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1. 发明专利

JP2014166996A Nuclear receptor binding agents 有权
标题翻译：核受体结合剂
公开(公告)号：JP2014166996A
公开(公告)日：2014-09-11
申请号：JP2014033091
申请日：2014-02-24
申请人： Gtx Inc , ジーティーエックス・インコーポレイテッド
发明人： JAMES T DALTON , CHRISTINA BARRETT , DUANE D MILLER , HONG SEOUNG-SOO , YALI HE , MICHAEL L MOHLER , RAMESH NARAYANAN , WU ZHONGZHI
IPC分类号： C07C233/75 , A61K31/167 , A61P3/06 , A61P9/00 , A61P9/10 , A61P13/08 , A61P13/12 , A61P15/12 , A61P17/14 , A61P19/10 , A61P29/00 , A61P35/00 , A61P35/02 , C07C235/56
CPC分类号： A61K31/138 , A61K31/40 , A61K31/445 , A61K31/55 , C07D221/12
摘要： PROBLEM TO BE SOLVED: To provide a novel class of agents modulating activity of steroid nuclear receptors, particularly, selective estrogen receptor modulators (SERMs), which are applicable for use in prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate cancer and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.SOLUTION: The invention provides compounds represented by the structure of the formula VI.
摘要翻译：要解决的问题：提供调节类固醇核受体活性的新一类试剂，特别是适用于预防和/或治疗各种疾病和病症的选择性雌激素受体调节剂（SERMs），包括预防和治疗前列腺癌和乳腺癌等癌症，骨质疏松症，激素相关疾病，潮热或血管舒缩症状，神经系统疾病，心血管疾病和肥胖症。解决方案：本发明提供由式VI结构表示的化合物。

2. 发明申请

WO2008091555A3 NUCLEAR RECEPTOR BINDING AGENTS 审中-公开
标题翻译：核受体结合剂
公开(公告)号：WO2008091555A3
公开(公告)日：2008-10-09
申请号：PCT/US2008000736
申请日：2008-01-22
申请人： GTX INC , DALTON JAMES T , MILLER DUANE D , MOHLER MICHAEL L , WU ZHONGZHI , HONG SEOUNG-SOO , SRIVASTAVA DEVESH
发明人： DALTON JAMES T , MILLER DUANE D , MOHLER MICHAEL L , WU ZHONGZHI , HONG SEOUNG-SOO , SRIVASTAVA DEVESH
IPC分类号： A01N43/42 , A01N55/02 , A61K31/555
CPC分类号： A61K31/472 , C07D217/22 , C07D217/24
摘要： The present invention relates to a novel class of nuclear receptor binding agents (NRBAs). The NRBAs are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, inflammatory diseases, oxidative stress related disorders such as Parkinson's and stroke, neurological disorders, ophthalamic disorders, cardiovascular disease, and obesity.
摘要翻译：本发明涉及一类新的核受体结合剂（NRBAs）。 NRBAs适用于预防和/或治疗各种疾病和病症，包括预防和治疗诸如前列腺和乳腺癌，骨质疏松症，激素相关疾病，炎性疾病，氧化应激相关疾病如帕金森病和中风，神经障碍，眼科疾病，心血管疾病和肥胖。

3. 发明申请

WO2007062230A2 NUCLEAR RECEPTOR BINDING AGENTS 审中-公开
标题翻译：核受体结合剂
公开(公告)号：WO2007062230A2
公开(公告)日：2007-05-31
申请号：PCT/US2006045451
申请日：2006-11-28
申请人： GTX INC , DALTON JAMES T , BARRETT CHRISTINA , HE YALI , HONG SEOUNG-SOO , MILLER DUANE D , MOHLER MICHAEL L , NARAYANAN RAMESH , WU ZHONGZHI
发明人： DALTON JAMES T , BARRETT CHRISTINA , HE YALI , HONG SEOUNG-SOO , MILLER DUANE D , MOHLER MICHAEL L , NARAYANAN RAMESH , WU ZHONGZHI
IPC分类号： A61K31/55 , A01N31/14 , A61K31/138 , A61K31/40 , A61K31/445
CPC分类号： A61K31/138 , A61K31/40 , A61K31/445 , A61K31/55 , C07D221/12
摘要： The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.
摘要翻译：本发明涉及一类新型选择性雌激素受体调节剂（SERM）。 SERM化合物适用于预防和/或治疗各种疾病和病症，包括预防和治疗癌症，例如前列腺癌和乳腺癌，骨质疏松症，激素相关性疾病，潮热或血管舒缩症状，神经病症，心血管疾病和肥胖症。

