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![IMMEDIATE RELEASE PHARMACEUTICAL FORMULATION OF 4-[3-(4-CYCLOPROPANECARBONYL-PIPERAZINE-1-CARBONYL)-4-FLUORO-BENZYL]-2H-PHTHALAZIN-1-ONE](/abs-image/US/2022/08/11/US20220249474A1/abs.jpg.150x150.jpg)
公开(公告)号：US20220249474A1
公开(公告)日：2022-08-11
申请号：US17483070
申请日：2021-09-23
发明人： Michael Karl Bechtold , Julie Kay Cahill , Katja Maren Fastnacht , Kieran James Lennon , Bernd Harald Liepold , Claudia Bettina Packhaeuser , Benedikt Steitz
摘要： The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.
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公开(公告)号：US20210244706A1
公开(公告)日：2021-08-12
申请号：US17035179
申请日：2020-09-28
IPC分类号： A61K31/366 , A61K31/00 , A61K31/405 , A61K31/4184 , A61K31/4706 , A61K31/473 , A61K31/502 , A61K31/517 , A61K31/522 , A61K31/675
摘要： The present invention relates to the recognition that inhibition of the base excision repair pathway is selectively lethal in cells which are deficient in HR dependent DNA DSB repair. Methods and means relating to the treatment of cancers which are deficient in HR dependent DNA DSB repair using inhibitors which target base excision repair components, such as PARP, is provided herein.
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公开(公告)号：US20170281637A1
公开(公告)日：2017-10-05
申请号：US15626282
申请日：2017-06-19
发明人： Heather Mary Ellen Duggan , Frederic Georges Marie Leroux , Karine Fabienne Malagu , Niall Morrison Barr Martin , Keith Menear , Graeme Cameron Murray Smith
IPC分类号： A61K31/5377 , C07D475/08 , C07D475/10 , C07D413/14 , A61K31/565 , C07D471/04 , A61K45/06
CPC分类号： A61K31/5377 , A61K31/565 , A61K45/06 , C07D413/14 , C07D471/04 , C07D475/08 , C07D475/10
摘要： There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
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公开(公告)号：US20170226124A1
公开(公告)日：2017-08-10
申请号：US15411101
申请日：2017-01-20
发明人： Niall Morrison Barr Martin , Graeme Cameron Smith , Stephen Philip Jackson , Vincent Junior M. Loh , Xiao-Ling Fan Cockcroft , Ian Timothy Williams Matthews , Keith Allan Menear , Frank Kerrigan , Alan Ashworth
IPC分类号： C07D495/04 , C07D243/08 , C07D405/12 , C07D417/14 , C07D417/12 , C07D403/12 , C07D401/12 , C07D409/12 , C07D237/32 , C07D413/12
CPC分类号： A61K31/502 , A61K31/00 , A61K31/506 , A61K31/5377 , A61K31/551 , A61K45/06 , A61N5/10 , C07D237/32 , C07D243/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D491/04 , C07D495/04
摘要： Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X=NRX then n is 1 or 2 and if X=CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.
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公开(公告)号：US20160000781A1
公开(公告)日：2016-01-07
申请号：US14853360
申请日：2015-09-14
发明人： Niall Morrison Barr Martin , Graeme Cameron Smith , Stephen Philip Jackson , Vincent Junior M Loh , Xiao-Ling Fan Cockcroft , Ian Timothy Williams Matthews , Keith Allan Menear , Frank Kerrigan , Alan Ashworth
IPC分类号： A61K31/502 , A61N5/10 , A61K31/5377 , A61K31/551 , A61K45/06 , A61K31/506
CPC分类号： A61K31/502 , A61K31/00 , A61K31/506 , A61K31/5377 , A61K31/551 , A61K45/06 , A61N5/10 , C07D237/32 , C07D243/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D491/04 , C07D495/04
摘要： Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X═NRX then n is 1 or 2 and if X═CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.
摘要翻译： 式（I）的化合物：其中A和B一起表示任选取代的稠合芳环; X可以是NRX或CRXRY; 如果X = NRX则n为1或2，如果X = CRXRY则n为1; RX选自H，任选取代的C 1-20烷基，C 5-20芳基，C 3-20杂环基，酰氨基，硫代酰氨基，酯，酰基和磺酰基; RY选自H，羟基，氨基; 或RX和RY可以一起形成螺C 3-7环烷基或杂环基; RC1和RC2均为氢，或当X为CRXRY时，RC1，RC2，RX和RY与它们所连接的碳原子一起形成任选取代的稠合芳环; 并且R 1选自H和卤素。
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公开(公告)号：US09169235B2
公开(公告)日：2015-10-27
申请号：US14483663
申请日：2014-09-11
发明人： Niall Morrison Barr Martin , Graeme Cameron Smith , Stephen Philip Jackson , Vincent Junior M Loh , Xiao-Ling Fan Cockcroft , Ian Timothy Williams Matthews , Keith Allan Menear , Frank Kerrigan , Alan Ashworth
IPC分类号： C07D403/10 , A61K31/00 , C07D237/32 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D491/04 , C07D495/04 , A61K31/502 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D403/14
CPC分类号： A61K31/502 , A61K31/00 , A61K31/506 , A61K31/5377 , A61K31/551 , A61K45/06 , A61N5/10 , C07D237/32 , C07D243/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D491/04 , C07D495/04
摘要： Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X═NRX then n is 1 or 2 and if X═CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.
