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1. 发明授权

US6166033A 2-carbonylthiazole derivatives and use of the same 失效
标题翻译： 2-羰基噻唑衍生物及其用途
公开(公告)号：US6166033A
公开(公告)日：2000-12-26
申请号：US269021
申请日：1999-11-05
申请人： Atsuro Nakazato , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Makoto Gotoh , Masanori Yoshida
发明人： Atsuro Nakazato , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Makoto Gotoh , Masanori Yoshida
IPC分类号： A61K31/425 , C07D417/06 , A61K31/4535 , A61K31/496 , C07D211/70 , C07D401/14 , C07D413/06
CPC分类号： C07D417/06
摘要： This invention provides a 2-carbonylthiazole derivative represented by formula (I): ##STR1## wherein each of Ar.sup.1 and Ar.sup.2 represents a phenyl group or a substituted phenyl group; R.sup.1 represents an alkoxy group having 1 to 5 carbon atoms, a hydroxyl group or an amino group; Y.sup.1 --Y.sup.2 represents CH--CO or C.dbd.CR.sup.2, wherein R.sup.2 represents a hydrogen atom or an alkyl group having 1 to 5 carbon atoms; and n is an integer of from 1 to 4, or a pharmaceutically acceptable salt thereof. The disclosed compounds are useful as drugs for preventing and treating dopamine D receptor-related morbid states such as schizophrenia and problematic behavior caused by cerebrovascular accidents and senile dementia and do not induce extrapyramidal disorders as side effects.
摘要翻译： PCT No.PCT / JP97 / 03342 Sec。 371日期1999年11月5日 102（e）1999年11月5日PCT PCT 1997年9月19日PCT公布。公开号WO98 / 12195 日期：1998年3月26日本发明提供由式（I）表示的2-羰基噻唑衍生物：其中Ar1和Ar2各自表示苯基或取代的苯基; R1表示碳原子数1〜5的烷氧基，羟基或氨基。 Y1-Y2表示CH-CO或C = CR2，其中R2表示氢原子或具有1至5个碳原子的烷基; 和n为1〜4的整数，或其药学上可接受的盐。所公开的化合物可用作预防和治疗多巴胺D受体相关的病态，如精神分裂症和由脑血管意外和老年痴呆引起的问题行为的药物，并且不诱导锥体外系疾病作为副作用。

2. 发明授权

US06806275B2 Arylpiperidine derivatives and use thereof 失效
标题翻译：芳基哌啶衍生物及其用途
公开(公告)号：US06806275B2
公开(公告)日：2004-10-19
申请号：US10120408
申请日：2002-04-12
申请人： Masashi Nagamine , Makoto Gotoh , Masanori Yoshida , Atsuro Nakazato , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa
发明人： Masashi Nagamine , Makoto Gotoh , Masanori Yoshida , Atsuro Nakazato , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa
IPC分类号： A61K31505
CPC分类号： C07D401/14 , C07D409/14 , C07D417/14
摘要： The present invention provides an arylpiperidine derivative of the formula (I) or a pharmaceutically acceptable salt thereof, which has antipsychotic effect: wherein D is a carbon atom or a nitrogen atom, E is a CH group or a nitrogen atom, G is an oxygen atom, a sulfur atom, a nitrogen atom or an NH group, Y1 is a hydrogen atom or a halogen atom, n is an integer of 1 to 4, and R1 is a group represented by any of the formulas (i) to (iv) defined in the specification.
摘要翻译：本发明提供具有抗精神病作用的式（I）的芳基哌啶衍生物或其药学上可接受的盐，其中D为碳原子或氮原子，E为CH基或氮原子，G为氧原子，硫原子，氮原子或NH基，Y 1为氢原子或卤素原子，n为1〜4的整数，R 1为由式（i）至（iv）。

