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1. 发明授权

EP1613326B1 (3-{3-'(2,4-BIS-TRIFLUORMETHYL-BENZYL)-(5-ETHYL-PYRIMIDIN-2-YL)-AMINO]-PROPOXY}-PHENYL)-ACETIC ACID AND RELATED COMPOUNDS AS MODULATORS OF PPARS AND METHODS OF TREATING METABOLIC DISORDERS 有权
标题翻译：（3- {3 - “（2,4-双 - 三氟甲基 - 苄基） - （5-乙基 - 嘧啶-2-基）氨基]丙氧基}苯基）乙酸和相关化合物作为PPARs的AND METHOD的调节剂代谢疾病的治疗
公开(公告)号：EP1613326B1
公开(公告)日：2006-09-13
申请号：EP04759820.6
申请日：2004-04-07
申请人： Kalypsys, Inc.
发明人： LIU, Kevin , ZHAO, Cunxiang
IPC分类号： A61K31/505 , A61K31/4402 , A61K31/426 , A61K31/421 , C07D239/42 , C07D213/38 , C07D277/82 , C07D263/58 , A61P3/04
CPC分类号： C07D239/42 , C07D213/38 , C07D213/74 , C07D263/58 , C07D277/82
摘要： Disclosed are compounds of formula I as modulators of peroxisome proliferator activated receptors (PPARs) for the treatment of metabolic diseases such as obesity: wherein Ar1 is selected from the group consisting of a monocyclic heteroarornatic ring structure and a bicyclic heteroaromatic ring structure; Ar2 is selected from the group consisting of a monocyclic, a bicyclic, and a tricyclic carbocyclic aryl ring structure R1 is selected from the group consisting of alkyl, optionally substituted a five-membered or six-membered heteroarylring or a six-membered aryl ring, optionally substituted R2 is selected from the group consisting of hydrogen; alkyl, optionally substituted a five-membered or six-membered heteroaryl ring or a six-membered aryl ring, optionally substituied cyano; nitro; an amino; an amido; perhaloalkyl; and halogen; R3 is selected from the group consisting of hydrogen; alkyl, optionally substituted and B is a five-membered or six-membered heteroaryl ring, or -(CH2)j-C(O)OR4, wherein j is 0 or I 1 when Ar2 is a bicyclic or tricyclic carbocyclic ring structure and j is 1 when Ar2 is a monocyclic carbocyclic ring structure; and R4 is selected from the group consisting of hydrogen; alkyl, optionally substituted a five-membered or six-membered heteroaryl ring or a six-membered aryl ring, optionally substituted. The obtional substituents are as defined in claim 1.

2. 发明申请

WO2007076473A3 SUBSTITUTED PYRIMIDINYLOXY UREAS USEFUL AS INHIBITORS OF PROTEIN KINASES 审中-公开
公开(公告)号：WO2007076473A3
公开(公告)日：2007-07-05
申请号：PCT/US2006/062551
申请日：2006-12-22
申请人： KALYPSYS, INC. , LANG, Hengyuan , GAHMAN, Timothy, C. , HERBERT, Mark, R. , ZHAO, Cunxiang , WASH, Paul, L. , DAVIS, Robert, L.
发明人： LANG, Hengyuan , GAHMAN, Timothy, C. , HERBERT, Mark, R. , ZHAO, Cunxiang , WASH, Paul, L. , DAVIS, Robert, L.
IPC分类号： C07D213/81 , C07D401/04 , C07D403/04 , C07D403/14 , C07D413/14 , C07D417/04 , C07D487/04 , A61K31/4439 , A61K31/506 , A61P35/00 , A61P17/06 , A61P27/06
摘要： The present invention relates to compounds and methods useful as inhibitors of protein kinases, including B-Raf and several receptor tyrosine and cytoplasmic tyrosine kinases. The present invention is directed to new substituted pyrimidinyloxy urea compounds of Formulas II, III and IV and compositions and their application as pharmaceuticals for the treatment of disease. Methods of modulating of protein kinase activity in a human or animal subject are also provided for the treatment diseases such as cancers.

