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1. 发明申请

US20140221333A1 BTK INHIBITORS 审中-公开
标题翻译： BTK抑制剂
公开(公告)号：US20140221333A1
公开(公告)日：2014-08-07
申请号：US14233478
申请日：2012-07-19
申请人： Adrianus Petrus Antonius De Man , Jan-Gerard Sterrenburg , Han C.A. Raaijmakers , Allard Kaptein , Arthura A. Oubrie , Johannes Bernardus Maria Rewinkel , Christiaan Gerardus Johannes Maria Jans , Jacobus C.H.M. Wijkamans , Tjeerd A. Barf , Alan B. Cooper , Ronald M. Kim , Sobhana Babu Boga , Hugh Y. Zhu , Xiaolei Gao , Xin Yao , Rajan Anand , Hao Wu , Shilan Liu , Chundao Yang , Abdul-Basit Alhassan , James Wang , Younong Yu , Jian Liu , Henry M. Vaccaro
发明人： Adrianus Petrus Antonius De Man , Jan-Gerard Sterrenburg , Han C.A. Raaijmakers , Allard Kaptein , Arthura A. Oubrie , Johannes Bernardus Maria Rewinkel , Christiaan Gerardus Johannes Maria Jans , Jacobus C.H.M. Wijkamans , Tjeerd A. Barf , Alan B. Cooper , Ronald M. Kim , Sobhana Babu Boga , Hugh Y. Zhu , Xiaolei Gao , Xin Yao , Rajan Anand , Hao Wu , Shilan Liu , Chundao Yang , Abdul-Basit Alhassan , James Wang , Younong Yu , Jian Liu , Henry M. Vaccaro
IPC分类号： C07D487/04 , C07D513/04 , A61K31/55 , A61K31/5377 , A61K31/53 , A61K31/4985 , A61K31/541
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/06 , C07D471/04 , C07D513/04 , C07D519/00
摘要： Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
摘要翻译：提供根据式（I）的6-5元稠合吡啶环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，提供了使用元稠合的吡啶环化合物来治疗布鲁丁的酪氨酸激酶（Btk）介导的病症。

2. 发明申请

US20140155406A1 4-IMIDAZOPYRIDAZIN-1-YL-BENZAMIDES AND 4-IMIDAZOTRIAZIN-1-YL-BENZAMIDES BTK INHIBITORS 审中-公开
标题翻译： 4-咪唑并吡嗪-1-基-L-苯甲酰胺和4-咪唑氧基-1-YL-苯甲酮BTK抑制剂
公开(公告)号：US20140155406A1
公开(公告)日：2014-06-05
申请号：US14233429
申请日：2012-07-11
申请人： Petrus Antonius De Adrianus Man , Jacobus C.H.M. Wijkmans , Jan-Gerard Sterrenburg , Han C.A. Raaijmakers , Tjeerd A. Barf , Rogier Christian Buijsman , Arthur A. Oubrie , Johannes Bernardus Maria Rewinkel , Christiaan Gerardus Johannes Maria Jans , Herman Thijs Stock
发明人： Petrus Antonius De Adrianus Man , Jacobus C.H.M. Wijkmans , Jan-Gerard Sterrenburg , Han C.A. Raaijmakers , Tjeerd A. Barf , Rogier Christian Buijsman , Arthur A. Oubrie , Johannes Bernardus Maria Rewinkel , Christiaan Gerardus Johannes Maria Jans , Herman Thijs Stock
IPC分类号： A61K31/506 , C07D487/04 , A61K31/4985
CPC分类号： A61K31/506 , A61K31/4985 , C07D487/04 , C07D519/00
摘要： The present invention relates to 6-5 membered fused pyridine ring compounds of formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
摘要翻译：本发明涉及式（I）的6-5元稠合吡啶环化合物或其药学上可接受的盐，或涉及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6-5元稠合吡啶环化合物在治疗布鲁特酪氨酸激酶（Btk）介导的病症中的用途。

