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21. 发明授权

US6118010A Process for the preparation of 1-alkoxycarbonyl-3-phenylpropyl derivatives 有权
标题翻译： 1-烷氧基羰基-3-苯基丙基衍生物的制备方法
公开(公告)号：US6118010A
公开(公告)日：2000-09-12
申请号：US147255
申请日：1998-11-10
申请人： Yasuyoshi Ueda , Akira Matsumoto , Hajime Manabe
发明人： Yasuyoshi Ueda , Akira Matsumoto , Hajime Manabe
IPC分类号： C07D233/36 , B01J23/44 , C07B61/00 , C07C227/16 , C07C227/42 , C07C229/36 , C07C237/12 , C07D209/42 , C07D209/52 , C07D215/48 , C07D217/26 , C07D223/16 , C07D285/12 , C07D453/02 , C07D495/10 , C07K1/113 , C07K5/02 , C07K5/062 , C07K5/078 , C07D207/08 , C07C229/28
CPC分类号： C07C227/42 , C07C227/16 , C07K5/022 , C07K5/0222 , C07K5/06139 , Y02P20/55
摘要： To produce an 1-alkoxycarbonyl-3-phenylpropyl derivative having little amount of impurities and good quality by a simple, efficient and highly productive process which comprises catalytically reducing an 1-alkoxycarbonyl-3-oxo-3-phenylpropyl derivative. 1-Alkoxycarbonyl-3-phenyl-propyl derivative is provided and obtained by catalytic redution being carried out in an alcohol or a solvent containing the alcohol in the presence of a strong acid having a concentration of 0.4 to 0.5 N, the amount of the strong acid being at least 3 equivalents based on one equivalent of the 1-alkoxycarbonyl-3-oxo-3-phenylpropyl derivative (1 mole).
摘要翻译： PCT No.PCT / JP97 / 01543 Sec。 371日期：1998年11月10日 102（e）1998年11月10日日期PCT提交1997年5月8日PCT公布。出版物WO97 / 43246 日期1997年11月20日为了通过简单，有效和高生产率的方法制备具有少量杂质和良好质量的1-烷氧基羰基-3-苯基丙基衍生物，其包括催化还原1-烷氧基羰基-3-氧代-3-苯基丙基衍生物。提供1-烷氧基羰基-3-苯基 - 丙基衍生物，通过在浓度为0.4〜0.5N的强酸存在下，在醇或含有醇的溶剂中进行催化重洗，获得强力基于1当量的1-烷氧基羰基-3-氧代-3-苯基丙基衍生物（1摩尔），酸为至少3当量。

22. 发明授权

US6069275A Monomers and polymers and latices therefrom 失效
标题翻译：单体及其聚合物和胶乳
公开(公告)号：US6069275A
公开(公告)日：2000-05-30
申请号：US14552
申请日：1998-01-28
申请人： Norman Shachat , Zenyk Kosarych
发明人： Norman Shachat , Zenyk Kosarych
IPC分类号： C07D233/32 , C07D233/36 , C07D239/10 , C08F20/36 , C08F20/60 , C09D133/06 , C09D133/14 , C09D133/24 , C07C269/00 , C07C273/00 , C08F226/06
CPC分类号： C09D133/062 , C07D233/32 , C07D233/36 , C08F20/36
摘要： A novel monomer composition for promoting wet adhesion of latex polymers for paints is provided. The composition consists essentially of a monomer having the formula: ##STR1## The preferred monomer is derived from the reaction of hydroxyethyl methacrylate with isophorone diisocyanate followed by reaction of the monourethane product the N-aminoethyl ethylene urea. The monomer is preferably copolymerized in an emulsion polymerization with acrylic and/or vinyl monomers.
摘要翻译：提供了用于促进胶乳聚合物用于油漆的湿粘合性的新型单体组合物。该组合物基本上由具有下式的单体组成：优选的单体衍生自甲基丙烯酸羟乙酯与异佛尔酮二异氰酸酯的反应，然后使单氨基甲酸酯产物N-氨基乙基亚乙基脲反应。单体优选在乳液聚合中与丙烯酸和/或乙烯基单体共聚。

