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1. 发明申请

WO2008133344A3 PIPERIDINE DERIVATIVE AND USE THEREOF 审中-公开
标题翻译：哌啶衍生物及其用途
公开(公告)号：WO2008133344A3
公开(公告)日：2009-11-12
申请号：PCT/JP2008058304
申请日：2008-04-23
申请人： TAKEDA PHARMACEUTICAL , SHIRAI JUNYA , MORIMOTO SHINJI , SUGIYAMA HIDEYUKI , SAKAUCHI NOBUKI , YOSHIKAWA TAKESHI
发明人： SHIRAI JUNYA , MORIMOTO SHINJI , SUGIYAMA HIDEYUKI , SAKAUCHI NOBUKI , YOSHIKAWA TAKESHI
IPC分类号： C07D211/60 , A61K31/451 , A61P1/00 , A61P13/02 , A61P25/00 , C07D401/06 , C07D405/06 , C07D409/04 , C07D409/14 , C07D413/06 , C07D417/06
CPC分类号： C07D211/60 , C07D401/06 , C07D405/06 , C07D409/04 , C07D409/14 , C07D413/06 , C07D417/06
摘要： The present invention provides a novel piperidine derivative and a tachykinin receptor antagonist containing same, as well as a compound represented by the formula (I) wherein R1 is carbamoylmethyl, methylsulfonylethylcarbonyl and the like; R2 is methyl or cyclopropyl; R3 is a hydrogen atom or methyl; R4 is a chlorine atom or trifluoromethyl; R5 is a chlorine atom or trifluoromethyl; and a group represented by the formula (II) is a group represented by the formula (III) wherein R6 is a hydrogen atom, methyl, ethyl or isopropyl; R7 is a hydrogen atom, methyl or a chlorine atom; and R8 is a hydrogen atom, a fluorine atom, a chlorine atom or methyl; or 3-methylthiophen-2-yl, and a salt thereof.
摘要翻译：本发明提供了一种新颖的哌啶衍生物和含有它的速激肽受体拮抗剂，以及由式（I）表示的化合物，其中R 1是氨甲酰基甲基，甲基磺酰基乙基羰基等; R2是甲基或环丙基; R3是氢原子或甲基; R4是氯原子或三氟甲基; R5是氯原子或三氟甲基; 由式（II）表示的基团是由式（III）表示的基团，其中R 6是氢原子，甲基，乙基或异丙基; R7是氢原子，甲基或氯原子; R8为氢原子，氟原子，氯原子或甲基; 或3-甲基噻吩-2-基及其盐。

2. 发明申请

WO02092606A8 FUSED IMIDAZOLIDINE DERIVATIVES, PROCESS FOR PREPARATION OF THE SAME AND USE THEREOF 审中-公开
标题翻译：稠合咪唑啉衍生物，其制备方法及其用途
公开(公告)号：WO02092606A8
公开(公告)日：2002-12-19
申请号：PCT/JP0204640
申请日：2002-05-14
申请人： TAKEDA CHEMICAL INDUSTRIES LTD , FUNABASHI YASUNORI , TAKIZAWA MASAYUKI , MORIMOTO SHINJI , NOTOYA KOHEI
发明人： FUNABASHI YASUNORI , TAKIZAWA MASAYUKI , MORIMOTO SHINJI , NOTOYA KOHEI
IPC分类号： A61K31/542 , A61K31/554 , A61P19/02 , A61P19/08 , A61P43/00 , C07D513/04 , C07F9/6561
CPC分类号： C07D513/04 , A61K31/542 , A61K31/554 , C07F9/6561
摘要： Compounds represented by the general formula (I) and having excellent inhibitory activity against the degradation of cartilage matrix; or salts or sulfoxides of the same: (I) wherein R 1 is −(S) n −R 2 (wherein R 2 is optionally substituted hydrocarbyl or the like; and n is an integer of 0 to 2) or the like; R 5 is hydrogen, optionally substituted hydrocarbyl, or the like; symbol (II) is a group represented by the general formula (III) or the like; and symbol (IV) is a group represented by the general formula (V) or the like: (II) (III) (IV) (V) [wherein R 6 is hydrogen, optionally substituted hydrocarbyl, or the like; R 10 is −ZR 15 (wherein Z is −SO 2 − or the like; and R 15 is optionally substituted hydrocarbyl or the like) or the like; and R 11 is hydrogen or the like].
摘要翻译：通式（I）表示的化合物对软骨基质的降解具有优异的抑制活性; 或其盐或亚砜：（I）其中R 1是 - （S）n -R 2 SP 2（其中R 1， 2是任选取代的烃基等;并且n是0至2的整数）等; R 5是氢，任选取代的烃基等; 符号（II）是由通式（III）等表示的基团; 和符号（IV）为由通式（V）等表示的基团：（II）（III）（IV）（V）[其中R 6是氢，任选取代的烃基，或类似物; R 10是-ZR 15（其中Z是-SO 2 - 等）;和R 15是任选取代的烃基等）等; 并且R 11是氢或类似物]。

