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41. 发明授权

US4855323A Leukotriene antagonists, a process for the preparation thereof, and the use thereof for the treatment of diseases 失效
标题翻译：白三烯拮抗剂，其制备方法及其用于治疗疾病的用途
公开(公告)号：US4855323A
公开(公告)日：1989-08-08
申请号：US223129
申请日：1988-07-22
申请人： Gunther Wess , Wilhelm Bartmann , Gerhard Beck , Hiristo Anagnostopulos
发明人： Gunther Wess , Wilhelm Bartmann , Gerhard Beck , Hiristo Anagnostopulos
IPC分类号： A61K31/38 , A61K31/085 , A61K31/10 , A61K31/12 , A61K31/165 , A61K31/19 , A61K31/215 , A61K31/22 , A61K31/381 , A61K31/395 , A61K31/41 , A61K31/44 , A61K31/535 , A61K31/5375 , A61P1/04 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07C41/00 , C07C43/00 , C07C43/178 , C07C43/20 , C07C43/235 , C07C43/263 , C07C45/00 , C07C47/52 , C07C49/84 , C07C51/00 , C07C59/125 , C07C65/21 , C07C67/00 , C07C69/007 , C07C69/025 , C07C69/675 , C07C69/92 , C07C201/00 , C07C235/06 , C07C235/16 , C07C239/00 , C07C239/14 , C07C313/00 , C07C317/00 , C07C317/04 , C07C317/18 , C07C317/22 , C07C317/24 , C07C317/44 , C07C317/46 , C07C323/16 , C07C323/19 , C07C323/22 , C07C323/52 , C07C323/56 , C07C323/60 , C07C323/65 , C07D213/30 , C07D257/04 , C07D295/18 , C07D317/36 , C07D333/16
CPC分类号： C07D317/36 , A61K31/10 , A61K31/215 , C07C323/00
摘要： Leukotriene antagonists, a process for the preparation thereof, and the use thereof for the treatment of diseases ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and X have the indicated meanings, a process for the preparation of these compounds, the use thereof as pharmaceuticals, and pharmaceutical products based on these compounds, are described.
摘要翻译：白细胞三烯拮抗剂，其制备方法及其用于治疗其中R1，R2，R3，R4，R5和X具有指定含义的疾病的用途，其制备方法化合物，其作为药物的用途，以及基于这些化合物的药物。

42. 发明授权

US4833161A Carboxylic acid derivatives and pharmaceutical compositions and uses 失效
标题翻译：羧酸衍生物和药物组合物及用途
公开(公告)号：US4833161A
公开(公告)日：1989-05-23
申请号：US141312
申请日：1988-01-06
申请人： Hans P. Wolff , Hans-Frieder Kuhnle
发明人： Hans P. Wolff , Hans-Frieder Kuhnle
IPC分类号： A61K31/19 , A61K31/195 , A61K31/33 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61P3/00 , A61P3/08 , A61P3/10 , C07C59/64 , C07C67/00 , C07C229/22 , C07C313/00 , C07C315/00 , C07C315/02 , C07C315/04 , C07C317/46 , C07C317/48 , C07C319/14 , C07C319/20 , C07C323/52 , C07C323/54 , C07C323/56 , C07C323/65 , C07D213/55 , C07D233/64 , C07D263/32 , C07D307/54 , C07D333/24 , C07D333/32 , C07D333/34 , C07D521/00
CPC分类号： C07D333/24
摘要： The present invention provides carboxylic acid derivatives of the general formula: ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are optionally substituted aryl radicals or optionally substituted heterocyclic radicals, A is a straight-chained or branched, saturated or unsaturated alkylene chain containing up to 10 carbon atoms which can contain an oxygen, sulphur or nitrogen atom and is optionally substituted by a hydroxyl group, Y is an S(O).sub.n group or an oxygen atom, n is 0, 1 or 2 and B is a valency bond or a saturated or unsaturated alkylene radical containing up to 5 carbon atoms; as well as the physiologically acceptable salts, esters and amides thereof, with the proviso that(a) R.sub.1 and R.sub.2 are not simultaneously aryl radicals and(b) when an unsaturated alkylene chain is present which contains a heteroatom, the heteroatom is not connected to an unsaturated aliphatic carbon atom.The present invention also provides processes for the preparation of these new compounds and pharmaceutical compositions containing them.
摘要翻译：本发明提供以下通式的羧酸衍生物：其中R 1和R 2可以相同或不同，是任选取代的芳基或任选取代的杂环基，A是直链或支链的，含有至多10个碳原子的饱和或不饱和亚烷基链，其可以含有氧，硫或氮原子，并且任选被羟基取代，Y是S（O）n基团或氧原子，n是0,1 或2和B是价键或含有至多5个碳原子的饱和或不饱和亚烷基; 以及其生理上可接受的盐，酯和酰胺，条件是（a）R 1和R 2不同时为芳基，和（b）当存在含有杂原子的不饱和亚烷基链时，杂原子不连接不饱和脂肪族碳原子。本发明还提供了制备这些新化合物和含有它们的药物组合物的方法。

