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1. 发明申请

US20070015799A1 Glyoxalase inhibitors 审中-公开
标题翻译：乙二醛酶抑制剂
公开(公告)号：US20070015799A1
公开(公告)日：2007-01-18
申请号：US10556901
申请日：2004-05-14
申请人： Mark Ashton , Alan Davidson , Russell Thomas , Mark Whittaker
发明人： Mark Ashton , Alan Davidson , Russell Thomas , Mark Whittaker
IPC分类号： A61K31/4436 , A61K31/44 , A61K31/381
CPC分类号： C07D405/04 , A61K31/10 , A61K31/381 , A61K31/44 , A61K31/4436 , C07C323/62 , C07D213/85 , C07D217/26 , C07D409/04 , C07D409/14
摘要： This invention relates to compounds of formula (I) which are glyoxalase I inhibitors, pharmaceutical salts or compositions comprising such compounds, and the use of such compositions and compounds to treat various conditions alleviated by the inhibition of glyoxalase 1. Wherein X is N or CH. R2 is H, CF3; or optionally substituted C5-6 aryl, C3-7 cycloalkyl, C5-7 heterocyclyl. R3 is H; or optionally substituted C5-6 aryl, C3-7 cycloalkyl, C5-7 heterocyclyl. Alternatively R2 and R3 together form an optionally substituted C3-4alkylene group wherein L3 and L4 are single bonds thus forming a C5-6 ring fused with the aromatic ring to which L3 and L4 are attached. L3 and L4 are independently selected from a single bond, optionally substituted C1-4 alkylene, -L9YN(OH)C(═O)L10- and -L9C(═O)N(OH)YL10-, wherein L9 and L10 are independently selected from optionally substituted C1-4 alkylene, C5-6 arylene, C1-4 alkylene-C5-6arylene and a single bond, wherein Y is NH or a single bond.
摘要翻译：本发明涉及作为乙二醛酶I抑制剂的式（I）化合物，包含这些化合物的药物盐或组合物，以及这些组合物和化合物用于治疗通过抑制乙二醛酶1减轻的各种病症的用途。其中X是N或CH 。 R 2是H，CF 3 N; 或任选取代的C 5-6芳基，C 3-7环烷基，C 5-7杂环基。 R 3是H; 或任选取代的C 5-6芳基，C 3-7环烷基，C 5-7杂环基。或者R 2和R 3一起形成任选取代的C 3-4亚烷基，其中L 3和L 3 因此形成与L 3和L 4的芳环稠合的C 5〜6环， SUP>连接。 L 3和L 4独立地选自单键，任选取代的C 1-4亚烷基，-L 9， SUP-YN（OH）C（-O）L 10 - 和-L 9 C（ - ）N（OH）Y L 10 - ，其中L 9和L 10独立地选自任选取代的C 1-4 - 亚烷基，C 5-6 - 亚芳基，C 1-4亚烷基-C 5-6亚芳基和单键，其中Y是NH或单键。

2. 发明申请

US20060205697A1 Novel betulin derivatives, preparation thereof and use thereof 审中-公开
标题翻译：新颖的桦木醇衍生物，其制备及其用途
公开(公告)号：US20060205697A1
公开(公告)日：2006-09-14
申请号：US11272019
申请日：2005-11-14
申请人： Gary Robinson , Carl Wild , Mark Ashton , Russell Thomas , Christian Montalbetti , Thomas Coulter , Filippo Magaraci , Robert Townsend , Theodore Nitz
发明人： Gary Robinson , Carl Wild , Mark Ashton , Russell Thomas , Christian Montalbetti , Thomas Coulter , Filippo Magaraci , Robert Townsend , Theodore Nitz
IPC分类号： A61K31/66 , C07J51/00 , C07J53/00 , A61K31/58
CPC分类号： C07J51/00 , C07J53/00
摘要： The present invention relates to novel synthetic derivatives of betulin and the use of such derivatives as pharmaceuticals. The present invention is directed to novel compounds of Formula I: or a pharmaceutically acceptable salt or prodrug thereof.
摘要翻译：本发明涉及新颖的桦木素合成衍生物和药物衍生物的用途。本发明涉及新的式I化合物：或其药学上可接受的盐或前药。

