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1. 发明授权

US5298622A Spiroindane opiate analogs 失效
标题翻译：螺环素类鸦片类似物
公开(公告)号：US5298622A
公开(公告)日：1994-03-29
申请号：US60638
申请日：1993-05-12
申请人： Philip S. Portoghese , Shigenori Ohkawa , Scott T. Moe
发明人： Philip S. Portoghese , Shigenori Ohkawa , Scott T. Moe
IPC分类号： C07D489/08 , C07D489/09 , A61K31/485
CPC分类号： C07D489/08 , Y02P20/55
摘要： The present invention provides biologically active compounds of the formulas (I) and (II): (* CHEMICAL STRUCTURE *) (I) (* CHEMICAL STRUCTURE *) (II) wherein R3 is H or a hydroxyl protecting group, R2 is OH, H or a protected hydroxyl group, R1 is alkyl, cycloalkylalkyl, aryl, aralkyl, cycloalkenylalkyl, alkenyl, allyl or furanylalkyl; and R4 and R5 are individually H, halo, NO2, NH2, (C1-C5)alkyl, (C1-C5)alkoxy, or together are methylene-dioxy or benzo; and the pharmaceutically acceptable salts thereof.
摘要翻译：本发明提供式（I）和（II）的生物活性化合物：其中R 3是H或羟基保护基，R 2是OH，H或保护的羟基 R 1是烷基，环烷基烷基，芳基，芳烷基，环烯基烷基，烯基，烯丙基或呋喃基烷基; 并且R 4和R 5分别为H，卤素，NO 2，NH 2，（C 1 -C 5）烷基，（C 1 -C 5）烷氧基，或一起为亚甲基 - 二氧基或苯并; 及其药学上可接受的盐。

2. 发明授权

US07750037B2 Antidepressant 失效
标题翻译：抗抑郁药
公开(公告)号：US07750037B2
公开(公告)日：2010-07-06
申请号：US11475539
申请日：2006-06-27
申请人： Shigenori Ohkawa , Masaomi Miyamoto
发明人： Shigenori Ohkawa , Masaomi Miyamoto
IPC分类号： A61K31/4035 , C07D405/02
CPC分类号： C07D405/04 , C07D307/79 , C07D405/12 , C07D409/12 , C07D491/04 , C07D491/10
摘要： A PKB (Akt) activating agent comprising a compound represented by the formula (I): wherein R1 and R2: H, a hydrocarbon group or a heterocyclic group or R1 and R2 form a ring in cooperation with the adjacent carbon atom; R3: H, a hydrocarbon group or a heterocyclic group; W: represents a group represented by the formulas: wherein ring A: an optionally substituted benzene ring; ring B: an optionally substituted 5- to 7-membered nitrogen-containing heterocycle; R4: an aliphatic hydrocarbon group substituted with an aromatic group and further optionally substituted, or an acyl group containing an aromatic group; R5: H, C1-6 alkyl or acyl; R4c: an aromatic group, an aliphatic hydrocarbon group or acyl; and X: O or S; Y: O, S or NH; and ring C: an optionally substituted benzene ring, or a salt or a prodrug thereof, and use of the activating agent in prevention or treatment of depression, anxiety, manic-depressive psychosis or PTSD are provided.
摘要翻译：一种PKB（Akt）活化剂，其包含由式（I）表示的化合物：其中R1和R2：H，烃基或杂环基或R1和R2与相邻碳原子一起形成环; R3：H，烃基或杂环基; W：表示由下式表示的基团：其中环A：任选取代的苯环; 环B：任选取代的5-至7-元含氮杂环; R4：被芳基取代并进一步任选取代的脂族烃基或含芳基的酰基; R5：H，C1-6烷基或酰基; R4c：芳基，脂族烃基或酰基; 和X：O或S; Y：O，S或NH; 和环C：任选取代的苯环，或其盐或前药，并且提供了用于预防或治疗抑郁，焦虑，躁狂抑郁性精神病或PTSD的活化剂。

