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1. 发明申请

WO2003053361A3 PYRROLOPYRIMIDINE A2b SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE 审中-公开
公开(公告)号：WO2003053361A3
公开(公告)日：2003-07-03
申请号：PCT/US2002/040890
申请日：2002-12-20
申请人： OSI PHARMACEUTICALS, INC. , CASTELHANO, Arlindo, L. , McKIBBEN, Bryan , STEINIG, Arno, G.
发明人： CASTELHANO, Arlindo, L. , McKIBBEN, Bryan , STEINIG, Arno, G.
IPC分类号： C07D487/04
摘要： A compound having the structure wherein, R 1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, -C(=O)NR a R b , -NR a R b , -NRaC(=O)NR a R b , -NR a C(=O)OR a , -OC(=O)NR a R b , or -NHC(=O)R a ; R 2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxyl, carboxyl, -C(=O)NR a R b , -NR a R b , -NR a C(=O)NR a R b , -NR a C(=O)OR a , -OC(=O)NR a R b , or -NHC(=O)R a , or R 1 , R 2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with -(CH 2 ) 2 OH or -CH 2 C(=O)OH; R 3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C 1 -C 15 )alkyl, (C 1 -C 15 )alkoxyl, or -NR a R b ; R 4 is hydrogen or substituted or unsubstituted (C 1 -C 15 )alkyl; R 5 is -(CH 2 ) m OR 6 , -CHNOR 7 , -C(=O)NR 8 R 9 , -(CH 2 ) m C(=O)OR 10 , -(CH 2 ) k C(=O)NR 11 R 12 .

2. 发明申请

WO2003053361A2 PYRROLOPYRIMIDINE A2b SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE 审中-公开
标题翻译：吡咯烷酮A2b选择性拮抗剂化合物，它们的合成和用途
公开(公告)号：WO2003053361A2
公开(公告)日：2003-07-03
申请号：PCT/US2002/040890
申请日：2002-12-20
申请人： OSI PHARMACEUTICALS, INC. , CASTELHANO, Arlindo, L. , McKIBBEN, Bryan , STEINIG, Arno, G.
发明人： CASTELHANO, Arlindo, L. , McKIBBEN, Bryan , STEINIG, Arno, G.
IPC分类号： A61K
CPC分类号： C07D487/04
摘要： The subject invention provides compounds having the structure: wherein, R 1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, -C(=O)NR a R b , -NR a R b , -NRaC(=O)NR a R b , -NR a C(=O)OR a , -OC(=O)NR a R b , or -NHC(=O)R a ; R 2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxyl, carboxyl, -C(=O)NR a R b , -NR a R b , -NR a C(=O)NR a R b , -NR a C(=O)OR a , -OC(=O)NR a R b , or -NHC(=O)R a , or R 1 , R 2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with -(CH 2 ) 2 OH or -CH 2 C(=O)OH; R 3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C 1 -C 15 )alkyl, (C 1 -C 15 )alkoxyl, or -NR a R b ; R 4 is hydrogen or substituted or unsubstituted (C 1 -C 15 )alkyl; R 5 is -(CH 2 ) m OR 6 , -CHNOR 7 , -C(=O)NR 8 R 9 , -(CH 2 ) m C(=O)OR 10 , -(CH 2 ) k C(=O)NR 11 R 12 ; wherein R 6 is a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring; R 7 is hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl; R 8 and R 9 are each independently hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl, (C 1 -C 30 )alkylamino, (C 1 -C 30 )alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R 8 , N, and R 9 together form a substituted or unsubstituted 4-8 membered heterocyclic ring; R 10 is hydrogen or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or heterocyclic ring; R 11 , N and R 12 together form a 4-8 membered heterocyclic ring; R a and R b are each independently hydrogen or alkyl; m is 0, 1, 2 or 3; and k is 1, 2 or 3, or a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A 2b adenosine receptor in a subject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention.
摘要翻译：具有以下结构的化合物，其中R 1是取代或未取代的烷基，其中所述取代基是羟基，二羟基，羧基，-C（= O）NR b R a， sb> b ，-NR a R sb> b ，-NR a C（= O）NR a s b> （= O）OR a sb>，-OC（= O）NR a s b> a a sb>或-NHC（= O）R sb> a ; R 2是氢或取代或未取代的烷基，其中所述取代基是羟基，二羟基，羧基，-C（= O）NR b R a R b， sb>，-NR a b a a R b s b C b C b C a C b C b C b C b C a C b R b s > b ，-NR a C（= O）OR a ，-OC（= O）NR a 或者-NHC（= O）R a a a / bb，或R 1，R 2和R 3共同形成取代基哌嗪，取代的氮杂环丁烷环，或被 - （CH 2）2 - （OH）或-CH 2 S 2 C（= O）OH取代的吡咯烷环 ; R 3是取代或未取代的苯基或5-6元杂芳基环，其中取代基是卤素，羟基，氰基，（C 1 -C 15）-C 15 烷基，（C 1 -C 15烷基）烷氧基，或-NR b R b，b b b， ; R 4是氢或取代或未取代的（C 1 -C 15）烷基; R 5是-S（CH 3）2，其中R 1是-S（CH 3）s，，-C（= O）NR 8 R 9， - （CH 2）s（= O））OR 10 ， - （CH 2 ） k C（= O）NR 11 < 。

