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1. 发明申请

WO2004093799A3 THYROID RECEPTOR LIGANDS 审中-公开
公开(公告)号：WO2004093799A3
公开(公告)日：2004-11-04
申请号：PCT/US2004/011883
申请日：2004-04-16
申请人： BRISTOL-MYERS SQUIBB COMPANY , RYONO, Dennis, E. , HANGELAND, Jon, J. , FRIENDS, Todd, J. , DEJNEKA, Tamara , DEVASTHALE, Pratik , CARINGAL, Yolanda, V. , ZHANG, Minsheng , DOWEYKO, Arthur, M.P. , MALM, Johan , SANIN, Andrei
发明人： RYONO, Dennis, E. , HANGELAND, Jon, J. , FRIENDS, Todd, J. , DEJNEKA, Tamara , DEVASTHALE, Pratik , CARINGAL, Yolanda, V. , ZHANG, Minsheng , DOWEYKO, Arthur, M.P. , MALM, Johan , SANIN, Andrei
IPC分类号： A61K31/16
摘要： Thyroid receptor ligands are provided which have the general formula (I), wherein: R1 is formula (II); R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, provided that at least one of R2 and R3 is other than hydrogen; R4 is formula (III); R5 and R6 are the same or different and are selected from hydrogen, aryl, heteroaryl, alkyl, cycloalkyl, aralkyl or heteroaralkyl. R7 is aryl, heteroaryl, alkyl, aralkyl, or heteroaralkyl; R8 is aryl, heteroaryl, or cycloalkyl; R9 is R7 or hydrogen; R10 is hydrogen, halogen, cyano or alkyl; R11 and R12 are each independently selected from the group consisting of hydrogen, halogen, alkoxy, hydroxy (-OH) cyano, and alkyl; R13 is carboxylic acid (COOH) or esters thereof, phosphonic and phosphinic acid or esters thereof, sulfonic acid, tetrazole, hydroxamic acid, thiazolidinedione, acylsulfonamide, or other carboxylic acid surrogates known in the art; R14 and R15 may be the same or different and are selected from hydrogen and alkyl, or R14 and R15 may be joined together forming a chain of 2 to 5 methylene groups [-(CH2)m-, m = 2, 3, 4 or 5], thus forming 3- to 6-membered cycloalkyl rings; R16 is hydrogen or alkyl of 1 to 4 carbons; R17 and R18 are the same or different and selected from hydrogen, halogen and alkyl; n is 0 or an integer from 1 to 4; X is oxygen (-O-), sulfur (-S-), sulfonyl (-SO2-), sulfenyl (-SO-) selenium (-Se-), carbonyl (-CO-), amino (-NH-) or methylene (-CH2-); wherein the substituents are as described herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T 3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.

2. 发明申请

WO2005009392A2 DIHYDROPYRIMIDONE INHIBITORS OF CALCIUM CHANNEL FUNCTION 审中-公开
标题翻译：钙通道功能的二氢吲哚酮抑制剂
公开(公告)号：WO2005009392A2
公开(公告)日：2005-02-03
申请号：PCT/US2004/023909
申请日：2004-07-23
申请人： BRISTOL-MYERS SQUIBB COMPANY , BISACCHI, Gregory, S. , MURUGESAN, Natesan , EWING, William, R. , YU, Guixue , GU, Zhengxiang , FRIENDS, Todd, J. , ZHANG, Minsheng
发明人： BISACCHI, Gregory, S. , MURUGESAN, Natesan , EWING, William, R. , YU, Guixue , GU, Zhengxiang , FRIENDS, Todd, J. , ZHANG, Minsheng
IPC分类号： A61K
CPC分类号： C07D239/28 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/04 , C07D417/12
摘要： Compounds having the Formula (I) enantiomers, diastereomers, solvates and salts thereof, where R 1 , R 2 , R 3 , R 4 , A, X, and J are described herein, are inhibitors of calcium channel function, and are useful in treating calcium channel-dependent disorders, including hypertension.
摘要翻译：其中R 1，R 2，R 3，R 4，A，X和J在本文中描述的具有式（I）对映异构体，非对映异构体，溶剂合物和盐的化合物是钙通道功能，并且可用于治疗钙通道依赖性疾病，包括高血压。

