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1. 发明授权

US07943635B2 Benzylimidazolyl substituted 2-quinoline and quinazoline derivatives for use as farnesyl transferase inhibitors 有权
标题翻译：苄基咪唑基取代的2-喹啉和喹唑啉衍生物，用作法呢基转移酶抑制剂
公开(公告)号：US07943635B2
公开(公告)日：2011-05-17
申请号：US11758346
申请日：2007-06-05
申请人： Patrick René Angibaud , Marc Gaston Venet , Christophe Meyer , Henry Joseph Breslin
发明人： Patrick René Angibaud , Marc Gaston Venet , Christophe Meyer , Henry Joseph Breslin
IPC分类号： A61K31/44 , C07D471/16 , C07D487/16
CPC分类号： C07D401/06 , C07D401/14 , C07D471/04
摘要： This invention comprises the novel compounds of formula (I) wherein r, t, Y1, Y2, R1, R2, R3, R5, R6 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中r，t，Y1，Y2，R 1，R 2，R 3，R 5，R 6和R 7具有定义的含义，具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

2. 发明申请

US20110224255A1 TRIPEPTIDYL PEPTIDASE INHIBITORS 有权
标题翻译： TRIPEPTIDYL肽抑制剂
公开(公告)号：US20110224255A1
公开(公告)日：2011-09-15
申请号：US13111010
申请日：2011-05-19
申请人： Henry Joseph Breslin , Hans Louis Jos De Winter , Michael Joseph Kukla
发明人： Henry Joseph Breslin , Hans Louis Jos De Winter , Michael Joseph Kukla
IPC分类号： A61K31/4709 , C07D401/04 , C07D233/54 , C07D271/08 , A61K31/4178 , A61K31/422 , A61P25/00
CPC分类号： C07D401/04 , C07D403/04 , C07D403/12 , C07D413/04 , C07D417/04
摘要： The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds. wherein n is an integer 0 or 1; X represents O; S; or —(CR4R5)m— wherein m is an integer 1 or 2; R4 and R5 are each independently from each other hydrogen or C1-4alkyl; R1 is C1-6alkylcarbonyl optionally substituted with hydroxy; C1-6alkyloxycarbonyl; aminoC1-6alkylcarbonyl wherein the C1-6alkyl group is optionally substituted with C3-6cycloalkyl; mono- and di(C1-4alkyl)aminoC1-6alkylcarbonyl; aminocarbonyl substituted with aryl; C1-6alkylcarbonyloxyC1-6alkylcarbonyl; C1-6alkyloxycarbonylaminoC1-6alkylcarbonyl wherein the amino group is optionally substituted with C1-4alkyl; an amino acid; C1-6alkyl substituted with amino; or arylcarbonyl; R2 is an optionally substituted 5-membered heterocycle, or R2 is optionally substituted benzimidazole; R3 is a bivalent radical —CH2CH2— optionally substituted with halo or phenylmethyl; or R3 is a bivalent radical of formula
摘要翻译：本发明涉及新型的式（I）化合物，其是负责灭活内源性神经肽如缩胆囊肿（CCKs）的膜三肽基肽酶的抑制剂。本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及用作所述化合物的药物。其中n为整数0或1; X表示O; S; 或 - （CR 4 R 5）m - ，其中m是整数1或2; R 4和R 5各自独立地为氢或C 1-4烷基; R1是任选被羟基取代的C 1-6烷基羰基; C 1-6烷氧基羰基; 氨基C 1-6烷基羰基，其中C 1-6烷基任选被C 3-6环烷基取代; 单和二（C 1-4烷基）氨基C 1-6烷基羰基; 被芳基取代的氨基羰基; C 1-6烷基羰氧基C 1-6烷基羰基; C 1-6烷氧基羰基氨基C 1-6烷基羰基，其中氨基任选被C 1-4烷基取代; 氨基酸; 被氨基取代的C1-6烷基; 或芳基羰基; R2是任选取代的5元杂环，或R 2是任选取代的苯并咪唑; R3是任选被卤素或苯基甲基取代的二价基团-CH 2 CH 2; 或R 3是式的二价基团

3. 发明申请

US20080255191A1 BENZYLIMIDAZOLYL SUBSTITUTED 2-QUINOLINE AND QUINAZOLINE DERIVATIVES FOR USE AS FARNESYL TRANSFERASE INHIBITORS 有权
标题翻译：苄基咪唑取代的2-喹啉和喹唑啉衍生物，用作呋喃葡萄糖转移酶抑制剂
公开(公告)号：US20080255191A1
公开(公告)日：2008-10-16
申请号：US11758346
申请日：2007-06-05
申请人： Patrick Rene Angibaud , Marc Gaston Venet , Christophe Meyer , Henry Joseph Breslin
发明人： Patrick Rene Angibaud , Marc Gaston Venet , Christophe Meyer , Henry Joseph Breslin
IPC分类号： A61K31/4709 , C07D403/08 , A61K31/4155 , C07D401/08
CPC分类号： C07D401/06 , C07D401/14 , C07D471/04
摘要： This invention comprises the novel compounds of formula (I) wherein r, t, Y1, Y2, R1, R2, R3, R5, R6 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中r，t，Y 1，Y 2，R 1，R 2， 2，R 3，R 5，R 6和R 7具有定义的含义，具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

