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41. 发明申请

US20030114649A1 5,5-Disubstituted thiazolidine derivative pesticides 失效
标题翻译： 5,5-二取代噻唑烷衍生物农药
公开(公告)号：US20030114649A1
公开(公告)日：2003-06-19
申请号：US10241625
申请日：2002-09-11
申请人： Nippon Soda Co., Ltd.
发明人： Isao Iwataki , Vladimir F. Rudchenko , Thomas Kurz , Charles R. Semer IV , Thomas A. Kucharek , Detlef Geffken
IPC分类号： C07H017/02 , C07D417/02 , C07D277/14
CPC分类号： C07D277/50 , C07D277/42 , C07D277/54
摘要： Fungicidal 5,5-disubstituted thiazolidine derivatives are provided having the formula; 1 wherein R1 is selected from the group consisting of C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 cycloalkyl, and optionally substituted phenyl; R2 is phenyl substituted by An; A is each independently selected from the group consisting of H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 alkenyloxy, C1-C6 alkynyloxy, nitro, optionally substituted amino, C1-C6 alkylthio, C1-C6 alkoxycarbonyl, phenoxy, phenyl, optionally substituted pyridyl, optionally substituted thienyl, and optionally substituted furyl; n is 0-5; X is O; Y is selected from the group consisting of O, S, NnullOH, optionally substituted arylimino, optionally substituted alkylimino, optionally substituted carbamoyloxyimino, optionally substituted sulfamoyloxyimino, optionally substituted aroyloxyimino, optionally substituted alkoxycarbonyloxyimino, optionally substituted alkylhydrazono, optionally substituted phenylhydrazono, and alkylsulfenyl; and Z is optionally substituted phenylamino.
摘要翻译：提供具有下式的杀真菌的5,5-二取代的噻唑烷衍生物：其中R 1选自C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6环烷基和任选取代的苯基; R2是被An取代的苯基; A各自独立地选自H，卤素，C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6烷氧基，C 1 -C 6烯氧基，C 1 -C 6炔氧基，硝基，任选取代的氨基，C 1 -C 6烷硫基， C 1 -C 6烷氧基羰基，苯氧基，苯基，任选取代的吡啶基，任选取代的噻吩基和任选取代的呋喃基; n为0-5; X是O; Y选自O，S，N-OH，任选取代的芳基亚氨基，任选取代的烷基亚氨基，任选取代的氨基甲酰氧基亚氨基，任选取代的氨磺酰氧基亚氨基，任选取代的芳酰氧基亚氨基，任选取代的烷氧基羰基氧亚氨基，任选取代的烷基亚肼基，任选取代的苯基亚肼基， ; Z是任选取代的苯基氨基。

42. 发明授权

US06344484B1 Tyrosine alkoxyguanidines as integrin inhibitors 有权
标题翻译：酪氨酸烷氧基胍作为整联蛋白抑制剂
公开(公告)号：US06344484B1
公开(公告)日：2002-02-05
申请号：US09502006
申请日：2000-02-11
申请人： Bruce E. Tomczuk , Yu Kai Lee
发明人： Bruce E. Tomczuk , Yu Kai Lee
IPC分类号： A61K31216
CPC分类号： C07D333/62 , C07C311/06 , C07C311/10 , C07C311/13 , C07C311/19 , C07C311/29 , C07C311/42 , C07C311/46 , C07C317/14 , C07C2602/42 , C07D231/18 , C07D233/84 , C07D271/12 , C07D277/54 , C07D311/70 , C07D333/34 , C07D409/04
摘要： The present invention relates to novel tyrosine alkoxyguanidine compounds that are inhibitors of alpha V (&agr;v) integrins, for example &agr;v&bgr;3 and &agr;v&bgr;5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by &agr;v&bgr;3 and &agr;v&bgr;5 integrins, including conditions such as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, m and n are defined herein.
摘要翻译：本发明涉及作为αV（alphav）整联蛋白抑制剂的新型酪氨酸烷氧基胍化合物，例如阿尔法博3和阿尔法肽5整联蛋白，其药学上可接受的盐及其药物组合物。这些化合物可用于治疗由α1β和α-α5整联蛋白介导的病理状态，包括肿瘤生长，转移，再狭窄，骨质疏松症，炎症，黄斑变性，糖尿病性视网膜病变和类风湿性关节炎等疾病。这些化合物具有以下通式：其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R11，m和n如本文所定义。

