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1. 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。

2. 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。

3. 发明申请

WO2008011072A3 SELECTIVE ANDROGEN RECEPTOR MODULATORS, ANALOGS AND DERIVATIVES THEREOF AND USES THEREOF 审中-公开
标题翻译：选择性安定剂受体调节剂，其模拟物及其衍生物及其用途
公开(公告)号：WO2008011072A3
公开(公告)日：2008-06-05
申请号：PCT/US2007016311
申请日：2007-07-19
申请人： OSURF OHIO STATE UNIVERSITY RE , UNIV TENNESSEE RES FOUNDATION , DALTON JAMES T , MILLER DUANE D , RAKOV IGOR , BOHL CASEY , MOHLER MICHAEL L
发明人： DALTON JAMES T , MILLER DUANE D , RAKOV IGOR , BOHL CASEY , MOHLER MICHAEL L
IPC分类号： C07C255/00 , C07D207/00
CPC分类号： C07D241/04 , C07C255/54 , C07C255/58 , C07C255/60 , C07C317/46 , C07C323/60 , C07C335/18 , C07D233/86
摘要： This invention provides new compounds and uses thereof in treating a variety of diseases or conditions in a subject, including,inter alia, prostate cancer, muscle wasting diseases and/or disorders or a bone-related diseases and/or disorders.
摘要翻译：本发明提供了新的化合物及其用于治疗受试者中各种疾病或病症的新用途，包括前列腺癌，肌肉消瘦疾病和/或病症或与骨相关的疾病和/或病症。

4. 发明申请

WO2008011073A2 SELECTIVE ANDROGEN RECEPTOR MODULATORS, ANALOGS AND DERIVATIVES THEREOF AND USES THEREOF 审中-公开
标题翻译：选择性雄激素受体调节剂，类似物及其衍生物及其用途
公开(公告)号：WO2008011073A2
公开(公告)日：2008-01-24
申请号：PCT/US2007016312
申请日：2007-07-19
申请人： OSURF , UNIV TENNESSEE RES FOUNDATION , DALTON JAMES T , MILLER DUANE D , RAKOV IGOR , BOHL CASEY , MOHLER MICHAEL L
发明人： DALTON JAMES T , MILLER DUANE D , RAKOV IGOR , BOHL CASEY , MOHLER MICHAEL L
IPC分类号： A61K31/473
CPC分类号： C07D241/04 , C07C255/54 , C07C255/58 , C07C255/60 , C07C317/46 , C07C323/60 , C07C335/18 , C07D233/86
摘要： This invention provides nuclear hormone receptor binding compounds, compositions comprising the same and methods of uses thereof in treating a variety of diseases or conditions in a subject, including, inter-alia, prostate cancer and/or diseases or disorders of bone and muscle.
摘要翻译：本发明提供了核激素受体结合化合物，包含其的组合物以及其在治疗受试者中的多种疾病或病症（包括尤其包括前列腺癌和/或骨骼和肌肉疾病或病症）中的用途的方法。

5. 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。

6. 发明申请

WO2004035739A3 TREATING ANDROGEN DECLINE IN AGING MALE (ADAM)-ASSOCIATED CONDITIONS WITH SARMS 审中-公开
标题翻译：用SARMS治疗老年男性（ADAM）相关病症的雄激素降低
公开(公告)号：WO2004035739A3
公开(公告)日：2004-09-30
申请号：PCT/US0332513
申请日：2003-10-14
申请人： GTX INC , DALTON JAMES T , MILLER DUANE D , STEINER MITCHELL S , VEVERKA KAREN A
发明人： DALTON JAMES T , MILLER DUANE D , STEINER MITCHELL S , VEVERKA KAREN A
IPC分类号： C07K14/72 , A61K31/165 , A61K31/40 , A61K31/41 , A61K31/435 , A61K31/44
CPC分类号： C07K14/721
摘要： The present invention provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of an Androgen Decline in Aging Male (ADAM)- associated condition in a male subject, by administering to the subject a selective androgen receptor modulator (SARM) compound and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, crystal, or any combination thereof. The present invention further provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of sexual dysfunction, decreased sexual libido, erectile dysfunction, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, benign prostate hyperplasia or prostate cancer due to ADAM in a male subject, by administering to the subject a selective androgen receptor modulator (SARM) compound and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, crystal, or any combination thereof.
摘要翻译：本发明提供了通过向受试者施用选择性雄激素受体调节剂（SARM）化合物来治疗，预防，抑制，抑制或减少男性受试者中老化雄性（ADAM）相关病症中雄激素降低的发生的方法和/或其类似物，衍生物，异构体，代谢物，药学上可接受的盐，药物产品，水合物，N-氧化物，前药，多晶型物，晶体或其任何组合。本发明进一步提供治疗，预防，抑制，抑制或减少性功能障碍，性欲减退，勃起功能障碍，性腺机能减退症，肌肉减少症，骨质减少症，骨质疏松症，认知和情绪改变，抑郁症，贫血症，脱发（SARM）化合物和/或其类似物，衍生物，异构体，代谢物，药学上可接受的盐，药物产品或药物产品给予受试者，所述受试者是男性受试者中由于ADAM引起的肥胖，良性前列腺增生或前列腺癌。水合物，N-氧化物，前药，多晶型物，晶体或其任何组合。

