公开(公告)号：EP1362601A4

公开(公告)日：2005-07-06

申请号：EP02700679

申请日：2002-02-21

申请人： EISAI CO LTD

发明人： ONO NAOTO ,  SENBA TARO ,  HATA NAOKO ,  FUNAHASHI YASUHIRO ,  WAKABAYASHI TOSHIAKI

IPC分类号： A61P9/00 ,  A61P35/00 ,  C07D209/42 ,  C07K14/705 ,  G01N33/50 ,  G01N33/566

CPC分类号： G01N33/566 ,  C07D209/42 ,  C07K14/70546 ,  G01N2333/70546 ,  G01N2500/00

摘要： A method of examining the effect of a drug on the expression of an integrin which comprises the step of measuring the expression dose of the integrin in platelets of a patients to whom the drug has been administered and the step of evaluating the effect of the drug on the expression of the integrin in cells other than platelets on the basis of the expression dose thus measured.

公开(公告)号：EP1243583A4

公开(公告)日：2003-08-20

申请号：EP00985953

申请日：2000-12-27

申请人： EISAI CO LTD

发明人： HANEDA TORU ,  TSURUOKA AKIHIKO ,  KAMATA JUNICHI ,  OKABE TADASHI ,  TAKAHASHI KEIKO ,  NARA KAZUMASA ,  HAMAOKA SHINICHI ,  UEDA NORIHIRO ,  WAKABAYASHI TOSHIAKI ,  FUNAHASHI YASUHIRO ,  SEMBA TARO ,  HATA NAOKO ,  YAMAMOTO YUJI ,  OZAWA YOICHI ,  TSUKAHARA NAOKO ,  OWA TAKASHI

IPC分类号： A61K31/352 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/501 ,  A61P3/10 ,  A61P9/10 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D215/38 ,  C07D215/48 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D217/26 ,  C07D311/16 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D411/12 ,  C07D417/12 ,  C07D471/04 ,  A61P35/04

CPC分类号： C07D215/38 ,  C07D215/48 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D217/26 ,  C07D311/16 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D411/12 ,  C07D417/12 ,  C07D471/04

摘要： Heterocyclic compounds having sulfonamide or sulfonylurea groups, specifically heterocyclic compounds of general formula, pharmacologically acceptable salts of the same, or hydrates of both: (|) wherein A is hydrogen, halogeno, optionally halogenated C1-4 alkyl, or the like; B is optionally substituted aryl, monocyclic heteroaryl, or the like; K is a single bond or the like; T, W, X and Y are each independently =C(D) - (wherein D is hydrogen, halogeno, or the like) or nitrogen; U and V are each independently =C(D) -, nitrogen, oxygen, or the like; Z is a single bond or -CO-NH-; and R1 is hydrogen or the like.

摘要翻译： 本发明提供了含磺酰胺或磺酰脲的杂环化合物。 具体地说，提供由式（I）表示的杂环化合物，其药学上可接受的盐或它们的水合物。 式中，A为氢原子，卤素原子，可被卤素原子取代的C1-C4烷基或烷氧基或氰基; B是任选取代的芳基或单环杂芳基，或：（其中，环Q是可具有氮原子的芳环;环M是与环Q共享双键的环，其中 环可以具有杂原子;并且环Q和M可以共享氮原子）; K是单键; T，W，X和Y彼此相同或不同，并且各自为= C（D） - （其中，D为氢或卤素原子）或氮原子; U和V彼此相同或不同，并且各自为= C（D） - ，氮原子，-CH 2 - ，氧原子或-CO-; Z是单键或-CO-NH-; R1为氢原子等

公开(公告)号：EP1081151A4

公开(公告)日：2002-10-28

申请号：EP99917219

申请日：1999-04-28

申请人： MERCIAN CORP ,  EISAI CO LTD

发明人： WAKABAYASHI TOSHIAKI ,  KAWASE RENA ,  NARUSE NOBUAKI ,  FUJITA MASANORI ,  SAMESHIMA TOMOHIRO ,  WATANABE YOSHIO ,  DOBASHI KAZUYUKI ,  FUNAHASHI YASUHIRO ,  SENBA TARO