4. 发明申请

WO2005037206A3 ANTI-CANCER COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：抗癌化合物及其使用方法
公开(公告)号：WO2005037206A3
公开(公告)日：2005-08-04
申请号：PCT/US2004033697
申请日：2004-10-14
申请人： GTX INC , STEINER MITCHELL S , MILLER DUANE D , VEVERKA KAREN A , BARRETT CHRISTINA , HONG SEOUNG-SOO
发明人： STEINER MITCHELL S , MILLER DUANE D , VEVERKA KAREN A , BARRETT CHRISTINA , HONG SEOUNG-SOO
IPC分类号： A61K20060101 , A61K31/165 , A61K31/277 , A61K31/325 , A61K39/395 , C07C235/24 , C07C255/60 , C07C271/24 , C07C309/87 , C07C317/40 , C07C323/60 , C07D207/448 , C07F9/09
CPC分类号： C07D207/448 , C07C215/76 , C07C235/16 , C07C235/24 , C07C255/60 , C07C271/24 , C07C309/87 , C07C317/46 , C07C323/60 , C07D233/74
摘要： The present invention relates to a novel class of anti-cancer compounds which selectively target androgen receptor (AR)-expressing cancer, cells, such as prostate cancer cells and breast cancer cells, These agents comprise an androgen receptor (AR) binding moiety, which selectively tar-gets the compounds to (AR)-expressing cancer cells, and a cytotoxic alkylating moiety, such as a nitrogen mustard moiety, The inherent high density expression of the androgen receptor in certain cancers, such as prostate cancer and breast cancer, is thus used as a tool to selectively increase the intracellular concentration of cytotoxic compounds, such as alkylating agents, e,g. DNA alkylating agents, by selectively targeting the agents to the AR-expressing cancer cells. These agents, either alone or in a composition, are thus useful for treating, delaying the progression of, treating the recurrence of, suppressing, inhibiting or reducing the incidence of cancers characterized by the presence of AR-expressing cells, such as prostate cancer. Accordingly, the present invention provides a) methods of selectively killing an (AR)-expressing cancer, cell; b) methods of inducing apoptosis in an (AR) expressing cancer cell; c) methods of treating a cancer characterized by the presence of AR-expressing cells in a subject; d) methods of delaying the progression of a cancer characterized by the presence of AR-expressing cells in a subject; e) methods of treating the recurrence of a cancer characterized by the presence of AR-expressing cells in a subject; f) methods of suppressing, inhibiting or reducing the incidence of a cancer characterized by the presence of'AR-expressing cells in a subject; and g) methods of treating metastasis of a cancer characterized by the presence of AR.-expressing cells in a subject; by administering to the subject or by contacting the cancer cells with a compound comprising an androgen receptor, ligand moiety and an alkylating moiety, such as the novel compounds described herein.
摘要翻译：本发明涉及一种新型的抗癌化合物，其选择性靶向表达癌症的雄激素受体（AR），诸如前列腺癌细胞和乳腺癌细胞的细胞。这些药物包含雄激素受体（AR）结合部分，其中选择性地将化合物引向表达（AR）的癌细胞，以及细胞毒性烷基化部分，例如氮芥部分。某些癌症如前列腺癌和乳腺癌中雄激素受体的固有高密度表达是因此用作选择性地增加细胞毒性化合物如烷化剂的细胞内浓度的工具，例如， DNA烷化剂，通过选择性将靶向靶向表达AR的癌细胞。因此，单独或组合物中的这些药物可用于治疗，延缓进展，治疗复发，抑制，抑制或降低以表达AR的细胞如前列腺癌为特征的癌症的发病率。因此，本发明提供：a）选择性地杀死（AR）表达的癌症，细胞; b）在（AR）表达癌细胞中诱导凋亡的方法; c）治疗特征为在受试者中存在表达AR的细胞的癌症的方法; d）延迟在受试者中以表达AR的细胞存在为特征的癌症进展的方法; e）治疗特征为在受试者中存在表达AR的细胞的癌症复发的方法; f）抑制，抑制或降低癌症发生率的方法，其特征在于在受试者中存在α表达细胞; 和g）治疗癌症转移的方法，其特征在于在受试者中存在表达AR的细胞; 通过对受试者施用或通过使癌细胞与包含雄激素受体，配体部分和烷基化部分的化合物例如本文所述的新化合物接触。

