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1. 发明申请

WO2010081859A1 6-PHENYL-LH-IMIDAZO [4, 5-C] PYRIDINE-4-CARBONITRILE DERIVATIVES AS CATHEPSIN S AND/OR CATHEPSIN K INHIBITORS 审中-公开
标题翻译： 6-苯基-LH-咪唑并[4,5-C]吡啶-4-羰基酮衍生物，为CATHEPSIN S和/或CATHEPSIN K抑制剂
公开(公告)号：WO2010081859A1
公开(公告)日：2010-07-22
申请号：PCT/EP2010/050418
申请日：2010-01-14
申请人： N.V. ORGANON , CAI, Jiaqiang , BENNETT, David, Jonathan , ROBINSON, John, Stephen , JONES, Philip, Stephen
发明人： CAI, Jiaqiang , BENNETT, David, Jonathan , ROBINSON, John, Stephen , JONES, Philip, Stephen
IPC分类号： C07D471/04 , A61K31/437 , A61P19/10 , A61P25/02 , A61P29/00 , A61P17/06
CPC分类号： C07D471/04
摘要： The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula (I) to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.
摘要翻译：本发明涉及具有通式（I）的6-苯基-1H-咪唑并[4,5-c]吡啶-4-甲腈衍生物，其中药物组合物包含它们，以及这些衍生物用于制备的药物组合物用于治疗组织蛋白酶S相关疾病如动脉粥样硬化，肥胖，炎症和免疫疾病如类风湿性关节炎，牛皮癣，癌症和慢性疼痛如神经性疼痛的药物。

2. 发明申请

WO2009010491A1 6-PHENYL-1H-IMIDAZO[4,5-C]PYRIDINE-4-CARBONITRILE DERIVATIVES AS CATHEPSIN INHIBITORS 审中-公开
标题翻译： 6-苯基-1H-咪唑并[4,5-C]吡啶-4-羰基酮衍生物作为CATHEPSIN抑制剂
公开(公告)号：WO2009010491A1
公开(公告)日：2009-01-22
申请号：PCT/EP2008/059172
申请日：2008-07-14
申请人： N.V. ORGANON , CAI, Jiaqiang , RANKOVIC, Zoran , JONES, Philip, Stephen , BENNETT, David, Jonathan , FRADERA, Xavier
发明人： CAI, Jiaqiang , RANKOVIC, Zoran , JONES, Philip, Stephen , BENNETT, David, Jonathan , FRADERA, Xavier
IPC分类号： C07D471/04 , A61K31/437 , A61P19/00 , A61P17/00 , A61P29/00
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula (I), to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such asatherosclerosis,obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer,and chronic pain, such as neuropathic pain.
摘要翻译：本发明涉及具有通式（I）的6-苯基-1H-咪唑并[4,5-c]吡啶-4-甲腈衍生物，涉及包含其的药物组合物以及这些衍生物用于制备用于治疗组织蛋白酶S相关疾病如动脉粥样硬化，肥胖，炎症和免疫疾病如类风湿性关节炎，牛皮癣，癌症和慢性疼痛如神经性疼痛的药物。

