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1. 发明专利

JP2004131497A Cis-cyclopropane derivative 审中-公开
公开(公告)号：JP2004131497A
公开(公告)日：2004-04-30
申请号：JP2003323829
申请日：2003-09-17
申请人： Kyowa Hakko Kogyo Co Ltd , Satoshi Shuto , 協和醗酵工業株式会社 , 周東智
发明人： SHUTO SATOSHI , KAZUTA YUJI , MATSUDA AKIRA
IPC分类号： C07D233/64 , A61K31/417 , A61P1/00 , A61P3/04 , A61P9/00 , A61P25/00 , A61P25/02 , A61P25/08 , A61P25/20 , A61P29/00 , A61P37/08 , A61P43/00
摘要： PROBLEM TO BE SOLVED: To provide a cis-cyclopropane derivative or its pharmacologically acceptable salt having histamine H
3 acceptor agonistic activity and/or antagonistic activity and useful as a prophylactic and/or a remedy for allergy, inflammation, cardiac or cerebrovascular disease, gastrointestinal trouble, central nervous system trouble, psychiatric trouble of the central nervous system, epilepsy, spasm, obesity, somnipathy, etc.
SOLUTION: A pharmaceutical contains the cis-cyclopropane derivative expressed by formula (I) [R
1 is H, a substituted or unsubstituted lower alkyl or the like; R
2 and R
3 are identical to or different from each other and are each H, a substituted or unsubstituted lower alkyl or the like; and Q is -CR
4 =CR
5 -CHR
6 - (R
4 , R
5 , and R
6 are identical to or different from each other and are H or a substituted or unsubstituted lower alkyl), -CHR
4 -CHR
5 - or -CHR
4 -CHR
5 -CHR
6 -] or its pharmacologically acceptable salt as an active ingredient.
COPYRIGHT: (C)2004,JPO

2. 发明授权

US5200515A 5'-trifluoromethyl-2'-deoxy-uridine phospholipid compounds 失效
标题翻译： 5'-三氟甲基-2'-脱氧尿苷磷脂化合物
公开(公告)号：US5200515A
公开(公告)日：1993-04-06
申请号：US701125
申请日：1991-05-16
申请人： Satoshi Shuto , Hiromichi Itoh , Takumi Obara , Tatsuro Fujiwara
发明人： Satoshi Shuto , Hiromichi Itoh , Takumi Obara , Tatsuro Fujiwara
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61P35/00 , C07H19/10 , C12P19/30
CPC分类号： C07H19/10 , A61K47/48053 , C12P19/305
摘要： Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each C.sub.16-18 long-chain aliphatic acyl and are the same or different; and pharmacologically acceptable salts thereof are disclosed. These novel compounds are effective against 5-FU-resistant tumor cells, have low toxicity, and are not inactivated by nucleoside phosphorylase in vivo.

3. 发明授权

US5187174A 6'-deoxy-6'-halo-neplanocin A and its production 失效
标题翻译： 6'-脱氧-6'-卤代 - 尼泊那康A及其生产
公开(公告)号：US5187174A
公开(公告)日：1993-02-16
申请号：US673177
申请日：1991-03-18
申请人： Satoshi Shuto , Takumi Obara , Hiromichi Itoh , Takehiro Koshio , Tatsuro Fujiwara , Masao Yaso
发明人： Satoshi Shuto , Takumi Obara , Hiromichi Itoh , Takehiro Koshio , Tatsuro Fujiwara , Masao Yaso
IPC分类号： C07D473/00
CPC分类号： C07D473/00 , Y02P20/55
摘要： A compound of the formula ##STR1## wherein A is adenine-9-yl and X is halogen, Preferably iodine, or a pharmaceutically acceptable salt thereof. It is a novel derivative of neplanocin A and has almost the same level of cytotoxic activity. However, it is not inactivated by the action of adenosine deaminase. It is produced by replacing a hydroxyl at position-6' in neplanocin A or 2', 3'-O-protected neplanocin A with halogen by use of a halogenating agent, and when hydroxyl at position-2' or -3' is protected, removing the protective group thereof.
摘要翻译：式IMA的化合物，其中A是腺嘌呤-9-基，X是卤素，优选碘，或其药学上可接受的盐。它是奈曲立诺A的新型衍生物，具有几乎相同的细胞毒活性水平。然而，它不会被腺苷脱氨酶的作用所灭活。通过使用卤化剂用卤素取代在neplanocin A或2'，3'-O保护的neplanocin A中的6'位的羟基，并且当位置-2'或-3'的羟基被保护时，，除去其保护基。

