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71. 发明授权

US5599924A Electron-deficient porphyrins and processes and intermediates for preparing same 失效
标题翻译：电子缺陷卟啉及其制备方法和中间体
公开(公告)号：US5599924A
公开(公告)日：1997-02-04
申请号：US234651
申请日：1994-04-28
申请人： Michael J. Therien , Stephen DiMagno
发明人： Michael J. Therien , Stephen DiMagno
IPC分类号： A61K31/409 , A61K31/555 , A61K41/00 , A61K47/48 , A61K49/00 , A61K51/04 , A61L2/08 , A61L2/18 , A61P31/04 , B01J27/10 , B01J27/12 , B01J31/02 , B01J31/18 , B01J31/22 , B01J31/24 , C07C29/50 , C07D207/32 , C07D207/33 , C07D207/333 , C07D207/335 , C07D487/22 , C07D513/22 , C07D519/00 , C07F3/00 , C07F7/08 , C07F7/10 , C07H23/00 , C08F8/42 , C08F30/04 , C08F38/00 , C08G61/12 , C08G73/06 , C08G79/00 , C08G83/00 , C09B47/00 , C09B47/08 , C09B69/10 , G01N27/12 , G01N27/40 , G03G5/06 , G03G5/07
CPC分类号： A61K47/48069 , A61K31/555 , A61K41/0071 , A61K47/48023 , A61K51/0485 , B01J31/0244 , B01J31/1805 , B01J31/1815 , B01J31/2409 , C07C29/50 , C07D207/33 , C07D207/333 , C07D207/335 , C07D487/22 , C07F7/082 , C07F7/0832 , C08F30/04 , C08G73/0611 , C08G79/00 , C09B47/00 , C09B69/10 , C09B69/108 , G01N27/126 , G03G5/0696 , G03G5/076 , B01J2231/42 , B01J2231/70 , B01J2231/72 , B01J2531/025 , B01J2531/26 , B01J2531/824 , B01J2531/922 , B01J2531/96
摘要： Electron-deficient porphyrins are provided, as well as processes and intermediates for their preparation. In preferred embodiments, the electron-deficient porphyrins are prepared by condensing pyrrole derivatives and removing water thus formed from the resulting reaction mixture.
摘要翻译：提供了电子缺陷卟啉，以及其制备方法和中间体。在优选的实施方案中，电子缺陷卟啉通过将吡咯衍生物缩合并从所得反应混合物除去由此形成的水来制备。

72. 发明授权

US5371199B1 Substituted porphyrins porphyrin-containing polymers and synthetic methods therefor 失效
标题翻译：取代卟啉卟啉聚合物及其合成方法
公开(公告)号：US5371199B1
公开(公告)日：1995-12-26
申请号：US92994392
申请日：1992-08-14
申请人： UNIV PENNSYLVANIA
发明人： THERIEN MICHAEL J , DIMAGNO STEPHEN G
IPC分类号： A61K31/409 , A61K31/555 , A61K41/00 , A61K47/48 , A61K49/00 , A61K51/04 , A61L2/08 , A61L2/18 , A61P31/04 , B01J31/02 , B01J31/18 , B01J31/22 , B01J31/24 , C07C29/50 , C07D207/32 , C07D207/33 , C07D207/333 , C07D487/22 , C07D513/22 , C07D519/00 , C07F3/00 , C07F7/08 , C07F7/10 , C07H23/00 , C08F8/42 , C08F30/04 , C08F38/00 , C08G61/12 , C08G73/06 , C08G79/00 , C08G83/00 , C09B47/00 , C09B47/08 , C09B69/10 , G01N27/12 , G01N27/40 , G03G5/06 , G03G5/07 , C01F17/00 , C01G55/00
CPC分类号： A61K41/0071 , A61K31/555 , A61K47/54 , A61K47/546 , A61K51/0485 , B01J31/0244 , B01J31/1805 , B01J31/1815 , B01J31/2409 , B01J2231/42 , B01J2531/025 , B01J2531/22 , B01J2531/26 , B01J2531/824 , C07C29/50 , C07D207/33 , C07D207/333 , C07D487/22 , C07D519/00 , C07F7/082 , C07F7/0832 , C08F30/04 , C08G73/0611 , C08G79/00 , C09B47/00 , C09B69/10 , C09B69/108 , G01N27/126 , G03G5/0696 , G03G5/076
摘要： Porphyrins substituted with, for example, vinyl and acetylene groups are provided, along with polymers containing the same. In preferred embodiments, the substituted porphyrins are prepared by coupling halogenated porphyrins with anionic groups via metal-mediated cross-coupling reactions under stoichiometric or catalytic conditions.

