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1. 发明授权

US10314807B2 Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS) 有权
公开(公告)号：US10314807B2
公开(公告)日：2019-06-11
申请号：US15371104
申请日：2016-12-06
申请人： GTx, Inc.
发明人： James T. Dalton , Mitchell S. Steiner , Ramesh Narayanan , Sunjoo Ahn
IPC分类号： A61K31/167 , A61K31/277 , A61K31/4704 , A61K31/404 , A61K9/00 , A61K9/02 , A61K9/06 , A61K9/08 , A61K9/10 , A61K9/107 , A61K9/16 , A61K9/20 , A61K9/48
摘要： This invention relates to the treatment of breast cancer in a subject, for example a female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer; advanced breast cancer; breast cancer that has failed SERM (tamoxifen, toremifene), aromatase inhibitor, palbociclib (Ibrance), trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and/or fulvestrant treatments; metastasis in a subject suffering from breast cancer; and/or HER2-positive; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.

2. 发明申请

US20170007567A1 METHOD OF TREATING HER2-POSITIVE BREAST CANCERS WITH SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMS) 审中-公开
标题翻译：用选择性雄激素受体调节剂（SARMS）治疗HER2阳性乳腺癌的方法
公开(公告)号：US20170007567A1
公开(公告)日：2017-01-12
申请号：US15075373
申请日：2016-03-21
申请人： GTx, Inc.
发明人： James T. DALTON , Mitchell S. Steiner , Ramesh Narayanan , Sunjoo Ahn
IPC分类号： A61K31/277 , A61K31/167
CPC分类号： A61K31/277 , A61K9/4866 , A61K31/167
摘要： This invention relates to the treatment of breast cancer in a subject, for example a female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer; advanced breast cancer; breast cancer that has failed SERM (tamoxifen, toremifene), aromatase inhibitor, palbociclib (Ibrance), trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and/or fulvestrant treatments; metastasis in a subject suffering from breast cancer; and/or HER2-positive; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.
摘要翻译：本发明涉及治疗受试者，例如女性受试者的乳腺癌。包括以下方法：治疗转移性乳腺癌; 难治性乳腺癌; AR阳性乳腺癌; AR阳性难治性乳腺癌; AR阳性转移性乳腺癌; AR阳性和ER阳性乳腺癌; 三阴性乳腺癌; 晚期乳腺癌和（或）阿司匹林，阿伐他汀，阿伐他汀，阿伐他汀，阿伐他汀，阿伐他汀，阿伐他汀，阿伐他汀，阿伐他汀，阿伐他汀，阿伐他汀，阿伐他汀，氟维司群治疗; 患有乳腺癌的受试者的转移; 和/或HER2阳性; 包括给予受试者治疗有效量的选择性雄激素受体调节剂（SARM）化合物。

3. 发明申请

US20160128968A1 METHOD OF TREATING ANDROGEN RECEPTOR (AR) -POSITIVE BREAST CANCERS WITH SELECTIVE ANDROGEN RECEPTOR MODULATOR (SARMS) 有权
标题翻译：用选择性受体调节剂（SARMS）治疗原始受体（AR） - 乳腺癌的方法
公开(公告)号：US20160128968A1
公开(公告)日：2016-05-12
申请号：US14798208
申请日：2015-07-13
申请人： GTx, Inc.
发明人： James T. DALTON , Mitchell S. Steiner , Ramesh Narayanan , Sunjoo Ahn
IPC分类号： A61K31/277 , A61K9/50 , A61K9/48
CPC分类号： A61K31/277 , A61K9/4808 , A61K9/50 , A61K31/167
摘要： This invention relates to the treatment of breast cancer in a subject, for example a female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer; advanced breast cancer; breast cancer that has failed SERM (tamoxifen, toremifene), aromatase inhibitor, trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and/or fulvestrant treatments; metastasis in a subject suffering from breast cancer; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.
摘要翻译：本发明涉及治疗受试者，例如女性受试者的乳腺癌。包括以下方法：治疗转移性乳腺癌; 难治性乳腺癌; AR阳性乳腺癌; AR阳性难治性乳腺癌; AR阳性转移性乳腺癌; AR阳性和ER阳性乳腺癌; 三阴性乳腺癌; 晚期乳腺癌和（或）氟维司群治疗，其中SERM（他莫昔芬，托瑞米芬），芳香酶抑制剂，曲妥珠单抗（赫赛汀，阿霉素，阿坦曲坦），奥妥珠单抗（Perjeta），拉帕替尼，依西美坦（Aromasin），贝伐珠单抗（Avastin）患有乳腺癌的受试者的转移; 包括向受试者施用治疗有效量的选择性雄激素受体调节剂（SARM）化合物。

