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81. 发明授权

US07498354B2 Pyrrolo[2,3-D]imidazoles for the treatment of hyperproliferative disorders 失效
标题翻译：吡咯并[2,3-D]咪唑用于治疗过度增殖性疾病
公开(公告)号：US07498354B2
公开(公告)日：2009-03-03
申请号：US11397031
申请日：2006-03-30
申请人： Andrew Philip Crew , Bijoy Panicker , Han-Qing Dong
发明人： Andrew Philip Crew , Bijoy Panicker , Han-Qing Dong
IPC分类号： A61K31/4162 , C07D235/00
CPC分类号： C07D487/04
摘要： or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of tumors and cancers.
摘要翻译：或其药学上可接受的盐或N-氧化物可用于治疗肿瘤和癌症。

82. 发明授权

US07485658B2 N-substituted pyrazolyl-amidyl-benzimidazolyl c-Kit inhibitors 失效
标题翻译： N-取代的吡唑基 - 氨基 - 苯并咪唑基c-Kit抑制剂
公开(公告)号：US07485658B2
公开(公告)日：2009-02-03
申请号：US10919973
申请日：2004-08-16
申请人： Joshua Bolger , Arlindo L. Castelhano , Andrew Phillip Crew , Radoslaw Laufer , An-Hu Li , Colin Peter Sambrook Smith , Yingchuan Sun
发明人： Joshua Bolger , Arlindo L. Castelhano , Andrew Phillip Crew , Radoslaw Laufer , An-Hu Li , Colin Peter Sambrook Smith , Yingchuan Sun
IPC分类号： A61K31/4184 , C07D403/02
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。

83. 发明授权

US07465726B2 Substituted pyrrolo[2.3-B]pyridines 失效
标题翻译：取代的吡咯并[2,3-B]吡啶
公开(公告)号：US07465726B2
公开(公告)日：2008-12-16
申请号：US11194158
申请日：2005-08-01
申请人： Saleh Ahmed , Oscar Barba , Jason Bloxham , Graham Dawson , William Gattrell , John Kitchin , Neil Anthony Pegg , Imaad Saba , Shazia Sadiq , Colin Peter Sambrook Smith , Don Smyth , Amo G. Steinig , Robin Wilkes , Bijoy Panicker , Paula Tavares , Matthew Cox , An-Hu Li , Hanqing Dong , Lifu Ma , Kenneth (‘Ken’) Foreman , Qinghua (‘Felix’) Weng , Kathryn Stolz
发明人： Saleh Ahmed , Oscar Barba , Jason Bloxham , Graham Dawson , William Gattrell , John Kitchin , Neil Anthony Pegg , Imaad Saba , Shazia Sadiq , Colin Peter Sambrook Smith , Don Smyth , Amo G. Steinig , Robin Wilkes , Bijoy Panicker , Paula Tavares , Matthew Cox , An-Hu Li , Hanqing Dong , Lifu Ma , Kenneth (‘Ken’) Foreman , Qinghua (‘Felix’) Weng , Kathryn Stolz
IPC分类号： A61K31/437 , A61K31/496 , A61K31/5355 , A61K31/541 , A61K31/5513 , A61K31/551 , C07D471/04 , C07D223/04 , C07D243/08 , C07D241/04 , C07D413/10 , C07D413/06 , C07D413/08 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/14 , A61K31/04 , A61K31/519 , C07D487/04
CPC分类号： C07D471/02 , C07D487/02 , C07D487/04
摘要： Compounds represented by Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least two of the Abl, Aurora-A, Blk, c-Raf, cSRC, Src, PRK2, FGFR3, Flt3, Lck, Mek1, PDK-1, GSK3β, EGFR, p70S6K, BMX, SGK, CaMKII, Tie-2, IGF-1R, Ron, Ret, and KDR kinases in animals, including humans, for the treatment and/or prevention of various diseases and conditions such as cancer.
摘要翻译：由式（I）表示的化合物或其立体异构体或其药学上可接受的盐是Abl，Aurora-A，Blk，c-Raf，cSRC，Src，PRK2，FGFR3，Flt3，Lck，Mek1，PDK中的至少两种的抑制剂 -1，GSK3beta，EGFR，p70S6K，BMX，SGK，CaMKII，Tie-2，IGF-1R，Ron，Ret和KDR激酶，用于治疗和/或预防各种疾病和病症，癌症。

