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1. 发明申请

US20050026985A1 Pharmaceutically active compounds and methods of use 失效
标题翻译：药物活性化合物和使用方法
公开(公告)号：US20050026985A1
公开(公告)日：2005-02-03
申请号：US10921471
申请日：2004-08-19
申请人： Hitesh Shroff , Adulla Reddy , Nabil El Tayar , Nadia Brugger , Catherine Jorand-Lebrun , Giampiero de Luca
发明人： Hitesh Shroff , Adulla Reddy , Nabil El Tayar , Nadia Brugger , Catherine Jorand-Lebrun , Giampiero de Luca
IPC分类号： C07D231/12 , A61K31/415 , A61K31/4155 , A61K31/4439 , A61K31/4545 , A61K31/4725 , A61K31/497 , A61P5/34 , A61P15/08 , A61P43/00 , C07D401/04 , C07D401/14 , C07D403/14 , C07D405/04 , C07D409/14 , A61K31/416
CPC分类号： C07D401/04 , A61K31/415 , A61K31/4155 , A61K31/4439 , A61K31/4725 , C07D409/14
摘要： The invention provides substituted pyrazole compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for the treatment of mammalian infertility.
摘要翻译：本发明提供取代的吡唑化合物，以及使用或包含一种或多种这类化合物的治疗方法和药物组合物。本发明的化合物可用于治疗哺乳动物不育症。

2. 发明授权

US08404690B2 Piperazine-2-carboxamide derivatives 失效
标题翻译：哌嗪-2-甲酰胺衍生物
公开(公告)号：US08404690B2
公开(公告)日：2013-03-26
申请号：US10545296
申请日：2004-02-06
申请人： Patrick Page , Catherine Jorand-Lebrun , Russell J. Thomas , Matthias Schwarz
发明人： Patrick Page , Catherine Jorand-Lebrun , Russell J. Thomas , Matthias Schwarz
IPC分类号： A61K31/497 , C07D401/00
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, R1 and R2 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。

3. 发明申请

US20110288066A1 PHENOXY ACETIC ACID DERIVATIVES 失效
标题翻译：苯氧乙酸衍生物
公开(公告)号：US20110288066A1
公开(公告)日：2011-11-24
申请号：US13147389
申请日：2010-02-09
申请人： Stefano Crosignani , Catherine Jorand-Lebrun , Christophe Cleva , Adeline Pretre
发明人： Stefano Crosignani , Catherine Jorand-Lebrun , Christophe Cleva , Adeline Pretre
IPC分类号： A61K31/192 , C07C315/04 , C07D295/192 , A61K31/5375 , C07C317/50 , A61K31/195 , C07D333/64 , A61K31/381 , C07D275/06 , A61K31/428 , C07D333/76 , C07C233/54 , A61K31/196 , C07C59/66 , C07C51/367 , C07D213/71 , A61K31/44 , C07D205/04 , A61K31/397 , C07D295/112 , A61K31/495 , C07D401/12 , A61K31/4427 , A61P25/28 , A61P29/00 , A61P17/00 , A61P11/06 , A61P1/00 , C07C317/46
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。

4. 发明授权

US07947851B2 1,1′-(1,2-ethynediyl)bis-benzene derivatives as PTP 1-B inhibitors 有权
标题翻译： 1,1'-（1,2-乙炔二基）双苯衍生物作为PTP 1-B抑制剂
公开(公告)号：US07947851B2
公开(公告)日：2011-05-24
申请号：US11547861
申请日：2005-03-29
申请人： Dominique Swinnen , Catherine Jorand-Lebrun , Patrick Gerber , Jerome Gonzalez , Agnes Bombrun
发明人： Dominique Swinnen , Catherine Jorand-Lebrun , Patrick Gerber , Jerome Gonzalez , Agnes Bombrun
IPC分类号： C07D333/34 , C07C65/03 , C07C211/44 , C07C233/65 , C07C311/15 , A61K31/165 , A61P3/10
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。

