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公开(公告)号:US5484588A
公开(公告)日:1996-01-16
申请号:US965289
申请日:1993-02-02
申请人: Kazumasa Ogino , Haruo Shimamura , Kazuyuki Tomisawa , Fumio Urushizaki , Masami Nemoto , Tuguchika Yoshida
发明人: Kazumasa Ogino , Haruo Shimamura , Kazuyuki Tomisawa , Fumio Urushizaki , Masami Nemoto , Tuguchika Yoshida
CPC分类号: A01N33/04 , A01N25/006 , A01N33/06
摘要: There are provided attracting and ingestion-stimulating agents for cockroach comprising as the active ingredient one or more compounds represented by the formula ##STR1## wherein R represents an amino group or an aminomethyl group. The attracting and ingestion-stimulating agents for cockroach exhibit a very potent attracting and ingestion-stimulating activity in the known species of house cockroach, both male and female.
摘要翻译: PCT No.PCT / JP91 / 01059 Sec。 371日期:1993年2月2日 102(e)日期1993年2月2日PCT 1991年8月8日PCT PCT。 公开号WO92 / 02134 日本1992年2月20日。提供用于蟑螂的吸引和摄取刺激剂,其包含作为活性成分的一种或多种由式“IMAGE”表示的化合物,其中R表示氨基或氨基甲基。 蟑螂的吸引和摄入刺激剂在已知的男性和女性的蟑螂种类中都表现出非常强烈的吸引和摄入刺激活性。
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公开(公告)号:US06894168B2
公开(公告)日:2005-05-17
申请号:US10347288
申请日:2003-01-21
IPC分类号: A61K31/519 , A61P1/00 , A61P7/10 , A61P9/10 , A61P9/12 , A61P17/02 , A61P25/08 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P29/00 , A61P37/02 , A61P43/00 , C07D473/00 , C07D487/04 , C07D211/78
CPC分类号: A61K31/519 , C07D473/00 , C07D487/04
摘要: Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C5 alkyl group, or the like; Y1—Y2 represents (R4)C═C(R5), (R6)C═N, N═N, (R7) N—CO, or N═C(R8); X1, X2, and X3 are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R3, R4, R5, and R6 are identical or different, and each represents a hydrogen atom or an alkyl group; R7 represents a hydrogen atom, a C1-C5 alkyl group, or the like; and R8 represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided. The derivatives described above are effective for diseases which are believed to involve CRF.
摘要翻译: 由下式表示的氨基甲酰基四氢吡啶衍生物:[式中,R 1,R 2和R 2'相同或不同,各自表示氢原子,C 1 C 5 -C 15烷基等; Y 1 - (CH 2)2(R 4 S)(R 5),(R 6) CN,NN,(R 7)N-CO或NC(R 8); X 1,X 2和X 3相同或不同,各自表示氢原子,卤素原子等; R 3,R 4,R 5和R 6相同或不同,并且各自表示氢 原子或烷基; R 7表示氢原子,C 1 -C 5烷基等; 和R 8表示氢原子或氨基甲酰基]或其药学上可接受的盐,以及其制备中间体。 上述衍生物对于被认为涉及CRF的疾病是有效的。
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公开(公告)号:US6162832A
公开(公告)日:2000-12-19
申请号:US529218
申请日:2000-04-10
申请人: Tomomi Ota , Misa Nakanishi , Izumi Aibe , Minoru Taguchi , Kazuyuki Tomisawa
发明人: Tomomi Ota , Misa Nakanishi , Izumi Aibe , Minoru Taguchi , Kazuyuki Tomisawa
IPC分类号: C07C217/90 , A61K31/135
CPC分类号: C07C217/90
摘要: A 2-phenoxyaniline derivative represented by the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or a lower alkoxy group, R.sup.2 is a halogen atom or a nitro group, and R.sup.3 is a hydrogen atom or a halogen atom, or a pharmaceutically acceptable salt thereof.