3. 发明申请

WO2003094845A3 PYRIDINE-BASED THYROID RECEPTOR LIGANDS 审中-公开
公开(公告)号：WO2003094845A3
公开(公告)日：2003-11-20
申请号：PCT/US2003/014222
申请日：2003-05-07
申请人： BRISTOL-MYERS SQUIBB COMPANY , ZHANG, Minsheng , HANGELAND, Jon , CARINGAL, Yolanda , FRIENDS, Todd
发明人： ZHANG, Minsheng , HANGELAND, Jon , CARINGAL, Yolanda , FRIENDS, Todd
IPC分类号： C07D213/30
摘要： Novel pyridine-based thyroid receptor ligands are provided which have the general formula (I) wherein: X is oxygen (-O-), sulfur (-S-), sulfoxide (-S(O)-), sulfonyl (-SO 2 -), CR 8 R 8 ' or NR 8 ; Y is -NR 8 , oxygen (-O-), -CH 2 - or sulfur (-S-); Z is a bond or substituted or unsubstituted C 1-4 alkyl; and wherein the substituents are as described herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T 3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.

4. 发明申请

WO2003094845A2 PYRIDINE-BASED THYROID RECEPTOR LIGANDS 审中-公开
标题翻译：基于吡啶的甲状腺受体配体
公开(公告)号：WO2003094845A2
公开(公告)日：2003-11-20
申请号：PCT/US2003/014222
申请日：2003-05-07
申请人： BRISTOL-MYERS SQUIBB COMPANY , ZHANG, Minsheng , HANGELAND, Jon , CARINGAL, Yolanda , FRIENDS, Todd
发明人： ZHANG, Minsheng , HANGELAND, Jon , CARINGAL, Yolanda , FRIENDS, Todd
IPC分类号： A61K
CPC分类号： C07D213/69 , C07D213/68 , C07D213/70 , C07D213/73 , C07D213/74 , C07D213/75 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12
摘要： Novel pyridine-based thyroid receptor ligands are provided which have the general formula (I) wherein: X is oxygen (-O-), sulfur (-S-), sulfoxide (-S(O)-), sulfonyl (-SO 2 -), CR 8 R 8 ' or NR 8 ; Y is -NR 8 , oxygen (-O-), -CH 2 - or sulfur (-S-); Z is a bond or substituted or unsubstituted C 1-4 alkyl; and wherein the substituents are as described herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T 3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.
摘要翻译：提供了具有通式（I）的新型吡啶类甲状腺受体配体，其中：X是氧（-O-），硫（-S-），亚砜（-S（O） - ），磺酰基（-SO 2 - ），CR8R8'或NR8; Y是-NR 8，氧（-O-），-CH 2 - 或硫（-S-）; Z是键或取代或未取代的C 1-4烷基; 并且其中取代基如本文所述。此外，提供了一种用于预防，抑制或治疗与代谢功能障碍相关或依赖于T3调节基因的表达的疾病或病症的方法，其中如上所述的化合物以治疗有效量施用。

5. 发明申请

WO2010077839A1 SUBSTITUTED OXINDOL CB2 AGONISTS FOR PAIN TREATMENT 审中-公开
标题翻译：用于治疗疼痛的替代OXINDOL CB2激动剂
公开(公告)号：WO2010077839A1
公开(公告)日：2010-07-08
申请号：PCT/US2009/067967
申请日：2009-12-15
申请人： WYETH LLC (FORMERLY KNOWN AS WYETH) , DOLLINGS, Paul, Jeffrey , DONNELL, Andrew, Forrest , GILBERT, Adam, Matthew , ZHANG, Minsheng , HARRISON, Boyd, Lynn , STANTON III, Charles, John , O'NEIL, Steven, Victor , HAVRAN, Lisa, Marie , CHONG, Dan, Chaekoo
发明人： DOLLINGS, Paul, Jeffrey , DONNELL, Andrew, Forrest , GILBERT, Adam, Matthew , ZHANG, Minsheng , HARRISON, Boyd, Lynn , STANTON III, Charles, John , O'NEIL, Steven, Victor , HAVRAN, Lisa, Marie , CHONG, Dan, Chaekoo
IPC分类号： C07D209/34 , C07D209/38 , C07D491/10 , A61K31/404 , A61P25/04
CPC分类号： C07D491/10 , C07D209/34 , C07D209/38
摘要： Provided are 3-substituted oxindole derivatives which are agonists of the CB2 receptor, pharmaceutical compositions containing the same, and methods of treatment related to CB2-mediated disorders (e.g., pain, cancer etc.) using the 3-substituted oxindole derivatives and compositions described herein.
摘要翻译：提供作为CB 2受体的激动剂的3-取代的羟基吲哚衍生物，含有它们的药物组合物，以及使用3-取代的羟基吲哚衍生物和所述组合物与CB2介导的病症（例如疼痛，癌症等）有关的治疗方法于此。