23. 发明授权

US5994376A 1,3-dihydro-1-(phenylalkyl)-2H-imidazol-2-one compounds and their use for treating allergic, atopic or inflammatory diseases 失效
标题翻译： 1,3-二氢-1-（苯基烷基）-2H-咪唑-2-酮化合物及其用于治疗过敏性，特应性或炎性疾病的用途
公开(公告)号：US5994376A
公开(公告)日：1999-11-30
申请号：US930296
申请日：1997-09-29
申请人： Eddy Jean Edgard Freyne , Gaston Stanislas Marcella Diels , Jose Ignacio Andres-Gil , Francisco Javier Fernandez-Gadea
发明人： Eddy Jean Edgard Freyne , Gaston Stanislas Marcella Diels , Jose Ignacio Andres-Gil , Francisco Javier Fernandez-Gadea
IPC分类号： C07D233/32 , A61K31/415 , A61K31/4166 , A61K31/44 , A61K31/4427 , A61K31/443 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/08 , C07D233/36 , C07D233/38 , C07D233/70 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12
CPC分类号： C07D401/06 , C07D233/36 , C07D233/38 , C07D233/70
摘要： The present invention describes 1,3-dihydro-1-(phenylalkyl)-2H-imidazol-2-one compounds and their use for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases.
摘要翻译： PCT No.PCT / EP96 / 01394 Sec。 371日期：1997年9月29日 102（e）1997年9月29日PCT PCT 1996年3月28日PCT公布。出版物WO96 / 31485 日期：1996年10月10日本发明描述了1,3-二氢-1-（苯基烷基）-2H-咪唑-2-酮化合物及其用于治疗与异常酶促或催化活性有关的疾病状态的温血动物磷酸二酯酶IV（PDE IV）和/或与细胞因子的生理有害过量相关的疾病状态，特别是过敏性，特应性和炎性疾病。

24. 发明授权

US5972964A Aminomethylindans, -benzofurans and -benzothiophenes 失效
标题翻译：氨基甲基丹宁， - 苯并呋喃和苯并噻吩
公开(公告)号：US5972964A
公开(公告)日：1999-10-26
申请号：US955376
申请日：1997-10-22
申请人： Jens Perregaard
发明人： Jens Perregaard
IPC分类号： C07D295/12 , A61K31/136 , A61K31/34 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4166 , A61K31/445 , A61K31/495 , A61P9/00 , A61P9/10 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/30 , C07C211/58 , C07C211/60 , C07C233/15 , C07C233/43 , C07C233/80 , C07C255/58 , C07C275/26 , C07C275/28 , C07C275/40 , C07C311/05 , C07C311/08 , C07C311/21 , C07C327/22 , C07C327/26 , C07D209/14 , C07D233/32 , C07D233/36 , C07D307/81 , C07D333/58 , C07D405/06 , C07D405/12 , C07D409/12
CPC分类号： C07D233/32 , C07C211/60 , C07C233/43 , C07C233/80 , C07C275/40 , C07C311/08 , C07D209/14 , C07D307/81 , C07D333/58 , C07C2101/08 , C07C2101/14 , C07C2102/08
摘要： Compounds of formula I ##STR1## wherein R1.dbd.(cyclo)alk(en)yl, aralkyl, alkyl(oxy)carbonyl, CONH2, etc.; R2.dbd.H, (cyclo)alk(en)yl, aralkyl, etc.; R3-R5.dbd.H, halo, alkyl, alkoxy, etc.; R6,R7.dbd.H, alkyl; R6R7.dbd.atoms to complete a ring; R8,R9.dbd.groups cited for R2, 2-oxoimidazolidinoalkyl, etc.; NR8R9=heterocyclyl; 1 of X,Y=CH2 and the other.dbd.CH2, O, S were prepd. Thus, 1-indancarboxylic acid was converted in 5 steps to 1-(N,N-dipropylaminomethyl)-6-formylaminoindane oxalate which had ED50 of 0.0055.mu.M/kg s.c. in the 8--OH DPAT cue agonism test in rats.
摘要翻译：式Ⅰ化合物，其中R1 =（环）烷（烯）基，芳烷基，烷基（氧基）羰基，CONH2等; R2 = H，（环）烷（en）基，芳烷基等; R3-R5 = H，卤素，烷基，烷氧基等; R6，R7 = H，烷基; R6R7 =原子完成环; R8，R9 = R2，2-氧代咪唑烷基烷基等引用的基团; NR8R9 =杂环基; 1的X，Y = CH 2，另一个= CH 2，O，S。因此，将1-二氢化茚羧酸按5分钟转化为ED50为0.0055.mu.M / kg·s的1-（N，N-二丙基氨基甲基）-6-甲酰氨基茚满草酸盐。在大鼠的8-OH DPAT提示激动试验中。

