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1. 发明授权

US06649767B2 Process for preparing 1,4-dihydropyridine compounds 失效
标题翻译：制备1,4-二氢吡啶化合物的方法
公开(公告)号：US06649767B2
公开(公告)日：2003-11-18
申请号：US10224928
申请日：2002-08-20
申请人： Kunio Satake , Noriaki Murase
发明人： Kunio Satake , Noriaki Murase
IPC分类号： C07D21302
CPC分类号： C07D417/06
摘要： A process for preparing a 1,4-dihydropyridine compound comprising contacting an enamine compound and a compound having a structure of in the presence of a base; and treating the reaction mixture thus obtained in the presence of an acid or a combination of acids under mild reaction conditions. A resulting 1,4-dihydropyridine compound is useful as an anti-inflammatory agent or the like.
摘要翻译：一种制备1,4-二氢吡啶化合物的方法，包括使烯胺化合物和具有在碱存在下的结构的化合物接触; 并在温和的反应条件下，在酸或酸的组合存在下处理由此得到的反应混合物。得到的1,4-二氢吡啶化合物可用作抗炎剂等。

2. 发明授权

US06506775B1 Substituted benzylaminopiperidine compounds 失效
标题翻译：取代的苄基氨基哌啶化合物
公开(公告)号：US06506775B1
公开(公告)日：2003-01-14
申请号：US09564398
申请日：2000-05-01
申请人： Kunio Satake , Yuji Shishido , Hiroaki Wakabayashi
发明人： Kunio Satake , Yuji Shishido , Hiroaki Wakabayashi
IPC分类号： C07D21156
CPC分类号： C07D211/56
摘要： The invention provides a compound of formula (I): and its pharmaceutically acceptable salts, wherein R is halo C2-C8 alkenyl or halo C2-C8 alkynyl; R1 is hydrogen, halo or C1-C6 alkoxy; or R and R1, together with the two carbon atoms to which they are attached, form a C4-C6 cycloalkyl or a C4-C6 oxacycloalkyl ring wherein said ring may be optionally substituted by one or more substituents selected from the group consisting of halo, C1-C6 alkyl and halo C1-C6 alkyl; X is C1-C6 alkoxy, halo C1-C6 alkoxy, phenoxy or halo; and Ar is phenyl optionally substituted by halo. These compounds are useful in the treatment of a gastrointestinal disorder; a central nervous system (CNS) disorder; an inflammatory disease; emesis; urinary incontinence; pain; migraine; sunburn; diseases, disorders and adverse conditions caused by Heliobacter pylori; or angiogenesis especially CNS disorders in a mammalian subject, especially humans.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的盐，其中R为卤代C 2 -C 8烯基或卤代C 2 -C 8炔基; R 1为氢，卤素或C 1 -C 6烷氧基;或R和R 1与它们连接的两个碳原子形成C 4 -C 6环烷基或C 4 -C 6氧杂环烷基环，其中所述环可任选地被一个或多个选自卤素，C 1 -C 6烷基和卤代C 1 -C 6烷基的取代基取代， C6烷基; X是C1-C6烷氧基，卤代C1-C6烷氧基，苯氧基或卤代; 并且Ar是任选被卤素取代的苯基。这些化合物可用于治疗胃肠道疾病; 中枢神经系统（CNS）障碍; 炎性疾病; 呕吐尿失禁疼痛; 偏头痛晒斑; 由幽门螺杆菌引起的疾病，病症和不良状况; 或血管发生，尤其是哺乳动物受试者尤其是人类的CNS疾病。

3. 发明授权

US5086062A Antiallergy and antiinflammatory benzoxazolinones 失效
标题翻译：抗真菌和抗炎药苯并噻唑啉酮
公开(公告)号：US5086062A
公开(公告)日：1992-02-04
申请号：US529971
申请日：1990-05-29
申请人： Kazuo Ando , Nobuko Asai , Fumitaka Ito , Takashi Mano , Masami Nakane , Kunio Satake , Kaoru Shimada
发明人： Kazuo Ando , Nobuko Asai , Fumitaka Ito , Takashi Mano , Masami Nakane , Kunio Satake , Kaoru Shimada
IPC分类号： C12N9/99 , A61K31/42 , A61K31/423 , A61K31/424 , A61K31/435 , A61K31/445 , A61P29/00 , A61P37/08 , A61P43/00 , C07D263/58 , C07D407/02 , C07D409/12 , C07D413/12 , C07D493/08
CPC分类号： C07D263/58 , C07D413/12 , C07D493/08 , Y02P20/55
摘要： This invention relates to certain benzoxazolinones which inhibit lipoxygenase and/or cyclooxygenase enzymes. Such compounds are useful in inhibiting such enzymes, per se, and are useful in treating allergic and inflammatory conditions in a mammal. This invention also relates to methods of inhibiting lipoxygenase and/or cyclooxygenase in a mammal with such benzoxazolinones; methods of treating an allergic condition in a mammal with such compounds; methods of treating an inflammatory condition in a mammal with such compounds; and pharmaceutical compositions comprising the benzoxazolinones hereof.