3. 发明专利

AR066267A1 DERIVADOS DE PIPERIDINA COMO ANTAGONISTAS DEL RECEPTOR DE TAQUIQUININA 未知
公开(公告)号：AR066267A1
公开(公告)日：2009-08-05
申请号：ARP080101711
申请日：2008-04-23
申请人： TAKEDA PHARMACEUTICAL
发明人： SHIRAI JUNYA , MORIMOTO SHINJI , YOSHIKAWA TAKESHI , SAKAUCHI NOBUKI , SUGIYAMA HIDEYUKI
IPC分类号： C07D211/62 , C07D401/04 , C07D401/16 , C07D405/04 , C07D405/06 , C07D409/04 , C07D49/14 , C07D413/04 , C07D413/06 , C07D417/06 , A61K31/451 , A61K31/4523 , A61K31/453 , A61K31/4535 , A61K31/454 , A61P1/00 , A61P13/00 , A61P25/00
摘要： Reivindicacion 1: Un compuesto caracterizado por la formula: 1 donde es: (1) carbamoilmetilo, (2) metilsulfoniletilcarbonilo, (3) aminosulfonilpropilcarbonilo, (4) fenilsulfoniletilcarbonilo, (5) piridin-2-ilcarbonilo, (6) 5-metoxicarbonilpiridin-2-ilcarbonilo, (7) 5-hidroxipiridin-2-ilcarbonilo, (8) 6-hidroxipiridin-2-ilcarbonilo, (9) 5-bromopiridin-2-ilcarbonilo, (10) 6-metilpiridin-2-ilcarbonilo, (11) 5-carbamoilpiridin-2-ilcarbonilo, (12) 2-aminopiridin-5-ilcarbonilo, (13) 2-acetilaminopiridin-5-ilcarbonilo, (14) piridin-3-ilcarbonilo, (15) pirazin-2-ilcarbonilo, (16) pirimidin-5-ilcarbonilo, (17) 2-aminopirimidin-5-ilcarbonilo, (18) 2-acetilaminopirimidin-5-ilcarbonilo, (19) 2-metoxicarbonilaminopirimidin-5-ilcarbonilo, (20) azetidin-3-ilcarbonilo, (21) 1-ter-butoxicarbonilazetidin-3-ilcarbonilo, (22) 1-(1-hidroxi-1-metiletilcarbonil)azetidin-3-ilcarbonilo, (23) 1-hidroximetilcarbonilazetidin-3-ilcarbonilo, (24) adamantan-1-ilcarbonilo, (25) 1-carbamoil-1-metiletilcarbonilo, (26) dimetilaminometilcarbonilo, (27)1,2,3,4-tetrahidropirimidin2,4-dion-1-ilmetilcarbonilo, (28)2,3,5,6-tetrahidropirimidin2, 6-dion-4-ilmetilcarbonilo, (29) 1-hidroximetilcarbonilpiperidin-4-ilcarbonilo, (30) 1-etoxicarbonilpiperidin-4-ilcarbonilo, (31) 1-isopropoxicarbonilpiperidin-4-ilcarbonilo, (32) 1-ciclopropilsulfonilpiperidin-4-ilcarbonilo, (33) 1-(1-hidroxietilcarbonil)piperidin-4-ilcarbonilo, (34) 5,5-dimetiloxazolidin2,4-dion-3-ilmetilcarbonilo,(35) 5,5-dimetiloxazolidin2,4-dion-3-iletilcarbonilo, (36) oxazolidin2,4-dion-3-ilmetilcarbonilo, (37)1-(2-hidroxi-2-metilpropilcarbonil)piperidin-4-ilcarbonilo, (38) 3-metilimidazolidin4,4-dimetil-2,5-dion-1-ilmetilcarbonilo, (39) 4,4-dimetilpiperidin2,6-dion-1-ilmetilcarbonilo, (40) morfolin-2,6-dion-1-ilmetilcarbonilo, (41) imidazol-2-ilcarbonilo, (42) imidazol-4-ilcarbonilo, (43) 5,5-dimetiloxazolidin2,4-dion-3-iletilo, (44) 5,5-dimetiloxazolidin2,4-dion-3-ilpropilo, (45) 6-cloropiridazin-3-ilo, (46) 6-acetilaminopiridazin-3-ilo, (47) 5-metil-1,3,4-tiadiazol-2-ilo, (48) 5-acetilaminopiridin-2-ilo, (49) 4-nitrotiazol-2-ilo, (50) 2,2,2-tricloroetoxicarbonilo, (51) etilsulfonilo, (52) ciclopropilsulfonilo, (53)isobutilsulfonilo, (54) 1-benciloxicarbonilpiperidin-4-ilsulfonilo, (55) 1-hidroximetilcarbonilpiperidin-4-ilsulfonilo, (56) etoxietilsulfonilo, (57) hidroxietilsulfonilo, (58) morfolin-1-iletilsulfonilo, (59) 5,5-dimetiloxazolidin2,4-dion-3-iletilsulfonilo, (60) indol-6-ilcarbonilo, (61) bencimidazol-6-ilcarbonilo, (62) benzotiazol-2-ilcarbonilo, (63) tiazol-2-ilcarbonilo, (64) ciclopropilaminocarbonilmetilo, (65) 