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1. 发明申请

WO2008139845A1 NOVEL AMIDE DERIVATIVE 审中-公开
标题翻译：新颖的衍生物
公开(公告)号：WO2008139845A1
公开(公告)日：2008-11-20
申请号：PCT/JP2008057711
申请日：2008-04-22
申请人： DAIICHI SANKYO CO LTD , UTO YOSHIKAZU , KIYOTSUKA YOHEI , KURATA HITOSHI , OGATA TSUNEAKI , OKUYAMA RYO , ABE MANABU , HARADA JUN , KONO KEITA
发明人： UTO YOSHIKAZU , KIYOTSUKA YOHEI , KURATA HITOSHI , OGATA TSUNEAKI , OKUYAMA RYO , ABE MANABU , HARADA JUN , KONO KEITA
IPC分类号： C07D277/20 , A61K31/426 , A61K31/433 , A61K31/5377 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P7/00 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/12 , A61P15/00 , A61P19/02 , A61P19/06 , A61P25/00 , A61P25/04 , A61P27/02 , A61P27/12 , A61P43/00 , C07D277/46 , C07D277/56 , C07D285/12 , C07D285/135 , C07D333/36
CPC分类号： C07D277/46 , C07D277/20 , C07D277/56 , C07D285/12 , C07D285/135 , C07D333/36
摘要： Disclosed is an amide derivative having an excellent SCD inhibitory activity or a pharmacologically acceptable salt thereof. Specifically disclosed is an amide derivative represented by the general formula (I) below, or a pharmacologically acceptable salt thereof. [chemical formula 1] (I) (In the formula, R 1 represents a hydroxy group, a C 1 -C 6 alkoxy group, a C 2 -C 6 hydroxyalkoxy group or the like; R 2 represents a hydroxy group, a C 1 -C 6 alkoxy group, a C 2 -C 6 hydroxyalkoxy group or the like; R 3 represents a hydrogen atom or the like; R 4 represents a C 6 -C 10 aryl group which may be substituted at one to five positions independently by a group selected from the substituent group A, or the like; V represents a group represented by the formula: -NH- or a single bond; W represents a group represented by the formula: -NH- or a single bond; T represents a group represented by the formula: =C(R 5 )- or a nitrogen atom; and Q represents a group represented by the formula: =C(R 6 )- or a nitrogen atom.)
摘要翻译：公开了具有优异的SCD抑制活性的酰胺衍生物或其药理学上可接受的盐。具体公开了下述通式（I）表示的酰胺衍生物或其药理学上可接受的盐。 [化学式1]（I）（式中，R 1表示羟基，C 1 -C 6烷氧基， C 2 -C 6羟基烷氧基等; R 2表示羟基，C 1〜 C 6 -C 6烷氧基，C 2 -C 6羟基烷氧基等; R 3表示氢原子等; R 4表示可以在一至五个位置上独立地被一个或多个取代基取代的C 6 -C 10芳基，选自取代基A等的基团; V表示由式-NH-或单键表示的基团; W表示由下式表示的基团：-NH-或单键; T表示基团由式：= C（R 5） - 或氮原子表示; Q表示由下式表示的基团：= C（R 6） - 或氮原子）

