公开(公告)号：US11285151B2

公开(公告)日：2022-03-29

申请号：US16549226

申请日：2019-08-23

申请人： Emory University

发明人： Michael G. Natchus ,  Richard Arrendale ,  Dennis Liotta ,  Ketan Desai ,  Hyunsuk Shim

IPC分类号： A61K31/506 ,  A61K45/06 ,  A61K31/4166 ,  A61K31/57 ,  A61K31/575 ,  A61K31/58 ,  A61K31/505 ,  A61K31/137 ,  A61K31/138 ,  A61K31/167 ,  A61K31/444 ,  A61K38/20 ,  C07D403/12 ,  C07D213/74 ,  C07D401/12 ,  C07D239/42 ,  C07D213/72 ,  C07C211/53 ,  C07C233/64 ,  C07C255/58 ,  C07C211/52 ,  C07C229/60 ,  C07C279/04 ,  C07C279/18 ,  C07C211/27 ,  C07C233/11 ,  C07C233/58 ,  C07C233/65 ,  C07C233/75 ,  C07C237/40

摘要： The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.

公开(公告)号：US11124475B2

公开(公告)日：2021-09-21

申请号：US16625840

申请日：2018-03-15

申请人： CHENGDU KAOENSI SCIENCE AND TECHNOLOGY CO., LTD.

发明人： Hu Zheng ,  Lingling Weng

IPC分类号： C07C277/08 ,  C07C279/14 ,  C07C279/18 ,  C07C279/26 ,  C07C279/28 ,  C07D209/16 ,  C07D213/73 ,  C07D233/50 ,  C07D233/64 ,  C07D245/02 ,  C07D277/48 ,  C07D295/027 ,  C07D295/215 ,  C07D487/04

摘要： A hydrogen sulfide donor in an organic salt form and a preparation method thereof. The hydrogen sulfide donor exists as a salt formed by organic compounds with an alkaline motif and hydrogen sulfide with weak acidity. The hydrogen sulfide donor features with a simple structure, and an easy preparation method. Moreover, hydrogen sulfide donors in different forms can be prepared according to research and development needs. After the hydrogen sulfide donor enters an organism, the process of in vivo dissociation and hydrogen sulfide supply is simple, rapid, and effective, and there is no requirement for enzyme or any other complicated condition, and thus, the hydrogen sulfide donor has a great application prospect and value.

公开(公告)号：US20190330157A1

公开(公告)日：2019-10-31

申请号：US16429507

申请日：2019-06-03

申请人： REGENTS OF THE UNIVERSITY OF MINNESOTA

发明人： Swati S. More ,  Robert Vince

IPC分类号： C07D233/44 ,  A61P25/16 ,  C07C279/08 ,  A61P35/00 ,  A61P5/48 ,  C07C279/06 ,  C07D239/47 ,  C07D239/22 ,  C07C335/12 ,  C07D213/61 ,  C07C335/40 ,  C07C335/04 ,  C07D239/18 ,  C07D239/06 ,  C07D233/64 ,  C07D233/52 ,  C07D233/50 ,  C07D231/38 ,  C07C281/18 ,  C07C281/16 ,  C07C281/14 ,  C07C279/22 ,  C07C279/18

摘要： The invention provides methods for producing analgesia in an animal comprising administering to the animal a compound of the formula Ia′, Ib′, Ic′, and Id′: and pharmaceutically acceptable salts thereof, wherein the variables A, R6, R7, R8, R9, Rx, L, X, Y, and Z have the meaning as described herein.

