专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

41. 发明申请

WO2004076407A2 PYRROLIDINE DERIVATIVES AS OXYTOCIN ANTAGONISTS 审中-公开
标题翻译：吡咯啉衍生物作为氧化物拮抗剂
公开(公告)号：WO2004076407A2
公开(公告)日：2004-09-10
申请号：PCT/EP2004/050142
申请日：2004-02-16
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , SCHWARZ, Matthias , JORAND-LEBRUN, Catherine , VALOGNES, Delphine
发明人： SCHWARZ, Matthias , JORAND-LEBRUN, Catherine , VALOGNES, Delphine
IPC分类号： C07D
CPC分类号： C07D413/06 , C07D207/22
摘要： The present invention relates to novel pyrrolidine derivatives of Formula (I), its geometrical isomers, its optically active forms as enantiomers, diastercomers, mixtures of these and its racemate forms, as well as salts thereof, wherein: R 1i s selected from the group comprising or consisting of H and C 1 -C 6 -alkyl; R 2 is selected from the group comprising or consisting of hydrogen, C I -C 6 -alkyl, C I -C 6 alkyl aryl, heteroaryl, C I -C 6 alkyl heteroaryl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkenyl aryl, C 2 -C 6 alkenyl heteroaryl, C 2 -C 6 -alkynyl, C 2 -C 6 -alkynyl aryl, C 2 C 6 -alkynyl heteroaryl, C 3 -C 8 cycloalkyl, heterocycloalkyl, CI-C6-alkyl cycloallcyl, CI-C6-alkyI heterocycloalkyl, CIC6 alkyl carboxy, acyl, C I -C 6 -alkyl acyl, C I -C 6 -alkyl acyloxy, C I -C 6 -alkyl alkoxy, alkoxycarbonyl, C I -C 6 -alkyI alkoxycarbonyl, aminocarbonyl, C I -C 6 -alkyl aminocarbonyl, C I -C 6 -alkyl acylarnino, C I -C 6 -alkyl ureido, amino, C I -C 6 alkyl amino, sulfonyloxy, C I -C 6 alkyl sulfonyloxy, sulfonyl, C I -C 6 -alkyl sulfonyl, sulfinyl, C I -C 6 -alkyl sulfinyl, C I -C 6 alkyl sulfanyl, C I -C 6 -alkyl sulfonylamino;
摘要翻译：本发明涉及式（I）的新型吡咯烷衍生物，其几何异构体，其作为对映体的光学活性形式，diastercomers，它们的混合物及其外消旋体形式，以及其盐，其中：R 1选自由H和C 1 -C 6烷基组成或由其组成的基团; R 2选自氢，C 1 -C 6 - 烷基，C 1 -C 6烷基芳基，杂芳基，C 1 -C 6烷基杂芳基，C 2 -C 6 - 烯基，C 2 -C 6 - 链烯基芳基， C 1 -C 6烷基杂芳基，C 2 -C 6炔基，C 2 -C 6炔基芳基，C 2 -C 6炔基杂芳基，C 3 -C 8环烷基，杂环烷基， C 1-6烷基酰氧基，C 1 -C 6烷基烷氧基，烷氧基羰基，C 1 -C 6烷基烷氧基羰基，氨基羰基，C 1 -C 6烷基氨基羰基，C 1 -C 6烷基酰基氨基，C 1 -C 6烷基脲基，氨基，C1-C6烷基氨基，磺酰氧基，C1-C6烷基磺酰氧基，磺酰基，C1-C6烷基磺酰基，亚磺酰基，C1-C6烷基亚磺酰基，C1-C6烷基硫烷基，C1-C6烷基磺酰基氨基;

42. 发明申请

WO2004071390A3 PIPERAZINE-2-CARBOXAMIDE DERIVATIVES 审中-公开
公开(公告)号：WO2004071390A3
公开(公告)日：2004-08-26
申请号：PCT/EP2004/050093
申请日：2004-02-06
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , PAGE, Patrick , JORAND-LEBRUN, Catherine , THOMAS, Russel J. , SCHWARZ, Matthias
发明人： PAGE, Patrick , JORAND-LEBRUN, Catherine , THOMAS, Russel J. , SCHWARZ, Matthias
IPC分类号： A61K31/495
摘要： The present invention is related to piperazine -2-carboxamide derivatives of formula (I) for the treatment and/or prophylaxis of preterm labor, premature birth, dysmenorrhea and for stopping labor prior to cesarean delivery. Wherein A, X, Y, R 1 and R 2 are as defined in the description.

