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91. 发明专利

CA2649022C COCRYSTAL OF C-GLYCOSIDE DERIVATIVE AND L-PROLINE 未知
公开(公告)号：CA2649022C
公开(公告)日：2012-05-29
申请号：CA2649022
申请日：2007-04-04
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： IMAMURA MASAKAZU , NAKANISHI KEITA , SHIRAKI RYOTA , ONDA KENICHI , SASUGA DAISUKE , YUDA MASAMICHI
IPC分类号： C07D407/10 , A61K31/381 , A61P3/10
摘要： A cocrystal of (1S)-1,5-anhydro-1-[3-(1-benzothien-2--ylmethyl)-4-fluorophenyl]-D-glucitol and L-proline. It is a cocrystal of known compound A, which has a constant quality, is superior in storage stability, has no moisture absorptivity, and is suitable as a crystal of a drug substance used for preparing pharmaceuticals.

92. 发明专利

AT556052T 未知
公开(公告)号：AT556052T
公开(公告)日：2012-05-15
申请号：AT05781323
申请日：2005-08-31
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： KIKUCHI KAZUMI , FUJIYASU JIRO , WATANABE TOSHIHIRO , NAGAKURA YUKINORI , TOMIYAMA HIROSHI , SONEGAWA MOTOHARU , TOKUZAKI KAZUO , IWAI YOSHINORI
IPC分类号： C07D211/16 , C07D211/18 , C07D211/22 , C07D211/28 , C07D211/34 , C07D211/42 , C07D211/62 , C07D401/06
摘要： The piperidine derivative of the present invention in which the 4-position of the piperidine ring is bonded, via vinylene, to a mono-substituted (-R 1 ) or unsubstituted benzene ring and the 1-position of the piperidine ring has an acyl group [-C(=O)-R 4 ], or a pharmaceutically acceptable salt thereof has an excellent sodium channel inhibition action and an excellent analgesic action and shows a high analgesic effect particularly to neurogenic pain. The present compound is useful as a sodium channel inhibitor of low side effect

