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1. 发明申请

US20180186807A1 COMPOUNDS AND USES THEREOF FOR THE MODULATION OF HEMOGLOBIN 审中-公开
公开(公告)号：US20180186807A1
公开(公告)日：2018-07-05
申请号：US15680794
申请日：2017-08-18
申请人： Global Blood Therapeutics, Inc.
发明人： Calvin W. Yee , Zhe Li
IPC分类号： C07D493/08 , C07D487/08 , C07D401/04 , C07C235/24 , C07D231/40 , C07D213/75 , C07D309/14
CPC分类号： C07D493/08 , C07C235/24 , C07D213/75 , C07D231/40 , C07D309/14 , C07D401/04 , C07D487/08
摘要： Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.

2. 发明授权

US09447063B2 Disubstituted adamantyl derivative or pharmaceutically acceptable salt thereof, production method for same, and pharmaceutical composition for suppressing cancer metastasis comprising same as active ingredient 有权
标题翻译：二取代金刚烷基衍生物或其药学上可接受的盐，其制备方法和用于抑制癌转移的药物组合物，其包含与活性成分
公开(公告)号：US09447063B2
公开(公告)日：2016-09-20
申请号：US14724248
申请日：2015-05-28
申请人： KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY , DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION
发明人： Mi Sun Won , Kyeong Lee , Bo Kyung Kim , Hyun Seung Ban , Seohyun Son , Kyung-Sook Chung
IPC分类号： A61K31/167 , C07D307/42 , C07C235/24 , A61K45/06 , A61K31/341 , C07C231/12
CPC分类号： C07D307/42 , A61K31/167 , A61K31/341 , A61K45/06 , C07C231/12 , C07C235/24 , C07C2603/74 , A61K2300/00 , A61K31/67
摘要： The present invention relates to a novel disubstituted adamantyl derivative or the pharmaceutically acceptable salts thereof, a method for preparing the same, and a pharmaceutical anticancer or antimetastasis composition comprising the same as an active ingredient. The disubstituted adamantyl derivative of the present invention suppressed accumulation of HIF-1α, inhibiting the expression of the metastasis related protein Twist dose-dependently. Thus, the disubstituted adamantyl derivative of the invention is effective in inhibiting the expressions of the metastasis related proteins, β-catenin and RohA, and the EMT related genes such as MMP2 and MMP9, without cytotoxicity. Therefore, the disubstituted adamantyl derivative or the pharmaceutically acceptable salts thereof of the invention can be efficiently used as a pharmaceutical anticancer or antimetastasis composition.
摘要翻译：本发明涉及新的二取代金刚烷基衍生物或其药学上可接受的盐，其制备方法，以及含有该活性成分的药物抗癌或抗转移组合物。本发明的二取代金刚烷基衍生物抑制HIF-1α的积累，抑制转移相关蛋白的表达量呈剂量依赖性。因此，本发明的二取代金刚烷基衍生物可有效抑制转移相关蛋白，β-连环蛋白和RohA以及EMT相关基因如MMP2和MMP9的表达，无细胞毒性。因此，本发明的二取代金刚烷基衍生物或其药学上可接受的盐可以有效地用作药物抗癌或抗转移组合物。

3. 发明授权

US08969342B2 Compounds and methods for treating mammalian gastrointestinal microbial infections 有权
标题翻译：用于治疗哺乳动物胃肠道微生物感染的化合物和方法
公开(公告)号：US08969342B2
公开(公告)日：2015-03-03
申请号：US13257418
申请日：2010-03-22
申请人： Lizbeth K. Hedstrom , Gregory D. Cuny , Deviprasad R. Gollapalli , Boris Striepen , Suresh Kumar Gorla , Mandapati Kavitha
发明人： Lizbeth K. Hedstrom , Gregory D. Cuny , Deviprasad R. Gollapalli , Boris Striepen , Suresh Kumar Gorla , Mandapati Kavitha
IPC分类号： A61K31/535
CPC分类号： C07D401/12 , C07C233/15 , C07C235/24 , C07C235/38 , C07C237/20 , C07C255/60 , C07C275/28 , C07C275/30 , C07C275/42 , C07C309/15 , C07D209/08 , C07D209/12 , C07D209/30 , C07D215/38 , C07D235/26 , C07D237/32 , C07D249/06 , C07D263/56 , C07D263/57 , C07D295/192 , C07D401/04 , C07D401/14 , C07D409/04 , C07D413/04 , C07D417/04 , C07D417/14 , C07D471/08 , C07D491/052
摘要： Described herein are compounds, and pharmaceutically acceptable salts and prodrugs thereof, which are useful as inhibitors of IMPDH. In certain embodiments, a compound of the invention selectively inhibits a parasitic IMPDH versus a host IMPDH. Further, the invention provides pharmaceutical compositions comprising one or more compounds of the invention. The invention also relates to methods of treating various parasitic and bacterial infections in mammals. Moreover, the compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.
摘要翻译：本文描述了可用作IMPDH抑制剂的化合物及其药学上可接受的盐和前药。在某些实施方案中，本发明的化合物选择性地抑制寄生IMPDH相对于宿主IMPDH。此外，本发明提供包含一种或多种本发明化合物的药物组合物。本发明还涉及治疗哺乳动物中各种寄生虫和细菌感染的方法。此外，化合物可以单独使用或与其它治疗或预防剂如抗病毒剂，抗炎剂，抗微生物剂和免疫抑制剂组合使用。

