Crystalline Anhydrate Forms Of A Pharmaceutical
    1.
    发明申请
    Crystalline Anhydrate Forms Of A Pharmaceutical 有权
    一种药物的结晶无水形式

    公开(公告)号:US20160083415A1

    公开(公告)日:2016-03-24

    申请号:US14459528

    申请日:2014-08-14

    IPC分类号: C07J7/00

    摘要: The invention provides and describes solid state 17α-ethynyl-androst-5-ene-3β,7β,17β-triol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-androst-5-ene-3β,7β,17β-triol include Form I anhydrate and Form IV and Form V solvates. The invention further relates to solid and suspension formulations containing 17α-ethynyl-androst-5-ene-3β,7β,17β-triol in a described solid state form and use of the formulations to treat hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, and autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-androst-5-ene-3β,7β,17β-triol and uses of such formulations in treating the described conditions.

    摘要翻译: 本发明提供并描述了固态17α-乙炔基 - 雄甾-5-烯-3β,其中包括无定形和结晶形式及其特定多态形式的17β-三醇。 17α-乙炔基 - 雄甾-5-烯-3&bgr; 7&bgr,17&bgr三醇的水合物和溶剂化物包括I型无水物和IV型和V型溶剂合物。 本发明还涉及含有所述固态形式的17α-乙炔基 - 雄甾-5-烯-3β,17α,17β-三醇的固体和悬浮液制剂,以及该制剂用于治疗高血糖病症如2型 糖尿病和代谢综合征以及自身免疫病症,如类风湿性关节炎,溃疡性结肠炎和1型糖尿病,以及受试者或人类患者的其他炎症相关病症。 本发明还涉及从17α-乙炔基 - 雄甾-5-烯-3β,7α,17β-三醇的固体形式制备液体制剂的方法以及这些制剂在治疗所述病症中的用途。

    Treatment Methods Using Pharmaceutical Solid State Forms

    公开(公告)号:US20160175322A9

    公开(公告)日:2016-06-23

    申请号:US14459493

    申请日:2014-08-14

    IPC分类号: A61K31/57

    摘要: The invention provides and describes solid state 17α-ethynyl-androst-5-ene-3β,7β,17β-triol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-androst-5-ene-3β,7β,17β-triol include Form I anhydrate and Form IV and Form V solvates. The invention further relates to solid and suspension formulations containing 17α-ethynyl-androst-5-ene-3β,7β,17β-triol in a described solid state form and use of the formulations to treat hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, and autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-androst-5-ene-3β,7β,17β-triol and uses of such formulations in treating the described conditions.

    TREATMENT METHODS USING PHARMACEUTICAL SOLID STATE FORMS
    3.
    发明申请
    TREATMENT METHODS USING PHARMACEUTICAL SOLID STATE FORMS 审中-公开
    使用药物固体状态的治疗方法

    公开(公告)号:US20120302537A1

    公开(公告)日:2012-11-29

    申请号:US13563996

    申请日:2012-08-01

    摘要: The invention provides and describes solid state 17α-ethynyl-androst-5-ene-3β,7β,17β-triol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-androst-5-ene-3β,7β,17β-triol include Form I anhydrate and Form IV and Form V solvates. The invention further relates to solid and suspension formulations containing 17α-ethynyl-androst-5-ene-3β,7β,17β-triol in a described solid state form and use of the formulations to treat hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, and autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-androst-5-ene-3β,7β,17β-triol and uses of such formulations in treating the described conditions.

    摘要翻译: 本发明提供并描述了固态17α-乙炔基 - 雄甾-5-烯-3β,其中包括无定形和结晶形式及其特定多态形式的17β-三醇。 17α-乙炔基 - 雄甾-5-烯-3&bgr; 7&bgr,17&bgr三醇的水合物和溶剂化物包括I型无水物和IV型和V型溶剂合物。 本发明还涉及含有所述固态形式的17α-乙炔基 - 雄甾-5-烯-3β,17α,17β-三醇的固体和悬浮液制剂,以及该制剂用于治疗高血糖病症如2型 糖尿病和代谢综合征以及自身免疫病症,如类风湿性关节炎,溃疡性结肠炎和1型糖尿病,以及受试者或人类患者的其他炎症相关病症。 本发明还涉及从17α-乙炔基 - 雄甾-5-烯-3β,7α,17β-三醇的固体形式制备液体制剂的方法以及这些制剂在治疗所述病症中的用途。

