公开(公告)号：US20240352053A1

公开(公告)日：2024-10-24

申请号：US18683571

申请日：2022-08-19

申请人： BETTA PHARMACEUTICALS CO., LTD

发明人： Liang CHEN ,  Changyong QIU ,  Xiangyong LIU ,  Jian TANG ,  Lieming DING ,  Jiabing WANG

IPC分类号： C07F9/6558 ,  A61K31/675 ,  C07C55/10 ,  C07C57/15 ,  C07C59/245 ,  C07C59/255 ,  C07C309/04

CPC分类号： C07F9/65583 ,  A61K31/675 ,  C07C55/10 ,  C07C57/15 ,  C07C59/245 ,  C07C59/255 ,  C07C309/04 ,  C07B2200/13

摘要： The present invention relates to salt and crystal form of an EGFR inhibitor, and a composition and the use thereof. The salt and crystal form of the EGFR inhibitor as represented by formula I of the present invention can be used for treating or preventing epidermal growth factor receptor-mediated diseases or medical conditions (such as L858R activation mutants, exon 19 deletion activation mutants, T790M resistance mutants and C797S resistant mutants) in certain mutant forms.

公开(公告)号：US20240066132A1

公开(公告)日：2024-02-29

申请号：US18352345

申请日：2023-07-14

申请人： NOVARTIS AG

发明人： David Weninger BARNES ,  Avirup BOSE ,  Alexandra Marshall BRUCE ,  Alokesh DUTTAROY ,  Chikwendu IBEBUNJO ,  Aaron KANTER ,  Louise Clare KIRMAN ,  Changgang LOU ,  Aimee Richardson USERA ,  Ken YAMADA ,  Jun YUAN ,  Frederic ZECRI

IPC分类号： A61K47/54 ,  A61K38/095 ,  A61K38/16 ,  A61K38/17 ,  A61K38/18 ,  A61K38/22 ,  A61K45/06 ,  C07C55/02 ,  C07C55/22 ,  C07C57/02 ,  C07C57/18 ,  C07C59/245 ,  C12N15/113

CPC分类号： A61K47/543 ,  A61K47/542 ,  A61K38/095 ,  A61K38/164 ,  A61K38/1709 ,  A61K38/1825 ,  A61K38/1841 ,  A61K38/2221 ,  A61K45/06 ,  C07C55/02 ,  C07C55/22 ,  C07C57/02 ,  C07C57/18 ,  C07C59/245 ,  C12N15/113 ,  C12N2310/14 ,  C12N2310/351

摘要： The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3:






wherein R1, R2, R3, R4, Ak, n, m and p are defined herein. The invention also relates to a method for manufacturing the conjugate of the invention such as GDF15 conjugate, and its therapeutic uses such as treatment or prevention of metabolic disorders or diseases, type 2 diabetes mellitus, obesity, pancreatitis, dyslipidemia, alcoholic and nonalcoholic fatty liver disease/steatohepatitis and other progressive liver diseases, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, metabolic syndrome, hypertension, cardiovascular disease, atherosclerosis, peripheral arterial disease, stroke, heart failure, coronary heart disease, diabetic complications (including but not limited to chronic kidney disease), neuropathy, gastroparesis and other metabolic disorders. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

公开(公告)号：US20230219892A1

公开(公告)日：2023-07-13

申请号：US18007726

申请日：2021-06-03

申请人： Curasen Therapeutics, Inc.

发明人： Wei Chen ,  Bing Xue ,  David Scott Carter

IPC分类号： C07D213/84 ,  C07C69/78 ,  C07C61/06 ,  C07C59/08 ,  C07C59/11 ,  C07C59/245 ,  C07C59/255 ,  C07C59/06 ,  C07C57/15 ,  C07C57/145 ,  C07C309/30

CPC分类号： C07D213/84 ,  C07C57/15 ,  C07C57/145 ,  C07C59/06 ,  C07C59/08 ,  C07C59/11 ,  C07C59/245 ,  C07C59/255 ,  C07C61/06 ,  C07C69/78 ,  C07C309/30 ,  C07B2200/13

摘要： The present disclosure relates generally to various forms and compositions useful as beta adrenergic agonists and uses of the same in the treatment of diseases associated with an adrenergic receptor. In one aspect, the disclosure provides a crystalline solid form of Compound 1: selected from Form A and Form B and salt forms thereof.

公开(公告)号：US20180127417A1

公开(公告)日：2018-05-10

申请号：US15846757

申请日：2017-12-19

申请人： Merck Sharp & Dohme Corp.