3. 发明申请

WO2007076474A1 NOVEL SUBSTITUTED PYRIDINYLOXY AND PYRIMIDINYLOXY AMIDES USEFUL AS INHIBITORS OF PROTEIN KINASES 审中-公开
标题翻译：新型取代的吡啶并吡啶和吡啶二恶烷作为蛋白激酶的抑制剂有用
公开(公告)号：WO2007076474A1
公开(公告)日：2007-07-05
申请号：PCT/US2006/062552
申请日：2006-12-22
申请人： KALYPSYS, INC. , LANG, Hengyuan , GAHMAN, Timothy, C. , HERBERT, Mark, R. , ZHAO, Cunxiang , WASH, Paul, L. , DAVIS, Robert, L.
发明人： LANG, Hengyuan , GAHMAN, Timothy, C. , HERBERT, Mark, R. , ZHAO, Cunxiang , WASH, Paul, L. , DAVIS, Robert, L.
IPC分类号： C07D401/04 , C07D401/14 , C07D413/04 , A61K31/4439 , A61P35/04
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/04 , C07D413/14
摘要： The present invention relates to compounds and methods useful as inhibitors of protein kinases, including B-Raf and several receptor tyrosine and cytoplasmic tyrosine kinases. The present invention is directed to new substituted pyrimidinyloxy urea compounds of Formulas II, III and IV and compositions and their application as pharmaceuticals for the treatment of disease. Methods of modulating of protein kinase activity in a human or animal subject are also provided for the treatment diseases such as cancers.
摘要翻译：本发明涉及可用作蛋白激酶抑制剂的化合物和方法，包括B-Raf和若干受体酪氨酸和细胞质酪氨酸激酶。本发明涉及式II，III和IV的新的取代的嘧啶氧基脲化合物及其组合物及其作为用于治疗疾病的药物的应用。调节人或动物受试者中蛋白激酶活性的方法也用于治疗疾病如癌症。

4. 发明申请

WO2004092130A2 N-CONTAINING HETEROAROMATIC COMPOUNDS AS MODULATORS OF PPARS AND METHODS OF TREATING METABOLIC DISORDERS 审中-公开
标题翻译：作为PPARS调节剂的N-含有异构体化合物和治疗代谢紊乱的方法
公开(公告)号：WO2004092130A2
公开(公告)日：2004-10-28
申请号：PCT/US2004/010737
申请日：2004-04-07
申请人： KALYPSYS, INC. , LIU, Kevin , ZHAO, Cunxiang
发明人： LIU, Kevin , ZHAO, Cunxiang
IPC分类号： C07D209/00
CPC分类号： C07D213/74 , C07D213/79 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12
摘要： Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
摘要翻译：公开了作为过氧化物酶体增殖物激活受体的调节剂的化合物，包含其的药物组合物和使用其的治疗疾病的方法，（I）其中（i）是单环或双酯芳族部分，其中至少一个环原子是并且选自（ii），（iii），（iv），（v）和（vi）组成的组; L选自由键和CH2组成的组。

5. 发明申请

WO2007109577A1 ALKYLAMINE-SUBSTITUTED BICYCLIC ARYL COMPOUNDS USEFUL AS MODULATORS OF PPAR 审中-公开
标题翻译：作为PPAR调节剂的有用的亚苄基取代的双环芳烃化合物
公开(公告)号：WO2007109577A1
公开(公告)日：2007-09-27
申请号：PCT/US2007/064226
申请日：2007-03-16
申请人： KALYPSYS, INC. , ZHAO, Cunxiang
发明人： ZHAO, Cunxiang
IPC分类号： A61K31/506 , C07D239/02 , A61P9/00
CPC分类号： C07D405/12 , A61K31/506 , A61K31/517 , A61K31/538 , C07D401/12
摘要： The present invention relates to novel alkylamine-substituted bicyclic aryl compounds, pharmaceutical compositions comprising the same, useful as modulators of PPAR, and methods for the treatment or prevention of disease.
摘要翻译：本发明涉及新的烷基胺取代的二环芳基化合物，包含其的药物组合物，可用作PPAR的调节剂，以及用于治疗或预防疾病的方法。