2. 发明公开

EP1291430A4 CERAMIDE KINASE AND DNA ENCODING THE SAME 审中-公开
标题翻译： CERAMIDKINASE UNDDAFÜRKODIERENDE DNS
公开(公告)号：EP1291430A4
公开(公告)日：2004-06-30
申请号：EP01936941
申请日：2001-06-11
申请人： SANKYO CO
发明人： SUGIURA MASAKO , KONO KEITA , KOHAMA TAKAFUMI
IPC分类号： A61K31/7125 , A61P3/04 , A61P3/10 , A61P7/00 , A61P25/00 , A61P29/00 , A61P31/18 , A61P35/00 , C12N1/21 , C12N9/12 , C12N15/54 , A61K48/00 , C07K16/40 , C12Q1/48
CPC分类号： C12N9/1205 , A61K31/7125
摘要： A novel protein having a ceramide kinase activity which would be usable as a target of preventives or remedies for nerve diseases, inflammation, HIV, type 2 diabetes, obesity, sepsis, arteriosclerosis and cancer. More particularly, a protein comprising the amino acid sequence represented by amino acid nos. 1 to 537 in SEQ ID NO:2 in Sequence Listing; a DNA encoding this protein; a recombinant DNA vector containing this DNA; a host transformed by this recombinant DNA vector; a process for producing the above ceramide kinase and use of this protein. Use of this process makes it possible to search for novel compounds having an activity of specifically activating or inhibiting ceramide kinase and being useful as remedies for nerve diseases, anti-inflammatory agents, remedies for HIV, anti-type 2 diabetic agents, antiobestic agents, antiseptic agents, antiarteriosclerotic agents and carcinostatic agents.
摘要翻译：具有神经酰胺激酶活性的新型蛋白质，可用作神经疾病，炎症，HIV，2型糖尿病，肥胖症，败血症，动脉硬化症和癌症的预防或治疗的靶标。更特别地，包含由氨基酸编号代表的氨基酸序列的蛋白质。序列表中SEQ ID NO：2的1至537位; 编码这种蛋白质的DNA; 含有该DNA的重组DNA载体; 该重组DNA载体转化的宿主; 生产上述神经酰胺激酶的方法和该蛋白质的用途。该方法的使用使得可以寻找具有特异性激活或抑制神经酰胺激酶活性并可用作神经疾病治疗剂的新化合物，抗炎剂，HIV治疗剂，抗2型糖尿病剂，抗肥胖剂，防腐剂，抗动脉硬化剂和抗癌剂。

3. 发明专利

AU2002349676A1 4-OXOQUINOLINE DERIVATIVES 未知
公开(公告)号：AU2002349676A1
公开(公告)日：2003-06-10
申请号：AU2002349676
申请日：2002-11-19
申请人： SANKYO CO
发明人： HASEGAWA TOHRU , IKEDA TAKUYA , KONO KEITA , KURATA HITOSHI
IPC分类号： A61P3/06 , A61P9/10 , A61P43/00 , C07D215/56 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/4995 , A61K31/675 , C07D401/12 , C07D409/12 , C07D487/08

4. 发明专利

AU6273401A Ceramide kinase and dna encoding the same 未知
公开(公告)号：AU6273401A
公开(公告)日：2001-12-24
申请号：AU6273401
申请日：2001-06-11
申请人： SANKYO CO
发明人： SUGIURA MASAKO , KONO KEITA , KOHAMA TAKAFUMI
IPC分类号： A61K31/7125 , A61P3/04 , A61P3/10 , A61P7/00 , A61P25/00 , A61P29/00 , A61P31/18 , A61P35/00 , C12N1/21 , C12N9/12 , C12N15/54 , A61K48/00 , C07K16/40 , C12Q1/48

5. 发明专利

NO20003773L 未知
公开(公告)号：NO20003773L
公开(公告)日：2001-01-23
申请号：NO20003773
申请日：2000-07-21
申请人： SANKYO CO
发明人： KURATA HITOSHI , KOHAMA TAKAFUMI , KONO KEITA , KITAYAMA KEN
IPC分类号： C07C211/43 , A61K31/13 , A61K31/133 , A61K31/135 , A61K31/137 , A61K31/196 , A61K31/4409 , A61P3/06 , A61P9/10 , A61P35/00 , C07C211/40 , C07C211/45 , C07C211/50 , C07C225/20 , C07C229/16 , C07C233/40 , C07C233/42 , C07C233/44 , C07C233/78 , C07C239/16 , C07C251/48 , C07C309/14 , C07C323/32 , C07D209/14 , C07D209/16 , C07D213/06 , C07D213/38 , C07D213/74 , C07D333/10 , C07D333/20 , C07D333/36 , C07C219/00
摘要： Compounds of formula (I): Çin which: R and R each represents a variety of organic groups; R and R each represents hydrogen or a variety of organic groups; A represents a group of formula (A-1): in which: R represents hydrogen, hydroxy or alkyl, R represents hydroxy, alkoxy, alkylthio or an amine residue, X and Y each represents oxygen or sulphur, and Z represents a direct single bond between the nitrogen atom shown and the benzene ring shown in formula (I), or an alkylene group, G represents a single bond, alkylene or substituted alkylene; the broken line represents a single or double bond; when the broken line represents a double bond, D represents a carbon atom; and E represents an =N-O- group; when the broken line represents a single bond, D represents a CH group or a nitrogen atom, and E represents an oxygen atom, a sulphur atom, an -NH- group or a -CO- group; and pharmaceutically acceptable salts, esters or other derivatives thereof have the ability to inhibit an ileal bile transporter and so may be used to treat or prevent hypercholesterolaemia.