4. 发明授权

US06194442B1 5-substituted picolinic acid compounds and their method of use 失效
标题翻译： 5-取代吡啶甲酸化合物及其使用方法
公开(公告)号：US06194442B1
公开(公告)日：2001-02-27
申请号：US09460483
申请日：1999-12-14
申请人： Hideo Hirai , Katsuomi Ichikawa , Nakao Kojima , Hiroyuki Nishida , Kunio Satake , Nobuji Yoshikawa
发明人： Hideo Hirai , Katsuomi Ichikawa , Nakao Kojima , Hiroyuki Nishida , Kunio Satake , Nobuji Yoshikawa
IPC分类号： A61K3144
CPC分类号： A61K31/44 , Y02A50/411
摘要： The present invention provides novel 5-substituted picolinic acid compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are independently H, C2-C6 acyl or halo-substituted benzoyl; and R3 is —C(O)O—C1-C6 alkyl, C(O)OH, CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, with the proviso that when R2 is acetyl and R3 is methoxycarbonyl, R1 is not H; and that when R3 is CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, R1 and R2 are H. The present invention also relates to a pharmaceutical composition comprising compound of the present invention, which is useful in the treatment of IL-1 and TNF mediated diseases or the like. The present invention further relates to a process for producing the compounds of the formula (I).
摘要翻译：本发明提供式（I）的新的5-取代的吡啶甲酸化合物或其药学上可接受的盐：其中R 1和R 2独立地为H，C 2 -C 6酰基或卤素取代的苯甲酰基; 并且R 3是-C（O）O-C 1 -C 6烷基，C（O）OH，CN，CONH 2，CONHCH 3，CON（CH 3）2,1-甲基四唑或2-甲基四唑，条件是当R 2是乙酰基和 R3是甲氧基羰基，R1不是H; 当R3为CN，CONH2，CONHCH3，CON（CH3）2,1-甲基四唑或2-甲基四唑时，R 1和R 2为H.本发明还涉及含有本发明化合物的药物组合物，其有用在治疗IL-1和TNF介导的疾病等中。本发明还涉及制备式（I）化合物的方法。

5. 发明授权

US5504095A Aminobenzosultam derivatives as lipoxygenase inhibitors 失效
标题翻译：氨基苯并磺酰胺衍生物作为脂氧合酶抑制剂
公开(公告)号：US5504095A
公开(公告)日：1996-04-02
申请号：US359709
申请日：1994-12-20
申请人： Masami Nakane , Kunio Satake , Kazuo Ando , Hiroaki Wakabayashi
发明人： Masami Nakane , Kunio Satake , Kazuo Ando , Hiroaki Wakabayashi
IPC分类号： C07D275/06 , C07D279/02 , C07D285/00 , C07D285/14 , C07D285/15 , C07D285/16 , C07D291/08 , C07D417/12 , C07D419/12 , A61K31/41
CPC分类号： C07D275/06 , C07D279/02 , C07D285/14 , C07D285/15 , C07D285/16 , C07D291/08 , C07D417/12 , C07D419/12
摘要： Aminobenzosultam derivatives, which are inhibitors of lipoxygenase, having the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein Ar is cycloalkyl having five to seven carbon atoms, tetrahydropyranyl, pyridyl, oxazolyl, phenyl or substituted phenyl wherein said substituent is methyl, methoxy, fluoro, chloro or trifluoromethyl; n is an integer of 1 to 3; X is hydrogen, methyl, methoxy, fluoro, chloro or trifluoromethyl; Z is --NH--, --O--, or --CH.sub.2 --; and R.sup.1 is hydrogen or alkyl having one to three carbon atoms.
摘要翻译：作为脂氧合酶抑制剂的氨基苯并磺酰胺衍生物，其具有式及其药学上可接受的酸加成盐，其中Ar是具有5-7个碳原子的环烷基，四氢吡喃基，吡啶基，恶唑基，苯基或取代的苯基，其中所述取代基是甲基，甲氧基，氟，氯或三氟甲基; n为1〜3的整数。 X是氢，甲基，甲氧基，氟，氯或三氟甲基; Z是-NH-，-O-或-CH 2 - ; 并且R 1是氢或具有1-3个碳原子的烷基。