3. 发明授权

US06407121B1 Arylpiperidine derivatives and use thereof 失效
标题翻译：芳基哌啶衍生物及其用途
公开(公告)号：US06407121B1
公开(公告)日：2002-06-18
申请号：US09646080
申请日：2000-09-13
申请人： Masashi Nagamine , Makoto Gotoh , Masanori Yoshida , Atsuro Nakazato , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa
发明人： Masashi Nagamine , Makoto Gotoh , Masanori Yoshida , Atsuro Nakazato , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa
IPC分类号： A61K31445
CPC分类号： C07D401/14 , C07D405/14 , C07D417/14
摘要： The present invention provides an arylpiperidine derivative of the formula (I) or a pharmaceutically acceptable salt thereof, which has antipsychotic effect: wherein D is a carbon atom or a nitrogen atom, E is a CH group or a nitrogen atom, G is an oxygen atom, a sulfur atom, a nitrogen atom or an NH group, Y1 is a hydrogen atom or a halogen atom, n is an integer of 1 to 4, and R1 is a group represented by any of the formulas (i) to (iv) defined in the specification.
摘要翻译：本发明提供具有抗精神病作用的式（I）的芳基哌啶衍生物或其药学上可接受的盐，其中D为碳原子或氮原子，E为CH基或氮原子，G为氧原子，硫原子，氮原子或NH基，Y1是氢原子或卤素原子，n是1〜4的整数，R1是由式（i）〜（iv）中的任一个表示的基团）。

4. 发明授权

US06329525B1 1,2-Dihydro-2-oxoquinoline derivatives 失效
标题翻译： 1,2-二氢-2-氧代喹啉衍生物
公开(公告)号：US06329525B1
公开(公告)日：2001-12-11
申请号：US09555568
申请日：2000-06-01
申请人： Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Makoto Gotoh , Masanori Yoshida
发明人： Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Makoto Gotoh , Masanori Yoshida
IPC分类号： C07D215227
CPC分类号： C07D401/06 , C07D215/54 , C07D241/44
摘要： A 1,2-dihydro-2-oxoquinoline derivative represented by the formula: wherein Ar is a pyridyl group or a group represented by the formula: (wherein X3 and X4 are the same or different, and are each a hydrogen atom, a halogen atom, a C1-5 alkyl group, a C1-5 alkoxy group, a hydroxyl group or a trifluoromethyl group), Y is a nitrogen atom, CH or C(OH), R1 and R2 are the same or different, and are each a hydrogen atom, a C1-10 alkyl group, a C3-15 alkoxyalkyl group or a C3-15 alkylaminoalkyl group, or R1 and R2 taken together with the nitrogen atom to which they are attached form a cyclic amino group, X1 and X2 are the same or different, and are each a hydrogen atom, a C1-5 alkyl group, a C1-5 alkoxy group or a halogen atom, or X1 and X2 taken together form an alkylenedioxy group, and n is an integer of 1 to 3; or a pharmaceutically acceptable salt thereof.
摘要翻译：由下式表示的1,2-二氢-2-氧代喹啉衍生物：其中Ar是吡啶基或由下式表示的基团：（其中X 3和X 4相同或不同，并且各自为氢原子，卤素原子，C 1-5烷基，C 1-5烷氧基，羟基或三氟甲基），Y是氮原子，CH或C（OH），R 1和R 2相同或不同，各自相同或不同氢原子，C 1-10烷基，C 3-15烷氧基烷基或C 3-15烷基氨基烷基，或者R 1和R 2与它们所连接的氮原子一起形成环状氨基，X 1和X 2是相同或不同，各自为氢原子，C1-5烷基，C1-5烷氧基或卤素原子，或X1和X2一起形成亚烷基二氧基，n为1〜3的整数 ; 或其药学上可接受的盐。

