公开(公告)号：EP2003131A4

公开(公告)日：2009-12-16

申请号：EP07740490

申请日：2007-03-30

申请人： TAISHO PHARMA CO LTD ,  NISSAN CHEMICAL IND LTD

发明人： OKUBO TAKETOSHI ,  KUMAGAI TOSHIHITO ,  ISHII TAKAAKI ,  NAKAMURA TOSHIO ,  ABE KUMI ,  AMADA YURI ,  ISHIZAKA TOMOKO ,  SUN XIANG-MIN ,  SEKIGUCHI YOSHINORI ,  SASAKO SHIGETADA ,  SHIMIZU TAKANORI ,  NAGATSUKA TAKAYUKI

IPC分类号： C07D401/12 ,  A61K31/4365 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61P25/22 ,  A61P25/24

CPC分类号： C07D401/12

公开(公告)号：EP1048655A4

公开(公告)日：2001-04-18

申请号：EP98957145

申请日：1998-12-03

申请人： TAISHO PHARMA CO LTD ,  NIHON NOHYAKU CO LTD

发明人： NAKAZATO ATSURO ,  OKUBO TAKETOSHI ,  KUMAGAI TOSHIHITO ,  CHAKI SHIGEYUKI ,  TOMISAWA KAZUYUKI ,  NAGAMINE MASASHI ,  GOTOH MAKOTO ,  YOSHIDA MASANORI

IPC分类号： C07D215/54 ,  C07D241/44 ,  C07D401/06 ,  C07D491/056 ,  A61K31/47 ,  A61K31/495 ,  C07D215/56

CPC分类号： C07D401/06 ,  C07D215/54 ,  C07D241/44

摘要： 1,2-Dihydro-2-oxoquinoline derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, wherein Ar represents pyridyl or group represented by general formula (II) (wherein X?3 and X4¿ are the same or different and each represents hydrogen, halogeno, C¿1-5? alkyl, C1-5 alkoxy, hydroxy, or trifluoromethyl); Y represents nitrogen, CH, or C(OH); R?1 and R2¿ are the same or different and each represents hydrogen, C¿1-10? alkyl, C3-15 alkoxyalkyl, or C3-15 alkylaminoalkyl or R?1 and R2¿ form a cycloamino group together with the adjacent nitrogen atom; X?1 and X2¿ are the same or different and each represents hydrogen, C¿1-5? alkyl, C1-5 alkoxy, or halogeno or X?1 and X2¿ together represent alkylenedioxy; and n is an integer of 1 to 3.

公开(公告)号：EP1176146A4

公开(公告)日：2003-07-09

申请号：EP00907999

申请日：2000-03-10

申请人： TAISHO PHARMA CO LTD

发明人： NAKAZATO ATSURO ,  OKUBO TAKETOSHI ,  KUMAGAI TOSHIHITO ,  TOMISAWA KAZUYUKI

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 ,  C07D473/34 ,  A61K31/52 ,  C07D207/34 ,  C07D211/78

CPC分类号： A61K31/519 ,  C07D473/00 ,  C07D487/04

摘要： Carbamoyl tetrahydropyridine derivatives represented by general formula (1) and being efficacious against CRF-related diseases; medicinally acceptable salts of the same; and intermediates for the preparation thereof, wherein R?1 and R2¿ are each independently hydrogen, C¿1?-C5 alkyl, or the like; Y?1-Y2 is (R4)C=C(R5), (R6¿)C=N, N=N, (R7)N-CO, or N=C(R?8); X1, X2 and X3¿ are each independently hydrogen, halogeno, or the like; R?3, R4, R5 and R6¿ are each independently hydrogen or alkyl; R7 is hydrogen, C¿1?-C5 alkyl, or the like; and R?8¿ is hydrogen or carbamoyl.