6. 发明申请

WO2012116050A2 PHOSPHORUS CONTAINING COMPOUNDS AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：含有蛋白质的化合物作为蛋白激酶抑制剂
公开(公告)号：WO2012116050A2
公开(公告)日：2012-08-30
申请号：PCT/US2012/026083
申请日：2012-02-22
申请人： ETERNITY BIOSCIENCE INC. , HU, Baihua , HE, Kan , ZHANG, Minsheng
发明人： HU, Baihua , HE, Kan , ZHANG, Minsheng
IPC分类号： A61K31/675 , C07F9/58 , C07F9/6558 , C07F9/6509 , A61P35/00
CPC分类号： C07F9/582 , C07F9/588 , C07F9/650964 , C07F9/65583
摘要： The present invention relates to compounds represented by formula (I), which can modulate the activity of protein kinases. The invention also relates to a composition containing a compound of formula (I), and a method for synthesizing and using such compound for preventing or treating ALK or cMet mediated disorders or conditions.
摘要翻译：本发明涉及可以调节蛋白激酶活性的由式（I）表示的化合物。本发明还涉及包含式（I）化合物的组合物，以及用于合成和使用该化合物以预防或治疗ALK或cMet介导的病症或病症的方法。

7. 发明申请

WO2008080120A3 3-AMINO CHROMANE DERIVATIVES 审中-公开
公开(公告)号：WO2008080120A3
公开(公告)日：2008-07-03
申请号：PCT/US2007/088693
申请日：2007-12-21
申请人： WYETH , ZHANG, Minsheng , STANTON, Charles, J., III , HATZENBUHLER, Nicole, T. , HARRISON, Boyd, Lynn
发明人： ZHANG, Minsheng , STANTON, Charles, J., III , HATZENBUHLER, Nicole, T. , HARRISON, Boyd, Lynn
IPC分类号： C07D405/12 , A61K31/33 , A61P25/00
摘要： The present invention relates to 3-amino chromane derivatives; to compositions containing such compounds; to methods of synthesizing such compounds; and to methods of using such compounds and compositions containing such compounds in the treatment of serotonin disorders, such as depression and anxiety.