43. 发明申请

WO1997028141A1 NOVEL AROMATIC PIPERAZINES DERIVED FROM SUBSTITUTED CYCLOAZANES, METHOD FOR PREPARING SAME, PHARMACEUTICAL COMPOSITIONS, AND USE THEREOF AS DRUGS 审中-公开
标题翻译：从取代的环孢菌素衍生的新型芳香哌嗪，其制备方法，药物组合物及其作为药物的用途
公开(公告)号：WO1997028141A1
公开(公告)日：1997-08-07
申请号：PCT/FR1997000203
申请日：1997-02-03
申请人： PIERRE FABRE MEDICAMENT , HALAZY, Serge , JORAND-LEBRUN, Catherine , PAUWELS, Peter , CHOPIN, Philippe , MARIEN, Marc
发明人： PIERRE FABRE MEDICAMENT
IPC分类号： C07D295/20
CPC分类号： C07D295/205 , C07D211/16 , C07D211/22 , C07D211/26 , C07D211/32 , C07D211/46 , C07D211/58 , C07D211/70 , C07D243/08 , C07D295/215
摘要： Compounds of formula (I), wherein R1 is hydrogen or straight or branched C1-6 alkyl, Z2 is O, NH, CH2O or CH2NH, each of R2 and R3, which are the same or different, is hydrogen or a group selected from straight or branched alkyl, alkoxy, thioether, nitrile, trifluoromethyl or halogen (F, Cl, Br, I), or, when they are adjacent, R2 and R3, taken together, form a 5- or 6-membered ring in order to form, e.g., naphthyl, tetrahydronaphthyl, benzopyrane or benzodioxane, X-Y is NCH2, CH-CH2, C=CH, N or NCH2CH2, and Z1 is -(CH2)n, -(CH2)n CO-, -CO-, -CO(CH2)n-, -SO2-, -SO2(CH2)n-, -O(CH2)n-, -O(CH2)nCO-, -OCO-, -NH(CH2)n-, -NH(CH2)nCO-, -NHCO-, -NHCO(CH2)n-, -NH(CH2)nSO2-, -NHSO2-, -NHSO2(CH2)n-, -CH=CHCO-, -CCCO- -(CH2)nSO2-, -O(CH2)nSO2-.
摘要翻译：式（I）化合物，其中R 1是氢或直链或支链C 1-6烷基，Z 2是O，NH，CH 2 O或CH 2 NH，R 2和R 3各自相同或不同，是氢或选自直链或支链烷基，烷氧基，硫醚，腈，三氟甲基或卤素（F，Cl，Br，I），或者当它们相邻时，R 2和R 3一起形成5-或6-元环，以便形式，例如萘基，四氢萘基，苯并吡喃或苯并二恶烷，XY是NCH 2，CH-CH 2，C = CH，N或NCH 2 CH 2，且Z 1是 - （CH 2）n - ， - （CH 2）n CO-，-CO-， CO（CH 2）n - ，-SO 2 - ， - SO 2（CH 2）n - ， - O（CH 2）n - ， - O（CH 2）n CO-， - OCO-， - NH （CH 2）n - ，（CH 2）n - ，（CH 2）n - ， - CH 2 - nSO 2 - ， - O（CH 2）n SO 2 - 。

44. 发明申请

WO2020181283A1 CARBOXAMIDE-PYRIMIDINE DERIVATIVES AS SHP2 ANTAGONISTS 审中-公开
公开(公告)号：WO2020181283A1
公开(公告)日：2020-09-10
申请号：PCT/US2020/021726
申请日：2020-03-09
申请人： MERCK PATENT GMBH , JORAND-LEBRUN, Catherine , BOIVIN, Roch , MOCHALKIN, Igor , JOHNSON, Theresa , LINDE, Nina , MUSCH, Doreen , KUMAR, Deepak
发明人： JORAND-LEBRUN, Catherine , BOIVIN, Roch , MOCHALKIN, Igor , JOHNSON, Theresa , LINDE, Nina , MUSCH, Doreen , KUMAR, Deepak
IPC分类号： C07D401/04 , C07D403/04 , C07D239/42 , C07D405/14 , C07D413/04 , C07D491/107 , A61P35/00 , A61K31/506 , C07D451/14
摘要： The invention relates to carboxamide-pyrimidine derivatives of the general formula (I), or a pharmaceutically acceptable salt thereof, and the use of the compounds of the present invention for the treatment of hyperproliferative diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.