4. 发明授权

US08722929B2 N-[2-amino-4-(phenylmethoxy)phenyl] amides and related compounds as potassium channel modulators 有权
标题翻译： N- [2-氨基-4-（苯基甲氧基）苯基]酰胺和相关化合物作为钾通道调节剂
公开(公告)号：US08722929B2
公开(公告)日：2014-05-13
申请号：US11870368
申请日：2007-10-10
申请人： Jean-Michel Vernier , Jianlan Song , Huanming Chen , Zhi Hong
发明人： Jean-Michel Vernier , Jianlan Song , Huanming Chen , Zhi Hong
IPC分类号： C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00
CPC分类号： C07C233/43 , C07C233/44 , C07C235/16 , C07C235/24 , C07C271/28
摘要： This invention provides compounds of formula A and formula B which are modulators of potassium ion channels and are useful for the treatment of seizure disorders.
摘要翻译：本发明提供了作为钾离子通道调节剂的式A和式B化合物，可用于治疗癫痫发作。

5. 发明授权

US08686154B2 Compounds and compositions for delivering active agents 失效
标题翻译：用于递送活性剂的化合物和组合物
公开(公告)号：US08686154B2
公开(公告)日：2014-04-01
申请号：US12482320
申请日：2009-06-10
申请人： Donald J. Sarubbi , Eugene N. Barantsevitch
发明人： Donald J. Sarubbi , Eugene N. Barantsevitch
IPC分类号： C07D211/60 , A61K31/445
CPC分类号： C07D209/48 , A61K9/1617 , A61K31/195 , A61K31/445 , A61K31/4965 , A61K31/727 , A61K38/21 , A61K38/23 , A61K38/27 , A61K38/28 , A61K38/29 , A61K45/06 , C07C229/42 , C07C233/51 , C07C233/54 , C07C233/69 , C07C233/81 , C07C233/83 , C07C235/12 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/64 , C07C235/66 , C07C235/74 , C07C237/12 , C07C237/20 , C07C237/36 , C07C237/40 , C07C237/42 , C07C243/38 , C07C259/06 , C07C271/28 , C07C271/54 , C07D211/62 , C07D213/81 , C07D213/82 , C07D239/42 , C07D241/24 , C07D257/04 , C07D295/192 , C07D311/12 , C07D311/24 , C07D311/30 , A61K2300/00
摘要： Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
摘要翻译：提供了可用于递送活性剂的载体化合物及其组合物。也提供给药和制备方法。

6. 发明申请

US20120220577A1 GLYCINE B ANTAGONISTS 审中-公开
标题翻译：糖蛋白B拮抗剂
公开(公告)号：US20120220577A1
公开(公告)日：2012-08-30
申请号：US13375954
申请日：2010-06-04
申请人： Markus Henrich , Angela Hansen , Jens Nagel , Valerjans Kauss , Jevgenijs Rozhkovs , Ginta Grunsteine , Dina Trifanova
发明人： Markus Henrich , Angela Hansen , Jens Nagel , Valerjans Kauss , Jevgenijs Rozhkovs , Ginta Grunsteine , Dina Trifanova
IPC分类号： A61K31/19 , C07C271/22 , A61K31/27 , C07D211/60 , A61K31/445 , C07D207/08 , A61K31/40 , C07D215/14 , A61K31/47 , C07D265/36 , A61K31/538 , C07D265/30 , A61K31/5375 , C07D257/04 , A61K31/41 , A61P29/00 , A61P25/02 , C07C63/34
CPC分类号： C07C311/51 , C07C49/84 , C07C65/24 , C07C235/20 , C07C235/22 , C07C235/24 , C07C237/42 , C07C255/16 , C07C255/44 , C07C255/60 , C07C271/20 , C07C2601/02 , C07C2602/08 , C07C2602/10 , C07D207/16 , C07D207/273 , C07D209/42 , C07D211/60 , C07D213/36 , C07D213/50 , C07D213/74 , C07D215/06 , C07D215/48 , C07D217/02 , C07D217/26 , C07D233/90 , C07D257/04 , C07D257/06 , C07D265/36 , C07D277/42 , C07D295/185 , C07D307/85 , C07D403/04 , C07D513/04
摘要： The invention relates to naphthalene derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders.
摘要翻译：本发明涉及萘衍生物及其药学上可接受的盐。本发明还涉及制备这些化合物的方法。本发明的化合物是甘氨酸B拮抗剂，因此可用于控制和预防各种疾病，包括神经障碍。