73. 发明授权

US5371199A Substituted porphyrins, porphyrin-containing polymers, and synthetic methods therefor 失效
标题翻译：取代的卟啉，含卟啉的聚合物及其合成方法
公开(公告)号：US5371199A
公开(公告)日：1994-12-06
申请号：US929943
申请日：1992-08-14
申请人： Michael J. Therien , Stephen G. DiMagno
发明人： Michael J. Therien , Stephen G. DiMagno
IPC分类号： A61K31/409 , A61K31/555 , A61K41/00 , A61K47/48 , A61K49/00 , A61K51/04 , A61L2/08 , A61L2/18 , A61P31/04 , B01J31/02 , B01J31/18 , B01J31/22 , B01J31/24 , C07C29/50 , C07D207/32 , C07D207/33 , C07D207/333 , C07D487/22 , C07D513/22 , C07D519/00 , C07F3/00 , C07F7/08 , C07F7/10 , C07H23/00 , C08F8/42 , C08F30/04 , C08F38/00 , C08G61/12 , C08G73/06 , C08G79/00 , C08G83/00 , C09B47/00 , C09B47/08 , C09B69/10 , G01N27/12 , G01N27/40 , G03G5/06 , G03G5/07 , C01F17/00 , C01G55/00
CPC分类号： A61K47/48069 , A61K31/555 , A61K41/0071 , A61K47/48023 , A61K51/0485 , B01J31/0244 , B01J31/1805 , B01J31/1815 , B01J31/2409 , C07C29/50 , C07D207/33 , C07D207/333 , C07D487/22 , C07D519/00 , C07F7/082 , C07F7/0832 , C08F30/04 , C08G73/0611 , C08G79/00 , C09B47/00 , C09B69/10 , C09B69/108 , G01N27/126 , G03G5/0696 , G03G5/076 , B01J2231/42 , B01J2531/025 , B01J2531/22 , B01J2531/26 , B01J2531/824
摘要： Porphyrins substituted with, for example, vinyl and acetylene groups are provided, along with polymers containing the same. In preferred embodiments, the substituted porphyrins are prepared by coupling halogenated porphyrins with carbon-centered anionic groups via metal-mediated crosscoupling reactions under stoichiometric or catalytic conditions.
摘要翻译：提供了用例如乙烯基和乙炔基取代的卟啉以及含有它们的聚合物。在优选的实施方案中，通过在化学计量或催化条件下通过金属介导的交叉耦合反应将卤代卟啉与碳中心的阴离子基团偶联来制备取代的卟啉。

74. 发明授权

US5260309A 4,5,6,11-tetrahydrobenzo [6,7] cycloocta [1,2-b]thiophen-6,11-imines and 6,11-dihydrobenzo [6,7] cycloocta [1,2-b] thiophen-6,11-imines 失效
标题翻译： 4,5,6,11-四氢苯并[6,7]环辛[1,2-b]噻吩-6,11-亚胺和6,11-二氢苯并[6,7]环辛[1,2-b] 6,11-亚胺
公开(公告)号：US5260309A
公开(公告)日：1993-11-09
申请号：US828892
申请日：1992-01-29
申请人： Ralph P. Robinson
发明人： Ralph P. Robinson
IPC分类号： C07D495/18 , C07D513/22 , A61K31/38
CPC分类号： C07D495/18
摘要： The present invention relates to compounds of the formula ##STR1## wherein the broken line represents a saturated or an olefinic bond, R.sup.1 and R.sup.4 are each hydrogen or C.sub.1 to C.sub.6 alkyl, and R.sup.2 and R.sup.3 are each hydrogen, C.sub.1 to C.sub.6 alkyl, halogen, C.sub.1 to C.sub.6 alkoxy or C.sub.1 to C.sub.6 alkylthio, and pharmaceutically acceptable salts thereof, pharmaceutical compounds containing the same, methods of preparing the foregoing compounds, and to novel intermediates in the preparation of the foregoing compounds. These compounds are useful as agents in the prevention of neuronal damage in the brain following cerebral ischemia and during the progression of Alzheimer's disease and also as anticonvulsants.
摘要翻译： PCT No.PCT / US89 / 02387第 371日期1992年1月29日 102（e）日期1992年1月29日PCT提交1989年6月1日PCT公布。 WO90 / 15060 PCT出版物 1990年12月13日。本发明涉及下式化合物：其中虚线代表饱和或烯键，R 1和R 4各自为氢或C 1至C 6烷基，R 2和R 3各自为氢 C 1〜C 6烷基，卤素，C 1〜C 6烷氧基或C 1〜C 6烷硫基，及其药学上可接受的盐，含有该化合物的药物组合物，制备上述化合物的方法，以及制备上述化合物的新中间体。这些化合物可用作预防脑缺血后和阿尔茨海默氏病进程期间脑内神经元损伤以及作为抗惊厥药的药剂。