发明人： Frank Chen ,  Carmela Molinaro ,  W. Peter Wuelfing ,  Nobuyoshi Yasuda ,  Jianguo Yin ,  Yong-Li Zhong ,  Joseph Lynch

IPC分类号： C07D471/20 ,  C07D211/76 ,  C07D209/42 ,  C07C233/47 ,  C07C57/38 ,  C07C63/04 ,  C07C59/245 ,  C07C205/57

CPC分类号： C07D471/20 ,  C07B2200/13 ,  C07C57/38 ,  C07C59/245 ,  C07C63/04 ,  C07C205/57 ,  C07C233/47 ,  C07D209/42 ,  C07D211/76 ,  C07D417/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/20

摘要： The invention encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, which are CGRP receptor antagonists useful for the treatment of migraine.

公开(公告)号：US09963537B2

公开(公告)日：2018-05-08

申请号：US15174069

申请日：2016-06-06

申请人： Mitsubishi Chemical Corporation

发明人： Teruhiko Ohara ,  Naoki Suzuki ,  Yasuko Nakajima ,  Hiroto Itou ,  Takayuki Aoshima ,  Naoki Sugai ,  Takanao Matsumoto

IPC分类号： C08G18/42 ,  A43B13/04 ,  A43B1/14 ,  A43B1/00 ,  C08G18/08 ,  C09D175/06 ,  C09J175/06 ,  C07C69/34 ,  C07C69/40 ,  C07C69/66 ,  C07C69/675 ,  C07C69/70 ,  C07C69/704 ,  C08G63/06 ,  C08G63/20 ,  C08G63/60 ,  C08G18/66 ,  C08G18/76 ,  C07C59/245 ,  C08G63/16 ,  C08G101/00

CPC分类号： C08G18/4238 ,  A43B1/00 ,  A43B1/14 ,  A43B13/04 ,  C07C59/245 ,  C07C69/34 ,  C07C69/40 ,  C07C69/66 ,  C07C69/675 ,  C07C69/70 ,  C07C69/704 ,  C08G18/14 ,  C08G18/4241 ,  C08G18/4286 ,  C08G18/664 ,  C08G18/7657 ,  C08G18/7671 ,  C08G63/06 ,  C08G63/16 ,  C08G63/20 ,  C08G63/60 ,  C08G2101/0008 ,  C08G2410/00 ,  C09D175/06 ,  C09J175/06

摘要： The invention relates to a method for producing a biomass-resource-derived polyurethane, which comprises: reacting a dicarboxylic acid and an aliphatic diol to produce a polyester polyol; and reacting the polyester polyol and a polyisocyanate compound, wherein the dicarboxylic acid contains at least one component derived from biomass resources, a content of an organic acid in the dicarboxylic acid is more than 0 ppm and not more than 1,000 ppm relative to the dicarboxylic acid, and a pKa value of the organic acid at 25° C. is not more than 3.7.

公开(公告)号：US09913821B2

公开(公告)日：2018-03-13

申请号：US15143987

申请日：2016-05-02

申请人： Panion & BF Biotech, Inc.

发明人： David W. K. Kwok ,  Nikolay Mintchev Stoynov

IPC分类号： A61K31/295

CPC分类号： C07F15/025 ,  A61K31/295 ,  C07C51/41 ,  C07C51/412 ,  C07C51/418 ,  C07C59/265 ,  C07F15/02 ,  C07C55/10 ,  C07C59/255 ,  C07C53/08 ,  C07C59/245 ,  C07C57/15

摘要： The present invention discloses a novel form of ferric organic compounds, including a form of ferric citrate, which are soluble over a wider range of pH, and which have a large active surface area. The ferric organic compounds of the present invention can be delivered effectively by oral route with better delivery to treat patients suffering from hyperphosphatemia, metabolic acidosis and other disorders responsive to ferric organic compound therapy.

公开(公告)号：US20170073296A1

公开(公告)日：2017-03-16

申请号：US15361783

申请日：2016-11-28

申请人： LABORATORIYA BIO ZET, LLC

发明人： Igor I. ZOTKIN ,  Nadezhda V. KUZNETSOVA ,  Larisa V. KABANOVA

IPC分类号： C07C59/50 ,  A01N55/02

CPC分类号： C07C59/50 ,  A01N55/02 ,  A01N59/16 ,  A01N59/20 ,  C01G3/00 ,  C01G9/00 ,  C07C55/08 ,  C07C55/10 ,  C07C57/04 ,  C07C59/06 ,  C07C59/08 ,  C07C59/105 ,  C07C59/245 ,  C07C59/255 ,  C07C229/24 ,  C07C229/76 ,  C07F1/00 ,  C07F1/005 ,  C07F3/003 ,  C09D5/14 ,  D21H21/36 ,  D21H25/02

摘要： Zinc or copper (II) salt which can be used as a biocide, having the general formula CH2C(R1)CO—M—OCOR2(OH)m(COOH)n wherein M is Zn or Cu, R1 is selected from the group comprising hydrogen and methyl, R2 is substituted C1-C5 alkyl, m=0-5, n=0-2, m+n=1-5.

