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1. 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。

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

WO2004065389A1 PYRROLOPYRIMIDINE DERIVATIVES USEFUL AS MODULATORS OF MULTIDRUG RESISTANCE 审中-公开
标题翻译：用作多抗电荷调节剂的吡咯烷酮衍生物
公开(公告)号：WO2004065389A1
公开(公告)日：2004-08-05
申请号：PCT/GB2004/000274
申请日：2004-01-23
申请人： XENOVA LIMITED , MILTON, John , WREN, Stephen , WANG, Shouming , FOLKES, Adrian , CHUCKOWREE, Irina , HANCOX, Timothy , MILLER, Warren , SOHAL, Sukhjit
发明人： MILTON, John , WREN, Stephen , WANG, Shouming , FOLKES, Adrian , CHUCKOWREE, Irina , HANCOX, Timothy , MILLER, Warren , SOHAL, Sukhjit
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A compound which is a pyrrolopyrimidine of formula (I) wherein: R 1 is selected from R 9 and halogen; R 2 is NR 6 R 7 ; R 3 is selected from H, C 1 -C 6 alkyl which is unsubstituted or substituted and -(CH2) n Ar; R 4 is selected from H, C 1 -C 6 alkyl and -(CH 2 )„ Ar; or R 3 and R 4 form, together with the N and C atoms to which they are attached, a fused five-, six-, seven- or eight-membered N-containing saturated ring which is unsubstituted or substituted; R 5 is selected from CN, C0 2 R 9 , C(O)NR 10 R 11 , -(CH 2 ) n OH, -(CH 2 ) n R 10 R n , -C = CH, -C(S)NR 10 R 11 , -C(NH 2 )=NOR 9 , -C(R 9 )=NOR 9 , -C(NH 2 )NH, -C(O)R 9 and an unsaturated 5- or 6-membered heterocyclic group which contains 1, 2 or 3 heteroatoms selected from N, O and S and which is unsubstituted or substituted; R 6 and R 7 , which are the same or different, are selected from C 1 -C 6 alkyl which is unsubstituted or substituted, -(CH 2 ) n X and -(CH 2 ) n Ar; or R 6 and R 7 form, together with the nitrogen atom to which they are attached, a saturated five-, six-, seven- or eight-membered heterocyclic group which contains one nitrogen atom and 0 or from 1 to 3 additional heteroatoms selected from N, O and S, which is unsubstituted or substituted and which optionally contains one or two bridgehead atoms; R 10 and R 11 , which are the same or different, are selected from H, C 1 -C 6 alkyl which is unsubstituted or substituted, -(CH 2 ) n C 3 -C 10 cycloalkyl and -(CH 2 ) n Ar; or R 10 and R 11 form, together with the nitrogen atom