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1.发明申请PYRIMIDINE COMPOUNDS AS INHIBITORS OF PROTEIN KINASES IKK EPSILON AND/OR TBK-1, PROCESSES FOR THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开作为蛋白激酶抑制剂的吡嗪化合物IKK EPSILON和/或TBK-1，其制备方法和含有它们的药物组合物
公开(公告)号：WO2012010826A1
公开(公告)日：2012-01-26
申请号：PCT/GB2011/001075
申请日：2011-07-18
Applicant: DOMAINEX LIMITED , PERRIOR, Trevor, Robert , NEWTON, Gary, Karl , STEWART, Mark, Richard , AQIL, Rehan
Inventor： PERRIOR, Trevor, Robert , NEWTON, Gary, Karl , STEWART, Mark, Richard , AQIL, Rehan
IPC: C07D239/42 , C07D401/12 , C07D401/14 , C07D403/12 , A61K31/506 , A61P29/00 , A61P35/00
CPC classification number: C07D403/10 , C07D239/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/14 , C07D417/14
Abstract: C Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases ΙΚΚε and/or TBK-1 : in which: R 1 represents an aliphatic heterocyclyl group having 4, 5, 6 or 7 ring atoms, bonded to the phenyl group shown in formula I through a ring nitrogen atom, and optionally substituted by one or more substituents defined in the Specification; R 2 represents a phenyl or heteroaryl group which is optionally substituted by one or more substituents defined in the Specification; and each of R 3 and R 4 independently represents a hydrogen atom or a C 1-4 alkyl group.
Abstract translation: C通式（I）的化合物及其盐可用于治疗与蛋白激酶e和/或TBK-1的异常活性相关的疾病，其中：R1表示具有4个或更多个的脂肪族杂环基， 5,6或7个环原子，通过环氮原子与式I所示的苯基键合，并且任选被一个或多个在本说明书中定义的取代基取代; R 2表示任选被本说明书中定义的一个或多个取代基取代的苯基或杂芳基; R 3和R 4各自独立地表示氢原子或C 1-4烷基。
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2.发明申请PYRUVAMIDE COMPOUNDS AS INHIBITORS OF DUST MITE GROUP 1 PEPTIDASE ALLERGEN 审中-公开PYRUVAMIDE化合物作为DITE MITE GROUP 1 PEPTIDASE ALLERGEN的抑制剂
公开(公告)号：WO2011089396A3
公开(公告)日：2012-04-26
申请号：PCT/GB2011000079
申请日：2011-01-21
Applicant: ST GEORGE S HOSPITAL MEDICAL SCHOOL , UNIV MANCHESTER , ROBINSON CLIVE , ZHANG JIHUI , GARROD DAVID RONALD , PERRIOR TREVOR ROBERT , NEWTON GARY KARL , JENKINS KERRY , BEEVERS REBEKAH ELISABETH , KIMBERLEY MERIEL RUTH , STEWART MARK RICHARD
Inventor： ROBINSON CLIVE , ZHANG JIHUI , GARROD DAVID RONALD , PERRIOR TREVOR ROBERT , NEWTON GARY KARL , JENKINS KERRY , BEEVERS REBEKAH ELISABETH , KIMBERLEY MERIEL RUTH , STEWART MARK RICHARD
CPC classification number: C07K5/0202 , A01N37/46 , A01N43/16 , A01N43/30 , A01N43/36 , A01N43/38 , A01N43/40 , A01N43/42 , A01N43/48 , A01N43/60 , A01N43/72 , A01N43/84 , A61K38/00 , A61K38/06 , A61K38/07 , A61K45/06 , C07K5/06008 , C07K5/06034 , C07K5/06078 , C07K5/06139 , C07K5/06191 , C07K5/0804 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0821 , C07K5/0827
Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain pyruvamide compounds of the formula (X) (for convenience, collectively referred to herein as "PVA compounds"), which, inter alia, inhibit a dust mite Group 1 peptidase allergen (e.g., Der p 1, Der f 1, Eur m 1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit a dust mite Group 1 peptidase allergen, and in the treatment of diseases and disorders that are mediated by a dust mite Group 1 peptidase allergen; that are ameliorated by the inhibition of a dust mite Group 1 peptidase allergen; asthma; rhinitis; allergic conjunctivitis; atopic dermatitis; an allergic condition which is triggered by dust mites; an allergic condition which is triggered by a dust mite Group 1 peptidase allergen; and canine atopy.
