公开(公告)号：US20080312435A1

公开(公告)日：2008-12-18

申请号：US11667728

申请日：2005-10-31

Applicant: 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

Inventor： 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: C07D417/12 ,  C07D213/75 ,  C07D277/46 ,  C07D231/40 ,  C07D263/48

CPC classification number: C07D417/12 ,  C07D213/75 ,  C07D231/40 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20050038259A1

公开(公告)日：2005-02-17

申请号：US10489205

申请日：2002-09-09

Applicant: John Falck ,  Noriyuki Miyata ,  Naoya Ono ,  Tomomichi Chonan ,  Hitomi Hirano ,  Yoshihisa Toda ,  Tohru Tanami ,  Shigeru Okuyama

Inventor： John Falck ,  Noriyuki Miyata ,  Naoya Ono ,  Tomomichi Chonan ,  Hitomi Hirano ,  Yoshihisa Toda ,  Tohru Tanami ,  Shigeru Okuyama

IPC: C07D277/20 ,  A61K31/047 ,  A61K31/08 ,  A61K31/16 ,  A61K31/18 ,  A61K31/185 ,  A61K31/201 ,  A61K31/231 ,  A61K31/275 ,  A61K31/41 ,  A61K31/426 ,  A61P1/02 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P11/08 ,  A61P13/12 ,  A61P15/00 ,  A61P15/06 ,  A61P17/02 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P31/00 ,  A61P31/04 ,  A61P37/02 ,  A61P37/06 ,  A61P43/00 ,  C07C33/04 ,  C07C33/044 ,  C07C33/42 ,  C07C59/01 ,  C07C59/42 ,  C07C59/46 ,  C07C59/60 ,  C07C69/708 ,  C07C69/732 ,  C07C235/28 ,  C07C255/15 ,  C07C255/16 ,  C07C259/06 ,  C07C309/08 ,  C07C309/10 ,  C07C309/20 ,  C07C309/23 ,  C07C309/24 ,  C07C309/68 ,  C07C311/04 ,  C07C311/17 ,  C07C311/51 ,  C07C317/44 ,  C07C323/52 ,  C07C323/66 ,  C07D257/04 ,  C07D277/34 ,  C07D277/12 ,  C11C3/00

CPC classification number: C07D257/04 ,  C07C33/044 ,  C07C33/423 ,  C07C33/426 ,  C07C59/42 ,  C07C59/46 ,  C07C59/60 ,  C07C69/708 ,  C07C235/28 ,  C07C255/15 ,  C07C259/06 ,  C07C309/10 ,  C07C309/20 ,  C07C309/23 ,  C07C309/24 ,  C07C309/68 ,  C07C311/17 ,  C07C311/51 ,  C07C317/44 ,  C07C323/52 ,  C07C323/66 ,  C07C2601/08 ,  C07C2601/14 ,  C07D277/34

Abstract: A hydroxyeicosenoic acid analog represented by the following Formula (I), the bond ≡ represents a cis-vinylene group or an ethynylene group; Y represents CH2, O or S(O)p wherein p is 0, 1 or 2; m represents an integer of 1 to 4 inclusive; n represents an integer of 0 to 3 inclusive; the sum of m and n is an integer of 3 to 7 inclusive; R1 represents a C1-4 alkyl group or a C3-8 cycloalkyl group; R2 represents a hydrogen atom or a methyl group; R3 represents COR4, a nitrile group, a halogen atom, a tetrazole group or a thiazolidinedione group; R4 represents OR6, NHR6, N(OH)R6, NHSO2R5, glycerol or functionalized glycerols; R5 represents a C1-15 alkyl group, a C6-10 aryl group or a C7-14 aryl group substituted with alkyl groups, halogens or amino groups; R6 represents a hydrogen, a C1-10 alkyl group or a C1-10 alkyl group substituted with a hydroxyl group, or a pharmaceutically acceptable salt or hydrate thereof. The compounds of the present invention are useful as an elastase release inhibitor.