43. 发明授权

US4741846A 2,4,6-trifunctionalized phenols 失效
标题翻译： 2,4,6-三官能化酚
公开(公告)号：US4741846A
公开(公告)日：1988-05-03
申请号：US758014
申请日：1985-07-24
申请人： Samuel Evans
发明人： Samuel Evans
IPC分类号： C07C67/00 , C07C313/00 , C07C323/16 , C07C323/52 , C07C323/56 , C08K5/375 , C09K15/14 , C09K15/28 , C09K15/30 , C10M135/24 , C10M135/26 , C10M135/32 , C10M169/04 , C10N30/00 , C10N30/08 , C10N30/10 , C10N40/25 , C07C149/273
CPC分类号： C10M135/24 , C07C323/00 , C08K5/375 , C09K15/14 , C10M2215/14 , C10M2215/18 , C10M2215/182
摘要： Novel compounds of the formula I ##STR1## are described. The radicals R.sup.1, R.sup.2 and R.sup.3 are hydroxyl-substituted alkyl, --C(R.sup.4 R.sup.5)--(CHR.sup.6).sub.m --W, --(CH.sub.2).sub.2 --OCOR.sup.10 or ##STR2## and W is --COR.sup.7, --COOR.sup.7, --CON(R.sup.9 R.sup.15) or CN. The other radicals are customary hydrocarbon radicals.The novel substances can be employed as stabilizers for organic polymers or for lubricants.
摘要翻译：描述了式I的新型化合物（I）。基团R 1，R 2和R 3是羟基取代的烷基，-C（R 4 R 5） - （CHR 6）m W， - （CH 2）2 -OCOR 10或者X和W是-COR 7，-COOR 7，-CON（R 9 R 15）或 CN。其他基团是常规烃基。新型物质可用作有机聚合物或润滑剂的稳定剂。

44. 发明授权

US4740514A Tetrazole substituted compounds and their anti-allergic use 失效
标题翻译：四唑取代的化合物及其抗过敏用途
公开(公告)号：US4740514A
公开(公告)日：1988-04-26
申请号：US866663
申请日：1986-05-27
申请人： John Goldsworthy , Winston S. Marshall , John P. Verge
发明人： John Goldsworthy , Winston S. Marshall , John P. Verge
IPC分类号： A61K31/41 , A61P11/00 , A61P37/08 , C07C67/00 , C07C313/00 , C07C315/02 , C07C317/24 , C07C317/44 , C07C323/22 , C07C323/56 , C07C323/62 , C07C323/65 , C07C325/00 , C07C331/10 , C07D257/04
CPC分类号： C07D257/04
摘要： There are described compounds of the formula ##STR1## in which R.sup.1 is hydrogen or C.sub.1-6 alkyl, R.sup.2 is hydrogen, C.sub.1-6 alkyl or C.sub.3-6 alkenyl, X and Y are each oxygen, sulphur, sulphinyl or sulphonyl, n is 2 to 6 and Z is 1H-tetrazol-5-yl, 1H-tetrazol-5-ylthio, 1H-tetrazol-5-ylsulphinyl, 1H-tetrazol-5-ylsulphonyl, cyano or thiocyano, provided that when both X and Y are oxygen Z is 1H-tetrazol-5-ylthio, 1H-tetrazol-5-ylsulphinyl, 1H-tetrazol-5-ylsulphonyl or thiocyano; and salts thereof. The compounds in which Z is other than cyano or thiocyano have pharmaceutical activity and inhibit leukotriene action or formation.

