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1. 发明申请

US20100280107A1 TREATING BENIGN PROSTATE HYPERPLASIA WITH SARMS 失效
标题翻译：用SARMS处理BENIGN PROSTATE HYPERPLASIA
公开(公告)号：US20100280107A1
公开(公告)日：2010-11-04
申请号：US12826842
申请日：2010-06-30
申请人： James T. DALTON , Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka , Wenqing Gao
发明人： James T. DALTON , Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka , Wenqing Gao
IPC分类号： A61K31/277 , A61P13/08 , A61P17/14 , A61K31/167
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-α 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, N-oxide, or any combination thereof as described herein. This invention also provides a method of inhibiting a 5-α reductase type 1 and/or type 2 enzyme, comprising contacting the enzyme with an effective 5-α 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-α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，N-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-α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。

2. 发明申请

US20100144871A1 Treating muscle wasting with selective androgen receptor modulators 失效
标题翻译：用选择性雄激素受体调节剂治疗肌肉消瘦
公开(公告)号：US20100144871A1
公开(公告)日：2010-06-10
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： A61K31/277 , A61P21/00 , 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。

3. 发明授权

US07705182B2 Multi-substituted selective androgen receptor modulators and methods of use thereof 有权
标题翻译：多取代的选择性雄激素受体调节剂及其使用方法
公开(公告)号：US07705182B2
公开(公告)日：2010-04-27
申请号：US10371155
申请日：2003-02-24
申请人： James T. Dalton , Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka , Dong Jin Hwang , Jiyun Chen
发明人： James T. Dalton , Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka , Dong Jin Hwang , Jiyun Chen
IPC分类号： C07C233/05 , A61K31/16
CPC分类号： C07C235/24
摘要： This invention provides androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; and/or g) decreasing the incidence of, halting or causing a regression of prostate cancer.
摘要翻译：本发明提供雄激素受体靶向剂（ARTA）。这些药剂定义了一种新的化合物亚类，它们是选择性雄激素受体调节剂（SARM）。已经发现几种SARM化合物对雄激素受体具有非甾类化合物的意想不到的雄激素和合成代谢活性。已经发现其他SARM化合物对雄激素受体具有非甾类配体的意想不到的抗雄激素活性。 SARM化合物，单独或作为组合物，可用于a）男性避孕; b）治疗各种激素相关病症，例如与老年雄性雄激素降低有关的病症（ADAM），如疲劳，抑郁，性欲降低，性功能障碍，勃起功能障碍，性腺机能减退，骨质疏松症，脱发，贫血，肥胖，肌营养不良，骨质减少，骨质疏松症，良性前列腺增生，情绪和认知和前列腺癌的改变; c）治疗与男性雄激素降低相关的病症（ADIF），如性功能障碍，性欲降低，性腺机能减退，肌营养不良，骨质减少，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖，子宫内膜异位症，乳腺癌癌症，子宫癌和卵巢癌; d）治疗和/或预防急性和/或慢性肌肉消瘦病症; e）预防和/或治疗干眼症状; f）口服雄激素替代疗法; 和/或g）降低前列腺癌的发生率，停止或导致消退。