公开(公告)号：US10369121B2

公开(公告)日：2019-08-06

申请号：US15502981

申请日：2014-08-25

申请人： THE CATHOLIC UNIVERSITY OF KOREA INDUSTRY—ACADEMIC COOPERATION FOUNDATION

发明人： Mi-La Cho ,  Chul-Woo Yang ,  Dong-Yun Shin ,  Min-Jung Park ,  Seon-Yeong Lee ,  Sung-Hee Lee ,  Eun-Ji Yang ,  Hye-Jin Son ,  Eun-Kyung Kim ,  Jae-Kyung Kim

IPC分类号： A61K31/155 ,  C07C279/18 ,  C07C279/20 ,  C07C279/26

摘要： The present invention relates to a biguanide derivative compound capable of effectively preventing and treating immune diseases. The biguanide-based derivative compound according to the present invention inhibits the generation of IL-17 and TNF-α, which are inflammatory cytokines, increases the activity of regulatory T cells having an immunomodulatory function, and exhibits excellent therapeutic effects in animal models of immune diseases. Accordingly, the biguanide-based derivative compound can be usefully used as an immunosuppressant or a pharmaceutical composition capable of preventing or treating various immune diseases, such as autoimmune diseases, inflammatory diseases, and transplant rejection, caused by the dysregulation of immune responses.

公开(公告)号：US10100006B2

公开(公告)日：2018-10-16

申请号：US15819758

申请日：2017-11-21

申请人： THE CATHOLIC UNIVERSITY OF KOREA INDUSTRY—ACADEMIC COOPERATION FOUNDATION

发明人： Mi-La Cho ,  Dong-Yun Shin ,  Sung-Hwan Park ,  Chul-Woo Yang ,  Jong-Young Choi ,  Min-Jung Park ,  Hye-Jin Son ,  Sung-Hee Lee ,  Seon-Yeong Lee ,  Eun-Kyung Kim ,  Jae-Kyung Kim ,  Seung-Hun Lee ,  Seong-Hyeok Park

IPC分类号： C07C279/18

摘要： Provided is a novel compound capable of effectively preventing and treating immune diseases and a use thereof. The novel compound of the present subject matter has effects of inhibiting the production of inflammatory cytokines, increasing the activity of regulatory T cells having immunoregulatory functions, inhibiting the production of auto-antibodies to regulate excessive immune responses, and inhibiting the differentiation of osteoclasts, and thus can be used for treating immune diseases, such as autoimmune disease, inflammatory disease, and transplant rejection diseases, which are caused by abnormal regulation of various kinds of immune response.

公开(公告)号：US20170333370A1

公开(公告)日：2017-11-23

申请号：US15502981

申请日：2014-08-25

申请人： THE CATHOLIC UNIVERSITY OF KOREA INDUSTRY-ACADEMIC COOPERATION FOUNDATION

发明人： Mi-La CHO ,  Chul-Woo YANG ,  Dong-Yun SHIN ,  Min-Jung PARK ,  Seon-Yeong LEE ,  Sung-Hee LEE ,  Eun-Ji YANG ,  Hye-Jin SON ,  Eun-Kyung KIM ,  Jae-Kyung KIM

IPC分类号： A61K31/155 ,  C07C279/18 ,  C07C279/26

CPC分类号： A61K31/155 ,  A61K2121/00 ,  A61K2300/00 ,  C07C279/18 ,  C07C279/26

摘要： The present invention relates to a biguanide derivative compound capable of effectively preventing and treating immune diseases. The biguanide-based derivative compound according to the present invention inhibits the generation of IL-17 and TNF-α, which are inflammatory cytokines, increases the activity of regulatory T cells having an immunomodulatory function, and exhibits excellent therapeutic effects in animal models of immune diseases. Accordingly, the biguanide-based derivative compound can be usefully used as an immunosuppressant or a pharmaceutical composition capable of preventing or treating various immune diseases, such as autoimmune diseases, inflammatory diseases, and transplant rejection, caused by the dysregulation of immune responses.

公开(公告)号：US09534014B2

公开(公告)日：2017-01-03

申请号：US14320351

申请日：2014-06-30

申请人： Signature Therapeutics, Inc.