摘要翻译： 式（I）的化合物：其中A和B一起表示任选取代的稠合芳环; X可以是NRX或CRXRY; 如果X = NRX则n为1或2，如果X = CRXRY则n为1; RX选自H，任选取代的C 1-20烷基，C 5-20芳基，C 3-20杂环基，酰氨基，硫代酰氨基，酯，酰基和磺酰基; RY选自H，羟基，氨基; 或RX和RY可以一起形成螺C 3-7环烷基或杂环基; RC1和RC2均为氢，或当X为CRXRY时，RC1，RC2，RX和RY与它们所连接的碳原子一起形成任选取代的稠合芳环; 并且R 1选自H和卤素。
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27.发明申请公开(公告)号：US20140135315A1
公开(公告)日：2014-05-15
申请号：US13859270
申请日：2013-04-09
发明人： Heather Mary Ellen DUGGAN , Frederic Georges Marie LEROUX , Karine Fabienne MALAGU , Niall Morrison Barr MARTIN , Keith MENEAR , Graeme Cameron Murray SMITH
IPC分类号： C07D471/04 , C07D475/10
CPC分类号： A61K31/5377 , A61K31/565 , A61K45/06 , C07D413/14 , C07D471/04 , C07D475/08 , C07D475/10
摘要： There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
摘要翻译： 提供式I化合物或其药学上可接受的盐。 还提供了制备式1化合物的方法和式1化合物作为药物和用于治疗癌症的用途。
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公开(公告)号：US20040023968A1
公开(公告)日：2004-02-05
申请号：US10426147
申请日：2003-04-29
发明人： Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Penny Jane Eversley , Xiao-Ling Cockcroft , Frank Kerrigan , Janet Hoare , Lesley Dixon
IPC分类号： A61K031/502 , C07D43/02
CPC分类号： C07D401/10 , C07D237/32 , C07D403/10 , C07D495/04
摘要： A compound of formula: 1 or an isomer, salt, solvate, chemically protected form, or prodrug thereof, wherein A and B together represent an optionally substituted, fused aromatic ring; RL is a C5-7 aryl group substituted in the meta position by the group R2, and optionally further substituted; wherein R2 is selected from: 2 and its use as a pharmaceutical, in particular for the treatment of diseases ameliorated by inhibiting the activity of PARP.
摘要翻译： 下式化合物或其异构体，盐，溶剂合物，化学保护形式或前药，其中A和B一起表示任选取代的稠合芳环; R L是由R 2基团在间位取代的任选进一步取代的C 5-7芳基; 其中R 2选自：及其作为药物的用途，特别是用于治疗通过抑制PARP的活性而改善的疾病。
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公开(公告)号：US20020183325A1
公开(公告)日：2002-12-05
申请号：US10021506
申请日：2001-10-30
发明人： Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Charles Richard White , Roger Frank Newton , Diane Gillian Douglas , Penny Jane Eversley , Julia Vile
IPC分类号： A61K031/502
CPC分类号： C07D401/12 , A61K31/50 , A61K31/502 , C07D237/32 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： A method of treatment of a disease of the human or animal body mediated by PARP comprising administering to such a subject a therapeutically effective amount of a compound of formula: 1 or an isomer, salt, solvate, chemically protected form, and prodrug thereof, wherein: A and B together represent an optionally substituted, fused aromatic ring; RC is represented by nullLnullRL, where L is of formula: null(CH2)n1nullQn2null(CH2)n3nullwherein n1, n2 and n3 are each selected from 0, 1, 2 and 3, the sum of n1, n2 and n3 is 1, 2 or 3 and Q is selected from O, S, NH, C(nullO) or nullCR1R2null, where R1 and R2 are independently selected from hydrogen, halogen or optionally substituted C1-7 alkyl, or may together with the carbon atom to which they are attached form a C3-7 cyclic alkyl group, which may be saturated (a C3-7 cycloalkyl group) or unsaturated (a C3-7 cycloalkenyl group), or one of R1 and R2 may be attached to an atom in RL to form an unsaturated C3-7 cycloalkenyl group which comprises the carbon atoms to which R1 and R2 are attached in Q, null(CH2)n3null (if present) and part of RL; and RL is optionally substituted C5-20 aryl; and RN is selected from hydrogen, optionally substituted C1-7 alkyl, C3-20 heterocyclyl, and C5-20 aryl, hydroxy, ether, nitro, amino, amido, thiol, thioether, sulfoxide and sulfone.
摘要翻译： 一种治疗由PARP介导的人体或动物体的疾病的方法，包括向所述受试者施用治疗有效量的式：或其异构体，盐，溶剂化物，化学保护形式及其前药的化合物，其中： A和B一起表示任选取代的稠合芳环; RC由-L-RL表示，其中L为下式：<段落lvl =“0”> in-line-formula> - （CH2）n1-Qn2-（CH2）n3 - 其中n1，n2和n3各自选自0,1,2和3，n1，n2和n3的和为1,2或3，Q选自O，S，NH，C（= O）或 -CR1R2-，其中R1和R2独立地选自氢，卤素或任选取代的C 1-7烷基，或者可以与它们所连接的碳原子一起形成C 3-7环状烷基，其可以是饱和的（a C 3-7环烷基）或不饱和（C 3-7环烯基），或者R 1和R 2中的一个可以连接到RL中的原子上以形成不饱和的C 3-7环烯基，其包含其中R 1和R 2 连接在Q， - （CH2）n3-（如果存在）和部分RL; 并且RL是任选取代的C 5-20芳基; 并且RN选自氢，任选取代的C 1-7烷基，C 3-20杂环基和C 5-20芳基，羟基，醚，硝基，氨基，酰胺基，硫醇，硫醚，亚砜和砜。
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