Abstract translation: 由下式（I）表示的羟基二十碳烯酸类似物，键=表示顺式亚乙烯基或亚乙炔基; Y表示CH 2，O或S（O）p，其中p为0,1或2; m表示1〜4的整数， n表示0〜3的整数， m和n的和为3〜7的整数， R 1表示C 1-4烷基或C 3-8环烷基; R 2表示氢原子或甲基; R 3表示COR 4，腈基，卤素原子，四唑基或噻唑烷二酮基; R 4表示OR 6，NHR 6，N（OH）R 6，NHSO 2 R 5，甘油或官能化甘油; R 5代表C1-15烷基，C6-10芳基或被烷基，卤素或氨基取代的C7-14芳基; R 6表示氢，C 1-10烷基或被羟基取代的C 1-10烷基，或其药学上可接受的盐或水合物。 本发明的化合物可用作弹性蛋白酶释放抑制剂。

公开(公告)号：US20050020680A1

公开(公告)日：2005-01-27

申请号：US10489204

申请日：2002-09-09

Applicant: John Falck ,  Noriyuki Miyata ,  Naoya Ono ,  Tomomichi Chonan ,  Hitomi Hirano ,  Yoshihisa Toda ,  Tohru Tanami ,  Shigeru Okuyama

Inventor： John Falck ,  Noriyuki Miyata ,  Naoya Ono ,  Tomomichi Chonan ,  Hitomi Hirano ,  Yoshihisa Toda ,  Tohru Tanami ,  Shigeru Okuyama

IPC: C07C33/044 ,  C07C33/42 ,  C07C59/42 ,  C07C59/46 ,  C07C59/60 ,  C07C69/708 ,  C07C235/28 ,  C07C255/15 ,  C07C259/06 ,  C07C309/10 ,  C07C309/20 ,  C07C309/23 ,  C07C309/24 ,  C07C309/68 ,  C07C311/17 ,  C07C311/51 ,  C07C317/44 ,  C07C323/52 ,  C07C323/66 ,  C07D257/04 ,  C07D277/34 ,  A61K31/185 ,  C07

CPC classification number: C07D257/04 ,  C07C33/044 ,  C07C33/423 ,  C07C33/426 ,  C07C59/42 ,  C07C59/46 ,  C07C59/60 ,  C07C69/708 ,  C07C235/28 ,  C07C255/15 ,  C07C259/06 ,  C07C309/10 ,  C07C309/20 ,  C07C309/23 ,  C07C309/24 ,  C07C309/68 ,  C07C311/17 ,  C07C311/51 ,  C07C317/44 ,  C07C323/52 ,  C07C323/66 ,  C07C2601/08 ,  C07C2601/14 ,  C07D277/34

Abstract: A hydroxyfattysulfonic acid analog represented by Formula (I): wherein X is an ethylene group, a vinylene group or an ethynylene group; Y is an ethylene group, a vinylene group, an ethynylene group, OCH2 or S(O)pCH2 wherein p is 0, 1 or 2; m is an integer of 1 to 5 inclusive; n is an integer of 0 to 4 inclusive; R1 is a C1-8 alkyl group, a C3-8 cycloalkyl group, a C1-4 alkyl group substituted with a C3-8 cycloalkyl group, a C1-4 alkyl group substituted with an aryl group or a C1-4 alkyl group substituted with an aryloxy group; R2 is a hydrogen atom or a methyl group; R1 and R2 together with the carbon atom to which they are attached may form a C3-8 cycloalkyl group; R3 is a hydrogen atom or a C2-8 acyl group; R4 is OR5 or NHR6, wherein R5 is a hydrogen atom, a C1-4 alkyl group, an alkali metal, an alkaline earth metal or an ammonium group and R6 is a hydrogen atom or a C1-4 alkyl group; or a pharmaceutically acceptable salt or a hydrate thereof. The compounds of the present invention are useful as an elastase release inhibitor.

