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1. 发明授权

US11884656B2 Pyrrole derivatives as PLK1 inhibitors 有权
公开(公告)号：US11884656B2
公开(公告)日：2024-01-30
申请号：US17453959
申请日：2021-11-08
申请人： SENTINEL ONCOLOGY LIMITED
发明人： Robert George Boyle , David Winter Walker , Richard Justin Boyce
IPC分类号： C07D413/14 , C07D207/32 , C07D231/12 , C07D261/08 , C07D401/04 , C07D403/10 , C07D405/14 , C07D409/04 , A61P35/00 , C07D207/325 , C07D401/14 , C07D403/12 , C07D413/12
CPC分类号： C07D413/14 , A61P35/00 , C07D207/325 , C07D231/12 , C07D261/08 , C07D401/04 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/14 , C07D409/04 , C07D413/12
摘要： The invention provides compounds of the formula (3):

or a pharmaceutically acceptable salt or tautomer thereof, wherein:
Z is a 5-membered heteroaryl ring containing one or two nitrogen ring members and optionally one further heteroatom ring member selected from N and O;
ring X is a benzene or pyridine ring;
ring Y is a benzene, pyridine, thiophene or furan ring;
Ar1 is an optionally substituted benzene, pyridine, thiophene or furan ring;
m is 0, 1 or 2;
n is 0, 1 or 2;
R1 is selected from various substituents:
R2 is selected from hydrogen and a C1-4 hydrocarbon group;
R3 is selected from hydrogen and a C1-4 hydrocarbon group;
R4 is selected from various substituents;
R5 is selected from various substituents;
Ar2 is an optionally substituted phenyl, pyridyl or pyridone group;
R6 is a group Q1-Ra—Rb;
Q1 is absent or is a C1-3 saturated hydrocarbon linker;
Ra is selected from O; C(O); C(O)O; CONRc; N(Rc)CO; N(Rc)CONRc, NRc; and SO2NRc;
Rb is selected from hydrogen and various substituents;
and Rb is selected from R4.

The compounds are useful in the treatment of cancers.

2. 发明授权

US10730882B2 2-aminoquinazoline derivatives as P70S6 kinase inhibitors 有权
公开(公告)号：US10730882B2
公开(公告)日：2020-08-04
申请号：US16442071
申请日：2019-06-14
申请人： SENTINEL ONCOLOGY LIMITED
发明人： Robert George Boyle , David Winter Walker
IPC分类号： C07D487/04 , C07D403/04 , A61P25/28 , A61P35/04
摘要： The invention provides compound that inhibit or modulate the activity of p70S6 kinase, the compounds being of the formula (1): or a salt, tautomer or N-oxide thereof; wherein: one of Y and Z is R3 and the other is Ar2; Q1 is an optionally substituted C1-8 alkylene group; and wherein a carbon atom of the C1-8 alkylene group may optionally be replaced by a cyclopropane-1,1-diyl or cyclobutane-1,1-diyl group provided that the total number of carbon atoms in an alkylene group containing such a replacement does not exceed 8; Q2 is a bond or an optionally substituted C1-8 alkylene group R1 is selected from hydrogen, NRxRy and a group Cy1; Rx and Ry are each is selected from hydrogen, C1-4 hydrocarbyl or hydroxy-C1-4 hydrocarbyl; or NRxRy forms an optionally substituted 4 to 7-membered heterocyclic ring; Cy1 is an optionally substituted C-linked 3 to 7 membered monocyclic non-aromatic carbocyclic or heterocyclic; R2 and R4 are each is selected from hydrogen, fluorine, chlorine, optionally substituted C1-2 alkyl and optionally substituted C1-2 alkoxy; R3 is selected from hydrogen, fluorine, chlorine, optionally substituted C1-2 alkyl and optionally substituted C1-2 alkoxy; Ar1 is an optionally substituted monocyclic 5 or 6-membered aryl or heteroaryl ring; and Ar2 is an optionally substituted bicyclic 8 to 11-membered heteroaryl group. The compounds are useful in medicine, for example in the treatment of a disease or condition selected from cancers, neurodevelopmental diseases and neurodegenerative diseases.