5. 发明授权

US07589232B2 Alkynyl aryl carboxamides 失效
标题翻译：炔基芳基甲酰胺
公开(公告)号：US07589232B2
公开(公告)日：2009-09-15
申请号：US10565538
申请日：2004-07-20
申请人： Dominique Swinnen , Patrick Gerber , Jerome Gonzalez , Agnes Bombrun , Catherine Jorand-Lebrun
发明人： Dominique Swinnen , Patrick Gerber , Jerome Gonzalez , Agnes Bombrun , Catherine Jorand-Lebrun
IPC分类号： C07C299/34 , A61K31/195
CPC分类号： A61K31/192 , A61K31/194 , A61K31/381 , A61K31/4402 , A61K31/4406 , A61K38/28 , A61K45/06 , C07C233/18 , C07C233/20 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/81 , C07C235/08 , C07C235/16 , C07C255/19 , C07C2601/08 , C07C2601/14 , C07C2602/10 , C07D213/40 , C07D213/48 , C07D213/81 , C07D213/82 , C07D231/14 , C07D231/56 , C07D261/18 , C07D307/79 , C07D317/68 , C07D319/08 , C07D333/24 , C07D333/70 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , A61K2300/00
摘要： The present invention is related to alkynyl aryl carboxamides of Formula (I′) and use thereof for the treatment and/or prevention of an inflammatory disorder, 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 alkynyl aryl carboxamides of Formula (I′) to modulate, notably to inhibit the activity of PTPs. (I′) A is a C2-C15 alkynyl, C2-C6-alkynyl aryl, C2-C6-alkynyl heteroaryl. Cy is an aryl, heteroaryl, cycloalkyl or heterocycle group; n is either 0 or 1. Cy′ is an aryl, which may optionally be fused by a 3-8 membered cycloalkyl. R1 and R2 are independently from each other is selected from the group consisting of hydrogen or (C1-C6)alkyl. R4 and R5 are each independently from each other selected from the group consisting of H, hydroxy. C1-C6 alkyl, carboxy, C1-C6 alkoxy, C1-C3 alkyl carboxy, C2-C3 alkenyl carboxy, C2-C3 alkynyl carboxy, amino or R4 and R5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R4 or R5 is not a hydrogen or C1-C6 alkyl.
摘要翻译：本发明涉及式（I'）的炔基芳基甲酰胺及其用于治疗和/或预防由胰岛素抵抗或高血糖介导的炎性疾病，肥胖症和/或代谢障碍的用途，其包括I型和/或 II，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，本发明涉及使用式（I'）的炔基芳基甲酰胺来调节，特别是抑制PTP的活性。（I'）A是C 2 -C 15炔基，C 2 -C 6炔基芳基，C 2 -C 6炔基杂芳基。 Cy是芳基，杂芳基，环烷基或杂环基团; n是0或1. Cy'是可以任选被3-8元环烷基稠合的芳基。 R 1和R 2彼此独立地选自氢或（C 1 -C 6）烷基。 R 4和R 5各自独立地选自H，羟基。 C 1 -C 6烷基，羧基，C 1 -C 6烷氧基，C 1 -C 3烷基羧基，C 2 -C 3烯基羧基，C 2 -C 3炔基羧基，氨基或R 4和R 5可以形成不饱和或饱和的杂环，或者R 5不是氢或C 1 -C 6烷基。