    Solid state forms of a pharmaceutical
    4.
    发明授权
    Solid state forms of a pharmaceutical 有权
    固体形式的药物

    公开(公告)号:US08252947B2

    公开(公告)日:2012-08-28

    申请号:US12418559

    申请日:2009-04-03

    IPC分类号: C07J5/00 C07J7/00 A61K31/56

    摘要: The invention provides and describes solid state 17α-ethynyl-androst-5-ene-3β, 7β,17β-triol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-androst-5-ene-3β, β,17β-triol include Form I anhydrate and Form IV and Form V solvates. The invention further relates to solid and suspension formulations containing 17α-ethynyl-androst-5-ene-3β,7β,17β-triol in a described solid state form and use of the formulations to treat hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, and autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-androst-5-ene-3β, 7β,17β-triol and uses of such formulations in treating the described conditions.

    摘要翻译: 本发明提供并描述了固态17α-乙炔基 - 雄甾-5-烯-3和bgr,17和b-三醇,包括无定形和结晶形式及其特定的多晶型物。 17α-乙炔基 - 雄甾-5-烯-3&bgr;,17β-三醇的水合物和溶剂化物包括Form I无水物和IV型和V型溶剂合物。 本发明还涉及含有所述固态形式的17α-乙炔基 - 雄甾-5-烯-3β,17α,17β-三醇的固体和悬浮液制剂,以及该制剂用于治疗高血糖病症如2型 糖尿病和代谢综合征以及自身免疫病症,如类风湿性关节炎,溃疡性结肠炎和1型糖尿病,以及受试者或人类患者的其他炎症相关病症。 本发明还涉及从固体形式的17α-乙炔基 - 雄甾-5-烯-3β,7α,17β-三醇制备液体制剂的方法以及这些制剂在治疗所述病症中的用途。

    Treatment Methods Using Pharmaceutical Solid State Forms
    5.
    发明申请
    Treatment Methods Using Pharmaceutical Solid State Forms 有权
    使用药物固体形式的治疗方法

    公开(公告)号:US20160045516A1

    公开(公告)日:2016-02-18

    申请号:US14459493

    申请日:2014-08-14

    IPC分类号: A61K31/57

    摘要: The invention provides and describes solid state 17α-ethynyl-androst-5-ene-3β,7β,17β-triol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-androst-5-ene-3β,7β,17β-triol include Form I anhydrate and Form IV and Form V solvates. The invention further relates to solid and suspension formulations containing 17α-ethynyl-androst-5-ene-3β,7β,17β-triol in a described solid state form and use of the formulations to treat hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, and autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-androst-5-ene-3β,7β,17β-triol and uses of such formulations in treating the described conditions.

    摘要翻译: 本发明提供并描述了固态17α-乙炔基 - 雄甾-5-烯-3β,其中包括无定形和结晶形式及其特定多态形式的17β-三醇。 17α-乙炔基 - 雄甾-5-烯-3&bgr; 7&bgr,17&bgr三醇的水合物和溶剂化物包括I型无水物和IV型和V型溶剂合物。 本发明还涉及含有所述固态形式的17α-乙炔基 - 雄甾-5-烯-3β,17α,17β-三醇的固体和悬浮液制剂,以及该制剂用于治疗高血糖病症如2型 糖尿病和代谢综合征以及自身免疫病症,如类风湿性关节炎,溃疡性结肠炎和1型糖尿病,以及受试者或人类患者的其他炎症相关病症。 本发明还涉及从17α-乙炔基 - 雄甾-5-烯-3β,7α,17β-三醇的固体形式制备液体制剂的方法以及这些制剂在治疗所述病症中的用途。

    CRYSTALLINE ANHYDRATE FORMS OF A PHARMACEUTICAL
    6.
    发明申请
    CRYSTALLINE ANHYDRATE FORMS OF A PHARMACEUTICAL 审中-公开
    药物的结晶形式