3. 发明申请

US20130065900A1 PHARMACEUTICAL COMPOUNDS 有权
标题翻译：药物化合物
公开(公告)号：US20130065900A1
公开(公告)日：2013-03-14
申请号：US13697743
申请日：2011-05-12
申请人： Robert George Boyle , David Winter Walker , Richard Justin Boyce
发明人： Robert George Boyle , David Winter Walker , Richard Justin Boyce
IPC分类号： A61K31/5377 , C07D241/26 , C07D405/12 , C07D403/12 , A61K31/4965 , A61N5/10 , C07D413/12 , C07D413/02 , A61K31/497 , C07D403/02
CPC分类号： C07D241/26 , A61K31/4965 , A61K31/497 , A61K31/5377 , A61N5/10 , C07D241/20 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The invention provides a compound of the formula (1): or a salt, N-oxide or tautomer thereof; wherein R1 is cyano or C1-4 alkyl; R2 is hydrogen or C1-4 alkyl; R3 is hydrogen or C1-4 alkyl; R4 and R5 are the same or different and each is selected from hydrogen, saturated C1-4 hydrocarbyl and saturated C1-4 hydrocarbyloxy; R6 and R7 are the same or different and each is selected from hydrogen, halogen, CN, C1-4 alkyl and C1-4 alkoxy wherein the C1-4 alkyl and C1-4 alkoxy are each optionally substituted with hydroxy, C1-2 alkoxy or by one or more flourine atoms; R8 is hydrogen or C1-4 alkyl; Q is an alkylene chain of 1 to 4 carbon atoms in length between the moiety Ar and the nitrogen atom N, wherein one or more of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with one or two C1-4 alkyl groups, or wherein one carbon atom of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with a group —CH2CH2— which together with the said one carbon atom forms a cyclopropyl group; m is 1, 2, 3 or 4; n is 0 or 1; and Ar is a monocyclic or bicyclic aryl or heteroaryl group of 5 to 10 ring members containing 0, 1, 2, 3 or 4 heteroatom ring members selected from O, N and S, the aryl or heteroaryl group being optionally substituted with one to four substituents R13 as defined in the claims.The compounds are inhibitors of Chk-1 kinase and are active against cancers.
摘要翻译：本发明提供式（1）化合物或其盐，N-氧化物或其互变异构体; 其中R1是氰基或C1-4烷基; R2是氢或C1-4烷基; R3是氢或C1-4烷基; R4和R5相同或不同，各自选自氢，饱和C 1-4烃基和饱和C 1-4烃氧基; R 6和R 7相同或不同，各自选自氢，卤素，CN，C 1-4烷基和C 1-4烷氧基，其中C 1-4烷基和C 1-4烷氧基各自任选被羟基，C 1-2烷氧基或通过一个或多个荧光原子; R8是氢或C1-4烷基; Q是部分Ar和氮原子N之间的长度为1至4个碳原子的亚烷基链，其中亚烷基链的1至4个碳原子中的一个或多个可以任选被一个或两个C 1-4烷基取代基团，或其中亚烷基链的1至4个碳原子的一个碳原子可以任选被基团-CH 2 CH 2取代，所述基团与所述一个碳原子一起形成环丙基; m为1,2,3或4; n为0或1; 并且Ar是具有0至1个，2个，3个或4个选自O，N和S的杂原子环成员的5至10个环成员的单环或双环芳基或杂芳基，芳基或杂芳基任选被一至四个取代基R 13如权利要求中所定义。这些化合物是Chk-1激酶的抑制剂并且对癌症有活性。

