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81. 发明申请

US20030032808A1 Tri-and bidentate amido ligands prepared by palladium0 coupling and metallation threreof to form metal-amido catalysts 失效
标题翻译：通过钯偶合和金属化反应制备三元和二齿的酰氨基配体，形成金属 - 酰胺催化剂
公开(公告)号：US20030032808A1
公开(公告)日：2003-02-13
申请号：US10116732
申请日：2002-04-02
发明人： Jonas C. Peters , Steven D. Brown , Seth B. Harkins
IPC分类号： C07F009/576 , C07F009/572 , C07D213/54
CPC分类号： C07F15/045 , C07F7/003 , C07F9/5022 , C07F9/60 , C07F15/0066 , C07F15/0086 , C08F10/00 , C08F4/7054
摘要： This invention provides an amido ligand and its synthesis. Use of the amide ligand in a variety of metal complexes, and transition metals in particular, is also provided.
摘要翻译：本发明提供了酰胺配体及其合成。还提供了酰胺配体在各种金属络合物中的用途，特别是过渡金属。

82. 发明授权

US5952369A Pyrrolidinyl hydroxamic acid compounds and their production process 失效
标题翻译：吡咯烷基异羟肟酸化合物及其制备方法
公开(公告)号：US5952369A
公开(公告)日：1999-09-14
申请号：US913823
申请日：1997-09-26
申请人： Fumitaka Ito
发明人： Fumitaka Ito
IPC分类号： C07D295/12 , A61K31/40 , A61K31/4025 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P1/00 , A61P7/00 , A61P7/10 , A61P23/00 , A61P25/00 , A61P25/04 , A61P25/28 , A61P29/00 , A61P43/00 , C07D20060101 , C07D207/12 , C07D213/54 , C07D295/13 , C07D307/79 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , A61K31/41
CPC分类号： C07D213/54 , C07D207/12 , C07D295/13 , C07D307/79 , C07D405/12 , C07D409/12 , Y02P20/55
摘要： A compound of formula (I) ##STR1## and its pharmaceutically acceptable salt, wherein A is hydrogen or OY, wherein Y is a hydroxy protecting group; Ar is phenyl optionally substituted with one or more substituents selected from halo, hydroxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, CF.sub.3, C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyloxy and carboxy-C.sub.1 -C.sub.4 alkyloxy;X is phenyl, naphthyl, biphenyl, indanyl, benzofuranyl, benzothiophenyl, 1-tetralone-6-yl,C.sub.1 -C.sub.4 alkylenedioxy, pyridyl, furyl and thienyl these groups optionally being substituted with up to three substituents selected from halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, NO.sub.2, CF.sub.3 and SO.sub.2 CH.sub.3 ; andR is hydrogen, C.sub.1 -C.sub.4 alkyl or a hydroxy protecting group. These compounds and pharmaceutical compositions containing them are useful as analgesic, anti-inflammatory, diuretic, anesthetic or neuroprotective agents, or an agent for stroke or treatment of functional bowel diseases such as abdominal pain, for the treatment of a mammalian subject, especially a human subject. Further, the present invention provides processes for producing the hydroxamic compounds of formula (I) and their intermediate compounds of the formula. ##STR2##
摘要翻译： PCT No.PCT / JP96 / 00820 Sec。 371日期：1997年9月26日 102（e）1997年9月26日PCT PCT 1996年3月28日PCT公布。 WO96 / 30339 PCT公开号日期：1996年10月3日一种式（I）化合物及其药学上可接受的盐，其中A为氢或OY，其中Y为羟基保护基; Ar是任选被一个或多个选自卤素，羟基，C 1 -C 4烷基，C 1 -C 4烷氧基，CF 3，C 1 -C 4烷氧基-C 1 -C 4烷氧基和羧基-C 1 -C 4烷氧基的取代基取代的苯基; X是苯基，萘基，联苯基，茚满基，苯并呋喃基，苯并噻吩基，1-四氢萘酮-6-基，C 1 -C 4亚烷基二氧基，吡啶基，呋喃基和噻吩基，这些基团任选被至多三个选自卤素，C 1 -C 4烷基， C 1 -C 4烷氧基，羟基，NO 2，CF 3和SO 2 CH 3; 和R是氢，C 1 -C 4烷基或羟基保护基。这些化合物和含有它们的药物组合物可用作止痛剂，抗炎剂，利尿剂，麻醉剂或神经保护剂，或用于中风或治疗功能性肠病如腹痛的药剂，用于治疗哺乳动物受试者，特别是人学科。此外，本发明提供了制备式（I）的异羟肟酸化合物及其下式的中间体化合物的方法。

