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    • 2. 发明申请
    • Radiolabeled selective androgen receptor modulators and their use in prostate cancer imaging and therapy
    • 放射性标记的选择性雄激素受体调节剂及其在前列腺癌成像和治疗中的应用
    • US20080193380A1
    • 2008-08-14
    • US11984838
    • 2007-11-21
    • James T. DaltonDuane D. MillerLeonid I. KirkovskyArnab Mukherjee
    • James T. DaltonDuane D. MillerLeonid I. KirkovskyArnab Mukherjee
    • A61K51/04C07C233/07
    • A61K51/04A61K51/0402A61K51/0406A61K51/0446A61K51/0455A61K51/0459
    • Provided is a class of radiolabeled androgen receptor targeting agents (ARTA), useful for prostate cancer imaging and in treating or preventing prostate cancer. The agents define a new subclass of radiolabeled compounds, which are selective androgen receptor modulators (SARM), which demonstrate antiandrogenic activity of a nonsteroidal ligand for the androgen receptor, and/or which bind irreversibly to the androgen receptor. The present invention further provides methods for a) imaging of cancer in a subject, b) imaging an androgen receptor-containing tissue in a subject, c) in-vivo imaging in a subject, d) treating a subject suffering from prostate cancer, e) delaying the progression of prostate cancer in a subject suffering from prostate cancer, f) preventing the recurrence of prostate cancer in a subject suffering from prostate cancer, and g) treating the recurrence of prostate cancer in a subject suffering from prostate cancer, which comprise using the radiolabeled compounds of the present invention. The present invention further provides a method of producing the radiolabeled SARM compounds, and precursor compounds useful in the preparation of the radiolabeled SARM compounds.
    • 提供了一类用于前列腺癌成像和治疗或预防前列腺癌的放射性标记的雄激素受体靶向剂(ARTA)。 这些试剂定义了一种放射性标记化合物的新亚类,它们是选择性雄激素受体调节剂(SARM),其表现出非甾类配体对雄激素受体的抗雄激素活性和/或不依赖于雄激素受体的结合。 本发明进一步提供a)用于a)成像受试者中的癌症的方法,b)使受试者中含有雄激素受体的组织成像,c)受试者体内成像,d)治疗患有前列腺癌的受试者,e )延迟患有前列腺癌的受试者的前列腺癌的进展,f)预防患有前列腺癌的受试者中前列腺癌的复发,以及g)治疗患有前列腺癌的受试者中前列腺癌的复发,其包括 使用本发明的放射性标记的化合物。 本发明还提供了一种制备放射性标记的SARM化合物的方法,以及可用于制备放射性标记的SARM化合物的前体化合物。
    • 9. 发明授权
    • Radiolabeled selective androgen receptor modulators and their use in prostate cancer imaging and therapy
    • 放射性标记的选择性雄激素受体调节剂及其在前列腺癌成像和治疗中的应用
    • US07344700B2
    • 2008-03-18
    • US10371210
    • 2003-02-24
    • James T. DaltonDuane D. MillerLeonid I. KirkovskyArnab Mukherjee
    • James T. DaltonDuane D. MillerLeonid I. KirkovskyArnab Mukherjee
    • A61K51/00
    • A61K51/04A61K51/0402A61K51/0406A61K51/0446A61K51/0455A61K51/0459
    • Provided is a class of radiolabeled androgen receptor targeting agents (ARTA), useful for prostate cancer imaging and in treating or preventing prostate cancer. The agents define a new-subclass of radiolabeled compounds, which are selective androgen receptor modulators (SARM), which demonstrate antiandrogenic activity of a nonsteroidal ligand for the androgen receptor, and/or which bind irreversibly to the androgen receptor. The present invention further provides methods for a) imaging of cancer in a subject, b) imaging an androgen receptor-containing tissue in a subject, c) in-vivo imaging in a subject, d) treating a subject suffering from prostate cancer, e) delaying the progression of prostate cancer in a subject suffering from prostate cancer, f) preventing the recurrence of prostate cancer in a subject suffering from prostate cancer, and g) treating the recurrence of prostate cancer in a subject suffering from prostate cancer, which comprise using the radiolabeled compounds of the present invention. The present invention further provides a method of producing the radiolabeled SARM compounds, and precursor compounds useful in the preparation of the radiolabeled SARM compounds.
