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1. 发明申请

WO0250061A8 PIPERAZINE DERIVATIVES FOR TREATMENT OF BACTERIAL INFECTIONS 审中-公开
标题翻译：用于治疗细菌感染的哌啶衍生物
公开(公告)号：WO0250061A8
公开(公告)日：2002-07-25
申请号：PCT/GB0105653
申请日：2001-12-19
申请人： SMITHKLINE BEECHAM PLC , DARTOIS CATHERINE GENEVIEVE YV , MARKWELL ROGER EDWARD , MORVAN MARCEL , NADLER GUY MARGUERITE MARIE GE , PEARSON NEIL DAVID
发明人： DARTOIS CATHERINE GENEVIEVE YV , MARKWELL ROGER EDWARD , MORVAN MARCEL , NADLER GUY MARGUERITE MARIE GE , PEARSON NEIL DAVID
IPC分类号： A61K31/496 , A61K31/498 , A61K31/538 , A61K31/5415 , A61P31/04 , C07D401/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D417/06 , C07D417/12 , C07D471/04 , C07D401/14 , A61K31/495
CPC分类号： C07D401/12 , C07D405/12 , C07D409/06 , C07D417/06 , C07D471/04
摘要： Piperazine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man(represented by formula (I).
摘要翻译：哌嗪衍生物及其药学上可接受的衍生物可用于哺乳动物，特别是人类（由式（I）表示）的哺乳动物细菌感染的治疗方法。

2. 发明专利

BG101769A INDOLE DERIVATIVES USEFUL IN THE TREATMENT OF OSTEOPOROSIS 未知
公开(公告)号：BG101769A
公开(公告)日：1998-04-30
申请号：BG10176997
申请日：1997-07-07
申请人： FARINA CARLO , GAGLIARDI STEFANIA , PARINI CARLO , PINZA MARIO , NADLER GUY MARGUERITE MARIE G , MORVAN MARCEL JEAN-MARIE
发明人： FARINA CARLO , GAGLIARDI STEFANIA , PARINI CARLO , PINZA MARIO , NADLER GUY MARGUERITE MARIE G , MORVAN MARCEL JEAN-MARIE
IPC分类号： C07D487/04 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/475 , A61K31/495 , A61K31/50 , A61K31/505 , A61K31/535 , A61P3/06 , A61P7/00 , A61P19/10 , A61P25/28 , A61P31/12 , A61P31/18 , A61P35/00 , A61P37/00 , A61P37/04 , A61P43/00 , C07D209/18 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , C07D451/04 , C07D453/02 , C07D471/04 , C07D473/34 , C07D521/00 , C07F9/572 , C07D209/14 , C07D209/12
摘要： A compound of formulaor a salt thereof, or a solvate thereof, wherein either. (1) Rarepresents a group R5 which is hydrogen, alkyl or optionallysubstituted aryl and Rb represents a moiety of formula (a)wherein X represents a hydroxy or an alkoxy group wherein thealkyl group may be substituted or unsubstituted or X represents agroup NRsRt, wherein Rs, and Rt each independently representhydrogen, alkyl, substituted alkyl, optionally substitutedalkenyl, optionally substituted aryl, optionally substitutedarylalkyl, an optionally substituted heterocyclic group or anoptionally substituted heterocyclyhlkyl group, or Rs, and Rttogether may form a heterocyclic group; R1 represents an alkyl ora substituted or unsubstituted aryl group; and R2, R3 and R4 eachindependently represent hydrogen, alkyl, aryl or substituted arylor (2) Ra represents a moiety of the above defined formula (a) andRb represents the above defined R5, R6 and R7 each independentlyrepresents hydrogen, hydroxy, amino, alkoxy, optionallysubstituted aryloxy, optionally substituted benzyloxy, alkylamino,dialkylamino, halo, trifluoromethyl, trifluomnethoxy, nitro,alkyl, carboxy, carbalkoxy, carbamoyl, akylcarbamoyl, or R6 and R7together represent methylenedioxy, carbonyldioxy orcarbonyldiamino; and R8 represents hydrogen, hydroxy, alkanoyl,alkyl, aminoalkyl, hydroxyalkyl, carboxyalkyl, carbalkoxyalkyl,carbamoyl or aminosulphonyl; a process for the preparation of sucha compound, a pharmaceutical composition comprising such acompound and the use of such a compound in medicine.20 claims

