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1. 发明申请

WO2006067466A3 PYRAZINES AND PYRIDINES AND DERIVATIVES THEREOF AS THERAPEUTIC COMPOUNDS 审中-公开
标题翻译：作为治疗化合物的吡咯并吡啶及其衍生物
公开(公告)号：WO2006067466A3
公开(公告)日：2007-07-05
申请号：PCT/GB2005005011
申请日：2005-12-22
申请人： WELLCOME TRUST LTD , SPRINGER CAROLINE JOY , NICULESCU-DUVAZ ION , ROMAN VELA ESTEBAN , GILL ADRIAN LIAM , TAYLOR RICHARD DAVID , MARAIS RICHARD MALCOLM
发明人： SPRINGER CAROLINE JOY , NICULESCU-DUVAZ ION , ROMAN VELA ESTEBAN , GILL ADRIAN LIAM , TAYLOR RICHARD DAVID , MARAIS RICHARD MALCOLM
IPC分类号： C07D241/20 , A61K31/444 , A61K31/497 , A61P35/00 , C07D213/74 , C07D317/46 , C07D319/18 , C07D321/10 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07D213/74 , C07D241/20 , C07D317/46 , C07D319/18 , C07D321/10 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention pertains to certain pyrazines and pyridines, and dervatives thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc., and more particularly to compounds of the formulae: (I) wherein: Q is independently -N= or -CH=; one of R P2 and R P3 is independently a group of the formula -J 1 -L 1 -Z; wherein: if Q is -N=, then -J 1 -L 1 -Z is independently: -NH-Z; -O-Z; or S-Z; if Q is -CH=, then -J 1 -L 1 -Z is independently: -NH-(CH 2 ) n -Z, wherein n is independently 0 or 1; -O-Z; or -S-Z; Z is independently: C 6-14 carboaryl, C 5-14 heteroaryl, C 3-12 carbocyclic, C 3-12 heterocyclic; and is independently unsubstituted or substituted; the other of R P2 and R P3 is independently -H, -NHR N1 , or -NHC(=O)R N2 ; wherein: R N1 , if present, is independently -H or aliphatic saturated C 1-4 alkyl; R N2 , if present, is independently -H or aliphatic saturated C 1-4 alkyl; one of R P5 and R P6 is independently a group of the formula -W-Y; wherein: W is independently: a covalent bond; -NR N4 -, -O-, -S-, -C(=O)-, -CH 2 -; -NR N4 -CH 2 -, -O-CH 2 -, -S-CH 2 -, -C(=O)-CH 2 -, -(CH 2 ) 2 -; -CH 2 -NR N4 -, -CH 2 -O-, -CH 2 -S-, or -CH 2 -C(=O)-; wherein R N4 , if present, is independently -H or aliphatic saturated C 1-4 alkyl; Y is independently: C 6-14 carboaryl, C 5-14 heteroaryl, C 3-12 carbocyclic, C 3-12 heterocyclic; and is independently unsubstituted or substituted; the other of R P5 and R P6 is independently -H; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, e.g., both in vitro and in vivo, to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc.
摘要翻译：本发明涉及某些吡嗪和吡啶及其衍生物，其特别是抑制RAF（例如，B RAF）活性，抑制细胞增殖，治疗癌症等，更具体地涉及下式的化合物：（I ）其中：Q独立地为-N =或-CH =; R“P2”和“R”中的一个独立地是式-I-1-L-1-Z的基团 ; 其中：如果Q是-N =，则-J 1 -L 1 -Z独立地是：-NH-Z; -O-Z; 或S-Z; 如果Q是-CH =，则-J 1 -L 1 -Z独立地是：-NH-（CH 2 CH 2） n -Z，其中n独立地为0或1; -O-Z; 或-S-Z; Z独立地为：C 6-14芳烷基，C 5-14杂芳基，C 3-12碳环，C 3-12 杂环; 并且独立地是未取代的或取代的; R 2 P2和R 3 P 2中的另一个独立地为-H，-NHR 1 N 1或-NHC（= O）R N 2 ; 其中：如果存在，R“独立地为-H或脂族饱和C 1-4烷基; 如果存在，则R 2独立地为-H或脂族饱和C 1-4烷基; R 5 P 5和R 6 P 6中的一个独立地是式-W-Y的基团; 其中：W独立地为：共价键; -NR N - ， - O - ， - S - ， - C（= O） - ， - CH 2 - 。 -NR N4 - CH 2 - ， - O-CH 2 - ， - S-CH 2 - ， - -C（= O）-CH 2 - ， - （CH 2）2 - ; - （CH 2）2 - -CH 2，-NR N 4 - ， - CH 2 -O - ， - CH 2 -S-，或-CH 2 -C（= O） - ; 其中R“N4”（如果存在）独立地是-H或脂族饱和C 1-4烷基; Y独立地为：C 6-14碳芳基，C 5-14杂芳基，C 3-12碳环，C 3-12 杂环基; 并且独立地是未取代的或取代的; R“P5”和“R”P6中的另一个独立地是-H; 酰胺，酯，醚，N-氧化物，化学保护形式及其前体药物。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两者抑制RAF（例如B-RAF）活性抑制受体酪氨酸激酶（RTK）的用途，活性，抑制细胞增殖，以及通过抑制RAF，RTK等改善增殖条件如癌症（例如结肠直肠癌，黑素瘤）等的疾病和病症的治疗。

