首页> 外国专利> Derivatives of 1, 3 - dihydro imidazo 4, 5 pyridin-3 (- 2 - one as TLR7 agonist receptor, a method for their preparation, Intermediates for the synthesis of the same, which includes a Pharmaceutical Composition and its use in preparation of a Medicament for the treatment of Viral Infections.

Derivatives of 1, 3 - dihydro imidazo 4, 5 pyridin-3 (- 2 - one as TLR7 agonist receptor, a method for their preparation, Intermediates for the synthesis of the same, which includes a Pharmaceutical Composition and its use in preparation of a Medicament for the treatment of Viral Infections.

机译:1,3-二氢咪唑并[4,5]吡啶3(-2-一种作为TLR7激动剂受体的衍生物),其制备方法,其合成中间体,包括药物组合物及其在制备中的用途用于治疗病毒感染的药物。

摘要

Derivatives of 1,3 Dihydro imidazo [4,5-c] pyridin - 2 - ona as immune response Modifiers of formula (1), which Act selectively on agonist receptors similar to toii (TLR), Uses Thereof, processes for the preparation thereof, and Intermediates used in the prepared Ation of the same and compositions containing Said inhibitors.These inhibitors are useful in a variety of Therapeutic areas including the treatment of infectious diseases such as hepatitis (e.g., hepatitis, HBC), genetically related Viral Infections and cancer.Claim 1: a compound of formula (1) or a pharmaceutically acceptable Salt or solvate of the compound or tautomero, in which (a) and is a direct link, and R3 is selected from aryl, alkyl and rent C1 C1 - 6 - 4 - or c1-4 alkyl, or (b); and it is alquileno c1-4, and R3 is selected from aryl,Cycloalkyl C3 - 7 and a heterociclilo 3 to 10 members; Z is Oxygen or is absent; r1 is selected from h, halogen, Oh, CN, cycloalkyl alkyl C1 - C3 - 6, 7 - 5 alkoxy, C1, nhso2r6 nr6r7 -, -, - C (o) - co2r6, R6, nr6r7, - C (o) - C (o) nr6so2r8, aryl and heterociclilo 3 to 10 members; R2 is selected Between o H, halogen, alkyl, cycloalkyl C1 - C3 - 6, 7 - 6 - alkoxy, C1, nr6r7, co2r6 -, - C (o) nr6r7,- C (o) nr6so2r8, and heterociclilo 3 to 10 members; or R1 and R2 can be joined to form a Union type alquileno C2 - 5, incorporating such Union Option 1 or 2 heteroatoms selected each one of them independently of N, o and s is absent; R4 and R5 is selected from h, cicloalq Uilo C3 - 7, aryl, aryl, (CH2) - C (o) - co2r9, R9, rent - C1 - 6 - or - C (o) - Rent R9, C1 - 6 - or - co2r9,- C (o) - Rent nr9r10 C1 -, 6 - or - C (o) - Rent nr9r10 and C1 - 6 - or - P (o) (OH) 2; R4 and R5 is absent or is selected between R9, - C (o) - co2r9, R9, let C1 - 6 - - or - C (o) - R9, rent or co2r9 C1 - 6 - -, - C (o) - Rent nr9r10 C1 -, 6 - or - C (o) - Rent nr9r10 and C1 - 6 - or - P (o) (OH) 2, each of R6 and R7 Select independ Ientemente between C1 - 6 h, alkyl, cycloalkyl C3 - 7- Hire C1 and C3 cycloalkyl - 6 - - 7; or R6 and R7 taken together with nitrogen Heterocycles that are United to form a saturated