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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

US20180360805A1 SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：US20180360805A1
公开(公告)日：2018-12-20
申请号：US15981636
申请日：2018-05-16
申请人： GTx, Inc. , University of Tennessee Research Foundation
发明人： Ramesh NARAYANAN , Duane D. MILLER , Thamarai PONNUSAMY , Dong-Jin HWANG , Yali HE , Jayaprakash PAGADALA , Charles B, DUKE , Christopher C. COSS , James T. DALTON
IPC分类号： A61K31/404 , A61K31/437 , A61K31/4184 , A61K31/47 , A61K31/472 , A61K31/403 , A61K31/416 , A61K31/4192 , A61P35/00
CPC分类号： A61K31/404 , A61K31/403 , A61K31/416 , A61K31/4184 , A61K31/4192 , A61K31/437 , A61K31/47 , A61K31/472 , A61P35/00
摘要： This invention provides novel indole, indazole, benzimidazole, benzotriazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, 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.

3. 发明申请

US20180353460A1 METHODS OF TREATING UROLOGICAL DISORDERS USING SARMs 审中-公开
公开(公告)号：US20180353460A1
公开(公告)日：2018-12-13
申请号：US15912421
申请日：2018-03-05
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.

4. 发明申请

US20170095446A1 SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF 有权
公开(公告)号：US20170095446A1
公开(公告)日：2017-04-06
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 , A61K31/437 , A61K31/416 , A61K31/47 , A61K31/472 , A61K31/403 , A61K9/00 , A61K31/4184
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.

5. 发明申请

US20170079733A1 AUTONOMOUS CRITICAL CARE SYSTEMS AND INTEGRATED COMBAT CASUALTY CARE SYSTEMS 审中-公开
公开(公告)号：US20170079733A1
公开(公告)日：2017-03-23
申请号：US15274618
申请日：2016-09-23
申请人： Athena GTX, Inc.
发明人： Mark Darrah , Cesar Gradilla , John Elson , Ellen Miller
IPC分类号： A61B50/20 , A61B5/08 , A61M5/168 , G06F19/00 , A61M16/00 , A61G1/00 , A61G1/048 , A61G1/052 , A61B5/00 , A61M1/00
CPC分类号： G16H40/63 , A61B5/0022 , A61B5/0205 , A61B5/742 , A61B50/31 , A61B2505/01 , A61G1/00 , A61G1/048 , A61M5/168 , A61M16/0051 , A61M16/01 , A61M16/024 , A61M16/101 , A61M2016/1025 , A61M2205/17 , A61M2205/3553 , A61M2205/3561 , A61M2205/3584 , A61M2205/3592 , A61M2205/36 , A61M2205/502 , A61M2205/8206 , A61M2209/08 , A61M2230/00 , A61M2230/04 , A61M2230/432 , G06F19/321 , G06F19/3418 , G06F19/3481
摘要： Systems, devices, and methods for monitoring and treating a patient on route to a medical facility are disclosed. The system comprises a critical care unit; at least one patient monitoring device coupled to the critical care unit, wherein the critical care unit obtains physiological data about the patient from each patient monitoring device; at least one patient treatment device coupled to the critical care unit, wherein the critical care unit provides treatment instructions to each patient treatment device; a two way communications device coupled to the critical care unit; and a remote communications terminal in communication with the two way communications device. The critical care unit preferably sends the physiological data to the remote communications terminal and receives the treatment instructions from the remote communications terminal via the two way communications device.

6. 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。

7. 发明申请

US20160128969A1 SOLID FORMS OF SELECTIVE ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：选择性受体调节剂的固体形式
公开(公告)号：US20160128969A1
公开(公告)日：2016-05-12
申请号：US14875181
申请日：2015-10-05
申请人： GTx, Inc.
发明人： James T. DALTON , Thomas G. BIRD , Tai AHN , David A. DICKASON , Seoung-Soo HONG
IPC分类号： A61K31/277
CPC分类号： A61K31/277 , C07C253/30 , C07C255/60
摘要： The present invention relates to solid forms of (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide and process for producing the same.
摘要翻译：本发明涉及（S）-N-（4-氰基-3-（三氟甲基）苯基）-3-（4-氰基苯氧基）-2-羟基-2-甲基丙酰胺的固体形式及其制备方法。

8. 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。

9. 发明申请

US20160106702A1 METHODS OF TREATING UROLOGICAL DISORDERS USING SARMs 审中-公开
标题翻译：使用SARM治疗尿路疾病的方法
公开(公告)号：US20160106702A1
公开(公告)日：2016-04-21
申请号：US14885818
申请日：2015-10-16
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 , A61K31/167
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 and pelvic-floor disorders by administering a SARM compound of the invention.
摘要翻译：本发明涉及通过施用本发明的SARM化合物来治疗，预防，抑制和/或抑制泌尿系统疾病如尿失禁，包括压力性尿失禁和骨盆底层疾病的方法。

10. 发明授权

US09150501B2 Solid forms of selective androgen receptor modulators 有权
标题翻译：选择性雄激素受体调节剂的固体形式
公开(公告)号：US09150501B2
公开(公告)日：2015-10-06
申请号：US14058896
申请日：2013-10-21
申请人： GTX, INC.
发明人： James T. Dalton , Thomas G. Bird , Tai Ahn , David A. Dickason , Seoung-Soo Hong
IPC分类号： C07C255/60 , C07C253/30
CPC分类号： A61K31/277 , C07C253/30 , C07C255/60
摘要： The present invention relates to solid forms of (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide and process for producing the same.
摘要翻译：本发明涉及（S）-N-（4-氰基-3-（三氟甲基）苯基）-3-（4-氰基苯氧基）-2-羟基-2-甲基丙酰胺的固体形式及其制备方法。

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