3. 发明授权

US09290504B2 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides as Btk inhibitors 有权
标题翻译： 4-咪唑并哒嗪-1-基 - 苯甲酰胺和4-咪唑并三嗪-1-基 - 苯甲酰胺作为Btk抑制剂
公开(公告)号：US09290504B2
公开(公告)日：2016-03-22
申请号：US14233418
申请日：2012-07-11
申请人： Tjeerd A. Barf , Christiaan Gerardus Johannes Maria Jans , Petrus Antonius De Adrianus Man , Arthur A. Oubrie , Hans C. A. Raaijmakers , Johannes Bernardus Maria Rewinkel , Jan-Gerard Sterrenburg , Jacobus C. H. M. Wijkmans
发明人： Tjeerd A. Barf , Christiaan Gerardus Johannes Maria Jans , Petrus Antonius De Adrianus Man , Arthur A. Oubrie , Hans C. A. Raaijmakers , Johannes Bernardus Maria Rewinkel , Jan-Gerard Sterrenburg , Jacobus C. H. M. Wijkmans
IPC分类号： A61K31/4985 , C07D487/04 , C07D519/00 , A61K31/501 , A61K31/506 , A61K31/55
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/55 , C07D519/00 , Y02A50/411
摘要： The present invention relates to 6-5 membered fused pyridine ring compounds according to formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to formula I in the treatment of Brutons Tyrosine Kinase (Btk) mediated disorders.
摘要翻译：本发明涉及式（I）的6-5元稠合吡啶环化合物或其药学上可接受的盐，或涉及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，本发明涉及根据式I的6-5元稠合吡啶环化合物在治疗Brutons酪氨酸激酶（Btk）介导的病症中的用途。

4. 发明授权

US08658794B2 8-methyl-1-phenyl-imidazol[1,5-a]pyrazine compounds as Lck inhibitors and uses thereof 有权
标题翻译： 8-甲基-1-苯基 - 咪唑并[1,5-a]吡嗪化合物作为Lck抑制剂及其用途
公开(公告)号：US08658794B2
公开(公告)日：2014-02-25
申请号：US13577417
申请日：2011-02-03
申请人： Adrianus Petrus Antonius de Man , Johannes Bernardus Maria Rewinkel , Christiaan Gerardus Johannes Maria Jans , Hans Cornelis Andreas Raaijmakers , Jacobus Cornelis Henricus Maria Wijkmans
发明人： Adrianus Petrus Antonius de Man , Johannes Bernardus Maria Rewinkel , Christiaan Gerardus Johannes Maria Jans , Hans Cornelis Andreas Raaijmakers , Jacobus Cornelis Henricus Maria Wijkmans
IPC分类号： C07D495/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides 8-methyl-1-phenyl-imidazo[1,5-a]pyrazine derivatives according to formula I or pharmaceutically acceptable salts thereof. The compounds of the current invention show inhibitory activity against Lck and can be used for the treatment of Lck-mediated diseases or Lck-mediated conditions such as inflammatory disorders.
摘要翻译：本发明提供了根据式I的8-甲基-1-苯基 - 咪唑并[1,5-a]吡嗪衍生物或其药学上可接受的盐。本发明的化合物显示出对Lck的抑制活性，可用于治疗Lck介导的疾病或Lck介导的病症如炎症性疾病。