6. 发明申请

WO2004093879A1 (3-{3-‘(2,4-BIS-TRIFLUORMETHYL-BENZYL)-(5-ETHYL-PYRIMIDIN-2-YL)-AMINO!-PROPOXY}-PHENYL)-ACETIC ACID AND RELATED COMPOUNDS AS MODULATORS OF PPARS AND METHODS OF TREATING METABOLIC DISORDERS 审中-公开
标题翻译：（3- {3 - （（2,4-BIS-三氟甲基）苄基） - （5-乙基 - 嘧啶-2-基） - 氨基} - 苯基） - 甲酸和相关化合物作为PPARS的调节剂治疗代谢障碍的方法
公开(公告)号：WO2004093879A1
公开(公告)日：2004-11-04
申请号：PCT/US2004/010970
申请日：2004-04-07
申请人： KALYPSYS, INC. , LIU, Kevin , ZHAO, Cunxiang
发明人： LIU, Kevin , ZHAO, Cunxiang
IPC分类号： A61K31/505
CPC分类号： C07D239/42 , C07D213/38 , C07D213/74 , C07D263/58 , C07D277/82
摘要： Disclosed are compounds of formula I as modulators of peroxisome proliferator activated receptors (PPARs) for the treatment of metabolic diseases such as obesity: wherein Ar 1 is selected from the group consisting of a monocyclic heteroarornatic ring structure and a bicyclic heteroaromatic ring structure; Ar 2 is selected from the group consisting of a monocyclic, a bicyclic, and a tricyclic carbocyclic aryl ring structure R 1 is selected from the group consisting of alkyl, optionally substituted a five-membered or six-membered heteroarylring or a six-membered aryl ring, optionally substituted R 2 is selected from the group consisting of hydrogen; alkyl, optionally substituted a five-membered or six-membered heteroaryl ring or a six-membered aryl ring, optionally substituied cyano; nitro; an amino; an amido; perhaloalkyl; and halogen; R 3 is selected from the group consisting of hydrogen; alkyl, optionally substituted and B is a five-membered or six-membered heteroaryl ring, or -(CH 2 )j-C(O)OR 4 , wherein j is 0 or I 1 when Ar 2 is a bicyclic or tricyclic carbocyclic ring structure and j is 1 when Ar 2 is a monocyclic carbocyclic ring structure; and R 4 is selected from the group consisting of hydrogen; alkyl, optionally substituted a five-membered or six-membered heteroaryl ring or a six-membered aryl ring, optionally substituted. The obtional substituents are as defined in claim 1.
摘要翻译：公开了作为用于治疗代谢疾病如肥胖症的过氧化物酶体增殖物激活受体（PPAR）的调节剂的式I化合物：其中Ar1选自单环杂芳环结构和双环杂芳环结构; Ar 2选自单环，双环和三环碳环芳基环结构，R 1选自烷基，任选被五元或六元杂芳基环或六元芳环取代，任选取代的R 2选自氢; 烷基，任选取代五元或六元杂芳环或六元芳环，任选取代的氰基; 硝基; 氨基; 一个amido; 全卤; 和卤素; R3选自氢; 烷基，任选取代，B是五元或六元杂芳环，或 - （CH 2）j C（O）OR 4，其中当Ar 2是双环或三环碳环结构时，j是0或I 1，并且j是1 当Ar 2是单环碳环结构时; 并且R 4选自氢; 烷基，任选被取代的任选被取代的五元或六元杂芳基环或六元芳环。所述取代基如权利要求1所定义。

7. 发明公开

EP1735280A1 ARYL SULFONAMIDE AND SULFONYL COMPOUNDS AS MODULATORS OF PPAR AND METHODS OF TREATING METABOLIC DISORDERS 审中-公开
标题翻译： ARYLSULFONAMID-和-SULFONYLVERBINDUNGEN AS PPAR和方法的代谢疾病的治疗调节剂
公开(公告)号：EP1735280A1
公开(公告)日：2006-12-27
申请号：EP05736067.9
申请日：2005-04-07
申请人： Kalypsys, Inc.
发明人： ZHAO, Cunxiang , MALECHA, James, W. , NOBLE, Stewart, A. , DURON, Sergio, Gonzalez , LINDSTROM, Andrew, Kenneth , SHIAU, Andrew, K.
IPC分类号： C07D211/96 , C07D241/04 , C07D213/74 , C07D487/08 , C07D263/58 , C07D277/82 , C07D239/42 , C07D401/04 , C07D417/04 , C07D241/20 , C07D317/66 , C07D307/79 , C07D237/20 , C07D307/46 , A61K31/451
CPC分类号： C07D211/96 , C07D213/74 , C07D237/20 , C07D239/42 , C07D241/20 , C07D263/58 , C07D277/82 , C07D295/26 , C07D307/46 , C07D307/79 , C07D317/66 , C07D401/04 , C07D417/04 , C07D487/08
摘要： Aryl sulfonamide and sulfonyl compounds of formula (I) as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.

8. 发明申请

WO2009032754A2 HETEROCYCLODIAZEPINE CANNABINOID RECEPTOR MODULATORS FOR TREATMENT OF DISEASE 审中-公开
标题翻译：用于治疗疾病的异鸟胆碱受体调节剂
公开(公告)号：WO2009032754A2
公开(公告)日：2009-03-12
申请号：PCT/US2008/074632
申请日：2008-08-28
申请人： KALYPSYS, INC. , GAHMAN, Timothy, C. , ZHAO, Cunxiang , LANG, Hengyuan , MASSARI, Mark, E.
发明人： GAHMAN, Timothy, C. , ZHAO, Cunxiang , LANG, Hengyuan , MASSARI, Mark, E.
IPC分类号： C07D471/04 , C07D487/04 , C07D491/044 , A61K31/4353
CPC分类号： C07D487/04 , C07D471/04 , C07D491/044
摘要： The present invention relates to compounds and methods useful as modulators of CB2 for the treatment or prevention of disease states including, but not limited to pain, autoimmune disease, malabsorption syndrome, pulmonary disease, osteoporosis, muscle spasm in cancer, neuromuscular disorder, and atherosclerosis progression.
摘要翻译：本发明涉及可用作CB2调节剂用于治疗或预防疾病状态的化合物和方法，包括但不限于疼痛，自身免疫疾病，吸收不良综合征，肺部疾病，骨质疏松症，癌症中的肌肉痉挛，神经肌肉疾病和动脉粥样硬化进展。