4. 发明申请

US20110130394A1 PHARMACEUTICAL COMPOUNDS 有权
标题翻译：药物化合物
公开(公告)号：US20110130394A1
公开(公告)日：2011-06-02
申请号：US13003945
申请日：2009-07-15
申请人： Robert George Boyle , David Winter Walker
发明人： Robert George Boyle , David Winter Walker
IPC分类号： A61K31/541 , C07D401/14 , A61K31/4725 , A61K31/496 , C07D413/14 , A61K31/5377 , C07D417/14 , A61P35/00
CPC分类号： C07D401/12 , C07D401/14
摘要： The invention provides kinase inhibitor compounds of the formula (1): or salts, solvates, tautomers or N-oxides thereof; wherein X is O, CO, X1C(X2), C(X2)X1, X1C(X2)X1, S, SO, SO2, NRc, SO2NRc or NRcSO2; m is 0-2; n is 0-1; q is 0-2; A is C1-6 alkylene optionally interrupted by O; R1 is halogen, cyano, nitro, an optionally substituted acyclic C1-6 hydrocarbon group, optionally substituted C3-7 cycloalkyl, optionally substituted phenyl, optionally substituted five membered heteroaryl, NR2R3, Ra—Rb, O—Rb or C(O)NR2R8; R4 is fluorine, chlorine, methyl or cyano; R2 is hydrogen or optionally substituted C1-4 alkyl; R3 is Ra—Rb; or NR2R3 forms a 4 to 7 membered non-aromatic heterocyclic ring; Ra is a bond, C(X2), C(X2)X1, SO, SO2 or SO2NRc; Rb is hydrogen or an optionally substituted 3 to 7-membered carbocyclic or heterocyclic ring or an optionally substituted C1-12 acyclic hydrocarbon group; Rc is hydrogen or a C1-4 hydrocarbon group; Rd is O, CO, X1C(X2), C(X2)X1, X1C(X2)X1, S, SO, SO2, NRc, SO2NRc or NRcSO2; X1 is O, S or NRc; X2 is ═O, ═S or ═NRc; but excluding the compound wherein m, n and q are all 0, A is CH2 and NR2R3 is a 2-phenylmorpholin-4-yl group.
摘要翻译：本发明提供式（1）的激酶抑制剂化合物：或其盐，溶剂合物，互变异构体或N-氧化物; 其中X是O，CO，X1C（X2），C（X2）X1，X1C（X2）X1，S，SO，SO2，NRc，SO2NRc或NRcSO2; m为0-2; n为0-1; q为0-2; A是任选被O中断的C 1-6亚烷基; R 1为卤素，氰基，硝基，任选取代的无环C 1-6烃基，任选取代的C 3-7环烷基，任选取代的苯基，任选取代的五元杂芳基，NR2R3，Ra-Rb，O-Rb或C（O）NR2R8 ; R4是氟，氯，甲基或氰基; R2是氢或任选取代的C 1-4烷基; R3是Ra-Rb; 或NR 2 R 3形成4至7元非芳族杂环; R a是键，C（X 2），C（X 2）X 1，SO，SO 2或SO 2 NR c; Rb是氢或任选取代的3至7元碳环或杂环或任选取代的C1-12无环烃基; Rc是氢或C 1-4烃基; Rd为O，CO，X1C（X2），C（X2）X1，X1C（X2）X1，S，SO，SO2，NRc，SO2NRc或NRcSO2; X1是O，S或NRc; X2为═O，═S或= NRR; 但不包括m，n和q全部为0的化合物，A为CH 2且NR 2 R 3为2-苯基吗啉-4-基。

5. 发明公开

US20240140908A1 A PHARMACEUTICAL SALT OF AN ARYLPYRROLE DERIVATIVE 审中-公开
公开(公告)号：US20240140908A1
公开(公告)日：2024-05-02
申请号：US18245999
申请日：2021-09-23
申请人： SENTINEL ONCOLOGY LIMITED
发明人： Meriel Ruth MAJOR , Robert George BOYLE , Stuart TRAVERS , David Winter WALKER , Julian Scott NORTHEN , Stefania SANTONI
IPC分类号： C07D207/337 , A61P35/00 , C07C59/255
CPC分类号： C07D207/337 , A61P35/00 , C07C59/255 , C07B2200/07 , C07B2200/13
摘要： The present invention relates to (R)-4-[5-(4-chlorophenyl)-1-[2-(trifluoromethyl)-phenyl]pyrrol-2-yl]-N-[2-(dimethylamino)-ethyl]benzamide (+)-L-tartrate salt, methods for its preparation, pharmaceutical compositions containing it and its use in treating diseases such as cancer.