three to six members optionally containing one or two additional heteroatoms selected from N, o and S; R8 is selected from C1 - C3 alkyl and cycloalkyl - 7 6 Faith Nile; each R9 and R10 is selected regardless of C1 - 6 h, alkyl, cycloalkyl C3 - 7Aryl, aryl and heterociclilo - (CH2) 3 to 10 members; or R9 and R10, taken together with nitrogen which are United,Form a group heterociclilo 3 to 10 members; R11 and R12 are independently selected from H and alkyl C1 - 6; or R11 and R12 along with N that are United to form a saturated heterociclilo 3 to 6 members optionally containing one or two additional heteroatoms selected from N, o and S; While these groups alkyl, cycloalkyl, alkoxy,Aryl and heterociclilo optionally substituted with one or more Atoms or groups independently selected from Halogen, Oh, CN, CF3, oxo alkyl, cycloalkyl C1 - C3 - 6, 7 - 6 - alkoxy, C1, C1 alquileno - 6 - 6 or - alkyl - C1, C1 - Rent - Oh, nr11r12, - Let C1 - 6 - nr11r12, aryl and heterociclilo 3 to 10 members; under the condition that when R1 and R2 and R5 are H and Z are absent.Then (a) is not when R4 and R3 is methyl - Ethyl; and (b) R4 is not H or Methyl and - When R3 is Methyl.
机译:1,3二氢咪唑并[4,5-c]吡啶-2-酮的衍生物作为免疫应答的式(1)修饰剂,其选择性作用于类似于toii(TLR)的激动剂受体,用途及其制备方法,以及用于制备该抑制剂的中间体和含有上述抑制剂的组合物。这些抑制剂可用于多种治疗领域,包括治疗传染性疾病,例如肝炎(例如肝炎,HBC),遗传相关病毒感染和癌症1:式(1)的化合物或该化合物或互变异构体的药学上可接受的盐或溶剂化物,其中(a)是直接连接,且R 3选自芳基,烷基和C 1 -C 6- 4-或c1-4烷基,或(b); R 3为alquileno c1-4,R 3选自芳基,环烷基C 3-7和杂环基3-10元。 Z是氧或不存在; r1选自h,卤素,Oh,CN,环烷基烷基C1-C3-6、7-5烷氧基,C1,nhso2r6 nr6r7-,-,-C(o)-co2r6,R6,nr6r7,-C(o) -C(o)nr6so2r8,芳基和杂亚基3至10个成员; R 2在H,卤素,烷基,环烷基C1-C3-6、7-6-烷氧基,C1,nr6r7,co2r6-,-C(o)nr6r7,-C(o)nr6so2r8和杂环基3至10之间选择成员;或R 1和R 2可以连接形成联合型alquileno C 2-5,其结合了这样的联合选择1或2的杂原子,它们各自独立于N,o和s而被选择; R4和R5选自h,cicloalq Uilo C3-7,芳基,芳基,(CH2)-C(o)-co2r9,R9,租金-C1-6-或-C(o)-租金R9,C1-6 -或-co2r9,-C(o)-租赁nr9r10 C1-,6-或-C(o)-租赁nr9r10和C1-6-或-P(o)(OH)2; R4和R5不存在或在R9,-C(o)-co2r9,R9,让C1-6--或-C(o)-R9,Rent或co2r9之间选择C1-6----C(o) -租nr9r10 C1-,6-或-C(o)-租nr9r10和C1-6-或-P(o)(OH)2,R6和R7各自在C1-6h,烷基,环烷基之间选择独立的键C3-7-租用C1和C3环烷基-6-7;或R 6和R 7与氮杂环一起被结合形成饱和的三至六个成员,任选地含有一个或两个选自N,o和S的另外的杂原子;或R 8选自C 1 -C 3烷基和环烷基-7 Faith Nile;每个R9和R10的选择不考虑C1-6小时,烷基,C3-7环烷基,芳基,芳基和杂Cl-(CH2)3-10元;或R 9和R 10与氮一起被结合,形成3至10个杂杂环基团; R11和R12独立地选自H和烷基C1-6; R11和R12与N一起形成饱和的杂环3-6个成员,任选地含有一个或两个选自N,o和S的杂原子;或这些烷基,环烷基,烷氧基,芳基和杂环基任选被一个或多个独立选自卤素,Oh,CN,CF 3,氧代烷基,环烷基C 1 -C 3-6、7-6-烷氧基,C 1的原子或基团取代, C1 alquileno-6-6或-烷基-C1,C1-租-哦,nr11r12,-让C1-6-nr11r12,芳基和杂环基3到10个成员;在不存在R 1和R 2和R 5为H和Z的条件下,则(a)在R 4和R 3为甲基时不存在。 (b)R4不是H或甲基,以及-当R3是甲基时。

著录项

  • 公开/公告号AR059481A1

    专利类型

  • 公开/公告日2008-04-09

    原文格式PDF

  • 申请/专利权人 PFIZER LIMITED;

    申请/专利号AR2007P100607

  • 申请日2007-02-13

  • 分类号C07D471/04;A61K31/4353;A61P31/12;A61P35/00;

  • 国家 AR

  • 入库时间 2022-08-21 20:08:59

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