75. 发明授权

US5114934A Tricyclic pyridone derivatives 失效
标题翻译：三聚吡啶衍生物
公开(公告)号：US5114934A
公开(公告)日：1992-05-19
申请号：US359616
申请日：1989-06-01
申请人： Ulf Fischer , Fernand Schneider , Ulrich Widmer
发明人： Ulf Fischer , Fernand Schneider , Ulrich Widmer
IPC分类号： C07D237/00 , A61K20060101 , A61K31/38 , A61K31/395 , A61K31/44 , A61K31/495 , A61K31/50 , A61K31/535 , A61P21/02 , A61P25/08 , A61P25/20 , C07D20060101 , C07D221/00 , C07D223/02 , C07D237/26 , C07D257/00 , C07D333/00 , C07D471/00 , C07D471/04 , C07D495/00 , C07D495/04 , C07D495/06 , C07D495/08 , C07D495/14 , C07D513/00 , C07D513/02 , C07D513/04 , C07D513/06 , C07D513/08 , C07D513/12 , C07D513/14 , C07D513/16 , C07D513/18 , C07D513/20 , C07D513/22 , C07D519/00
CPC分类号： C07D471/04 , C07D495/14 , C07D513/04 , C07D513/14
摘要： The compounds of the formula ##STR1## wherein R.sub.a, R.sub.b, R.sub.c, R.sub.d are defined in the specification and pharmaceutically acceptable addition salts are disclosed. The compounds of formula I have valuable pharmacological properties and can be used for the control of prevention of illnesses. In particular, they have muscle relaxant, seditive-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, isomnia, anxiety states and/or convulsions.

76. 发明授权

US4824947A Substituted phthalocyanine 失效
公开(公告)号：US4824947A
公开(公告)日：1989-04-25
申请号：US162514
申请日：1988-03-01
申请人： William M. Stark
发明人： William M. Stark
IPC分类号： B41M5/26 , C07D513/22 , C09B47/04 , C09B47/06 , C09B47/20 , C09B47/22 , C09D11/02 , G11B7/248 , C07D487/22 , C09B , C09B47/30
CPC分类号： C09D11/037 , C09B47/045 , C09B47/063 , C09B47/064 , C09B47/20 , C09B47/22 , G11B7/248
摘要： A phthalocyanine compound of the formula: ##STR1## wherein Pc is a phthalocyanine nucleus;each R independently is optionally substituted phenyl;m is 4 to 12;V is H or C.sub.1-4 -alkyl;each R.sup.1 independently is optionally substituted phenylene or naphthylene in which the S atom and group N-V are attached to adjacent nuclear carbon atoms;and n is 2 to 6;provided that R is not R.sup.1 -NHV.The compounds have a significant absorption band in the near infra red and are soluble in non-polar organic media. The compounds are useful in many applications where absorption of infra-red radiation is desirable, such as in OCR readable inks, security printing and reprographic toners.

77. 发明授权

US4769456A Sulfenamide derivatives and their production 失效
标题翻译：亚磺酰胺衍生物及其生产
公开(公告)号：US4769456A
公开(公告)日：1988-09-06
申请号：US14352
申请日：1987-02-13
申请人： Akira Nohara , Yoshitaka Maki
发明人： Akira Nohara , Yoshitaka Maki
IPC分类号： C07D513/16 , A61K31/33 , A61K31/54 , A61P1/04 , C07D513/14 , C07D513/22
CPC分类号： C07D513/14
摘要： The compound of the formula ##STR1## wherein R.sup.1 is hydrogen, methoxy or trifluormethyl, R.sup.2 and R.sup.3 are the same or different and are each hydrogen or methyl, R.sup.4 is a fluorinated lower alkyl having 2 to 5 carbon atoms and 1 to 11 fluorine atoms and X.sup.- is a pharmaceutically acceptable anion, respectively, possesses both strong antisecretory activity and gastric mucosal protective activity, which is produced by reacting a pyridine derivative of the formula ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the same meaning as defined above, with an acid.
摘要翻译：其中R 1为氢，甲氧基或三氟甲基，R 2和R 3相同或不同，各自为氢或甲基，R 4为含有2至5个碳原子的氟化低级烷基和1至11个氟原子的式分别具有药学上可接受的阴离子，其具有强的抗分泌活性和胃粘膜保护活性，其通过使式（ⅩⅧ）的吡啶衍生物与其中R1，R2，R3和R4具有与定义相同的含义以上，用酸。

