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    • 1. 发明申请
    • NOVEL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, AND METHODS OF USE FOR SAME
    • 新化合物,含有该化合物的药物组合物及其使用方法
    • US20100120901A1
    • 2010-05-13
    • US12686691
    • 2010-01-13
    • Francis P. KuhajdaSusan M. MedghalchiJill M. McFaddenJagan ThupariCraig A. Townsend
    • Francis P. KuhajdaSusan M. MedghalchiJill M. McFaddenJagan ThupariCraig A. Townsend
    • A61K31/381C07D333/32A61P3/00A61P31/00
    • C07D409/12C07D333/32
    • A pharmaceutical composition comprising a pharmaceutical diluent and a compound of formula IV wherein R21=H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, —CH2OR25, —C(O)R25, —CO(O)R25, —C(O)NR25R26, —CH2C(O)R25, or —CH2C(O)NHR25, where R25 and R26 are each independently H, C1-C10 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing one or more halogen atoms. R22=—OH, —OR27, —OCH2C(O)R27, —OCH2C(O)NHR27, —OC(O)R27, —OC(O)OR27, —OC(O)NHNH—R5, or —OC(O)NR27R28, where R27 and R28 are each independently H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, and where R27 and R28 can each optionally contain halogen atoms; R23 and R24, the same or different from each other, are C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl. Methods of using such formulations for the treatment of cancer, to effect weight loss, to treat microbially-based infections, to inhibit neuropeptide-Y and/or fatty acid synthase, and to stimulate CPT-1.
    • 包含药物稀释剂和式IV化合物的药物组合物,其中R 21 = H,C 1 -C 20烷基,环烷基,烯基,芳基,芳基烷基或烷基芳基,-CH 2 OR 25,-C(O)R 25,-CO(O)R 25 ,-C(O)NR 25 R 26,-CH 2 C(O)R 25或-CH 2 C(O)NHR 25,其中R 25和R 26各自独立地为H,C 1 -C 10烷基,环烷基,烯基,芳基,芳烷基或烷芳基, 一个或多个卤素原子。 R22 = -OH,-OR27,-OCH2C(O)R27,-OCH2C(O)NHR27,-OC(O)R27,-OC(O)OR27,-OC(O)NHNH-R5或-OC )NR 27 R 28,其中R 27和R 28各自独立地为H,C 1 -C 20烷基,环烷基,烯基,芳基,芳基烷基或烷基芳基,并且其中R 27和R 28可各自任选含有卤素原子; R 23和R 24彼此相同或不同,为C 1 -C 20烷基,环烷基,烯基,芳基,芳基烷基或烷基芳基。 使用这些制剂治疗癌症,减轻体重,治疗基于微生物的感染,抑制神经肽Y和/或脂肪酸合成酶以及刺激CPT-1的方法。
    • 2. 发明申请
    • NOVEL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, AND METHODS OF USE FOR SAME
    • 新化合物,含有该化合物的药物组合物及其使用方法
    • US20100029752A1
    • 2010-02-04
    • US12309418
    • 2006-07-26
    • Francis P. KuhajdaCraig A. TownsendSusan M. MedghalchiJill M. McFadden
    • Francis P. KuhajdaCraig A. TownsendSusan M. MedghalchiJill M. McFadden
    • A61K31/381C07D307/34C07D307/26A61P35/00
    • C07D333/38C07D409/12
    • A pharmaceutical composition containing a pharmaceutical diluent and a compound of formula II: wherein: R8═H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, —C(O)R4, where R4 is H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms, or —OH, —OR7 or —NR7, where R7 is H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms; R9=—OR5, —NR5, —NH—NH—R5 where R5 is H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, allyl, or alkylaryl, optionally containing halogen atoms; R10═H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, or —CH2C(O)R6, where R6 is OR7 and NR7, where R7═H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, allyl, or alkylaryl and can optionally contain halogen atoms. Also included in the invention are methods of using the pharmaceutical compositions and the chemical compounds used in the compositions.
