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1. 发明申请

WO2009112490A1 SULFONAMIDES AS ZAP-70 INHIBITORS 审中-公开
标题翻译：磺酰胺作为ZAP-70抑制剂
公开(公告)号：WO2009112490A1
公开(公告)日：2009-09-17
申请号：PCT/EP2009/052789
申请日：2009-03-10
申请人： CELLZOME LIMITED , MAJOR, Jeremy , HARRISON, Richard, John , RAMSDEN, Nigel , MIDDLEMISS, David , KRUSE, Ulrich , DREWES, Gerard
发明人： MAJOR, Jeremy , HARRISON, Richard, John , RAMSDEN, Nigel , MIDDLEMISS, David , KRUSE, Ulrich , DREWES, Gerard
IPC分类号： C07D239/48 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D401/12 , C07D407/12 , A61K31/505 , A61K31/506 , A61K31/538 , A61K31/5377 , A61P37/06 , A61P37/08
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention relates to compounds of formula (I), wherein R 1 to R 9 and R 4a have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of ZAP-70 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immuno logically- mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中R1至R9和R4a具有在说明书和权利要求书中引用的含义。所述化合物可用作ZAP-70的抑制剂，用于治疗或预防免疫学，炎症，自身免疫，过敏性疾病和免疫逻辑介导的疾病。本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。

2. 发明申请

WO2005110963A1 (BIPHENYL-3-YL)-CARBOXYLIC ACIDS AND DERIVATIVES THEREOF AND THEIR USE IN THERAPY 审中-公开
标题翻译：（BIPHENYL-3-YL） - 羧酸及其衍生物及其在治疗中的使用
公开(公告)号：WO2005110963A1
公开(公告)日：2005-11-24
申请号：PCT/EP2005/005444
申请日：2005-05-19
申请人： CELLZOME AG , RAMSDEN, Nigel , WILSON, Francis , REID, Alison , READER, Valerie , MILLER, Warren , HARRISON, Richard, John , SUNOSE, Mihiro , HERNANDEZ-PERNI, Remedios , MAJOR, Jeremy , BOUSSARD, Cyrille , SMELT, Kathryn , TAYLOR, Jess , LEFORMAL, Adeline , CANSFIELD, Andrew , BURCKHARDT, Svenja
发明人： RAMSDEN, Nigel , WILSON, Francis , REID, Alison , READER, Valerie , MILLER, Warren , HARRISON, Richard, John , SUNOSE, Mihiro , HERNANDEZ-PERNI, Remedios , MAJOR, Jeremy , BOUSSARD, Cyrille , SMELT, Kathryn , TAYLOR, Jess , LEFORMAL, Adeline , CANSFIELD, Andrew , BURCKHARDT, Svenja
IPC分类号： C07C57/58
CPC分类号： C07C61/40 , C07C51/09 , C07C51/353 , C07C51/363 , C07C57/58 , C07C59/64
摘要： The present invention relates to compounds having the general formula (I) with the definitions of R I -R 3 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds as a medicament, preferably for the treatment of Alzheimer's disease and their use for the modulation of g-secretase activity.
摘要翻译：本发明涉及具有下面给出的R 1 -R 3定义的通式（I）的化合物和/或其盐或酯。此外，本发明涉及所述化合物作为药物，优选用于治疗阿尔茨海默氏病及其用于调节g-分泌酶活性的用途。