78. 发明授权

US4725691A 2-[8-quinolinyl]-sulphinyl-1H-benzimidazole 失效
标题翻译： 2- [8-喹啉基] - 亚磺酰基-1H-苯并咪唑
公开(公告)号：US4725691A
公开(公告)日：1988-02-16
申请号：US913689
申请日：1986-09-30
申请人： Arne E. Brandstrom , Per L. Lindberg , Bjorn Wallmark
发明人： Arne E. Brandstrom , Per L. Lindberg , Bjorn Wallmark
IPC分类号： A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/54 , A61P1/00 , A61P1/04 , A61P43/00 , C07D401/12 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/052 , C07D495/04 , C07D513/14 , C07D513/16 , C07D513/22
CPC分类号： C07D401/12 , C07D513/14
摘要： Novel compounds of the formula IIIa ##STR1## wherein R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a are the same or different and are hydrogen, an alkyl, alkoxy optionally completely or predominantly substituted by fluorine or chlorine, halogen, --CN, --CF.sub.3, --NO.sub.2, --COR, --COOR, aryl, aryloxy or arylalkoxy group, or adjacent groups R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a together with the adjacent carbon atoms in the benzimidazole ring form a 5-, 6- or 7-membered monocyclic ring or a 9-, 10- or 11-membered bicyclic ring, which rings may be saturated or unsaturated and may contain 0-3 heteroatoms selected from N and O and which rings may be optionally substituted with 1-4 substitutents selected from alkyl groups with 1-3 carbon atoms, halogen preferably F or Cl, alkylene radicals containing 4-5 carbon atoms giving spiro compounds, or two or four of these substituents together form one or two oxy groups ##STR2## whereby if R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a together with the adjacent carbon atoms in the benzimidazole ring form two rings they may be condensed with each other, R.sup.5a is hydrogen or an alkyl group, R.sup.6a is hydrogen or an alkyl group or R.sup.5a and R.sup.6a are joined together to form an alkylene chain, R.sup.7a is hydrogen, an alkyl, alkoxy, alkenyloxy or alkynyloxy group, R.sup.8a is hydrogen or an alkyl group, or R.sup.6a and R.sup.7a, or R.sup.7a and R.sup.8a together with the adjacent carbon atoms in the pyridinium ring form a ring wherein the part constituted by R.sup.6a and R.sup.7a or R.sup.7a and R.sup.8a, is --CH.dbd.CH--CH.dbd.CH--, --O--(CH.sub.2).sub.p --, --CH.sub.2 (CH.sub.2).sub.p --, --O--CH.dbd.CH--, --NH--CH.dbd.CH--, ##STR3## or --S--(CH.sub.2).sub.p --, wherein p is 2, 3 or 4 and the O, S and N atoms always are attached to position 3 in the compound IIIa, R is a alkyl, cycloalkyl, aryl or arylalkyl group, and X.sup.- is a pharmaceutically acceptable anion, process for preparation thereof, pharmaceutical compositions containing such compounds and their use in medicine.

79. 发明授权

US4710504A Anti-depressant spiro hexahydro arylquinolizine derivatives, composition, and method of use therefor 失效
标题翻译：抗抑郁螺旋六氢芳基喹啉衍生物，组合物及其用途
公开(公告)号：US4710504A
公开(公告)日：1987-12-01
申请号：US848262
申请日：1986-04-04
申请人： John J. Baldwin , Joel R. Huff , Joseph P. Vacca , Steven D. Young , Jane deSolms , James P. Guare, Jr.
发明人： John J. Baldwin , Joel R. Huff , Joseph P. Vacca , Steven D. Young , Jane deSolms , James P. Guare, Jr.
IPC分类号： C07D471/20 , C07D491/22 , C07D495/22 , C07D498/22 , C07D513/22 , A61K31/415 , A61K31/305 , C07D455/00
CPC分类号： C07D471/20 , C07D491/22 , C07D495/22 , C07D498/22 , C07D513/22
摘要： Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, platelet aggregation inhibitors, antiobesity agents, and modifiers of gastrointestinal motility.
摘要翻译：取代的六氢芳基喹啉及其药学上可接受的盐是选择性α2-肾上腺素能受体拮抗剂，因此可用作抗抑郁药，抗高血压药，眼用抗高血压药，抗糖尿病药，血小板聚集抑制剂，抗肥胖剂和消化道运动性改良剂。