4. 发明授权

US4921951A Nucleoside-phospholipid conjugate 失效
标题翻译：核苷 - 磷脂缀合物
公开(公告)号：US4921951A
公开(公告)日：1990-05-01
申请号：US102043
申请日：1987-09-28
申请人： Satoshi Shuto , Hiromichi Itoh , Kiyofumi Fukukawa , Masatoshi Tsujino
发明人： Satoshi Shuto , Hiromichi Itoh , Kiyofumi Fukukawa , Masatoshi Tsujino
IPC分类号： C07D473/00 , C07H19/10
CPC分类号： C07D473/00 , C07H19/10
摘要： Novel nucleoside-phospholipid conjugates of the formula ##STR1## wherein R.sub.1 is C.sub.14-24 long chain aliphatic acyl or C.sub.1-24 aliphatic alkyl and N.sub.s is a nucleoside residue; and pharmacologically acceptable salts thereof are prepared in a one-step reaction by reacting the corresponding nucleoside and glycerophospholipid derivative in the presence of phospholipase D-P.
摘要翻译：其中R1是C14-24长链脂族酰基或C1-24脂族烷基和Ns的新型核苷 - 磷脂缀合物是一种核苷残基; 其药理学上可接受的盐通过在磷脂酶D-P的存在下使相应的核苷和甘油磷脂衍生物反应而在一步反应中制备。

5. 发明授权

US4797479A Nucleoside-phospholipid conjugate 失效
标题翻译：核苷 - 磷脂缀合物
公开(公告)号：US4797479A
公开(公告)日：1989-01-10
申请号：US852881
申请日：1986-04-15
申请人： Satoshi Shuto , Hiromichi Ito , Kiyofumi Fukukawa , Hideo Sakakibara , Masatoshi Tsujino
发明人： Satoshi Shuto , Hiromichi Ito , Kiyofumi Fukukawa , Hideo Sakakibara , Masatoshi Tsujino
IPC分类号： C07D473/00 , C07D473/34 , C07H19/052 , C07H19/10 , C07H19/207 , C07H19/20
CPC分类号： C07D473/00 , C07D473/34 , C07H19/052 , C07H19/10 , C07H19/207
摘要： A compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are long-chain fatty acid residue, and Ns is nucleoside residue selected from the group consisting of 5-fluorouridine-5'-yl, 5-fluoro-2'-deoxyuridine-5'-yl-, bredinin-5'-yl, tubercidine-5'-yl-, neplanocin A-6'-yl-, 5-fluorocytidine-5'-yl-, arabinosylcytosine-5'-yl, arabinocyl-5-fluorocytosine-5'-yl-, arabinosyladenine-5'-yl- and arabinosylthymine-5 '-yl-, and pharmacologically acceptable salts thereof, having antitumor activity.
摘要翻译：式IMA的化合物，其中R1和R2是长链脂肪酸残基，Ns是选自5-氟尿嘧啶-5'-基，5-氟-2'-脱氧尿苷-5 ' - 基 - ，bredinin-5'-基，结核苷-5'-基 - ，尼泊洛环素A-6'-基 - ，5-氟胞苷-5'-基 - ，阿拉伯糖基胞嘧啶-5'-基，阿拉伯糖基-5- 氟胞嘧啶-5'-基 - ，阿拉伯糖基腺苷-5'-基 - 和阿拉伯糖基胸腺嘧啶-5'-基 - 及其药理学上可接受的盐，具有抗肿瘤活性。