45. 发明申请

WO2016127025A1 MACROCYCLIC COMPOUNDS AS IRAK1/4 INHIBITORS AND USES THEREOF 审中-公开
标题翻译：大环化合物作为IRAK1 / 4抑制剂及其用途
公开(公告)号：WO2016127025A1
公开(公告)日：2016-08-11
申请号：PCT/US2016/016709
申请日：2016-02-05
申请人： MERCK PATENT GMBH , CHEN, Xiaoling , YU, Henry , LAN, Ruoxi , JORAND-LEBRUN, Catherine , JOHNSON, Theresa L. , GOUTOPOULOS, Andreas
发明人： CHEN, Xiaoling , YU, Henry , LAN, Ruoxi , JORAND-LEBRUN, Catherine , JOHNSON, Theresa L. , GOUTOPOULOS, Andreas
IPC分类号： C07D487/18 , A61P35/00
CPC分类号： C07D471/22 , C07D487/18 , C07D498/18 , C07D498/22 , C07D513/22
摘要： The present invention relates to compounds of Formula (I) and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors. Wherein: Ring A is a 5-membered heterocylic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5- membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each of which is optionally substituted; Ring B is a 6-membered aryl, or a 6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each of which is optionally substituted; Ring C is a 5-membered heterocylic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5- membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each of which is optionally substituted.
摘要翻译：本发明涉及可用作IRAK抑制剂的式（I）化合物及其药学上可接受的组合物。其中环A是具有1-4个独立地选自氮，氧或硫的杂原子的5元杂环，或具有1-4个独立地选自氮，氧或硫的杂原子的5-元单环杂芳基环; 它们各自任选被取代; 环B是6元芳基或具有1-4个独立地选自氮，氧或硫的杂原子的6元单环杂芳基环; 它们各自任选被取代; 环C是具有1-4个独立地选自氮，氧或硫的杂原子的5元杂环，或具有1-4个独立地选自氮，氧或硫的杂原子的5-元单环杂芳基环; 它们各自任选被取代。

46. 发明申请

WO2010100144A1 FUSED BICYCLIC COMPOUNDS AS INHIBITORS FOR PI3 KINASE 审中-公开
标题翻译：作为PI3激酶抑制剂的熔融双相化合物
公开(公告)号：WO2010100144A1
公开(公告)日：2010-09-10
申请号：PCT/EP2010/052615
申请日：2010-03-02
申请人： MERCK SERONO S.A. , SWINNEN, Dominique , JORAND-LEBRUN, Catherine , GRIPPI-VALLOTTON, Tania , GERBER, Patrick , GONZALEZ, Jerome , SHAW, Jeffrey , JEYAPRAKASHNARAYANAN, Seenisamy
发明人： SWINNEN, Dominique , JORAND-LEBRUN, Catherine , GRIPPI-VALLOTTON, Tania , GERBER, Patrick , GONZALEZ, Jerome , SHAW, Jeffrey , JEYAPRAKASHNARAYANAN, Seenisamy
IPC分类号： C07D277/82 , C07D417/04 , C07D419/12 , C07D471/04 , C07D487/04 , A61K31/428 , A61K31/415 , A61K31/44 , A61P29/00
CPC分类号： C07D277/82 , C07D417/04 , C07D419/12 , C07D471/04 , C07D487/04
摘要： The invention relates to compounds of formula (I) for the regulation of phosphoinositides 3-kinases activity and related diseases.
摘要翻译：本发明涉及用于调节磷酸肌醇3-激酶活性和相关疾病的式（I）化合物。

47. 发明申请

WO2010092043A1 PHENOXY ACETIC ACID DERIVATIVES 审中-公开
标题翻译：苯氧乙酸衍生物
公开(公告)号：WO2010092043A1
公开(公告)日：2010-08-19
申请号：PCT/EP2010/051567
申请日：2010-02-09
申请人： MERCK SERONO S.A. , CROSIGNANI, Stefano , JORAND-LEBRUN, Catherine , CLEVA, Christophe , PRETRE, Adeline
发明人： CROSIGNANI, Stefano , JORAND-LEBRUN, Catherine , CLEVA, Christophe , PRETRE, Adeline
IPC分类号： C07C59/70 , A61P7/06 , A61P37/00 , A61P25/28 , A61P17/00 , A61K31/192 , C07D213/30 , C07D213/65 , C07D213/71 , C07D213/76 , C07D233/64 , C07D277/24 , C07D333/28 , C07D401/12 , C07D295/096
CPC分类号： C07D233/64 , C07C59/70 , C07C233/25 , C07C233/75 , C07C235/42 , C07C255/54 , C07C311/08 , C07C311/29 , C07C317/22 , C07C317/40 , C07C317/46 , C07C2601/08 , C07D205/04 , C07D213/30 , C07D213/64 , C07D213/65 , C07D213/71 , C07D213/76 , C07D213/89 , C07D231/12 , C07D233/22 , C07D275/06 , C07D277/24 , C07D295/096 , C07D295/192 , C07D295/26 , C07D333/28 , C07D333/54 , C07D333/64 , C07D333/76 , C07D401/12
摘要： The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses.
摘要翻译：本发明提供式（I）的苯氧基乙酸衍生物用于治疗CRTH2相关疾病和选自哮喘，特应性皮炎和炎性皮肤病的疾病。