6. 发明授权

US4360582A Photopolymerizable element comprising a soluble or dispersible oriented film support 失效
标题翻译：包含可溶或可分散的取向膜载体的可光聚合元件
公开(公告)号：US4360582A
公开(公告)日：1982-11-23
申请号：US295960
申请日：1981-08-25
申请人： Tadashi Taguchi , Noboru Fujikawa , Mitsuo Kohno , Katsumi Yoshitake , Kunio Satake
发明人： Tadashi Taguchi , Noboru Fujikawa , Mitsuo Kohno , Katsumi Yoshitake , Kunio Satake
IPC分类号： G03F7/09 , G03F7/095 , G03F7/26 , H05K3/00 , H05K3/06 , G03C1/90 , G03C1/78 , G03C1/96 , G03C5/00
CPC分类号： H05K3/064 , G03F7/092 , G03F7/0955 , G03F7/26 , H05K2201/0108 , H05K2203/0783 , H05K2203/1394 , H05K3/0082 , H05K3/0094 , Y10S430/136 , Y10S430/14 , Y10S430/162
摘要： A photopolymerizable element comprising a layer of a photopolymerizable composition and a liquid developer-soluble or -dispersible transparent oriented film support laminated onto one surface of the photopolymerizable composition layer is advantageously employed for the production of a polymeric image without stripping of the film support. The element may further comprise a strippable protective film provided on the other surface of the photopolymerizable composition layer. The element of this invention is useful especially for the production of photoresists which are advantageously used for the manufacture of printed circuit boards.
摘要翻译：包含可光聚合组合物层和层压在可光聚合组合物层的一个表面上的液体显影剂可溶或可分散透明取向膜载体的可光聚合元件有利地用于生产聚合物图像而不剥离膜载体。元件还可以包括设置在可光聚合组合物层的另一表面上的可剥离保护膜。本发明的元件特别用于制造有利地用于制造印刷电路板的光致抗蚀剂。

7. 发明申请

US20050171354A1 Piperidinylaminomethyl trifluoromethyl cyclic ether compounds as substance P antagonists 审中-公开
标题翻译：哌啶基氨基甲基三氟甲基环醚化合物作为物质P拮抗剂
公开(公告)号：US20050171354A1
公开(公告)日：2005-08-04
申请号：US10991977
申请日：2004-11-18
申请人： Kunio Satake
发明人： Kunio Satake
IPC分类号： A61K20060101 , A61K31/443 , A61K31/445 , A61K31/4453 , A61K31/452 , A61K31/4523 , A61K31/4525 , A61K31/453 , A61P1/00 , A61P1/04 , A61P1/08 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/00 , A61P13/02 , A61P15/00 , A61P15/10 , A61P17/00 , A61P17/02 , A61P19/02 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/04 , A61P37/00 , A61P37/08 , A61P43/00 , C07D20060101 , C07D211/06 , C07D211/56 , C07D295/00 , C07D307/78 , C07D307/87 , C07D311/76 , C07D405/12 , C07D45/02
CPC分类号： C07D307/87 , C07D311/76 , C07D405/12
摘要： This invention provides a compound of the formula: and its pharmaceutically acceptable salts, wherein R1 is C1-C6 alkyl; R2 is hydrogen, C1-C6 alkyl, halo C1-C6 alkyl or phenyl; R3 is hydrogen or halo; R4 and R5 are independently hydrogen, C1-C6 alkyl or halo C1-C6 alkyl; and n is one, two or three. These compounds are useful as analgesics or anti-inflammatory agents, or in the treatment of cardiovascular diseases, allergic disorders, angiogenesis, CNS disorders, emesis, gastrointestinal disorders, sunburn, urinary incontinence, or diseases, disorders or adverse conditions caused by Helicobacter pylori, or the like, in a mammalian subject, especially humans. Intermediates for preparation of the compounds of Formula (I) are also disclosed.
摘要翻译：本发明提供下式的化合物及其药学上可接受的盐，其中R 1是C 1 -C 6烷基; R 2是氢，C 1 -C 6烷基，卤代C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，烷基或苯基; R 3是氢或卤素; R 4和R 5独立地是氢，C 1 -C 6烷基或卤素C 1 C 6 -C 6烷基; 而n是一，二或三。这些化合物可用作止痛剂或抗炎剂，或用于治疗心血管疾病，过敏性疾病，血管生成，CNS障碍，呕吐，胃肠道疾病，晒伤，尿失禁或由幽门螺杆菌引起的疾病，病症或不利条件，或哺乳动物受试者，特别是人类。还公开了制备式（I）化合物的中间体。

