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1. 发明申请

US20080312435A1 Imine Compound 审中-公开
标题翻译：亚胺化合物
公开(公告)号：US20080312435A1
公开(公告)日：2008-12-18
申请号：US11667728
申请日：2005-10-31
申请人： Shiuji Saito , Hiroshi Ohta , Tomoko Ishizaki , Mitsukane Yoshinaga , Makoto Tatsuzuki , Yuji Yokobori , Yasumitsu Tomishima , Aki Morita , Yoshihisa Toda , Kimiko Tokugawa , Ayaka Kaku , Tomomi Murakami , Hiromitsu Yoshimura , Shingo Sekine , Takao Yoshimizu
发明人： Shiuji Saito , Hiroshi Ohta , Tomoko Ishizaki , Mitsukane Yoshinaga , Makoto Tatsuzuki , Yuji Yokobori , Yasumitsu Tomishima , Aki Morita , Yoshihisa Toda , Kimiko Tokugawa , Ayaka Kaku , Tomomi Murakami , Hiromitsu Yoshimura , Shingo Sekine , Takao Yoshimizu
IPC分类号： C07D417/12 , C07D213/75 , C07D277/46 , C07D231/40 , C07D263/48
CPC分类号： C07D417/12 , C07D213/75 , C07D231/40 , C07D401/12 , C07D409/12 , C07D413/12
摘要： An imine compound represented by the formula: wherein A represents a heterocyclic group; R1, R2, an R3 each represent a hydrogen atom, a halogen atom, a C1-10 alkyl group optionally substituted with an aryl group(s) substituted with a halogen atom(s), a C3-10 cycloalkyl group, a C1-6 haloalkyl group, a C1-10 alkoxy group, etc.; R4 represents an optionally substituted C1-10 alkyl, C2-6 alkenyl, or aryl group; R5 represents a hydrogen atom, a C1-10 alkoxy group, a C1-6 haloalkyl group, an optionally substituted C1-10 alkyl or C2-6 alkenyl group, an optionally substituted aryl or heterocyclic group, etc.; W represents —CO—, —CO—CO—, —CO—NH—, —CS—NH—, or —SO2—, or a cannabinoid-receptor agonist comprising said imine compound as an active ingredient. The imine compound of the present invention has a cannabinoid-receptor agonist effect, and is useful as a therapeutic or prophylactic drug for pains and autoimmune diseases.
摘要翻译：由下式表示的亚胺化合物：其中A表示杂环基; R 1，R 2，R 3各自表示氢原子，卤素原子，任选被被卤素原子取代的芳基取代的C 1-10烷基，C 3-10环烷基， 6卤代烷基，C1-10烷氧基等; R 4表示任选取代的C 1-10烷基，C 2-6烯基或芳基; R5表示氢原子，C1-10烷氧基，C1-6卤代烷基，任选取代的C 1-10烷基或C 2-6烯基，任选取代的芳基或杂环基等; W表示-CO-，-CO-CO-，-CO-NH-，-CS-NH-或-SO 2 - 或包含所述亚胺化合物作为活性成分的大麻素受体激动剂。本发明的亚胺化合物具有大麻素受体激动剂作用，可用作疼痛和自身免疫疾病的治疗或预防药物。