7. 发明申请

US20100279871A1 OPTICALLY ACTIVE (R)-ARYLOXYPROPIONIC ACID AMIDES AND HERBICIDAL COMPOSITION COMPRISING SAME 有权
标题翻译：光学活性的活性丙烯酸酰胺和包含其的除草剂组合物
公开(公告)号：US20100279871A1
公开(公告)日：2010-11-04
申请号：US12667506
申请日：2008-07-02
申请人： Joo-kyung Kim , Dong-hoo Kim , Hyung-ho Kim , Kyung-hyun Kim , Cheol-su Yoon , In-cheon Hwang
发明人： Joo-kyung Kim , Dong-hoo Kim , Hyung-ho Kim , Kyung-hyun Kim , Cheol-su Yoon , In-cheon Hwang
IPC分类号： A01N43/60 , C07C233/00 , C07D277/00 , C07D277/62 , C07D235/00 , C07D241/02 , A01N43/78 , A01N43/52 , A01N47/10 , A01P13/00
CPC分类号： C07C235/24 , A01N39/02 , A01N43/40 , A01N43/52 , A01N43/56 , A01N43/58 , A01N43/60 , A01N43/76 , A01N43/78 , A01N43/80 , C07D213/75 , C07D231/40 , C07D235/30 , C07D241/20 , C07D263/58 , C07D277/46 , C07D277/82 , C07D413/12 , C07D417/12
摘要： The present invention relates to an optically active (R)-aryloxypropionic acid amide compound which has high selectivity and safety for protecting a crop such as rice, wheat, barley and soy bean, and exhibits excellent herbicidal activity against weeds, and a herbicidal composition comprising the same.
摘要翻译：本发明涉及对保护作物如水稻，小麦，大麦和大豆的高选择性和安全性的光学活性（R） - 丙氧基丙酸酰胺化合物，并且对杂草具有优异的除草活性，以及除草组合物，其包含一样。

8. 发明授权

US07803970B2 Multi-substitued selective androgen receptor modulators and methods of use thereof 失效
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：US07803970B2
公开(公告)日：2010-09-28
申请号：US10861905
申请日：2004-06-07
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 , A61K31/65
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。

9. 发明授权

US07763656B2 Use of Acetylamino benzoic acid compounds for nonsense suppression and the treatment of disease 失效
标题翻译：使用乙酰氨基苯甲酸化合物进行无味抑制和治疗疾病
公开(公告)号：US07763656B2
公开(公告)日：2010-07-27
申请号：US11789625
申请日：2007-04-24
申请人： Richard G. Wilde , Ellen M. Welch , James Jan Takasugi , Neil G. Almstead , Steven Marc Rubenstein , Holger Beckmann
发明人： Richard G. Wilde , Ellen M. Welch , James Jan Takasugi , Neil G. Almstead , Steven Marc Rubenstein , Holger Beckmann
IPC分类号： A61K31/19
CPC分类号： C07C235/24 , C07C235/74 , C07C323/60 , C07C327/42 , C07C2601/08 , C07C2602/08 , C07C2602/10 , C07D207/273 , C07D209/48 , C07D213/74 , C07D239/38 , C07D257/04 , C07D271/10 , C07D317/64
摘要： Novel acetylamino benzoic acid compounds, methods of using and pharmaceutical compositions comprising an acetylamino benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.
摘要翻译：公开了新型乙酰氨基苯甲酸化合物，使用方法和包含乙酰氨基苯甲酸衍生物的药物组合物。所述方法包括治疗或预防通过调节过早翻译终止或无义介导的mRNA衰变而改善的疾病或改善与其相关的一种或多种症状的方法。

10. 发明授权

US07645898B2 Selective androgen receptor modulators and method 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：US07645898B2
公开(公告)日：2010-01-12
申请号：US11505499
申请日：2006-08-17
申请人： James T. Dalton , Duane D. Miller
发明人： James T. Dalton , Duane D. Miller
IPC分类号： C07C255/50 , A61K31/275
CPC分类号： C07D271/12 , C07C235/24 , C07C255/54 , C07C255/60 , C07C317/44 , C07C323/62 , C07C335/18 , C07D209/08
摘要： This invention provides SARM compounds and uses thereof 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化合物及其用于治疗受试者中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。

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