4-hidroxipiperidin-1-ilcarbonilmetilo, (66) 1-ter-butoxicarbonilpiperidin-4-ilo, (67) piperidin-4-ilo, (68) 1-isopropoxicarbonilpiperidin-4-ilo, (69) 1-aminocarbonilcarbonilpiperidin-4-ilo, (70) 1-carbamoilpiperidin-4-ilo, (71) 1-hidroximetilcarbonilpiperidin-4-ilo, (72) 1-(1-hidroxi-1-metiletilcarbonil)piperidin-4-ilo, (73) 1-carbamoil-1-metiletilo, (74) 1-acetilpiperidin-4-ilmetilo, (75) 4-carbamoilpiperidin-1-ilcarbonilmetilo, (76) 3-oxopiperazin-1-ilcarbonilmetilo, (77) metoxicarboniletilo, (78) carbamoiletilo, (79)ciclopenten-3-on-1-ilo, (80) 4,4-dimetilciclohexen-3-on-1-ilo, (81) 2-hidroxi-1-metiletilo, (82) 1-carbamoiletilo, (83) 2-metilsulfonil-1-metiletilo, (84) 3-hidroxi-3-metilbutilo, (85) 4-acetilaminobenzoílo, (86) 4-cianobenzoílo, (87) 4-carbamoilbenzoílo, (88) 10-canfosulfonilo, (89) 6-cloropiridazin-3-ilo, (90) piridin-2-ilo, (91)1-(1-hidroxi-1-metiletilcarbonil)piperidin-4-ilcarbonilo, (92) 1-metoximetilcarbonilpiperidin-4-ilcarbonilo, (93) 1-aminocarbonilpiperidin-4-ilcarbonilo(94) 1-aminocarbonilcarbonilpiperidin-4-ilcarbonilo (95) 1-isopropilpiperidin-4-ilcarbonilo, (96)1-(1-hidroxiciclopropilcarbonil)piperidin-4-ilcarbonilo, (97) tetrazol-5-ilmetilcarbonilo, (98) 1-(tetrazol-1-ilmetilcarbonil)piperidin-4-ilcarbonilo,(99)1-(acetilaminometilcarbonil)piperidin-4-ilcarbonilo, (100) 2-hidroxietilcarbonilo, (101) tiomorfolin-1,1-dioxido-4-ilmetilcarbonilo, (102) dimetilaminosulfonilo, (103) 4-acetilaminofenilsulfonilo, (104) piridin-2-ilsulfonilo, (105) piridin-3-ilsulfonilo, (106) 6-cloropiridin-3-ilsulfonilo, (107) 6-(morfolin-1-il)piridin-3-ilsulfonilo, (108) piperidin-3-ilcarbonilo (109) 1-ter-butoxicarbonilpiperidin-3-ilcarbonilo (110) 1-metoxicarbonilpiperidin-3-ilcarbonilo, (111) 1-acetilpiperidin-3-ilcarbonilo, (112) 1-hidroximetilcarbonilpiperidin-3-ilcarbonilo, (113) 1-(1-hidroxi-1-metiletilcarbonil) piperidin-3-ilcarbonilo, (114) 1-metilsulfonilmetilcarbonilpiperidin-3-ilcarbonilo, (115) 1-metilsulfonilpiperidin-3-ilcarbonilo, (116) 1-aminocarbonilcarbonilpiperidin-3-ilcarbonilo, (117) 4-hidroximetilcarbonilaminociclohexan-1-ilcarbonilo, (118) 4-metoximetilcarbonilaminociclohexan-1-ilcarbonilo, (119) 4-aminocarbonilaminociclohexan-1-ilcarbonilo, (120) 4-aminocarbonilcarbonilaminociclohexan-1-ilcarbonilo, (121) 4-metilsulfonilaminociclohexan-1-ilcarbonilo, (122) tetrahidrofuran-3-ilcarbonilo, (123) tiazolidin-2-on-4-ilcarbonilo, (124) 1-ter-butoxicarbonilpirrolidin-3-ilcarbonilo, (125) 1-metoxicarbonilpirrolidin-3-ilcarbonilo o (126) 1-hidroximetilcarbonilpirrolidin-3-ilcarbonilo; R2 es metilo o ciclopropilo; R3 es un átomo de hidrogeno o metilo; R4 es un átomo de cloro o trifluorometilo; R5 es un átomo de cloro o trifluorometilo; yun grupo representado por la formula 2 es un grupo representado por la formula 3 donde R6 es un átomo de hidrogeno, metilo, etilo o isopropilo; R7 es un átomo de hidrogeno, metilo o átomo de cloro; y R8 es un átomo de hidrogeno, un átomo de fluor,un átomo de cloro o metilo; o 3-metiltiofen-2-ilo; o una sal del mismo.