84. 发明申请

US20080300249A1 Isothiazole Derivatives Useful as Anticancer Agents 有权
标题翻译：异噻唑衍生物可用作抗癌剂
公开(公告)号：US20080300249A1
公开(公告)日：2008-12-04
申请号：US12181803
申请日：2008-07-29
申请人： Eric R. Larson , Mark C. Noe , Thomas G. Gant
发明人： Eric R. Larson , Mark C. Noe , Thomas G. Gant
IPC分类号： C07D275/03 , A61K31/425 , A61K31/497 , C07D411/00 , C07D417/02 , A61K31/454 , A61K31/5377 , A61P35/00
CPC分类号： C07D275/03 , C07C33/46 , C07C327/58 , C07D231/12 , C07D233/56 , C07D249/08 , C07D417/12 , C07D487/08
摘要： The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X1, R1, R2 and R3 are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods treating hyperproliferative disorders in mammals by administering the above compounds.
摘要翻译：本发明涉及式1的化合物及其药学上可接受的盐，前药和溶剂化物，其中X1，R1，R2和R3如本文所定义。本发明还涉及含有上述化合物的药物组合物和通过施用上述化合物治疗哺乳动物过度增殖性疾病的方法。

85. 发明授权

US07442709B2 N3-substituted imidazopyridine c-Kit inhibitors 失效
标题翻译： N 3取代的咪唑并吡啶c-Kit抑制剂
公开(公告)号：US07442709B2
公开(公告)日：2008-10-28
申请号：US10921418
申请日：2004-08-16
申请人： Arlindo L. Castelhano , Andrew Phillip Crew , Han-Qing Dong , Radoslaw Laufer , An-Hu Li , Li Qiu , Colin Peter Sambrook Smith , Tao Zhang
发明人： Arlindo L. Castelhano , Andrew Phillip Crew , Han-Qing Dong , Radoslaw Laufer , An-Hu Li , Li Qiu , Colin Peter Sambrook Smith , Tao Zhang
IPC分类号： A61K31/44 , C07D471/02 , C07D491/02
CPC分类号： C07D471/04
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。

86. 发明申请

US20080261943A1 PYRROLOPYRIMIDINE A2B SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE 失效
公开(公告)号：US20080261943A1
公开(公告)日：2008-10-23
申请号：US10536119
申请日：2007-06-19
申请人： Arlindo Castelhano , Bryan McKibben , Arno Steinig
发明人： Arlindo Castelhano , Bryan McKibben , Arno Steinig
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： The subject invention provides compounds having the structure: wherein, R1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NRaRb, —NRaRb, —NRaC(═O)NRaRb, —NRaC(═O)ORa, —OC(═O)NRaRb, or —NH C(═O) Ra; R2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NRaRb, —NRaRb, —NRaC(═O)NRaRb, —NRaC(═O)ORa, —OC(═O)NRaRb, or —NHC(═O)Ra, or R1, R2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH2)2OH or —CH2C(═O)OH; R3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C1-C15)alkyl, (C1-C15)alkoxy, or —NRaRb; R4 is hydrogen or substituted or unsubstituted (C1-C15)alkyl; R5 is —(CH2)mOR6, —CHNOR7, —C(═O)NR8R9, —(CH2)mC(═O)OR10, —(CH2)kC(═O)NR11R12; wherein R6 is a substituted or unsubstituted (C1-C30)alkyl, (C3-C10)cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring; R7 is hydrogen, or a substituted or unsubstituted (C1-C30)alkyl, (C1-C30)alkylaryl; R8 and R9 are each independently hydrogen, or a substituted or unsubstituted (C1-C30)alkyl, (C1-C30)alkylaryl, (C1-C30)alkylamino, (C1-C30)alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R8, N, and R9 together form a substituted or unsubstituted 4-8 membered heterocyclic ring; R10 is hydrogen or a substituted or unsubstituted (C1-C30)alkyl, (C3-C10)cycloalkyl, or an aryl, heteroaryl or heterocyclic ring; R11, N and R12 together form a 4-8 membered heterocyclic ring; Ra and Rb 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 A2b 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.