3. 发明申请

WO2006021441A1 BIPHENYL-CARBOXYLIC ACIDS AND DERIVATIVES THEREOF AND THEIR USE IN THERAPY 审中-公开
标题翻译：双酚 - 羧酸及其衍生物及其在治疗中的应用
公开(公告)号：WO2006021441A1
公开(公告)日：2006-03-02
申请号：PCT/EP2005/009188
申请日：2005-08-25
申请人： CELLZOME AG , RAMSDEN, Nigel , WILSON, Francis , REID, Alison , READER, Valerie , MILLER, Warren , HARRISON, Richard, John , SUNOSE, Mihiro , HERNANDEZ-PERNI, Remedios , MAJOR, Jeremy , BOUSSARD, Cyrille , SMELT, Kathryn , TAYLOR, Jess , LEFORMAL, Adeline , CANSFIELD, Andrew , BURCKHARDT, Svenja
发明人： RAMSDEN, Nigel , WILSON, Francis , REID, Alison , READER, Valerie , MILLER, Warren , HARRISON, Richard, John , SUNOSE, Mihiro , HERNANDEZ-PERNI, Remedios , MAJOR, Jeremy , BOUSSARD, Cyrille , SMELT, Kathryn , TAYLOR, Jess , LEFORMAL, Adeline , CANSFIELD, Andrew , BURCKHARDT, Svenja
IPC分类号： C07C57/58 , A61K31/192 , A61K31/216 , A61P25/28
CPC分类号： C07C57/58 , C07C57/62
摘要： The present invention relates to compounds having the general formula (I) with the definitions of R 1 -R 4 given below, and/or salt or ester thereof. Furthermore, the invention relates to the use of said compounds as a medicament, preferably for the treatment of Alzheimer's disease and their use for the modulation of γ-secretase activity.
摘要翻译：本发明涉及具有通式（I）的化合物及其盐或酯，其定义如下：其中R 1，R 2，R 4，此外，本发明涉及所述化合物作为药物，优选用于治疗阿尔茨海默氏病及其用于调节γ-分泌酶活性的用途。

4. 发明申请

WO2011134831A1 PYRAZOLE COMPOUNDS AS JAK INHIBITORS 审中-公开
标题翻译：吡咯化合物作为JAK抑制剂
公开(公告)号：WO2011134831A1
公开(公告)日：2011-11-03
申请号：PCT/EP2011/056158
申请日：2011-04-18
申请人： CELLZOME LIMITED , HARRISON, Richard, John , OXENFORD, Sally , HOBSON, Andrew , RAMSDEN, Nigel , MILLER, Warren
发明人： HARRISON, Richard, John , OXENFORD, Sally , HOBSON, Andrew , RAMSDEN, Nigel , MILLER, Warren
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00 , A61P29/00
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of formula (I), wherein R 1 , R 2 , R 1a , R 1b have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中R1，R2，R1a，R1b具有在说明书和权利要求书中引用的含义。所述化合物可用作JAK抑制剂，用于治疗或预防免疫学，炎症，自身免疫，过敏性疾病和免疫介导的疾病。本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。

5. 发明申请

WO2011029807A1 ORTHO SUBSTITUTED PYRIMIDINE COMPOUNDS AS JAK INHIBITORS 审中-公开
标题翻译： ORTHO替代吡嗪化合物作为JAK抑制剂
公开(公告)号：WO2011029807A1
公开(公告)日：2011-03-17
申请号：PCT/EP2010/063077
申请日：2010-09-07
申请人： CELLZOME LIMITED , HARRISON, Richard, John , HOBSON, Andrew , RAMSDEN, Nigel
发明人： HARRISON, Richard, John , HOBSON, Andrew , RAMSDEN, Nigel
IPC分类号： C07D239/48 , C07D403/12 , A61K31/505 , A61K31/506 , A61P37/00 , A61P35/00
CPC分类号： C07D403/12 , C07D239/48
摘要： The present invention relates to compounds of formula (I), wherein X 1 to X 3 , R, R 2 to R 7 and AA have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中X1至X3，R，R2至R7和AA具有在说明书和权利要求书中引用的含义。所述化合物可用作JAK抑制剂，用于治疗或预防免疫学，炎症，自身免疫，过敏性疾病和免疫介导的疾病。本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。

6. 发明申请

WO2010146133A1 HETEROCYCLYLAMINOPYRIMIDINES AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的杂环亚氨基嘧啶
公开(公告)号：WO2010146133A1
公开(公告)日：2010-12-23
申请号：PCT/EP2010/058574
申请日：2010-06-17
申请人： CELLZOME LIMITED , SUNOSE, Mihiro , MAJOR, Jeremy , HARRISON, Richard, John , FREEMAN, Jay , MOREL, Adeline
发明人： SUNOSE, Mihiro , MAJOR, Jeremy , HARRISON, Richard, John , FREEMAN, Jay , MOREL, Adeline
IPC分类号： C07D403/12 , C07D413/12 , A61K31/506 , A61P37/00 , A61P29/00
CPC分类号： C07D403/12 , C07D413/12
摘要： The invention relates to compounds of formula (I), wherein R 1 to R 6 and T 0 have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of ZAP-70, Syk or JAK3 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中R1至R6和T0具有在说明书和权利要求书中引用的含义。所述化合物可用作ZAP-70，Syk或JAK3的抑制剂，用于治疗或预防免疫学，炎症，自身免疫，过敏性疾病，免疫介导的疾病。本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。