2. 发明授权

US4600540A Benzoylpropionic acid derivatives 失效
标题翻译：苯甲酰丙酸衍生物
公开(公告)号：US4600540A
公开(公告)日：1986-07-15
申请号：US741127
申请日：1985-06-04
申请人： Kazuyuki Tomisawa , Kazuya Kameo , Toru Matsunaga , Shiuji Saito , Kaoru Sota
发明人： Kazuyuki Tomisawa , Kazuya Kameo , Toru Matsunaga , Shiuji Saito , Kaoru Sota
IPC分类号： A61K31/265 , A61K31/10 , A61K31/185 , A61P37/00 , C07C20060101 , C07C67/00 , C07C313/00 , C07C325/00 , C07C327/04 , C07C327/20 , C07C327/22 , C07C327/32 , C07C153/023
CPC分类号： C07C327/00
摘要： Benzoylpropionic acid derivatives represented by the general formula ##STR1## (wherein R.sup.1 represents a hydrogen atom, a lower alkyl group or a benzyl group, R.sup.2 represents a lower alkyl group or a phenyl group, X represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a phenoxy group or a halogenophenoxy group, and Y represents a hydrogen atom or a lower alkyl group). The compounds have immunomodulative function and are effective for treatment of diseases caused by abnormal immunofunction.
摘要翻译：由通式（I）表示的苯甲酰基丙酸衍生物（其中R1表示氢原子，低级烷基或苄基，R2表示低级烷基或苯基，X表示氢原子，卤素原子，低级烷基，低级烷氧基，苯氧基或卤代苯氧基，Y表示氢原子或低级烷基）。该化合物具有免疫调节功能，对于治疗由异常免疫功能引起的疾病有效。

3. 发明授权

US5374764A 5-aminosulfonanilide compounds 失效
标题翻译： 5-氨基磺酰苯胺化合物
公开(公告)号：US5374764A
公开(公告)日：1994-12-20
申请号：US190123
申请日：1994-02-03
申请人： Kensei Yoshikawa , Shiuji Saito , Yohichi Shimazaki , Mariko Kashiwa , Katsuo Hatayama
发明人： Kensei Yoshikawa , Shiuji Saito , Yohichi Shimazaki , Mariko Kashiwa , Katsuo Hatayama
IPC分类号： C07C311/08 , C07C311/02
CPC分类号： C07C311/08 , C07C2101/14
摘要： 5-Aminosulfonanilide compounds represented by the formula: ##STR1## (wherein R is a hydrogen atom, a formyl group, an acetyl group, a propionyl group, an n-butyryl group, an n-valeryl group, an ethoxyoxalyl group, an n-propoxyoxalyl group, a methoxycarbonylacetyl group or a 3-ethoxycarbonylpropionyl group) have potent anti-inflammatory, antipyretic, analgesic and anti-allergic actions, and therefore they are useful as anti-inflammatory, antipyretic, analgesic and anti-allergic agents.
摘要翻译： PCT No.PCT / JP92 / 01013 Sec。 371日期：1994年2月3日 102（e）日期1994年2月3日PCT提交1992年8月7日PCT公布。公开号WO93 / 03008 日期：1993年2月18日5-氨基磺酰苯胺化合物由下式表示：其中R为氢原子，甲酰基，乙酰基，丙酰基，正丁酰基，正戊酰基，乙氧基草酰基，正丙氧基草酰基，甲氧基羰基乙酰基或3-乙氧基羰基丙酰基）具有有效的抗炎，解热，镇痛和抗过敏作用，因此它们可用作抗炎，解热，止痛和抗 - 过敏剂。