3. 发明申请

US20050148561A1 Novel triterpene derivatives, preparation thereof and use thereof 审中-公开
标题翻译：新型三萜衍生物，其制备方法及用途
公开(公告)号：US20050148561A1
公开(公告)日：2005-07-07
申请号：US10949875
申请日：2004-09-27
申请人： Carl Wild , Gary Robinson , Mark Ashton , Russell Thomas
发明人： Carl Wild , Gary Robinson , Mark Ashton , Russell Thomas
IPC分类号： A61K31/513 , A61K31/522 , A61K31/551 , A61K31/57 , A61K31/7072 , A61K31/7076 , A61K38/20 , A61K38/21 , C07C69/00 , C07C69/40 , C07C69/42 , C07C69/608 , C07C69/708 , C07J1/00 , C07J53/00
CPC分类号： C07C69/708 , C07C69/40 , C07C69/42 , C07C69/608 , C07C2603/52 , C07J1/00 , C07J53/00 , C07J63/008
摘要： The present invention relates to novel synthetic derivatives of triterpenes and the use of such derivatives as pharmaceuticals. The present invention is directed to novel compounds of Formula I: or pharmaceutically acceptable salt or ester thereof, wherein R1 is a carboxyalkanoyl, where the alkanoyl chain can be interrupted by a nitrogen, sulfur or oxygen atom, or combinations thereof.
摘要翻译：本发明涉及三萜烯的新型合成衍生物和药物衍生物的用途。本发明涉及新的式I化合物或其药学上可接受的盐或酯，其中R 1是羧烷基，其中烷酰基链可被氮，硫或氧原子间隔，或其组合。

4. 发明申请

US20070203134A1 Benzimidazole Acetonitriles 审中-公开
标题翻译：苯并咪唑乙腈
公开(公告)号：US20070203134A1
公开(公告)日：2007-08-30
申请号：US10571470
申请日：2004-09-10
申请人： Matthias Schwarz , Pascale Gaillard , Patrick Page , Jean-Pierre Gotteland , Russell Thomas
发明人： Matthias Schwarz , Pascale Gaillard , Patrick Page , Jean-Pierre Gotteland , Russell Thomas
IPC分类号： A61K31/5377 , A61K31/506 , C07D413/14 , C07D403/02
CPC分类号： C07D403/06 , C07D403/14 , C07D413/14 , C07D417/14
摘要： The present invention is related to benzimidazole acetonitriles as well as to pharmaceutical formulations containing such benzimidazole acetonitriles of formula (I). Said benzimidazole acetonitriles are useful in the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS) (I). The present invention is furthermore related to methods of preparing benzoxazole acetonitriles. G is pyrimidinyl; L is an amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatom selected from N, O, S or L is an acylamino moiety; R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, carboxy, aminocarbonyl, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C1-C6-alkoxy, aryl, halogen, cyano or hydroxy; R2 is selected from the group comprising or consisting of hydrogen, C1-C6-alkyl, C2-C6alkenyl, C2-C6-alkynyl, or C1-C6-alkoxy.
摘要翻译：本发明涉及苯并咪唑乙腈和含有式（I）的苯并咪唑乙腈的药物制剂。所述苯并咪唑乙腈可用于治疗由胰岛素抵抗或高血糖介导的代谢紊乱，包括II型糖尿病，葡萄糖耐量不足，胰岛素抵抗，肥胖，多囊卵巢综合征（PCOS）（I））。本发明还涉及制备苯并恶唑乙腈的方法。 G是嘧啶基; L是含有至少一个选自N，O，S或L的杂原子的氨基或3-8元杂环烷基是酰氨基部分; R 1选自氢，磺酰基，氨基，羧基，氨基羰基，C 1 -C 6 - 烷基，C 1 -C 6 - 烷基， C 2 -C 6 - 烯基，C 2 -C 6 - 炔基或C 1 -C 6 - C 1 -C 6 - 烷氧基，芳基，卤素，氰基或羟基; R 2选自包含或由氢，C 1 -C 6 - 烷基，C 2 H 2基团组成的组 C 1 -C 6亚烷基，C 2 -C 6亚炔基或C 1 -C 6亚烷基， 6 - 烷氧基。