3. 发明申请

WO2011086125A1 1H-[1,2,3]TRIAZOLO[4,5-c]PYRIDINE-4-CARBONITRILE DERIVATIVES 审中-公开
标题翻译： 1H- [1,2,3]三唑[4,5-c]吡啶-4-羰基衍生物
公开(公告)号：WO2011086125A1
公开(公告)日：2011-07-21
申请号：PCT/EP2011/050393
申请日：2011-01-13
申请人： N.V. ORGANON , CAI, Jiaqiang , BENNETT, David, Jonathan , JONES, Philip, Stephen
发明人： CAI, Jiaqiang , BENNETT, David, Jonathan , JONES, Philip, Stephen
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00
CPC分类号： C07D471/04
摘要： The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R 1 is H or (C 1-3 )alkyl; R 2 is halogen or (C 1-4 )alkyl, optionally substituted with one or more halogens; n is 1 -3; X is O or CH 2 ; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the S n ....S 2 substites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.
摘要翻译：本发明涉及式（I）的1H- [1,2,3]三唑并[4,5-c]吡啶-4-腈衍生的组织蛋白酶S抑制剂，其中R 1是H或（C 1-3）烷基; R2是卤素或任选被一个或多个卤素取代的（C 1-4）烷基; n为1-3; X是O或CH2; U，V和W是CH; 或U，V和W之一为N; Y是能够与组织蛋白酶S的活性位点的Sn ... S2方位相互作用的基团; 或其药学上可接受的盐用于包含其的药物组合物以及这些衍生物用于制备用于治疗组织蛋白酶S相关疾病如动脉粥样硬化，肥胖症，炎症和免疫疾病如类风湿病的药物中的用途关节炎，牛皮癣，癌症和慢性疼痛，如神经性疼痛。

4. 发明申请

WO2007080191A1 6-PHENYL-1H-IMIDAZO[4, 5-C]PYRIDINE-4-CARBONITRILE DERIVATIVES AS CATHEPSIN K AND S INHIBITORS 审中-公开
标题翻译： 6-苯基-1H-咪唑并[4,5-C]吡啶-4-羰基酮衍生物作为CATHEPSIN K和S抑制剂
公开(公告)号：WO2007080191A1
公开(公告)日：2007-07-19
申请号：PCT/EP2007/050356
申请日：2007-01-15
申请人： N.V. ORGANON , CAI, Jiaqiang , RANKOVIC, Zoran , JONES, Philip, Stephen , BENNETT, David, Jonathan , CUMMING, Iain , GILLESPIE, Jonathan
发明人： CAI, Jiaqiang , RANKOVIC, Zoran , JONES, Philip, Stephen , BENNETT, David, Jonathan , CUMMING, Iain , GILLESPIE, Jonathan
IPC分类号： C07D471/04 , A61K31/437 , A61P19/00 , C07D519/00 , C07F7/10
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula (I), to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S and/or cathepsin K related diseases such as osteoporosis, atherosclerosis, inflammation and immune disorders, such as rheumatoid arthritis, and chronic pain, such as neuropathic pain.
摘要翻译：本发明涉及具有通式（I）的6-苯基-1H-咪唑并[4,5-c]吡啶-4-甲腈衍生物，涉及包含其的药物组合物以及这些衍生物用于制备用于治疗组织蛋白酶S和/或组织蛋白酶K相关疾病如骨质疏松症，动脉粥样硬化，炎症和免疫疾病如类风湿性关节炎和慢性疼痛如神经性疼痛的药物。