4. 发明授权

US4594197A 3-benzoyl-2-mercaptopropionic acid derivatives 失效
标题翻译： 3-苯甲酰基-2-巯基丙酸衍生物
公开(公告)号：US4594197A
公开(公告)日：1986-06-10
申请号：US646230
申请日：1984-08-31
申请人： Kazuyuki Tomisawa , Kazuya Kameo , Toru Matsunaga , Shiuji Saito , Yoshimoto Nakashima , Kaoru Sota
发明人： Kazuyuki Tomisawa , Kazuya Kameo , Toru Matsunaga , Shiuji Saito , Yoshimoto Nakashima , Kaoru Sota
IPC分类号： A61K31/195 , A61K31/19 , A61K31/194 , A61K31/215 , A61P3/00 , A61P29/00 , A61P37/04 , C07C59/84 , C07C59/88 , C07C59/90 , C07C67/00 , C07C313/00 , C07C323/56 , C07C327/20 , C07C327/22 , C07C149/40 , C07C153/023 , C07C157/09
CPC分类号： C07C327/00 , C07C323/00 , C07C59/84 , C07C59/88 , C07C59/90
摘要： 3-Benzoyl-2-mercaptopropionic acid derivatives represented by the general formula ##STR1## (wherein, X represents a hydrogen atom, a halogen atom, hydroxy group, a lower alkyl group or a lower alkoxy group, Y represents a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group, Z represents a hydrogen atom or an acyl group, and R represents a hydrogen atom or a lower alkyl group). These compounds have immunomodulative function and are effective for the treatment of diseases caused by abnormal immunofunction.
摘要翻译：由通式“IMAGE”表示的3-苯甲酰基-2-巯基丙酸衍生物（其中，X表示氢原子，卤素原子，羟基，低级烷基或低级烷氧基，Y表示氢原子，卤素原子，低级烷基或低级烷氧基，Z表示氢原子或酰基，R表示氢原子或低级烷基）。这些化合物具有免疫调节功能，对于治疗异常免疫功能引起的疾病有效。

5. 发明授权

US5521311A 5-aminoacetylaminosulfonanilide compounds 失效
标题翻译： 5-氨基乙酰氨基磺酰苯胺化合物
公开(公告)号：US5521311A
公开(公告)日：1996-05-28
申请号：US501029
申请日：1995-08-14
申请人： Kensei Yoshikawa , Shiuji Saito , Yohichi Shimazaki , Mariko Kashiwa , Katsuo Hatayama
发明人： Kensei Yoshikawa , Shiuji Saito , Yohichi Shimazaki , Mariko Kashiwa , Katsuo Hatayama
IPC分类号： C07C311/08 , C07D295/15 , C07D295/073
CPC分类号： C07D295/15 , C07C311/08 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： The present compounds represented by the formula: ##STR1## (wherein R.sup.1 is a phenyl group, a halophenyl group or a cycloalkyl group having 3 to 8 carbon atoms, R.sup.2 is a hydrogen atom or an alkyl group having 1 to 5 carbon atoms, R.sup.3 is a hydrogen atom, an alkyl group having 1 to 7 carbon atoms, a cycloalkyl group having 3 to 8 carbon atoms, an alkenyl group having 3 to 5 carbon atoms or a benzyl group, or R.sup.2 and R.sup.3 are bonded together to form a 5- to 7-membered heterocycle) and salts thereof have potent anti-inflammatory, antipyretic, analgesic and anti-allergic actions with less side effects such as gastrointestinal disorders and with such a high safety as to permit long-term administration.
摘要翻译： PCT No.PCT / JP94 / 00228 Sec。 371日期1995年8月14日 102（e）日期1995年8月14日PCT 1994年2月16日PCT PCT。第WO94 / 19318号公报日本公开日：1994年9月1日。由下式表示的本发明化合物：其中R1为苯基，卤代苯基或碳原子数为3〜8的环烷基，R2为氢原子或具有 1至5个碳原子，R 3是氢原子，具有1至7个碳原子的烷基，具有3至8个碳原子的环烷基，具有3至5个碳原子的烯基或苄基，或R 2和R 3 被结合在一起以形成5-至7-元杂环），其盐具有有效的抗炎，解热，镇痛和抗过敏作用，具有较少的副作用，例如胃肠道疾病，并具有如此高的安全性，长期管理。