43. 发明授权

US06335334B1 Sulfur substituted sulfonylaminocarboxylic acid N-arylamides, their preparation, their use and pharmaceutical preparations comprising them 有权
标题翻译：硫取代磺酰氨基羧酸N-芳基酰胺，其制备方法及其应用和包含它们的药物制剂
公开(公告)号：US06335334B1
公开(公告)日：2002-01-01
申请号：US09349933
申请日：1999-07-08
申请人： Ursula Schindler , Karl Schönafinger , Hartmut Strobel
发明人： Ursula Schindler , Karl Schönafinger , Hartmut Strobel
IPC分类号： A61K315375
CPC分类号： C07C311/21 , C07C311/46 , C07C311/51 , C07C311/58 , C07C317/40 , C07C323/42 , C07C323/52 , C07C323/60 , C07C331/12 , C07C2601/02 , C07C2601/14 , C07C2602/04 , C07C2602/08 , C07D207/12 , C07D207/16 , C07D207/20 , C07D207/48 , C07D209/10 , C07D209/14 , C07D211/46 , C07D211/54 , C07D211/62 , C07D211/96 , C07D213/71 , C07D213/78 , C07D213/80 , C07D213/82 , C07D215/36 , C07D221/20 , C07D231/18 , C07D231/38 , C07D231/42 , C07D233/84 , C07D235/18 , C07D239/06 , C07D239/26 , C07D239/42 , C07D243/08 , C07D261/10 , C07D261/16 , C07D265/30 , C07D277/04 , C07D277/36 , C07D277/46 , C07D277/52 , C07D277/54 , C07D277/64 , C07D279/12 , C07D295/26 , C07D333/34 , C07D333/38 , C07D333/40 , C07D401/12 , C07D413/12 , C07D491/10
摘要： The present invention relates to compounds of the formula I wherein A1, A2, R1, R2, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.
摘要翻译：本发明涉及式I化合物，其中A1，A2，R1，R2，R3，X和n如权利要求中所定义，它们是用于治疗和预防疾病的有价值的药物活性化合物，例如心血管疾病如高血压，心绞痛，心功能不全，血栓形成或动脉粥样硬化。式I的化合物能够调节身体的环鸟苷酸（cGMP）的产生，并且通常适用于治疗和预防与扰乱的cGMP平衡相关的疾病。本发明还涉及制备式I化合物的方法，其用于治疗和预防上述疾病和用于制备用于此目的的药物以及包含式I化合物的药物制剂。

44. 发明授权

US6124351A Amino acid derivatives having a nitric oxide synthase inhibiting action 失效
标题翻译：具有一氧化氮合酶抑制作用的氨基酸衍生物
公开(公告)号：US6124351A
公开(公告)日：2000-09-26
申请号：US776928
申请日：1997-02-11
申请人： Toshihiko Makino , Toshiaki Nagafuji
发明人： Toshihiko Makino , Toshiaki Nagafuji
IPC分类号： C07C335/32 , C07D277/18 , C07D277/28 , C07D277/42 , C07D277/54 , C07D279/06 , A61K31/215
CPC分类号： C07C335/32 , C07D277/18 , C07D277/42 , C07D277/54 , C07D279/06
摘要： Compounds represented by the general formula (I): ##STR1## (where R.sub.1 denotes a hydrogen atom, a straight-chained or branched alkoxycarbonyl group having 1-6 carbon atoms in which the alkyl portion may optionally have a substituent, or an optionally substituted straight-chained or branched acyl group having 1-9 carbon atoms;R.sub.2 denotes a hydrogen atom or an optionally substituted straight-chained or branched alkyl group having 1-6 carbon atoms;R.sub.3 denotes an optionally substituted straight-chained or branched alkyl group having 1-6 carbon atoms or an optionally substituted straight-chained or branched alkenyl group having 2-6 carbon atoms;R.sub.4 denotes a hydrogen atom;or alternatively R.sub.3 and R.sub.4 may combine together to form an optionally substituted 5- to 7-membered ring; andn denotes an integer of 2-4, provided that when R.sub.3 is a methyl group, n is not 3 at the same time) or pharmaceutically acceptable salts thereof.
摘要翻译： PCT No.PCT / JP95 / 01630 Sec。 371日期1997年2月11日 102（e）日期1997年2月11日PCT 1995年8月16日PCT PCT。公开号WO96 / 06076 日期：2002年2月29日由通式（I）表示的化合物：其中R1表示氢原子，烷基部分可以具有取代基的具有1-6个碳原子的直链或支链烷氧基羰基，或任选取代的具有1-9个碳原子的直链或支链酰基; R2表示氢原子或任选取代的具有1-6个碳原子的直链或支链烷基; R3表示任选取代的直链或支链烷基具有1-6个碳原子的基团或具有2-6个碳原子的任选取代的直链或支链烯基; R4表示氢原子;或者R3和R4可以结合在一起形成任选取代的5-至7-元环; n表示2-4的整数，条件是当R3为甲基时，n不同时为3）或其药学上可接受的盐。