4. 发明申请

US20180325858A1 METHODS OF TREATING UROLOGICAL DISORDERS USING SARMs 审中-公开
公开(公告)号：US20180325858A1
公开(公告)日：2018-11-15
申请号：US15910505
申请日：2018-03-02
申请人： GTx, Inc.
发明人： Ramesh Narayanan , Jeffrey G. Hesselberg , Mary Ann Johnston , Robert H. Getzenberg
IPC分类号： A61K31/277 , A61K31/00 , A61K31/167
CPC分类号： A61K31/277 , A61K31/00 , A61K31/167
摘要： The present invention is directed to methods of treating, preventing, suppressing and/or inhibiting urological disorders such as urinary incontinence including stress urinary incontinence, urge urinary incontinence, mixed incontinence, and pelvic floor disorders by administering a SARM compound of the invention.

5. 发明授权

US10093613B2 Selective androgen receptor degrader (SARD) ligands and methods of use thereof 有权
公开(公告)号：US10093613B2
公开(公告)日：2018-10-09
申请号：US15830688
申请日：2017-12-04
申请人： GTx, Inc. , University of Tennessee Research Foundation
发明人： Ramesh Narayanan , Duane D. Miller , Thamarai Ponnusamy , Dong-Jin Hwang , Charles B. Duke , Christopher C. Coss , Amanda Jones , James T. Dalton
IPC分类号： C07C237/20 , A61P35/00 , A61P25/00 , A61P5/28
摘要： This invention provides novel 3-amino propanamide selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

6. 发明授权

US09814698B2 Selective androgen receptor degrader (SARD) ligands and methods of use thereof 有权
公开(公告)号：US09814698B2
公开(公告)日：2017-11-14
申请号：US15135334
申请日：2016-04-21
申请人： GTx, Inc. , University of Tennessee Research Foundation
发明人： Ramesh Narayanan , Duane D. Miller , Thamarai Ponnusamy , Dong-Jin Hwang , Jayaprakash Pagadala , Charles B. Duke , Christopher C. Coss , James T. Dalton , Yali He
IPC分类号： A61K31/404 , A61K9/00 , A61K31/437 , A61K31/4184 , A61K31/47 , A61K31/472 , A61K31/403 , A61K31/416
CPC分类号： A61K31/404 , A61K9/0014 , A61K31/403 , A61K31/405 , A61K31/416 , A61K31/4184 , A61K31/437 , A61K31/47 , A61K31/472 , A61K45/06 , C07C271/02 , C07D209/08 , C07D209/42 , C07D215/18 , C07D217/04 , C07D231/56 , C07D235/16 , C07D487/04
摘要： This invention provides novel indole, indazole, benzimidazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

7. 发明授权

US09744149B2 Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs) 有权
公开(公告)号：US09744149B2
公开(公告)日：2017-08-29
申请号：US14798208
申请日：2015-07-13
申请人： GTx, Inc.
发明人： James T. Dalton , Mitchell S. Steiner , Ramesh Narayanan , Sunjoo Ahn
IPC分类号： A61K31/167 , A61K31/277 , A61K9/48 , A61K9/50
CPC分类号： A61K31/277 , A61K9/4808 , A61K9/50 , A61K31/167
摘要： This invention relates to the treatment of breast cancer in a subject, for example a female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer; advanced breast cancer; breast cancer that has failed SERM (tamoxifen, toremifene), aromatase inhibitor, trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and/or fulvestrant treatments; metastasis in a subject suffering from breast cancer; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.