3. 发明申请

WO2006058993A1 DERIVES D’ARYLPIPERAZINE ET LEUR UTILISATION COMME LIGANDS SELECTIFS DU RECEPTEUR D3 DE LA DOPAMINE 审中-公开
标题翻译： ARYLPIPERAZINE衍生物及其作为DOPAMINE D3受体选择的配体使用
公开(公告)号：WO2006058993A1
公开(公告)日：2006-06-08
申请号：PCT/FR2005/002964
申请日：2005-11-29
申请人： BIOPROJET , CAPET, Marc , DANVY, Denis , DARTOIS, Catherine , LEVOIN, Nicolas , MORVAN, Marcel , BERREBI-BERTRAND, Isabelle , CALMELS, Thierry , ROBERT, Philippe , SCHWARTZ, Jean-Charles , LECOMTE, Jeanne-Marie
发明人： CAPET, Marc , DANVY, Denis , DARTOIS, Catherine , LEVOIN, Nicolas , MORVAN, Marcel , BERREBI-BERTRAND, Isabelle , CALMELS, Thierry , ROBERT, Philippe , SCHWARTZ, Jean-Charles , LECOMTE, Jeanne-Marie
IPC分类号： C07D209/44 , C07D405/12
CPC分类号： C07D209/44 , C07D405/12
摘要： L'invention concerne des composés de formule générale (I): leur procédé de préparation, ainsi que leur utilisation en tant qu'agent thérapeutique.
摘要翻译：本发明涉及通式（I）的化合物，其制备方法及其作为治疗剂的用途。

4. 发明申请

WO1996021644A1 INDOLE DERIVATIVES USEFUL IN THE TREATMENT OF OSTEOPOROSIS 审中-公开
标题翻译：用于治疗OSTEOPOROSIS的单独使用衍生物
公开(公告)号：WO1996021644A1
公开(公告)日：1996-07-18
申请号：PCT/EP1996000157
申请日：1996-01-08
申请人： SMITHKLINE BEECHAM S.P.A. , FARINA, Carlo , GAGLIARDI, Stefania , PARINI, Carlo , PINZA, Mario , NADLER, Guy, Marguerite, Marie, Gérard , MORVAN, Marcel, Jean-Marie
发明人： SMITHKLINE BEECHAM S.P.A.
IPC分类号： C07D209/14
CPC分类号： C07D231/12 , C07D209/18 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , C07D451/04 , C07D453/02 , C07D471/04 , C07D473/34 , C07F9/5728
摘要： A compound of formula (I) or a salt thereof, or a solvate thereof, wherein either: (i) Ra represents a group R5 which is hydrogen, alkyl or optionally substituted aryl and Rb represents a moiety of formula (a); wherein X represents a hydroxy or an alkoxy group wherein the alkyl group may be substituted or unsubstituted or X represents a group NRsRt wherein Rs and Rt each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, an optionally substituted heterocyclic group or an optionally substituted heterocyclylalkyl group, or Rs and Rt together may form a heterocyclic group; R1 represents an alkyl or a substituted or unsubstituted aryl group; and R2, R3 and R4 each independently represent hydrogen, alkyl, aryl or substituted aryl or (ii) Ra represents a moiety of the above defined formula (a) and Rb represents the above defined R5; R6 and R7 each independently represents hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R6 and R7 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; and R8 represents hydrogen, hydroxy, alkanoyl, alkyl, aminoalkyl, hydroxyalkyl, carboxyalkyl, carbalkoxyalkyl, carbamoyl or aminosulphonyl; a process for the preparation of such a compound, a pharmaceutical composition comprising such a compound and the use of such a compound in medicine.
摘要翻译：式（I）化合物或其盐或其溶剂合物，其中：（i）Ra表示氢，烷基或任选取代的芳基的基团R 5，R b表示式（a）的部分; 其中X表示羟基或烷氧基，其中烷基可以是取代或未取代的或X表示基团NRsRt，其中R 5和R t各自独立地表示氢，烷基，取代的烷基，任选取代的烯基，任选取代的芳基，任选取代的芳基烷基，任选取代的杂环基或任选取代的杂环基烷基，或者R 1和R 2一起可以形成杂环基; R1表示烷基或取代或未取代的芳基; 并且R 2，R 3和R 4各自独立地表示氢，烷基，芳基或取代的芳基或（ii）R a表示上述定义的式（a）的部分，R b表示上述定义的R 5; R6和R7各自独立地表示氢，羟基，氨基，烷氧基，任选取代的芳氧基，任选取代的苄氧基，烷基氨基，二烷基氨基，卤素，三氟甲基，三氟甲氧基，硝基，烷基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基或R6和R7一起表示亚甲二氧基，羰基二氧基或羰基二氨基; R8代表氢，羟基，烷酰基，烷基，氨基烷基，羟基烷基，羧基烷基，碳烷氧基烷基，氨基甲酰基或氨基磺酰基; 制备这种化合物的方法，包含这种化合物的药物组合物和这种化合物在医药中的用途。