8. 发明申请

WO2004092155A1 FLUORO-AND TRIFLUOROALKYL-CONTAINING HETEROCYCLIC SULFONAMIDE INHIBITORS OF BETA AMYLOID PRODUCTION AND DERIVATIVES THEREOF 审中-公开
标题翻译：含氟和含三氟甲磺酸的苯甲酰胺酰胺抑制剂的制备及其衍生物
公开(公告)号：WO2004092155A1
公开(公告)日：2004-10-28
申请号：PCT/US2004/009268
申请日：2004-03-26
申请人： WYETH , KREFT, Anthony, Frank , RESNICK, Lynn , MAYER, Scott, Christian , DIAMANTIDIS, George , COLE, Derek, Cecil , WANG, Tingzhong , GALANTE, Rocco, John , HOKE, Molly , HARRISON, Boyd, Lynn , ZHANG, Minsheng
发明人： KREFT, Anthony, Frank , RESNICK, Lynn , MAYER, Scott, Christian , DIAMANTIDIS, George , COLE, Derek, Cecil , WANG, Tingzhong , GALANTE, Rocco, John , HOKE, Molly , HARRISON, Boyd, Lynn , ZHANG, Minsheng
IPC分类号： C07D333/34
CPC分类号： C07D333/62 , C07D231/18 , C07D333/34
摘要： Compounds of Formula (I), are provided where T is CHO, COR 8 , or C(OH)R 1 R 2 ; R 1 and R 2 are hydrogen, optionally substituted lower alkyl, CF 3 , optionally substituted alkenyl, or optionally substituted alkynyl; R 3 is hydrogen or optionally substituted lower alkyl; R 4 is (CF 3 ) n alkyl, (CF 3 ) n (substitutedalkyl), (CF 3 ) n alkylphenyl, (CF 3 )nalkyl(substitutedphenyl), or (F) n cycloalkyl; n=1-3; R 5 is hydrogen, halogen, CF 3 , diene fused to Y when Y=C, or substituted diene fused to Y when Y=C; W, Y and Z are C, CR 6 or N where at least one of W, Y or Z are C; R 6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO 2 , or NR 7 ; R 7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R 8 is lower alkyl, CF 3 , or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.
摘要翻译：提供式（I）化合物，其中T是CHO，COR8或C（OH）R 1 R 2; R 1和R 2是氢，任选取代的低级烷基，CF 3，任选取代的烯基或任选取代的炔基; R3是氢或任选取代的低级烷基; R4是（CF3）n烷基，（CF3）n（取代烷基），（CF3）n烷基苯基，（CF3）n烷基（取代苯基）或（F）n环烷基; N = 1-3; 当Y = C时，R 5为氢，卤素，CF 3，与Y稠合的二烯，或Y = C时与Y稠合的取代二烯; W，Y和Z是C，CR 6或N，其中W，Y或Z中的至少一个是C; R6是氢，卤素或任选取代的低级烷基; X是O，S，SO 2或NR 7; R 7是氢，任选取代的低级烷基，任选取代的苄基或任选取代的苯基; 且R 8为低级烷基，CF 3或任选取代的苯基。还描述了制备和使用这些化合物抑制β-淀粉样蛋白产生和治疗阿尔茨海默病和唐氏综合征的方法。

9. 发明申请

WO2012125521A1 QUINAZOLINEDIONES AND THEIR USE 审中-公开
标题翻译：喹诺酮类及其用途
公开(公告)号：WO2012125521A1
公开(公告)日：2012-09-20
申请号：PCT/US2012/028698
申请日：2012-03-12
申请人： ETERNITY BIOSCIENCE INC. , LIU, Dong , ZHANG, Minsheng , HE, Kan , ZHANG, Lianshan
发明人： LIU, Dong , ZHANG, Minsheng , HE, Kan , ZHANG, Lianshan
IPC分类号： C07D239/80
CPC分类号： C07D239/96 , C07D239/80 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04 , C07D487/04
摘要： The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts or prodrugs thereof, which inhibit the poly(ADP-ribose) polymerases (PARP) and therefore are useful for treating diseases, disorders, and conditions related to PARP. The present invention also discloses pharmaceutical compositions comprising a compound of formula (I), and methods of using such compounds to inhibit PARP enzymes, and to treat diseases, disorders, and conditions related to PARP.
摘要翻译：本发明公开了抑制聚（ADP-核糖）聚合酶（PARP）的式（I）化合物或其药学上可接受的盐或前药，因此可用于治疗与PARP相关的疾病，病症和病症。本发明还公开了包含式（I）化合物的药物组合物，以及使用这些化合物抑制PARP酶以及治疗与PARP有关的疾病，病症和病症的方法。

