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    • 4. 发明申请
    • CONTRACEPTIVE COMPOSITIONS CONTAINING CYCLIC CARBAMATES AND AMIDE DERIVATIVES
    • 含有环状碳酸酯和酰胺衍生物的合成组合物
    • WO0066225A8
    • 2002-05-30
    • PCT/US0011846
    • 2000-05-01
    • AMERICAN HOME PRODLIGAND PHARM INCGRUBB GARY SZHI LINJONES TODD KSANTILLI ARTHUR ATEGLEY CHRISTOPHER MVIET ANDREW QZHANG PUWENFENSOME ANDREWWROBEL JAY EEDWARDS JAMES P
    • GRUBB GARY SZHI LINJONES TODD KSANTILLI ARTHUR ATEGLEY CHRISTOPHER MVIET ANDREW QZHANG PUWENFENSOME ANDREWWROBEL JAY EEDWARDS JAMES P
    • C07D498/04A61K31/40A61K31/445A61K31/535A61K31/5365A61K31/56A61K45/06A61P15/18A61K31/565A61K31/57
    • A61K31/56A61K31/40A61K31/445A61K31/535A61K31/565A61K45/06A61K2300/00
    • This invention relates to cyclic combination therapies and regimens utilizing, in combination with progestins, estrogens, or both, substituted indoline derivative compounds which are antagonists of the progesterone receptor having general structure (I) wherein A and B are independent substituents selected from S, CH or N; provided that when A is S, B is CH or N; and when B is S, A is CH or N; and A and B cannot both be CH; and when A and B both equal N, one N may be optionally substituted with a C1 to C6 alkyl group; R1 and R2 are independent substituents selected from the group of H, C1 to C6 alkyl, substituted C1 to C6 alkyl, C2 to C6 alkenyl, substituted C2 to C6 alkenyl, C2 to C6 alkynyl, substituted C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, substituted aryl, heterocyclic, substituted heterocyclic, COR , or NR COR ; or R and R are fused to form optionally substituted 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic ring, the heterocyclic ring containing one to three heteroatoms selected from the group of O, S and N; or pharmaceutically useful salts thereof. These methods of treatment may be used for contraception or for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses of the invention include stimulation of food intake.
    • 本发明涉及利用与孕激素,雌激素或两者作为孕酮受体的拮抗剂的代用药物,其具有一般结构(I)的循环组合疗法和方案,其中A和B是选自S,CH 或N; 条件是当A为S时,B为CH或N; 当B为S时,A为CH或N; A和B不能同时为CH; 并且当A和B均等于N时,一个N可以任选地被C 1至C 6烷基取代; R1和R2是选自H,C1至C6烷基,取代C1至C6烷基,C2至C6烯基,取代C2至C6烯基,C2至C6炔基,取代C2至C6炔基,C3至C8环烷基的独立取代基 取代的C 3至C 8环烷基,芳基,取代的芳基,杂环基,取代的杂环基,COR A或NR C CORA; 或R 1和R 2稠合形成任选取代的3至8元螺环烷基,烯基或杂环,所述杂环含有一至三个选自O,S和N的杂原子; 或其药学上有用的盐。 这些治疗方法可用于避孕或治疗和/或预防继发性闭经,功能障碍性出血,子宫平滑肌瘤,子宫内膜异位症; 多囊卵巢综合征,子宫内膜,卵巢,乳腺,结肠,前列腺的癌和腺癌,或副作用最小化或周期性月经出血。 本发明的额外用途包括刺激食物摄取。