Abstract translation: 本发明一般涉及治疗化合物领域，更具体地涉及式（X）的某些丙酮酰胺化合物（为了方便起见，统称为“PVA化合物”），其特别是抑制尘螨组 1肽酶变应原（例如，Der p 1，Der f 1，Eur m 1）。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制尘螨组1肽酶变应原和治疗由 尘螨组1肽酶变应原; 通过抑制尘螨组1肽酶变应原而得到改善; 哮喘; 鼻炎; 过敏性结膜炎 特应性皮炎; 由尘螨触发的过敏状况; 由尘螨组1肽酶变应原触发的过敏状况; 和犬特应性
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3.发明申请ALDEHYDE COMPOUNDS AS INHIBITORS OF DUST MITE GROUP 1 PEPTIDASE ALLERGEN AND THEIR USE 审中-公开作为杀菌剂组合物的杀虫剂化合物1杀菌剂过敏原及其使用
公开(公告)号：WO2012004554A1
公开(公告)日：2012-01-12
申请号：PCT/GB2011/001011
申请日：2011-07-04
Applicant: ST GEORGE'S HOSPITAL MEDICAL SCHOOL , THE UNIVERSITY OF MANCHESTER , ROBINSON, Clive , ZHANG, Jihui , GARROD, David Ronald , PERRIOR, Trevor Robert , NEWTON, Gary Karl , JENKINS, Kerry , STEWART, Mark Richard , KIMBERLEY, Meriel Ruth
Inventor： ROBINSON, Clive , ZHANG, Jihui , GARROD, David Ronald , PERRIOR, Trevor Robert , NEWTON, Gary Karl , JENKINS, Kerry , STEWART, Mark Richard , KIMBERLEY, Meriel Ruth
CPC classification number: C07K5/06191 , A61K38/00 , C07K5/06034 , C07K5/06078
Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aldehyde compounds of the following formula (A) (for convenience, collectively referred to herein as "ALD compounds"), which, inter alia , inhibit a dust mite Group 1 peptidase allergen ( e.g. , Der p 1, Der f 1, Eur m 1 ). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo , to inhibit a dust mite Group 1 peptidase allergen, and in the treatment of diseases and disorders that are mediated by a dust mite Group 1 peptidase allergen; that are ameliorated by the inhibition of a dust mite Group 1 peptidase allergen; asthma; rhinitis; allergic conjunctivitis; atopic dermatitis; an allergic condition which is triggered by dust mites; an allergic condition which is triggered by a dust mite Group 1 peptidase allergen; and canine atopy.
Abstract translation: 本发明一般涉及治疗化合物领域，更具体地涉及以下式（A）的某些醛化合物（为了方便起见，统称为“ALD化合物”），其特别地抑制尘螨 第1组肽酶变应原（例如，Der p 1，Der f 1，Eur m 1）。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制尘螨组1肽酶变应原和治疗由 尘螨1组肽酶变应原; 通过抑制尘螨组1肽酶变应原而得到改善; 哮喘; 鼻炎; 过敏性结膜炎 特应性皮炎; 由尘螨触发的过敏状况; 由尘螨组1肽酶变应原触发的过敏状况; 和犬特应性
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4.发明申请PYRUVAMIDE COMPOUNDS AS INHIBITORS OF DUST MITE GROUP 1 PEPTIDASE ALLERGEN AND THEIR USE. 审中-公开PYRUVAMIDE化合物作为DITE MITE 1 PEPTIDASE ALLERGEN及其使用的抑制剂。
公开(公告)号：WO2011089396A2
公开(公告)日：2011-07-28
申请号：PCT/GB2011/000079
申请日：2011-01-21
Applicant: ST GEORGE'S HOSPITAL MEDICAL SCHOOL , THE UNIVERSITY OF MANCHESTER , ROBINSON, Clive , ZHANG, Jihui , GARROD, David, Ronald , PERRIOR, Trevor, Robert , NEWTON, Gary, Karl , JENKINS, Kerry , BEEVERS, Rebekah, Elisabeth , KIMBERLEY, Meriel, Ruth , STEWART, Mark, Richard
Inventor： ROBINSON, Clive , ZHANG, Jihui , GARROD, David, Ronald , PERRIOR, Trevor, Robert , NEWTON, Gary, Karl , JENKINS, Kerry , BEEVERS, Rebekah, Elisabeth , KIMBERLEY, Meriel, Ruth , STEWART, Mark, Richard
CPC classification number: C07K5/0202 , A01N37/46 , A01N43/16 , A01N43/30 , A01N43/36 , A01N43/38 , A01N43/40 , A01N43/42 , A01N43/48 , A01N43/60 , A01N43/72 , A01N43/84 , A61K38/00 , A61K38/06 , A61K38/07 , A61K45/06 , C07K5/06008 , C07K5/06034 , C07K5/06078 , C07K5/06139 , C07K5/06191 , C07K5/0804 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0821 , C07K5/0827
Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain pyruvamide compounds of the formula (X) (for convenience, collectively referred to herein as "PVA compounds"), which, inter alia, inhibit a dust mite Group 1 peptidase allergen (e.g., Der p 1, Der f 1, Eur m 1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo , to inhibit a dust mite Group 1 peptidase allergen, and in the treatment of diseases and disorders that are mediated by a dust mite Group 1 peptidase allergen; that are ameliorated by the inhibition of a dust mite Group 1 peptidase allergen; asthma; rhinitis; allergic conjunctivitis; atopic dermatitis; an allergic condition which is triggered by dust mites; an allergic condition which is triggered by a dust mite Group 1 peptidase allergen; and canine atopy.
Abstract translation: 本发明一般涉及治疗化合物领域，更具体地涉及式（X）的某些丙酮酰胺化合物（为了方便起见，统称为“PVA化合物”），其特别是抑制尘螨组 1肽酶变应原（例如，Der p 1，Der f 1，Eur m 1）。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制尘螨组1肽酶变应原和治疗由 尘螨1组肽酶变应原; 通过抑制尘螨组1肽酶变应原而得到改善; 哮喘; 鼻炎; 过敏性结膜炎 特应性皮炎; 由尘螨触发的过敏状况; 由尘螨组1肽酶变应原触发的过敏状况; 和犬特应性
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