4. 发明申请

US20120165519A1 Fused Bicyclic Derivatives of 2,4-Diaminopyrimidine as ALK and c-MET Inhibitors 有权
标题翻译： 2,4-二氨基嘧啶的双酚衍生物作为ALK和c-MET抑制剂
公开(公告)号：US20120165519A1
公开(公告)日：2012-06-28
申请号：US13413322
申请日：2012-03-06
申请人： Gulzar Ahmed , Henry Joseph Breslin , Jason Burke , Matthew A. Curry , James L. Diebold , Bruce Dorsey , Benjamin J. Dugan , Daming Feng , Diane E. Gingrich , Tao Guo , Keith S. Learn , Joseph G. Lisko , Rong-qiang Liu , Eugen Mesaros , Karen Milkiewicz , Gregory R. Ott , Jay P. Theroff , Tho V. Thieu , Rabindranath Tripathy , Theodore L. Underiner , Gregory J. Wells , Craig A. Zificsak
发明人： Gulzar Ahmed , Henry Joseph Breslin , Jason Burke , Matthew A. Curry , James L. Diebold , Bruce Dorsey , Benjamin J. Dugan , Daming Feng , Diane E. Gingrich , Tao Guo , Keith S. Learn , Joseph G. Lisko , Rong-qiang Liu , Eugen Mesaros , Karen Milkiewicz , Gregory R. Ott , Jay P. Theroff , Tho V. Thieu , Rabindranath Tripathy , Theodore L. Underiner , Gregory J. Wells , Craig A. Zificsak
IPC分类号： C07D403/14 , C07D498/04 , C07D413/12 , C07D409/14 , C07D405/12 , C07D417/14 , C07D401/14 , C07D405/14 , C07D403/12 , C07D413/14
CPC分类号： C07D239/48 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.
摘要翻译：本发明提供式I或II化合物或其药学上可接受的盐形式，其中R1，R2，R3，R4，R5，A1，A2，A3，A4和A5如本文所定义。式I或II的化合物具有ALK和/或c-Met抑制活性，并且可用于治疗增殖性疾病。

5. 发明申请

US20090221555A1 FUSED BICYCLIC DERIVATIVES OF 2,4-DIAMINOPYRIMIDINE AS ALK AND c-MET INHIBITORS 有权
标题翻译： 2,4-二氨基嘧啶作为ALK和c-MET抑制剂的熔融双相衍生物
公开(公告)号：US20090221555A1
公开(公告)日：2009-09-03
申请号：US12162851
申请日：2007-10-23
申请人： Gulzar Ahmed , Adolph Bohnstedt , Henry Joseph Breslin , Jason Burke , Matthew A. Curry , James L. Diebold , Bruce Dorsey , Benjamin J. Dugan , Daming Feng , Diane E. Gingrich , Tao Guo , Koc-Kan Ho , Keith S. Learn , Joseph G. Lisko , Rong-qiang Liu , Eugen Mesaros , Karen Milkiewicz , Gregory R. Ott , Jonathan Parrish , Jay P. Theroff , Tho V. Thieu , Rabindranath Tripathy , Theodore L. Underiner , Jason C. Wagner , Linda Weinberg , Gregory J. Wells , Ming You , Craig A. Zificsak
发明人： Gulzar Ahmed , Adolph Bohnstedt , Henry Joseph Breslin , Jason Burke , Matthew A. Curry , James L. Diebold , Bruce Dorsey , Benjamin J. Dugan , Daming Feng , Diane E. Gingrich , Tao Guo , Koc-Kan Ho , Keith S. Learn , Joseph G. Lisko , Rong-qiang Liu , Eugen Mesaros , Karen Milkiewicz , Gregory R. Ott , Jonathan Parrish , Jay P. Theroff , Tho V. Thieu , Rabindranath Tripathy , Theodore L. Underiner , Jason C. Wagner , Linda Weinberg , Gregory J. Wells , Ming You , Craig A. Zificsak
IPC分类号： A61K31/55 , C07D239/02 , A61K31/505 , C07D403/00 , C07D413/14 , A61K31/5377 , C07D413/00 , C07D403/14
CPC分类号： C07D239/48 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.
摘要翻译：本发明提供式I或II化合物或其药学上可接受的盐形式，其中R1，R2，R3，R4，R5，A1，A2，A3，A4和A5如本文所定义。式I或II的化合物具有ALK和/或c-Met抑制活性，并且可用于治疗增殖性疾病。

