公开(公告)号：US08445534B2

公开(公告)日：2013-05-21

申请号：US12632619

申请日：2009-12-07

申请人： James T. Dalton ,  Duane D. Miller ,  Donghua Yin ,  Yali He

发明人： James T. Dalton ,  Duane D. Miller ,  Donghua Yin ,  Yali He

IPC分类号： A61K31/275

CPC分类号： C07C235/24 ,  A61K31/16 ,  A61K31/167 ,  A61K31/277 ,  C07C255/60

摘要： This invention provides methods for treatment and inhibition of a male subject having an Androgen Decline in Aging Male (ADAM)-associated condition, for example sexual dysfunction, decreased sexual libido, erectile dysfunction, hypogonadism, sarcopenia, osteopenia, osteoporosis, an alteration in cognition and mood, depression, anemia, hair loss, obesity, muscle loss, dry eye, memory loss, benign prostate hyperplasia and/or prostate cancer, 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, pro-drug, polymorph, crystal, or any combination thereof.

摘要翻译： 本发明提供了用于治疗和抑制雄性雄性雄激素降低（ADAM）相关病症的男性受试者的方法，例如性功能障碍，性欲性降低，勃起功能障碍，性腺机能减退，肌肉减少症，骨质减少症，骨质疏松症，认知改变 通过向受试者施用选择性雄激素受体调节剂（SARM）化合物和/或其类似物，通过向受试者施用选择性雄激素受体调节剂（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，水合物，N-氧化物，前药，多晶型物，晶体或其任何组合。

公开(公告)号：US08309603B2

公开(公告)日：2012-11-13

申请号：US12730094

申请日：2010-03-23

申请人： James T. Dalton ,  Duane D. Miller ,  Jeff Kearbey

发明人： James T. Dalton ,  Duane D. Miller ,  Jeff Kearbey

IPC分类号： A61K31/275

CPC分类号： C07C255/60 ,  A23K20/111 ,  A23K50/10 ,  A23K50/30

摘要： This invention is directed to a feed composition and method of affecting the carcass composition by increasing the lean mass, reducing the fat mass, and/or reducing the percent fat mass comprising SARM compounds.

摘要翻译： 本发明涉及通过增加瘦体重，降低脂肪量和/或降低包含SARM化合物的脂肪百分比来影响胴体成分的饲料组合物和方法。

公开(公告)号：US08110562B2

公开(公告)日：2012-02-07

申请号：US11826987

申请日：2007-07-19

申请人： James T. Dalton ,  Duane D. Miller ,  Igor Rakov ,  Casey Bohl ,  Michael L. Mohler

发明人： James T. Dalton ,  Duane D. Miller ,  Igor Rakov ,  Casey Bohl ,  Michael L. Mohler

IPC分类号： A61K31/473 ,  A61K31/675 ,  C07D219/04 ,  C07D215/06

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： 本发明提供核激素受体结合化合物，包含其的组合物及其用于治疗受试者中各种疾病或病症的用途，包括尤其是前列腺癌和/或骨骼和肌肉的疾病或病症。

公开(公告)号：US08008348B2

公开(公告)日：2011-08-30

申请号：US10861923

申请日：2004-06-07

申请人： Mitchell S. Steiner ,  Karen A. Veverka ,  James T. Dalton ,  Duane D. Miller

发明人： Mitchell S. Steiner ,  Karen A. Veverka ,  James T. Dalton ,  Duane D. Miller

IPC分类号： A61K31/275 ,  A61K31/32 ,  A61K31/16 ,  A61K31/165

CPC分类号： A61K31/00 ,  A61K31/167

摘要： This invention provides: 1) a method of treating a subject suffering from a muscle wasting disorder; 2) a method of preventing a muscle wasting disorder in a subject; 3) a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; 4) a method of treating, preventing, inhibiting, reducing or suppressing muscle wasting in a subject suffering from a muscle wasting disorder; and/or 5) a method of treating, preventing, inhibiting, reducing or suppressing muscle protein catabolism in a subject suffering from a muscle wasting disorder, 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）治疗患有肌肉消瘦障碍的受试者的方法; 2）预防受试者的肌肉消瘦障碍的方法; 3）治疗，预防，抑制，抑制或减轻患有肌肉消瘦障碍的受试者的肌肉损失的方法; 4）一种治疗，预防，抑制，减少或抑制患有肌肉消瘦障碍的受试者的肌肉消瘦的方法; 和/或5）通过向受试者施用选择性雄激素受体调节剂（SARM）和/或类似物衍生物，治疗，预防，抑制，减少或抑制患有肌肉消瘦疾病的受试者的肌肉蛋白分解代谢的方法 ，所述SARM化合物的异构体，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，杂质或晶体，或其任何组合。

