Selective estrogen receptor modulators
    61.
    发明申请
    Selective estrogen receptor modulators 有权
    选择性雌激素受体调节剂

    公开(公告)号:US20030105148A1

    公开(公告)日:2003-06-05

    申请号:US10216253

    申请日:2002-08-09

    摘要: The present invention provides, inter alia, triphenylethylene derivatives, such as, 3-null4-null6-(3-Methoxy-phenyl)-8,9-dihydro-7H-benzocyclohepten-5-ylnull-phenylnull-acrylic acid, as selective estrogen receptor modulators. Also provided are methods for the treatment and/or prevention of estrogen stimulated diseases in mammals including breast, uterine, ovarian, prostrate and colon cancer, osteoporosis, cardiovascular disease, and benign proliferative disorders, as well as pharmaceutical compositions of the compounds of the present invention.

    摘要翻译: 本发明特别提供三苯基乙烯衍生物,例如3- {4- [6-(3-甲氧基 - 苯基)-8,9-二氢-7H-苯并环庚烯-5-基] - 苯基} - 丙烯酸 ,作为选择性雌激素受体调节剂。 还提供了用于治疗和/或预防哺乳动物包括乳腺,子宫,卵巢,前列腺和结肠癌,骨质疏松症,心血管疾病和良性增殖性疾病的哺乳动物中雌激素刺激性疾病的方法,以及本发明化合物的药物组合物 发明。

    Process of using 1-methyl-2-pyrrolidinone as a pyridine replacement
    62.
    发明申请
    Process of using 1-methyl-2-pyrrolidinone as a pyridine replacement 审中-公开
    使用1-甲基-2-吡咯烷酮作为吡啶替代物的方法

    公开(公告)号:US20020188147A1

    公开(公告)日:2002-12-12

    申请号:US10121888

    申请日:2002-04-12

    发明人: Allen D. Johnston

    IPC分类号: C07C39/28 C07C069/76

    摘要: A process to prepare an ester which reacts an acid and a base in a solvent which contains 1-methyl-2-pyrrolidinone. The use of 1-methyl-2-pyrrolidinone can replace pyridine solvent. The pyridine solvent is a challenge for disposal and safe handling.

    摘要翻译: 一种制备在含有1-甲基-2-吡咯烷酮的溶剂中使酸和碱反应的酯的方法。 使用1-甲基-2-吡咯烷酮可以代替吡啶溶剂。 吡啶溶剂是处理和安全处理的难题。

    Novel delta dicarbonyl compounds and methods for using the same
    63.
    发明申请
    Novel delta dicarbonyl compounds and methods for using the same 失效
    新型三羰基化合物及其使用方法

    公开(公告)号:US20020137775A1

    公开(公告)日:2002-09-26

    申请号:US09858948

    申请日:2001-05-17

    摘要: Amidomethyl esters, carbonylmercaptomethyl esters, keto-containing esters, amidomethyl thioesters, amidomethyl amides, and methylene dithioesters are disclosed. The novel compounds have two carbonyl groups connected by a linking moiety having an oxygen, sulfur or nitrogen attached to a methylene group, to which is further attached a sulfur, nitrogen or CH2 group. Methods of treating illnesses and conditions, such as cancer, hemological disorders, inherited metabolic disorders and others, using these compounds are also disclosed.

    摘要翻译: 公开了甲基酯,羰基巯基甲基酯,含酮基酯,酰胺基甲基硫酯,酰胺基甲基酰胺和亚甲基二硫代酯。 新化合物具有通过连接到亚甲基上的具有氧,硫或氮的连接部分连接的两个羰基,其还连接有硫,氮或CH 2基团。 还公开了使用这些化合物治疗疾病和病症如癌症,血液病症,遗传性代谢障碍等的方法。

    Unsaturated derivatives at the 4-position of 6-tert-butyl-1, 1- dimethylindane and their use in human and veterinary medicine and in cosmetics
    66.
    发明授权
    Unsaturated derivatives at the 4-position of 6-tert-butyl-1, 1- dimethylindane and their use in human and veterinary medicine and in cosmetics 失效
    6-叔丁基-1,1-二甲基茚满的4-位不饱和衍生物及其在人兽药和化妆品中的用途

    公开(公告)号:US06180674B2

    公开(公告)日:2001-01-30

    申请号:US09158892

    申请日:1998-09-23

    IPC分类号: A61K3119

    摘要: 6-tert-Butyl-1,1-dimethylindane derivatives which are unsaturated in the 4-position of formula: X represents: (i) either a radical of formula: and Y represents a radical of formula: (ii) or a radical of formula: and Y represents either a radical of formula (b) or a radical of formula: Z being —O—, —S— or R1 represents —CH3, —(CH2)p—OR4, —(CH2)p—COR5 or —S(O)t—R6, p being 0, 1, 2 or 3, t being 0, 1 or 2, R2 represents H or lower alkyl, R3 represents H, lower alkyl or —COR7, R4 represents H, lower alkyl, —COR7, aryl, aralkyl, mono- or polyhydroxyalkyl, or a polyether radical, R5 represents H, lower alkyl, —OR8 or —N(r′)(r″), R6 represents H or lower alkyl, R7 represents lower alkyl, R8 represents H, alkyl, alkenyl, alkynyl, aryl, aralkyl, mono- or polyhydroxyalkyl, a sugar residue or an amino acid residue, r′ and r″ represent H, lower alkyl, —COR7, aryl, a sugar residue or an amino acid residue or r′ and r″ form a heterocycle, and the salts of the compounds of formula (I). Use in the topical and systemic treatment of dermatological conditions, as well as in cosmetics.

    摘要翻译: 在式X中4-位不饱和的6-叔丁基-1,1-二甲基茚满衍生物表示:(i)下式的基团:Y表示式(ⅱ)的基团或基团 并且Y表示式(b)的基团或式Z的基团是-O - , - S-或R 1表示-CH 3, - (CH 2)p -OR 4, - (CH 2)p -OR 5或 - S(O)t-R6,p为0,1,2或3,t为0,1或2,R2为H或低级烷基,R3为H,低级烷基或-COR7,R4为H,低级烷基, -COR 7,芳基,芳烷基,单 - 或多羟基烷基或聚醚基,R 5表示H,低级烷基,-OR 8或-N(r')(r“),R 6表示H或低级烷基,R 7表示低级烷基 R8代表H,烷基,烯基,炔基,芳基,芳烷基,单或多羟基烷基,糖残基或氨基酸残基,r'和r“代表H,低级烷基,-COR7,芳基,糖残基或 氨基酸残基或r'和r“形成杂环,和式(I)化合物的盐。在局部和系统中使用 ic治疗皮肤病学条件,以及化妆品。