和自主神经系统的功能障碍。

7. 发明授权

US4100350A 3-Substituted propanoic acid derivatives 失效
标题翻译： 3-取代的丙酸衍生物
公开(公告)号：US4100350A
公开(公告)日：1978-07-11
申请号：US773628
申请日：1977-03-02
申请人： William Dawson , Michael John Foulis , Norman James Albert Gutteridge , Colin William Smith
发明人： William Dawson , Michael John Foulis , Norman James Albert Gutteridge , Colin William Smith
IPC分类号： A01N37/42 , C07C79/46 , A01N9/24 , C07C69/76
CPC分类号： A01N37/42 , Y10S514/822
摘要： The invention provides 3-(2-formyl-3-hydroxy-5-oxocyclopent-1-enyl)-p ropanoic acid and derivatives thereof having anti-thrombotic activity coupled with low toxicity. Also provided is a method for preparing such compounds by subjecting a 3-[3-hydroxy-5-oxo-2-(.beta.-styryl)cyclopent-1-enyl]-propanoic acid or derivative thereof to oxidative cleavage.
摘要翻译：本发明提供具有抗血栓形成活性和低毒性的3-（2-甲酰基-3-羟基-5-氧代环戊-1-烯基） - 对 - 戊酸及其衍生物。还提供了通过使3- [3-羟基-5-氧代-2-（β-苯乙烯基）环戊-1-烯基] - 丙酸或其衍生物进行氧化裂解来制备此类化合物的方法。

8. 发明授权

US4039571A Organic derivatives 失效
标题翻译：有机衍生物
公开(公告)号：US4039571A
公开(公告)日：1977-08-02
申请号：US637782
申请日：1975-12-04
申请人： William Dawson , Michael John Foulis , Norman James Albert Gutteridge , Colin William Smith
发明人： William Dawson , Michael John Foulis , Norman James Albert Gutteridge , Colin William Smith
IPC分类号： C07C405/00 , C07D309/12 , C07F9/54 , C12P7/40 , C07C177/00
CPC分类号： C12P7/40 , C07C405/00 , C07D309/12 , C07F9/5407 , Y02P20/55 , Y10S435/874
摘要： Propanoic acid derivatives of formula: ##STR1## where X represents a ketonic or hydroxylic function, R.sup.1 is a C.sub.1.sub.-8 alkyl group optionally substituted by hydroxy or --COOH and R.sup.2 is hydrogen or a protecting group, having spasmolytic activity.
摘要翻译：其中X表示酮或羟基官能团，R1是任选被羟基或-COOH取代的C 1-8烷基，R 2是具有解吸活性的氢或保护基的丙酸衍生物。

9. 发明授权

US4000189A Pharmacologically active propanoic acid derivatives 失效
标题翻译：药物活性丙酸衍生物
公开(公告)号：US4000189A
公开(公告)日：1976-12-28
申请号：US459831
申请日：1974-04-10
申请人： William Dawson , Michael John Foulis , Norman James Albert Gutteridge , Colin William Smith
发明人： William Dawson , Michael John Foulis , Norman James Albert Gutteridge , Colin William Smith
IPC分类号： C07C59/84 , C07C65/22 , C07C65/14 , C07C65/20
CPC分类号： C07C59/84
摘要： The invention provides styryl cyclopentenyl propanoic acids and derivatives thereof having spasmolytic activity coupled with low toxicity. Also provided is a method of preparing styryl cyclopentenyl propanoic acid compounds which involves cyclising 7-hydroxy-5,8-dioxo-10-phenyldec-9-enoic acid in the presence of a base.

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