5. 发明申请

WO2007039470A1 4-PHENYL-6-SUBSTITUTED-PYRIMIDINE-2-CARBONITRILE DERIVATIVES 审中-公开
标题翻译： 4-苯基-6-取代的嘧啶-2-羰基衍生物
公开(公告)号：WO2007039470A1
公开(公告)日：2007-04-12
申请号：PCT/EP2006/066562
申请日：2006-09-21
申请人： N.V. ORGANON , RANKOVIC, Zoran , CAI, Jiaqiang
发明人： RANKOVIC, Zoran , CAI, Jiaqiang
IPC分类号： C07D239/42 , C07D239/34 , C07D239/38 , C07D239/36 , C07D403/04 , C07D401/04 , C07D403/12 , C07D401/12 , A61K31/505 , A61K31/506 , A61P19/10 , A61P9/10
CPC分类号： C07D239/34 , C07D239/36 , C07D239/38 , C07D239/42 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12
摘要： The invention relates to 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives having Formula (I) wherein R represents 1-3 optional substituents independently selected from (C 1-4 )- alkyl (optionally substituted with one or more halogens), (C 1-4 )alkyloxy (optionally substituted with one or more halogens) and halogen; X is NR 1 , O or S; R 1 is H or (C 1-4 )alkyl; Y is (C 1-4 )alkyl, benzyl or (C 2-6 )alkyl, substituted with a group selected from OH, (C 1-4 )alkyloxy, NR 2 R 3 , a 4-8 membered saturated heterocyclic ring comprising 1 or 2 heteroatoms selected from O, S and NR 4 , and a 5 or 6-membered aromatic heterocyclic group comprising 1-4 N atoms; or R 1 and Y form together with the nitrogen to which they are bonded a 5-8 membered saturated heterocyclic ring, optionally comprising a further heteroatom selected from O, S, NR 4 and NO; the ring being optionally substituted with NR 2 R 3 or with 1 to 4 (C 1-3 )alkyl groups; R 2 and R 3 are independently H or (C 1-4 )alkyl; or R 2 and R 3 form together with the nitrogen to which they are bonded a 4-8 membered saturated heterocyclic ring, optionally comprising a further heteroatom selected from O, S and NR 4 ; R 4 is H, (C 1-6 )alkyl,(C 3-6 ) cycloalkyl, (C 3-6 )cycloalkyl(C 1-4 )alkyl, (C 1-4 )alkyloxy-(C 1-4 )alkyl, benzyl, amido- (C 1-4 )alkyl, (C 1-6 )alkyloxycarbonyl(C 1-4 )alkyl or carboxy(C 1-4 )alkyl; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives for the preparation of a medicament for the treatment of cathepsin K and cathepsin S related disorders, e.g. osteoporosis, atherosclerosis, inflammation and immune disorders such as rheumatoid arthritis and chronic pain.
摘要翻译：本发明涉及具有式（I）的4-苯基-6-取代 - 嘧啶-2-甲腈衍生物，其中R表示1-3个任选的取代基，其独立地选自（C 1-4 - ） - 烷基（任选被一个或多个卤素取代），（C 1-4烷基）烷氧基（任选被一个或多个卤素取代）和卤素; X是NR 1，O或S; R 1是H或（C 1-4烷基）烷基; Y是（C 1-4 - ）烷基，苄基或被选自OH，（C 1-4）烷基的（C 1-6）烷基取代的（C 1-6 - NR 3 R 3，含有1或2个选自O，S和NR 4的杂原子的4-8元饱和杂环和含有1-4个N原子的5或6元芳族杂环基; 或R 1和Y与它们所键合的氮一起形成5-8元饱和杂环，任选地包含另外的选自O，S，NR 4的杂原子 >和NO; 该环任选地被NR 2 R 3 3或与1至4个（C 1-3 - ）烷基取代; R 2和R 3独立地是H或（C 1-4烷基）烷基; 或R 2和R 3 3与它们所连接的氮一起形成4-8元饱和杂环，任选地包含另外的选自O，S的杂原子和 NR _{4 ; R 4是H，（C 1-6）烷基，（C 3-6）环烷基，（C 3-6）（C 1-4）烷基，（C 1-4烷基）烷氧基 - （C 1-4 - ）烷基，苄基，酰氨基 - （C 1-4 - ）烷基，（C 1-6 - ）烷氧基羰基（C 1-4 - ）烷基或羧基（C _{1-4 ）烷基; 或其药学上可接受的盐，包含其的药物组合物，以及这些4-苯基-6-取代 - 嘧啶-2-甲腈衍生物在制备用于治疗组织蛋白酶K和组织蛋白酶的药物中的用途 S相关疾病，例如骨质疏松症，动脉粥样硬化，炎症和免疫疾病如类风湿性关节炎和慢性疼痛。}}