摘要翻译： 可以用作杀生物剂的锌或铜（II）盐，具有通式CH 2 C（R 1）CO-M-OCOR 2（OH）m（COOH）n，其中M是Zn或Cu，R 1选自 氢和甲基，R2是取代的C1-C5烷基，m = 0-5，n = 0-2，m + n = 1-5。

公开(公告)号：US20170035741A1

公开(公告)日：2017-02-09

申请号：US15064498

申请日：2016-03-08

申请人： Sunesis Pharmaceuticals, Inc.

发明人： Anantha SUDHAKAR ,  Tamilarasan SUBRAMANI ,  Mohamed Sheik Mohamed Mujeebur RAHUMAN ,  Ramar SUBBIAH

IPC分类号： A61K31/4375 ,  A61K9/00 ,  A61K45/06 ,  A61K9/08

CPC分类号： A61K31/4375 ,  A61K9/0019 ,  A61K9/08 ,  A61K45/06 ,  A61K47/10 ,  A61K47/20 ,  C07C59/245 ,  C07D207/16 ,  C07D471/04 ,  Y02P20/55

摘要： Methods of preparing (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid are disclosed. Also provided are pharmaceutical compositions comprising (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid, and methods of treatment using such compositions.

摘要翻译： 制备（+） - 1,4-二氢-7 - [（3S，4S）-3-甲氧基-4-（甲基氨基）-1-吡咯烷基] -4-氧代-1-（2-噻唑基）-1 ，8-萘啶-3-羧酸。 还提供了包含（+） - 1,4-二氢-7 - [（3S，4S）-3-甲氧基-4-（甲基氨基）-1-吡咯烷基] -4-氧代-1-（2-噻唑基 ）-1,8-萘啶-3-羧酸，以及使用这种组合物的处理方法。

公开(公告)号：US09522911B2

公开(公告)日：2016-12-20

申请号：US14338923

申请日：2014-07-23

申请人： Jeil Pharmaceutical Co., Ltd.

发明人： In-Hae Ye ,  Chun-Ho Park ,  Jong-Hee Choi ,  Dong-il Kang

IPC分类号： C07D471/04 ,  C07C53/06 ,  C07C55/10 ,  C07C55/14 ,  C07C57/145 ,  C07C57/15 ,  C07C59/245 ,  C07C59/255 ,  C07C229/24 ,  C07C307/02 ,  C07C309/04 ,  C07C309/19 ,  C07C309/29 ,  C07D239/22

CPC分类号： C07D471/04 ,  C07C53/06 ,  C07C55/10 ,  C07C55/14 ,  C07C57/145 ,  C07C57/15 ,  C07C59/245 ,  C07C59/255 ,  C07C229/24 ,  C07C307/02 ,  C07C309/04 ,  C07C309/19 ,  C07C309/29 ,  C07D239/22

摘要： The present invention relates to a novel crystalline acid salt of a tricyclic derivative or a hydrate thereof and a production method thereof. The crystalline acid salt or the hydrate thereof according to the present invention is stable with respect to humidity and stable with respect to hygroscopicity, and the quality control during manufacturing drugs is favorable. In addition, the crystalline acid salt or the hydrate thereof may be used in a pharmaceutical composition for preventing or treating neuropathic pain, epilepsy, stroke, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis (ALS), Huntington's disease, schizophrenia, chronic and acute pain, ischemic brain injury, neuronal loss after hypoxia, trauma and nerve damage, which are medical conditions induced by PARP overactivity.

摘要翻译： 本发明涉及三环衍生物或其水合物的新型结晶酸盐及其制备方法。 根据本发明的结晶酸盐或其水合物在湿度方面是稳定的，并且在吸湿性方面是稳定的，并且制造药物期间的质量控制是有利的。 此外，结晶酸盐或其水合物可用于预防或治疗神经性疼痛，癫痫，中风，阿尔茨海默病，帕金森病，肌萎缩性侧索硬化（ALS），亨廷顿病，精神分裂症，慢性和急性 疼痛，缺血性脑损伤，缺氧后的神经元损失，创伤和神经损伤，这是由PARP过度活动引起的医学病症。

公开(公告)号：US09328133B2

公开(公告)日：2016-05-03

申请号：US14502774

申请日：2014-09-30

申请人： Panion & BF Biotech, Inc.

发明人： David W. K. Kwok ,  Nikolay Mintchev Stoynov

IPC分类号： C07C51/41 ,  C07F15/02 ,  A61K31/295

CPC分类号： C07F15/025 ,  A61K31/295 ,  C07C51/41 ,  C07C51/412 ,  C07C51/418 ,  C07C59/265 ,  C07F15/02 ,  C07C55/10 ,  C07C59/255 ,  C07C53/08 ,  C07C59/245 ,  C07C57/15

摘要： The present invention discloses a novel form of ferric organic compounds, including a form of ferric citrate, which are soluble over a wider range of pH, and which have a large active surface area. The ferric organic compounds of the present invention can be delivered effectively by oral route with better delivery to treat patients suffering from hyperphosphatemia, metabolic acidosis and other disorders responsive to ferric organic compound therapy.