45. 发明授权

US5491158A Thiosemicarbazonethiones 失效
标题翻译：硫代氨基硫脲
公开(公告)号：US5491158A
公开(公告)日：1996-02-13
申请号：US244081
申请日：1994-05-16
申请人： Martin Missbach
发明人： Martin Missbach
IPC分类号： A61K31/425 , A61K31/426 , A61K31/44 , A61P29/00 , C07D277/20 , C07D277/50 , C07D277/54 , C07D417/12
CPC分类号： C07D417/12 , C07D277/54
摘要： The invention relates to novel thiosemicarbazonethiones of formula (I) wherein R.sub.1 is lower alkyl, lower alk-2-en-1-yl or also lower alk-2-yn-1-yl, R.sub.2 and R.sub.3 are each independently of the other hydrogen or lower alkyl or, taken together, are lower alkylidene, R.sub.4 is hydrogen, lower alkyl, lower alkoxy, aryl or aryl-lower alkyl, R.sub.5 is lower alkyl, aryl, aryl-lower alkyl, unsaturated or saturated heterocyclyl-lower alkyl, or is also lower alkyloxycarbonyl-lower alkyl, and the salts thereof, to a process for the preparation of these compounds, to pharmaceutical compositions containing them, and to the use thereof as medicaments. ##STR1##
摘要翻译： PCT No.PCT / EP93 / 02607 Sec。 371日期1994年5月16日 102（e）日期1994年5月16日PCT提交1993年9月25日PCT公布。出版物WO94 / 07874 日本1994年4月14日。本发明涉及式（I）的新型硫代缩氨基硫脲，其中R 1为低级烷基，低级烷-2-烯-1-基或低级烷-2-炔-1-基，R2和R3 各自独立地为氢或低级烷基，或者一起为低级亚烷基，R4为氢，低级烷基，低级烷氧基，芳基或芳基 - 低级烷基，R5为低级烷基，芳基，芳基 - 低级烷基，不饱和或不饱和的饱和的杂环基 - 低级烷基，或者也可以是低级烷氧基羰基 - 低级烷基及其盐，制备这些化合物的方法，含有它们的药物组合物，以及作为药物的用途。（一）

46. 发明授权

US5418235A Aminoalkyl-substituted 5-mercaptothiazoles, the preparation and use thereof 失效
标题翻译：氨基烷基取代的5-巯基噻唑的制备和应用
公开(公告)号：US5418235A
公开(公告)日：1995-05-23
申请号：US162145
申请日：1993-12-13
申请人： Beatrice Rendenbach-Mueller , Liliane Unger , Hans-Juergen Teschendorf
发明人： Beatrice Rendenbach-Mueller , Liliane Unger , Hans-Juergen Teschendorf
IPC分类号： A61K31/435 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/495 , A61K31/496 , A61P9/12 , A61P25/16 , A61P25/18 , C07D277/20 , C07D277/40 , C07D277/54 , C07D417/12 , C07D417/14
CPC分类号： C07D417/12 , C07D277/54
摘要： Aminoalkyl-substituted 5-mercaptothiazoles of the formula ##STR1## where R.sup.1, n and A have the meanings stated in the description, and the preparation thereof are described.The compounds are suitable for controlling diseases.
摘要翻译： PCT No.PCT / EP92 / 01004 Sec。 371日期：1993年12月13日 102（e）日期1993年12月13日PCT提交1992年5月8日PCT公布。出版物WO92 / 22540 日期：12月23日，1992.具有式（I）的氨基烷基取代的5-巯基噻唑，其中R1，n和A具有说明书中所述的含义及其制备。该化合物适用于控制疾病。