6. 发明授权

US08247432B2 Tripeptidyl peptidase inhibitors 有权
标题翻译：三肽基肽酶抑制剂
公开(公告)号：US08247432B2
公开(公告)日：2012-08-21
申请号：US13111010
申请日：2011-05-19
申请人： Henry Joseph Breslin , Hans Louis Jos De Winter , Michael Joseph Kukla
发明人： Henry Joseph Breslin , Hans Louis Jos De Winter , Michael Joseph Kukla
IPC分类号： A61K31/4709 , A61K31/4178 , A61K31/422 , A61P25/00 , C07D401/04 , C07D233/54 , C07D271/08
CPC分类号： C07D401/04 , C07D403/04 , C07D403/12 , C07D413/04 , C07D417/04
摘要： The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs).
摘要翻译：本发明涉及新型的式（I）化合物，其是负责灭活内源性神经肽如缩胆囊肿（CCKs）的膜三肽基肽酶的抑制剂。

7. 发明授权

US08148391B2 Fused bicyclic derivatives of 2,4-diaminopyrimidine as ALK and c-Met inhibitors 有权
标题翻译： 2,4-二氨基嘧啶作为ALK和c-Met抑制剂的稠合双环衍生物
公开(公告)号：US08148391B2
公开(公告)日：2012-04-03
申请号：US12162851
申请日：2007-10-23
申请人： Gulzar Ahmed , Henry Joseph Breslin , Jason Burke , Matthew A. Curry , James L. Diebold , Bruce Dorsey , Benjamin J. Dugan , Daming Feng , Diane E. Gingrich , Tao Guo , Keith S. Learn , Joseph G. Lisko , Rong-Qiang Liu , Eugen Florin Mesaros , Karen Milkiewicz , Gregory R. Ott , Jay P. Theroff , Tho V. Thieu , Rabindranath Tripathy , Theodore L. Underiner , Gregory J. Wells , Craig A. Zificsak
发明人： Gulzar Ahmed , Henry Joseph Breslin , Jason Burke , Matthew A. Curry , James L. Diebold , Bruce Dorsey , Benjamin J. Dugan , Daming Feng , Diane E. Gingrich , Tao Guo , Keith S. Learn , Joseph G. Lisko , Rong-Qiang Liu , Eugen Florin Mesaros , Karen Milkiewicz , Gregory R. Ott , Jay P. Theroff , Tho V. Thieu , Rabindranath Tripathy , Theodore L. Underiner , Gregory J. Wells , Craig A. Zificsak
IPC分类号： A61K31/505 , C07D239/02
CPC分类号： C07D239/48 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.
摘要翻译：本发明提供式I或II化合物或其药学上可接受的盐形式，其中R1，R2，R3，R4，R5，A1，A2，A3，A4和A5如本文所定义。式I或II的化合物具有ALK和/或c-Met抑制活性，并且可用于治疗增殖性疾病。

