公开(公告)号：WO2010046639A1

公开(公告)日：2010-04-29

申请号：PCT/GB2009/002504

申请日：2009-10-21

Applicant: UCB PHARMA S.A. ,  JENKINS, Kerry ,  LOCK, Christopher, James ,  RATCLIFFE, Andrew, James

Inventor： JENKINS, Kerry ,  LOCK, Christopher, James ,  RATCLIFFE, Andrew, James

IPC: C07D495/04 ,  A61P29/00 ,  A61K31/4365

CPC classification number: C07D495/04

Abstract: A series of heteroaryl-substituted fused pyridine derivatives, in particular heteroaryl-substituted thieno[3,2-6]pyridine derivatives, being selective inhibitors of PO kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.

Abstract translation: 一系列杂芳基取代的稠合吡啶衍生物，特别是杂芳基取代的噻吩并[3,2-6]吡啶衍生物，是PO激酶的选择性抑制剂，因此在医学中有益，例如在治疗炎症，自身免疫 ，心血管，神经变性，代谢，肿瘤，伤害性或眼科疾病。

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

IPC: C07K5/06 ,  C07K5/08 ,  A61P37/08 ,  A61P37/06

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

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

IPC: C07K5/06 ,  A01N43/00 ,  A61K38/06 ,  A61P37/08 ,  C07K5/08

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

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

IPC: C07K5/06 ,  A61K38/05 ,  A61P33/14

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

公开(公告)号：WO2008001076A1

公开(公告)日：2008-01-03

申请号：PCT/GB2007/002390

申请日：2007-06-26

Applicant: UCB PHARMA S.A. ,  ALEXANDER, Rikki, Peter ,  AUJLA, Pavandeep, Singh ,  CRÉPY, Karen, Viviane, Lucile ,  FOLEY, Anne, Marie ,  FRANKLIN, Richard, Jeremy ,  HAUGHAN, Alan, Findlay ,  HORSLEY, Helen, Tracey ,  JONES, William, Mark ,  LALLEMAND, Bénédicte, Irma, Léonce, Frédérique ,  MACK, Stephen, Robert ,  MORGAN, Trevor ,  PASAU, Patrick, Marie, Ghislain ,  PHILLIPS, David, Jonathan ,  SABIN, Verity, Margaret ,  BUCKLEY, George, Martin ,  JENKINS, Kerry ,  PERRY, Benjamin, Garfield

Inventor： ALEXANDER, Rikki, Peter ,  AUJLA, Pavandeep, Singh ,  CRÉPY, Karen, Viviane, Lucile ,  FOLEY, Anne, Marie ,  FRANKLIN, Richard, Jeremy ,  HAUGHAN, Alan, Findlay ,  HORSLEY, Helen, Tracey ,  JONES, William, Mark ,  LALLEMAND, Bénédicte, Irma, Léonce, Frédérique ,  MACK, Stephen, Robert ,  MORGAN, Trevor ,  PASAU, Patrick, Marie, Ghislain ,  PHILLIPS, David, Jonathan ,  SABIN, Verity, Margaret ,  BUCKLEY, George, Martin ,  JENKINS, Kerry ,  PERRY, Benjamin, Garfield

IPC: C07D513/04 ,  C07D519/00 ,  C07D513/12 ,  A61K31/437 ,  A61K31/519

CPC classification number: C07D495/04 ,  C07D513/04 ,  C07D513/12 ,  C07D519/00

Abstract: A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.

Abstract translation: 一系列6,7-二氢[1,3]噻唑并[5,4-c]吡啶-4（5H） - 酮衍生物及其类似物，其在2-位被任选取代的吗啉-4- 作为PI3激酶的选择性抑制剂，因此在医学中有益，例如在治疗炎性，自身免疫，心血管，神经退行性，代谢性，肿瘤学，伤害性感受性或眼科疾病中。