4. 发明专利

CA2887598A1 CYCLOPROPANAMINE COMPOUND AND USE THEREOF 未知
公开(公告)号：CA2887598A1
公开(公告)日：2014-04-17
申请号：CA2887598
申请日：2013-10-11
申请人： TAKEDA PHARMACEUTICAL
发明人： TOMITA NAOKI , TOMITA DAISUKE , TOMINARI YUSUKE , IMAMURA SHINICHI , MORIMOTO SHINJI , KOJIMA TAKUTO , TOYOFUKU MASASHI , HATTORI YASUSHI , KAKU TOMOHIRO , ITO MITSUHIRO
IPC分类号： C07C237/40 , A61K31/166 , A61K31/167 , A61K31/415 , A61K31/4453 , A61P25/14 , A61P25/16 , A61P25/28 , A61P43/00 , C07C237/30 , C07C237/38 , C07D231/40 , C07D295/18 , C12N9/99 , C12N15/09
摘要： The present invention provides a compound that: has a lysine-specific demethylase-1-inhibiting effect; and provides utility as a drug for preventing or treating schizophrenia, Alzheimer's disease, Parkinson's disease, and Huntington chorea. The present invention pertains to a compound expressed by formula (1) or salt thereof (where (A) represents a hydrocarbon group optionally having a substitution group or a heterocyclic group optionally having a substitution group; (B) represents a benzene ring optionally having a substitution group; (R1), (R2), and (R3) independently represent a hydrogen, a hydrocarbon group optionally having a substitution group, or a heterocyclic ring group optionally having a substitution group; (A) and (R1) can be bonded together to form, with an adjacent nitrogen atom, a cyclic group optionally having a substitution group; and (R2) and (R3) can be bonded together to form, with an adjacent hydrogen atom, a cyclic group optionally having a substitution group).

