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Heteromorphic derivatives as PARP inhibitors
专利权人:
LUPIN LIMITED
发明人:
KARCHE, Navnath Popat,TILEKAR, Ajay Ramchandra,KURHADE, Sanjay Pralhad,JADHAV, Ganesh Rajaram,GUPTA, Nishant Ramniwasji,SINHA, Neelima,PALLE, Venkata P.,KAMBOJ, Rajender Kumar
申请号:
PE2018000206
公开号:
PE20181144A1
申请日:
2016.08.13
申请国别(地区):
PE
年份:
2018
代理人:
摘要:
General formula compound (I),The dotted line is a simple or double link; X and y are independent of C or N; ring AR is composed of (a) a heteroaromatic ring composed of six members, consisting of one to two N atoms, consisting of X and carbon; and (b) a heteroaromatic ring composed of five members, consisting of one to two heteroorganisms selected from n or y, In this case, X and y are selected at the same time instead of being selected at the same time; R1 is selected independently of halogen, nitric acid, cyanogen, etc.; R2 is h, halogen, nitric acid, etc.; R3 is selected independently of halogen and alternative or unsubstituted tar; R4 is selected independently as alternative tar or No substituteOr two r4s form an oxo (= O) in the same carbon,Among other things, ring B is cyclopentadiene, isopropene, etc.; R5 is independent of halogen, nitro, etc.; P is selected from 0, 1 and 2; Q, R, s is selected from 0, 1, 2 and 3. It also refers to pharmacology composers including formula compound (I),Your Taurus, tridimensional or salt. The most popular compounds are: (R) - 4 - (4 - (3 - (5-oxo-5, 6-dihydro-1, 6-naftiridin-7-il) cycloopent-2-en-1-il) piperazin-1-il) benzonitrilo, (R) - 4 - (3 - (3-fluoro-5-oxo-5, 6-dihydro-1, 6-naftridin-7-il) cycloopent-2-en-1-il) pipeterazonil. These compounds are inhibitors of polymerase (PARP) and can be used to treat or prevent cancer causing diseases such as liver cancer and melanoma.Se refiere a compuestos de formula general (I), donde las rayas discontinuas son un enlace sencillo o doble; X e Y son independientemente C o N; el anillo Ar es seleccionado de a) un anillo heteroaromatico de 6 miembros que contiene de 1 a 2 atomos de N, siendo X e Y carbono y b) un anillo heteroaromatico de 5 miembros que contiene de 1 a 2 heteroatomos seleccionados de N, O y S, en el que tanto X como Y no se seleccionan como N al mismo tiempo; R1 es seleccionado independientemente de halogeno, nitro, ciano, entre otros; R2 es H, halogeno, nitro, entre ot
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