5. 发明专利

AU2008209581B2 Nuclear receptor binding agents 未知
公开(公告)号：AU2008209581B2
公开(公告)日：2013-05-23
申请号：AU2008209581
申请日：2008-01-22
申请人： GTX INC
发明人： DALTON JAMES T , WU ZHONGZHI , MILLER DUANE D , MOHLER MICHAEL L , HONG SEOUNG-SOO , SRIVASTAVA DEVESH
IPC分类号： C07D217/24 , A01N43/42 , A01N55/02 , A61K31/555
摘要： The present invention relates to a novel class of nuclear receptor binding agents (NRBAs). The NRBAs are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, inflammatory diseases, oxidative stress related disorders such as Parkinson's and stroke, neurological disorders, ophthalamic disorders, cardiovascular disease, and obesity.

6. 发明专利

AU2006318400B2 Nuclear receptor binding agents 未知
公开(公告)号：AU2006318400B2
公开(公告)日：2012-04-05
申请号：AU2006318400
申请日：2006-11-28
申请人： GTX INC
发明人： DALTON JAMES T , NARAYANAN RAMESH , HE YALI , MILLER DUANE D , MOHLER MICHAEL L , HONG SEOUNG-SOO , WU ZHONGZHI , BARRETT CHRISTINA
IPC分类号： C07C233/65 , A61K31/165
摘要： The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.

7. 发明专利

NO20092822A 未知
公开(公告)号：NO20092822A
公开(公告)日：2009-10-21
申请号：NO20092822
申请日：2009-08-11
申请人： GTX INC
发明人： DALTON JAMES T , MILLER DUANE D , MOHLER MICHAEL L , WO ZHONGZHI , HONG SEOUNG-SOO , SRIVASTAVA DEVESH
IPC分类号： A61K31/4709 , C07D217/22 , C07D217/24
CPC分类号： A61K31/472 , C07D217/22 , C07D217/24 , Y02A50/463
摘要： A compound, or its optical isomer, pharmaceutically acceptable salt, pharmaceutical product, N- oxide, hydrate or any combination thereof, represented by the structure of Formula VI: wherein R 1 is hydrogen; R 2 is hydrogen, COOH, -C(=NH)-OH, -CH=CH 2 , hydroxyl, cyano, OCOR, alkenyl, OSO 2 CF 3 , or protected hydroxyl; R 3 , R 8 and R 9 are hydrogen; R 10 is hydrogen, halogen, CH=CHCO 2 H, CH=CHCO 2 R, -CH=CH 2 , cyano, aryl, 4-methoxyphenyl, 4-hydroxyphenyl, alkenyl, alkyl, or haloalkyl; R 11 is hydrogen, halogen, cyano, or SO 2 R; R 6 is hydrogen, halogen, or C 1 -C 6 -alkyl; R 7 is hydrogen or halogen; R' is hydrogen, Alk or COR; R" is hydrogen, Alk or COR; and R is alkyl, haloalkyl, dihaloalkyl, trihaloalkyl, aryl, benzyl, halogen, alkenyl, CN, or NO 2 ; and Alk is a linear alkyl of 1-7 carbons, branched alkyl of 1-7 carbons, or cycloalkyl of 3-8 carbons; for use in treating, delaying onset, reducing the incidence of, or reducing the severity of a fatty liver condition in a subject.