5. 发明授权

US06281355B1 Nitrogen-containing tetracyclic compounds 失效
标题翻译：含氮四环化合物
公开(公告)号：US06281355B1
公开(公告)日：2001-08-28
申请号：US09555570
申请日：2000-06-01
申请人： Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Makoto Gotoh , Kuniaki Kondoh , Masanori Yoshida
发明人： Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Makoto Gotoh , Kuniaki Kondoh , Masanori Yoshida
IPC分类号： A61K31403
CPC分类号： C07D471/04 , C07D495/04
摘要： A nitrogen-containing tetracyclic compound represented by the formula: wherein Y1—Y2—Y3 is N—C═N or a group represented by the formula: C═C—NR3 (wherein R3 is a hydrogen atom, a C1-5 alkyl group or a nitrogen-containing C2-10 alkyl group), Y4 is S, SO, SO2, CH2 or a group represented by the formula: NR4 (wherein R4 is a C1-5 alkanoyl group or a C1-5 alkyl group), R1 and R2 are the same or different, and are each a hydrogen atom, a C1-10 alkyl group, a C3-15 alkoxyalkyl group or a C3-15 alkylaminoalkyl group, or R1 and R2 taken together with the nitrogen atom to which they are attached form a cyclic amino group, X1 and X2 are the same or different, and are each a hydrogen atom, a C1-5 alkyl group, a C1-5 alkoxy group or a halogen atom, and n is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.
摘要翻译：一种由下式表示的含氮四环化合物：其中Y1-Y2-Y3为NC = N或由下式表示的基团：C = C-NR3（其中R3为氢原子，C1-5烷基或含氮的C2-10烷基），Y4是S，SO，SO2，CH2或由下式表示的基团：NR4（其中R4是C1-5烷酰基或C1-5烷基），R1和R2 各自为氢原子，C 1-10烷基，C 3-15烷氧基烷基或C 3-15烷基氨基烷基，或者R 1和R 2与它们所连接的氮原子一起形成环状氨基，X1和X2相同或不同，分别为氢原子，C1-5烷基，C1-5烷氧基或卤素原子，n为0,1或2; 或其药学上可接受的盐。

6. 发明授权

US06380384B1 1,2-dihydro-2-oxoquinoline derivatives 失效
标题翻译： 1,2-二氢-2-氧代喹啉衍生物
公开(公告)号：US06380384B1
公开(公告)日：2002-04-30
申请号：US09829203
申请日：2001-04-10
申请人： Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Makoto Gotoh , Masanori Yoshida
发明人： Atsuro Nakazato , Taketoshi Okubo , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Makoto Gotoh , Masanori Yoshida
IPC分类号： C07D40106
CPC分类号： C07D401/06 , C07D215/54 , C07D241/44
摘要： A 1,2-dihydro-2-oxoquinoline derivative represented by the formula: wherein Ar is a pyridyl group or a group represented by the formula: (wherein X3 and X4 are the same or different, and are each a hydrogen atom, a halogen atom, a C1-5 alkyl group, a C1-5 alkoxy group, a hydroxyl group or a trifluoromethyl group), Y is a nitrogen atom, CH or C(OH), R1 and R2 are the same or different, and are each a hydrogen atom, a C1-10 alkyl group, a C3-15 alkoxyalkyl group or a C3-15 alkylaminoalkyl group, or R1 and R2 taken together with the nitrogen atom to which they are attached form a cyclic amino group, X1 and X2 are the same or different, and are each a hydrogen atom, a C1-5 alkyl group, a C1-5 alkoxy group or a halogen atom; or X1 and X2 taken together form an alkylenedioxy group, and n is an integer of 1 to 3; or a pharmaceutically acceptable salt thereof.
摘要翻译：由下式表示的1,2-二氢-2-氧代喹啉衍生物：其中Ar是吡啶基或由下式表示的基团：（其中X 3和X 4相同或不同，并且各自为氢原子，卤素原子，C 1-5烷基，C 1-5烷氧基，羟基或三氟甲基），Y是氮原子，CH或C（OH），R 1和R 2相同或不同，各自相同或不同氢原子，C 1-10烷基，C 3-15烷氧基烷基或C 3-15烷基氨基烷基，或者R 1和R 2与它们所连接的氮原子一起形成环状氨基，X 1和X 2是相同或不同，并且各自为氢原子，C1-5烷基，C1-5烷氧基或卤素原子; 或者X1和X2一起形成亚烷基二氧基，n为1〜3的整数。或其药学上可接受的盐。