to which they are attached, a saturated five or six membered heterocyclic group which contains a nitrogen atom and 0 or from to 3 additional heteroatoms selected from O, S and N, which is unsubstituted or substituted and which is optionally fused to a benzene ring which is unsubstituted or substituted; n is the same or different when more than one is present within a given substituent group and is 0 or an integer of from 1 to 6; X is selected from -CN, -C0 2 R 9 and -NR 10 R 11 ; R 9 is the same or different when more than one is present within a given substituent group and is selected from -H, -QAr, -(CH 2 ) n Ar, C 1 -C 6 alkyl which is unsubstituted or substituted and -(CH 2 ) n C 3 -C 10 cycloalkyl, wherein the cycloalkyl moiety is optionally fused to a benzene ring which is unsubstituted or substituted; Q is C 2 -C 6 alkenylene or alkynylene; and Ar is an unsaturated C 6 -C 10 membered carbocyclic group or an unsaturated 5-11 membered heterocyclic group, which groups are unsubstituted or substituted; or a pharmaceutically acceptable salt thereof. These compounds have activity as inhibitors of MRP (multidrug resistant protein) and may thus be used to modulate multidrug resistance, for instance in potentiating the cytotoxicity of a chemotherapeutic agent.
摘要翻译：化合物，其是式（I）的吡咯并嘧啶，其中：R 1选自R 9和卤素; R 2是NR 6 R 7; R 3选自H，未取代或取代的C 1 -C 6烷基和 - （CH 2）n Ar; R 4选自H，C 1 -C 6烷基和 - （CH 2）“Ar;或R 3和R 4形式，与它们所连接的N和C原子一起，未取代或取代的六元，七元或八元的含N饱和环; R 5选自CN，CO 2 R 9，C（O）NR 10 R 11， - （ CH 2）n OH， - （CH 2）n R 10 R n，-C = CH，-C（S）NR 10 R 11，-C（NH 2）= NOR 9，-C（ R 9）= NOR 9，-C（NH 2）NH，-C（O）R 9和不饱和的5-或6-元杂环基，其含有1,2或3个选自N， O和S是未取代或取代的; R 6和R 7相同或不同，选自未取代或取代的C 1 -C 6烷基， - （CH 2）n X和 - （CH 2） nAr;或R 6和R 7与它们所连接的氮原子一起形成饱和的五元，六元，七元或八元杂环基，其含有一个氮原子且为0或从 1至3个选自N，O和S的杂原子，其是未取代的或取代的并且其任选地包含一个或两个桥头原子; R 10和R 11相同或不同，选自H，未取代或取代的C 1 -C 6烷基， - （CH 2）n C 3 -C 10环烷基和 - （CH 2）n Ar; 或R 10和R 11与它们所连接的氮原子一起形成饱和的五或六元杂环基，其含有氮原子和0或至少3个选自O，S的另外的杂原子， N是未取代或取代的，并且任选地与未被取代或取代的苯环稠合; 当给定的取代基中存在多于一个时，n相同或不同，为0或1-6的整数; X选自-CN，-CO 2 R 9和-NR 10 R 11; R 9在给定的取代基中存在多于一个且选自-H，-QAr， - （CH 2）nAr，未取代或取代的C 1 -C 6烷基和 - （CH 2） nC 3 -C 10环烷基，其中环烷基部分任选地与未被取代或取代的苯环稠合; Q是C 2 -C 6亚烯基或亚炔基; 和Ar是不饱和的C 6 -C 10的碳环基团或不饱和的5-11元杂环基团，这些基团是未取代的或取代的; 或其药学上可接受的盐。这些化合物具有作为MRP（多药耐药蛋白）的抑制剂的活性