6. 发明申请

US20110213143A1 COMPOUND HAVING TAFIA INHIBITORY ACTIVITY 审中-公开
标题翻译：具有TAFIA抑制活性的化合物
公开(公告)号：US20110213143A1
公开(公告)日：2011-09-01
申请号：US13126685
申请日：2009-10-28
申请人： Hideaki Amada , Daisuke Matsuda , Masahiro Bohno , Shiuji Saito , Ayako Bohno
发明人： Hideaki Amada , Daisuke Matsuda , Masahiro Bohno , Shiuji Saito , Ayako Bohno
IPC分类号： C07D487/04 , C07D471/04 , C07D498/04 , C07D471/14
CPC分类号： C07D471/04 , C07D487/04
摘要： Provided are compounds having superior TAFIa inhibitory activity. Specifically, there are provided compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof: wherein A is a benzene ring or a pyridine ring; X is the formula —(CH2)—, the formula —(CH2)2—, an oxygen atom, a nitrogen atom or a single bond; Y is the formula —(CH2)3—NH—R3, the formula —(CH2)4—NH—R3 or a 2-aminopyridyl group; R3 is a hydrogen atom, a C1-6 alkyl group, or the formula —CO2R4; R4 is a C1-6 alkyl group, the formula —CHR5OC(O)R6, or a substituent having the structure represented by the following formula Ia; R5 is a C1-6 alkyl group; R6 is a C1-6 alkyl group, a C3-8 cycloalkyl group, or a phenyl group; R7 is a C1-6 alkyl group or a phenyl group; R1 is a hydrogen atom, a halogen atom, a C1-4 alkyl group substituted by 1-3 halogen atoms, a C1-10 alkyl group, a C1-8 alkoxy group, a C3-8 cycloalkyl group, a C3-8 cycloalkoxy group, a C4-14 cycloalkylalkyl group, or a phenyl group; R2 is CO2R8, or a tetrazolyl group; R8 is a hydrogen atom, a C1-10 alkyl group, or a substituent having the structure represented by the following formula Ib or Ic; m and n are each an integer of zero or one.
摘要翻译：提供具有优异TAFIa抑制活性的化合物。具体地，提供由下式（I）表示的化合物或其药学上可接受的盐：其中A是苯环或吡啶环; X是式 - （CH 2） - ，式 - （CH 2）2 - ，氧原子，氮原子或单键; Y是式 - （CH2）3-NH-R3，式 - （CH2）4-NH-R3或2-氨基吡啶基; R 3是氢原子，C 1-6烷基或式-CO 2 R 4; R4是C1-6烷基，式-CHR5OC（O）R6或具有由下式Ia表示的结构的取代基; R5是C1-6烷基; R6是C1-6烷基，C3-8环烷基或苯基; R7是C1-6烷基或苯基; R1是氢原子，卤素原子，被1-3个卤素原子取代的C1-4烷基，C1-10烷基，C1-8烷氧基，C3-8环烷基，C3-8环烷氧基基团，C4-14环烷基烷基或苯基; R2是CO2R8或四唑基; R8是氢原子，C1-10烷基或具有由下式Ib或Ic表示的结构的取代基; m和n分别为0或1的整数。

7. 发明授权

US06355663B1 Substituted isoxazolylthiophene compounds 失效
标题翻译：取代的异恶唑基噻吩化合物
公开(公告)号：US06355663B1
公开(公告)日：2002-03-12
申请号：US09786119
申请日：2001-03-01
申请人： Masahiro Harada , Junko Takeda , Toshio Nakamura , Shiuji Saito
发明人： Masahiro Harada , Junko Takeda , Toshio Nakamura , Shiuji Saito
IPC分类号： C07D41304
CPC分类号： C07D413/04
摘要： This invention provides a substituted isoxazolylthiophene compound represented by the formula wherein R1 and R2 individually represent an alkyl group of 1-5 carbon atoms, R3 represents a cyano group or a group CONR5R6 (in which R5 and R6 individually represent a hydrogen atom or an alkyl group of 1-10 carbon atoms), R4 represents an alkyl group of 1-5 carbon atoms or a phenyl group, and n is an integer of 0-2, or a salt thereof. The compounds of the invention are useful for the treatment or prevention of various bone diseases or nerve diseases, because they specifically enhance the action of the cell differentiation induction factors found in a living body.
摘要翻译：本发明提供由通式R 1和R 2表示的取代的异恶唑基噻吩化合物，各自表示1-5个碳原子的烷基，R3表示氰基或CONR5R6基团（其中R5和R6各自表示氢原子或烷基 1-10个碳原子），R4代表1-5个碳原子的烷基或苯基，n是0-2的整数，或其盐。本发明的化合物可用于治疗或预防各种骨病或神经疾病，因为它们特异性地增强了活体中发现的细胞分化诱导因子的作用。