8. 发明授权

US5939434A Tetrazolyl-substituted quinuclidines as substance P antagonists 失效
标题翻译：作为物质P拮抗剂的四唑基取代的奎宁子
公开(公告)号：US5939434A
公开(公告)日：1999-08-17
申请号：US924171
申请日：1997-09-05
申请人： Kunio Satake
发明人： Kunio Satake
IPC分类号： A61K31/435 , A61K31/439 , A61P1/00 , A61P1/04 , A61P1/08 , A61P9/00 , A61P13/00 , A61P13/02 , A61P15/00 , A61P17/02 , A61P25/00 , A61P25/04 , A61P25/06 , A61P29/00 , A61P31/04 , A61P37/08 , A61P43/00 , C07D453/02 , A61K31/44
CPC分类号： C07D453/02
摘要： This invention provides a compound of the formula: ##STR1## and its pharmaceutically acceptable salts, wherein R.sup.1 is halo, C.sub.1 -C.sub.6 alkyl, halo C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or halo C.sub.1 -C.sub.6 alkoxy; R.sup.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, halo C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyl-S-, C.sub.1 -C.sub.6 alkyl-SO--, C.sub.1 -C.sub.6 alkyl-SO.sub.2 --, cyclopropyl, phenyl, --NH.sub.2, --NH(CH.sub.3), --NHC(.dbd.O)CH.sub.3, --N(CH.sub.3).sub.2, --N(C.sub.2 H.sub.5).sub.2 or --CH.sub.2 C(.dbd.O)CF.sub.3 ; Ar.sup.1 and Ar.sup.2 are independently phenyl, halophenyl or thienyl; X is NH, O or S; and Y is hydrogen, --COOR.sup.3 or --CONR.sup.4 R.sup.5, wherein R.sup.3, R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 -C.sub.6 alkyl. These compounds are useful as analgesics or anti-inflammatory agents, or in the treatment of allergic disorders, angiogenesis, CNS disorders, emesis, gastrointestinal disorders, sunburn, urinary incontinence, or diseases, disorders or adverse conditions caused by Helicobacter pylori, or the like, in a mammalian subject, especially human, especially as analgesics or anti-inflammatory agents in the periphery.
摘要翻译：本发明提供下式化合物及其药学上可接受的盐，其中R 1为卤素，C 1 -C 6烷基，卤代C 1 -C 6烷基，C 1 -C 6烷氧基或卤代C 1 -C 6烷氧基; R2是氢，C1-C6烷基，卤代C1-C6烷基，C1-C6烷基-S-，C1-C6烷基-SO-，C1-C6烷基-SO2-，环丙基，苯基，-NH2，-NH（CH3 ），-NHC（= O）CH 3，-N（CH 3）2，-N（C 2 H 5）2或-CH 2 C（= O）CF 3; Ar1和Ar2独立地是苯基，卤代苯基或噻吩基; X是NH，O或S; 并且Y是氢，-COOR 3或-CONR 4 R 5，其中R 3，R 4和R 5独立地是氢或C 1 -C 6烷基。这些化合物可用作止痛剂或抗炎剂，或用于治疗过敏性疾病，血管生成，CNS紊乱，呕吐，胃肠道疾病，晒伤，尿失禁或由幽门螺杆菌引起的疾病，病症或不利条件等，在哺乳动物受试者，特别是人类，特别是在周边的止痛剂或抗炎剂。