5. 发明申请

WO2004111052A1 PYRROLOPYRIMIDINE DERIVATIVES AS MODULATORS OF MULTI-DRUG RESISTANCE (MDR) 审中-公开
标题翻译：作为多药耐药（MDR）的调节剂的吡咯烷酮衍生物
公开(公告)号：WO2004111052A1
公开(公告)日：2004-12-23
申请号：PCT/GB2004/002523
申请日：2004-06-11
申请人： XENOVA LIMITED , WANG, Shouming , HANCOX, Timothy , MILLER, Warren , HARRISON, John , CHUCKOWREE, Irina , BAKER, Stewart , FOLKES, Adrian , WAN, Nan, Chi
发明人： WANG, Shouming , HANCOX, Timothy , MILLER, Warren , HARRISON, John , CHUCKOWREE, Irina , BAKER, Stewart , FOLKES, Adrian , WAN, Nan, Chi
IPC分类号： C07D487/04
CPC分类号： C07D471/14 , C07D487/04
摘要： A compound which is a pyrrolopyrimidine of formula (I) wherein R 1 is selected from H, C l -C 6 alkyl which is unsubstituted or substituted, (CH 2 ) n Ar 1 , (CH 2 ) p NR 4 R 5 , halogen and (CH 2 ) p X; R 2 is CH 2 ) p Ar l ; R 3 is selected from H, C l -C 6 alkyl which is unsubstituted or substituted, (CH 2 ) p Z and (CH 2 ) p Ar l ; P is an unsaturated 5, 6, or 7 membered carbocyclic or heterocyclic ring which is unsubstituted or substituted; R 4 and R 5 which are the same or different are selected from H, C l -C 6 alkyl which is unsubstituted or substituted, (CH 2 ) n C 3 -C 10 cycloalkyl, (CH 2 ) n Ar 1 , and (CH 2 ) n OR 6 , or R 4 and R 5 together with the nitrogen atom to which they are attached, form a saturated five or six membered nitrogen containing heterocyclic ring which may contain one extra heteroatom selected from 0, N and S and which is unsubstituted or substituted; R 6 is selected from H, C l -C 6 alkyl which is unsubstituted or substituted, C 3 -C 10 cycloalkyl, (CH 2 ) n OC 1 -C 6 alkyl which is unsubstituted or substituted, (CH 2 ) n O(CH 2 ) n Ar 1 , (CH 2 ) n CO 2 C 1 -C 6 ,alkyl which is unsubstituted or substituted and (CH 2 ) n Ar 1 ; X is selected from CN, azide, (CH 2 ) n NHSO 2 R 6 and (CH 2 ) n NHCOR 6 ; Z is selected from CN, CO 2 R 6 and CONR 4 R 5 ; Ar 1 is the same or different when more than one is present within a given substituent group and is an unsaturated C 6 -C 10 membered carbocylic group or an unsaturated 5-11 membered heterocycle, either of which is unsubstituted or substituted; p is an integer of 1 to 6; n is the same or different when more than one is present within a given substituent group and is 0 or an integer of 1 to 6; with the proviso that the pyrrolepyrimidine compound of formula (I) is other than 1-(4-benzyl-piperazin-1-yl)-9H-2,4,9-triaza-fluorene; and the pharmaceutically acceptable salts thereof, have activity as inhibitors of MRP (multidrug resistant protein) and may thus be used to modulate multidrug resistance, for instance in potentiating the cytotoxicity of a chemotherapeutic agent.
摘要翻译：化合物，其是式（I）的吡咯并嘧啶，其中R 1选自H，未取代或取代的C 1 -C 6烷基，（CH 2）n Ar 1，（CH 2）p NRR 5 R 5，，卤素和（CH 2）pX; R 2是CH 2）pAr 1; R 3选自H，未被取代或取代的C 1 -C 6烷基，（CH 2）pZ和（CH 2）p Ar 1; P是未取代或取代的不饱和5,6或7元碳环或杂环; （CH 2）n C 3 -C 10环烷基，（CH 2）n Ar 1和（CH 2）n C 3 -C 10环烷基，C 1 -C 4烷基， nOR 6或R 4和R 5与它们所连接的氮原子一起形成饱和的五或六元含氮杂环，其可含有一个选自0，N和S的杂原子并且其是未取代或取代的; R 6选自未取代或取代的C 1 -C 6烷基，C 3 -C 10环烷基，未取代或取代的（CH 2）n O（CH 2）n Ar 1（CH 2）n OC 1 -C 6烷基，）nCO2C1-C6，未取代或取代的烷基和（CH2）nAr 1; X选自CN，叠氮化物，（CH 2）n NHSO 2 R 6和（CH 2）n NHCOR 6; Z选自CN，CO 2 R 6和CONR 4 R 5; 当在给定的取代基中存在多于一个时，Ar 1是相同或不同的，并且是不饱和的C 6 -C 10元碳环基或不饱和5-11元杂环，其中任一个是未取代的或取代的; p为1〜6的整数。当给定取代基中存在多于一个时，n相同或不同，为0或1〜6的整数; 条件是式（I）的吡咯嘧啶化合物不是1-（4-苄基 - 哌嗪-1-基）-9H- 2,4,9-三氮杂芴; 和其药学上可接受的盐具有作为MRP（多药耐药性蛋白）的抑制剂的活性，因此可用于调节多药耐药性，例如增强化学治疗剂的细胞毒性。

6. 发明公开

EP2566867A1 PYRAZOLE COMPOUNDS AS JAK INHIBITORS 审中-公开
标题翻译：吡唑，JAK抑制剂
公开(公告)号：EP2566867A1
公开(公告)日：2013-03-13
申请号：EP11714581.3
申请日：2011-04-18
申请人： Cellzome Limited
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.

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