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    Method of treating bone loss by stimulation of calcitonin
    11.
    发明授权
    Method of treating bone loss by stimulation of calcitonin 失效
    通过刺激降钙素治疗骨质流失的方法

    公开(公告)号：US06221874B1

    公开(公告)日：2001-04-24

    申请号：US09303972

    申请日：1999-05-03

    Applicant: Adam Matthew Gilbert ,  Gerardo Francisco ,  Magda Asselin

    Inventor： Adam Matthew Gilbert ,  Gerardo Francisco ,  Magda Asselin

    IPC: C07D47306

    CPC classification number: C07D473/06 ,  A61K31/522

    Abstract: Compounds of the formula R1 and R2 are independently alkyl of 1 to 6 carbon atoms, allyl, or substituted allyl of 3 to 6 carbon atoms; R3 is hydrogen, alkyl of 1 to 6 carbon atoms, or cycloalkyl of 3 to 10 carbon atoms; and R4 is phenyl or naphthyl substituted with alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms or NR5R6; substituted or unsubstituted phenylalkyl wherein the alkyl group contains 1 to 6 carbon atoms; substituted or unsubstituted 5 to 10 membered heteroaryl having 1 to 3 heteroatoms selected from N, S and O; substituted or unsubstituted cycloalkyl of 3 to 10 carbon atoms; or substituted or unsubstituted cycloalkylalkyl of 4 to 10 carbon atoms; provided that phenyl or naphthyl is substituted with NR5R6 when R1 and R2 is alkyl, are useful in the treatment of various disorders associated bone loss by increased transcription and elevation of plasma calcitonin levels. Such disorders include, but are not limited to: Paget's Disease, post menopausal osteoporosis, senile osteoporosis, and glucocorticoid-induced osteoporosis.

    Abstract translation: 式R1和R2的化合物独立地为1至6个碳原子的烷基，烯丙基或3至6个碳原子的取代的烯丙基; R3为氢，1〜6个碳原子的烷基或3〜10个碳原子的环烷基; R4为苯基或被1-6个碳原子的烷基取代的萘基，具有1-6个碳原子的烷氧基或NR5R6; 取代或未取代的苯基烷基，其中烷基含有1至6个碳原子; 取代或未取代的具有1至3个选自N，S和O的杂原子的5至10元杂芳基; 3至10个碳原子的取代或未取代的环烷基; 或取代或未取代的4-10个碳原子的环烷基烷基; 条件是当R 1和R 2为烷基时苯基或萘基被NR 5 R 6取代，可用于通过增加转录和升高血浆降钙素水平来治疗与骨丢失相关的各种疾病。 这种病症包括但不限于：佩吉特氏病，绝经后骨质疏松症，老年性骨质疏松症和糖皮质激素诱导的骨质疏松症。

    Diaminopyrazoles
    19.
    发明授权
    Diaminopyrazoles 失效

    公开(公告)号：US06172222B2

    公开(公告)日：2001-01-09

    申请号：US09327065

    申请日：1999-06-07

    Applicant: Adam Matthew Gilbert ,  Zhen-jia Chen

    Inventor： Adam Matthew Gilbert ,  Zhen-jia Chen

    IPC: C07D40112

    CPC classification number: C07D231/38 ,  C07D401/12

    Abstract: This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula wherein: R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R1 and R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl; R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2; n is 0 or 1; R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons; and all crystalline forms and the pharmaceutically acceptable salts thereof.

    Pyrazolopyrimidine-2,4-dione sulfonamides
    20.
    发明授权
    Pyrazolopyrimidine-2,4-dione sulfonamides 失效
    吡唑并嘧啶-2,4-二酮磺酰胺

    公开(公告)号：US6133273A

    公开(公告)日：2000-10-17

    申请号：US304180

    申请日：1999-05-03

    Applicant: Adam Matthew Gilbert ,  Zhen-jia Chen ,  Gerardo De La Cruz Francisco ,  Magda Asselin

    Inventor： Adam Matthew Gilbert ,  Zhen-jia Chen ,  Gerardo De La Cruz Francisco ,  Magda Asselin

    IPC: A61K31/519 ,  C07D487/04 ,  A61K31/4162

    CPC classification number: C07D487/04 ,  A61K31/519

    Abstract: A compound of formula (I) ##STR1## wherein: X=N and Y=CH or X=CH and Y=NR.sub.1 and R.sub.2 are independently, straight chain alkyl of 2 to 12 carbon atoms, branched chain alkyl of 3 to 10 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, aryl of 4 to 10 carbon atoms, 4 to 10 membered heteroaryl or a moiety of the formula (CH.sub.2).sub.m -A wherein m is 1 to 9 and A is cycloalkyl of 3 to 7 carbon atoms; and R.sub.3 is a straight chain alkyl of 1 to 12 carbon atoms, branched chain alkyl of 3 to 10 carbon atoms, aryl of 4 to 10 carbon atoms or 4 to 10 membered heteroaryl for use in the treatment of disorders associated with bone loss by increased transcription and elevation of plasma calcitonin levels.

    Abstract translation: 式（I）的化合物，其中：X = N，Y = CH或X = CH，Y = N R 1，R 2独立地为2至12个碳原子的直链烷基，3至10个碳原子的支链烷基， 3至10个碳原子的环烷基，4至10个碳原子的芳基，4至10元杂芳基或式（CH2）mA部分，其中m为1至9，A为3至7个碳原子的环烷基; 并且R 3是1至12个碳原子的直链烷基，3至10个碳原子的支链烷基，4至10个碳原子的芳基或4至10元杂芳基，用于治疗与骨丢失相关的疾病增加 血浆降钙素水平的转录和升高。

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