摘要翻译: PCT No.PCT / JP98 / 04729 Sec。 371日期2000年04月10日 102(e)日期2000年4月10日PCT提交1998年10月20日PCT公布。 公开号WO99 / 20598 日期1999年4月29日由下式表示的2-苯氧基苯胺衍生物:其中R1是氢原子或低级烷氧基,R2是卤素原子或硝基,R3是氢原子或卤原子,或 其药学上可接受的盐。
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公开(公告)号:US06600038B1
公开(公告)日:2003-07-29
申请号:US09914534
申请日:2001-08-30
IPC分类号: C07D47334
CPC分类号: A61K31/519 , C07D473/00 , C07D487/04
摘要: Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C5 alkyl group, or the like; Y1-Y2 represents (R4)C═C(R5), (R6)C═N, N═N, (R7)N—CO, or N═C(R8); X1, X2, and X3 are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R3, R4, R5, and R6 are identical or different, and each represents a hydrogen atom or an alkyl group; R7 represents a hydrogen atom, a C1-C5 alkyl group, or the like; and R8 represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided. The derivatives described above are effective for diseases which are believed to involve CRF.
摘要翻译: 由下式表示的氨基甲酰基四氢吡啶衍生物:[式中,R 1和R 2相同或不同,各自表示氢原子,C 1 -C 5烷基等; Y1-Y2表示(R4)C = C(R5),(R6)C = N,N = N,(R7)N-CO或N = C(R8) X1,X2和X3相同或不同,各自表示氢原子,卤素原子等; R3,R4,R5和R6相同或不同,各自表示氢原子或烷基; R7表示氢原子,C1-C5烷基等; 并且R8表示氢原子或氨基甲酰基]或其药学上可接受的盐,并且提供其制备的中间体。上述衍生物对于被认为涉及CRF的疾病是有效的。
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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。
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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。
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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
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公开(公告)号:US07279584B2
公开(公告)日:2007-10-09
申请号:US10568708
申请日:2004-08-18
IPC分类号: C07D207/16
CPC分类号: C07D207/16 , Y02P20/55
摘要: The present invention provides a safer method for production of a cis-4-fluoro-L-proline derivative under milder conditions and in good yield to give a product of high purity on an industrial scale at low cost. Namely, the present invention provides a method for producing a cis-4-fluoro-L-proline derivative, which comprises reacting a trans-4-hydroxy-L-proline derivative of the following Formula [I]: (wherein R1 represents a protecting group for an α-amino group, and R2 represents a protecting group for a carboxyl group) with N,N-diethyl-N-(1,1,2,3,3,3-hexafluoropropyl)amine in the presence of a hydrogen fluoride-scavenger.
摘要翻译: 本发明提供了一种在更温和的条件下生产顺式-4-氟-L-脯氨酸衍生物的更安全的方法,并以良好的产率,以低成本在工业规模上得到高纯度的产物。 即,本发明提供顺式-4-氟-L-脯氨酸衍生物的制造方法,该方法包括使下式[I]的反式-4-羟基-L-脯氨酸衍生物:其中R < 1代表α-氨基的保护基,R 2代表羧基的保护基)与N,N-二乙基-N-(1,1,2 ,3,3,3-六氟丙基)胺在氟化氢 - 清除剂的存在下反应。
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公开(公告)号:US20060281927A1
公开(公告)日:2006-12-14
申请号:US10568708
申请日:2004-08-18
IPC分类号: C07D207/02
CPC分类号: C07D207/16 , Y02P20/55
摘要: The present invention provides a safer method for production of a cis-4-fluoro-L-proline derivative under milder conditions and in good yield to give a product of high purity on an industrial scale at low cost. Namely, the present invention provides a method for producing a cis-4-fluoro-L-proline derivative, which comprises reacting a trans-4-hydroxy-L-proline derivative of the following Formula [I]: (wherein R1 represents a protecting group for an α-amino group, and R2 represents a protecting group for a carboxyl group) with N,N-diethyl-N-(1,1,2,3,3,3-hexafluoropropyl)amine in the presence of a hydrogen fluoride-scavenger.
摘要翻译: 本发明提供了一种在更温和的条件下生产顺式-4-氟-L-脯氨酸衍生物的更安全的方法,并以良好的产率,以低成本在工业规模上得到高纯度的产物。 即,本发明提供顺式-4-氟-L-脯氨酸衍生物的制造方法,该方法包括使下式[I]的反式-4-羟基-L-脯氨酸衍生物:其中R < 1代表α-氨基的保护基,R 2代表羧基的保护基)与N,N-二乙基-N-(1,1,2 ,3,3,3-六氟丙基)胺在氟化氢 - 清除剂的存在下反应。
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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)。
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