4. 发明授权

US06838484B2 Formulations comprising selective androgen receptor modulators 有权
标题翻译：包含选择性雄激素受体调节剂的制剂
公开(公告)号：US06838484B2
公开(公告)日：2005-01-04
申请号：US10270232
申请日：2002-10-15
申请人： Mitchell S. Steiner , Karen A. Veverka , James T. Dalton , Duane D. Miller , Yali He , Donghua Yin
发明人： Mitchell S. Steiner , Karen A. Veverka , James T. Dalton , Duane D. Miller , Yali He , Donghua Yin
IPC分类号： A61K31/167 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/24 , C07D209/08 , C07D215/22 , C07D215/227 , C07D271/12 , G01N30/72 , G01N30/88 , G01N33/543 , G01N33/74 , A61K31/16
CPC分类号： A61K31/167 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/24 , C07D209/08 , C07D215/227 , C07D271/12 , G01N30/7233 , G01N33/5438 , G01N33/74 , G01N2030/8813
摘要： The present invention relates to pharmaceutical compositions and formulations comprising a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia,osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; and/or e) decreasing the incidence of, halting or causing a regression of prostate cancer. The present invention provides pharmaceutical compositions comprising the selective androgen receptor modulator compounds, together with pharmaceutically acceptable excipients.
摘要翻译：本发明涉及包含新型雄激素受体靶向剂（ARTA）的药物组合物和制剂，其表现出雄激素受体的非甾体配体的雄激素和合成代谢活性。这些药剂定义了一种新的选择性雄激素受体调节剂（SARM）的化合物亚类，它们可用于a）男性避孕; b）治疗各种激素相关病症，例如与老年雄性雄激素降低有关的病症（ADAM），如疲劳，抑郁，性欲降低，性功能障碍，勃起功能障碍，性腺机能减退，骨质疏松症，脱发，贫血，肥胖，肌营养不良，骨质减少，骨质疏松症，良性前列腺增生，情绪和认知和前列腺癌的改变; c）治疗与男性雄激素降低相关的病症（ADIF），如性功能障碍，性欲降低，性腺机能减退，肌营养不良，骨质减少，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖，子宫内膜异位症，乳腺癌癌症，子宫癌和卵巢癌; d）治疗和/或预防慢性肌肉消瘦; 和/或e）降低前列腺癌的发生率，停止或导致消退。本发明提供了包含选择性雄激素受体调节剂化合物以及药学上可接受的赋形剂的药物组合物。

5. 发明授权

US07968721B2 Large-scale synthesis of selective androgen receptor modulators 有权
标题翻译：大规模合成选择性雄激素受体调节剂
公开(公告)号：US07968721B2
公开(公告)日：2011-06-28
申请号：US10754626
申请日：2004-01-12
申请人： Duane D. Miller , Karen A. Veverka , Kiwon Chung
发明人： Duane D. Miller , Karen A. Veverka , Kiwon Chung
IPC分类号： C07D215/00 , C07D209/04 , C07C205/00 , C07C391/00 , C07C311/00 , C07C233/00 , C07C235/00
CPC分类号： C07C231/12 , C07C235/24
摘要： This invention relates to a process for preparing a selective androgen receptor modulator (SARM) compound represented by the structure of formula I: wherein X is O; and T, Z, Y, Q, R and R1 are defined herein. The process includes coupling between an amide of formula II and a phenol of formula III followed by a purification step consisting of precipitating the compound of formula (I) in a mixture of alcohol and water alone.
摘要翻译：本发明涉及制备由式I结构表示的选择性雄激素受体调节剂（SARM）化合物的方法：其中X为O; 并且本文定义了T，Z，Y，Q，R和R1。该方法包括在式II的酰胺与式III的苯酚之间偶联，随后纯化步骤包括在醇和水的混合物中单独沉淀式（I）的化合物。

6. 发明申请

US20110082212A1 MULTI-SUBSTITUTED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：多选择性选择性受体调节剂及其使用方法
公开(公告)号：US20110082212A1
公开(公告)日：2011-04-07
申请号：US12880389
申请日：2010-09-13
申请人： James T. Dalton , Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka , Dong Jin Hwang , Jiyun Chen
发明人： James T. Dalton , Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka , Dong Jin Hwang , Jiyun Chen
IPC分类号： A61K31/167 , C07C233/15 , A61P15/16 , A61P35/00 , A61P27/04
CPC分类号： C07C235/24
摘要： This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; and/or g) decreasing the incidence of, halting or causing a regression of prostate cancer.
摘要翻译：本发明提供一类雄激素受体靶向剂（ARTA）。这些药剂定义了一种新的化合物亚类，它们是选择性雄激素受体调节剂（SARM）。已经发现几种SARM化合物对雄激素受体具有非甾类化合物的意想不到的雄激素和合成代谢活性。已经发现其他SARM化合物对雄激素受体具有非甾类配体的意想不到的抗雄激素活性。 SARM化合物，单独或作为组合物，可用于a）男性避孕; b）治疗各种激素相关病症，例如与老年雄性雄激素降低有关的病症（ADAM），如疲劳，抑郁，性欲降低，性功能障碍，勃起功能障碍，性腺机能减退，骨质疏松症，脱发，贫血，肥胖，肌营养不良，骨质减少，骨质疏松症，良性前列腺增生，情绪和认知和前列腺癌的改变; c）治疗与男性雄激素降低相关的病症（ADIF），如性功能障碍，性欲降低，性腺机能减退，肌营养不良，骨质减少，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖，子宫内膜异位症，乳腺癌癌症，子宫癌和卵巢癌; d）治疗和/或预防急性和/或慢性肌肉消瘦病症; e）预防和/或治疗干眼症状; f）口服雄激素替代疗法; 和/或g）降低前列腺癌的发生率，停止或导致消退。