5. 发明专利

PE20090277A1 DERIVADOS DE PIPERIDINA COMO ANTAGONISTAS DE TAQUIQUININAS 未知
公开(公告)号：PE20090277A1
公开(公告)日：2009-04-06
申请号：PE2008000700
申请日：2008-04-23
申请人： TAKEDA PHARMACEUTICAL
发明人： SHIRAI JUNYA , MORIMOTO SHINJI , SUGIYAMA HIDEYUKI , SAKAUCHI NOBUKI , YOSHIKAWA TAKESHI
IPC分类号： A61K31/445 , A61K31/4523 , A61K31/4545 , A61P1/00 , A61P13/00 , C07D401/00 , C07D401/04
摘要： REFERIDA A UN COMPUESTO DERIVADO DE PIPERIDINA DE FORMULA (I), DONDE R1 ES CARBAMOILMETILO, METILSULFONILETILCARBONILO, AMINOSULFONILPROPILCARBONILO, ENTRE OTROS; R2 ES METILO O CICLOPROPILO; R3 ES H O METILO; R4 Y R5 SON Cl O TRIFLUOROMETILO; EL GRUPO A ES UN FENILO SUSTITUIDO CON R6, R7 Y R8; R6 ES H, METILO, ETILO O ISOPROPILO; R7 ES H, METILO O Cl; R8 ES F, CL, 3-METILTIOFEN-2-ILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (3S,4S)-N-[3,5-BIS(TRIFLUOROMETIL)BENCIL]-1-{[1-(HIDROXIACETIL)PIPERIDIN-4-IL]CARBONIL}-N-METIL-3-(2-METILFENIL)PIPERIDIN-4-CARBOXAMIDA, (3R*,4R*)-N-[3,5-BIS(TRIFLUOROMETIL)BENCIL]-1-[2-(CICLOPROPILAMINO)-2-OXOETIL]-3-(4-FLUORO-2-METILFENIL)-N-METILPIPERIDIN-4-CARBOXAMIDA, (3S,4S)-N-[3,5-BIS(TRIFLUOROMETIL)BENCIL]-1-[(5,5-DIMETIL-2,4-DIOXO-1,3-OXAZOLIDIN-3-IL)ACETIL]-3-(4-FLUORO-2-METILFENIL)-N-METILPIPERIDIN-4-CARBOXAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS TIENEN ACTIVIDAD ANTAGONISTA DEL RECEPTOR DE TAQUIQUININA, PARTICULARMENTE, SOBRE EL RECEPTOR DE LA SUSTANCIA P, Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES GASTROINTESTINALES, DEL TRACTO URINARIO INFERIOR, ENFERMEDAD NEUROLOGICA CENTRAL, ENTRE OTRAS