3. 发明申请

US20050148650A1 Antidepressant 审中-公开
标题翻译：抗抑郁药
公开(公告)号：US20050148650A1
公开(公告)日：2005-07-07
申请号：US10506269
申请日：2003-02-28
申请人： Shigenori Ohkawa , Masaomi Miyamoto
发明人： Shigenori Ohkawa , Masaomi Miyamoto
IPC分类号： A61P25/00 , A61P25/14 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D307/79 , C07D405/04 , C07D405/12 , C07D409/12 , C07D491/04 , C07D491/056 , C07D491/10 , C07D491/107 , A61K31/4035 , A61K31/407
CPC分类号： C07D405/04 , C07D307/79 , C07D405/12 , C07D409/12 , C07D491/04 , C07D491/10
摘要： A PKB (Akt) activating agent comprising a compound represented by the formula (I): wherein R1 and R2: H, a hydrocarbon group or a heterocyclic group or R1 and R2 form a ring in cooperation with the adjacent carbon atom; R3: H, a hydrocarbon group or a heterocyclic group; W: represents a group represented by the formulas: wherein ring A: an optionally substituted benzene ring; ring B: an optionally substituted 5- to 7-membered nitrogen-containing heterocycle; R4: an aliphatic hydrocarbon group substituted with an aromatic group and further optionally substituted, or an acyl group containing an aromatic group; R5: H, C1-6 alkyl or acyl; R4c: an aromatic group, an aliphatic hydrocarbon group or acyl; and X:O or S; Y:O, S or NH; and ring C: an optionally substituted benzene ring, or a salt or a prodrug thereof, and use of the activating agent in prevention or treatment of depression, anxiety, manic-depressive psychosis or PTSD are provided.
摘要翻译：一种PKB（Akt）活化剂，其包含由式（I）表示的化合物：其中R 1和R 2：H，烃基或杂环基或R 与相邻的碳原子一起形成环;和<！ - SIPO

4. 发明授权

US06872718B1 Tricyclic dihydrobenzofuran derivatives, process for the preparation thereof and agents 失效
标题翻译：三环二氢苯并呋喃衍生物，其制备方法和试剂
公开(公告)号：US06872718B1
公开(公告)日：2005-03-29
申请号：US10069180
申请日：2000-08-18
申请人： Shigenori Ohkawa , Tadatoshi Hashimoto , Tetsuya Tsukamoto
发明人： Shigenori Ohkawa , Tadatoshi Hashimoto , Tetsuya Tsukamoto
IPC分类号： A61P9/08 , A61P9/10 , A61P13/02 , A61P25/00 , A61P25/16 , A61P25/28 , C07D491/04 , C07D491/048 , D07D491/048 , A61K31/407 , A61K31/4741 , A61K31/55
CPC分类号： C07D491/04
摘要： A compound represented by the formula: wherein Ring A is a non-aromatic 5- to 7-membered nitrogen-containing heterocyclic ring which may be further substituted, Ring B is benzene ring which is further substituted, Ring C is a dihydrofuran-ring which may be further substituted and R is hydrogen atom or an acyl group or a salt thereof has an excellent lipid peroxidation inhibitory activity and is useful as a lipid peroxidation inhibitor.
摘要翻译：一种由下式表示的化合物：其中环A是可进一步被取代的非芳族5-至7-元含氮杂环，环B为进一步取代的苯环，环C为二氢呋喃环，其中可以进一步被取代，R是氢原子或酰基或其盐具有优异的脂质过氧化抑制活性，可用作脂质过氧化抑制剂。

5. 发明授权

US06583146B1 Thiazolopyrimidine compounds, its production and use 失效
标题翻译：噻唑并嘧啶化合物，其生产和使用
公开(公告)号：US06583146B1
公开(公告)日：2003-06-24
申请号：US09889139
申请日：2001-07-12
申请人： Shigenori Ohkawa , Naoyuki Kanzaki , Seiji Miwatashi
发明人： Shigenori Ohkawa , Naoyuki Kanzaki , Seiji Miwatashi
IPC分类号： A61K31519
CPC分类号： C07D513/04 , A61K31/519
摘要： Compounds represented by general formula (I): and salts thereof, exhibiting excellent adenosine A3 receptor antagonism: wherein A is an optionally substituted benzene ring; B may be further substituted; and R1 is an optionally substituted cyclic group.
摘要翻译：由通式（I）表示的化合物及其盐，显示出优异的腺苷A3受体拮抗作用：其中A为任选取代的苯环; B可以进一步被取代; 并且R 1是任选取代的环状基团。