5. 发明授权

US08133885B2 Non steroidal glucocorticoid receptor modulators 失效
标题翻译：非类固醇糖皮质激素受体调节剂
公开(公告)号：US08133885B2
公开(公告)日：2012-03-13
申请号：US11816113
申请日：2006-02-14
申请人： Ralf Plate , Guido Jenny Rudolf Zaman , Pedro Harold Han Hermkens , Christiaan Gerardus Johannes Maria Jans , Rogier Christian Buijsman , Adrianus Petrus Antonius De Man , Paolo Giovanni Martino Conti , Scott James Lusher , Willem Hendrik Abraham Dokter
发明人： Ralf Plate , Guido Jenny Rudolf Zaman , Pedro Harold Han Hermkens , Christiaan Gerardus Johannes Maria Jans , Rogier Christian Buijsman , Adrianus Petrus Antonius De Man , Paolo Giovanni Martino Conti , Scott James Lusher , Willem Hendrik Abraham Dokter
IPC分类号： A61P29/00 , A61K31/551 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to compounds having general Formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to pharmaceutical compositions comprising said compounds and the use of these derivatives to modulate glucocorticoid receptor activity.
摘要翻译：本发明涉及具有通式（I）的化合物或其药学上可接受的盐。本发明还涉及包含所述化合物的药物组合物和这些衍生物用于调节糖皮质激素受体活性的用途。

6. 发明申请

US20090062262A1 NON STEROIDAL GLUCOCORTICOID RECEPTOR MODULATORS 失效
公开(公告)号：US20090062262A1
公开(公告)日：2009-03-05
申请号：US11816113
申请日：2006-02-14
申请人： Ralf Plate , Guido Jenny Rudolf Zaman , Pedro Harold Han Hermkens , Christiaan Gerardus Johannes Maria Jans , Rogier Christian Buijsman , Adrianus Petrus Antonius De Man , Paolo Giovanni Martino Conti , Scott James Lusher , Willem Hendrik Abraham Dokter
发明人： Ralf Plate , Guido Jenny Rudolf Zaman , Pedro Harold Han Hermkens , Christiaan Gerardus Johannes Maria Jans , Rogier Christian Buijsman , Adrianus Petrus Antonius De Man , Paolo Giovanni Martino Conti , Scott James Lusher , Willem Hendrik Abraham Dokter
IPC分类号： A61K31/551 , C07D471/04 , A61P29/00 , A61P37/00
CPC分类号： C07D471/04
摘要： The present invention relates to compounds having general Formula (I) or a pharmaceutically acceptable salt thereof. In this formula R1 is H or (1-4C)alkyl; R2 is —C(O)R15 or —S(O)2R15; R3 is H, (1-4C)alkyl or —OR16; R4 is H, (1-4C)alkyl or —OR16; R6 is H or —C(H)NOR16; R7 is H or halogen, cyano; (1-6C)alkyl, (2-6C)alkenyl or (2-6C)alkynyl, all three optionally substituted with OH, halogen or NH2; —C(H)NOR16, —OR16, —C(O)R16, or —C(O)OR16; R8 is H, cyano, halogen, nitro; (1-6C) alkyl, (2-6C)alkenyl, (2-6C)alkynyl or —O(1-6C)alkyl, all optionally substituted with amino, hydroxyl or halogen; (hetero)aryl, optionally substituted with cyano, halogen, (1-4C)alkyl, (1-4C)alkoxy, (1-4C)alkoxy(1-4C)alkyl; —C(O)R18, —C(O)OR19, —C(O)NHR17, —NHC(O)R20, —C(1-4C)alkylNOR21; —C(H)NOR16, or —NHS(O)2R21; R9 is H, halogen, cyano or (1-4C)alkyl optionally substituted with halogen; R10 is H or (1-4C)alkyl; R11 is H; R12 is H, cyano or (1-4C)alkyl; R13 is H, (1-4C)alkyl, halogen or formyl; R14 is H, halogen, cyano, (1-4C)alkyl, (2-6C)alkenyl, C(O)R21 or (hetero)aryl; R15 is H; (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, —O(2-6C)alkyl, —O(2-6C)alkenyl or —O(2-6C)alkynyl, all optionally substituted with one or more OH, halogen, cyano or (hetero)aryl, (hetero)aryl, optionally substituted with (1-4C)alkyl, halogen, cyano, nitro or amino, NH2, (di)(1-4C)alkylamino, (1-4C)alkyl(1-4C)alkoxyamine, (1-4C)alkylthio(1-4C)alkyl or (1-4C)alkoxy(1-4C)alkyl; R16 is H, (1-6C)alkyl, (2-6C)alkenyl or (2-6C)alkynyl; R17 is H, (1-6C)alkyl, optionally substituted with halogen, (1-4C)alkoxy or (hetero)aryl, optionally substituted with halogen, (1-4C)alkyl or (1-25 4C)alkoxy; (3-6C)cycloalkyl or (hetero)aryl, optionally substituted with halogen, (1-4C)alkyl or (1-4C)alkoxy; R18 is H, NH2, C(O)R21 or (1-4C)alkyl, optionally substituted with OH, halogen, cyano or —S(1-4C)alkyl; R19 is H or (1-6C)alkyl, optionally substituted with OH or halogen; R20 is H, (1-6C)alkyl or (2-6C)alkenyl, both optionally substituted by halogen, O(1-6C)alkyl, (hetero)aryl, optionally substituted with (1-4C)alkyl or halogen; (3-6C)cycloalkyl; (1-6C)alkoxy; (1-6C)alkenyloxy; or (hetero)aryl, optionally substituted with (1-4C)alkyl); NH2, —NH(1-6C)alkyl or —NH(hetero)aryl and R21 is H or (1-6C)alkyl. The present invention also relates to pharmaceutical compositions comprising said compounds and the use of these derivatives to modulate glucocorticoid receptor activity.

