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1. 发明申请

US20040102480A1 Phenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia 失效
标题翻译：苯氧基 - 乙酸可用于治疗胰岛素抵抗和高血糖症
公开(公告)号：US20040102480A1
公开(公告)日：2004-05-27
申请号：US10300997
申请日：2002-11-21
申请人： Wyeth
发明人： Michael S. Malamas , Jay E. Wrobel , Arlene J. Dietrich , Zenan Li , Iwan Gunawan
IPC分类号： A61K031/4439 , A61K031/427 , A61K031/422 , A61K031/4178 , C07D417/02 , C07D413/02 , C07D43/02
CPC分类号： C07D333/60 , C07D307/80 , C07D333/56
摘要： This invention provides compounds of Formula I having the structure 1 wherein: A is O, S, or N; B is null(CH2)mnull, nullCH(OH)null, or carbonyl; R1 is hydrogen, halogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, or trifluoromethyl; R2 is alkyl of 1-18 carbon atoms, aryl of 6-10 carbon atoms, arylalkyl of 7-15 carbon atoms, Het-alkyl wherein the alkyl moiety is 1-6 carbon atoms; Het is 2 R2a is alkylene of 1-3 carbon atoms; G is oxygen, sulfur, or nitrogen; R3, R4 are each, independently, hydrogen, halogen, alkyl of 1-3 carbon atoms, aryl of 6-10 carbon atoms or a heterocyclic ring of 5 to 7 ring atom containing 1 to 3 heteroatoms selected from oxygen, nitrogen, sulfur; R5 is hydrogen, alkyl of 1-6 carbon atoms, nullCH(R7)R8, nullC(CH2)nCO2R9, nullC(CH3)2CO2R9, nullCH(R7)(CH2)nCO2R9, or CH(R7)C6H4CO2R9; R6 is hydrogen, halogen, alkyl of 1-6 carbon atoms, or nullOR5; mnull1-6; nnull1-6; R7 is hydrogen, alkyl of 1-6 carbon atoms, aryl of 6-10 carbon atoms, or arylalkyl of 7-15 carbon atoms; R8 is nullCO2R10, nullCONHR10, tetrazole, or nullPO3; R9 and R10 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, aryl of 6-10 carbon atoms, or arylalkyl of 7-15 carbon atoms; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
摘要翻译：本发明提供具有以下结构的式I化合物：其中：A是O，S或N; B是 - （CH 2）m - ， - CH（OH） - 或羰基; R 1是氢，卤素，1-6个碳原子的烷基，1-6个碳原子的烷氧基或三氟甲基; R 2是1-18个碳原子的烷基，6-10个碳原子的芳基，7-15个碳原子的芳基烷基，其中烷基部分是1-6个碳原子的Het-烷基; Het是R 2a是1-3个碳原子的亚烷基; G是氧，硫或氮; R 3，R 4各自独立地为氢，卤素，1-3个碳原子的烷基，6-10个碳原子的芳基或含有1至3个选自以下的杂原子的5至7个环原子的杂环：氧，氮，硫; R 5是氢，1-6个碳原子的烷基，-CH（R 7）R 8，-C（CH 2）n CO 2 R 9，-C（CH 3）2 CO 2 R 9，-CH （R 7）（CH 2）n CO 2 R 9或CH（R 7）C 6 H 4 CO 2 R 9; R 6是氢，卤素，1-6个碳原子的烷基或-OR 5; m = 1-6; n = 1-6; R 7是氢，1-6个碳原子的烷基，6-10个碳原子的芳基或7-15个碳原子的芳基烷基; R 8是-CO 2 R 10，-CONHR 10，四唑或-PO 3; R 9和R 10各自独立地为氢，1-6个碳原子的烷基，6-10个碳原子的芳基或7-15个碳原子的芳基烷基; 或其药学上可接受的盐，其可用于治疗与胰岛素抵抗或高血糖相关的代谢紊乱。

2. 发明申请

US20030207927A1 Phenyl benzisoxazoles as estrogenic agents 失效
标题翻译：苯基苯并恶唑作为雌激素剂
公开(公告)号：US20030207927A1
公开(公告)日：2003-11-06
申请号：US10316616
申请日：2002-12-11
申请人： Wyeth
发明人： Michael S. Malamas , Tam Q. Dinh , Iwan Gunawan , Michael D. Collini , Heather A. Harris , James C. Keith JR. , Leo M. Albert
IPC分类号： C07D275/04 , C07D275/06 , C07D261/20 , A61K031/425 , A61K031/42
CPC分类号： C07D261/20
摘要： This invention provides estrogen receptor modulators of formula I, having the structure 1 wherein, R1, R2, and R3 are as defined in the specification, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供式I的雌激素受体调节剂，其具有其中R 1，R 2和R 3如说明书中所定义的结构或其药学上可接受的盐。

3. 发明申请

US20030199562A1 Substituted benzoxazoles as estrogenic agents 失效
公开(公告)号：US20030199562A1
公开(公告)日：2003-10-23
申请号：US10309699
申请日：2002-12-04
申请人： Wyeth
发明人： Michael S. Malamas , Robert E. McDevitt , Iwan Gunawan , Eric S. Manas , Michael D. Collini , Heather A. Harris , James C. Keith JR. , Leo M. Albert , C. Richard Lyttle
IPC分类号： A61K031/428 , A61K031/423 , A61K031/4184
CPC分类号： C07D263/57 , C07D235/18 , C07D277/66 , C07D413/04 , C07D417/04
摘要： This invention provides estrogen receptor modulators of formula I, having the structure 1 wherein R1, R2, R2a, R3, R3a, and R4, and X as defined in the specification, or a pharmaceutically acceptable salt thereof.

4. 发明申请

US20030171412A1 Naphthyl benzoxazoles and benzisoxazoles as estrogenic agents 失效
标题翻译：萘基苯并恶唑和苯并异恶唑作为雌激素
公开(公告)号：US20030171412A1
公开(公告)日：2003-09-11
申请号：US10316641
申请日：2002-12-11
申请人： Wyeth
发明人： Michael S. Malamas , Iwan Gunawan , Heather A. Harris , James C. Keith JR. , Leo M. Albert
IPC分类号： A61K031/428 , A61K031/422 , A61K031/423 , A61K031/4184 , C07D277/62 , C07D275/06 , C07D263/60
CPC分类号： C07D263/57 , C07D231/56 , C07D261/20
摘要： This invention provides estrogen receptor modulators of formula 1, having the structure 1 wherein R1, R2, R3, and R4, and X as defined in the specification, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供式1的雌激素受体调节剂，其具有如说明书中所定义的R 1，R 2，R 3和R 4以及X的结构或其药学上可接受的盐。

5. 发明申请

US20030055079A1 Azolidines as beta-3 adrenergic receptor agonists 失效
公开(公告)号：US20030055079A1
公开(公告)日：2003-03-20
申请号：US10227225
申请日：2002-08-23
申请人： Wyeth
发明人： Michael Sotirios Malamas , Elwood Eugene Largis , Iwan Gunawan , Zenan Li
IPC分类号： C07D498/02 , C07D491/02 , C07D471/02 , C07D417/02 , C07D413/02 , C07D43/02
CPC分类号： C07D417/12 , C07D277/42
摘要： This invention provides compounds of Formula I having the structure 1 wherein, A, X, Y, Z, W, R1, R2, R3, R4, R5, and R6 are as defined hereinbefore or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.

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