6. 发明申请

WO2016187788A1 FUSED TRICYCLIC HETEROCYCLIC COMPOUNDS USEFUL FOR TREATING HIV INFECTION 审中-公开
标题翻译：用于治疗艾滋病毒感染的FUSED TRICYCLIC HETEROCYCLIC COMPOUNDE有用
公开(公告)号：WO2016187788A1
公开(公告)日：2016-12-01
申请号：PCT/CN2015/079730
申请日：2015-05-25
申请人： MERCK SHARP & DOHME CORP. , YU, Tao , GRAHAM, Thomas H. , WADDELL, Sherman T. , MCCAULEY, John A. , STAMFORD, Andrew W. , SANDERS, John M. , HU, Lihong , CAI, Jiaqiang , ZHAO, Lianyun
发明人： YU, Tao , GRAHAM, Thomas H. , WADDELL, Sherman T. , MCCAULEY, John A. , STAMFORD, Andrew W. , SANDERS, John M. , HU, Lihong , CAI, Jiaqiang , ZHAO, Lianyun
IPC分类号： C07D487/14 , C07D471/14 , C07D491/147 , A61K31/437 , A61K31/4355 , A61P31/18
CPC分类号： C07D491/147 , A61K31/427 , A61K31/4355 , A61K31/437 , A61K31/4375 , A61K31/4402 , A61K31/505 , A61K31/513 , A61K31/52 , A61K31/635 , A61K31/675 , A61P31/18 , C07D471/14 , A61K2300/00
摘要： Fused tricyclic heterocycle derivatives of formula (I) and pharmaceutically acceptable salts thereof, compositions comprising at least one fused tricyclic heterocycle derivative, and methods of using the fused tricyclic heterocycle derivatives for treating or preventing HIV infection in a subject are provided.
摘要翻译：提供式（I）的稠合三环杂环衍生物及其药学上可接受的盐，包含至少一种稠合三环杂环衍生物的组合物，以及使用稠合三环杂环衍生物治疗或预防受试者中HIV感染的方法。

7. 发明申请

WO2016109222A1 TERTIARY ALCOHOL IMIDAZOPYRAZINE BTK INHIBITORS 审中-公开
标题翻译：仲胺醇咪唑啉BTK抑制剂
公开(公告)号：WO2016109222A1
公开(公告)日：2016-07-07
申请号：PCT/US2015/066233
申请日：2015-12-17
申请人： MERCK SHARP & DOHME CORP. , LIU, Jian , KOZLOWSKI, Joseph, A. , ANDRESEN, Brian, M , BOGA, Sobhana Babu , GAO, Xiaolei , GUIADEEN, Deodialsingh , CAI, Jiaqiang , LIU, Shilan , WANG, Dahai , WU, Hao , YANG, Chundao
发明人： LIU, Jian , KOZLOWSKI, Joseph, A. , ANDRESEN, Brian, M , BOGA, Sobhana Babu , GAO, Xiaolei , GUIADEEN, Deodialsingh , CAI, Jiaqiang , WANG, Dahai , WU, Hao , YANG, Chundao
IPC分类号： A61K31/5377 , A61K31/55 , C07D487/04 , A61K31/541
CPC分类号： C07D487/04 , A61K31/4985 , A61K45/06
摘要： The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, or pharmaceutically acceptable salts thereof, Formula I or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.
摘要翻译：本发明提供了布鲁顿的式I的酪氨酸激酶（Btk）抑制剂化合物或其药学上可接受的盐，式I或包含这些化合物的药物组合物及其在治疗中的用途。特别地，本发明涉及式I的Btk抑制剂化合物在治疗Btk介导的病症中的用途。

8. 发明申请

WO2016109221A1 BTK INHIBITORS 审中-公开
标题翻译： BTK抑制剂
公开(公告)号：WO2016109221A1
公开(公告)日：2016-07-07
申请号：PCT/US2015/066229
申请日：2015-12-17
申请人： MERCK SHARP & DOHME CORP. , LIU, Jian , KOZLOWSKI, Joseph, A. , ALHASSAN, Abdul-Basit , BOGA, Sobhana Babu , GAO, Xiaolei , GUIADEEN, Deodialsingh , WANG, Jyhshing , XU, Jiayi , YU, Wensheng , YU, Younong , CAI, Jiaqiang , LIU, Shilan , WANG, Dahai , WU, Hao , YANG, Chundao
发明人： LIU, Jian , KOZLOWSKI, Joseph, A. , ALHASSAN, Abdul-Basit , BOGA, Sobhana Babu , GAO, Xiaolei , GUIADEEN, Deodialsingh , WANG, Jyhshing , XU, Jiayi , YU, Wensheng , YU, Younong , CAI, Jiaqiang , WANG, Dahai , WU, Hao , YANG, Chundao
IPC分类号： A61K31/5377 , A61K31/55 , C07D487/04 , A61K31/541
CPC分类号： A61K45/06 , C07D519/00
摘要： The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, or pharmaceutically acceptable salts thereof, Formula I or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.
摘要翻译：本发明提供了布鲁顿的式I的酪氨酸激酶（Btk）抑制剂化合物或其药学上可接受的盐，式I或包含这些化合物的药物组合物及其在治疗中的用途。特别地，本发明涉及式I的Btk抑制剂化合物在治疗Btk介导的病症中的用途。