6. 发明申请

US20120115714A1 CATALYST PRECURSOR, METHOD FOR PRODUCING THE SAME, METHOD FOR USING THE SAME, AND REACTOR THAT USES THE SAME 有权
标题翻译：催化剂前体，其制造方法，使用该催化剂的方法和使用该催化剂的反应器
公开(公告)号：US20120115714A1
公开(公告)日：2012-05-10
申请号：US13384281
申请日：2010-07-16
申请人： Mitsuhiro Arisawa , Satoshi Shuto , Naoyuki Hoshiya
发明人： Mitsuhiro Arisawa , Satoshi Shuto , Naoyuki Hoshiya
IPC分类号： B01J27/045 , B01J27/02 , C07D295/033 , C07D491/113 , C07F15/00 , C07C1/20 , C07C231/12 , C07C27/00 , C07C41/30 , C07C201/12 , C07C17/26 , B01J19/00 , C07C67/347
CPC分类号： C07D491/113 , B01J23/44 , B01J23/52 , B01J27/04 , B01J31/06 , B01J35/002 , B01J35/04 , B01J35/06 , B01J37/0207 , B01J37/0209 , B01J37/0225 , B01J37/20 , B01J2231/42 , B01J2231/4211 , B01J2231/4255 , B01J2231/4261 , B01J2231/4266 , B01J2231/4283 , C07C1/321 , C07C17/263 , C07C41/30 , C07C231/12 , C07C2523/44 , C07C2523/52 , C07C15/52 , C07C25/18 , C07C43/225 , C07C233/11
摘要： The present invention provides the catalyst precursor that has excellent safety and stability, has high stable activity retention rate, can be recycled, increases yield resulted from a reaction, and is easily processed into various forms. The catalyst precursor comprises a structure in which the entire structure is composed of gold or a gold-based alloy and the surface of the structure is modified with elemental sulfur, or at least the surface of the structure is composed of gold or a gold-based alloy and the surface of the structure is modified with elemental sulfur, and a catalytic metal compound supported on the structure, wherein the catalyst precursor has peaks derived from the catalytic metal compound and also sulfur as analyzed by photoelectron spectroscopy, and wherein the peak derived from sulfur is of the sulfur 1s orbital observed within a range of 2470 eV±2 eV in terms of the peak top position.
摘要翻译：本发明提供了具有优异的安全性和稳定性，具有高稳定活性保持率，可回收利用，增加反应产率的催化剂前体，易于加工成各种形式。催化剂前体包括其中整个结构由金或金基合金构成并且结构表面用元素硫改性的结构，或至少该结构的表面由金或金基组成合金，结构表面用元素硫改性，负载在该结构上的催化金属化合物，其中催化剂前体具有衍生自催化金属化合物的峰和通过光电子能谱分析的硫，并且其中衍生自在峰顶位置方面，硫是在2470eV±2eV的范围内观察到的硫1s轨道。

7. 发明授权

US5621142A Aminoalkylcyclopropane derivatives 失效
标题翻译：氨基烷基环丙烷衍生物
公开(公告)号：US5621142A
公开(公告)日：1997-04-15
申请号：US682776
申请日：1996-07-30
申请人： Daisuke Mochizuki , Satoshi Shuto
发明人： Daisuke Mochizuki , Satoshi Shuto
IPC分类号： C07B57/00 , C07C237/24 , C07C233/58
CPC分类号： C07B57/00 , C07C237/24 , C07C2101/02
摘要： Disclosed are a novel optically active compound represented by formula (1), a racemic modification thereof, and a pharmaceutically acceptable acid addition salt of the optically active compound or racemic modification thereof: ##STR1## wherein R is a straight chain or branched C.sub.1 -C.sub.5 aliphatic group which is saturated or unsaturated, or a phenyl group which is unsubstituted or substituted with 1 to 3 substituents which are each independently selected from the group consisting of a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a nitro group, an amino group, a hydroxyl group and a C.sub.1 -C.sub.4 alkoxy group; and mark * indicates an asymmetric carbon atom.The novel optically active aminoalkylcyclopropane derivative of the present invention, a racemic modification thereof, and a pharmaceutically acceptable acid addition salt of the optically active aminoalkylcyclopropane derivative or racemic modification thereof have remarkably high antagonistic activity with respect to NMDA receptor, as compared to known aminomethylcyclopropane derivatives and is useful as a preventive agent for cerebral infarction and a protective agent against ischemic diseases.
摘要翻译： PCT No.PCT / JP95 / 00254 Sec。 371日期：1996年7月30日 102（e）日期1996年7月30日PCT提交1995年2月22日PCT公布。公开号WO95 / 22521 日期：1995年8月24日公开了由式（1）表示的新型光学活性化合物，其外消旋化合物和旋光活性化合物的药学上可接受的酸加成盐或其外消旋变性：其中R为或者是未取代的或被1〜3个取代基取代的苯基，所述取代基各自独立地选自卤原子，C1-C4烷基硝基，氨基，羟基和C 1 -C 4烷氧基; 标记*表示不对称碳原子。与已知的氨基甲基环丙烷衍生物相比，本发明的新型光学活性氨基烷基环丙烷衍生物，其外消旋修饰物和光学活性氨基烷基环丙烷衍生物或其外消旋修饰的药学上可接受的酸加成盐相对于NMDA受体具有非常高的拮抗活性作为脑梗塞的预防剂和对缺血性疾病的保护剂有用。