Abstract translation: 由式（I）表示的羟基脂肪磺酸类似物：其中X是亚乙基，亚乙烯基或亚乙炔基; Y是亚乙基，亚乙烯基，亚乙炔基，OCH 2或S（O）pCH 2，其中p是0,1或2; m为1〜5的整数， n为0〜4的整数， R 1是C 1-8烷基，C 3-8环烷基，被C 3-8环烷基取代的C 1-4烷基，被芳基取代的C 1-4烷基或C 1-4 被芳氧基取代的烷基; R 2是氢原子或甲基; R 1和R 2与它们所连接的碳原子一起可以形成C 3-8环烷基; R 3是氢原子或C 2-8酰基; R 4是OR 5或NHR 6，其中R 5是氢原子，C 1-4烷基，碱金属，碱土金属或铵基，R 6是 氢原子或C 1-4烷基; 或其药学上可接受的盐或其水合物。 本发明的化合物可用作弹性蛋白酶释放抑制剂。

公开(公告)号：US5457249A

公开(公告)日：1995-10-10

申请号：US180811

申请日：1994-01-10

Applicant: Toshihiro Sagane ,  Yoichiro Tsuji ,  Yoshihisa Toda

Inventor： Toshihiro Sagane ,  Yoichiro Tsuji ,  Yoshihisa Toda

IPC: C07C5/22 ,  C07C13/00

CPC classification number: C07C5/2206 ,  C07C2102/42 ,  C07C2103/86

Abstract: A process for isomerization of an endo-form of aromatic group-containing norbornenes represented by the following formula (I) to an exo-form which comprises bringing the endo-form into contact with a solid acid catalyst. ##STR1## wherein p is 0 or an integer of 1 or more, q and r are each 0, 1 or 2, R.sup.1 to R.sup.15 are each independently hydrogen or halogen atom, aliphatic hydrocarbon group, aromatic hydrocarbon group or alkoxy group, R.sup.5 (or R.sup.6) are R.sup.9 (or R.sup.7) may be linked together through an alkylene group of 1-3 carbons or may be directly linked together.

Abstract translation: 由下式（I）表示的含内酰基基团的降冰片烯内酯形式异构化的方法包括使内型物与固体酸催化剂接触。 （I）其中p为0或1或更大的整数，q和r各自为0,1或2，R 1至R 15各自独立地为氢或卤素原子，脂族烃基，芳族烃基或烷氧基 R 5（或R 6）为R 9（或R 7）可以通过1-3个碳的亚烷基连接在一起，或者可以直接连接在一起。

公开(公告)号：US4406859A

公开(公告)日：1983-09-27

申请号：US440526

申请日：1982-11-10

Applicant: Yoshihisa Toda ,  Hiroshi Yamamoto ,  Kenzi Sata

Inventor： Yoshihisa Toda ,  Hiroshi Yamamoto ,  Kenzi Sata

IPC: C22C9/00 ,  C22C9/06 ,  C22B25/00

CPC classification number: C22C9/06

Abstract: Anticorrosion copper alloy essentially consisting of 4.5-32 wt % of Ni, 0.3-2.5 wt % of Fe, one or more elements selected from 0.01-1.0 wt % of In, 0.003-0.2 wt % of Pd and 0.003-0.1 wt % of Pt, and the balance of Cu and normal impurities. Further, an anticorrosion copper alloy essentially consisting of 4.5-22 wt % of Ni, 1.3-2.5 wt % of Fe, one or more elements selected from 0.1-1.0 wt % of In, 0.01-0.2 wt % of Pd and 0.01-0.1 wt % of Pt, and the balance of Cu and normal impurities; and said Fe being kept in a state of solid solution in a matrix of said copper alloy.

Abstract translation: 防腐铜合金基本上由4.5-32wt％的Ni，0.3-2.5wt％的Fe，一个或多个元素选自0.01-1.0wt％的In，0.003-0.2wt％的Pd和0.003-0.1wt％的 Pt，余量为Cu和正常杂质。 此外，主要由4.5-22重量％的Ni，1.3-2.5重量％的Fe，一种或多种选自0.1-1.0重量％的In，0.01-0.2重量％的Pd和0.01-0.1重量％的元素组成的防腐铜合金 Pt的重量％，余量为Cu和正常杂质; 并且所述Fe被保持在所述铜合金基体中的固溶状态。