6. 发明授权

US06248766B1 Tricyclic compounds, their production and use 失效
标题翻译：三环化合物，其生产和使用
公开(公告)号：US06248766B1
公开(公告)日：2001-06-19
申请号：US09254446
申请日：1999-03-09
申请人： Shigenori Ohkawa , Masaki Setoh , Zen-ichi Terashita
发明人： Shigenori Ohkawa , Masaki Setoh , Zen-ichi Terashita
IPC分类号： A61K31428
CPC分类号： C07D277/60 , C07D277/84 , C07D513/04
摘要： A compound of the formula: wherein R1 is H or a substituent; m is 1-3; Ar is an aromatic group which may be substituted; X is a bond or a divalent straight-chain group having 1-6 atoms which may be substituted; Y is —S—, —O—, or —N(R2— (R2 is H or a substituent group), Z is —N═ or —C(R3)═ (R3 is H or a hydrocarbon group), ring A is a benzene ring; ring B is a 5- to 7-membered ring which may be substituted, or a salt thereof is useful for eliciting a prostaglandin I2 receptor agonistic effect.
摘要翻译：下式的化合物：其中R 1是H或取代基; m为1-3; Ar是可以被取代的芳基; X是可以被取代的具有1-6个原子的键或二价直链基团; Y是-S-，-O-或-N（R2-（R2是H或取代基），Z是-N =或-C（R3）=（R3是H或烃基），环A 是苯环;环B是可被取代的5-至7-元环，或其盐可用于引发前列腺素I2受体激动作用。

7. 发明授权

US5116861A Nitrosothiol derivatives and their use 失效
标题翻译：硝基苯酚衍生物及其用途
公开(公告)号：US5116861A
公开(公告)日：1992-05-26
申请号：US562626
申请日：1990-08-03
申请人： Giichi Goto , Shigenori Ohkawa , Shoji Fukumoto
发明人： Giichi Goto , Shigenori Ohkawa , Shoji Fukumoto
IPC分类号： A61K38/00 , C07C381/00 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/093
CPC分类号： C07K5/0819 , C07C381/00 , C07K5/0215 , C07K5/0606 , A61K38/00
摘要： Novel nitrosothiol derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.3 is a hydrogen atom, an acyl group or a hydrocarbon residue which may be substituted; X.sup.1 is a hydrogen atom, an acyl group, a lower alkoxy group or a hydrocarbon residue which may be substituted; X.sup.2 is an acyl group or a carboxyl group which may be esterified or which may form an amide; with proviso that when X.sup.2 is a carboxyl group X.sup.1 is not a hydrogen atom or acetyl group and that when both R.sup.1 and R.sup.2 are hydrogen atoms X.sup.1 is not acetyl group or .gamma.-glutamyl group, and salts thereof, show excellent hypotensive action, antiarrhythmic action, anti-anginal action, cardiotonic action or coronary vasodilation, thus being useful as therapeutic or prophylactic agents for the cardiovascular diseases such as hypertension and angina pectoris.

8. 发明授权

US07507841B2 Cannabinoid receptor modulator 有权
标题翻译：大麻素受体调节剂
公开(公告)号：US07507841B2
公开(公告)日：2009-03-24
申请号：US11822941
申请日：2007-07-11
申请人： Shigenori Ohkawa , Tetsuya Tsukamoto , Yoshihiro Kiyota , Mika Goto , Shouzou Yamamoto , Masato Shimojou , Masaki Setou
发明人： Shigenori Ohkawa , Tetsuya Tsukamoto , Yoshihiro Kiyota , Mika Goto , Shouzou Yamamoto , Masato Shimojou , Masaki Setou
IPC分类号： C07D307/76
CPC分类号： C07D307/83 , A61K31/343 , A61K31/357 , A61K31/381 , A61K31/4025 , A61K31/4178 , A61K31/426 , A61K31/443 , A61K31/453 , A61K31/506 , C07D307/79 , C07D307/86 , C07D333/54 , C07D405/04
摘要： A cannabinoid receptor modulator containing a compound represented by Formula (I0) wherein, X is an oxygen atom, etc., R0 is an optionally substituted acylamino group, ring A0 is a benzene ring which may further have a substituent in addition to R0, and ring B is an optionally substituted 5-membered heterocycle, or a salt thereof or a prodrug thereof.
摘要翻译：含有由式（I0）表示的化合物的大麻素受体调节剂，其中X是氧原子等，R 0是任选取代的酰基氨基，环A 0是除了R 0之外还可以具有取代基的苯环，和环B是任选取代的5元杂环，或其盐或其前药。