9. 发明申请

WO2016106625A1 BTK INHIBITORS 审中-公开
标题翻译： BTK抑制剂
公开(公告)号：WO2016106625A1
公开(公告)日：2016-07-07
申请号：PCT/CN2014/095766
申请日：2014-12-31
申请人： MERCK SHARP & DOHME CORP. , LIU, Jian , KOZLOWSKI, Joseph A. , ALHASSAN, Abdul-Basit , BOGA, Sobhana Babu , GAO, Xiaolei , GUIADEEN, Deodialsingh , WANG, Jyhshing , XU, Jiayi , YU, Wensheng , YU, Younong , CAI, Jiaqiang , LIU, Shilan , WANG, Dahai , WU, Hao , YANG, Chundao
发明人： LIU, Jian , KOZLOWSKI, Joseph A. , ALHASSAN, Abdul-Basit , BOGA, Sobhana Babu , GAO, Xiaolei , GUIADEEN, Deodialsingh , WANG, Jyhshing , XU, Jiayi , YU, Wensheng , YU, Younong , CAI, Jiaqiang , LIU, Shilan , WANG, Dahai , WU, Hao , YANG, Chundao
IPC分类号： C07D487/04 , C07D471/04 , C07D519/06 , A61K31/4985 , A61K31/5365 , A61K31/506 , A61K31/519 , A61K31/53 , A61K31/437 , A61P19/02 , A61P11/00 , A61P21/04 , A61P25/00 , A61P3/10 , A61P7/02
CPC分类号： A61K45/06 , C07D519/00
摘要： Provided are Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders is provided.
摘要翻译：提供了根据式I的Bruton的酪氨酸激酶（Btk）抑制剂化合物或其药学上可接受的盐，包含这些化合物的药物组合物及其在治疗中的用途。特别地，提供了使用Btk抑制剂式I化合物治疗Btk介导的病症。

10. 发明申请

WO2016057753A1 SUBSTITUTED PYRIMIDINES AS INHIBITORS OF HIF PROLYL HYDROXYLASE 审中-公开
标题翻译：作为HIF-PRLYL羟化酶抑制剂的取代的嘧啶
公开(公告)号：WO2016057753A1
公开(公告)日：2016-04-14
申请号：PCT/US2015/054626
申请日：2015-10-08
申请人： MERCK SHARP & DOHME CORP , UJJAINWALLA, Fez , TAN, John Qiang , DANG, Qun , SINZ, Christopher J. , WANG, Ming , CHEN, Yili , CAI, Jiaqiang
发明人： UJJAINWALLA, Fez , TAN, John Qiang , DANG, Qun , SINZ, Christopher J. , WANG, Ming , CHEN, Yili , CAI, Jiaqiang
IPC分类号： C07D471/20 , C07D401/14 , C07D471/04
CPC分类号： C07D239/36 , A61P7/06 , C07D413/06
摘要： The present invention concerns compounds of Formula I that inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
摘要翻译：本发明涉及抑制HIF脯氨酰羟化酶的式I化合物，它们用于增强促红细胞生成素的内源产生的用途，以及用于治疗与促红细胞生成素的内源性产生减少有关的疾病如贫血等疾病，以及包含这种化合物和药物载体的药物组合物。

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