8. 发明申请

US20170166526A1 SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：US20170166526A1
公开(公告)日：2017-06-15
申请号：US15331777
申请日：2016-10-21
申请人： GTx, Inc. , University of Tennessee Research Foundation
发明人： Ramesh Narayanan , Duane D. Miller , Thamarai Ponnusamy , Dong-Jin Hwang , Jayaprakash Pagadala , Charles B. Duke , Christopher C. Coss , James T. Dalton , Yali He
IPC分类号： C07D209/08 , C07D209/42 , C07D215/00 , C07D471/04 , C07D231/56 , C07D217/04 , A61K9/00 , C07D235/04
CPC分类号： C07D209/08 , A61K9/0014 , C07D209/42 , C07D209/86 , C07D209/88 , C07D215/00 , C07D215/06 , C07D217/04 , C07D231/56 , C07D235/04 , C07D235/06 , C07D471/04
摘要： This invention provides novel indole, indazole, benzimidazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

9. 发明申请

US20170137374A1 SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF 有权
公开(公告)号：US20170137374A1
公开(公告)日：2017-05-18
申请号：US15331751
申请日：2016-10-21
申请人： GTx, Inc. , University of Tennessee Research Foundation
发明人： Ramesh Narayanan , Duane D. MILLER , Thamarai PONNUSAMY , Dong-Jin HWANG , Charles B. DUKE , Christopher C. COSS , Amanda JONES , James T. DALTON
IPC分类号： C07C255/60
CPC分类号： C07C255/60 , A61K9/0014 , A61K31/277 , A61K45/06 , C07B2200/07 , A61K2300/00
摘要： This invention provides novel 3-amino propanamide selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

10. 发明申请

US20140018433A1 METHOD OF TREATING ANDROGEN RECEPTOR (AR) -POSITIVE BREAST CANCERS WITH SELECTIVE ANDROGEN RECEPTOR MODULATOR (SARMS) 有权
标题翻译：用选择性受体调节剂（SARMS）治疗原始受体（AR） - 乳腺癌的方法
公开(公告)号：US20140018433A1
公开(公告)日：2014-01-16
申请号：US13789005
申请日：2013-03-07
申请人： GTx, Inc.
发明人： James T. Dalton , Mitchell S. Steiner , Ramesh Narayanan , Sunjoo Ahn
IPC分类号： C07C271/02 , A61K45/06 , A61K31/325
CPC分类号： C07C271/02 , A61K31/167 , A61K31/325 , A61K45/06 , Y02A50/395
摘要： This invention relates to the treatment of androgen receptor-positive breast cancer in a subject, for example a female subject. Accordingly, this invention provides methods of: a) treating a subject suffering from breast cancer; b) treating a subject suffering from metastatic breast cancer; c) treating a subject suffering from refractory breast cancer; d) treating a subject suffering from AR-positive breast cancer; e) treating a subject suffering from AR-positive refractory breast cancer; f) treating a subject suffering from AR-positive metastatic breast cancer; g) treating a subject suffering from AR-positive and ER-positive breast cancer; h) treating a subject suffering from triple negative breast cancer; i) treating a subject suffering from advanced breast cancer; j) treating a subject suffering from breast cancer that has failed SERM (tamoxifen, toremifene), aromatase inhibitor, trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and/or fulvestrant treatments; k) treating, preventing, suppressing or inhibiting metastasis in a subject suffering from breast cancer; l) prolonging survival of a subject with breast cancer, and/or m) prolonging the progression-free survival of a subject with breast cancer; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound, comprising administering to the subject a therapeutically effective amount of a SARM compound of this invention.
摘要翻译：本发明涉及治疗受试者中雄激素受体阳性乳腺癌，例如女性受试者。因此，本发明提供了以下方法：a）治疗患有乳腺癌的受试者; b）治疗患有转移性乳腺癌的受试者; c）治疗难治性乳腺癌患者; d）治疗患有AR阳性乳腺癌的受试者; e）治疗患有AR阳性难治性乳腺癌的受试者; f）治疗患有AR阳性转移性乳腺癌的受试者; g）治疗患有AR阳性和ER阳性乳腺癌的受试者; h）治疗患有三阴性乳腺癌的受试者; i）治疗晚期乳腺癌患者; j）治疗患有SERM（他莫昔芬，托瑞米芬），芳香酶抑制剂，曲妥珠单抗（赫赛汀，阿霉素，阿曲曲坦），奥妥珠单抗（Perjeta），拉帕替尼，依西美坦（Aromasin），贝伐珠单抗（Avastin） /或氟维司群治疗; k）治疗，预防，抑制或抑制患有乳腺癌患者的转移; l）延长患有乳腺癌的受试者的存活，和/或m）延长乳腺癌患者的无进展生存期; 包括向受试者施用治疗有效量的选择性雄激素受体调节剂（SARM）化合物，其包括向受试者施用治疗有效量的本发明的SARM化合物。

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