公开(公告)号：EP1652843A4

公开(公告)日：2010-07-28

申请号：EP04748296

申请日：2004-08-05

申请人： ASTELLAS PHARMA INC ,  RATIONAL DRUG DESIGN LAB

发明人： KONTANI TORU ,  MIYATA JUNJI ,  HAMAGUCHI WATARU ,  KAWANO TOMOAKI ,  KAMIKAWA AKIO ,  SUZUKI HIROSHI ,  SUDO KENJI

IPC分类号： C07D249/06 ,  A61K31/4192 ,  A61K31/421 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/4427 ,  A61P31/18 ,  A61P31/22 ,  C07D263/32 ,  C07D271/06 ,  C07D335/02 ,  C07D413/12

CPC分类号： C07D335/02 ,  C07D413/12

公开(公告)号：EP1340750A4

公开(公告)日：2004-01-21

申请号：EP01981033

申请日：2001-11-08

申请人： YAMANOUCHI PHARMA CO LTD ,  RATIONAL DRUG DESIGN LAB

发明人： KONTANI TORU ,  MIYATA JUNJI ,  HAMAGUCHI WATARU ,  MIYAZAKI YOJI ,  SUZUKI HIROSHI ,  NAKAI EIICHI ,  KAGEYAMA SHUNJI

IPC分类号： A61K8/42 ,  A61P31/22 ,  C07D277/40 ,  C07D277/62 ,  C07D277/64 ,  C07D277/74 ,  C07D417/12 ,  C07D417/14 ,  A61K31/426 ,  A61K31/427 ,  A61K31/428 ,  A61K31/433 ,  A61K31/439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/536 ,  A61K31/5415

CPC分类号： C07D277/74 ,  C07D277/40 ,  C07D277/62 ,  C07D277/64 ,  C07D417/12 ,  C07D417/14

摘要： Novel amide derivatives characterized in that, in N({[4-(substituted thiazol-4-yl)phenyl]carbamoyl}methyl)amide derivatives, the N atom in the amido group carries an aryl or heteroaryl substituent (i.e., an aromatic ring group) directly attached thereto. Because of having an excellent anti-herpesviral activity, these amide derivatives are useful as drugs and antiviral agents, in particular, preventives or remedies for various diseases caused by the infection with herpesviruses, more specifically, various herpesvirus infections such as pox (blister) caused by the infection with varicella zoster virus, herpes zoster caused by the recurrent infection with latent varicella zoster virus, herpes labialis and herpes encephalitis caused by the infection with HSV-1 and genital herpes caused by the infection with HSV-2.

摘要翻译： 新型酰胺衍生物的特征在于，在N（{[4-（取代的噻唑-4-基）苯基]氨基甲酰基}甲基）酰胺衍生物中，酰氨基中的N原子带有芳基或杂芳基取代基（即芳环 组）直接附在其上。 由于具有优异的抗疱疹病毒活性，这些酰胺衍生物可用作药物和抗病毒剂，特别是对由疱疹病毒感染引起的各种疾病的预防或治疗，更具体地说，各种疱疹病毒感染如引起的痘（水疱） 由水痘带状疱疹病毒感染引起的复发性潜伏水痘带状疱疹病毒引起的带状疱疹，HSV-1感染引起的唇疱疹和疱疹脑炎以及HSV-2感染引起的生殖器疱疹。

公开(公告)号：EP1783122A4

公开(公告)日：2008-12-10

申请号：EP05765585

申请日：2005-07-07

申请人： ASTELLAS PHARMA INC ,  KOTOBUKI PHARMACEUTICAL CO LTD

发明人： TOMIYAMA HIROSHI ,  YOKOTA MASAYUKI ,  NODA ATSUSHI ,  KOBAYASHI Y ,  OGASAWARA JUNKO ,  HAYASHI YASUMASA ,  INAKOSHI MASATOSHI ,  NAKAMURA HIROFUMI ,  KOIDE TOKUO ,  SAKAMOTO KENICHIRO ,  YAMASHITA YOHEI ,  MIYAFUJI AKIO ,  SUZUKI TAKAYUKI ,  KAWANO NORIYUKI ,  MIYATA JUNJI ,  IMAMURA MASAKAZU ,  SUGANE TAKASHI

IPC分类号： C07D309/10 ,  C07C43/225 ,  C07C49/223 ,  C07H7/04 ,  C07H15/04

CPC分类号： C07C49/255 ,  C07C45/48 ,  C07C45/63 ,  C07C45/71 ,  C07C49/245 ,  C07H7/04 ,  C07H15/04

摘要： A process for producing azulene derivatives useful as Na+-glucose cotransporter inhibitor easily and simply in high yield at a low cost which is industrially advantageous and excellent in environmental protection, characterized by subjecting at least one compound selected from among specific penta- and tetraacyl precursors of the azulene derivatives and salts of the precursors to reduction and deblocking to obtain a C-glycoside compound; and useful intermediates obtained in the above process.