45. 发明授权

US4594197A 3-benzoyl-2-mercaptopropionic acid derivatives 失效
标题翻译： 3-苯甲酰基-2-巯基丙酸衍生物
公开(公告)号：US4594197A
公开(公告)日：1986-06-10
申请号：US646230
申请日：1984-08-31
申请人： Kazuyuki Tomisawa , Kazuya Kameo , Toru Matsunaga , Shiuji Saito , Yoshimoto Nakashima , Kaoru Sota
发明人： Kazuyuki Tomisawa , Kazuya Kameo , Toru Matsunaga , Shiuji Saito , Yoshimoto Nakashima , Kaoru Sota
IPC分类号： A61K31/195 , A61K31/19 , A61K31/194 , A61K31/215 , A61P3/00 , A61P29/00 , A61P37/04 , C07C59/84 , C07C59/88 , C07C59/90 , C07C67/00 , C07C313/00 , C07C323/56 , C07C327/20 , C07C327/22 , C07C149/40 , C07C153/023 , C07C157/09
CPC分类号： C07C327/00 , C07C323/00 , C07C59/84 , C07C59/88 , C07C59/90
摘要： 3-Benzoyl-2-mercaptopropionic acid derivatives represented by the general formula ##STR1## (wherein, X represents a hydrogen atom, a halogen atom, hydroxy group, a lower alkyl group or a lower alkoxy group, Y represents a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group, Z represents a hydrogen atom or an acyl group, and R represents a hydrogen atom or a lower alkyl group). These compounds have immunomodulative function and are effective for the treatment of diseases caused by abnormal immunofunction.
摘要翻译：由通式“IMAGE”表示的3-苯甲酰基-2-巯基丙酸衍生物（其中，X表示氢原子，卤素原子，羟基，低级烷基或低级烷氧基，Y表示氢原子，卤素原子，低级烷基或低级烷氧基，Z表示氢原子或酰基，R表示氢原子或低级烷基）。这些化合物具有免疫调节功能，对于治疗异常免疫功能引起的疾病有效。