2. 发明专利

CA2591208A1 PYRAZINES AND PYRIDINES AND DERIVATIVES THEREOF AS THERAPEUTIC COMPOUNDS 未知
公开(公告)号：CA2591208A1
公开(公告)日：2006-06-29
申请号：CA2591208
申请日：2005-12-22
申请人： WELLCOME TRUST LTD
发明人： MARAIS RICHARD MALCOLM , NICULESCU-DUVAZ ION , SPRINGER CAROLINE JOY , GILL ADRIAN LIAM , ROMAN VELA ESTEBAN , TAYLOR RICHARD DAVID
IPC分类号： C07D241/20 , A61K31/444 , A61K31/497 , A61P35/00 , C07D213/74 , C07D317/46 , C07D319/18 , C07D321/10 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention pertains to certain 6-carboaryloxy-pyrazin-2-yl-carboaryl-amines of the following formula, and pharmaceutically acceptable salts thereof, which, inter alia, inhibit RAF (e.g., B-RAF) activity, inhibit cell proliferation, treat cancer, etc., wherein Q is independently —N═; RP3 is independently a group of the formula -J1-L1-Z; -J1L1-Z is independently —NH—Z; Z is independently C6-14carboaryl and is independently unsubstituted or substituted; RP2 is independently —H; RP5 is independently a group of the formula —W—Y; W is independently —O—; Y is independently C6-14 carboaryl and is independently unsubstituted or substituted; and RP6 is independently —H. The present invention also pertains to pharmaceutical compositions comprising such compounds.

3. 发明专利

AU2005317890A1 Pyrazines and pyridines and derivatives thereof as therapeutic compounds 未知
公开(公告)号：AU2005317890A1
公开(公告)日：2006-06-29
申请号：AU2005317890
申请日：2005-12-22
申请人： THE WELLCOME TRUST LTD
发明人： SPRINGER CAROLINE JOY , MARAIS RICHARD MALCOLM , GILL ADRIAN LIAM , NICULESCU-DUVAZ ION , VELA ESTEBAN ROMAN , TAYLOR RICHARD DAVID
IPC分类号： C07D213/74 , C07D241/20 , C07D317/46 , C07D319/18 , C07D321/10 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention pertains to certain 6-carboaryloxy-pyrazin-2-yl-carboaryl-amines of the following formula, and pharmaceutically acceptable salts thereof, which, inter alia, inhibit RAF (e.g., B-RAF) activity, inhibit cell proliferation, treat cancer, etc., wherein Q is independently —N═; RP3 is independently a group of the formula -J1-L1-Z; -J1L1-Z is independently —NH—Z; Z is independently C6-14carboaryl and is independently unsubstituted or substituted; RP2 is independently —H; RP5 is independently a group of the formula —W—Y; W is independently —O—; Y is independently C6-14 carboaryl and is independently unsubstituted or substituted; and RP6 is independently —H. The present invention also pertains to pharmaceutical compositions comprising such compounds.

4. 发明专利

NZ556125A Pyrazine derivatives for inhibiting RAF activity 未知
公开(公告)号：NZ556125A
公开(公告)日：2010-12-24
申请号：NZ55612505
申请日：2005-12-22
申请人： WELLCOME TRUST LTD
发明人： SPRINGER CAROLINE JOY , NICULESCU-DUVAZ ION , ROMAN VELA ESTEBAN , GILL ADRIAN LIAM , TAYLOR RICHARD DAVID , MARAIS RICHARD MALCOLM
IPC分类号： C07D241/20 , A61K31/444 , A61K31/497 , A61P35/00 , C07D213/74 , C07D317/46 , C07D319/18 , C07D321/10 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Disclosed is an aminopyrazine derivative of formula (I), wherein W is -NRN4-, -O-, or -S-, RN4 is H or C1-4alkyl, Y is an optionally substituted carbocycle or heteroaryl, Z is optionally substituted phenyl, and wherein the optional substituents are as defined in the specification. Also disclosed by the specification are pyrazine and pyridine derivatives of formula (II), wherein Q is N or CH, and wherein the other substituents are as defined in the specification. Also disclosed is the use of any of the above compounds for inhbiting RAF activity and for treating conditions ameliorated by the inhibition of RAF, such as cancer, melanoma, or malignant melanoma.

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