48. 发明申请

WO2005097773A1 1,1’-(1,2-ETHYNEDIYL)BIS-BENZENE DERIVATIVES AS PTP 1-B INHIBITORS 审中-公开
标题翻译： 1,1' - （1,2-ETHYNEDIYL）BIS-BENZENE衍生物作为PTP 1-B抑制剂
公开(公告)号：WO2005097773A1
公开(公告)日：2005-10-20
申请号：PCT/EP2005/051426
申请日：2005-03-29
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , SWINNEN, Dominique , JORAND-LEBRUN, Catherine , GERBER, Patrick , GONZALEZ, Jérôme , BOMBRUN, Agnès
发明人： SWINNEN, Dominique , JORAND-LEBRUN, Catherine , GERBER, Patrick , GONZALEZ, Jérôme , BOMBRUN, Agnès
IPC分类号： C07D333/34
CPC分类号： C07D319/08 , A61K38/28 , C07C33/28 , C07C51/31 , C07C63/66 , C07C65/28 , C07C67/343 , C07C69/76 , C07C211/29 , C07C217/58 , C07C229/38 , C07C229/60 , C07C229/64 , C07C233/31 , C07C233/81 , C07C233/87 , C07C235/46 , C07C235/84 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/42 , C07C311/04 , C07C311/13 , C07C311/19 , C07C311/21 , C07C311/29 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D333/34
摘要： The present invention is related to carboxylic acids of Formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of carboxylic acids of Formula (I) to modulate, notably to inhibit the activity of PTPs.
摘要翻译：本发明涉及式（I）的羧酸及其用于治疗和/或预防由胰岛素抵抗或高血糖介导的肥胖和/或代谢障碍的用途，其包括I型和/或II型糖，葡萄糖耐量不足，胰岛素抵抗，高脂血症，高甘油三酯血症，高胆固醇血症，多囊卵巢综合征（PCOS）。特别地，本发明涉及式（I）的羧酸的用途，特别是抑制PTP的活性。

49. 发明申请

WO2004071390A2 PIPERAZINE-2-CARBOXAMIDE DERIVATIVES 审中-公开
标题翻译：哌嗪-2-羧酰胺衍生物
公开(公告)号：WO2004071390A2
公开(公告)日：2004-08-26
申请号：PCT/EP2004050093
申请日：2004-02-06
申请人： APPLIED RESEARCH SYSTEMS , PAGE PATRICK , JORAND-LEBRUN CATHERINE , THOMAS RUSSEL J , SCHWARZ MATTHIAS
发明人： PAGE PATRICK , JORAND-LEBRUN CATHERINE , THOMAS RUSSEL J , SCHWARZ MATTHIAS
IPC分类号： A61K6/00 , A61K31/16 , A61K31/495 , A61P15/06 , C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D521/00 , A61K
CPC分类号： C07D231/12 , A61K31/16 , A61K31/495 , C07D233/56 , C07D241/04 , C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
摘要： The present invention is related to piperazine -2-carboxamide derivatives of formula (I) for the treatment and/or prophylaxis of preterm labor, premature birth, dysmenorrhea and for stopping labor prior to cesarean delivery. Wherein A, X, Y, R and R are as defined in the description.
摘要翻译：本发明涉及式（I）的哌嗪-2-甲酰胺衍生物，其用于治疗和/或预防早产，早产，痛经和用于在剖宫产分娩前停止劳动。其中A，X，Y，R 1和R 2如说明书中所定义。

50. 发明申请

WO2017049068A1 HETEROARYL COMPOUNDS AS IRAK INHIBITORS AND USES THEREOF 审中-公开
标题翻译：杂芳基化合物作为IRAK抑制剂及其用途
公开(公告)号：WO2017049068A1
公开(公告)日：2017-03-23
申请号：PCT/US2016/052104
申请日：2016-09-16
申请人： MERCK PATENT GMBH , JORAND-LEBRUN, Catherine , LAN, Ruoxi , CHEN, Austin , CLARK, Ryan C.
发明人： JORAND-LEBRUN, Catherine , LAN, Ruoxi , CHEN, Austin , CLARK, Ryan C.
IPC分类号： C07D413/14 , C07D491/08 , C07D403/04 , C07D413/04 , C07D417/04 , C07D487/08 , A61K31/4184 , A61P35/00 , A61P29/00
CPC分类号： C07D413/14 , A61K31/4184 , C07D401/04 , C07D403/04 , C07D413/04 , C07D417/04 , C07D471/08 , C07D487/08 , C07D491/08 , C07D498/08
摘要： The present invention relates to compounds of Formula (I) and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.
摘要翻译：本发明涉及用作IRAK抑制剂的式（I）化合物及其药学上可接受的组合物。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式