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    • 2. 发明申请
    • PHARMACEUTICAL COMPOSITION COMPRISING GAMMA-BUTYROBETAINE
    • 包含γ-丁二醛的药物组合物
    • WO2003022262A1
    • 2003-03-20
    • PCT/LV2002/000004
    • 2002-03-04
    • KALVINSH, IvarsVEVERIS, MarisBIRMANS, Anatolijs
    • KALVINSH, IvarsVEVERIS, MarisBIRMANS, Anatolijs
    • A61K31/205
    • A61K31/205A61K31/495A61K31/505
    • New medical use for gamma-butyrobetaine is disclosed. Also disclosed are pharmaceutical compositions, containing gamma-butyrobetaine or combination thereof with 3-(2,2,2-trimethylhydrazinium)propionate or sildenafil for oral, parenteral, subcutaneous, transdermal, topical, sublingual, intrauretral, intranasal or rectal application, useful for stimulation of sexual activity and potency in mammals. The disclosed compositions, when applied orally for 6 weeks to non-narcotized male rats substantially increase their sexual activity, decreasing the arousal time, increasing the number of copulations and resultativeness of mounting attempts. When applied by intracavernous or intravenous route said pharmaceutical compositions increase intracorporeal pressure and duration of erection, as well as restore stimulation-induced reflectory erection in narcotized animals.
    • 公开了γ-丁基甜菜碱的新用途。 还公开了含有γ-丁基甜菜碱或其与3-(2,2,2-三甲基肼)丙酸酯或西地那非的组合的药物组合物用于口服,肠胃外,皮下,透皮,局部,舌下,眼内,鼻内或直肠施用,可用于 刺激哺乳动物的性活动和潜力。 所公开的组合物当向非麻醉的雄性大鼠口服6周时大大增加其性活动,减少觉醒时间,增加交配次数和安装尝试的有效性。 当通过海绵体内或静脉内途径施用时,所述药物组合物增加体内压力和勃起持续时间,以及恢复麻醉动物中刺激诱导的反射勃起。
    • 8. 发明申请
    • CARBAMIC ACID COMPOUNDS COMPRISING AN ESTER OR KETONE LINKAGE AS HDAC INHIBITORS
    • 含有ESET或KETONE连接作为HDAC抑制剂的碳酸化合物
    • WO2004065354A1
    • 2004-08-05
    • PCT/GB2004/000147
    • 2004-01-19
    • TOPOTARGET UK LIMITEDFINN, Paul, W.KALVINSH, IvarsLOZA, EinarsGUTCAITS, AleksandrsOLUTNIKA, IrenaSERPIONOVA, LudmilaGAILITE, VijaBOKALDERE, Rasma
    • FINN, Paul, W.KALVINSH, IvarsLOZA, EinarsGUTCAITS, AleksandrsOLUTNIKA, IrenaSERPIONOVA, LudmilaGAILITE, VijaBOKALDERE, Rasma
    • C07C259/10
    • C07C251/48C07C259/10C07C2601/08C07C2601/14C07D211/32
    • This invention pertains to certain carbamic acid compounds of the formula (I), which inhibit HDAC (histone deacetylase) activity: wherein: J is a linking functional group and is independently: -O-C(=O)- or -C(=O)-O- or - C(=O)-; Cy is a cyclyl group and is independently: C 3-20 carbocyclyl, C 3-20 heterocyclyl, or C 5-20 aryl; and is optionally substituted; Q 1 is a cyclyl leader group, and is independently a divalent bidentate group obtained by removing two hydrogen atoms from a ring carbon atom of a saturated monocyclic hydrocarbon having from 4 to 7 ring atoms, or by removing two hydrogen atoms from a ring carbon atom of saturated monocyclic heterocyclic compound having from 4 to 7 ring atoms including 1 nitrogen ring atom or 1 oxygen ring atom; and is optionally substituted; Q 2 is an acid leader group, and is independently: C 1-8 alkylene; and is optionally substituted; or: Q 2 is an acid leader group, and is independently: C 5-20 arylene; C 5-20 arylene-C 1-7 alkylene; C 1-7 alkylene-C 5-20 arylene; or C 1-7 alkylene-C 5-20 arylene-C 1-7 alkylene; and is optionally substituted; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC,and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.
    • 本发明涉及抑制HDAC(组蛋白脱乙酰酶)活性的某些式(I)的氨基甲酸化合物:其中:J为连接官能团,独立地为:-OC(= O) - 或-C(= O) -O-或-C(= O) - ; Cy是环状基团,独立地为:C 3-20碳环基,C 3-20杂环基或C 5-20芳基; 并且任选被取代; Q 1是环状前导基团,并且独立地是通过从具有4至7个环原子的饱和单环烃的环碳原子中除去两个氢原子或通过从环中除去两个氢原子而获得的二价二齿基团 具有4〜7个环原子的饱和单环杂环化合物的碳原子,包括1个氮环原子或1个氧环原子; 并且任选被取代; Q 2是酸性引导基团,独立地为:C 1-8亚烷基; 并且任选被取代; 或:Q 2是酸引导基团,并且独立地为:C 5-20亚芳基; C5-20arylene-C1-7alkylene; C1-7alkylene-C5-20arylene; 或C 1-7亚烷基-C 5 - 亚芳基-C 1-7亚烷基; 并且任选被取代; 和其药学上可接受的盐,溶剂合物,酰胺,酯,醚,化学保护形式及其前药。 本发明还涉及包含这些化合物的药物组合物,以及这些化合物和组合物在体外和体内的用途,以抑制HDAC,以及治疗由HDAC,癌症,增殖性病症,牛皮癣等介导的病症 。