46. 发明授权

US4513005A SRS-A antagonists 失效
标题翻译： SRS-A拮抗剂
公开(公告)号：US4513005A
公开(公告)日：1985-04-23
申请号：US386570
申请日：1982-06-09
申请人： Stephen R. Baker , William B. Jamieson , William J. Ross , Alec Todd
发明人： Stephen R. Baker , William B. Jamieson , William J. Ross , Alec Todd
IPC分类号： C07B45/04 , C07C317/46 , C07C323/22 , C07C323/56 , C07C323/58 , C07D303/40 , C07D303/42 , C07D307/38 , C07D309/12 , C07D309/30 , C07D313/04 , C07F9/53 , C07K5/06 , C07C149/20 , A61K31/23 , A61K31/335
CPC分类号： C07D307/38 , C07B45/04 , C07C317/46 , C07C323/22 , C07C323/56 , C07C323/58 , C07D303/40 , C07D303/42 , C07D309/12 , C07D309/30 , C07D313/04 , C07F9/5304 , C07F9/5325 , C07K5/06034
摘要： There are described pharmacologically active compounds, useful in the treatment of allergic/inflammatory disorders involving SRS-A as causal mediator and which, in free acid form, are of formula I, ##STR1## in which R.sub.1 is (i) an aliphatic, saturated or unsaturated hydrocarbyl radical of up to 20 carbon atoms, unsubstituted or substituted by at least one substituent selected from halogen, hydroxy, C.sub.3-6 alkoxy, C.sub.3-6 cycloalkyl, aryl or heteroaryl, the cycloalkyl, aryl or heteroaryl being unsubstituted or substituted by at least one substituent selected from hydroxy, halogen and alkyl, alkenyl or alkynyl of up to 10 carbon atoms,(ii) cycloalkyl of 3 to 8 carbon atoms unsubstituted or substituted by alkyl, alkenyl or alkynyl of up to 16 carbon atoms, or(iii) aryl or heteroaryl, unsubstituted or substituted by hydroxyl, C.sub.1-4 alkoxy, halogen or alkyl, alkenyl or alkynyl of up to 16 carbon atoms; and R.sub.2 is(i) alkyl, cycloalkyl or alkenyl of up to 10 carbon atoms, unsubstituted or substituted by one or more substituents selected from aryl, cycloalkyl, halogen, hydroxy, NHR.sub.3 and COX, where R.sub.3 is H, C.sub.1-4 alkyl, aryl or an amino acid residue or COX, and X is OH, C.sub.1-4 alkyl, NH.sub.2 or an amino acid residue, or(ii) aryl or heteroaryl, unsubstituted or substituted by one or more substituents selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.2-5 acyl, halogen, hydroxy, carboxy, nitro, trihalomethyl, phenyl, C.sub.1-4 acylamino and NHR.sub.4, where R.sub.4 is hydrogen or C.sub.1-4 alkyl; and Y is --S--, --SO-- or --SO.sub.2 --,with the proviso that when --YR.sub.2 is glutathionyl, cysteinyl or cysteinylglycinyl, then R.sub.1 is other than an unsubstituted alkatetraenyl or alkapentaenyl radical of 12 to 16 carbon atoms.
摘要翻译：描述了用于治疗涉及SRS-A作为因果介质的过敏性/炎症性疾病，其游离酸形式为式I的化学活性化合物，其中R 1是（i）脂族，至少20个碳原子的饱和或不饱和烃基，未被取代或被至少一个选自卤素，羟基，C 3-6烷氧基，C 3-6环烷基，芳基或杂芳基的取代基取代，环烷基，芳基或杂芳基是未取代或取代的至少一个选自羟基，卤素和至多10个碳原子的烷基，烯基或炔基的取代基，（ii）未被取代或被至多16个碳原子的烷基，烯基或炔基取代的3至8个碳原子的环烷基，或（iii）未被取代或被羟基，C 1-4烷氧基，卤素或至多16个碳原子的烷基，链烯基或炔基取代的芳基或杂芳基; 并且R 2是（i）至少10个碳原子的烷基，环烷基或链烯基，未被取代或被一个或多个选自芳基，环烷基，卤素，羟基，NHR 3和COX的取代基取代，其中R 3是H，C 1-4烷基，芳基或氨基酸残基或COX，X为OH，C 1-4烷基，NH 2或氨基酸残基，或（ii）未被取代或被一个或多个选自C 1-4烷基，C 1 -4-烷氧基，C 2-5酰基，卤素，羟基，羧基，硝基，三卤甲基，苯基，C 1-4酰基氨基和NHR 4，其中R 4是氢或C 1-4烷基; 并且Y是-S-，-SO-或-SO 2 - ，条件是当-YR 2是谷胱甘肽基，半胱氨酰基或半胱氨酰甘氨酰基时，则R 1不同于未被取代的具有12至16个碳原子的烷基四烯基或烷基五烯基。