6. 发明申请

US20060004020A1 Pyrrolidine derivatives as oxytocin antagonists 有权
标题翻译：吡咯烷衍生物作为催产素拮抗剂
公开(公告)号：US20060004020A1
公开(公告)日：2006-01-05
申请号：US10518543
申请日：2003-07-04
申请人： Catherine Jorand-Lebrun , Jerome Dorbais , Anna Quattropani , Matthias Schwarz , Delphine Valognes
发明人： Catherine Jorand-Lebrun , Jerome Dorbais , Anna Quattropani , Matthias Schwarz , Delphine Valognes
IPC分类号： A61K31/496 , A61K31/4025 , A61K31/416 , A61K31/401 , C07D43/02 , C07D27/18
CPC分类号： C07D231/12 , C07D207/22 , C07D233/56 , C07D249/08 , C07D403/06
摘要： The present invention relates to novel pyrrolidine derivative of formula (I), its geometrical isomers, its optically active forms as enantiomers, diastereomers, mixtures of these and its racemate forms, as well as salts thereof, wherein R1 is selected from the group comprising or consisting of H and C1-C6-alkyl, for the prevention and/or treatment of preterm labor, premature birth or dysmenorrhea.
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，其作为对映异构体的光学活性形式，非对映体，这些及其外消旋体形式的混合物，及其盐，其中R 1〜选自由H和C 1 -C 6 - 烷基组成或由H和C 1 -C 6 - 烷基组成的组，用于预防和/或治疗早产，早产或痛经。

7. 发明申请

US20120115895A1 TRICYCLIC INDOLE-DERIVED SPIRO DERIVATIVES AS CRTH2 MODULATORS 审中-公开
标题翻译：作为CRTH2调节剂的TRICYCLIC INDOLE-DIVIVED SPIRO DERIVATIVES
公开(公告)号：US20120115895A1
公开(公告)日：2012-05-10
申请号：US13383857
申请日：2010-07-14
申请人： Stefano Crosignani , Catherine Jorand-Lebrun , Tania Grippi-Vallotton
发明人： Stefano Crosignani , Catherine Jorand-Lebrun , Tania Grippi-Vallotton
IPC分类号： A61K31/4439 , A61K31/422 , A61K31/4188 , C07D487/10 , A61P19/02 , A61P29/00 , A61P37/08 , A61P11/06 , A61P1/00 , A61K31/427 , A61P25/00
CPC分类号： C07D487/10
摘要： The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases. The compounds according to Formula (I) are suitable as modulators of CRTH2. The invention provides Spiro derivatives according to Formula (I) and related formulae that are useful in the treatment and/or prevention of diseases selected from allergic diseases such as allergic asthma, allergic rhinitis, allergic conjunctivitis, and inflammatory dermatoses such as atopic dermatitis, contact hypersensitivity, allergic contact dermatitis, chronic urticaria/chronic idiopathic/autoimmune urticaria, drag-induced exanthems (e.g., toxic epidermal necrolysis or Lyell's syndrome/Stevens-Johnson syndrome/drug hypersensitivity syndrome), photodermatosis or polymorphous light emption (e.g., photoirritant contact dermatitis, photoallergy contact dermatitis, chronic actinic dermatitis), and myositis neurodegenerative disorders such as neuropatic pain and other diseases with an inflammatory component such as rheumatoid arthritis, multiple sclerosis, osteoarthritis, and inflammatory bowel disease (IBD).
摘要翻译：本发明涉及用作药物活性化合物的式（I）化合物，以及含有该化合物的用于治疗过敏性疾病的药物制剂。根据式（I）的化合物适合作为CRTH2的调节剂。本发明提供了可用于治疗和/或预防选自过敏性疾病如过敏性哮喘，过敏性鼻炎，过敏性结膜炎和炎性皮肤病如特应性皮炎，接触的疾病的式（I）和相关配方的螺衍生物超敏反应，过敏性接触性皮炎，慢性荨麻疹/慢性特发性/自身免疫性荨麻疹，牵引性外阴（例如中毒性表皮坏死松解症或莱尔综合征/史蒂文斯 - 约翰逊综合征/药物过敏综合征），光照皮肤病或多形态光吸收（如光刺激性接触性皮炎，光敏性接触性皮炎，慢性光化性皮炎）和肌炎神经变性疾病如神经性疼痛和其它具有炎性成分的疾病，例如类风湿性关节炎，多发性硬化症，骨关节炎和炎症性肠病（IBD）。