7. 发明授权

US06291467B1 Heteroaromatic derivatives 失效
标题翻译：杂芳族衍生物
公开(公告)号：US06291467B1
公开(公告)日：2001-09-18
申请号：US09646309
申请日：2000-09-15
申请人： Atsuro Nakazato , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Makoto Gotoh , Masanori Yoshida
发明人： Atsuro Nakazato , Toshihito Kumagai , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Makoto Gotoh , Masanori Yoshida
IPC分类号： C07D41706
CPC分类号： C07D231/12 , C07D401/06 , C07D417/06
摘要： An aromaheterocyclic derivative represented by the formula: wherein Z is a group represented by the following formula: wherein Ar1 is a phenyl group or a phenyl group substituted with a halogen atom or an alkyl group of 1 to 5 carbon atoms, R2 is an alkyl group of 1 to 5 carbon atoms, Y is a hydrogen atom, a mercapto group, an alkylthio group of 1 to 5 carbon atoms, an amino group or an amino group substituted with one or two alkyl groups having 1 to 5 carbon atoms, Ar2 is a phenyl group of one or two substituents selected from the group consisting of a halogen atom, an alkyl group of 1 to 5 carbon atoms, an alkoxy group of 1 to 5 carbon atoms, a hydroxyl group and a trifluoromethyl group, or a phenyl group, B1-B2 is CH—CO or C═C(R1) (wherein R1 is a hydrogen atom or an alkyl group of 1 to 5 carbon atoms), and n is an integer of 1 to 4, or a pharmaceutically acceptable salt thereof, which is a dopamine D4 receptor antagonist compound having an antipsychotic action without causing extrapyramidal diseases.
摘要翻译：由下式表示的芳族杂环衍生物：其中Z为下式表示的基团：其中Ar1为苯基或被卤素原子或1〜5个碳原子的烷基取代的苯基，R2为烷基 1〜5个碳原子，Y为氢原子，巯基，1〜5个碳原子的烷硫基，氨基或被一个或两个碳原子数为1〜5的烷基取代的氨基，Ar2为选自卤素原子，1〜5个碳原子的烷基，1〜5个碳原子的烷氧基，羟基和三氟甲基，或苯基中的一个或两个取代基的苯基，B1-B2为CH-CO或C = C（R1）（其中R1为氢原子或1〜5个碳原子的烷基），n为1〜4的整数，或其药学上可接受的盐，其是具有抗精神病作用而不引起外敷的多巴胺D4受体拮抗剂化合物痉挛性疾病

8. 发明授权

US06476056B2 Heterocycle substituted aryloxyaniline derivatives and their use as MDR ligands 失效
标题翻译：杂环取代的芳氧基苯胺衍生物及其作为MDR配体的用途
公开(公告)号：US06476056B2
公开(公告)日：2002-11-05
申请号：US09922807
申请日：2001-08-07
申请人： Atsuro Nakazato , Taketoshi Okubo , Toshio Nakamura , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Kenji Yamamoto , Koichiro Harada , Masanori Yoshida
发明人： Atsuro Nakazato , Taketoshi Okubo , Toshio Nakamura , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Kenji Yamamoto , Koichiro Harada , Masanori Yoshida
IPC分类号： A61K3144
CPC分类号： C07D213/40 , C07C233/25 , C07C233/33 , C07C233/54 , C07C235/38 , C07C235/78 , C07C237/30 , C07C247/10 , C07C275/32 , C07C311/27 , C07C311/29 , C07C311/46 , C07C323/20 , C07C323/41 , C07C323/60 , C07D213/643 , C07D213/65 , C07D213/68
摘要： An aryloxyaniline derivative represented by the formula: wherein Ar1 and Ar2 are the same or different, and are each a substituted or unsubstituted phenyl group, a substituted or unsubstituted pyridyl group or a naphthyl group, provided that Ar1 and Ar2 are not both phenyl or both naphthyl and are not phenyl and naphthyl, R1 is a hydrogen atom, a substituted or unsubstituted alkyl group having 1 to 10 carbon atoms, an alkoxy group having 1 to 10 carbon atoms, a substituted or unsubstituted phenyl group or a group of the formula: —NR2(R3) (wherein R2 and R3 are the same or different, and are each a hydrogen atom or an alkyl group having 1 to 10 carbon atoms, X1 is a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, a phenoxy group, a halogen atom, a trifluoromethyl group, a carbamoyl group or an aminosulfonyl group, Y1 is a branched or unbranched alkylene group having 1 to 6 carbon atoms or a single bond; and pharmaceutically acceptable salts thereof.
摘要翻译：由下式表示的芳氧基苯胺衍生物：其中Ar1和Ar2相同或不同，并且各自为取代或未取代的苯基，取代或未取代的吡啶基或萘基，条件是Ar 1和Ar 2不同时为苯基或两者萘基，不是苯基和萘基，R1是氢原子，取代或未取代的碳原子数1〜10的烷基，碳原子数1〜10的烷氧基，取代或未取代的苯基或下式的基团： -NR2（R3）（其中R2和R3相同或不同，并且各自为氢原子或具有1-10个碳原子的烷基，X 1为氢原子，具有1至5个碳原子的烷基，具有1至5个碳原子的烷氧基，苯氧基，卤素原子，三氟甲基，氨基甲酰基或氨基磺酰基，Y1是具有1至6个碳原子或单键的支链或非支链亚烷基; 可以接受的盐。