7. 发明专利

AU1302301A Nitrogenous heterocycle derivatives 未知
公开(公告)号：AU1302301A
公开(公告)日：2001-06-06
申请号：AU1302301
申请日：2000-11-08
申请人： SANKYO CO
发明人： KURATA HITOSHI , KOHAMA TAKAFUMI , KONO KEITA , KITAYAMA KEN , HASEGAWA TOHRU
IPC分类号： A61K31/47 , A61P3/06 , A61P9/10 , A61P43/00 , C07D215/56 , A61K31/4709 , A61K31/5377 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04

8. 发明专利

NZ505927A Cyclobutene-1,2-dione derivatives for use in the inhibition of an ileal bile acid transporter 未知
公开(公告)号：NZ505927A
公开(公告)日：2001-05-25
申请号：NZ50592700
申请日：2000-07-21
申请人： SANKYO CO
发明人： KONO KEITA , KITAYAMA KEN , KURATA HITOSHI , KOHAMA TAKAFUMI
IPC分类号： C07C211/43 , A61K31/13 , A61K31/133 , A61K31/135 , A61K31/137 , A61K31/196 , A61K31/4409 , A61P3/06 , A61P9/10 , A61P35/00 , C07C211/40 , C07C211/45 , C07C211/50 , C07C225/20 , C07C229/16 , C07C233/40 , C07C233/42 , C07C233/44 , C07C233/78 , C07C239/16 , C07C251/48 , C07C309/14 , C07C323/32 , C07D209/14 , C07D209/16 , C07D213/06 , C07D213/38 , C07D213/74 , C07D333/10 , C07D333/20 , C07D333/36 , C07D211/68
摘要： A compound of the Formula (I) for use in the manufacture of medicaments for treating hypercholesterolaemia and for inhibition of an ileal bile acid transporter. Wherein; R1 represents a cycloalkyl group, an aryl group, a heterocyclic group, a cycloalkyl group substituted by at least one of substituents a and b, an aryl group substituted by at least one of substituents a and b, or a heterocyclic group substituted by at least one of substituents a and b; R2 represents a cycloalkyl group, an aryl group, a heterocyclic group, a cycloalkyl group substituted by at least one of substituents a, an aryl group substituted by at least one of substituents a, or a heterocyclic group substituted by at least one of substituents a; R3 and R4 are the same as or different from each other and each represents a hydrogen atom or one of substituents a; A represents a group of Formula (A-1); wherein R5 represents a hydrogen atom, a hydroxy group or a lower alkyl group, R6 represents a hydroxy group, a lower alkoxy group, a lower alkylthio group or an amine residue, X and Y are the same as or different from each other and each represents an oxygen atom or a sulphur atom, and Z represents a direct single bond between the nitrogen atom shown and the benzene ring shown in Formula (I), or an alkylene group having from 1 to 6 carbon atoms; G represents a single bond, an alkylene group having from 1 to 6 carbon atoms or an alkylene group having from 1 to 6 carbon atoms and substituted by at least one of substituents g; The broken line represents a single or double bond; When the broken line represents a double bond; D represents a carbon atom; E represents an =N-O- group; When the broken line represents a single bond; D represents a CH group or a nitrogen atom, and E represents an oxygen atom, a sulphur atom, an -NH- group or a -CO- group; The substituents a are selected from halogen atoms, hydroxy groups, cyano groups, nitro groups, lower alkyl groups, lower halo alkyl groups, lower alkoxy groups, lower alkylthio groups, amino groups, lower mono-alkyl amino groups and di(lower alkyl)amino groups. The substituents b are selected from carboxy groups, lower alkoxycarbonyl groups, carbamoyl groups, lower monoalkylcarbamoyl groups, di(lower alkyl)carbamoyl groups, nitro groups, cycloalkyl groups, aryl groups, aryloxy groups, aralkyloxy groups, arylthio groups and cycloalkyl, aryl, aryloxy, aralkyloxy and arylthio groups each substituted by at least one of substituents a; The substituents g are selected from hydroxy groups, oxo groups, cycloalkyl groups, aryl groups, heterocyclic groups, cycloalkyl groups substituted by at least one of substituents a and b, aryl groups substituted by at least one of substituents a and b, and heterocyclic groups substituted by at least one of substituents a and b.