25. 发明授权

US5731311A N,N-di(aryl) cyclic urea derivatives as anti-coagulants 失效
公开(公告)号：US5731311A
公开(公告)日：1998-03-24
申请号：US764374
申请日：1996-12-12
申请人： Raju Mohan , Michael M. Morrissey
发明人： Raju Mohan , Michael M. Morrissey
IPC分类号： A61K31/415 , A61K31/4166 , A61K31/4184 , A61K31/496 , A61K31/505 , A61K31/55 , A61P7/02 , C07D233/36 , C07D233/70 , C07D233/90 , C07D235/26 , C07D239/10 , C07D243/04 , A61K31/535 , A61K31/495 , C07D403/10 , C07D413/10
CPC分类号： C07D239/10 , C07D233/70 , C07D233/90 , C07D235/26 , C07D243/04
摘要： N,N-di(aryl) cyclic urea derivatives, such as the compounds of the following formula: ##STR1## wherein R.sup.1 is --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.11, --C(NH)N(H)C(O)R.sup.9, or --C(NH)N(H)C(O)OR.sup.11 ; R.sup.2 and R.sup.3 are independently hydrogen, halo, lower alkyl, lower haloalkyl, aryl, --OR.sup.11, --C(O)OR.sup.11, --C(O)N(R.sup.11)R.sup.12, --N(R.sup.11)R.sup.12, --N(H)C(O)R.sup.11, or --N(H)S(O).sub.2 R.sup.11 ; R.sup.4 is halo, lower haloalkyl, imidazolyl, --C(NH)NH.sub.2, --C(NH)NHOR.sup.11, --C(NH)N(H)C(O)R.sup.9, --C(NH)N(H)C(O)OR.sup.11, --OR.sup.11, --C(O)R.sup.13, --(CH.sub.2).sub.n C(O)OR.sup.11 (where n is 0 to 6), --C(O)N(R.sup.11)R.sup.12, or --N(R.sup.11)R.sup.12 ; R.sup.7 and R.sup.8 are independently hydrogen, lower alkyl, lower haloalkyl, 4-pyridinyl, --C(O)OR.sup.11, --C(O)N(R.sup.11)R.sup.12, or aryl (optionally substituted by one or more substituents selected from the group consisting of halo, hydroxy, lower alkyl, lower haloalkyl, lower alkoxy and --N(R.sup.11)R.sup.12); R.sup.11 and R.sup.12 are independently hydrogen, lower alkyl, aryl or lower aralkyl; or R.sup.13 is pyrrolidinyl, 4-morpholinyl, piperazinyl, N-methylpiperazinyl, or piperidinyl; or a pharmaceutically acceptable salt thereof, are disclosed herein as being inhibitors of factor Xa and thereby being useful as anticoagulants.