9. 发明授权

US06333358B1 Aryloxyaniline derivatives 失效
标题翻译：芳氧基苯胺衍生物
公开(公告)号：US06333358B1
公开(公告)日：2001-12-25
申请号：US09485006
申请日：2000-02-01
申请人： Atsuro Nakazato , Taketoshi Okubo , Toshio Nakamura , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Kenji Yamamoto , Koichiro Harada , Masanori Yoshida
发明人： Atsuro Nakazato , Taketoshi Okubo , Toshio Nakamura , Shigeyuki Chaki , Kazuyuki Tomisawa , Masashi Nagamine , Kenji Yamamoto , Koichiro Harada , Masanori Yoshida
IPC分类号： A61K31135
CPC分类号： C07D213/40 , C07C233/25 , C07C233/33 , C07C233/54 , C07C235/38 , C07C235/78 , C07C237/30 , C07C247/10 , C07C275/32 , C07C311/27 , C07C311/29 , C07C311/46 , C07C323/20 , C07C323/41 , C07C323/60 , C07D213/643 , C07D213/65 , C07D213/68
摘要： An aryloxyaniline derivative represented by the formula: wherein Ar1 and Ar2 are each a substituted or unsubstituted phenyl group, pyridyl group or naphthyl group, R1 is a hydrogen atom, an alkyl group, etc., X1 is a hydrogen atom, an alkyl group, etc., y1 is a branched or unbranched alkylene group having 1 to 6 carbon atoms or a single bond; or a pharmaceutically acceptable salt thereof can provide medicines having a high affinity for MDR, and therefore, exhibiting a therapeutic or preventive effect on anxiety, related diseases thereto, depression, etc.
摘要翻译：由下式表示的芳氧基苯胺衍生物：其中Ar1和Ar2各自为取代或未取代的苯基，吡啶基或萘基，R1为氢原子，烷基等，X1为氢原子，烷基， y1是具有1〜6个碳原子或单键的支链或非支链亚烷基; 或其药学上可接受的盐可以提供对MDR具有高亲和力的药物，因此对焦虑，其相关疾病，抑郁等具有治疗或预防作用。

10. 再颁专利

USRE36832E N-heteroaryl-N'-phenylurea derivatives, their production and use 失效
标题翻译： N-杂芳基-N'-苯基脲衍生物，其制备和用途
公开(公告)号：USRE36832E
公开(公告)日：2000-08-22
申请号：US100241
申请日：1998-06-19
申请人： Masashi Nagamine , Kenji Yamamoto , Yoshimitsu Matsui , Kenji Horiuchi , Masanori Yoshida
发明人： Masashi Nagamine , Kenji Yamamoto , Yoshimitsu Matsui , Kenji Horiuchi , Masanori Yoshida
IPC分类号： A61K31/34 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61P3/06 , A61P9/10 , A61P43/00 , C07D209/40 , C07D307/77 , C07D307/82 , C07D307/92 , C07D307/935 , C07D333/66 , C07D333/74 , C07D333/78 , C12N9/99
CPC分类号： C07D307/82 , C07D209/40 , C07D307/92 , C07D333/66 , C07D333/74 , C07D333/78
摘要： An N-heteroaryl-N'-phenylurea derivative represented by the general formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined in the description of the specification which is useful as a prophylactic and therapeutic agent for hypercholesterolemia, atherosclerosis and diseases caused by them.
摘要翻译：由通式（I）表示的N-杂芳基-N'-苯基脲衍生物：其中R1，R2，R3，R4，R5，R6和R7如说明书的描述中所定义，其可用作预防和治疗高胆固醇血症药物，动脉粥样硬化及其引起的疾病。

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