87. 发明授权

US07405218B2 Isothiazole derivatives useful as anticancer agents 有权
标题翻译：异噻唑衍生物可用作抗癌剂
公开(公告)号：US07405218B2
公开(公告)日：2008-07-29
申请号：US10357093
申请日：2003-02-03
申请人： Eric R. Larson , Mark C. Noe , Thomas G. Gant
发明人： Eric R. Larson , Mark C. Noe , Thomas G. Gant
IPC分类号： A61K31/426 , A61K31/427 , C07D275/03
CPC分类号： C07D275/03 , C07C33/46 , C07C327/58 , C07D231/12 , C07D233/56 , C07D249/08 , C07D417/12 , C07D487/08
摘要： The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X1, R1, R2 and R3 are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods treating hyperproliferative disorders in mammals by administering the above compounds.
摘要翻译：本发明涉及式1的化合物及其药学上可接受的盐，前药和溶剂合物，其中X 1，R 1，R 2， >和R 3'如本文所定义。本发明还涉及含有上述化合物的药物组合物和通过施用上述化合物治疗哺乳动物过度增殖性疾病的方法。

88. 发明申请

US20080070936A1 Compounds specific to adenosine A1 receptors and uses thereof 审中-公开
标题翻译：对腺苷A1受体特异的化合物及其用途
公开(公告)号：US20080070936A1
公开(公告)日：2008-03-20
申请号：US11903147
申请日：2007-09-20
申请人： Arlindo Castelhano , Bryan McKibben , David Witter
发明人： Arlindo Castelhano , Bryan McKibben , David Witter
IPC分类号： A61K31/519 , A61P11/00 , A61P25/00 , A61P9/00
CPC分类号： C07D487/04 , A61K31/519
摘要： This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.
摘要翻译：本发明涉及特异性抑制腺苷A 1受体的化合物以及这些化合物用于治疗受试者中Aβ1腺苷受体相关疾病的用途。

89. 发明授权

US07160890B2 Compounds specific to adenosine A3 receptor and uses thereof 失效
标题翻译：对腺苷A3受体特异性的化合物及其用途
公开(公告)号：US07160890B2
公开(公告)日：2007-01-09
申请号：US09728616
申请日：2000-12-01
申请人： Arlindo L. Castelhano , Bryan McKibben , David J. Witter
发明人： Arlindo L. Castelhano , Bryan McKibben , David J. Witter
IPC分类号： A01N43/90 , A61K31/52 , C07D239/00 , C07D487/00
CPC分类号： C07D487/04
摘要： This invention pertains to compounds which specifically inhibit the adenosine A3 receptor and the use of these compounds to treat a disease associated with A3 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A 3受体的化合物和这些化合物用于治疗受试者中与Aβ3腺苷受体相关的疾病的用途，包括给予该受试者治疗有效量的化合物。

90. 发明授权

US07064122B2 Pancreatic lipase inhibitor compounds, their synthesis and use 失效
公开(公告)号：US07064122B2
公开(公告)日：2006-06-20
申请号：US10326302
申请日：2002-12-20
申请人： David Witter , Arlindo Castelhano
发明人： David Witter , Arlindo Castelhano
IPC分类号： C07D498/04 , A61K31/5365 , A61K1/18 , A61K3/10
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, CH2 or NR5; Y is O or S; R1 is H, substituted or unsubstituted C1-C15 alkyl, C1-C8 alkylaryl, —C(O)OR4, —C(O)NR4R5, —CR6R6′OR4, —CR6R6′OC(O)R4, —CR6R6′OC(O)NHR7, —C(O)NR10R11, —C(O)NR8R9NR8R9, —N(R5)C(O)NHR5, or CH2R4; R2 is a substituted or unsubstituted, straight chain C1—C30 alkyl or branched C3-C30 alkyl, aryl, alkylaryl, arylalkyl, heteroarylalkyl or cycloalkyl; R3 is H or substituted or unsubstituted C1-C6 alkyl or C3-C10 cycloalkyl; R4 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl, —CH2-aryl, aryl —C1-C15 alkyl, heteroaryl-C1-C15alkyl or C3-C10 cycloalkyl; R5 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl C1-C30alkyl, heteroarylalkyl or cycloalkyl; R6 and R6′ are each independently H, substituted or unsubstituted C1-C6 alkyl, dialkyl or C3-C10 cycloalkyl or together form a 3-7 membered ring system; R7 is H or substituted or unsubstituted C1-C12 alkyl or C3-C10 cycloalkyl; R8 and R9 are each independently H, substituted or unsubstituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylaryl, or NR8R9 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.

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