公开(公告)号：EP1783124A4

公开(公告)日：2009-07-08

申请号：EP05774692

申请日：2005-08-26

申请人： ASTELLAS PHARMA INC

发明人： MIYATA JUNJI ,  YOKOTA MASAKI ,  NAITO RYO ,  KAMIKAWA AKIO ,  KAWAKAMI MASAKATSU ,  HATTORI KAZUYUKI

IPC分类号： C07D333/40 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/41 ,  A61K31/427 ,  A61K31/4436 ,  A61K31/4535 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61P1/00 ,  A61P3/00 ,  A61P3/10 ,  A61P19/06 ,  A61P43/00 ,  C07D333/28 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D417/10 ,  C07D417/12

CPC分类号： C07D333/40 ,  C07D409/04 ,  C07D409/10 ,  C07D417/10 ,  C07D417/12

摘要： A 2-phenylthiophene derivative represented by the following general formula (I) or a salt thereof, characterized by comprising a thiophene ring substituted by a carboxy group, etc. and a benzene ring having both of an electron-attracting group, e.g., a cyano group, and an electron-donating group, e.g., a substituted alkoxy group. (I) The compound is satisfactory in xanthine oxidase inhibitory activity and uric acid lowering activity and has no structure derived from any nucleic acid. The compound hence has an advantage that it is safer and more effective than conventional compounds. The compound is useful as a therapeutic or preventive agent for hyperuricemia, gout, inflammatory intestinal diseases, diabetic nephropathy, diabetic retinopathy, etc.

摘要翻译： 由下列通式（I）表示的2-苯基噻吩衍生物或其盐，其特征在于包含被羧基等取代的噻吩环和同时具有吸电子基团的苯环，例如氰基 基团和给电子基团，例如取代的烷氧基。 （I）该化合物在黄嘌呤氧化酶抑制活性和尿酸降低活性方面令人满意，并且没有来自任何核酸的结构。 因此该化合物具有比常规化合物更安全和更有效的优点。 该化合物可用作高尿酸血症，痛风，炎性肠病，糖尿病性肾病，糖尿病性视网膜病等的治疗剂或预防剂。

公开(公告)号：EP1293503A4

公开(公告)日：2008-04-02

申请号：EP01930192

申请日：2001-05-17

申请人： ASTELLAS PHARMA INC

发明人： TOBE TAKAHIKO ,  SUGANE TAKASHI ,  HAMAGUCHI WATARU ,  SHIMADA ITSURO ,  MAENO KYOICHI ,  MIYATA JUNJI ,  KIMIZUKA TETSUYA ,  SUZUKI TAKESHI ,  KOHARA ATSUYUKI ,  MORITA TAKUMA ,  ARLT MICHAEL ,  GREINER HARTMUT

IPC分类号： A61K31/41 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/5377 ,  A61P9/10 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  A61P43/00 ,  C07D249/08 ,  C07D249/10 ,  C07D249/12 ,  C07D249/14 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/10 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D495/04

CPC分类号： C07D249/08 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/5377 ,  C07D249/10 ,  C07D249/12 ,  C07D249/14 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/10 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D495/04

摘要： Triazole derivatives which have a glycine transporter inhibitory activity and are useful as drugs; and novel triazole derivatives. Because of having an excellent glycine transporter inhibitory activity, the above triazole derivatives are useful as remedies.

公开(公告)号：EP1783116A4

公开(公告)日：2008-03-05

申请号：EP05781016

申请日：2005-08-26

申请人： ASTELLAS PHARMA INC

发明人： MIYATA JUNJI ,  NAITO RYO ,  KAWAKAMI MASAKATSU ,  ASANO TORU

IPC分类号： C07D213/79 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12

CPC分类号： C07D213/79 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

摘要： A 2-phenylpyridine derivative represented by the following general formula (I) or a salt thereof. The compounds have satisfactory xanthine oxidase inhibitory activity and uric acid-lowering activity and are useful as a therapeutic or preventive agent for hyperuricemia, gout, inflammatory intestinal diseases, diabetic nephropathy, diabetic retinopathy, etc. [The symbols in the formula have the following meanings: R1: H, etc.; R2: -CO2H, etc.; R3 and R4: H, etc.; R5: -CN, etc.; R6: H, etc.; X: -O-, -N(R8)-, or -S-; (provided that the groups represented by R5 and -X-R7 are bonded in a meta position or the para position to the pyridyl group) R8: H, etc.; R7: C1-8 linear or branched alkyl, etc.; Y: a bond, etc.; and R9, R10, and R11: H, etc. (provided that when X is -N(R8)-, then R8 may be bonded to R7 to form a nitrogenous saturated heterocycle in cooperation with the adjacent nitrogen atom).]