26. 发明授权

US5728697A N,N-di(aryl) cyclic urea derivatives as anti-coagulants 失效
标题翻译： N，N-二（芳基）环脲衍生物作为抗凝剂
公开(公告)号：US5728697A
公开(公告)日：1998-03-17
申请号：US766373
申请日：1996-12-12
申请人： Raju Mohan , Michael M. Morrissey
发明人： Raju Mohan , Michael M. Morrissey
IPC分类号： A61K31/415 , A61K31/4166 , A61K31/4184 , A61K31/496 , A61K31/505 , A61K31/55 , A61P7/02 , C07D233/36 , C07D233/70 , C07D233/90 , C07D235/26 , C07D239/10 , C07D243/04 , A61K31/535 , C07D403/10 , C07D413/10
CPC分类号： C07D239/10 , C07D233/70 , C07D233/90 , C07D235/26 , C07D243/04
摘要： N,N-di(aryl) cyclic urea derivatives, such as the compounds of the following formula: ##STR1## wherein R.sup.1 is --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.11, --C(NH)N(H)C(O)R.sup.9, or --C(NH)N(H)C(O)OR.sup.11 ; R.sup.2 and R.sup.3 are independently hydrogen, halo, lower alkyl, lower haloalkyl, aryl, --OR.sup.11, --C(O)OR.sup.11, --C(O)N(R.sup.11)R.sup.12, --N(R.sup.11)R.sup.12, --N(H)C(O)R.sup.11, or --N(H)S(O).sub.2 R.sup.11 ; R.sup.4 is halo, lower haloalkyl, imidazolyl, --C(NH)NH.sub.2, --C(NH)NHOR.sup.11, --(CH.sub.2).sub.n C(O)OR.sup.11 (where n is 0 to 6), --C(O)N(R.sup.11)R.sup.12, or --N(R.sup.11)R.sup.12 ; R.sup.7 and R.sup.8 are independently hydrogen, lower alkyl, lower haloalkyl, 4-pyridinyl, --C(O)OR.sup.11, --C(O)N(R.sup.11)R.sup.12, or aryl (optionally substituted by one or more substituents selected from the group consisting of halo, hydroxy, lower alkyl, lower haloalkyl, lower alkoxy and --N(R.sup.11)R.sup.12); R.sup.11 and R.sup.12 are independently hydrogen, lower alkyl, aryl or lower aralkyl; or R.sup.13 is pyrrolidinyl, 4-morpholinyl, piperazinyl, N-methylpiperazinyl, or piperidinyl; or a pharmaceutically acceptable salt thereof, are disclosed herein as being inhibitors of factor Xa and thereby being useful as anticoagulants.
摘要翻译： N，N-二（芳基）环脲衍生物，例如下式的化合物：其中R 1是-C（NH）NH 2，-C（NH）N（H）OR 11，-C （NH）N（H）C（O）R 9或-C（NH）N（H）C（O）OR 11; R2和R3独立地是氢，卤素，低级烷基，低级卤代烷基，芳基，-OR11，-C（O）OR11，-C（O）N（R11）R12，-N（R11）R12，-N（H） C（O）R 11或-N（H）S（O）2 R 11; R4是卤素，低级卤代烷基，咪唑基，-C（NH）NH2，-C（NH）NHOR11， - （CH2）nC（O）OR11（其中n为0至6），-C（O）N（R11） R12或-N（R11）R12; R 7和R 8独立地是氢，低级烷基，低级卤代烷基，4-吡啶基，-C（O）OR 11，-C（O）N（R 11）R 12或芳基（任选被一个或多个选自卤素，羟基，低级烷基，低级卤代烷基，低级烷氧基和-N（R 11）R 12）; R 11和R 12独立地是氢，低级烷基，芳基或低级芳烷基; 或R 13为吡咯烷基，4-吗啉基，哌嗪基，N-甲基哌嗪基或哌啶基; 或其药学上可接受的盐在本文中公开为因子Xa的抑制剂，从而可用作抗凝血剂。

27. 发明授权

US5276049A Cyclic urea derivatives, pharmaceutical compositions containing these compounds and methods of using the same 失效
标题翻译：环状脲衍生物，含有这些化合物的药物组合物及其使用方法
公开(公告)号：US5276049A
公开(公告)日：1994-01-04
申请号：US849557
申请日：1992-03-11
申请人： Frank Himmelsbach , Helmut Pieper , Volkhard Austel , Guenter Linz , Thomas Mueller , Johannes Weisenberger , Wolfgang Eisert
发明人： Frank Himmelsbach , Helmut Pieper , Volkhard Austel , Guenter Linz , Thomas Mueller , Johannes Weisenberger , Wolfgang Eisert
IPC分类号： A61K31/41 , A61K31/415 , A61K31/4166 , A61K31/4184 , A61K31/433 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5355 , A61K31/54 , A61K31/541 , A61K31/675 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P29/00 , A61P35/00 , C07D211/58 , C07D233/30 , C07D233/32 , C07D233/36 , C07D233/70 , C07D233/72 , C07D233/74 , C07D233/76 , C07D235/26 , C07D239/10 , C07D239/36 , C07D249/12 , C07D285/10 , C07D309/12 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D471/04 , C07F9/6506
CPC分类号： C07D285/10 , C07D211/58 , C07D233/32 , C07D233/70 , C07D233/72 , C07D235/26 , C07D239/10 , C07D239/36 , C07D249/12 , C07D309/12 , C07D401/04 , C07D403/04 , C07D471/04 , C07F9/65061
摘要： The invention relates to cyclic urea derivatives of general formula ##STR1## wherein R.sub.a, R.sub.b, X and Y are as defined herein, pharmaceutical compositions containing the derivatives and processes for preparing them.
摘要翻译：本发明涉及通式为（I）的环脲衍生物，其中Ra，Rb，X和Y如本文所定义，含有衍生物的药物组合物及其制备方法。