8. 发明申请

US20070105913A1 Alkynyl aryl carboxamides 失效
标题翻译：炔基芳基甲酰胺
公开(公告)号：US20070105913A1
公开(公告)日：2007-05-10
申请号：US10565538
申请日：2004-07-20
申请人： Dominique Swinnen , Patrick Gerber , Jerome Gonzalez , Agnes Bombrun , Catherine Jorand-Lebrun
发明人： Dominique Swinnen , Patrick Gerber , Jerome Gonzalez , Agnes Bombrun , Catherine Jorand-Lebrun
IPC分类号： A61K31/44 , A61K31/40 , A61K31/24 , A61K31/195 , A61K31/16
CPC分类号： A61K31/192 , A61K31/194 , A61K31/381 , A61K31/4402 , A61K31/4406 , A61K38/28 , A61K45/06 , C07C233/18 , C07C233/20 , C07C233/51 , C07C233/52 , C07C233/54 , C07C233/55 , C07C233/63 , C07C233/81 , C07C235/08 , C07C235/16 , C07C255/19 , C07C2601/08 , C07C2601/14 , C07C2602/10 , C07D213/40 , C07D213/48 , C07D213/81 , C07D213/82 , C07D231/14 , C07D231/56 , C07D261/18 , C07D307/79 , C07D317/68 , C07D319/08 , C07D333/24 , C07D333/70 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , A61K2300/00
摘要： The present invention is related to alkynyl aryl carboxamides of Formula (I′) and use thereof for the treatment and/or prevention of an inflammatory disorder, 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 alkynyl aryl carboxamides of Formula (I′) to modulate, notably to inhibit the activity of PTPs. (I′) A is a C2-C15 alkynyl, C2-C6-alkynyl aryl, C2-C6-alkynyl heteroaryl. Cy is an aryl, heteroaryl, cycloalkyl or heterocycle group; n is either 0 or 1. Cy′ is an aryl., which may optionally be fused by a 3-8 membered cycloalkyl. R1 and R2 are independently from each other is selected from the group consisting of hydrogen or (C1-C6)alkyl. R4and R5 are each independently from each other selected from the group consisting of H, hydroxy. C1-C6 alkyl, carboxy, C1-C6 alkoxy, C1-C3 alkyl carboxy, C2-C3 alkenyl carboxy, C2-C3 alkynyl carboxy, amino or R4 and R5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R4 or R5 is not a hydrogen or C1-C6 alkyl.
摘要翻译：本发明涉及式（I'）的炔基芳基甲酰胺及其用于治疗和/或预防由胰岛素抵抗或高血糖介导的炎性疾病，肥胖症和/或代谢障碍的用途，其包括I型和/或 II，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，本发明涉及使用式（I'）的炔基芳基甲酰胺来调节，特别是抑制PTP的活性。（I'）A是C 2 -C 15炔基，C 2 -C 6 - 炔基芳基 C 2 -C 6 - 炔基杂芳基。 Cy是芳基，杂芳基，环烷基或杂环基团; n是0或1. Cy'是芳基，其可任选地被3-8元环烷基稠合。 R 1和R 2彼此独立地选自氢或（C 1 -C 6 - / SUB）烷基。 R 4和R 5各自彼此独立地选自H，羟基。 C 1 -C 6烷基，羧基，C 1 -C 6烷氧基，C 1 -C 6烷基，C 1 -C 6烷基， C 1 -C 3烷基羧基，C 2 -C 3链烯基羧基，C 2 -C 3烷基羧基，C 1 -C 3烷基羧基，亚磺酰基，氨基或R 4和R 5可以形成不饱和或饱和的杂环，由此R 4中的至少一个或者R 5不是氢或C 1 -C 6烷基。