9. 发明授权

US5721255A Substituted benzylamino nitrogen containing non-aromatic heterocycles 失效
标题翻译：取代的含有非芳族杂环的苄基氨基氮
公开(公告)号：US5721255A
公开(公告)日：1998-02-24
申请号：US387765
申请日：1995-02-15
申请人： Harry R. Howard , Masami Nakane , Masaya Ikunaka , Kunio Satake , Terry J. Rosen , John A. Lowe, III , Brian T. O'Neill , Fumitaka Ito
发明人： Harry R. Howard , Masami Nakane , Masaya Ikunaka , Kunio Satake , Terry J. Rosen , John A. Lowe, III , Brian T. O'Neill , Fumitaka Ito
IPC分类号： C07D333/36 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/41 , A61K31/425 , A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/451 , A61P9/08 , A61P11/16 , A61P25/02 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P29/00 , A61P37/00 , A61P37/08 , C07D207/14 , C07D209/52 , C07D211/56 , C07D401/12 , C07D417/12 , C07D453/02 , C07D487/08 , A61K31/47
CPC分类号： C07D401/12 , C07D211/56 , C07D417/12 , C07D453/02 , C07D487/08
摘要： The present invention relates to novel substituted benzylamino nitrogen containing non-aromatic heterocycles and, specifically, to compounds of the formula ##STR1## wherein W, R.sup.1, R.sup.2, R.sup.3 and A are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.
摘要翻译： PCT No.PCT / US93 / 04063。 371日期1995年2月15日 102（e）日期1995年2月15日PCT提交1993年5月5日PCT公布。公开号WO94 / 04496 1994年3月3日本发明涉及新的取代的苄基氨基氮的非芳族杂环，具体地说，涉及下式化合物其中W，R1，R2，R3和A如说明书中所定义，用于合成这些化合物的中间体。式I的新型化合物可用于治疗炎性和中枢神经系统疾病以及其它疾病。

10. 发明授权

US4211560A Process for producing image using laminated oriented cover film 失效
标题翻译：使用层压取向覆盖膜制作图像的方法
公开(公告)号：US4211560A
公开(公告)日：1980-07-08
申请号：US923763
申请日：1978-07-11
申请人： Tadashi Taguchi , Noboru Fujikawa , Mitsuo Kohno , Katsumi Yoshitake , Kunio Satake
发明人： Tadashi Taguchi , Noboru Fujikawa , Mitsuo Kohno , Katsumi Yoshitake , Kunio Satake
IPC分类号： G03F7/09 , G03F7/095 , G03F7/26 , H05K3/00 , H05K3/06 , G03C5/00 , G03C1/76
CPC分类号： H05K3/064 , G03F7/092 , G03F7/0955 , G03F7/26 , H05K2201/0108 , H05K2203/0783 , H05K2203/1394 , H05K3/0082 , H05K3/0094 , Y10S430/136 , Y10S430/14 , Y10S430/162
摘要： A process for producing an image which comprises the steps of:(1) applying to the surface of a substrate the surface of a photosensitive layer, the other surface of the photosensitive layer being adhered to a substantially transparent film support which is soluble or dispersible in a developer consisting essentially of a liquid capable of substantially dissolving or dispersing therein the areas of the layer other than those having a polymeric image produced by imagewise exposure in the step (2) below;(2) exposing the photosensitive layer, imagewise, to actinic radiation to form a polymeric image in the layer; and(3) washing away with the developer the film support and the areas of the layer other than those having the polymeric image to form an image of a polymeric material on the substrate. The photosensitive element having on its one side the above-mentioned specific film support and the process have a variety of applications and are useful for producing photoresists which are advantageously used for making printed circuit boards.
摘要翻译：一种用于制造图像的方法，包括以下步骤：（1）将感光层的表面施加到基底的表面，感光层的另一表面粘附到可溶或可分散于基本上由在下面的步骤（2）中能够基本上溶解或分散其中除了具有通过成像曝光产生的聚合物图像的层之外的层的区域的液体的显影剂; （2）将感光层成像曝光于光化辐射以在层中形成聚合物图像; 和（3）用显影剂除去膜载体和不同于具有聚合物图像的那些层的区域，以在基底上形成聚合物材料的图像。感光元件的一侧具有上述特定的膜支撑体，并且该方法具有各种应用，并且可用于制造有利地用于制造印刷电路板的光致抗蚀剂。

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