47. 发明授权

US4472316A 3-Benzoyl-2-mercaptopropionic acid derivatives 失效
标题翻译： 3-苯甲酰基-2-巯基丙酸衍生物
公开(公告)号：US4472316A
公开(公告)日：1984-09-18
申请号：US469000
申请日：1983-02-23
申请人： Kaoru Sota , Yasuhide Tachi , Kazuyuki Tomisawa , Kazuya Kameo , Toru Matsunaga , Jiro Sawada
发明人： Kaoru Sota , Yasuhide Tachi , Kazuyuki Tomisawa , Kazuya Kameo , Toru Matsunaga , Jiro Sawada
IPC分类号： A61K31/215 , A61K31/19 , A61P9/10 , C07C59/84 , C07C67/00 , C07C313/00 , C07C323/56 , C07C327/20 , C07C327/22 , C07C149/43 , C07C153/01
CPC分类号： C07C59/84 , C07C323/00 , C07C327/00
摘要： Novel compounds having the general formula ##STR1## wherein X is hydrogen or halogen, Y is hydrogen, halogen, methoxy or alkyl having 1 to 3 carbon atoms, Z is hydrogen, alkylcarbonyl having 2 to 6 carbon atoms or benzoyl, and R is hydrogen, alkali metal or alkyl having 1 to 5 carbon atoms, are disclosed. These compounds exhibit excellent hypolipidemic activity and little or no side effect.
摘要翻译：具有通式的新型化合物，其中X为氢或卤素，Y为氢，卤素，甲氧基或具有1至3个碳原子的烷基，Z为氢，具有2至6个碳原子的烷基羰基或苯甲酰基，R为氢，碱金属或具有1至5个碳原子的烷基。这些化合物表现出优异的降血脂活性，很少或没有副作用。

48. 发明授权

US4239915A Perfluoroalkyl carboxylic acids 失效
标题翻译：全氟烷基羧酸
公开(公告)号：US4239915A
公开(公告)日：1980-12-16
申请号：US747114
申请日：1976-12-02
申请人： Robert A. Falk
发明人： Robert A. Falk
IPC分类号： C09K3/18 , A01N25/30 , A61K8/70 , A61K47/12 , A61K47/20 , A61Q5/02 , A61Q17/00 , A61Q19/00 , A62D1/00 , B01F17/00 , B41N1/00 , B41N3/08 , C07C51/347 , C07C67/00 , C07C313/00 , C07C317/00 , C07C317/04 , C07C317/44 , C07C323/25 , C07C323/52 , C07C323/56 , C09D11/02 , C09K8/584 , C11D1/00 , C11D1/06 , D06M13/184 , D06M13/248 , G03C1/34 , G03C1/38 , G03C5/305 , G03C11/06
CPC分类号： A61Q19/00 , A01N25/30 , A61K47/12 , A61K47/20 , A61K8/70 , A62D1/00 , C07C317/44 , C07C323/25 , C07C323/52 , C07C323/56 , C09D11/03 , C09K8/584 , C11D1/004 , G03C1/34 , G03C1/385 , G03C11/06 , G03C5/3053 , A61Q17/00 , A61Q5/02 , B41N1/003
摘要： Gem-perfluoroalkylthio group containing acids of the formula(R.sub.f --R.sub.1 --X--.sub.2 C(R.sub.2)--B--(COOH).sub.gand alkyl esters thereof, wherein R.sub.f is a perfluoroalkyl, R.sub.1 is alkylene or alkylenethio- or oxy- or imino- alkylene, R.sub.2 is hydrogen, alkyl or phenyl, B is a covalent bond, alkylene or alkanetriyl and g is 1 or 2, can be prepared by the addition of a perfluoroalkylthiol to aldehydo or keto acids or esters. The compounds are useful as surface active agents, as intermediates to fluorochemical chromium complexes with low surface energies, or as oil and water repellents for textiles.
摘要翻译：含有式（Rf-R1-X-2C（R2）-B-（COOH）g的酸及其烷基酯的Gem-全氟烷基硫基，其中Rf是全氟烷基，R1是亚烷基或亚烷基或羟基或亚氨基 - 亚烷基，R 2是氢，烷基或苯基，B是共价键，亚烷基或烷三三烷基，g是1或2，可以通过向醛或酮酸或酯加入全氟烷基硫醇来制备，这些化合物可用作表面活性剂作为具有低表面能的含氟铬络合物的中间体，或作为纺织品的防油和防水剂。