7. 发明申请

WO2012037155A2 TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：酪氨酸激酶抑制剂
公开(公告)号：WO2012037155A2
公开(公告)日：2012-03-22
申请号：PCT/US2011051442
申请日：2011-09-13
申请人： GTX INC , DALTON JAMES T , MILLER DUANE D , HWANG DONG JIN , COSS CHRISTOPHER C
发明人： DALTON JAMES T , MILLER DUANE D , HWANG DONG JIN , COSS CHRISTOPHER C
IPC分类号： A61K31/4439 , A61P35/00 , C07D487/04 , C12N9/99
CPC分类号： C07D487/04
摘要： The present disclosure relates to the field of tyrosine kinase enzyme inhibition, in particular anaplastic lymphoma kinase (ALK) inhibition using novel small molecules. Provided are compounds capable to modulate ALK activity, compositions that comprise the compounds, and methods of using the compounds for the treatment or prevention of diseases or conditions that are characterized by ALK activity or expression.
摘要翻译：本公开涉及酪氨酸激酶抑制的领域，特别是使用新型小分子的间变性淋巴瘤激酶（ALK）抑制。提供能够调节ALK活性的化合物，包含该化合物的组合物，以及使用该化合物治疗或预防以ALK活性或表达为特征的疾病或病症的方法。

8. 发明申请

WO2012027481A1 COMPOUNDS FOR TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的化合物
公开(公告)号：WO2012027481A1
公开(公告)日：2012-03-01
申请号：PCT/US2011048980
申请日：2011-08-24
申请人： GTX INC , UNIV TENNESSEE REASEARCH FOUNDATION , DALTON JAMES T , MILLER DUANE D , LI CHIEN-MING , AHN SUNJOO , LU YAN , WANG ZHAO , CHEN JIANJUN , LI WEI , DUKE CHARLES
发明人： DALTON JAMES T , MILLER DUANE D , LI CHIEN-MING , AHN SUNJOO , LU YAN , WANG ZHAO , CHEN JIANJUN , LI WEI , DUKE CHARLES
IPC分类号： A01N43/50 , A61K31/415
CPC分类号： A61K31/415 , C07D233/60 , C07D263/32 , C07D277/24 , C07D277/42 , C07D403/04 , C07D403/12 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.
摘要翻译：本发明涉及具有抗癌活性的新化合物，制备这些化合物的方法及其用于治疗癌症和药物抗性肿瘤的用途，例如，黑素瘤，转移性黑素瘤，耐药性黑素瘤，前列腺癌和耐药前列腺癌。