IPC分类号： C07D493/10 ,  C12P17/16 ,  A61K31/35 ,  C12P17/18

CPC分类号： C07D493/10 ,  C12P17/162

摘要： Novel physiologically active substances having a neovascularization inhibitory effect. Compounds represented by general formula (1) or salts thereof are isolated from a liquid culture medium of a strain belonging to the genus Streptomyces and the structures are analyzed. In said formula, R1 represents hydrogen, aldehyde or lower acyl; R?2 and R3¿ may be the same or different and each represents hydrogen or lower alkoxy, or R?2 and R3¿ may represent together oxygen; R4 represents lower alkyl; and R5 represents hydrogen or lower alkyl, provided that the case where R1 is aldehyde, R?2 and R3¿ are different from each other and represent hydrogen or methoxy, R4 is ethyl and R5 is hydrogen is excluded.

公开(公告)号：EP1258252A4

公开(公告)日：2005-11-02

申请号：EP01948941

申请日：2001-02-01

申请人： EISAI CO LTD

发明人： WAKABAYASHI TOSHIAKI ,  FUNAHASHI YASUHIRO ,  HATA NAOKO ,  SEMBA TARO ,  YAMAMOTO YUJI ,  HANEDA TORU ,  OWA TAKASHI ,  TSURUOKA AKIHIKO ,  KAMATA JUNICHI ,  OKABE TADASHI ,  TAKAHASHI KEIKO ,  NARA KAZUMASA ,  HAMAOKA SHINICHI ,  UEDA NORIHIRO

IPC分类号： A61K45/06 ,  A61K31/00 ,  A61K31/145 ,  A61K31/18 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/506 ,  A61P7/02 ,  A61P9/10 ,  A61P17/06 ,  A61P19/02 ,  A61P19/10 ,  A61P35/00 ,  A61P35/04 ,  C07D209/08 ,  C07D209/12 ,  C07D209/30 ,  C07D209/34 ,  C07D209/42 ,  C07D215/38 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D311/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D411/12 ,  C07D417/12 ,  C07D471/04 ,  A61K45/00

CPC分类号： C07D471/04 ,  A61K31/00 ,  A61K31/18 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/4439 ,  A61K31/506 ,  C07D209/08 ,  C07D209/12 ,  C07D209/30 ,  C07D209/34 ,  C07D209/42 ,  C07D215/38 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D311/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D411/12 ,  C07D417/12

摘要： Integrin expression inhibitors and remedies for arteriosclerosis, psoriasis, cancer, retinal angiogenesis, diabetic retinitis or inflammatory diseases, anticoagulant agents and cancerous metastasis inhibitors based on the integrin inhibitory effect. Namely, integrin expression inhibitors containing as the active ingredient sulfonamide compounds represented by the following general formula (I), pharmacologically acceptable salts thereof or hydrates of the same wherein B represents optionally substituted C6-10 aryl or 6- to 10-membered heteroaryl wherein the ring may be partly saturated; K represents a single bond, -CH=CH- or -(CR4bR5b)mb- (wherein R?4b and R5b¿ may be the same or different and each represents hydrogen or C¿1-4? alkyl; and m?b¿ represents an integer of 1 or 2); R1 represents hydrogen or C¿1-6? alkyl; Z represents a single bond or CO-NH-; and R represents optionally substituted C6-10 aryl or 6- to 10-membered heteroaryl wherein the ring may be partly saturated.