8. 发明授权

US4885367A Sulfonanilide compounds 失效
标题翻译：磺酰苯胺化合物
公开(公告)号：US4885367A
公开(公告)日：1989-12-05
申请号：US271641
申请日：1988-11-16
申请人： Kensei Yoshikawa , Yutaka Ohuchi , Kazuto Sekiuchi , Shiuji Saito , Katsuo Hatayama , Kaoru Sota
发明人： Kensei Yoshikawa , Yutaka Ohuchi , Kazuto Sekiuchi , Shiuji Saito , Katsuo Hatayama , Kaoru Sota
IPC分类号： C07C311/08 , C07C311/09 , C07C317/40 , C07C323/35 , C07D211/46 , C07D309/12 , C07D335/02
CPC分类号： C07D211/46 , C07C311/08 , C07C311/09 , C07C317/40 , C07C323/35 , C07D309/12 , C07D335/02 , C07C2101/08 , C07C2101/14 , C07C2101/18 , C07C2102/42
摘要： Sulfonanilide compounds represented by the formula ##STR1## wherein R.sup.1 is a lower alkyl group or a trifluoromethyl group, R.sup.2 is a cycloalkylidenemethyl group, a group of the formula --A--R.sup.3 (wherein A is an oxygen atom, a sulfur atom, a sulfynyl group or a sulfinyl group and R.sup.3 is a cycloalkyl group having 5-8 carbon atoms; a cycloalkyl group having 5-8 carbon atoms substituted by one or two of a lower alkyl group, an oxo group, a hydroxyl group or a methanesulfonyloxy group, a tetrahydropyranyl group; a tetrahydrothiopyranyl group; or a 1-methyl-piperidyl group) or a group of the formula --B--R.sup.4 (wherein B is a carbonyl group, a hydroxymethylene group or a methylene group, R.sup.4 is a cycloalkyl group having 5-8 carbon atoms) and the pharmaceutically acceptable salts thereof have anti-inflammatory activity.

9. 发明授权

US4541959A Diphenylsulfide derivatives 失效
标题翻译：二苯硫醚衍生物
公开(公告)号：US4541959A
公开(公告)日：1985-09-17
申请号：US645356
申请日：1984-08-29
申请人： Kazuyuki Tomisawa , Kazuya Kameo , Toru Matsunaga , Shiuji Saito , Yoshimoto Nakashima , Kaoru Sata
发明人： Kazuyuki Tomisawa , Kazuya Kameo , Toru Matsunaga , Shiuji Saito , Yoshimoto Nakashima , Kaoru Sata
IPC分类号： A61K31/265 , A61K20060101 , A61K31/10 , A61P3/06 , A61P9/10 , C07C20060101 , C07C67/00 , C07C325/00 , C07C327/22 , C07C327/32 , C07C153/023
CPC分类号： C07C327/32
摘要： Diphenylsulfide derivatives represented by the general formula ##STR1## wherein, X represents a hydrogen atom, a chlorine atom or a methyl group, and R represents a hydrogen atom or a lower alkyl group. These diphenyl sulfides reduce lipids such as cholesterols and triglycerides in the blood of mammals.
摘要翻译：由通式表示的二苯硫醚衍生物，其中X表示氢原子，氯原子或甲基，R表示氢原子或低级烷基。这些二苯基硫化物在哺乳动物的血液中减少胆固醇和甘油三酯等脂质。

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