摘要翻译： 通式（1）表示的氨基甲酰基四氢吡啶衍生物对CRF相关疾病有效; 药物可接受的盐; 和用于制备它们的中间体，其中R 1和R 2各自独立地为氢，C 1 -C 5烷基等; （R 4）C = C（R 5），（R 6）C = N，N = N，（R 7）N -CO或N = C（R 8）。 X 1，X 2和X 3各自独立地为氢，卤代等; R 3，R 4，R 5和R 6各自独立地为氢或烷基; R 7是氢，C 1 -C 5烷基等; 而R 8是氢或氨基甲酰基。

公开(公告)号：EP1295608A4

公开(公告)日：2004-03-31

申请号：EP01943844

申请日：2001-06-27

申请人： TAISHO PHARMA CO LTD

发明人： NAKAZATO ATSURO ,  CHAKI SHIGEYUKI ,  OKUBO TAKETOSHI ,  OGAWA SHIN-ICHI ,  ISHII TAKAAKI

IPC分类号： A61K31/495 ,  A61K31/496 ,  A61K45/06 ,  A61P25/22 ,  A61P25/24 ,  C07D295/125 ,  C07D209/14 ,  A61P25/00 ,  C07D211/26 ,  C07D211/70 ,  C07D215/12 ,  C07D239/42 ,  C07D261/20 ,  C07D295/033 ,  C07D295/13 ,  C07D307/81 ,  C07D311/80 ,  C07D333/58

CPC分类号： C07D295/125 ,  A61K31/495 ,  A61K31/496 ,  A61K45/06 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14

摘要： A remedy for anxiety neurosis or depression which contains an MC4 receptor antagonist as the active ingredient; and a piperazine derivative represented by the formula [1] or a pharmaceutically acceptable salt thereof, wherein Ar1 represents (un)substituted phenyl, etc.; Ar2 represents (un)substituted naphthyl, quinolyl, a group represented by the formula [a] (wherein R4 is hydrogen or halogeno; and X-Y is CH-NH, CH-O, CH-S, or N-O), or a group represented by the formula [b] (wherein R5 is hydrogen, hydroxy, or C¿1-10? alkoxy); R?1¿ represents hydrogen, C¿1-10? alkyl, etc.; R?2 and R3¿ are the same or different and each is hydrogen or C¿1-10? alkyl; A-B represents N-CH2, CH-CH2, C(OH)-CH2, or C=CH; T?1¿ represents a single bond, -O-, etc.; and n is an integer of 1 to 10.

公开(公告)号：EP1048651A4

公开(公告)日：2001-09-19

申请号：EP98957146

申请日：1998-12-03

申请人： TAISHO PHARMA CO LTD ,  NIHON NOHYAKU CO LTD

发明人： NAKAZATO ATSURO ,  OKUBO TAKETOSHI ,  KUMAGAI TOSHIHITO ,  CHAKI SHIGEYUKI ,  TOMISAWA KAZUYUKI ,  NAGAMINE MASASHI ,  GOTOH MAKOTO ,  KONDOH KUNIAKI ,  YOSHIDA MASANORI

IPC分类号： C07D471/04 ,  C07D491/052 ,  C07D495/04 ,  C07D209/80 ,  A61K31/40 ,  A61K31/415 ,  A61K31/435 ,  A61K31/495 ,  C07D209/82 ,  C07D487/04 ,  C07D513/04

CPC分类号： C07D471/04 ,  C07D495/04

摘要： Nitrogen-containing tetracyclic compounds represented by general formula (I) or pharmaceutically acceptable salts thereof, wherein Y1-Y2-Y3 represents N-C=N or C=C-NR3 (wherein R3 represents hydrogen, C¿1-5? alkyl or nitrogen-containing C2-10 alkyl); Y?4¿ represents S, SO, SO¿2?, CH2 or NR?4¿ (wherein R4 represents C¿1-5? alkanoyl or C1-5 alkyl); R?1 and R2¿ are the same or different and each represents hydrogen, C¿1-10? alkyl, C3-15 alkoxyalkyl or C3-15 alkylaminoalkyl, or R?1 and R2¿ form together with the adjacent nitrogen atom cyclic amino; X?1 and X2¿ are the same or different and each represents hydrogen, C¿1-5? alkyl, C1-5 alkoxy or halogeno; and n is 0, 1 or 2.