7. 发明申请

WO2007124351A1 TERPHENYL DERIVATIVES FOR TREATMENT OF ALZHEIMER' S DISEASE 审中-公开
标题翻译：用于治疗阿尔茨海默病的泰勒衍生物
公开(公告)号：WO2007124351A1
公开(公告)日：2007-11-01
申请号：PCT/US2007/066951
申请日：2007-04-19
申请人： ORTHO-MCNEIL PHARMACEUTICAL, INC. , CELLZOME (UK) LTD. , WILSON, Francis , REID, Alison , READER, Valerie , HARRISON, Richard, John , SUNOSE, Mihiro , HERNADEZ-PERNI, Remedios , MAJOR, Jeremy , BOUSSARD, Cyrille , SMELT, Kathryn , TAYLOR, Jess , LEFORMAL, Adeline , CANSFIELD, Andrew , BURCKHARDT, Svenja , ZHANG, Yan , HO, Chih Yung
发明人： WILSON, Francis , REID, Alison , READER, Valerie , HARRISON, Richard, John , SUNOSE, Mihiro , HERNADEZ-PERNI, Remedios , MAJOR, Jeremy , BOUSSARD, Cyrille , SMELT, Kathryn , TAYLOR, Jess , LEFORMAL, Adeline , CANSFIELD, Andrew , BURCKHARDT, Svenja , ZHANG, Yan , HO, Chih Yung
IPC分类号： C07C51/09 , C07C57/38 , C07C57/58 , C07C59/64 , C07D257/04 , A61K31/192 , A61P25/28
CPC分类号： C07D257/04 , C07C51/09 , C07C57/38 , C07C57/58 , C07C59/56 , C07C59/64 , C07C63/331 , C07C69/65
摘要： The present invention relates to compounds having the general formula (I) with the definitions of X, Y, R 1 , R 2 , R 3 , R 4 , R 9 , R 10 given below, and solvates, hydrates, esters, and pharmaceutically acceptable salts thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of γ-secretase activity.
摘要翻译：本发明涉及具有通式（I）的化合物，其具有X，Y，R 1，R 2，R 3， R 4，R 9，R 10，及其溶剂合物，水合物，酯和药学上可接受的盐。此外，本发明涉及所述化合物用于治疗阿尔茨海默氏病及其用于调节γ-分泌酶活性的用途。

8. 发明申请

WO2006045554A1 (BIPHENYL) CARBOXYLIC ACIDS AND DERIVATIVES THEREOF 审中-公开
标题翻译：（BIPHENYL）羧酸及其衍生物
公开(公告)号：WO2006045554A1
公开(公告)日：2006-05-04
申请号：PCT/EP2005/011349
申请日：2005-10-21
申请人： CELLZOME AG , WILSON, Francis , REID, Alison , READER, Valerie , HARRISON, Richard, John , SUNOSE, Mihiro , HERNANDEZ-Perni, Remedios , MAJOR, Jeremy , BOUSSARD, Cyrille , SMELT, Kathryn , TAYLOR, Jess , LEFORMAL, Adeline , CANSFIELD, Andrew , BURCKHARDT, Svenja
发明人： WILSON, Francis , REID, Alison , READER, Valerie , HARRISON, Richard, John , SUNOSE, Mihiro , HERNANDEZ-Perni, Remedios , MAJOR, Jeremy , BOUSSARD, Cyrille , SMELT, Kathryn , TAYLOR, Jess , LEFORMAL, Adeline , CANSFIELD, Andrew , BURCKHARDT, Svenja
IPC分类号： C07C59/68 , C07C59/72 , C07D295/22 , C07D261/08 , C07D309/06 , C07D295/18 , C07C235/34 , C07C311/17 , C07C317/22 , A61P25/28 , A61K31/192
CPC分类号： C07C59/68 , C07C59/72 , C07C233/54 , C07C235/42 , C07C311/29 , C07C317/22 , C07C317/46 , C07C2601/02 , C07C2601/14 , C07D261/08 , C07D295/192 , C07D295/26 , C07D309/06
摘要： The present invention relates to compounds having the general formula (I) with the definitions of A, X, R 1 -R 6 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of γ-secretase activity.
摘要翻译：本发明涉及具有通式（I）的化合物，其具有以下给出的A，X，R 1〜R 6〜6的定义，和/或盐或酯它们。此外，本发明涉及所述化合物用于治疗阿尔茨海默氏病及其用于调节γ-分泌酶活性的用途。