47. 发明授权

US5256675A Thiazole derivatives, processes for production thereof and pharmaceutical compositions comprising the same 失效
标题翻译：噻唑衍生物，其制备方法和包含其的药物组合物
公开(公告)号：US5256675A
公开(公告)日：1993-10-26
申请号：US867085
申请日：1992-04-14
申请人： Masaaki Matsuo , Takashi Ogino , Norihiro Igari , Hachiro Seno , Kyoichi Shimomura
发明人： Masaaki Matsuo , Takashi Ogino , Norihiro Igari , Hachiro Seno , Kyoichi Shimomura
IPC分类号： C07D277/40 , C07D277/46 , C07D277/54 , C07D277/56 , C07D417/12 , A61K31/44 , A01N43/40 , C07D409/00 , C07D411/00
CPC分类号： C07D417/12 , C07D277/40 , C07D277/46 , C07D277/54 , C07D277/56
摘要： Compounds of the formula: ##STR1## wherein A is S, SO, or SO2, R1 is H or acyl, R2 is H, alkyl, hydroxyalkyl, halogen or carboxy, and R3 is pyridyl are claimed. The compounds are useful as therapeutic agents for the treatment of e.g. rheumatism, nephritis and thrombocytopenia.
摘要翻译：其中A是S，SO或SO 2，R 1是H或酰基，R 2是H，烷基，羟基烷基，卤素或羧基，R 3是吡啶基。这些化合物可用作治疗药物的治疗剂。风湿病，肾炎和血小板减少症。

48. 发明授权

US5153210A Compounds 失效
标题翻译：化合物
公开(公告)号：US5153210A
公开(公告)日：1992-10-06
申请号：US453055
申请日：1989-12-13
申请人： Anthony T. Ainsworth , David G. Smith
发明人： Anthony T. Ainsworth , David G. Smith
IPC分类号： A61K31/35 , A61K31/351 , A61K31/357 , A61K31/40 , A61K31/4015 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4406 , A61K31/4418 , A61K31/4425 , A61K31/443 , A61P3/00 , A61P3/04 , A61P3/08 , A61P25/02 , C07D207/40 , C07D207/416 , C07D211/22 , C07D211/52 , C07D211/70 , C07D211/86 , C07D213/30 , C07D213/69 , C07D231/08 , C07D231/20 , C07D233/22 , C07D233/60 , C07D233/61 , C07D237/14 , C07D257/04 , C07D261/12 , C07D263/24 , C07D263/48 , C07D265/30 , C07D265/32 , C07D277/10 , C07D277/24 , C07D277/34 , C07D277/54 , C07D307/12 , C07D307/30 , C07D307/42 , C07D307/68 , C07D309/38 , C07D309/40 , C07D317/00 , C07D317/26 , C07D317/30 , C07D333/14 , C07D405/10 , C07D407/12 , C07D521/00
CPC分类号： C07D207/416 , C07D211/22 , C07D211/70 , C07D211/86 , C07D213/30 , C07D213/69 , C07D231/08 , C07D233/22 , C07D237/14 , C07D257/04 , C07D261/12 , C07D263/24 , C07D263/48 , C07D265/30 , C07D265/32 , C07D277/10 , C07D277/34 , C07D277/54 , C07D307/12 , C07D307/42 , C07D307/68 , C07D309/40
摘要： A compound of the general formula (I): ##STR1## or a pharmaceutically acceptable ester thereof; or a pharmaceutically acceptable salt thereof, wherein,R.sup.o represents a substituted or unsubstituted aryl group or a substituted or unsubstituted benzofuranyl group,X represents a bond or --O--CH.sub.2 --,R.sup.1 represents a hydrogen atom or a moiety ##STR2## wherein R.sup.o and X are as defined above; R.sup.2 and R.sup.3 independently represent a hydrogen atom or an alkyl group,n represents an integer 1 or 2,Y represents a bond or a moiety --CH.sub.2 --O--, moiety A represents an aryl group,R.sup.4 represents a linking group, andR.sup.5 represents a substituted or unsubstituted, monocyclic or fused ring heterocyclic group, having up to four heteroatoms in each ring selected from, oxygen, nitrogen and sulphur; provided that R.sup.5 is not N-piperazinyl, N-piperadinyl, N-homopiperadinyl, N-pyrrolidinyl or N-morpholinyl; pharmaceutical compositions containing such compounds and their use in medicine and agriculture.
摘要翻译：通式（I）的化合物或其药学上可接受的酯; 或其药学上可接受的盐，其中，R a表示取代或未取代的芳基或取代或未取代的苯并呋喃基，X表示键或-O-CH 2 - ，R 1表示氢原子或部分。 X如上所定义; R2和R3独立地表示氢原子或烷基，n表示1或2的整数，Y表示键或部分-CH2-O-，部分表示芳基，R4表示连接基，R5表示取代或未取代的单环或稠环杂环基，在每个环中具有至多四个选自氧，氮和硫的杂原子; 条件是R 5不是N-哌嗪基，N-哌啶基，N-高哌啶基，N-吡咯烷基或N-吗啉基; 含有这些化合物的药物组合物及其在医药和农业中的应用。