6. 发明申请

US20220348565A1 PHARMACEUTICAL COMPOUNDS 有权
公开(公告)号：US20220348565A1
公开(公告)日：2022-11-03
申请号：US17754200
申请日：2020-09-25
申请人： SENTINEL ONCOLOGY LIMITED
发明人： Robert George BOYLE , Meriel Ruth MAJOR , Stuart TRAVERS , David Winter WALKER , Michal CZYZEWSKI , Derek John LONDESBROUGH , Julian Scott NORTHEN , Stefania SANTONI
IPC分类号： C07D413/02 , C07D403/02 , A61P35/00
摘要： The invention provides a composition of matter which:
(i) consists of at least 90% by weight of an atropisomer (2A) and 0-10% by weight of an atropisomer of formula (2B); or (ii) consists of at least 90% by weight of an atropisomer (2B) and 0-10% by weight of an atropisomer of formula (2A); wherein the atropisomer of formula (2A) and the atropisomer of formula (2B) are represented by: or are pharmaceutically acceptable salts or tautomers thereof, wherein ring X is a benzene or pyridine ring; ring Y is selected from a benzene ring, a pyridine ring and a thiophene ring; R1 is trifluoromethyl; R2 is hydrogen; R3 is hydrogen; m is 0 or 1; n is 0, 1 or 2; Ar1 is a monocyclic aromatic ring selected from benzene and pyridine; each monocyclic aromatic ring being unsubstituted or substituted with 1 or 2 substituents R5 as defined herein; and R4; R5 when present, R6 and R7 independently selected from various substituents as defined herein.
Also provided are individual atropisomers, pharmaceutical compositions and the uses of the atropisomers and compositions are inhibitors of PLK1- and PLK4 kinases, for example in the treatment of cancers.

7. 发明申请

US20210275525A1 PHARMACEUTICAL COMPOUNDS 有权
公开(公告)号：US20210275525A1
公开(公告)日：2021-09-09
申请号：US17191151
申请日：2021-03-03
申请人： SENTINEL ONCOLOGY LIMITED
发明人： Robert George BOYLE , David Winter WALKER , Richard Justin BOYCE , Scott PETERSON , Francine FAROUZ , Cong Hung VO
IPC分类号： A61K31/497 , C07D403/12 , A61K45/06 , A61K31/4155 , C07D401/14 , C07D405/14 , C07D413/14 , C07D403/14 , A61K31/454 , A61K31/5377 , A61K31/551 , C07D401/10
摘要： This invention relates to compounds that inhibit or modulate the activity of Chk-1 kinase. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds.

8. 发明申请

US20190292195A1 2-AMINOQUINAZOLINE DERIVATIVES AS P70S6 KINASE INHIBITORS 审中-公开
公开(公告)号：US20190292195A1
公开(公告)日：2019-09-26
申请号：US16442071
申请日：2019-06-14
申请人： SENTINEL ONCOLOGY LIMITED
发明人： Robert George BOYLE , David Winter WALKER
IPC分类号： C07D487/04 , A61P35/04 , C07D403/04 , A61P25/28
摘要： The invention provides compound that inhibit or modulate the activity of p70S6 kinase, the compounds being of the formula (1): or a salt, tautomer or N-oxide thereof; wherein: one of Y and Z is R3 and the other is Ar2; Q1 is an optionally substituted C1-8 alkylene group; and wherein a carbon atom of the C1-8 alkylene group may optionally be replaced by a cyclopropane-1,1-diyl or cyclobutane-1,1-diyl group provided that the total number of carbon atoms in an alkylene group containing such a replacement does not exceed 8; Q2 is a bond or an optionally substituted C1-8 alkylene group R1 is selected from hydrogen, NRxRy and a group Cy1; Rx and Ry are each is selected from hydrogen, C1-4 hydrocarbyl or hydroxy-C1-4 hydrocarbyl; or NRxRy forms an optionally substituted 4 to 7-membered heterocyclic ring; Cy1 is an optionally substituted C-linked 3 to 7 membered monocyclic non-aromatic carbocyclic or heterocyclic; R2 and R4 are each is selected from hydrogen, fluorine, chlorine, optionally substituted C1-2 alkyl and optionally substituted C1-2 alkoxy; R3 is selected from hydrogen, fluorine, chlorine, optionally substituted C1-2 alkyl and optionally substituted C1-2 alkoxy; Ar1 is an optionally substituted monocyclic 5 or 6-membered aryl or heteroaryl ring; and Ar2 is an optionally substituted bicyclic 8 to 11-membered heteroaryl group. The compounds are useful in medicine, for example in the treatment of a disease or condition selected from cancers, neurodevelopmental diseases and neurodegenerative diseases.