3. 发明申请

WO2003048120A2 COMPOUNDS SPECIFIC TO ADENOSINE A1 AND A3 RECEPTORS AND USES THEREOF 审中-公开
标题翻译：腺苷A1和A3受体特异性化合物及其用途
公开(公告)号：WO2003048120A2
公开(公告)日：2003-06-12
申请号：PCT/US2002/038055
申请日：2002-11-27
申请人： OSI PHARMACEUTICALS, INC. , CASTELHANO, Arlindo, L. , McKIBBEN, Bryan , WERNER, Douglas, S. , WITTER, David
发明人： CASTELHANO, Arlindo, L. , McKIBBEN, Bryan , WERNER, Douglas, S. , WITTER, David
IPC分类号： C07D
CPC分类号： C07D487/04
摘要： This invention pertains to compounds which specifically inhibit the adenosine A 1 and A 3 receptors and the use of these compounds to treat a disease associated with A 3 adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
摘要翻译：本发明涉及特异性抑制腺苷A1和A3受体的化合物以及这些化合物用于治疗受试者中与A3腺苷受体相关的疾病的用途，其包括向受试者施用治疗有效量的化合物。

4. 发明申请

WO2005021531A1 N-SUBSTITUTED BENZIMIDAZOLYL C-KIT INHIBITORS 审中-公开
标题翻译： N-取代苯并咪唑C-CIT抑制剂
公开(公告)号：WO2005021531A1
公开(公告)日：2005-03-10
申请号：PCT/US2004/026482
申请日：2004-08-16
申请人： OSI PHARMACEUTICALS, INC. , BOLGER, Joshua , CASTELHANO, Arlindo, L. , CREW, Andrew, Philip , DONG, Han-Qing , HONDA, Ayako , LAUFER, Radoslaw , LI, An-Hu , MULVIHILL, Kristen , QUI, Li , SAMBROOK, SMITH, Colin, Peter , SUN, Yingchuan , WYNNE, Graham, Michael , ZHANG, Tao
发明人： BOLGER, Joshua , CASTELHANO, Arlindo, L. , CREW, Andrew, Philip , DONG, Han-Qing , HONDA, Ayako , LAUFER, Radoslaw , LI, An-Hu , MULVIHILL, Kristen , QUI, Li , SAMBROOK, SMITH, Colin, Peter , SUN, Yingchuan , WYNNE, Graham, Michael , ZHANG, Tao
IPC分类号： C07D401/12
CPC分类号： C07D235/06 , C04B35/632 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14
摘要： Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐或N-氧化物可用于治疗癌症。

5. 发明申请

WO2005021537A1 N-SUBSTITUTED PYRAZOLYL-AMIDYL-BENZIMIDAZOLYL C-KIT INHIBITORS 审中-公开
标题翻译： N-取代的吡唑并咪唑基苯并咪唑C-CIT抑制剂
公开(公告)号：WO2005021537A1
公开(公告)日：2005-03-10
申请号：PCT/US2004/026481
申请日：2004-08-16
申请人： OSI PHARMACEUTICALS, INC. , BOLGER, Joshua , CASTELHANO, Arlindo, L. , CREW, Andrew, Phillip , LAUFER, Radoslaw , LI, An-Hu , SAMBROOK, SMITH, Colin, Peter , SUN, Yingchuan
发明人： BOLGER, Joshua , CASTELHANO, Arlindo, L. , CREW, Andrew, Phillip , LAUFER, Radoslaw , LI, An-Hu , SAMBROOK, SMITH, Colin, Peter , SUN, Yingchuan
IPC分类号： C07D403/12
CPC分类号： C07D403/12
摘要： Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐或N-氧化物可用于治疗癌症。