7. 发明授权

US08575152B2 Non-steroidal compounds useful as glucocorticoid receptor modulators 失效
标题翻译：用作糖皮质激素受体调节剂的非甾体化合物
公开(公告)号：US08575152B2
公开(公告)日：2013-11-05
申请号：US12065241
申请日：2006-08-25
申请人： Ralf Plate , Christiaan Gerardus Johannes Maria Jans
发明人： Ralf Plate , Christiaan Gerardus Johannes Maria Jans
IPC分类号： A61P5/44 , A61P29/00 , A61K31/55 , C07D471/04
CPC分类号： C07D471/04
摘要： This invention relates to novel amino acid derivatives of formula (I) wherein the R groups have the following meanings: —R1 is —H or —(1-4C)alkyl; —R2 is —C(O)R15 or —S(O)2R15; —R3 is —H, —(1-4C)alkyl or —OR16; —R4 is —H, —(1-4C)alkyl or —OR16; —R6 is —H or —C(R16)NOR16; —R7 is —H, -halogen, -cyano; —(1-6C)alkyl, —(2-6C)alkenyl or —(2-6C)alkynyl, all optionally substituted with -amino, -hydroxyl or -halogen; —R8 is —H, -cyano, -halogen, -nitro; —(1-6C)alkyl, —(2-6C)alkenyl, —(2-6C)alkynyl or —O(1-6C)alkyl, all optionally substituted with -amino, -hydroxyl or -halogen; -(hetero)aryl, optionally substituted with -cyano, -halogen, —(1-4C)alkyl, —(1-4C)alkoxy, —(1-4C)alkoxy(1-4C)alkyl or -(hetero)aryl; —C(R16)NOR16; —C(O)N(R17)2; —C(O)R18, —C(O)OR19, —NHC(O)R20, or —NHS(O)2R21; —R9 is —H, -halogen, -cyano, or —(1-4C)alkyl, optionally substituted with -halogen; —R10 is —H or —(1-4C)alkyl; —R11 is —H; —R12 is —H, -cyano or —(1-4C)alkyl; —R13 is —H, —(1-4C)alkyl, -halogen or -formyl; —R14 is —H, -halogen, -cyano, —(1-4C)alkyl or -(hetero)aryl; or a pharmaceutically acceptable salt thereof. The compounds of this invention are highly specific for the glucocorticoid receptor and may be used for treating inflammatory diseases.
摘要翻译：本发明涉及式（I）的新型氨基酸衍生物，其中R基具有以下含义：-R 1是-H或 - （1-4C）烷基; -R 2是-C（O）R 15或-S（O）2 R 15; -R 3是-H， - （1-4C）烷基或-OR 16; -R4是-H， - （1-4C）烷基或-OR16; -R6是-H或-C（R16）NOR16; -R 7是-H， - 卤素， - 氰基; - （1-6C）烷基， - （2-6C）烯基或 - （2-6C）炔基，全部被氨基，羟基或卤素取代; -R 8是-H， - 氰基， - 卤素， - 硝基; - （1-6C）烷基， - （2-6C）烯基， - （2-6C）炔基或-O（1-6C）烷基，全部被氨基，羟基或卤素取代; - （1-4）烷氧基， - （1-4C）烷氧基（1-4C）烷基或 - （杂）芳基， ; -C（R 16）NOR16; -C（O）N（R 17）2; -C（O）R 18，-C（O）OR 19，-NHC（O）R 20或-NHS（O）2 R 21; -R9是-H， - 卤素， - 氰基或 - （1-4C）烷基，任选被卤素取代; -R 10是-H或 - （1-4C）烷基; -R11为-H; -R12是-H， - 氰基或 - （1-4C）烷基; -R13是-H， - （1-4C）烷基， - 卤素或 - 甲酰基; -R14是-H， - 卤素， - 氰基， - （1-4C）烷基或 - （杂）芳基; 或其药学上可接受的盐。本发明化合物对糖皮质激素受体高度特异，可用于治疗炎性疾病。