6. 发明公开

EP2907802A4 CYCLOPROPANAMINE COMPOUND AND USE THEREOF 有权
标题翻译：环丙烷AMIN连接及其用途
公开(公告)号：EP2907802A4
公开(公告)日：2016-04-20
申请号：EP13845823
申请日：2013-10-11
申请人： TAKEDA PHARMACEUTICAL
发明人： TOMITA NAOKI , TOMITA DAISUKE , TOMINARI YUSUKE , IMAMURA SHINICHI , MORIMOTO SHINJI , KOJIMA TAKUTO , TOYOFUKU MASASHI , HATTORI YASUSHI , KAKU TOMOHIRO , ITO MITSUHIRO
IPC分类号： C07C237/40 , A61K31/166 , A61K31/167 , A61K31/415 , A61K31/4453 , A61P25/14 , A61P25/16 , A61P25/28 , A61P43/00 , C07C237/30 , C07C237/38 , C07D231/40 , C07D295/18 , C12N9/99 , C12N15/09
CPC分类号： C07D487/04 , A61K45/06 , C07C237/30 , C07C237/38 , C07C237/40 , C07C255/29 , C07C255/58 , C07C255/60 , C07C317/40 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/12 , C07D207/46 , C07D211/58 , C07D213/36 , C07D213/40 , C07D223/12 , C07D231/38 , C07D231/40 , C07D241/12 , C07D241/18 , C07D261/14 , C07D265/36 , C07D277/38 , C07D285/135 , C07D295/135 , C07D309/14 , C07D319/18 , C07D333/20 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D513/04
摘要： The present invention provides a compound having a lysine specific demethylase 1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for schizophrenia, Alzheimer's disease, Parkinson's disease or Huntington's disease, and the like. The present invention relates to a compound represented by the formula wherein A is a hydrocarbon group optionally having substituent(s), or a heterocyclic group optionally having substituent(s); B is a benzene ring optionally having further substituent(s); R 1 , R 2 and R 3 are each independently a hydrogen atom, a hydrocarbon group optionally having substituent(s), or a heterocyclic group optionally having substituent(s); A and R 1 are optionally bonded to each other to form, together with the adjacent nitrogen atom, a cyclic group optionally having substituent(s); and R 2 and R 3 are optionally bonded to each other to form, together with the adjacent nitrogen atom, a cyclic group optionally having substituent(s), or a salt thereof.

7. 发明专利

PE02772009A1 DERIVADOS DE PIPERIDINA COMO ANTAGONISTAS DE TAQUIQUININAS 未知
公开(公告)号：PE02772009A1
公开(公告)日：2009-04-06
申请号：PE0007002008
申请日：2008-04-23
申请人： TAKEDA PHARMACEUTICAL
发明人： SHIRAI JUNYA , MORIMOTO SHINJI , SUGIYAMA HIDEYUKI , SAKAUCHI NOBUKI , YOSHIKAWA TAKESHI
IPC分类号： A61K31/445 , A61K31/4523 , A61K31/4545 , A61P1/00 , A61P13/00 , C07D401/00 , C07D401/04
CPC分类号： C07D211/60 , C07D401/06 , C07D405/06 , C07D409/04 , C07D409/14 , C07D413/06 , C07D417/06
摘要： REFERIDA A UN COMPUESTO DERIVADO DE PIPERIDINA DE FORMULA (I), DONDE R1 ES CARBAMOILMETILO, METILSULFONILETILCARBONILO, AMINOSULFONILPROPILCARBONILO, ENTRE OTROS; R2 ES METILO O CICLOPROPILO; R3 ES H O METILO; R4 Y R5 SON Cl O TRIFLUOROMETILO; EL GRUPO A ES UN FENILO SUSTITUIDO CON R6, R7 Y R8; R6 ES H, METILO, ETILO O ISOPROPILO; R7 ES H, METILO O Cl; R8 ES F, CL, 3-METILTIOFEN-2-ILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (3S,4S)-N-[3,5-BIS(TRIFLUOROMETIL)BENCIL]-1-{[1-(HIDROXIACETIL)PIPERIDIN-4-IL]CARBONIL}-N-METIL-3-(2-METILFENIL)PIPERIDIN-4-CARBOXAMIDA, (3R*,4R*)-N-[3,5-BIS(TRIFLUOROMETIL)BENCIL]-1-[2-(CICLOPROPILAMINO)-2-OXOETIL]-3-(4-FLUORO-2-METILFENIL)-N-METILPIPERIDIN-4-CARBOXAMIDA, (3S,4S)-N-[3,5-BIS(TRIFLUOROMETIL)BENCIL]-1-[(5,5-DIMETIL-2,4-DIOXO-1,3-OXAZOLIDIN-3-IL)ACETIL]-3-(4-FLUORO-2-METILFENIL)-N-METILPIPERIDIN-4-CARBOXAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS TIENEN ACTIVIDAD ANTAGONISTA DEL RECEPTOR DE TAQUIQUININA, PARTICULARMENTE, SOBRE EL RECEPTOR DE LA SUSTANCIA P, Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES GASTROINTESTINALES, DEL TRACTO URINARIO INFERIOR, ENFERMEDAD NEUROLOGICA CENTRAL, ENTRE OTRAS

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