9. 发明申请

WO03065992A2 TREATING BENIGN PROSTATE HYPERPLASIA WITH SARMS 审中-公开
标题翻译：用SARMS处理BENIGN PROSTATE HYPERPLASIA
公开(公告)号：WO03065992A2
公开(公告)日：2003-08-14
申请号：PCT/US0303447
申请日：2003-02-06
申请人： GTX INC , STEINER MITCHELL S , VEVERKA KAREN A , MILLER DUANE D , DALTON JAMES T , CHUNG KIWON , GAO WENQING
发明人： STEINER MITCHELL S , VEVERKA KAREN A , MILLER DUANE D , DALTON JAMES T , CHUNG KIWON , GAO WENQING
IPC分类号： A61K45/00 , A61K31/00 , A61K31/167 , A61K31/277 , A61K31/56 , A61P13/08 , A61P43/00 , A61K
CPC分类号： A61K31/277 , A61K31/00 , A61K31/167 , A61K31/56
摘要： This invention provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of benign prostate hyperplasia in a male subject, by administering to the subject a selective androgen receptor modulator(SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein. This invention also provides a method of treating a subject suffering from hair loss, comprising the step of administering to the subject a therapeutically effective amount of a 5-a reductase enzyme type 1 and /or type 2 inhibitor, wherein said inhibitor is a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite,pharmaceutically acceptable salt, pharmaceutical product, hydrate, Woxide, or any combination thereof as described herein. This invention also provides a method of inhibiting a 5-a reductase type 1 and/or type 2 enzyme, comprising contacting the enzyme with an effective 5-a reductase inhibitory amount of a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof, as described herein.
摘要翻译：本发明提供了通过向受试者施用选择性雄激素受体调节剂（SARM）和/或其类似物，衍生物，异构体，代谢物来治疗，预防，抑制或降低男性患者良性前列腺增生的发生率的方法，药学上可接受的盐，药物产品，水合物，N-氧化物或其任何组合。本发明还提供了一种治疗脱发患者的方法，包括向受试者施用治疗有效量的1型和/或2型抑制剂的5-a还原酶的步骤，其中所述抑制剂是选择性雄激素受体调节剂（SARM）和/或其类似物，衍生物，异构体，代谢物，药学上可接受的盐，药物产品，水合物，氧化物或其任何组合。本发明还提供抑制1型和/或2型5α还原酶的方法，包括使酶与有效的5-a还原酶抑制量的选择性雄激素受体调节剂（SARM）和/或其类似物接触，衍生物，异构体，代谢物，药学上可接受的盐，药物产品，水合物，N-氧化物或其任何组合。

10. 发明申请

WO2007027582A3 TREATING RENAL DISEASE, BURNS, WOUNDS AND SPINAL CORD INJURY WITH SELECTIVE ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：用选择性的受体调节剂治疗肾上腺疾病，疱疹，伤口和脊髓损伤
公开(公告)号：WO2007027582A3
公开(公告)日：2007-10-25
申请号：PCT/US2006033490
申请日：2006-08-28
申请人： GTX INC , DALTON JAMES T , MILLER DUANE D
发明人： DALTON JAMES T , MILLER DUANE D
IPC分类号： A01N37/18 , C07C233/00
CPC分类号： A61K31/165 , A61K31/277 , A61K31/32 , A61K31/405 , A61K31/4704 , A61K31/4709 , A61K31/555 , A61K31/675
摘要： This invention provides: 1) a method of treating a subject suffering from, or predisposed to a kidney disease or disorder; 2) a method of treating a subject suffering from a wound, or reducing the incidence of, or mitigating the severity of a wound in a subject; 3) a method of treating a subject suffering from a burn, or reducing the incidence of, or mitigating the severity of a burn in a subject, comprising the step of administering to said subject a selective androgen receptor modulator (SARM) compound; 4) a method of treating a subject suffering from a spinal cord injury, by administering to the subject a selective androgen receptor modulator (SARM) and/or an analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, impurity or crystal of said SARM compound, or any combination thereof.
摘要翻译：本发明提供：1）治疗患有或易患肾病或病症的受试者的方法; 2）治疗患有伤口的受试者或降低受试者的伤口的发生或减轻其严重程度的方法; 3）治疗患有烧伤的受试者或降低受试者的烧伤的发生或减轻其严重程度的方法，其包括向所述受试者施用选择性雄激素受体调节剂（SARM）化合物的步骤; 4）通过向受试者施用选择性雄激素受体调节剂（SARM）和/或其类似物，衍生物，异构体，代谢物，药学上可接受的盐，药物产品，水合物N，治疗患有脊髓损伤的受试者的方法氧化物，前药，多晶型物，杂质或结晶，或其任何组合。

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