9. 发明专利

AU4875600A Cyclobutene derivatives, their preparation and their therapeutic uses 未知
公开(公告)号：AU4875600A
公开(公告)日：2001-02-01
申请号：AU4875600
申请日：2000-07-21
申请人： SANKYO CO
发明人： KURATA HITOSHI , KOHAMA TAKAFUMI , KONO KEITA , KITAYAMA KEN
IPC分类号： C07C211/43 , A61K31/13 , A61K31/133 , A61K31/135 , A61K31/137 , A61K31/196 , A61K31/4409 , A61P3/06 , A61P9/10 , A61P35/00 , C07C211/40 , C07C211/45 , C07C211/50 , C07C225/20 , C07C229/16 , C07C233/40 , C07C233/42 , C07C233/44 , C07C233/78 , C07C239/16 , C07C251/48 , C07C309/14 , C07C323/32 , C07D209/14 , C07D209/16 , C07D213/06 , C07D213/38 , C07D213/74 , C07D333/10 , C07D333/20 , C07D333/36 , C07C229/08 , C07D213/36 , C07D209/04 , A61K31/381 , A61K31/34 , A61K31/403 , A61K31/44 , A61P1/16
摘要： Compounds of formula (I): Çin which: R and R each represents a variety of organic groups; R and R each represents hydrogen or a variety of organic groups; A represents a group of formula (A-1): in which: R represents hydrogen, hydroxy or alkyl, R represents hydroxy, alkoxy, alkylthio or an amine residue, X and Y each represents oxygen or sulphur, and Z represents a direct single bond between the nitrogen atom shown and the benzene ring shown in formula (I), or an alkylene group, G represents a single bond, alkylene or substituted alkylene; the broken line represents a single or double bond; when the broken line represents a double bond, D represents a carbon atom; and E represents an =N-O- group; when the broken line represents a single bond, D represents a CH group or a nitrogen atom, and E represents an oxygen atom, a sulphur atom, an -NH- group or a -CO- group; and pharmaceutically acceptable salts, esters or other derivatives thereof have the ability to inhibit an ileal bile transporter and so may be used to treat or prevent hypercholesterolaemia.

10. 发明专利

ID26612A 未知
公开(公告)号：ID26612A
公开(公告)日：2001-01-25
申请号：ID20000613
申请日：2000-07-21
申请人： SANKYO CO
发明人： KURATA HITOSHI , KOHAMA TAKAFUMI , KONO KEITA , KITAYAMA KEN
IPC分类号： C07C211/43 , A61K31/13 , A61K31/133 , A61K31/135 , A61K31/137 , A61K31/196 , A61K31/4409 , A61P3/06 , A61P9/10 , A61P35/00 , C07C211/40 , C07C211/45 , C07C211/50 , C07C225/20 , C07C229/16 , C07C233/40 , C07C233/42 , C07C233/44 , C07C233/78 , C07C239/16 , C07C251/48 , C07C309/14 , C07C323/32 , C07D209/14 , C07D209/16 , C07D213/06 , C07D213/38 , C07D213/74 , C07D333/10 , C07D333/20 , C07D333/36
摘要： Compounds of formula (I): Çin which: R and R each represents a variety of organic groups; R and R each represents hydrogen or a variety of organic groups; A represents a group of formula (A-1): in which: R represents hydrogen, hydroxy or alkyl, R represents hydroxy, alkoxy, alkylthio or an amine residue, X and Y each represents oxygen or sulphur, and Z represents a direct single bond between the nitrogen atom shown and the benzene ring shown in formula (I), or an alkylene group, G represents a single bond, alkylene or substituted alkylene; the broken line represents a single or double bond; when the broken line represents a double bond, D represents a carbon atom; and E represents an =N-O- group; when the broken line represents a single bond, D represents a CH group or a nitrogen atom, and E represents an oxygen atom, a sulphur atom, an -NH- group or a -CO- group; and pharmaceutically acceptable salts, esters or other derivatives thereof have the ability to inhibit an ileal bile transporter and so may be used to treat or prevent hypercholesterolaemia.

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