公开(公告)号：US07855229B2

公开(公告)日：2010-12-21

申请号：US11220414

申请日：2005-09-07

申请人： James T. Dalton ,  Duane D. Miller ,  Mitchell S. Steiner ,  Karen A. Veverka

发明人： James T. Dalton ,  Duane D. Miller ,  Mitchell S. Steiner ,  Karen A. Veverka

IPC分类号： A61K31/275 ,  A61K31/32 ,  A61K31/16 ,  A61K31/165

CPC分类号： A61K31/277

摘要： This invention provides: 1) a method of treating a subject suffering from a muscle wasting disorder; 2) a method of preventing a muscle wasting disorder in a subject; 3) a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; 4) a method of treating, preventing, inhibiting, reducing or suppressing muscle wasting in a subject suffering from a muscle wasting disorder; and/or 5) a method of treating, preventing, inhibiting, reducing or suppressing muscle protein catabolism in a subject suffering from a muscle wasting disorder, 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）治疗患有肌肉消瘦障碍的受试者的方法; 2）预防受试者的肌肉消瘦障碍的方法; 3）治疗，预防，抑制，抑制或减轻患有肌肉消瘦障碍的受试者的肌肉损失的方法; 4）一种治疗，预防，抑制，减少或抑制患有肌肉消瘦障碍的受试者的肌肉消瘦的方法; 和/或5）通过向受试者施用选择性雄激素受体调节剂（SARM）和/或类似物衍生物，治疗，预防，抑制，减少或抑制患有肌肉消瘦疾病的受试者的肌肉蛋白分解代谢的方法 ，所述SARM化合物的异构体，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，杂质或晶体，或其任何组合。

公开(公告)号：US20100249228A1

公开(公告)日：2010-09-30

申请号：US12730094

申请日：2010-03-23

申请人： James T. Dalton ,  Duane D. Miller ,  Jeffrey D. Kearbey

发明人： James T. Dalton ,  Duane D. Miller ,  Jeffrey D. Kearbey

IPC分类号： A61K31/277 ,  C07C235/24 ,  A61K31/167 ,  C07C255/60 ,  A61P3/02

CPC分类号： C07C255/60 ,  A23K20/111 ,  A23K50/10 ,  A23K50/30

摘要： This invention is directed to a feed composition and method of affecting the carcass composition by increasing the lean mass, reducing the fat mass, and/or reducing the percent fat mass comprising SARM compounds.

摘要翻译： 本发明涉及通过增加瘦体重，降低脂肪量和/或降低包含SARM化合物的脂肪百分比来影响胴体成分的饲料组合物和方法。

公开(公告)号：US20100137430A1

公开(公告)日：2010-06-03

申请号：US12632619

申请日：2009-12-07

申请人： James T. DALTON ,  Duane D. Miller ,  Donghua Yin ,  Yali He

发明人： James T. DALTON ,  Duane D. Miller ,  Donghua Yin ,  Yali He

IPC分类号： A61K31/277 ,  A61K31/167 ,  A61P5/26

CPC分类号： C07C235/24 ,  A61K31/16 ,  A61K31/167 ,  A61K31/277 ,  C07C255/60

摘要： This invention provides methods for treatment and inhibition of a male subject having an Androgen Decline in Aging Male (ADAM)-associated condition, for example sexual dysfunction, decreased sexual libido, erectile dysfunction, hypogonadism, sarcopenia, osteopenia, osteoporosis, an alteration in cognition and mood, depression, anemia, hair loss, obesity, muscle loss, dry eye, memory loss, benign prostate hyperplasia and/or prostate cancer, 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, pro-drug, polymorph, crystal, or any combination thereof.