    公开(公告)号:US20120296105A1

    公开(公告)日:2012-11-22

    申请号:US13563982

    申请日:2012-08-01

    IPC分类号: C07J75/00 C07J1/00

    摘要: The invention provides and describes solid state 17α-ethynyl-androst-5-ene-3β,7β,17β-triol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-androst-5-ene-3β,7β,17β-triol include Form I anhydrate and Form IV and Form V solvates. The invention further relates to solid and suspension formulations containing 17α-ethynyl-androst-5-ene-3β,7β,17β-triol in a described solid state form and use of the formulations to treat hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, and autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-androst-5-ene-3β,7β,17β-triol and uses of such formulations in treating the described conditions.

    摘要翻译: 本发明提供并描述了固态17α-乙炔基 - 雄甾-5-烯-3β,其中包括无定形和结晶形式及其特定多态形式的17β-三醇。 17α-乙炔基 - 雄甾-5-烯-3&bgr; 7&bgr,17&bgr三醇的水合物和溶剂化物包括I型无水物和IV型和V型溶剂合物。 本发明还涉及含有所述固态形式的17α-乙炔基 - 雄甾-5-烯-3β,17α,17β-三醇的固体和悬浮液制剂,以及该制剂用于治疗高血糖病症如2型 糖尿病和代谢综合征以及自身免疫病症,如类风湿性关节炎,溃疡性结肠炎和1型糖尿病,以及受试者或人类患者的其他炎症相关病症。 本发明还涉及从17α-乙炔基 - 雄甾-5-烯-3β,7α,17β-三醇的固体形式制备液体制剂的方法以及这些制剂在治疗所述病症中的用途。

    SOLID STATE FORMS OF A PHARMACEUTICAL
    7.
    发明申请
    SOLID STATE FORMS OF A PHARMACEUTICAL 有权
    药物的固体状态

    公开(公告)号:US20090291933A1

    公开(公告)日:2009-11-26

    申请号:US12418559

    申请日:2009-04-03

    摘要: The invention provides and describes solid state 17α-ethynyl-androst-5-ene-3β,7β,17β-triol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-androst-5-ene-3β,7β,17β-triol include Form I anhydrate and Form IV and Form V solvates. The invention further relates to solid and suspension formulations containing 17α-ethynyl-androst-5-ene-3β,7β,17β-triol in a described solid state form and use of the formulations to treat hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, and autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-androst-5-ene-3β,7β,17β-triol and uses of such formulations in treating the described conditions.

    摘要翻译: 本发明提供并描述了固态17α-乙炔基 - 雄甾-5-烯-3β,7beta,17β-三醇,其包括无定形和结晶形式及其特定的多态形式。 17α-乙炔基 - 雄甾-5-烯-3β,7beta,17β-三醇的水合物和溶剂化物包括I型无水物和IV型和V型溶剂合物。 本发明还涉及含有所述固态形式的17α-乙炔基 - 雄甾-5-烯-3β,7beta,17β-三醇的固体和悬浮液制剂,以及该制剂用于治疗高血糖病症如2型糖尿病和代谢 综合征和自身免疫病症,例如类风湿性关节炎,溃疡性结肠炎和1型糖尿病以及受试者或人类患者的其它炎症相关病症。 本发明还涉及从17α-乙炔基 - 雄甾-5-烯-3β,7beta,17β-三醇的固态形式制备液体制剂的方法以及这些制剂在治疗所述条件中的用途。

    METHODS OF PREPARING PHARMACEUTICAL SOLID STATE FORMS
    8.
    发明申请
    METHODS OF PREPARING PHARMACEUTICAL SOLID STATE FORMS 有权
    制备药物固体状态的方法

    公开(公告)号:US20130345455A1

    公开(公告)日:2013-12-26

    申请号:US13919593

    申请日:2013-06-17

    IPC分类号: C07J7/00

    摘要: The invention provides and describes solid state 17α-ethynyl-5α-androstane-3α,17β-diol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-5α-androstane-3α,17β-diol include Form III anhydrate and Form I solvate. The invention further relates to solid and suspension formulations containing 17α-ethynyl-5α-androstane-3α,17β-diol in a described solid state form and use of the formulations to treat cancers or precancers such as prostate cancer or breast cancer in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-5α-androstane-3α,17β-diol and uses of such formulations in treating the described conditions.