49. 发明授权

US5124342A 4-hydroxythiazoles as 5-lipoxygenase inhibitors 失效
公开(公告)号：US5124342A
公开(公告)日：1992-06-23
申请号：US553836
申请日：1990-07-18
申请人： Francis A. J. Kerdesky , James H. Holms , Dee W. Brooks
发明人： Francis A. J. Kerdesky , James H. Holms , Dee W. Brooks
IPC分类号： C07D277/20 , A61K31/425 , A61K31/426 , A61K31/44 , A61P1/00 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D277/34 , C07D277/54 , C07D277/64 , C07D417/04
CPC分类号： C07D417/04 , C07D277/34 , C07D277/54 , C07D277/64
摘要： A composition for the inhibition of lipoxygenase enzymes comprising a pharmaceutically acceptable carrier and a compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, arylalkenyl, reduced heteroaryl, and reduced heteroarylalkyl and substituted derivatives thereof having one or more substituents independently selected from the group consisting of halogen, alkyl, halosubstituted alkyl, aryl, arylalkyl, reduced heteroaryl, arylalkoxy, cyano, nitro, COR.sub.4, SO.sub.2 R.sub.4, NR.sub.5 R.sub.6, OR.sub.6, COCX.sub.1 X.sub.2 NR.sub.6 R.sub.7, CON(OH)R.sub.6, NR.sub.6 COR.sub.4, CR.sub.5 (NH.sub.2)CO.sub.2 R.sub.5, NHCX.sub.1 X.sub.2 CO.sub.2 R.sub.5, N(OH)CONR.sub.5 R.sub.6, N(OH)COR.sub.4, NHCONR.sub.5 R.sub.6, C(NOH)NHOH and CONHNR.sub.5 R.sub.6 ;R.sub.3 is selected from the group consisting of hydrogen, a pharmaceutically acceptable salt, COR.sub.4, COCX.sub.1 X.sub.2 NR.sub.6 R.sub.7, CR.sub.8 R.sub.9 OR.sub.10, CH.sub.2 CR.sub.8 (OR.sub.10)CH.sub.2 OR.sub.11 and SiR.sub.12 R.sub.13 R.sub.14 ;R.sub.4 is selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced heteroaryl, reduced heteroarylalkyl, OR.sub.5, NHCX.sub.1 X.sub.2 CO.sub.2 R.sub.5 and NR.sub.6 R.sub.7 ;R.sub.5 is selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, reduced heteroaryl, and reduced heteroarylalkyl;R.sub.6 and R.sub.7 are independently selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, reduced heteroaryl, reduced heteroarylalkyl and (CH.sub.2).sub.n OR.sub.5 where n is 2-4 and R.sub.5 is as defined above;R.sub.8, R.sub.9, R.sub.10 and R.sub.11 are independently selected from the group consisting of hydrogen, alkyl, aryl, arylalkyl and (CH.sub.2).sub.n OR.sub.5 or at least two of R.sub.8, R.sub.9, R.sub.10 and R.sub.11 together form a ring system containing 5-10 atoms wherein said ring system is carbocyclic, heterocyclic or reduced heterocyclic and R.sub.5 and n are as defined above;R.sub.12, R.sub.13 and R.sub.14 are independently selected from the group consisting of alkyl and aryl; andX.sub.1 and X.sub.2 are independently selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, aryl, and arylalkyl; and the acid addition salts thereof.

50. 发明授权

US5104889A Thiazole derivatives 失效
标题翻译：噻唑衍生物
公开(公告)号：US5104889A
公开(公告)日：1992-04-14
申请号：US529694
申请日：1990-05-29
申请人： Kenichi Kanai , Kiyoto Goto , Kinji Hashimoto , Yoshiaki Tsuda
发明人： Kenichi Kanai , Kiyoto Goto , Kinji Hashimoto , Yoshiaki Tsuda
IPC分类号： A61K31/425 , A61K31/426 , A61P3/06 , A61P7/02 , A61P9/10 , A61P11/00 , A61P25/04 , A61P29/00 , A61P37/08 , C07D277/20 , C07D277/22 , C07D277/24 , C07D277/30 , C07D277/32 , C07D277/34 , C07D277/36 , C07D277/42 , C07D277/54 , C07D277/56 , C07D277/58 , C10M105/32 , C10M111/04 , C10M169/04
CPC分类号： C07D277/56 , C07D277/24 , C07D277/30 , C07D277/34 , C07D277/36 , C07D277/42 , C07D277/54 , C07D277/58 , C10M105/32 , C10M111/04 , C10M169/04
摘要： This invention provides thiazole derivative of the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A are as defined above, and salts thereof. These compounds have particularly potent angiogenesis inhibiting activity.

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