7. 发明授权

US07776921B2 Treating benign prostate hyperplasia with SARMS 失效
标题翻译：用SARMS治疗良性前列腺增生
公开(公告)号：US07776921B2
公开(公告)日：2010-08-17
申请号：US10359270
申请日：2003-02-06
申请人： James T. Dalton , Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka , Wenqing Gao
发明人： James T. Dalton , Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka , Wenqing Gao
IPC分类号： A61K31/16
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-α 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, N-oxide, or any combination thereof as described herein. This invention also provides a method of inhibiting a 5-α reductase type 1 and/or type 2 enzyme, comprising contacting the enzyme with an effective 5-α 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-α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，N-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-α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。

8. 发明授权

US07622503B2 Selective androgen receptor modulators and methods of use thereof 有权
标题翻译：选择性雄激素受体调节剂及其使用方法
公开(公告)号：US07622503B2
公开(公告)日：2009-11-24
申请号：US11146427
申请日：2005-06-07
申请人： James T. Dalton , Duane D. Miller , Karen A. Veverka
发明人： James T. Dalton , Duane D. Miller , Karen A. Veverka
IPC分类号： A61K31/275 , A61K31/165
CPC分类号： A61K31/277
摘要： This invention provides SARM compounds and their use in treating a variety of diseases or conditions in a subject, including, inter-alia, a muscle wasting disease and/or disorder or a bone-related disease and/or disorder.
摘要翻译：本发明提供了SARM化合物及其在治疗受试者中的各种疾病或病症的用途，包括特别是肌肉消耗疾病和/或病症或骨相关疾病和/或病症。

9. 发明授权

US07595402B2 Prodrugs of selective androgen receptor modulators and methods of use thereof 有权
标题翻译：选择性雄激素受体调节剂的前药及其使用方法
公开(公告)号：US07595402B2
公开(公告)日：2009-09-29
申请号：US11013214
申请日：2004-12-16
申请人： Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka , James T. Dalton
发明人： Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka , James T. Dalton
IPC分类号： C07D215/38
CPC分类号： C07F9/091 , A61K31/4704 , A61K47/548 , C07C235/24
摘要： The present invention provides prodrugs of selective androgen receptor modulators (SARMs), and their use in treating or reducing the incidence of osteoporosis, a variety of hormone-related conditions, conditions associated with Androgen Decline in Aging Male (ADAM); conditions associated with Androgen Decline in Female (ADIF), and muscular wasting conditions, obesity, dry eye conditions, and prostate cancer. The prodrugs are also useful in oral androgen replacement therapy and male contraception.
摘要翻译：本发明提供选择性雄激素受体调节剂（SARM）的前药，以及它们在治疗或降低骨质疏松症发生率，多种激素相关病症，与老年男性（ADAM）雄激素衰退相关的病症中的用途。与雄激素降低（ADIF）相关的病症，肌肉消瘦症，肥胖症，干眼症和前列腺癌。前药还可用于口服雄激素替代疗法和男性避孕。

10. 发明授权

US08088828B2 Treating benign prostate hyperplasia with SARMS 失效
标题翻译：用SARMS治疗良性前列腺增生
公开(公告)号：US08088828B2
公开(公告)日：2012-01-03
申请号：US12826842
申请日：2010-06-30
申请人： James T. Dalton , Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka , Wenqing Gao
发明人： James T. Dalton , Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka , Wenqing Gao
IPC分类号： A61K31/16
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-α 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, N-oxide, or any combination thereof as described herein. This invention also provides a method of inhibiting a 5-α reductase type 1 and/or type 2 enzyme, comprising contacting the enzyme with an effective 5-α 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-α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，N-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-α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。

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