9. 发明申请

WO2003059885A1 THERAPEUTIC ACRIDONE AND ACRIDINE COMPOUNDS 审中-公开
标题翻译：治疗阿司匹林和阿司匹林化合物
公开(公告)号：WO2003059885A1
公开(公告)日：2003-07-24
申请号：PCT/GB2003/000102
申请日：2003-01-14
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , NEIDLE, Stephen , HARRISON, Richard, John , KELLAND, Lloyd, Royston , GOWAN, Sharon, Michele , READ, Martin, Anthony , RESZKA, Anthony
发明人： NEIDLE, Stephen , HARRISON, Richard, John , KELLAND, Lloyd, Royston , GOWAN, Sharon, Michele , READ, Martin, Anthony , RESZKA, Anthony
IPC分类号： C07D219/08
CPC分类号： C07D219/08 , C07D219/10
摘要： This invention pertains to certain acridone and acridine compounds of the formula (1) which inhibit telomerase, regulate cell proliferation, etc., and/or treat cancer, proliferative conditions, etc.: wherein either: (a) K is =O, L is -H, alpha single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: J 1 is a 2- or 3-substituent; J 2 is a 6- or 7-substituent; J 1 and J 2 are each a group of the formula -N(R N )-W, wherein: R N is a nitrogen substituent and is hydrogen, C 1-7 alkyl, C 3-20 heterocyclyl, or C 5-20 aryl, and is optionally substituted; and, W is C 1-7 alkyl, C 3-20 heterocyclyl, or C 5-20 aryl, and is optionally substituted; and, wherein, when K is a 9-substituent, K is a group of the formula -N(R N )-Q, wherein: R N is an amino substituent and is hydrogen, C 1-7 alkyl, C 3-20 heterocyclyl, or C 5-20 aryl; and, Q is C 1-7 alkyl, C 3-20 heterocyclyl, or C 5-20 aryl, and is optionally substituted; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms thereof. 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 telomerase, to regulate cell proliferation, etc., and/or in the treatment of cancer, proliferative conditions, etc.
摘要翻译：本发明涉及抑制端粒酶，调节细胞增殖等，和/或治疗癌症，增殖病症等的式（1）的某些吖啶酮和吖啶化合物，其中：（a）K = O，L 是-H，α单键，β是双键，γ是单键（吖啶酮）; 或（b）K是9取代基，L不存在，α是双键，β是单键，γ是双键（吖啶）; 并且其中：J 1是2-或3-取代基; J 2是6-或7-取代基; J 1和J 2各自是式-N（R N）-W的基团，其中：R N是氮取代基，并且是氢，C 1-7烷基，C 3-20杂环基或 C5-20芳基，并且任选被取代; 并且W是C 1-7烷基，C 3-20杂环基或C 5-20芳基，并且任选被取代; 并且其中，当K为9-取代基时，K为式-N（R N）-Q的基团，其中：R N为氨基取代基，为氢，C 1-7烷基， 20杂环基或C5-20芳基; 且Q为C 1-7烷基，C 3-20杂环基或C 5-20芳基，并且任选被取代; 和其药学上可接受的盐，酯，酰胺，溶剂合物，水合物及其保护形式。本发明还涉及包含这种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，以抑制端粒酶，调节细胞增殖等，和/或治疗癌症，增殖性条件等

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