6. 发明申请

WO2007067709A1 PROCESS TO PREPARE SUBSTITUTED IMIDAZOPYRAZINE COMPOUNDS 审中-公开
标题翻译：制备取代的咪唑并吡嗪化合物的方法
公开(公告)号：WO2007067709A1
公开(公告)日：2007-06-14
申请号：PCT/US2006/046764
申请日：2006-12-07
申请人： OSI PHARMACEUTICALS, INC. , MULVIHILL, Kristen, Michelle , CASTELHANO, Arlindo, L.
发明人： MULVIHILL, Kristen, Michelle , CASTELHANO, Arlindo, L.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A method of preparing formula (A) ,wherein, X=C1, Br, I, comprises the step of treating formula (B), with N-chloro-, N-bromo-, or N-iodosuccinimide in a compatible solvent such as dimethylformamide (DMF) at 0-60° C followed by halogenation.
摘要翻译：制备式（A）的方法，其中X = Cl，Br，I包括用相容溶剂中的N-氯 - ，N-溴 - 或N-碘代琥珀酰亚胺处理式（B）的步骤，例如二甲基甲酰胺（DMF），0-60℃，随后卤化。

7. 发明申请

WO2009117482A8 MTOR INHIBITOR SALT FORMS 审中-公开
公开(公告)号：WO2009117482A8
公开(公告)日：2009-09-24
申请号：PCT/US2009/037505
申请日：2009-03-18
申请人： OSI PHARMACEUTICALS, INC , CASTELHANO, Arlindo, L. , MULVIHILL, Kristen, Michelle , VISOR, Gary, C. , RECHKA, Josef, A.
发明人： CASTELHANO, Arlindo, L. , MULVIHILL, Kristen, Michelle , VISOR, Gary, C. , RECHKA, Josef, A.
IPC分类号： C07D487/04 , A61K45/06
摘要： Salt forms of mTOR inhibitors of the Formula (I) and methods of preparation, formulation, and use in treating disease.

8. 发明申请

WO2006034111A1 (ARYLAMIDOARYL)SQUARAMIDE COMPOUNDS 审中-公开
标题翻译：（ARYLAMIDOARYL）磺酰胺化合物
公开(公告)号：WO2006034111A1
公开(公告)日：2006-03-30
申请号：PCT/US2005/033319
申请日：2005-09-15
申请人： OSI PHARMACEUTICALS, INC. , CREW, Andrew , LI, An-Hu , QIU, Li , CASTELHANO, Arlindo, L. , DONG, Hanqing , SMITH, Alun , TARDIBONO, Lawrence , ZHANG, Tao
发明人： CREW, Andrew , LI, An-Hu , QIU, Li , CASTELHANO, Arlindo, L. , DONG, Hanqing , SMITH, Alun , TARDIBONO, Lawrence , ZHANG, Tao
IPC分类号： C07D409/12 , C07D409/14 , A61K31/4709 , A61P35/00
CPC分类号： C07D409/14 , C07D409/12
摘要： Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A, Q, Y, R 5 , m and J are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, gastrointestinal stromal tumors (GIST), germ cell tumors, small cell lung carcinoma (SCLC), sinonasal natural killer/T-cell lymphoma, testicular cancer (seminoma), thyroid carcinoma, malignant melanoma, ovarian carcinoma, adenoid crystic carcinoma, acute meyelogenous leukemia (AML), breast carcinoma, pediatric T-cell acute lymphoblastic leukemia, neuroblastoma, mast cell leukemia, angiosarcoma, anaplastic large cell lymphoma, endometrial carcubinam abd oristate carcinoma.
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐或N-氧化物，其中A，Q，Y，R

9. 发明申请

WO2005021544A3 N3-SUBSTITUTED IMIDAZOPYRIDINE-DERIVATIVES AS C-KIT INHIBITORS 审中-公开
公开(公告)号：WO2005021544A3
公开(公告)日：2005-03-10
申请号：PCT/US2004/026483
申请日：2004-08-16
申请人： OSI PHARMACEUTICALS, INC. , CASTELHANO, Arlindo, L. , CREW, Andrew, Phillip , DONG, Han-Qing , LAUFER, Radoslaw , LI, An-Hu , QUI, Li , SAMBROOK SMITH, Colin, Peter , ZHANG, Tao
发明人： CASTELHANO, Arlindo, L. , CREW, Andrew, Phillip , DONG, Han-Qing , LAUFER, Radoslaw , LI, An-Hu , QUI, Li , SAMBROOK SMITH, Colin, Peter , ZHANG, Tao
IPC分类号： C07D471/04
摘要： Compounds represented by Formula (I): (I) or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.