    • 含有药物稀释剂和式II化合物的药物组合物:其中:R8-H,C1-C20烷基,环烷基,烯基,芳基,芳基烷基或烷基芳基,-C(O)R4,其中R4是H,C1- C20烷基,环烷基,烯基,芳基,芳基烷基或烷基芳基,任选地含有卤素原子,或-OH,-OR7或-NR7,其中R7是H,C1-C20烷基,环烷基,烯基,芳基,芳基烷基或烷基芳基, 任选地含有卤素原子; R9 = -OR5,-NR5,-NH-NH-R5,其中R5是H,C1-C20烷基,环烷基,烯基,芳基,芳基烷基,烯丙基或烷基芳基,任选地含有卤素原子; R 10 -H,C 1 -C 20烷基,环烷基,烯基,芳基,芳烷基或烷基芳基或-CH 2 C(O)R 6,其中R 6是OR 7和NR 7,其中R 7 -H,C 1 -C 20烷基,环烷基,烯基,芳基 ,芳基烷基,烯丙基或烷基芳基,并且可任选地含有卤素原子。 本发明还包括使用组合物中使用的药物组合物和化合物的方法。
    • 8. 发明授权
    • Compounds, pharmaceutical compositions containing same, and methods of use for same
    • 含有其的化合物,药物组合物及其用途方法
    • US07649012B2
    • 2010-01-19
    • US10520505
    • 2003-07-09
    • Francis P. KuhajdaSusan M. MedghalchiJill M. McFaddenJagan Thupari
    • Francis P. KuhajdaSusan M. MedghalchiJill M. McFaddenJagan Thupari
    • A61K31/381C07D333/32
    • C07D409/12C07D333/32
    • A pharmaceutical composition comprising a pharmaceutical diluent and a compound of formula IV wherein R21=H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, —CH2OR25, —C(O)R25, —CO(O)R25, —C(O)NR25R26, —CH2C(O)R25, or —CH2C(O)NHR25, where R25 and R26 are each independently H, C1-C10 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing one or more halogen atoms. R22=—OH, —OR27, —OCH2C(O)R27, —OCH2C(O)NHR27, —OC(O)R27, —OC(O)OR27, —OC(O)NHNH—R5, or —OC(O)NR27R28, where R27 and R28 are each independently H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, and where R27 and R28 can each optionally contain halogen atoms; R23 and R24, the same or different from each other, are C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl. Methods of using such formulations for the treatment of cancer, to effect weight loss, to treat microbially-based infections, to inhibit neuropeptide-Y and/or fatty acid synthase, and to stimulate CPT-1.
    • 包含药物稀释剂和式IV化合物的药物组合物,其中R 21 = H,C 1 -C 20烷基,环烷基,烯基,芳基,芳基烷基或烷基芳基,-CH 2 OR 25,-C(O)R 25,-CO(O)R 25 ,-C(O)NR 25 R 26,-CH 2 C(O)R 25或-CH 2 C(O)NHR 25,其中R 25和R 26各自独立地为H,C 1 -C 10烷基,环烷基,烯基,芳基,芳烷基或烷芳基, 一个或多个卤素原子。 R22 = -OH,-OR27,-OCH2C(O)R27,-OCH2C(O)NHR27,-OC(O)R27,-OC(O)OR27,-OC(O)NHNH-R5或-OC )NR 27 R 28,其中R 27和R 28各自独立地为H,C 1 -C 20烷基,环烷基,烯基,芳基,芳基烷基或烷基芳基,并且其中R 27和R 28可各自任选含有卤素原子; R 23和R 24彼此相同或不同,为C 1 -C 20烷基,环烷基,烯基,芳基,芳基烷基或烷基芳基。 使用这些制剂治疗癌症,减轻体重,治疗基于微生物的感染,抑制神经肽Y和/或脂肪酸合成酶以及刺激CPT-1的方法。