8. 发明授权

US09175004B2 Catalyst precursor, method for producing the same, method for using the same, and reactor that uses the same 有权
标题翻译：催化剂前体，其制备方法，使用方法以及使用该催化剂前体的反应器
公开(公告)号：US09175004B2
公开(公告)日：2015-11-03
申请号：US13384281
申请日：2010-07-16
申请人： Mitsuhiro Arisawa , Satoshi Shuto , Naoyuki Hoshiya
发明人： Mitsuhiro Arisawa , Satoshi Shuto , Naoyuki Hoshiya
IPC分类号： B01J23/52 , B01J31/28 , C07D491/113 , B01J27/04 , B01J35/00 , B01J35/04 , B01J35/06 , B01J37/02 , B01J37/20 , C07C1/32 , C07C17/263 , C07C41/30 , C07C231/12 , B01J23/44
CPC分类号： C07D491/113 , B01J23/44 , B01J23/52 , B01J27/04 , B01J31/06 , B01J35/002 , B01J35/04 , B01J35/06 , B01J37/0207 , B01J37/0209 , B01J37/0225 , B01J37/20 , B01J2231/42 , B01J2231/4211 , B01J2231/4255 , B01J2231/4261 , B01J2231/4266 , B01J2231/4283 , C07C1/321 , C07C17/263 , C07C41/30 , C07C231/12 , C07C2523/44 , C07C2523/52 , C07C15/52 , C07C25/18 , C07C43/225 , C07C233/11
摘要： The present invention provides the catalyst precursor that has excellent safety and stability, has high stable activity retention rate, can be recycled, increases yield resulted from a reaction, and is easily processed into various forms. The catalyst precursor comprises a structure in which the entire structure is composed of gold or a gold-based alloy and the surface of the structure is modified with elemental sulfur, or at least the surface of the structure is composed of gold or a gold-based alloy and the surface of the structure is modified with elemental sulfur, and a catalytic metal compound supported on the structure, wherein the catalyst precursor has peaks derived from the catalytic metal compound and also sulfur as analyzed by photoelectron spectroscopy, and wherein the peak derived from sulfur is of the sulfur 1s orbital observed within a range of 2470 eV±2 eV in terms of the peak top position.
摘要翻译：本发明提供了具有优异的安全性和稳定性，具有高稳定活性保持率，可回收利用，增加反应产率的催化剂前体，易于加工成各种形式。催化剂前体包括其中整个结构由金或金基合金构成并且结构表面用元素硫改性的结构，或至少该结构的表面由金或金基组成合金，结构表面用元素硫改性，负载在该结构上的催化金属化合物，其中催化剂前体具有衍生自催化金属化合物的峰和通过光电子能谱分析的硫，并且其中衍生自在峰顶位置方面，硫是在2470eV±2eV的范围内观察到的硫1s轨道。

9. 发明授权

US5051499A Novel nucleoside-phospholipid conjugate 失效
标题翻译：新型核苷 - 磷脂缀合物
公开(公告)号：US5051499A
公开(公告)日：1991-09-24
申请号：US445965
申请日：1989-11-28
申请人： Satoshi Shuto , Hiromichi Itoh , Kiyofumi Fukukawa , Masatoshi Tsujino
发明人： Satoshi Shuto , Hiromichi Itoh , Kiyofumi Fukukawa , Masatoshi Tsujino
IPC分类号： C07D473/00 , C07H19/10
CPC分类号： C07D473/00 , C07H19/10
摘要： Novel nucleoside-phospholipid conjugates of the formula ##STR1## wherein R.sub.1 is C.sub.14-24 long chain aliphatic acyl or C.sub.1-24 aliphatic alkyl, R.sub.2 is C.sub.2-10 aliphatic acyl or C.sub.1-24 aliphatic alkyl and N.sub.s is a nucleoside residue; and pharmacologically acceptable salts thereof are prepared in a one-step reaction by reacting the corresponding nucleoside and glycerophospholipid derivative in the presence of phospholipase D-P.

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