10. 发明申请

WO2003053944A1 PANCREATIC LIPASE INHIBITOR COMPOUNDS, THEIR SYNTHESIS AND USE 审中-公开
标题翻译：胰蛋白酶抑制剂化合物，它们的合成和用途
公开(公告)号：WO2003053944A1
公开(公告)日：2003-07-03
申请号：PCT/US2002/041272
申请日：2002-12-20
申请人： OSI PHARMACEUTICALS, INC. , WITTER, David , CASTELHANO, Arlindo, L.
发明人： WITTER, David , CASTELHANO, Arlindo, L.
IPC分类号： C07D265/12
CPC分类号： C07D513/04 , A61K31/5365 , A61K31/542 , C07D333/38 , C07D409/12 , C07D498/02 , C07D513/02
摘要： The subject invention features compounds having the structure:, wherein X is O, S, CH 2 or NR 5 ; Y is O or S; R 1 is H, substituted or unsubstituted C 1 C 15 alkyl, C 1 -C 8 alkylaryl, -C(O)OR 4 , -C(O)NR 4 R 5 , -CR 6 R 6' OR 4 ,-CR 6 R 6' OC(O)R4, - CR 6 R 6' OC(O)NHR 7 , -C(O)NR 1o R 11 , -C(O)NR 8 R 9 NR 8 R 9 , -N(R 5 )C(O)NHR 5 , or CH 2 R 4 ; R 2 is a substituted or unsubstituted, straight chain C 1 -C 30 alkyl or branched C 3 C 30 alkyl, aryl, alkylaryl, arylalkyl, heteroarylalkyl or cycloalkyl; R 3 is H or substituted or unsubstituted C 1 -C 6 alkyl or C 3 -C 10 cycloalkyl; R 4 is H or a substituted or unsubstituted, straight chain or branched, C 6 -C 30 alkyl, aryl, -CH 2 -aryl, aryl -C 1 -C 15 alkyl, heteroaryl-C 1 -C 15 alkyl or C 3 -C 10 cycloalkyl; R 5 is H or a substituted or unsubstituted, straight chain or branched, C 6 -C 30 alkyl, aryl C 1 -C 30 alkyl, heteroarylalkyl or cycloalkyl; R 6 and R 6' are each independently H, substituted or unsubstituted C 1 -C 6 alkyl, dialkyl or C 3 -C 10 cycloalkyl or together form a 3-7 membered ring system; R 7 is H or substituted or unsubstituted C 1 -C 12 alkyl or C 3 -C 10 cycloalkyl; R 8 and R 9 are each independently H, substituted or unsubstituted C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 alkylaryl, or NR 8 R 9 together form a substituted piperazine or piperidine ring or a dihydro-1H-isoquinoline ring system, or a specific enantiomer thereof, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating diabetes or obesity by administering a therapeutically effective amount of the compounds of the invention.
摘要翻译：本发明的特征在于具有以下结构的化合物：其中X是O，S，CH 2或NR b 5; Y为O或S; R 1是H，取代或未取代的C 1 -C 15烷基，C 1至C 8 -C 8烷基烷基芳基，-C（O）OR 4b，-C（O）NR b R 4，R 34，-CR sb， 6 OR 4 ， - CR 6 ，-C（O）NR a R b，C（O）NR 7 R 8， -C（O）NR 8，R 9，R 9，R 8，R 9，R 9，，-N（R 15）C（O）NHR 5或-SCH 2 R b R 4; R 2是取代或未取代的直链C 1 -C 30烷基或支链C 3 -C 30烷基或支链C 3〜烷基，芳基，烷基芳基，芳基烷基，杂芳基烷基或环烷基; R 3是H或取代或未取代的C 1 -C 6烷基或C 3 -C 3 -C 4烷基。 10环烷基; R 4是H或取代或未取代的直链或支链的C 6 -C 15烷基，芳基，-CH 3 b，芳基-C 1 -C 15烷基，杂芳基-C 1 -C 15烷基，芳基-C 1 -C 15烷基，杂芳基-C 1 -C 15烷基， sb>烷基或C 3 -C 30 -C 14环烷基; R 5是H或取代或未取代的直链或支链C 6 -C 15烷基，芳基C 1〜烷基，杂芳基烷基或环烷基; R 6和R 6分别独立地为H，取代或未取代的C 1 -C 6烷基，二烷基或C 3 -C 30烷基环烷基或一起形成3-7元环系; R 7是H或取代或未取代的C 1 -C 12烷基或C 3 -C 3 - 烷基。 10环烷基; R 8和R 9各自独立地为H，取代或未取代的C 1 -C 6烷基，C 6 - 烷基，C 1 -C 6烷基芳基或NR b 8烷基，一起形成取代的哌嗪或哌啶环或二氢-1H-异喹啉环体系或其特定的对映体或其互变异构体或其药学上可接受的盐和糖尿病治疗方法或肥胖，通过施用治疗有效量的本发明化合物。

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