9. 发明申请

WO2005115983A1 ARYL SULFONAMIDE AND SULFONYL COMPOUNDS AS MODULATORS OF PPAR AND METHODS OF TREATING METABOLIC DISORDERS 审中-公开
标题翻译：作为PPAR的调节剂的ARYL SULFONAMIDE和SUFFYYL化合物和治疗代谢障碍的方法
公开(公告)号：WO2005115983A1
公开(公告)日：2005-12-08
申请号：PCT/US2005/011751
申请日：2005-04-07
申请人： KALYPSYS, INC. , ZHAO, Cunxiang , MALECHA, James, W. , NOBLE, Stewart, A. , DURON, Sergio, Gonzalez , LINDSTROM, Andrew, Kenneth , SHIAU, Andrew, K.
发明人： ZHAO, Cunxiang , MALECHA, James, W. , NOBLE, Stewart, A. , DURON, Sergio, Gonzalez , LINDSTROM, Andrew, Kenneth , SHIAU, Andrew, K.
IPC分类号： C07D211/96
CPC分类号： C07D211/96 , C07D213/74 , C07D237/20 , C07D239/42 , C07D241/20 , C07D263/58 , C07D277/82 , C07D295/26 , C07D307/46 , C07D307/79 , C07D317/66 , C07D401/04 , C07D417/04 , C07D487/08
摘要： Aryl sulfonamide and sulfonyl compounds of formula (I) as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
摘要翻译：公开了芳基磺酰胺和作为过氧化物酶体增殖物激活受体的调节剂的式（I）的磺酰基化合物，包含其的药物组合物和使用其的治疗疾病的方法。

10. 发明申请

WO2005060958A1 (5- (2-PHENYL)-THIAZOL-5-YLMETHOXY)-INDOL-1-YL) -ACETIC ACID DERIVATIVES AND RELATED COMPOUNDS AS MODULATORS OF THE HUMAN PPAR-DELTA RECEPTOR FOR THE TREATMENT OF METABOLIC DISORDERS SUCH AS TYPE 2 DIABETES 审中-公开
标题翻译：（5-（2-苯基） - 噻唑-5-基甲氧基） - 茚满-1-基） - 甲酸衍生物及相关化合物作为人类PPAR-DELTA受体的调节剂，用于治疗代谢异常症状，如2型糖尿病
公开(公告)号：WO2005060958A1
公开(公告)日：2005-07-07
申请号：PCT/US2004/043031
申请日：2004-12-20
申请人： KALYPSYS, INC. , MALECHA, James, William , ZHAO, Cunxiang , ROBINSON, Carmen, Ka, Man , DURON, Sergio, Gonzalez , SERTIC, Michael , NOBLE, Stewart, A.
发明人： MALECHA, James, William , ZHAO, Cunxiang , ROBINSON, Carmen, Ka, Man , DURON, Sergio, Gonzalez , SERTIC, Michael , NOBLE, Stewart, A.
IPC分类号： A61K31/404
CPC分类号： C07D417/12 , C07D277/24 , C07D277/26 , C07D413/06 , C07D417/06
摘要： Disclosed are compounds having the structure of Formula (I) and pharmaceutically acceptable salts and solvates thereof [A]-[B]-[C] (I) wherein (a) [A] is [H]-[L]; wherein [H] represents a CCOH (or a hydrolyzable ester thereof) or tetrazole group [L] is: formula (II), b) [B] is a ring system selected from the group consisting of: e.g. formula (III); (IIIA), c) [C] is e.g. formula (IV); the other substituents and variables are defined in the claims; as modulators of the human PPAR-delta receptor for the treatment of metabolic disorders such as type 2 diabetes.
摘要翻译：公开了具有式（I）结构的化合物及其药学上可接受的盐和溶剂合物[A] - [B] - [C]（I）其中（a）[A]是[H] - [L] 其中[H]表示CCOH（或其可水解酯）或四唑基[L]为：式（II），b）[B]是选自以下的环系：式（III）; （IIIA），c）[C]是例如。式（IV）; 其它取代基和变量在权利要求书中定义; 作为用于治疗代谢性疾病如2型糖尿病的人类PPAR-δ受体的调节剂。

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