5. 发明申请

US20060074124A1 Methods of treating a disorder 审中-公开
标题翻译：治疗疾病的方法
公开(公告)号：US20060074124A1
公开(公告)日：2006-04-06
申请号：US11077664
申请日：2005-03-11
申请人： Andrew Napper , Peter Distefano , Rory Curtis , Jeffrey Hixon , Thomas McDonagh , L. Huber , Jonathan Solomon , Russell Thomas , Jean-Francois Pons
发明人： Andrew Napper , Peter Distefano , Rory Curtis , Jeffrey Hixon , Thomas McDonagh , L. Huber , Jonathan Solomon , Russell Thomas , Jean-Francois Pons
IPC分类号： A61K31/403 , C07D209/82
CPC分类号： A61K31/403 , A61K31/404 , A61K31/437 , A61K31/4439 , A61K31/497 , A61K31/5377 , C07D209/18 , C07D209/88 , C07D209/94 , C07D471/04
摘要： Compound of formula (I) and methods of treating disorders by administering a compound of formula (I) are described herein. Examples of disorders include neoplastic disorders, fat-cell related disorders, neurodegenerative disorders, and metabolic disorders.
摘要翻译：本文描述式（I）化合物和通过施用式（I）化合物治疗病症的方法。病症的实例包括肿瘤性疾病，脂肪细胞相关疾病，神经变性疾病和代谢紊乱。

6. 发明申请

US20060229343A1 Pyrrolidine oxadiazole-and thiadiazole oxime derivatives being oxytocin receptor antagonists 审中-公开
标题翻译：吡咯烷恶二唑和噻二唑肟衍生物是催产素受体拮抗剂
公开(公告)号：US20060229343A1
公开(公告)日：2006-10-12
申请号：US11449802
申请日：2006-06-09
申请人： Matthias Schwarz , Anna Quattropani , Patrick Page , Russell Thomas , Vincent Pomel
发明人： Matthias Schwarz , Anna Quattropani , Patrick Page , Russell Thomas , Vincent Pomel
IPC分类号： A61K31/433 , A61K31/4245 , C07D413/14 , C07D417/14
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention is related to pyrrolidine oxadiazole and thiadiazole derivatives for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such pyrrolidine oxadiazole derivatives. Said pyrrolidine derivatives are useful in the treatment and/or prevention of preterm labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including preterm labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation. B is a oxadiazole or thiadiazole group.
摘要翻译：本发明涉及用作药物活性化合物的吡咯烷恶二唑和噻二唑衍生物，以及含有这种吡咯烷恶二唑衍生物的药物制剂。所述吡咯烷衍生物可用于治疗和/或预防早产，早产和痛经。特别地，本发明涉及显示出显着调节，特别是催产素受体拮抗剂活性的吡咯烷衍生物。更优选地，所述化合物可用于治疗和/或预防催产素介导的疾病状态，包括早产，早产和痛经。本发明还涉及新型吡咯烷衍生物及其制备方法。 B是恶二唑或噻二唑基。

7. 发明申请

US20050261332A1 Sulfonamides and uses thereof 审中-公开
标题翻译：磺酰胺及其用途
公开(公告)号：US20050261332A1
公开(公告)日：2005-11-24
申请号：US11098315
申请日：2005-04-04
申请人： Peter Distefano , Andrew Napper , Rory Curtis , Jay Luly , Jean-Francois Pons , Russell Thomas , Manuel Navia , Thomas Coulter , Jeffrey Saunders , Bard Geesaman
发明人： Peter Distefano , Andrew Napper , Rory Curtis , Jay Luly , Jean-Francois Pons , Russell Thomas , Manuel Navia , Thomas Coulter , Jeffrey Saunders , Bard Geesaman
IPC分类号： A61K31/422 , A61K31/4245 , A61K31/454 , A61K31/4745 , C07C311/32 , C07D413/02 , C07D471/02 , C07D471/10 , C07D43/02
CPC分类号： C07D471/10 , C07C311/32 , C07D401/12
摘要： Compounds of formulas (I), (II), (III), and (IV) and methods of treating disorders by administering a compound of formula (I), (II), (III), or (IV) are described herein. Examples of disorders include neoplastic disorders, fat-cell related disorders, neurodegenerative disorders, and metabolic disorders.
摘要翻译：本文描述式（I），（II），（III）和（IV）的化合物和通过施用式（I），（II），（III）或（IV）的化合物来治疗病症的方法。病症的实例包括肿瘤性疾病，脂肪细胞相关疾病，神经变性疾病和代谢紊乱。