80. 发明授权

US4636499A Sulphenamides 失效
标题翻译：苯甲酰胺
公开(公告)号：US4636499A
公开(公告)日：1987-01-13
申请号：US739425
申请日：1985-05-30
申请人： Arne E. Brandstrom , Per L. Lindberg , Bjorn Wallmark
发明人： Arne E. Brandstrom , Per L. Lindberg , Bjorn Wallmark
IPC分类号： A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/54 , A61P1/00 , A61P1/04 , A61P43/00 , C07D401/12 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/052 , C07D495/04 , C07D513/14 , C07D513/16 , C07D513/22 , C07D513/04 , C07D513/12
CPC分类号： C07D401/12 , C07D513/14
摘要： Novel compounds of the formula IIIa ##STR1## wherein R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a are the same or different and are hydrogen, an alkyl, alkoxy optionally completely or predominantly substituted by fluorine or chlorine, halogen, --CN, --CF.sub.3, --NO.sub.2, --COR, --COOR, aryl, aryloxy or arylalkoxy group, or adjacent groups R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a together with the adjacent carbon atoms in the benzimidazole ring form a 5-, 6- or 7-membered monocyclic ring or a 9-, 10- or 11-membered bicyclic ring, which rings may be saturated or unsaturated and may contain 0-3 heteroatoms selected from N and O and which rings may be optionally substituted with 1-4 substitutents selected from alkyl groups with 1-3 carbon atoms, halogen perferably F or Cl, alkylene radicals containing 4-5 carbon atoms giving spiro compounds, or two or four of these substituents together form one or two oxy groups ##STR2## whereby if R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a together with the adjacent carbon atoms in the benzimidazole ring form two rings they may be condensed with each other, R.sup.5a is hydrogen or an alkyl group, R.sup.6a is hydrogen or an alkyl group or R.sup.5a and R.sup.6a are joined together to form an alkylene chain, R.sup.7a is hydrogen, an alkyl, alkoxy, alkenyloxy, or alkynyloxy group, R.sup.8a is hydrogen or an alkyl group, or R.sup.6a and R.sup.7a, or R.sup.7a and R.sup.8a together with the adjacent carbon atoms in the pyridinium ring form a ring wherein the part constituted by R.sup.6a and R.sup.7a or R.sup.7a and R.sup.8a, is --CH.dbd.CH--CH.dbd.CH--, --O--(CH.sub.2).sub.p --, --CH.sub.2 (CH.sub.2).sub.p --, --O--CH.dbd.CH--, --NH--CH.dbd.CH--, ##STR3## or --S--(CH.sub.2).sub.p --, wherein p is 2, 3 or 4 and the O, S and N atoms always are attached to position 3 in the compound IIIa, R is an alkyl, cycloalkyl, aryl or arylalkyl group, and X.sup.- is a pharmaceutically acceptable anion, process for preparation thereof, pharmaceutical compositions containing such compounds and their use in medicine.
摘要翻译：新的式IIIa化合物其中R 1a，R 2a，R 3a和R 4a相同或不同，为氢，烷基，任选完全或主要被氟或氯取代的烷氧基，卤素，-CN，-CF 3 - NO 2，-COR，-COOR，芳基，芳氧基或芳烷氧基或相邻基团R 1a，R 2a，R 3a和R 4a与苯并咪唑环中的相邻碳原子一起形成5-，6-或7-元单环或 9,10,10或11元双环，该环可以是饱和或不饱和的，并且可以含有0-3个选自N和O的杂原子，哪些环可以任选被1-4个选自烷基的取代基取代， 3个碳原子，卤素优选为F或Cl，含有4-5个碳原子的烯基，得到螺环化合物，或两个或四个这些取代基一起形成一个或两个氧基“IMAGE”，如果R1a，R2a，R3a和R4a连同苯并咪唑环中相邻的碳原子形成它们的两个环相互稠合，R5a为氢或烷基，R6a为氢或烷基或R5a和R6a连接在一起形成亚烷基链，R7a为氢，烷基，烷氧基，烯氧基或炔氧基， R8a是氢或烷基，或R6a和R7a或R7a和R8a与吡啶鎓环中的相邻碳原子一起形成环，其中由R6a和R7a或R7a和R8a构成的部分是-CH = CH-CH = CH-，-O-（CH 2）p - ， - CH 2（CH 2）p - ， - O-CH = CH-，-NH-CH = CH-，其中p是2,3或4，并且O，S和N原子总是连接到化合物IIIa中的3位，R是烷基，环烷基，芳基或芳基烷基，X是药学上可接受的阴离子，含有这些化合物的药物组合物及其在药物中的用途。

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