发明人： Thomas E. Jenkins ,  Julie D. Seroogy ,  Jonathan W. Wray

IPC分类号： A61K31/497 ,  C07K5/072 ,  A61K31/155 ,  A61K31/485 ,  A61K31/135 ,  A61K31/195 ,  A61K31/439 ,  A61K31/445 ,  A61K31/451 ,  A61K31/495 ,  A61K31/55 ,  A61K38/05 ,  C07C215/64 ,  C07C257/18 ,  C07C279/18 ,  C07D211/66 ,  C07D217/04 ,  C07D221/26 ,  C07D223/04 ,  C07D295/185 ,  C07D491/08 ,  A61K47/48

CPC分类号： C07K5/06121 ,  A61K31/135 ,  A61K31/155 ,  A61K31/195 ,  A61K31/439 ,  A61K31/445 ,  A61K31/451 ,  A61K31/485 ,  A61K31/495 ,  A61K31/55 ,  A61K38/05 ,  A61K47/50 ,  A61K47/54 ,  A61K47/543 ,  A61K47/56 ,  C07C215/64 ,  C07C257/18 ,  C07C279/18 ,  C07C2603/80 ,  C07D211/66 ,  C07D217/04 ,  C07D221/26 ,  C07D223/04 ,  C07D295/185 ,  C07D491/08

摘要： Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenolic opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the phenolic opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

摘要翻译： 提供了药物组合物及其使用方法，其中药物组合物包含提供酚类阿片样物质的酶控释放的酚类阿片样物质前药，以及与介导酶促控制释放的酶相互作用的酶抑制剂 来自前药的酚类阿片样物质，以减轻前药的酶裂解。

公开(公告)号：US20150376123A1

公开(公告)日：2015-12-31

申请号：US14847692

申请日：2015-09-08

申请人： HANALL BIOPHARMA CO., LTD.

发明人： Sung Wuk Kim ,  Sung Soo Jun ,  Chang Hee Min ,  Se Hwan Park ,  Yong Eun Kim ,  Duck Kim ,  Ji Sun Lee ,  Ju Hoon Oh

IPC分类号： C07C279/16 ,  C07C279/04 ,  C07D307/52 ,  C07D317/58 ,  C07C279/06 ,  C07C279/08 ,  C07D333/20 ,  C07D213/38 ,  C07C277/04 ,  C07C279/18

CPC分类号： A61K31/155 ,  A61K31/341 ,  A61K31/4406 ,  A61K31/472 ,  C07C277/04 ,  C07C279/04 ,  C07C279/06 ,  C07C279/08 ,  C07C279/16 ,  C07C279/18 ,  C07C279/26 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2603/74 ,  C07D213/38 ,  C07D307/52 ,  C07D317/58 ,  C07D333/20

摘要： A biguanide derivative compound with N4-N5 substitution, which is represented by Formula 1, or a pharmaceutically acceptable salt thereof, a method of preparing the same, and a pharmaceutical composition containing the same as an active ingredient are provided. The biguanide derivative may exhibit excellent effect on activation of AMPK and inhibition of cancer cell proliferation in a low dose, compared with conventional drugs, and thus, may be useful to treat diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer, etc.

摘要翻译： 提供了由式1表示的具有N4-N5取代的双胍衍生物化合物或其药学上可接受的盐，其制备方法和含有其的药物组合物作为活性成分。 与常规药物相比，双胍衍生物可能对AMPK的活化和低剂量的癌细胞增殖具有优异的效果，因此可用于治疗糖尿病，肥胖症，高脂血症，高胆固醇血症，脂肪肝，冠状动脉疾病 ，骨质疏松症，多囊卵巢综合征，代谢综合征，癌症等

公开(公告)号：US09205085B2

公开(公告)日：2015-12-08

申请号：US14356302

申请日：2012-11-07

申请人： Michael G. Natchus ,  Richard Arrendale ,  Dennis Liotta

发明人： Michael G. Natchus ,  Richard Arrendale ,  Dennis Liotta

IPC分类号： A61K31/506 ,  A61K38/20 ,  A61K31/444 ,  A61K31/167 ,  A61K31/138 ,  A61K31/137 ,  C07D239/42 ,  C07D213/72 ,  C07C255/58 ,  C07C233/64 ,  C07C211/53 ,  C07D403/12 ,  A61K31/505 ,  C07D213/74 ,  C07D401/12 ,  A61K45/06 ,  A61K31/4166 ,  A61K31/57 ,  A61K31/575 ,  A61K31/58 ,  C07C211/52 ,  C07C229/60 ,  C07C279/04 ,  C07C279/18 ,  C07C211/27 ,  C07C233/11 ,  C07C233/58 ,  C07C233/65 ,  C07C233/75 ,  C07C237/40