93. 发明专利

ES2363941T3 DERIVADOS DE C-GLUCOSIDO PARA EL TRATAMIENTO DE DIABETES. 未知
公开(公告)号：ES2363941T3
公开(公告)日：2011-08-19
申请号：ES08012499
申请日：2004-03-12
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： IMAMURA MASAKAZU , MURAKAMI TAKESHI , IKEGAI KAZUHIRO , IWASAKI FUMIYOSHI , SUGANE TAKASHI , KUROSAKI EIJI , TOMIYAMA HIROSHI , NODA ATSUSHI , KITTA KAYOKO , KOBAYASHI YOSHINORI , SHIRAKI RYOTA
IPC分类号： C07D405/10 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , A61P3/04 , A61P3/10 , C07D207/06 , C07D309/10 , C07D333/12 , C07D333/16 , C07D333/54 , C07D405/04 , C07D407/04 , C07D407/10 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D417/10 , C07D493/04 , C07D495/04
摘要： Un derivado de C-glucósido de la siguiente fórmula (I) y sales de los mismos: en la que el anillo A representa un anillo de benceno, el anillo B representa un anillo hetero bicíclico saturado o insaturado de ocho a diez miembros que tiene de 1 a 4 heteroátomos seleccionados entre N, S, y O, y X representa metileno, con la condición de que cuando el anillo B sea un anillo hetero bicíclico saturado o insaturado de ocho a diez miembros que tiene de 1 a 4 heteroátomos seleccionados entre N, S y O incluyendo un anillo de benceno, X se una al anillo B en una parte distinta del anillo de benceno incluido en el anillo B; R 1 a R 4 individualmente representan un átomo de hidrógeno, un alquilo inferior, -C(=O)-alquilo inferior, o -alquilen inferior-arilo; y R 5 a R 11 individualmente representan, alquilo inferior, un cicloalquilo, un halógeno, un alquilo inferior sustituido con halógeno, -OH, =O, -NH2, alquil sulfonil inferior-, alquil sulfonil inferior sustituido con halógeno, aril sulfonil-, un arilo, un anillo hetero monocíclico saturado o insaturado de 5 ó 6 miembros que tiene de 1 a 4 heteroátomos seleccionados entre N, S, y O, -alquilen inferior-OH, alquilen inferior-O-alquilo inferior, -alquilen inferior-O-C(=O) alquilo inferior, -alquilen inferior-O-alquilen inferior-COOH, -alquilen inferior-O-alquilen inferior-C(=O)-O-alquilo inferior, -alquilen inferior-NH2, -alquilen inferior-NH-alquilo inferior, -alquilen inferior-N(alquilo inferior)2, -alquilen inferior-NH-C(=O)-alquilo inferior, -COOH, -CN, -C(=O)-O-alquilo inferior, -C(=O)-NH2, -C(=O)-NH-alquilo inferior, C(=O)-N(alquilo inferior)2, -O-alquilo inferior, -O-cicloalquilo, -O-alquilen inferior-OH, -O-alquilen inferior-O-alquilo inferior, -O-alquilen inferior-COOH, -O-alquilen inferior-C(=O)-O-alquilo inferior, -O-alquilen inferior-C(=O)-NH2, -O alquilen inferior-C(=O)-NH-alquilo inferior, -O-alquilen inferior-C(=O)-N(alquilo inferior)2, -O-alquilen inferior-CH(OH) CH2(OH), -O-alquilen inferior-NH2, -O-alquilen inferior-NH-alquilo inferior, -O-alquilen inferior-N(alquilo inferior)2, -Oalquilen inferior-NH-C(=O)-alquilo inferior, -NH-alquilo inferior, -N(alquilo inferior)2, -NH-SO2-alquilo inferior, alquilo inferior sustituido con -NH-SO2-halógeno, -NH-alquilen inferior-OH, -NH-C(=O)-alquilo inferior, -NH-C(=O)-NH2, -NH C(=O)-NH-alquilo inferior, -NH-C(=O)-N(alquilo inferior)2, o -NH-C(=O)-O-alquilo inferior; y R 7 a R 11 individualmente representan un átomo de hidrógeno, un alquilo inferior, un cicloalquilo, un halógeno, un alquilo inferior sustituido con halógeno, -OH, =O, -NH2, alquil sulfonil inferior-, alquil sulfonil inferior sustituido con halógeno-, aril sulfonil-, un arilo, un anillo hetero monocíclico saturado o insaturado de cinco o seis miembros que tiene de 1 a 4 heteroátomos seleccionados entre N, S y O, -alquilen inferior-OH, -alquilen inferior-O-alquilo inferior, alquilen inferior-O-C(=O)-alquilo inferior, -alquilen inferior-O-alquilen inferior-COOH, -alquilen inferior-O-alquilen inferior-C(=O)-O-alquilo inferior, -alquilen inferior-NH2, -alquilen inferior-NH-alquilo inferior, -alquilen inferior-N(alquilo inferior)2, -alquilen inferior-NH-C(=O)-alquilo inferior, -COOH, -CN, -C(=O)-O-alquilo inferior, -C(=O)-NH2, -C(=O) NH-alquilo inferior, -C(=O)-N(alquilo inferior)2, -O-alquilo inferior, -O-cicloalquilo, -O-alquilen inferior-OH, -O-alquilen inferior-O-alquilo inferior, -O-alquilen inferior-COOH, -O-alquilen inferior-C(=O)-O-alquilo inferior, -O-alquilen inferior C(=O)-NH2, -O-alquilen inferior-C(=O)-NH-alquilo inferior, -O-alquilen inferior-C(=O)-N(alquilo inferior)2, -O-alquilen inferior-CH(OH)-CH2(OH), -O-alquilen inferior-NH2, -O-alquilen inferior-NH-alquilo inferior, - O-alquilen inferior- N(alquilo inferior)2, -O-alquilen inferior-NH-C(=O)-alquilo inferior, -NH-alquilo inferior, -N(alquilo inferior)2, -NH-SO2alquilo inferior, -NH-SO2-alquilo inferior sustituido con halógeno, -NH-alquilen inferior-OH, -NH-C(=O)-alquilo inferior, -NH-C(=O)-NH2, -NH-C(=O)-NH-alquilo inferior, -NH-C(=O)-N(alquilo inferior)2 o -NH-C(=O)-O-alquilo inferior; donde el término "inferior" se refiere a una cadena de carbono lineal o ramificada que tiene de 1-6 átomos de carbono.