9. 发明申请

US20090048307A1 5-pyridyl-1, 3-azole compounds, process for producing the same and use there of 审中-公开
标题翻译： 5-吡啶基-1,3-唑化合物，其制备方法和用途
公开(公告)号：US20090048307A1
公开(公告)日：2009-02-19
申请号：US11896072
申请日：2007-08-29
申请人： Shigenori Ohkawa , Naoyuki Kanzaki , Seiji Miwatashi
发明人： Shigenori Ohkawa , Naoyuki Kanzaki , Seiji Miwatashi
IPC分类号： A61K31/4439 , C07D413/04 , C07D417/04
CPC分类号： C07D417/14 , C07D417/04
摘要： An optionally N-oxidized compound represented by the formula: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-α inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-α.
摘要翻译：由下式表示的任选的N-氧化化合物：其中R1表示氢，烃，杂环，氨基，酰基，R2表示芳族基团，R3表示氢，吡啶基，芳香烃，X表示氧，任选氧化的硫，Y表示键，氧，任选氧化的硫，由式NR4表示的基团（R4表示氢，烃或酰基），Z表示键或二价无环烃或其盐具有优异的腺苷A3受体拮抗活性，并且为用作预防或治疗与腺苷A3受体有关的疾病的药剂。此外，化合物（I）或其盐具有p38 MAP激酶抑制活性和TNF-α抑制活性，并且用作预防或治疗与p38 MAP激酶相关的疾病和与TNF-α相关的疾病的药剂。

10. 发明申请

US20080021087A1 Cannabinoid receptor modulator 有权
标题翻译：大麻素受体调节剂
公开(公告)号：US20080021087A1
公开(公告)日：2008-01-24
申请号：US11822941
申请日：2007-07-11
申请人： Shigenori Ohkawa , Tetsuya Tsukamoto , Yoshihiro Kiyota , Mika Goto , Shouzou Yamamoto , Masato Shimojou , Masaki Setou
发明人： Shigenori Ohkawa , Tetsuya Tsukamoto , Yoshihiro Kiyota , Mika Goto , Shouzou Yamamoto , Masato Shimojou , Masaki Setou
IPC分类号： A61K31/34 , A61K31/381 , A61K31/40 , A61K31/4427 , A61P1/00 , A61P1/04 , A61P11/00 , A61P11/06 , A61P17/00 , A61P19/02 , A61P25/00 , A61P25/16 , A61P25/34 , A61P27/00 , A61P31/22 , C07D209/56 , C07D307/00 , C07D333/52 , C07D401/00 , C07D409/02 , C07D409/14 , C07D497/00
CPC分类号： C07D307/83 , A61K31/343 , A61K31/357 , A61K31/381 , A61K31/4025 , A61K31/4178 , A61K31/426 , A61K31/443 , A61K31/453 , A61K31/506 , C07D307/79 , C07D307/86 , C07D333/54 , C07D405/04
摘要： A cannabinoid receptor modulator containing a compound represented by Formula (I0) wherein, X is an oxygen atom, etc., R0 is an optionally substituted acylamino group, ring A0 is a benzene ring which may further have a substituent in addition to R0, and ring B is an optionally substituted 5-membered heterocycle, or a salt thereof or a prodrug thereof.
摘要翻译：含有由式（I ）表示的化合物的大麻素受体调节剂，其中X是氧原子等，R 0是任选取代的酰基氨基，环A 除了R 0 O以外，还可以具有取代基的苯环，环B是任选取代的5元杂环，或其盐或前药其中。

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