    摘要翻译: 本发明提供并描述了固态17α-乙炔基-5α-雄甾烷-3α,17β-二醇,其包括无定形和结晶形式及其特定的多态形式。 17α-乙炔基-5α-雄甾烷-3α,17β-二醇的水合物和溶剂化物包括III型无水物和I型溶剂合物。 本发明还涉及含有所述固体形式的17α-乙炔基-5α-雄甾烷-3α,17β-二醇的固体和悬浮液制剂,并且该制剂用于治疗受试者或人类中的癌症或前列腺癌如前列腺癌或乳腺癌 耐心。 本发明还涉及从17α-乙炔基-5α-雄甾烷-3α,17β-二醇的固体形式制备液体制剂的方法以及这些制剂在治疗所述病症中的用途。

    PHARMACEUTICAL SOLID STATE FORMS
    9.
    发明申请
    PHARMACEUTICAL SOLID STATE FORMS 有权
    药物固体状态

    公开(公告)号:US20090291932A1

    公开(公告)日:2009-11-26

    申请号:US12370510

    申请日:2009-02-12

    IPC分类号: C07J7/00 A61K31/56 A61P35/04

    摘要: The invention provides and describes solid state 17α-ethynyl-5α-androstane-3α,17β-diol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-5α-androstane-3α,17β-diol include Form III anhydrate and Form I solvate. The invention further relates to solid and suspension formulations containing 17α-ethynyl-5α-androstane-3α,17β-diol in a described solid state form and use of the formulations to treat cancers or precancers such as prostate cancer or breast cancer in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-5α-androstane-3α,17β-diol and uses of such formulations in treating the described conditions.

    摘要翻译: 本发明提供并描述了固态17α-乙炔基-5α-雄甾烷-3α,17β-二醇,其包括无定形和结晶形式及其特定的多态形式。 17α-乙炔基-5α-雄甾烷-3α,17β-二醇的水合物和溶剂化物包括III型无水物和I型溶剂合物。 本发明还涉及含有所述固体形式的17α-乙炔基-5α-雄甾烷-3α,17β-二醇的固体和悬浮液制剂,并且该制剂用于治疗受试者或人类中的癌症或前列腺癌如前列腺癌或乳腺癌 耐心。 本发明还涉及从17α-乙炔基-5α-雄甾烷-3α,17β-二醇的固体形式制备液体制剂的方法以及这些制剂在治疗所述病症中的用途。

    PHARMACEUTICAL SOLID STATE FORMS-2
    10.
    发明申请
    PHARMACEUTICAL SOLID STATE FORMS-2 审中-公开
    药物固体状态2

    公开(公告)号:US20130345184A1

    公开(公告)日:2013-12-26

    申请号:US13919386

    申请日:2013-06-17

    摘要: The invention provides and describes solid state 17α-ethynyl-5α-androstane-3α,17β-diol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17α-ethynyl-5α-androstane-3α,17β-diol include Form III anhydrate and Form I solvate. The invention further relates to solid and suspension formulations containing 17α-ethynyl-5α-androstane-3α,17β-diol in a described solid state form and use of the formulations to treat cancers or precancers such as prostate cancer or breast cancer in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17α-ethynyl-5α-androstane-3α,17β-diol and uses of such formulations in treating the described conditions.

    摘要翻译: 本发明提供并描述了固态17α-乙炔基-5α-雄甾烷-3α,17β-二醇,其包括无定形和结晶形式及其特定的多态形式。 17α-乙炔基-5α-雄甾烷-3α,17β-二醇的水合物和溶剂化物包括III型无水物和I型溶剂合物。 本发明还涉及含有所述固体形式的17α-乙炔基-5α-雄甾烷-3α,17β-二醇的固体和悬浮液制剂,并且该制剂用于治疗受试者或人类中的癌症或前列腺癌如前列腺癌或乳腺癌 耐心。 本发明还涉及从17α-乙炔基-5α-雄甾烷-3α,17β-二醇的固体形式制备液体制剂的方法以及这些制剂在治疗所述病症中的用途。