94. 发明专利

HK1142806A1 STABLE SOLID PREPARATION OF EGUALEN SODIUM 未知
公开(公告)号：HK1142806A1
公开(公告)日：2010-12-17
申请号：HK10109226
申请日：2010-09-27
申请人： KOTOBUKI PHARMACEUTICAL CO LTD
发明人： TOMIYAMA HIROSHI , SHIMADA TOMONORI , YOSHIDA TAKUJI
IPC分类号： A61K20060101 , A61P20060101

95. 发明专利

AU2003252370B2 Azulene derivatives and salts thereof 未知
公开(公告)号：AU2003252370B2
公开(公告)日：2008-11-06
申请号：AU2003252370
申请日：2003-08-04
申请人： KOTOBUKI PHARMACEUTICAL CO LTD , ASTELLAS PHARMA INC
发明人： KUROSAKI EIJI , IMAMURA MASAKAZU , KITTA KAYOKO , TOMIYAMA HIROSHI , IKEGAI KAZUHIRO , KOBAYASHI YOSHINORI , MURAKAMI TAKESHI , SUZUKI TAKAYUKI , NODA ATSUSHI
IPC分类号： C07D309/12 , A61P3/04 , A61P3/10 , A61P43/00 , C07D309/10
摘要： The present invention provides an azulene derivative and a salt thereof, wherein an azulene ring is bonded to a benzene ring directly or via a lower alkylene which may be substituted with a halogen atom and the benzene ring is directly bonded to the glucose residue, and it is usable as a Na -glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes-related diseases such as insulin-resistant diseases and obesity.

96. 发明专利

CA2494177C AZULENE DERIVATIVES AND SALTS THEREOF FOR USE AS NA+-GLUCOSE COTRANSPORTER INHIBITORS 未知
公开(公告)号：CA2494177C
公开(公告)日：2008-10-14
申请号：CA2494177
申请日：2003-08-04
申请人： YAMANOUCHI PHARMA CO LTD , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： MURAKAMI TAKESHI , IKEGAI KAZUHIRO , SUZUKI TAKAYUKI , KUROSAKI EIJI , TOMIYAMA HIROSHI , IMAMURA MASAKAZU , KOBAYASHI YOSHINORI , NODA ATSUSHI , KITTA KAYOKO
IPC分类号： C07H15/00 , A61K31/70 , A61K31/7028 , A61P3/04 , A61P3/10 , A61P43/00 , C07D309/10 , C07D309/12 , C07H7/04 , C07H13/00
摘要： Azulene derivatives represented by the following general formula (I) and salts thereof are useful as Na+-glucose cotransporter inhibitors in, for example, remedies for diabetes, etc., in particular, insulin-independent diabetes (type 2 diabetes), insulin-dependent diabetes (type 1 diabetes), etc., and remedies for various diabetes-related diseases such as insulin resistant disease and obesity. These compounds are characterized in that an azulene ring is bonded, either directly or via an optionally halogenated lower alkylene, to a benzene ring and the benzene ring is directly bonded to a sugar residue.

97. 发明专利

ZA200702379B Piperidine derivative or pharmaceutically acceptable salt thereof 未知
公开(公告)号：ZA200702379B
公开(公告)日：2008-07-30
申请号：ZA200702379
申请日：2005-08-31
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： KAZUMI KIKUCHI , JIRO FUJIYASU , TOSHIHIRO WATANABE , YUKINORI NAGAKURA , HIROSHI TOMIYAMA , MOTOHARU SONEGAWA , KAZUO TOKUZAKI , YOSHINORI IWAI
IPC分类号： A61K20090101 , A61P20090101 , C07D20090101
摘要： The piperidine derivative of the present invention in which the 4-position of the piperidine ring is bonded, via vinylene, to a mono-substituted (-R 1 ) or unsubstituted benzene ring and the 1-position of the piperidine ring has an acyl group [-C(=O)-R 4 ], or a pharmaceutically acceptable salt thereof has an excellent sodium channel inhibition action and an excellent analgesic action and shows a high analgesic effect particularly to neurogenic pain. The present compound is useful as a sodium channel inhibitor of low side effect