9. 发明授权

US10144726B2 Modulators of the p70S6 kinase for use in the treatment of brain disorders and triple-negative breast cancer 有权
公开(公告)号：US10144726B2
公开(公告)日：2018-12-04
申请号：US15549599
申请日：2016-02-15
申请人： SENTINEL ONCOLOGY LIMITED
发明人： Robert George Boyle , David Winter Walker
IPC分类号： A61K31/53 , A61K31/498 , A61P35/04 , C07D403/12 , C07D403/04
摘要： The invention provides compounds for use in the treatment of a disease or condition selected from brain disorders and triple-negative breast cancer, the compounds being of the formula (1): or a salt or tautomer thereof; wherein: X1 is N or N+(O−); X2 is N or CH; Q is selected from a C1-3 alkylene group, cyclopropane-1,1-diyl and cyclobutane-1,1-diyl; R1 is selected from hydrogen and C1-4 alkyl; R2, R3 and R4 are the same or different and each is selected from hydrogen and fluorine; Ar1 is a benzene, thiophene, naphthyl or pyridine ring optionally substituted with 1, 2 or 3 substituents selected from fluorine; chlorine; bromine; C1-4 hydrocarbyl; C1-4 hydrocarbyloxy; trifluoromethyl; difluoromethyl; cyano; trifluoromethoxy; difluoromethoxy; Ar2 is a monocyclic 5- or 6-membered heteroaryl ring containing 1, 2 or 3 heteroatom ring members selected from O, N and S and being optionally substituted with 1, 2 or 3 substituents selected from fluorine; C1-4 hydrocarbyl; amino; mono-C1-4 hydrocarbylamino and di-C1-4 hydrocarbylamino; and wherein, in each substituent consisting of or containing C1-4 hydrocarbyl, the C1-4 hydrocarbyl is selected from C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, cyclopropyl, cyclobutyl and cyclopropylmethyl.

10. 发明申请

US20100048540A1 Heterocyclic N-Oxides as Hypoxic Selective Protein Kinase Inhibitors 审中-公开
标题翻译：杂环型N-氧化物作为缺氧选择性蛋白激酶抑制剂
公开(公告)号：US20100048540A1
公开(公告)日：2010-02-25
申请号：US11815168
申请日：2006-02-01
申请人： Robert George Boyle , Stuart Travers
发明人： Robert George Boyle , Stuart Travers
IPC分类号： A61K31/551 , C07D413/10 , C07D471/04 , C07D243/08 , C07D215/40 , A61K31/5377 , A61K31/498 , A61K31/4709 , A61P35/00
CPC分类号： C07D239/76 , C07D215/48 , C07D215/60 , C07D239/94 , C07D241/20 , C07D241/54 , C07D253/07 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D471/04 , C07D487/04
摘要： The invention relates to novel heterocyclic N-oxides which are useful as hypoxic selective cytotoxic agents that mediate and/or inhibit cell proliferation, for example, through the activity of protein kinases. The invention is further related to pharmaceutical compositions containing such compounds and compositions, and to methods of treating cancer as well as other disease states associated with unwanted ahgiogenesis and/or cellular proliferation by administering effective amounts of such compounds.
摘要翻译：本发明涉及可用作介导和/或抑制细胞增殖的缺氧选择性细胞毒性剂的新型杂环N-氧化物，例如通过蛋白激酶的活性。本发明进一步涉及含有这些化合物和组合物的药物组合物，以及通过施用有效量的这种化合物治疗癌症以及与不想要的发生和/或细胞增殖相关的其它疾病状态的方法。

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