CPC分类号： A61K31/506 ,  A61K31/137 ,  A61K31/138 ,  A61K31/167 ,  A61K31/4166 ,  A61K31/444 ,  A61K31/505 ,  A61K31/57 ,  A61K31/575 ,  A61K31/58 ,  A61K38/2073 ,  A61K45/06 ,  C07C211/27 ,  C07C211/52 ,  C07C211/53 ,  C07C229/60 ,  C07C233/11 ,  C07C233/58 ,  C07C233/64 ,  C07C233/65 ,  C07C233/75 ,  C07C237/40 ,  C07C255/58 ,  C07C279/04 ,  C07C279/18 ,  C07D213/72 ,  C07D213/74 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  A61K2300/00

摘要： The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.

摘要翻译： 本公开提供了可用于治疗某些内分泌紊乱症状的某些化合物的使用方法，特别是与潮热相关的化合物。

公开(公告)号：US09199927B2

公开(公告)日：2015-12-01

申请号：US14344377

申请日：2012-09-14

申请人： Jiro Fujiyasu ,  Kazuhiko Ohne ,  Susumu Yamaki ,  Tomoyoshi Imaizumi ,  Takeshi Hondo ,  Keisuke Matsuura ,  Tomohki Satou ,  Satoshi Sasamura

发明人： Jiro Fujiyasu ,  Kazuhiko Ohne ,  Susumu Yamaki ,  Tomoyoshi Imaizumi ,  Takeshi Hondo ,  Keisuke Matsuura ,  Tomohki Satou ,  Satoshi Sasamura

IPC分类号： A61K31/47 ,  C07C229/02 ,  C07D215/38 ,  C07C279/18 ,  C07D213/79 ,  C07D215/20 ,  C07D215/48 ,  C07D215/50 ,  C07D333/38 ,  C07D333/40 ,  C07D233/64 ,  C07D257/04 ,  C07D271/06 ,  C07D207/16 ,  C07D277/20 ,  C07D277/56 ,  C07D209/20 ,  C07D209/42 ,  C07D295/12 ,  C07D211/62 ,  C07D217/26 ,  C07D271/07 ,  C07D295/13

CPC分类号： C07C279/18 ,  C07B2200/07 ,  C07C2601/02 ,  C07C2601/14 ,  C07D207/16 ,  C07D209/20 ,  C07D209/42 ,  C07D211/62 ,  C07D213/79 ,  C07D215/20 ,  C07D215/48 ,  C07D215/50 ,  C07D217/26 ,  C07D233/64 ,  C07D257/04 ,  C07D271/06 ,  C07D271/07 ,  C07D277/20 ,  C07D277/56 ,  C07D295/12 ,  C07D295/13 ,  C07D333/38 ,  C07D333/40

摘要： [Problem]Provided is a compound which is useful as an agent for preventing and/or treating renal diseases.[Means for Solution]The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they have found that a guanidinobenzoic acid compound has a trypsin inhibitory action, thereby completing the present invention. The guanidinobenzoic acid compound of the present invention can be used as an agent for preventing and/or treating renal disease as an agent which will substitute low-protein diet therapy, and an agent for preventing and/or treating trypsin-related diseases, for example, pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like.

摘要翻译： [问题]提供可用作预防和/或治疗肾脏疾病的药剂的化合物。 [解决方案]本发明人对具有胰蛋白酶抑制作用的化合物进行了广泛的研究，结果发现胍基苯甲酸化合物具有胰蛋白酶抑制作用，从而完成了本发明。 本发明的胍基苯甲酸化合物可以用作预防和/或治疗肾脏疾病的药剂，作为代替低蛋白饮食疗法的药剂，以及用于预防和/或治疗胰蛋白酶相关疾病的药剂，例如 ，胰腺炎，胃食管反流病，肝性脑病，流行性感冒等。