98. 发明专利

CA2673498A1 METHOD FOR PRODUCING C-GLYCOSIDE DERIVATIVE AND INTERMEDIATEFOR SYNTHESIS THEREOF 未知
公开(公告)号：CA2673498A1
公开(公告)日：2008-06-26
申请号：CA2673498
申请日：2007-12-20
申请人： KOTOBUKI PHARMACEUTICAL CO LTD , ASTELLAS PHARMA INC
发明人： KOMENOI KOUSUKE , NAKAMURA ATSUSHI , IMAMURA MASAKAZU , KASAI MAKOTO , SHIRAKI RYOTA , NAKANISHI KEITA
IPC分类号： C07D409/10 , A61K31/381 , A61P3/10 , C07D333/54
摘要： It is intended to provide a method for producing a C-glycoside derivative at high yield and low cost, which conforms to environmental protection and is industrially applicable. The C-glycoside derivative is useful for treatin g and preventing diabetes mellitus such as insulin-dependent diabetes mellit us (type 1 diabetes) and non-insulin-dependent diabetes mellitus (type 2 dia betes), and also various diabetes-related diseases including insulin-resista nt diseases and obesity.

99. 发明专利

AU2004251536B2 Serum cholesterol lowering agent or preventive or therapeutic agent for atherosclerosis 未知
公开(公告)号：AU2004251536B2
公开(公告)日：2007-11-15
申请号：AU2004251536
申请日：2004-06-15
申请人： KOTOBUKI PHARMACEUTICAL CO LTD
发明人： TOMIYAMA HIROSHI , KOSAKAI KAZUHIRO , YOKOTA MASAYUKI
IPC分类号： A61K31/216 , A61K31/397 , A61K31/40 , A61K45/00 , A61K45/06 , A61P3/06 , A61P9/10 , A61P43/00 , C07D405/10 , C07D405/12
摘要： A serum cholesterol lowing agent or a preventive or therapeutile agent for atherosclerosis, which each comprises a combination of a compound represented by the following general formula (I) or pharmaceutical acceptable salts thereof with a cholesterol biosynthesis inhibitor and/or a fibrate type cholesterol lowing agent. (I) (b) (a) [In the formula, A 1 , A 2 , A 3 and A 4 each is hydrogen, a group represented by the formula (b), or a group represented by the formula (a), provided that at least one of these is a group represented by the formula (a); A 2 is C 1-5 alkyl etc; and n. p, q and r each is an integer of 0, 1 or 2.

100. 发明专利

AT374769T 未知
公开(公告)号：AT374769T
公开(公告)日：2007-10-15
申请号：AT02703861
申请日：2002-02-20
申请人： KOTOBUKI PHARMACEUTICAL CO LTD
发明人： TOMIYAMA HIROSHI , YOKOTA MASAYUKI , NODA ATSUSHI , OHNO AKIRA
IPC分类号： C07D405/10 , A61K31/351 , A61K45/00 , A61P3/06 , C07D405/12
摘要： The compounds have the following general formula (I): Äwherein: A1, A3 and A4 are hydrogen atom, halogen atom, alkyl group having one to five carbon atoms, alkoxy group having one to five carbon atoms, -COOR1, a following formula (wherein: R1 is hydrogen atom or alkyl group having one to five carbon atoms) or a following formula Äwherein: R2 is -CH2OH group, -CH2OC(O)-R1 group or -CO2-R1 group; R3 is -OH group or-OC(O)-R1 group; R4 is -(CH2)kR5(CH2)1- (k and 1 are 0 or 1 more integer; k+1 is 10 or fewer integer); R5 means bond (single bond (-), -CH=CH-, -OCH2-, carbonyl group or -CH(OH)-.Ü. One of A1, A3 and A4 in formula (I) is must be the group in above mentioned formula (a). A2 is alkyl chain having one to five carbon atoms, alkoxy chain having one to five carbon atoms, alkenyl chain having one to five carbon atoms, hydroxyalkyl chain having one to five carbon atoms or carbonylalkyl chain having one to five carbon atoms. n, p, q or r are 0, 1 or 2.Ü or their pharmaceutical acceptable salts.

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