83. 发明授权

US5849775A Substituted benzoylguanidines process for their preparation, their use as a medicament or diagnostic, and pharmaceutical containing them 失效
标题翻译：取代的苯甲酰胍，其制备方法，它们作为药物或诊断用途，以及含有它们的药物
公开(公告)号：US5849775A
公开(公告)日：1998-12-15
申请号：US886037
申请日：1997-06-30
申请人： Jan-Robert Schwark , Heinz-Werner Kleemann , Hans-Jochen Lang , Andreas Weichert , Wolfgang Scholz , Udo Albus
发明人： Jan-Robert Schwark , Heinz-Werner Kleemann , Hans-Jochen Lang , Andreas Weichert , Wolfgang Scholz , Udo Albus
IPC分类号： A61K31/165 , A61K31/155 , A61K31/166 , A61K31/395 , A61K31/415 , A61K31/4164 , A61K31/4418 , A61P9/00 , A61P9/06 , A61P9/10 , A61P43/00 , C07C277/08 , C07C279/22 , C07C311/15 , C07C317/32 , C07C317/44 , C07C317/48 , C07C323/62 , C07D207/337 , C07D213/30 , C07D213/53 , C07D213/54 , C07D213/58 , C07D213/65 , C07D215/14 , C07D217/16 , C07D231/12 , C07D233/06 , C07D233/61 , C07D233/64 , C07D241/26 , C07D241/28 , C07C231/02 , C07C233/64 , C07D233/54
CPC分类号： C07D213/30 , C07C279/22 , C07C317/44 , C07D213/65 , C07D241/26 , C07C2101/08
摘要： Benzoylguaridines of the formula I ##STR1## are described in which: R(1), R(2), R(3), R(4), R(5) are as defined in the specification, and pharmaceutically tolerated salts thereof.
摘要翻译：其中描述了式I的苯甲酰基胍，其中：R（1），R（2），R（3），R（4），R（5）如本说明书中所定义，及其药学上耐受的盐。

88. 发明授权

US5602135A Phenyl or heteroaryl and tetrahydronaphthyl substituted diene compounds having retinoid like biological activity 失效
标题翻译：具有类视黄醇类似生物活性的苯基或杂芳基和四氢萘基取代的二烯化合物
公开(公告)号：US5602135A
公开(公告)日：1997-02-11
申请号：US458394
申请日：1995-06-02
申请人： Roshantha A. Chandraratna
发明人： Roshantha A. Chandraratna
IPC分类号： C07D237/08 , A61K31/19 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , A61P3/02 , A61P43/00 , C07C13/32 , C07C17/16 , C07C25/02 , C07C33/34 , C07C33/50 , C07C43/215 , C07C45/29 , C07C45/46 , C07C49/792 , C07C62/30 , C07C62/34 , C07C63/66 , C07C63/74 , C07C65/28 , C07C69/76 , C07C233/11 , C07C327/20 , C07D239/26 , C07D241/12 , C07D263/32 , C07D277/20 , C07D277/56 , C07D307/22 , C07D307/68 , C07D333/24 , C07D333/38 , C07F9/54 , C07D213/54
CPC分类号： C07F9/5428 , C07C17/16 , C07C45/29 , C07C45/46 , C07C49/792 , C07C63/66 , C07C69/76 , C07D307/22 , C07D307/68 , C07D333/38
摘要： Compounds of Formula 1 ##STR1## wherein m is 1-4; R.sub.1 -R.sub.4 independently are hydrogen, lower alkyl of 1 to 6 carbons, Cl, Br, or I; R.sub.5 is hydrogen, lower alkyl of 1 to 6 carbons, Cl, Br, I, lower alkoxy or lower thioalkoxy of 1-6 carbons; R.sub.6 is hydrogen, lower alkyl, Cl, Br, I, OR.sub.11, SR.sub.11, OCOR.sub.11, SCOR.sub.11, NH2, NHR.sub.11, N(R.sub.11).sub.2, NHCOR.sub.11 OR NR.sub.11 --COR.sub.11 ; R.sub.20 is independently hydrogen or lower alkyl; Y is an aromatic group such as phenyl or naphthyl, or a heteroaryl group selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl and oxazolyl; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, or CR.sub.7 OR.sub.13 O, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower aklylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.12 is lower alkyl, and R.sub.13 is divalent alkyl radical of 2-5 carbons, have retinoid like biological activity. In the compounds of the invention the A-B and the butadiene groups are attached to adjacent aromatic carbons of the Y moiety.
摘要翻译：式1化合物其中m为1-4; R 1 -R 4独立地是氢，1至6个碳的低级烷基，Cl，Br或I; R5是氢，1-6个碳的低级烷基，C1-6的低级烷氧基或低级烷氧基; R6是氢，低级烷基，Cl，Br，I，OR11，SR11，OCOR11，SCOR11，NH2，NHR11，N（R11）2，NHCOR11或NR11-COR11; R 20独立地是氢或低级烷基; Y是芳基，例如苯基或萘基，或选自吡啶基，噻吩基，呋喃基，哒嗪基，嘧啶基，吡嗪基，噻唑基和恶唑基的杂芳基。 A是（CH 2）n，其中n是0-5，具有3-6个碳的低级支链烷基，具有3-6个碳的环烷基，具有2-6个碳的烯基和1或2个双键，具有2-6个碳原子的炔基和 1或2个三键; B是氢，COOH或其药学上可接受的盐，COOR8，CONR9R10，-CH2OH，CH2OR11，CH2OCOR11，CHO，CH（OR12）2，CHOR13O，-COR7，CR7（OR12）2或CR7OR13O，其中R7是烷基，碳原子数为1〜5的环烷基或烯基，R8为碳原子数为1〜10的烷基或碳原子数为5〜10的环烷基，或R8为苯基或低级烷基苯基，R9和R10分别为氢，烷基 1〜10个碳原子的环烷基或5-10个碳原子的环烷基，或苯基或低级烷基苯基，R11为低级烷基，苯基或低级烷基苯基，R12为低级烷基，R13为2-5个碳原子的二价烷基，具有类视黄醇类似生物活性。在本发明的化合物中，A-B和丁二烯基团连接到Y部分的相邻芳族碳上。

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