摘要翻译： 本发明提供了用于治疗和抑制雄性雄性雄激素降低（ADAM）相关病症的男性受试者的方法，例如性功能障碍，性欲性降低，勃起功能障碍，性腺机能减退，肌肉减少症，骨质减少症，骨质疏松症，认知改变 通过向受试者施用选择性雄激素受体调节剂（SARM）化合物和/或其类似物，通过向受试者施用选择性雄激素受体调节剂（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，水合物，N-氧化物，前药，多晶型物，晶体或其任何组合。

公开(公告)号：US07662842B2

公开(公告)日：2010-02-16

申请号：US11458648

申请日：2006-07-19

申请人： Duane D. Miller ,  James T. Dalton ,  Veeresa Gududuru ,  Eunju Hurh

发明人： Duane D. Miller ,  James T. Dalton ,  Veeresa Gududuru ,  Eunju Hurh

IPC分类号： A61K31/426 ,  A61K31/427 ,  C07D417/02

CPC分类号： C07D277/06 ,  C07D277/14 ,  C07D277/20 ,  C07D277/34 ,  C07D277/56 ,  C07D417/04

摘要： Substituted thiazolidinone carboxylic acid amides and substituted thiazolidine carboxylic acid amides according to formulae (I) and (II) are disclosed where the various substituent groups are as defined in the specification. Methods of making these compounds, pharmaceutical compositions containing the compounds, and their use, particularly for treating or preventing cancer, are also disclosed.

摘要翻译： 公开了根据式（I）和（II）的取代的噻唑烷酮羧酸酰胺和取代的噻唑烷羧酸酰胺，其中各种取代基如说明书中所定义。 还公开了制备这些化合物的方法，含有这些化合物的药物组合物及其用途，特别是用于治疗或预防癌症的方法。

公开(公告)号：US07547728B2

公开(公告)日：2009-06-16

申请号：US10310150

申请日：2002-12-05

申请人： Mitchell S. Steiner ,  Karen A. Veverka ,  James T. Dalton ,  Duane D. Miller

发明人： Mitchell S. Steiner ,  Karen A. Veverka ,  James T. Dalton ,  Duane D. Miller

IPC分类号： A61K31/275 ,  A61K31/32 ,  A61K31/16 ,  A61K31/165

CPC分类号： A61K31/00 ,  A61K31/167 ,  Y02A50/465

摘要： This invention provides: 1) a method of treating a subject suffering from a muscle wasting disorder; 2) a method of preventing a muscle wasting disorder in a subject; 3) a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; 4) a method of treating, preventing, inhibiting, reducing or suppressing muscle wasting in a subject suffering from a muscle wasting disorder; and/or 5) a method of treating, preventing, inhibiting, reducing or suppressing muscle protein catabolism in a subject suffering from a muscle wasting disorder, 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.

摘要翻译： 本发明提供：1）治疗患有肌肉消瘦障碍的受试者的方法; 2）预防受试者的肌肉消瘦障碍的方法; 3）治疗，预防，抑制，抑制或减轻患有肌肉消瘦障碍的受试者的肌肉损失的方法; 4）一种治疗，预防，抑制，减少或抑制患有肌肉消瘦障碍的受试者的肌肉消瘦的方法; 和/或5）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，治疗，预防，抑制，减少或抑制患有肌肉消瘦疾病的受试者中的肌肉蛋白分解代谢的方法 ，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。

公开(公告)号：US20090062341A1

公开(公告)日：2009-03-05

申请号：US11604884

申请日：2006-11-28

申请人： James T. Dalton ,  Christina Barrett ,  Yali He ,  Seoung-Soo Hong ,  Duane D. Miller ,  Michael L. Mohler ,  Ramesh Narayanan ,  Zhongzhi Wu

发明人： James T. Dalton ,  Christina Barrett ,  Yali He ,  Seoung-Soo Hong ,  Duane D. Miller ,  Michael L. Mohler ,  Ramesh Narayanan ,  Zhongzhi Wu

IPC分类号： A61K31/4545 ,  C07C233/64 ,  A61K31/166 ,  A61K31/445 ,  C07D401/02 ,  C07K14/72 ,  C07D211/60 ,  C07D213/81 ,  A61K31/44

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： 本发明涉及新型选择性雌激素受体调节剂（SERM）。 SERM化合物可用于预防和/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，潮热或血管舒缩症状，神经系统疾病， 心血管疾病和肥胖。