8. 发明申请

US20050187237A1 Therapeutic compounds and uses thereof 失效
标题翻译：治疗化合物及其用途
公开(公告)号：US20050187237A1
公开(公告)日：2005-08-25
申请号：US10982997
申请日：2004-11-04
申请人： Peter Distefano , Andrew Napper , Rory Curtis , Jay Luly , Manuel Navia , Russell Thomas , Jean-Francois Pons , Jeffrey Saunders
发明人： Peter Distefano , Andrew Napper , Rory Curtis , Jay Luly , Manuel Navia , Russell Thomas , Jean-Francois Pons , Jeffrey Saunders
IPC分类号： A61K31/438 , A61K31/4747 , A61K31/5377 , C07D413/14 , C07D471/10
CPC分类号： C07D471/10 , C07D221/20 , C07D401/12
摘要： Compounds of formula (I) are described herein The compounds can be used, for example, to modulate growth hormone secretagogue receptor (GHS-R). In some instances, the compounds can be used to treat obesity.
摘要翻译：式（I）化合物在本文中描述。该化合物可用于例如调节生长激素促分泌素受体（GHS-R）。在一些情况下，化合物可用于治疗肥胖症。

9. 发明申请

US20070185104A1 Benzoxazole acetonitriles 审中-公开
标题翻译：苯并恶唑乙腈
公开(公告)号：US20070185104A1
公开(公告)日：2007-08-09
申请号：US10571323
申请日：2004-09-10
申请人： Matthias Schwarz , Pascale Gaillard , Patrick Page , Jean-Pierre Gotteland , Russell Thomas
发明人： Matthias Schwarz , Pascale Gaillard , Patrick Page , Jean-Pierre Gotteland , Russell Thomas
IPC分类号： A61K31/5377 , A61K31/506 , C07D413/14
CPC分类号： C07D491/10 , C07D413/06 , C07D413/14
摘要： The present invention is related to benzoxazole acetonitriles as well as to pharmaceutical formulations containing such benzoxazole acetonitriles pof formula (I). Said benzoxazole acetonitriles are useful in the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS). The present invention is furthermore related to methods of preparing benzoxazole acetonitriles (I). A is a pyrimidinyl.L is a secondary or tertiary amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatom. selected from N, O, S or L is an acylamino moiety. R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, C1C6-alkYl, C2-C6-alkenYl, C2-C6-alkynyl or C1-C6-alkoxy, aryl, halogen, carboxy, aminocarbonyl, cyano or hydroxy.
摘要翻译：本发明涉及苯并恶唑乙腈和含有该苯并恶唑乙腈的配方（I）的药物制剂。所述苯并恶唑乙腈可用于治疗由胰岛素抵抗或高血糖介导的代谢紊乱，包括II型糖尿病，葡萄糖耐量不足，胰岛素抵抗，肥胖，多囊卵巢综合征（PCOS）。本发明还涉及制备苯并恶唑乙腈（I）的方法。 A是嘧啶基，L是含有至少一个杂原子的仲或叔氨基或3-8元杂环烷基。选自N，O，S或L是酰氨基部分。 R 1选自包含或由氢，磺酰基，氨基，C 1 -C 6 - 烷基，C 2 -C 6 - 亚烷基，C 2 -C 6 - 炔基或C 1 -C 烷氧基，芳基，卤素，羧基，氨基羰基，氰基或羟基。

10. 发明申请

US20050209300A1 Methods of treating a disorder 审中-公开
标题翻译：治疗疾病的方法
公开(公告)号：US20050209300A1
公开(公告)日：2005-09-22
申请号：US10940269
申请日：2004-09-13
申请人： Andrew Napper , Peter Distefano , Rory Curtis , Jeffrey Hixon , Thomas McDonagh , L. Huber , Jonathan Solomon , Russell Thomas , Jean-Francois Pons
发明人： Andrew Napper , Peter Distefano , Rory Curtis , Jeffrey Hixon , Thomas McDonagh , L. Huber , Jonathan Solomon , Russell Thomas , Jean-Francois Pons
IPC分类号： A61K31/35 , A61K31/38 , A61K31/40 , A61K31/403 , A61K31/445 , C07D20060101
CPC分类号： A61K31/445 , A61K31/35 , A61K31/38 , A61K31/40 , A61K31/403 , C07D209/88
摘要： Compound of formula (I) and methods of treating disorders by administering a compound of formula (I) are described herein. Examples of disorders include neoplastic disorders, fat-cell related disorders, neurodegenerative disorders, and metabolic disorders.
摘要翻译：本文描述式（I）化合物和通过施用式（I）化合物治疗病症的方法。病症的实例包括肿瘤性疾病，脂肪细胞相关疾病，神经变性疾病和代谢紊乱。

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