    • 提供了一类用于前列腺癌成像和治疗或预防前列腺癌的放射性标记的雄激素受体靶向剂(ARTA)。 这些试剂定义了一种放射性标记化合物的新亚类,它们是选择性雄激素受体调节剂(SARM),其表现出雄激素受体的非甾族化合物的抗雄激素活性和/或不依赖于雄激素受体的结合。 本发明进一步提供a)用于a)成像受试者中的癌症的方法,b)使受试者中含有雄激素受体的组织成像,c)受试者体内成像,d)治疗患有前列腺癌的受试者,e )延迟患有前列腺癌的受试者的前列腺癌的进展,f)预防患有前列腺癌的受试者中前列腺癌的复发,以及g)治疗患有前列腺癌的受试者中前列腺癌的复发,其包括 使用本发明的放射性标记的化合物。 本发明还提供了一种制备放射性标记的SARM化合物的方法,以及可用于制备放射性标记的SARM化合物的前体化合物。
    • 10. 发明授权
    • Non-steroidal agonist compounds and their use in male hormone therapy
    • 非甾体激动剂化合物及其在男性激素治疗中的应用
    • US6160011A
    • 2000-12-12
    • US86699
    • 1998-05-29
    • Duane D. MillerLeonid I. KirkovskyJames T. DaltonArnab Mukherjee
    • Duane D. MillerLeonid I. KirkovskyJames T. DaltonArnab Mukherjee
    • A61K31/167A61K31/277C07C235/16C07C255/60C07C317/46C07C323/60A61K31/275
    • C07C323/60A61K31/167A61K31/277C07C235/16C07C255/60C07C317/46
    • The present invention relates to a nonsteroidal agonist compound having the formula: ##STR1## where R.sub.1, R.sub.2, and R.sub.3 are the same or different and are a hydrogen, a nitro, a cyano, a carbamoyl, a halogen, a perfluoroalkyl, a haloalkylamido, an isothiocyanate, an azide, a diazocarbonyl, a substituted oxirane, or a .beta.-chloroethylamine; R.sub.4 is a hydrogen, an alkyl, or is joined to R.sub.5 ; R.sub.5 is a hydrogen, a hydroxy, an alkoxy, an acyloxy, an amino, an alkylamino, a halogen, an alkyl, a haloalkyl, or is joined to R.sub.4 ; R.sub.6 is a hydrogen, an alkyl, or a haloalkyl; A.sub.1 and A.sub.2 is the same or different, each is direct link or an alkylene; X.sub.1 is an oxygen, a sulfur, a sulphinyl, a sulphonyl, an amino, an alkylimino, or an alkylene; R.sub.7 is a hydrogen, a halogen, an alkoxy, a haloalkoxy, an acyloxy, a haloacyloxy, an aryloxy, a thioalkyl, a thioraryl, an amino, an alkylimino, an alkylamido group, a haloalkylamido group, or a phenyl optionally substituted with a halogen, a nitro group, an alkyl, a haloalkyl, a cyano, a hydroxyl, a carboxylic group, an amino, an alkylamino group, a dialkylamino group, a bisalkylamino group, a haloalkylamino group, a dihaloalkylamino group, a bishaloalkylamino group, an acylamido group, a diacylamido group, an alkylacylamido group, a haloacylamido group, a bis(haloacyl)imido group, or an alkylhaloacylamido group. The present invention further relates to a method of producing the non-steroidal agonist compound, a composition containing the non-steroidal agonist compound, and methods of binding an androgen receptor, suppressing spermatogenesis, and providing hormonal therapy for androgen-dependent conditions.
    • 本发明涉及具有下式的非甾体激动剂化合物:其中R1,R2和R3相同或不同,为氢,硝基,氰基,氨基甲酰基,卤素,全氟烷基,卤代烷基酰氨基,异硫氰酸酯 ,叠氮化物,重氮羰基,取代的环氧乙烷或β-氯乙胺; R4是氢,烷基,或与R5连接; R5是氢,羟基,烷氧基,酰氧基,氨基,烷基氨基,卤素,烷基,卤代烷基,或与R4结合; R6是氢,烷基或卤代烷基; A1和A2相同或不同,各自为直链或亚烷基; X1是氧,硫,亚磺酰基,磺酰基,氨基,烷基亚氨基或亚烷基; R 7是氢,卤素,烷氧基,卤代烷氧基,酰氧基,卤代酰氧基,芳氧基,硫代烷基,芳基,氨基,烷基亚氨基,烷基酰氨基,卤代烷基酰氨基或任选被 卤素,硝基,烷基,卤代烷基,氰基,羟基,羧基,氨基,烷基氨基,二烷基氨基,双烷基氨基,卤代烷基氨基,二卤代烷基氨基,二卤代烷基氨基, 酰基酰氨基,二酰氨基,烷基酰氨基,卤代酰氨基,双(卤代酰基)亚氨基或烷基卤代酰胺基。 本发明还涉及生产非甾体激动剂化合物的方法,含有非甾体激动剂化合物的组合物,和结合雄激素受体的方法,抑制精子发生,以及为雄激素依赖性条件提供激素疗法。