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    • 4. 发明申请
    • Heterocyclic silicon compounds and their use in the treatment of diseases or conditions associated with gnrh (gonadotropin-releasing hormone)
    • 杂环硅化合物及其在治疗与gnrh(促性腺激素释放激素)相关的疾病或病症中的应用
    • US20060052344A1
    • 2006-03-09
    • US10531333
    • 2003-11-19
    • John MontanaIan FlemingReinhold TackeJurgen Daiss
    • John MontanaIan FlemingReinhold TackeJurgen Daiss
    • A61K31/695C07F7/08
    • C07F7/0812
    • A compound of formula (I) wherein one of X and Y is silicon, and the other is carbon or silicon; Z is oxygen, sulphur or —N(R)—, wherein R is hydrogen or alkyl; R1 is hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy or cycloalkyl; and R2 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, -alkyl-cycloalkyl, -alkyl-heterocycloalkyl, -alkyl-aryl or -alkyl-heteroaryl; or a pharmaceutically acceptable salt thereof. The compounds are used in the manufacture of a medicament for the treatment or prevention of a disease or condition associated with GnRH (gonadotropin-releasing hormone), e.g. for the treatment or prevention of progression of cancer (e.g. leukaemia therapy), of a fertility disorder, of HIV infection or AIDS, of Alzheimer's disease of fibrosis, of endometriosis, of uterine fibroids or of uterine leiomyoma.
    • 式(I)的化合物,其中X和Y中的一个是硅,另一个是碳或硅; Z是氧,硫或-N(R) - ,其中R是氢或烷基; R 1是氢,卤素,烷基,烯基,炔基,烷氧基或环烷基; 和R 2是烷基,烯基,炔基,环烷基,杂环烷基,芳基,杂芳基, - 烷基 - 环烷基 - - 烷基 - 杂环烷基, - 烷基 - 芳基或 - 烷基 - 杂芳基; 或其药学上可接受的盐。 所述化合物用于制备用于治疗或预防与GnRH(促性腺激素释放激素)相关的疾病或病症的药物,例如, 用于治疗或预防艾滋病的纤维化,子宫内膜异位症,子宫肌瘤或子宫肌瘤的癌症(例如白血病治疗),生殖障碍,艾滋病毒感染或艾滋病的进展
    • 8. 发明申请
    • TRIAZOLOPYRIDINE DERIVATIVES AND THEIR THERAPEUTIC USE
    • 三唑吡啶衍生物及其治疗用途
    • US20120088763A1
    • 2012-04-12
    • US13201716
    • 2010-02-16
    • Harry FinchJohn MontanaMonique Bodil Van NielChi-Kit WooJamie KnightBohdan Waszkowycz
    • Harry FinchJohn MontanaMonique Bodil Van NielChi-Kit WooJamie KnightBohdan Waszkowycz
    • A61K31/5377A61P11/00A61P11/06C07D471/04A61K31/437
    • C07D471/04
    • Compounds of formula (I) are inhibitors of p38 MAP kinase, useful as anti-inflammatory agents in the treatment of inter alia, diseases of the respiratory tract wherein; R1 is C1-C6 alkyl, C3-C6 cycloalkyl, phenyl which is optionally substituted, 5- or 6 membered monocyclic heteroaryl which is optionally substituted, or a radical of formula (II) wherein n is 1 or 2, and R3 and R4 are independently H or C1-C6 alkyl, or R3 and R4 taken together with the nitrogen to which they are attached form a 6-membered heterocyclic ring optionally containing a further heteroatom selected from N and O; Y is —O— or —S(O)p— wherein p is 0, 1 or 2; A is an optionally substituted divalent arylene radical, or a mono- or bicyclic heteroarylene radical, or a C3-C6 divalent cycloalkylene radical having 5 or 6 ring atoms, or a piperidinylene radical wherein the ring nitrogen is linked to R2NHC(═O)W—; W is a bond, —NH— or —C(RA)(RB), wherein RA and RB are independently H, methyl, ethyl, amino, hydroxyl or halo; and R2 is a radical as defined in the claims.
    • 式(I)化合物是p38MAP激酶的抑制剂,其可用作治疗特别是呼吸道疾病的抗炎剂,其中: R 1是C 1 -C 6烷基,C 3 -C 6环烷基,任选取代的苯基,任选被取代的5-或6-元单环杂芳基,或其中n是1或2的式(II)基团,R 3和R 4是 独立地是H或C 1 -C 6烷基,或者R 3和R 4与它们所连接的氮一起形成任选含有另外选自N和O的杂原子的6元杂环; Y是-O-或-S(O)p - ,其中p是0,1或2; A是任选取代的二价亚芳基,或单环或双环亚杂芳基或具有5或6个环原子的C 3 -C 6二价亚环烷基或哌啶子基,其中环氮连接至R 2 NHC(= O)W - ; W是键,-NH-或-C(RA)(RB),其中RA和RB独立地是H,甲基,乙基,氨基,羟基或卤素; 并且R 2是如权利要求中所定义的基团。