5. 发明申请

WO1994027967A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO1994027967A1
公开(公告)日：1994-12-08
申请号：PCT/EP1994001704
申请日：1994-05-24
申请人： SMITHKLINE BEECHAM LABORATOIRES PHARMACEUTIQUES , NADLER, Guy, Marguerite, Marie, Gérard , MORVAN, Marcel, Jean-Marie
发明人： SMITHKLINE BEECHAM LABORATOIRES PHARMACEUTIQUES
IPC分类号： C07D211/58
CPC分类号： C07D401/06 , C07D211/58 , C07D401/12 , C07D405/12 , C07D409/12
摘要： A compound of formula (I) or a salt thereof, or a solvate thereof, wherein A represents (CH2)n wherein n represents zero or an integer 1 or 2; B represents a C2-4n-alkylene group wherein each carbon is optionally substituted by a C1-6alkyl group; Z represents a bond (CH2)m wherein m is an integer in the range of from 1 to 4 or X-CH2-CH2 wherein X represents O or S; D represents CO, SO2, NH-CO, NH-SO2, -CH=CH- or P(O)OR4 wherein R4 is C1-6alkyl; Q represents aryl, aralkyl, aralkenyl or aralkynyl, wherein the aryl moiety may be substituted or unsubstituted with 1 to 5 substituents selected from the list consisting of nitro, halogen, alkylsulfonamide, 1-imidazo, alkyl or haloalkyl, or Q represents substituted furanyl, substituted thienyl or substituted or unsubstituted: pyranyl, thiazolyl, imidazolyl, triazolyl or the benzo fused equivalents of furanyl, pyranyl, thienyl, thiazolyl, imidazolyl or triazolyl, indolyl, oxoindolyl, indenyl, isoindenyl, indazolyl, indolizinyl or pyridinyl or cycloalkyl optionally fused to an aryl group; R1, R2 and R3 each independently represent H, alkyl, OH or alkoxy or, if attached to adjacent carbon atoms, any two of R1, R2 or R3 together with the carbon atoms to which they are attached may form a fused heterocyclic ring of four to six atoms wherein one, two or three of the said atoms are oxygen or nitrogen; and Ar represents substituted or unsubstituted aryl, wherein the optional substituents are the above defined R1, R2 and R3 or Ar represents a substituted or unsubstituted heteroaryl group; a process for preparing such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译：式（I）化合物或其盐或其溶剂化物，其中A表示（CH 2）n，其中n表示0或整数1或2; B表示C2-4n-亚烷基，其中每个碳任选被C 1-6烷基取代; Z表示键（CH 2）m，其中m是1至4的整数或X-CH 2 -CH 2，其中X表示O或S; D表示CO，SO 2，NH-CO，NH-SO 2，-CH = CH-或P（O）OR 4，其中R 4是C 1-6烷基; Q表示芳基，芳烷基，芳烯基或芳炔基，其中芳基部分可以被1至5个选自硝基，卤素，烷基磺酰胺，1-咪唑基，烷基或卤代烷基的取代基取代或未取代，或Q表示取代的呋喃基，取代或未取代的：吡喃基，噻唑基，咪唑基，三唑基或呋喃基，吡喃基，噻吩基，噻唑基，咪唑基或三唑基，吲哚基，氧代吲哚基，茚基，异吲哚基，吲唑基，中氮茚基或吡啶基或环烷基的苯并稠合当量。芳基; R 1，R 2和R 3各自独立地表示H，烷基，OH或烷氧基，或者如果连接到相邻的碳原子上，R 1，R 2或R 3中的任何两个与它们所连接的碳原子一起可以形成四个稠合杂环至六个原子，其中一个，两个或三个所述原子是氧或氮; 并且Ar表示取代或未取代的芳基，其中任选的取代基是上述定义的R 1，R 2和R 3或Ar表示取代或未取代的杂芳基; 制备这种化合物的方法，包含这些化合物的药物组合物和这些化合物在医药中的用途。

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