9. 发明申请

US20050215605A1 Thiazolidine carboxamide derivatives as modulators of the prostaglandin f receptor 审中-公开
公开(公告)号：US20050215605A1
公开(公告)日：2005-09-29
申请号：US10508014
申请日：2003-03-27
申请人： Patrick Page , Catherine Jorand-Lebrun , Anna Quattropani , Vincent Pomel , Matthias Schwarz , Estelle Hamelin
发明人： Patrick Page , Catherine Jorand-Lebrun , Anna Quattropani , Vincent Pomel , Matthias Schwarz , Estelle Hamelin
IPC分类号： A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K31/55 , A61P15/00 , A61P15/06 , A61P43/00 , C07D277/06 , C07D417/12 , C07D417/14
CPC分类号： C07D417/12 , A61K31/426 , A61K31/427 , C07D277/06 , C07D417/14 , Y02P20/582
摘要： The present invention is related to thiazolidine carboxamide derivatives of formula (II) for the treatment and/or prophylaxis of preterm labor, premature birth, dysmenorrhea and for stopping labor prior to cesarean delivery. G is selected from the group consisting of C1-C6-alkyl aryl, C1-C6-alkyl heteroaryl, C1-C6 Alkyl cycloalkyl, C1-C6-alkyl heteroaryl, aryl, heteroaryl, C3-C8-cycloalkyl or -heterocycloalkyl, said cycloalkyl or aryl or hetetoaryl groups may be fused with cycloalkyl or aryl or heteroaryl groups. R1 is selected from the group consisting of aryl, heteroaryl, C3-C8-cycloalkyl or -heterocyclo-alkyl, said (hetero)cycloalkyl or aryl or heteroaryl groups may be fused with (hetero)cycloalkyl or aryl or heteroaryl groups. R2 is selected from the group consisting of H, carboxy, acyl, alkoxycarbonyl, aminocarbonyl, C1-C5-alkyl carboxy, C1-C5-alkyl acyl, C1-C5-alkyl alkoxycarbonyl, C1-C5-alkyl aminocarbonyl, C1-C5-alkyl acyloxy, C1-C5-alkyl acylamino, C1-C5-alkyl ureido, C1-C5alkyl amino, C1-C5-alkyl alkoxy, C1-C5-alkyl sulfanyl, C1-C5-alkyl sulfinyl, C1-C5-alkyl sulfonyl, C1-C5-alkyl sulfonylamino, C1-C5-alkyl sulfonyloxy, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, heteroaryl, C3-C8-cycloalkyl, heterocycloalkyl, C1-C6-alkyl aryl, C2-C6-alkyl heteroaryl, C1-C6-alkyl cycloalkyl, C1-C6-alkyl heterocycloalkyl, C2-C6-alkenyl aryl, C2-C6-alkenyl heteroaryl, C2-C6-alkynyl aryl, or C2-C6-alkynyl heteroaryl.

10. 发明授权

US08415480B2 Thiazolidine carboxamide derivatives as modulators of the prostaglandin F receptor 有权
标题翻译：噻唑烷羧酰胺衍生物作为前列腺素F受体的调节剂
公开(公告)号：US08415480B2
公开(公告)日：2013-04-09
申请号：US12140682
申请日：2008-06-17
申请人： Patrick Naxos Page , Catherine Jorand-Lebrun , Anna Quattropani , Vincent Pomel , Matthias Schwarz , Estelle Hamelin , Russell J. Thomas
发明人： Patrick Naxos Page , Catherine Jorand-Lebrun , Anna Quattropani , Vincent Pomel , Matthias Schwarz , Estelle Hamelin , Russell J. Thomas
IPC分类号： A61K31/4402 , A61K31/426 , C07D417/12 , C07D277/46
CPC分类号： C07D417/12 , A61K31/426 , A61K31/427 , C07D277/06 , C07D417/14 , Y02P20/582
摘要： The present invention is related to thiazolidine carboxamide derivatives of formula (II) for the treatment and/or prophylaxis of preterm labor, premature birth, dysmenorrhea and for stopping labor prior to cesarean delivery.
摘要翻译：本发明涉及式（II）的噻唑烷羧酰胺衍生物，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。

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