49. 发明授权

US3985788A Phenyl propionic acids and derivatives thereof 失效
标题翻译：苯丙酸及其衍生物
公开(公告)号：US3985788A
公开(公告)日：1976-10-12
申请号：US403516
申请日：1973-10-04
申请人： Julius Diamond
发明人： Julius Diamond
IPC分类号： A61K31/19 , A61K31/21 , A61K31/26 , A61K31/27 , C07C47/55 , C07C57/58 , C07C205/56 , C07C205/61 , C07C229/34 , C07C233/47 , C07C255/57 , C07C313/30 , C07C317/44 , C07C323/56 , C07C327/32 , C07C381/02 , C07D277/34 , C07D277/54 , C07C63/33 , C07C69/76
CPC分类号： C07D277/54 , A61K31/19 , A61K31/21 , A61K31/26 , A61K31/27 , C07C205/56 , C07C205/61 , C07C229/34 , C07C233/47 , C07C255/57 , C07C313/30 , C07C317/44 , C07C323/56 , C07C327/32 , C07C381/02 , C07C47/55 , C07C57/58 , C07D277/34 , C07C2101/14
摘要： Novel .alpha.-halo-.beta.-(4-cyclohexylphenyl)propionic acids and their salts and esters are described. Therapeutic compositions containing same and a method of treating inflammation by their administration are also disclosed.
摘要翻译：描述了新的α-卤代-β-（4-环己基苯基）丙酸及其盐和酯。还公开了含有其的治疗组合物及其给药治疗炎症的方法。

50. 发明授权

US3867435A Substituted phenylacetic acid compounds 失效
标题翻译：取代的苯甲酸化合物
公开(公告)号：US3867435A
公开(公告)日：1975-02-18
申请号：US23371772
申请日：1972-03-10
申请人： RORER INC WILLIAM H
发明人： DIAMOND JULIUS , SANTORA NORMAN J
IPC分类号： A61K31/19 , A61K31/21 , A61K31/26 , A61K31/27 , C07C57/58 , C07C57/62 , C07C205/56 , C07C205/59 , C07C205/61 , C07C229/34 , C07C233/47 , C07C255/57 , C07C313/30 , C07C317/44 , C07C323/56 , C07C327/32 , C07C381/02 , C07D277/34 , C07D277/54 , C07C63/32 , C07C69/62
CPC分类号： C07C255/57 , A61K31/19 , A61K31/21 , A61K31/26 , A61K31/27 , C07C57/58 , C07C57/62 , C07C205/56 , C07C205/59 , C07C205/61 , C07C229/34 , C07C233/47 , C07C313/30 , C07C317/44 , C07C323/56 , C07C327/32 , C07C381/02 , C07C2601/14 , C07D277/34 , C07D277/54
摘要： Certain substituted Alpha -halo and Alpha mercaptophenylacetic acids and substituted phenylacetic acids having in Alpha -position a sulfur-containing group, a cyano group, or an amino group, their substantially non-toxic esters, salts, and acid amides as well as 5-phenyl substituted 2-imino-4oxothiazolidines and 5-phenyl substituted 2,4-dioxothiazolidines have a high anti-inflammatory, analgesic, and antipyretic activity, low toxicity, and/or a favorable therapeutic index with minor or no side-effects. Preferred compounds of this invention are Alpha ,m-dichloro-p-cyclohexylphenylacetic acids and its esters and salts.
摘要翻译：某些取代的α-卤代和α-巯基苯乙酸和具有α位的含硫基团，氰基或氨基的取代的苯乙酸，其基本上无毒的酯，盐和酰胺以及5 - 苯基取代的2-亚氨基-4-氧代噻唑烷和5-苯基取代的2,4-二氧代噻唑烷具有很高的抗炎，镇痛和解热活性，低毒性和/或有利的治疗指数，轻微或无副作用。本发明优选的化合物是α，间二氯对环己基苯基乙酸及其酯和盐。

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