8. 发明专利

AU2008209581A1 Nuclear receptor binding agents 未知
公开(公告)号：AU2008209581A1
公开(公告)日：2008-07-31
申请号：AU2008209581
申请日：2008-01-22
申请人： GTX INC
发明人： DALTON JAMES T , HONG SEOUNG-SOO , MILLER DUANE D , WU ZHONGZHI , MOHLER MICHAEL L
IPC分类号： A01N43/42 , A01N55/02 , A61K31/555
摘要： A compound, or its optical isomer, pharmaceutically acceptable salt, pharmaceutical product, N- oxide, hydrate or any combination thereof, represented by the structure of Formula VI: wherein R 1 is hydrogen; R 2 is hydrogen, COOH, -C(=NH)-OH, -CH=CH 2 , hydroxyl, cyano, OCOR, alkenyl, OSO 2 CF 3 , or protected hydroxyl; R 3 , R 8 and R 9 are hydrogen; R 10 is hydrogen, halogen, CH=CHCO 2 H, CH=CHCO 2 R, -CH=CH 2 , cyano, aryl, 4-methoxyphenyl, 4-hydroxyphenyl, alkenyl, alkyl, or haloalkyl; R 11 is hydrogen, halogen, cyano, or SO 2 R; R 6 is hydrogen, halogen, or C 1 -C 6 -alkyl; R 7 is hydrogen or halogen; R' is hydrogen, Alk or COR; R" is hydrogen, Alk or COR; and R is alkyl, haloalkyl, dihaloalkyl, trihaloalkyl, aryl, benzyl, halogen, alkenyl, CN, or NO 2 ; and Alk is a linear alkyl of 1-7 carbons, branched alkyl of 1-7 carbons, or cycloalkyl of 3-8 carbons; for use in treating, delaying onset, reducing the incidence of, or reducing the severity of a fatty liver condition in a subject.

9. 发明专利

EA019833B1 ВЕЩЕСТВА, СВЯЗЫВАЮЩИЕ ЯДЕРНЫЕ РЕЦЕПТОРЫ 未知
公开(公告)号：EA019833B1
公开(公告)日：2014-06-30
申请号：EA200970707
申请日：2008-01-22
申请人： GTX INC
发明人： DALTON JAMES T , MILLER DUANE D , MOHLER MICHAEL L , WU ZHONGZHI , HONG SEOUNG-SOO , SRIVASTAVA DEVESH
IPC分类号： A01N43/42 , A01N55/02 , A61K31/555
摘要： Изобретениеотноситсяк новомуклассувеществ, связывающихядерныерецепторы (NRBA). Вещества, связывающиеядерныерецепторы, можноприменятьдляиспользованияв предотвращениии/илилечениирядазаболеванийи состояний, включаяпредотвращениеи лечениерака, такогокакракпростатыи ракмолочнойжелезы, остеопороз, гормональныезаболевания, воспалительныезаболевания, связанныес окислительнымстрессомзаболевания, такиекакболезньПаркинсонаи инсульт, неврологическиерасстройства, заболеванияглаз, сердечно-сосудистыезаболеванияи ожирение.

10. 发明专利

CA2631331C NUCLEAR RECEPTOR BINDING AGENTS 未知
公开(公告)号：CA2631331C
公开(公告)日：2016-08-09
申请号：CA2631331
申请日：2006-11-28
申请人： GTX INC
发明人： DALTON JAMES T , BARRETT CHRISTINA , HE YALI , HONG SEOUNG-SOO , MILLER DUANE D , MOHLER MICHAEL L , NARAYANAN RAMESH , WU ZHONGZHI
IPC分类号： C07C233/65 , A61K31/166
摘要： The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.

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