8. 发明申请

US20080188459A1 Non-Steroidal Compounds Useful as Glucocorticoid Receptor Modulators 失效
公开(公告)号：US20080188459A1
公开(公告)日：2008-08-07
申请号：US12065241
申请日：2006-08-25
申请人： Ralf Plate , Christiaan Gerardus Johannes Maria Jans
发明人： Ralf Plate , Christiaan Gerardus Johannes Maria Jans
IPC分类号： C07D223/14 , A61K31/55 , A61P1/00 , A61P19/02 , A61P37/00
CPC分类号： C07D471/04
摘要： This invention relates to novel amino acid derivatives of formula (I) wherein the R groups have the following meanings: —R1 is —H or -(1-4C)alkyl; —R2 is —C(O)R15 or —S(O)2R15; —R3 is —H, -(1-4C)alkyl or —OR16; —R4 is —H, -(1-4C)alkyl or —OR16; —R6 is —H or —C(R16)NOR16; —R7 is —H, -halogen, -cyano; -(1-6C)alkyl, -(2-6C)alkenyl or -(2-6C)alkynyl, all optionally substituted with -amino, -hydroxyl or -halogen; —R8 is —H, -cyano, -halogen, -nitro; -(1-6C)alkyl, -(2-6C)alkenyl, -(2-6C)alkynyl or —O(1-6C)alkyl, all optionally substituted with -amino, -hydroxyl or -halogen; -(hetero)aryl, optionally substituted with -cyano, -halogen, -(1-4C)alkyl, -(1-4C)alkoxy, -(1-4C)alkoxy(1-4C)alkyl or -(hetero)aryl; —C(R16)NOR16; —C(O)N(R17)2; —C(O)R18, —C(O)OR19, —NHC(O)R20, or —NHS(O)2R21; —R9 is —H, -halogen, -cyano, or -(1-4C)alkyl, optionally substituted with -halogen; —R10 is —H or -(1-4C)alkyl; —R11 is —H; —R12 is —H, -cyano or -(1-4C)alkyl; —R13 is —H, -(1-4C)alkyl, -halogen or -formyl; —R14 is —H, -halogen, -cyano, -(1-4C)alkyl or -(hetero)aryl; or a pharmaceutically acceptable salt thereof. The compounds of this invention are highly specific for the glucocorticoid receptor and may be used for treating inflammatory diseases.

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