公开(公告)号：EP1415987A4

公开(公告)日：2004-08-18

申请号：EP01976786

申请日：2001-10-19

申请人： EISAI CO LTD

发明人： FUNAHASHI YASUHIRO ,  TSURUOKA AKIHIKO ,  MATSUKURA MASAYUKI ,  HANEDA TORU ,  FUKUDA YOSHIO ,  KAMATA JUNICHI ,  TAKAHASHI KEIKO ,  MATSUSHIMA TOMOHIRO ,  MIYAZAKI KAZUKI ,  NOMOTO KEN-ICHI ,  WATANABE TATSUO ,  OBAISHI HIROSHI ,  YAMAGUCHI ATSUMI ,  SUZUKI SACHI ,  NAKAMURA KATSUJI ,  MIMURA FUSAYO ,  YAMAMOTO YUJI ,  MATSUI JUNJI ,  MATSUI KENJI ,  YOSHIBA TAKAKO

IPC分类号： C07D239/34 ,  A61K20060101 ,  A61K31/4355 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4545 ,  A61K31/455 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/505 ,  A61K31/519 ,  A61K31/5377 ,  A61P20060101 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P17/06 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D20060101 ,  C07D207/34 ,  C07D213/26 ,  C07D213/68 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D215/18 ,  C07D215/22 ,  C07D215/233 ,  C07D215/36 ,  C07D215/38 ,  C07D215/48 ,  C07D239/42 ,  C07D239/46 ,  C07D239/88 ,  C07D249/04 ,  C07D261/14 ,  C07D277/48 ,  C07D307/68 ,  C07D319/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  C07D239/47

CPC分类号： C07D213/73 ,  A61K31/4706 ,  A61K31/4745 ,  A61K31/517 ,  A61K31/519 ,  C07D207/34 ,  C07D213/26 ,  C07D213/68 ,  C07D213/74 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D215/18 ,  C07D215/233 ,  C07D215/36 ,  C07D215/38 ,  C07D215/48 ,  C07D239/34 ,  C07D239/42 ,  C07D239/47 ,  C07D239/88 ,  C07D249/04 ,  C07D261/14 ,  C07D277/48 ,  C07D307/68 ,  C07D319/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

摘要： A compound represented by the following general formula: wherein A is a further optionally substituted group represented by the formula: X is an oxygen atom, a sulfur atom, -SO- or -SO2; Y is an optionally substituted C6-14 aryl group, an optionally substituted 5- to 14-membered aromatic heterocyclic group or an optionally substituted C1-6 alkylene group; E is a single bond or -NR -.

公开(公告)号：EP1074542A4

公开(公告)日：2002-02-06

申请号：EP00905321

申请日：2000-02-24

申请人： EISAI CO LTD

发明人： HANEDA TORU ,  TSURUOKA AKIHIKO ,  KAMATA JUNICHI ,  OKABE TADASHI ,  TAKAHASHI KEIKO ,  NARA KAZUMASA ,  HAMAOKA SHINICHI ,  UEDA NORIHIRO ,  OHWA TAKASHI ,  WAKABAYASHI TOSHIAKI ,  FUNAHASHI YASUHIRO ,  SEMBA TARO ,  HATA NAOKO ,  YAMAMOTO YUJI ,  OZAWA YOICHI ,  TSUKAHARA NAOKO

IPC分类号： A61K31/00 ,  A61K31/38 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/505 ,  A61K31/506 ,  A61P19/00 ,  A61P19/02 ,  A61P27/00 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D209/04 ,  C07D209/08 ,  C07D209/30 ,  C07D209/42 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12

CPC分类号： C07D401/12 ,  C07D209/04 ,  C07D209/30 ,  C07D209/42 ,  C07D403/12 ,  C07D409/12

摘要： Novel neovascularization inhibitors are constructed to provide antitumor agents which are superior in safety to conventional antitumor agents, are surely efficacious and can be administered over a prolonged period of time. Namely, indole compounds represented by general formula (I) or pharmacologically acceptable salts thereof or hydrates of the same wherein R represents hydrogen, etc.; R and R are the same or different and each represents hydrogen, etc.; R represents hydrogen or lower (C1-4) alkyl; and the ring A represents cyanophenyl, etc., provided that the following cases are excluded; the one where R , R and R are all hydrogen atoms; the one where R and R are both hydrogen atoms; and the one where the ring A is an aminosulfonylphenyl group and R and R are both halogen atoms; and provided that when the ring A is a cyanophenyl, 2-amino-5-pyridyl or 2-halogeno-5-pyridyl group and R is a cyano group or a halogen atom, then at least one of R and R is not hydrogen.