公开(公告)号：EP1004573A4

公开(公告)日：2000-10-18

申请号：EP98935326

申请日：1998-08-03

申请人： TAISHO PHARMA CO LTD ,  NIHON NOHYAKU CO LTD

发明人： NAKAZATO ATSURO ,  OKUBO TAKETOSHI ,  NAKAMURA TOSHIO ,  CHAKI SHIGEYUKI ,  TOMISAWA KAZUYUKI ,  NAGAMINE MASASHI ,  YAMAMOTO KENJI ,  HARADA KOICHIRO ,  YOSHIDA MASANORI

IPC分类号： 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 ,  C07D213/40 ,  C07D213/64 ,  C07D213/643 ,  C07D213/65 ,  C07D213/68 ,  A61K31/325 ,  A61K31/33 ,  C07C233/31 ,  C07C233/47 ,  C07C235/16 ,  C07C237/08 ,  C07C237/42 ,  C07C271/28

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： Aryloxyaniline derivatives represented by the general formula (I), wherein Ar?1 and Ar2¿ represent each a substituted or unsubstituted phenyl, pyridyl, or naphthyl group; R1 represents a hydrogen atom, an alkyl group or the like; X1 represents a hydrogen atom, an alkyl group or the like; and Y1 represents a branched or unbranched 1-6 C alkylene group or a single bond, or pharmaceutically acceptable salts thereof. The derivatives can provide medicines having high affinity for MDR exhibiting therapeutic and prophylactic effects on anxiety and associated diseases, depression, and the like.

摘要翻译： 由通式（I）表示的芳氧基苯胺衍生物，其中Ar 1和Ar 2各自代表取代或未取代的苯基，吡啶基或萘基; R1表示氢原子，烷基等; X1表示氢原子，烷基等; Y1表示支链或非支链1-6C亚烷基或单键，或其药学上可接受的盐。 该衍生物可提供对MDR具有高亲和力的药物，其显示对焦虑和相关疾病，抑郁症等的治疗和预防作用。

公开(公告)号：EP1299378A4

公开(公告)日：2004-01-28

申请号：EP01947819

申请日：2001-07-04

申请人： TAISHO PHARMA CO LTD

发明人： NAKAZATO ATSURO ,  KUMAGAI TOSHIHITO ,  OKUBO TAKETOSHI ,  KAMEO KAZUYA

IPC分类号： A61K31/4365 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/502 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61P1/00 ,  A61P1/14 ,  A61P7/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P17/14 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P29/00 ,  A61P37/02 ,  A61P43/00 ,  C07D401/04 ,  C07D401/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/4725

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04

摘要： A tetrahydropyridino or piperidino heterocyclic derivative represented by the formula [I]: A-Het [I]has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.

公开(公告)号：EP0976745A4

公开(公告)日：2001-11-28

申请号：EP98911002

申请日：1998-03-25

申请人： TAISHO PHARMA CO LTD

发明人： NAKAZATO ATSURO ,  KUMAGAI TOSHIHITO ,  OKUBO TAKETOSHI ,  AIBE IZUMI ,  TANAKA HIDEO ,  CHAKI SHIGEYUKI ,  OKUYAMA SHIGERU ,  TOMISAWA KAZUYUKI

IPC分类号： A61P25/08 ,  C07D401/04 ,  C07D405/14 ,  C07D409/14 ,  A61K31/505

CPC分类号： C07D401/04 ,  C07D405/14 ,  C07D409/14

摘要： 4-Tetrahydropyridylpyrimidine derivatives of general formula (I); and medicinally acceptable salts thereof, wherein Ar is phenyl optionally substituted with one to three groups selected from among halogeno, C1-C5 alkyl, C1-C5 alkoxy and trifluoromethyl, thienyl or furanyl; R1 is hydrogen, C¿1?-C5 alkyl or amino optionally substituted with one or two C1-C5 alkyl groups; R?2 is C¿1-C5 alkyl, C4-C7 cycloalkylalkyl, C2-C5 alkenyl or C2-C5 alkynyl; and X?1, X2 and X3¿ are each independently hydrogen, halogeno, C¿1?-C5 alkyl, C1-C5 alkoxy, C1-C5 alkylthio or amino optionally substituted with one or two C1-C5 alkyl groups. These compounds are efficacious against diseases in which CRF is believed to be concerned, for example, melancholia, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, digestive diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immunologic diseases and so on.