10. 发明申请

WO2010090680A1 SUBSTITUTED OXINDOLE CB2 AGONISTS 审中-公开
标题翻译：替代氧化物CB2激动剂
公开(公告)号：WO2010090680A1
公开(公告)日：2010-08-12
申请号：PCT/US2009/067981
申请日：2009-12-15
申请人： WYETH LLC , ZHANG, Minsheng , HARRISON, Boyd Lynn , STANTON, Charles J. III , HAVRAN, Lisa Marie , CHONG, Dan Chaekoo , CHILDERS, Wayne Everett , O'NEIL, Steven Victor
发明人： ZHANG, Minsheng , HARRISON, Boyd Lynn , STANTON, Charles J. III , HAVRAN, Lisa Marie , CHONG, Dan Chaekoo , CHILDERS, Wayne Everett , O'NEIL, Steven Victor
IPC分类号： C07D491/10 , A61K31/407
CPC分类号： C07D491/10
摘要： Provided are substituted compounds, or pharmaceutically acceptable salts thereof, wherein: R 1 is selected from -(CH 2 )nR a , -CH(OH)R a , -CH(OR b )R a , and -C(O)R a , or is selected from OR a , SR a , SOR a , SO 2 R a and NR a R b ; R 2 and R 3 are independently selected from H, halogen, OH, OR a , OWR a , C 1-6 alkyl, and WC 1-6 alkyl, wherein C 1-6 alkyl or OR a , is optionally substituted with 1, 2, or 3 substitutents independently selected from halogen, CN, OH, OR a , C 1-6 alkyl, C 1-6 haloalkyl, C 3-8 cycloalkyl, C 6-10 aryl and C 4-10 heteroaryl; or R 2 and R 3 , together with the carbon atom to which they are attached, join to form a ring selected from 3-8 membered cycloalkyl, 3-8 membered heterocycloalkyl, C 5 -C 7 oxycycloalkyl, C 5 . 7 dioxycycloalkyl and oxazolidinyl ring, each ring optionally substituted with 1, 2, or 3 substituents independently selected from halogen, CN, OH, 0R a , C 1-6 alkyl, C 1-6 haloalkyl, C 3-8 cycloalkyl, C 6-10 aryl and C 4-10 heteroaryl; R 4 is independently selected from H.C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 6-10 aryl, C 4-10 heteroaryl, -(CH 2 ) n -benzodioxane, -(CH 2 ) n - oxazolidinone and -(CH 2 ) n -C 1-6 haloalkyl, each of which is optionally substituted with 1, 2, or 3 substitutents independently selected from halogen, CN, OH, OR a , C 1-6 alkyl, C 1-6 haloalkyl, C 3.8 cycloalkyl, WC 3.8 cycloalkyl, C 6-10 aryl and C 4.10 heteroaryl; which are agonists of the CB2 receptor, pharmaceutical compositions containing the same, and methods of treatment related to CB2-mediated disorders (eg., pain, cancer etc.) using the substituted oxindole compounds and compositions described herein.
摘要翻译：提供了取代的化合物或其药学上可接受的盐，其中：R 1选自 - （CH 2）nR a，-CH（OH）R a，-CH（OR b）R a和-C（O）R a，或选自OR a ，SRa，SORa，SO2Ra和NRaRb; R 2和R 3独立地选自H，卤素，OH，OR a，OWR a，C 1-6烷基和WC 1-6烷基，其中C 1-6烷基或OR a任选被1,2或3个独立选择的取代基取代卤素，CN，OH，OR a，C 1-6烷基，C 1-6卤代烷基，C 3-8环烷基，C 6-10芳基和C 4-10杂芳基; 或R 2和R 3与它们所连接的碳原子连接形成选自3-8元环烷基，3-8元杂环烷基，C5-C7氧环烷基，C5.7二氧环烷基和恶唑烷基环的环，每个环任选地被1,2或3个独立地选自卤素，CN，OH，ORa，C 1-6烷基，C 1-6卤代烷基，C 3-8环烷基，C 6-10芳基和C 4-10杂芳基的取代基取代; R 4独立地选自H.C 1-6烷基，C 2-6烯基，C 2-6炔基，C 6-10芳基，C 4-10杂芳基， - （CH 2）n-苯并二恶烷， - （CH 2）n恶唑烷酮和 - （CH 2 ）n-C 1-6卤代烷基，其各自任选被1,2或3个独立地选自卤素，CN，OH，OR a，C 1-6烷基，C 1-6卤代烷基，C 3-8环烷基，WC 3的取代基取代。 8环烷基，C6-10芳基和C4.10杂芳基; 其是CB 2受体的激动剂，含有它们的药物组合物，以及使用本文所述的取代的羟吲哚化合物和组合物与CB2介导的病症（例如，疼痛，癌症等）有关的治疗方法。

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