8. 发明授权

US07592356B2 Triazoles as farnesyl transferase inhibitors 有权
标题翻译：三唑作为法呢基转移酶抑制剂
公开(公告)号：US07592356B2
公开(公告)日：2009-09-22
申请号：US11926858
申请日：2007-10-29
申请人： Ashis Kumar Saha , David William End , Bart Lieven Daniel De Corte , Henry Joseph Breslin , Li Liu
发明人： Ashis Kumar Saha , David William End , Bart Lieven Daniel De Corte , Henry Joseph Breslin , Li Liu
IPC分类号： A61K31/47 , C07D249/08
CPC分类号： C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12
摘要： a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(═O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; ═Z1—Z2═Z3— represents a radical of formula ═N—N═CH— (a-1), ═N—CH═N— (a-2), ═CH—N═N— (a-3); X is SO2, (CH2), wherein n is 1 to 4, C(═O), C(═S), or a direct bond; R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio; R3 is aryl, —NR5R6, a substituted or unsubstituted C1-14heterocycle, or C2-4alkenediyl substituted with a substituted or unsubstituted C1-14heterocycle or aryl; R4 is hydrogen, aryl, C3-7cycloalkyl, C1-6alkyl or C1-6alkyl substituted with C3-7cycloalkyl, hydroxycarbonyl, C1-4alkyloxycarbonyl or aryl; R5 and R6 are each independently selected from hydrogen, a substituted or unsubstituted C1-14heterocycle, aryl, C1-12alkyl and C1-12alkyl substituted with one or more substituents selected from hydroxy, aryl, aryloxy or a substituted or unsubstituted C1-14heterocycle.
摘要翻译：前药，N-氧化物，加成盐，季胺或其立体化学异构形式，其中L 1和L 2是R 1 -Y-，其中每个（R 1 -Y） - 取代基独立地彼此定义; Y是C1-4烷二基，C2-4亚烯基，C2-4炔二基，C（-O）或直接键; R1是氢，氰基，芳基或取代或未取代的C1-14杂环; -Z1-Z2-Z3-表示式-N-N-CH-（a-1），-N-CH-N-（a-2），-CH-N-N-（a-3） X是SO 2，（CH 2），其中n是1至4，C（-O），C（-S）或直接键; R 2是芳基，C 3-7环烷基，被一个或多个独立地选自羟基，芳基，芳氧基，取代或未取代的C 1-14杂环，C 3-7环烷基，羟基羰基，C 1-6烷氧基羰基，羟基C 1-6烷基，羟基C 1-6烷基，被一个或多个独立地选自羟基，芳基，芳氧基，取代或未取代的C 1-14杂环，C 3-7环烷基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷氧基羰基，C 1-6烷硫基，羟基C 1-6烷基，羟基C 1-6烷氧基，羟基C 1-6烷硫基和芳基C 1-6烷硫基; R3是芳基，-NR5R6，取代或未取代的C1-14杂环，或被取代或未取代的C1-14杂环或芳基取代的C2-4亚烯基; R4是氢，芳基，C3-7环烷基，C1-6烷基或被C3-7环烷基取代的C1-6烷基，羟基羰基，C1-4烷氧基羰基或芳基; R 5和R 6各自独立地选自氢，取代或未取代的C 1-14杂环，芳基，C 1-12烷基和被一个或多个选自羟基，芳基，芳氧基或取代或未取代的C 1-14杂环的取代基取代的C 1-12烷基。

9. 发明授权

US07241777B2 Benzylimidazolyl substituted 2-quinoline and quinazoline derivatives for use as farnesyl transferase inhibitors 有权
标题翻译：苄基咪唑基取代的2-喹啉和喹唑啉衍生物，用作法呢基转移酶抑制剂
公开(公告)号：US07241777B2
公开(公告)日：2007-07-10
申请号：US10508185
申请日：2003-03-18
申请人： Patrick René Angibaud , Marc Gaston Venet , Christophe Meyer , Henry Joseph Breslin
发明人： Patrick René Angibaud , Marc Gaston Venet , Christophe Meyer , Henry Joseph Breslin
IPC分类号： A01N43/42 , A61K31/47 , C07D215/00 , A61K31/498 , C07D43/02
CPC分类号： C07D401/06 , C07D401/14 , C07D471/04
摘要： This invention comprises the novel compounds of formula (I) wherein r, t, Y1, Y2, R1, R2, R3, R5, R6and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中r，t，Y 1，Y 2，R 1，R 2， 2，R 3，R 5，R 6和R 7具有定义的含义，具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

10. 发明授权

US07125891B2 Tripeptidyl peptidase inhibitors 有权
公开(公告)号：US07125891B2
公开(公告)日：2006-10-24
申请号：US10415623
申请日：2001-10-24
申请人： Henry Joseph Breslin , Hans Louis Jos De Winter , Michael Joseph Kukla
发明人： Henry Joseph Breslin , Hans Louis Jos De Winter , Michael Joseph Kukla
IPC分类号： A61K31/4725 , C07D217/08 , C07D217/22
CPC分类号： C07D401/04 , C07D403/04 , C07D403/12 , C07D413/04 , C07D417/04
摘要： The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds. wherein n is an integer 0 or 1; X represents O; S; or —(CR4R5)m— wherein m is an integer 1 or 2; R4 and R5 are each independently from each other hydrogen or C1-4alkyl; R1 is C1-6alkylcarbonyl optionally substituted with hydroxy; C1-6alkyloxycarbonyl; aminoC1-6alkylcarbonyl wherein the C1-6alkyl group is optionally substituted with C3-6cycloalkyl; mono- and di(C1-4alkyl)aminoC1-6alkylcarbonyl; aminocarbonyl substituted with aryl; C1-6alkylcarbonyloxyC1-6alkylcarbonyl; C1-6alkyloxycarbonylaminoC1-6alkylcarbonyl wherein the amino group is optionally substituted with C1-4alkyl; an amino acid; C1-6alkyl substituted with amino; or arylcarbonyl; R2 is an optionally substituted 5-membered heterocycle, or R2 is optionally substituted benzimidazole; R3 is a bivalent radical —CH2CH2— optionally substituted with halo or phenylmethyl; or R3 is a bivalent radical of formula

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