28. 发明授权

US5157124A Heterocyclic acetylenic amines having central nervous system activity 失效
标题翻译：具有中枢神经系统活性的杂环炔胺
公开(公告)号：US5157124A
公开(公告)日：1992-10-20
申请号：US853671
申请日：1992-03-19
申请人： Malcolm W. Moon , Richard F. Heier
发明人： Malcolm W. Moon , Richard F. Heier
IPC分类号： C07D207/09 , C07D233/36 , C07D233/70 , C07D521/00
CPC分类号： C07D249/08 , C07D207/09 , C07D231/12 , C07D233/36 , C07D233/56 , C07D233/70
摘要： Heterocyclic acetylenic amine compounds having the following structural formula ##STR1## having cholinergic agonist or antagonist activity useful in the treatment of mental disorders, extrapyramidal motor disorders, disorders of theparasympathetic nervous system and glaucoma or as analgesics for the treatment of pain. Typical central nervous system disorders for which the subject compounds can be used include cognitive disorders of all ages, including senile dementia, Alzheimer's disease and other related disorders. The compounds are particularly developed to improve mental performance when a mental deficiency is diagnosed.
摘要翻译：具有以下结构式的具有可用于治疗精神障碍的胆碱能激动剂或拮抗剂活性，锥体外系运动障碍，副交感神经系统疾病和青光眼的结构式的杂环炔胺化合物或作为治疗疼痛的镇痛药。可以使用主题化合物的典型的中枢神经系统疾病包括所有年龄的认知障碍，包括老年痴呆，阿尔茨海默病和其他相关疾病。当诊断出精神缺陷时，这些化合物特别开发用于改善心理表现。

29. 发明授权

US4988688A 4-(N-substituted amino)-2-butynyl-1-ureas and thioureas and derivatives thereof as centrally acting muscarinic agents 失效
标题翻译： 4-（N-取代氨基）-2-丁炔基-1-脲和硫脲及其衍生物作为中枢作用毒蕈碱药
公开(公告)号：US4988688A
公开(公告)日：1991-01-29
申请号：US388785
申请日：1989-08-02
申请人： Jeffrey A. Kester , Walter H. Moos , Anthony J. Thomas
发明人： Jeffrey A. Kester , Walter H. Moos , Anthony J. Thomas
IPC分类号： A61K31/17 , A61K31/40 , A61K31/445 , A61K31/535 , A61K31/5375 , A61P25/02 , A61P25/28 , B01J27/055 , B01J27/122 , C07B61/00 , C07C273/18 , C07C275/20 , C07C275/22 , C07C335/10 , C07C335/14 , C07D227/04 , C07D229/00 , C07D233/36 , C07D239/10 , C07D295/12 , C07D295/125 , C07D295/13 , C07D295/20
CPC分类号： C07D295/13 , C07C275/20
摘要： 4-(N-Substituted amino)-2-butynyl-1-ureas and thioureas and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetylcholine production or release.

30. 发明授权

US4735942A [[4 -[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-dioxolan-2-yl]-methyl]-1H- imidazoles and 1H-1,2,4-triazoles having antimicrobial properties 失效
标题翻译：具有抗微生物性的[[4- [4-（4-苯基-1-哌嗪基）苯氧基甲基] -1,3-二氧戊环-2-基] - 甲基] -1H-咪唑和1H-1,2,4-三唑
公开(公告)号：US4735942A
公开(公告)日：1988-04-05
申请号：US869537
申请日：1986-06-02
申请人： Jan Heeres , Raymond A. Stokbroekx , Leo J. J. Backx
发明人： Jan Heeres , Raymond A. Stokbroekx , Leo J. J. Backx
IPC分类号： C07D233/32 , C07D233/36 , C07D233/72 , C07D277/42 , C07D279/06 , C07D295/096 , C07D295/135 , C07D487/04 , C07D521/00 , A61K31/495 , C07D405/14 , C07D413/14 , C07D417/14
CPC分类号： C07D295/096 , C07D231/12 , C07D233/32 , C07D233/36 , C07D233/56 , C07D233/72 , C07D249/08 , C07D277/42 , C07D279/06 , C07D295/135 , C07D487/04
摘要： Substituted [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3 dioxolan-2-yl]methyl]-1H-imidazoles and 1H-1,2,4-triazoles having antimicrobial properties and being particularly useful in the treatment of vaginal candidosis.
摘要翻译：取代的[[4- [4-（4-苯基-1-哌嗪基）苯氧基甲基] -1,3-二氧戊环-2-基]甲基] -1H-咪唑和具有抗微生物性质的1H-1,2,4-三唑特别适用于治疗阴道念珠菌病。

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