公开(公告)号：US20200308163A1

公开(公告)日：2020-10-01

申请号：US16830110

申请日：2020-03-25

申请人： Neuropore Therapies, Inc.

发明人： Srinivasa Reddy NATALA ,  Wolfgang J. WRASIDLO ,  Emily M. STOCKING

IPC分类号： C07D417/10 ,  C07D231/12 ,  C07D413/06 ,  C07D405/04 ,  C07D401/06 ,  C07D403/10 ,  C07D401/10 ,  C07D413/10 ,  C07D405/14 ,  C07D403/14 ,  C07D413/14 ,  C07D409/10 ,  C07D498/02 ,  C07D207/06 ,  C07D211/10 ,  C07D265/30 ,  C07C235/56 ,  C07D265/36 ,  C07D487/08 ,  C07D471/08

摘要： The present disclosure relates to compounds, pharmaceutical compositions comprising such compounds, and use of such compounds in methods of treatment or in medicaments for treatment of inflammatory diseases and certain neurological disorders that are related to inflammatory signaling processes, including but not limited to misfolded proteins.

公开(公告)号：US10526336B2

公开(公告)日：2020-01-07

申请号：US15535315

申请日：2015-12-18

申请人： Merck Sharp & Dohme Corp.

发明人： Scott D. Kuduk ,  Nigel Liverton ,  Douglas C. Beshore ,  Na Meng ,  Yunfu Luo

IPC分类号： A61K31/519 ,  A61K31/4545 ,  A61K31/4985 ,  C07D487/04 ,  A61K45/06 ,  C07D471/04 ,  C07D498/02 ,  C07D498/04

摘要： The present invention is directed to fused heteroaryl derivative compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

公开(公告)号：US10385065B2

公开(公告)日：2019-08-20

申请号：US15302539

申请日：2015-04-10

申请人： Redx Pharma PLC

发明人： Andrew Ratcliffe ,  Anthony Huxley ,  David Lyth ,  Gary Noonan ,  Ralph Kirk ,  Mario Uosis-Martin ,  Neil Stokes

IPC分类号： C07D498/02 ,  C07D498/14 ,  C07D498/16 ,  A61K31/4375 ,  C07D519/00 ,  A61K31/4745 ,  A61K31/5383 ,  C07D498/04 ,  C07D513/04

摘要： The invention relates to antibacterial and anti-mycobacterial drug compounds of formula I. It also relates to pharmaceutical formulations of antibacterial drug compounds. It also relates to uses of the derivatives in treating bacterial infections, and methods of treating bacterial infections. The invention is also directed to antibacterial drug compounds capable of treating bacterial infections that are currently hard to treat with existing drug compounds, e.g., those caused by resistant bacterial or mycobacterial strains.

公开(公告)号：USRE46815E1

公开(公告)日：2018-05-01

申请号：US15172021

申请日：2016-06-02

申请人： Carna Biosciences, Inc.

发明人： Takayuki Irie ,  Ayako Sawa ,  Masaaki Sawa ,  Tokiko Asami ,  Yoko Funakoshi ,  Chika Tanaka

IPC分类号： C07D471/02 ,  C07D491/02 ,  C07D498/02 ,  C07D515/02 ,  C07D513/02 ,  C07D471/04 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  C07D519/00 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/541 ,  A61K31/437 ,  A61K31/496

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/541 ,  C07D519/00

摘要： To provide a novel furanone derivative, and a medicine including the same. The furanone derivative is represented by the formula (I): wherein A represents —COOR1 or a hydrogen atom; R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocycle; R2 and R3 are the same or different and each independently represent a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocycle, an optionally substituted heterocyclic fused ring, or an optionally substituted amino group; or alternatively, R2 and R3, taken together with the nitrogen atom to which they are attached, may form an optionally substituted heterocycle or an optionally substituted heterocyclic fused ring; and R4 represents a hydrogen atom or a halogen atom; with the proviso that when A represents —COOR1, R2 and R3 are not optionally substituted amino groups at the same time, and when A represents a hydrogen atom, R3 represents a hydrogen atom.

公开(公告)号：US09403819B2

公开(公告)日：2016-08-02

申请号：US14336871

申请日：2014-07-21

申请人： Takeda Pharmaceutical Company Limited

发明人： Edcon Chang

IPC分类号： A61K31/44 ,  C07D471/02 ,  C07D491/02 ,  C07D498/02 ,  C07D513/02 ,  C07D515/02 ,  C07D471/04

CPC分类号： C07D471/04

摘要： The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

摘要翻译： 本发明涉及抑制下式化合物的凋亡信号调节激酶1（“ASK1”），其中变量如本文所定义。 本发明还涉及包含这些化合物的药物组合物，试剂盒和制品; 用于制备化合物的方法和中间体; 以及使用所述化合物的方法。

公开(公告)号：US09394301B2

公开(公告)日：2016-07-19

申请号：US14658437

申请日：2015-03-16

申请人： Cancer Research Technology Limited

发明人： Grégoire Alexandre Pavé ,  James Donald Firth ,  Lorna Stewart ,  Laurent Jean Martin Rigoreau ,  Emma Louise Stanway

IPC分类号： A01N43/32 ,  A61K31/44 ,  C07D471/02 ,  C07D491/02 ,  C07D498/02 ,  C07D513/02 ,  C07D515/02 ,  C07D471/04 ,  A61K31/437 ,  C07D487/04

CPC分类号： C07D471/04 ,  A61K31/437 ,  C07D487/04

摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain triazolo compounds (referred to herein as TAZ compounds), and especially certain [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-c]pyrimidine compounds, which, inter alia, inhibit AXL receptor tyrosine kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit AXL receptor tyrosine kinase function, and in the treatment of diseases and conditions that are mediated by AXL receptor tyrosine kinase, that are ameliorated by the inhibition of AXL receptor tyrosine kinase function, etc., including proliferative conditions such as cancer, etc.

公开(公告)号：US09096531B2

公开(公告)日：2015-08-04

申请号：US13699692

申请日：2011-05-24

申请人： Hidekazu Masaki ,  Hiroshi Takasugi ,  Tomoyuki Nagayama ,  Ryutaro Shimono ,  Yujiro Uchino ,  Koichi Takayanagi

发明人： Hidekazu Masaki ,  Hiroshi Takasugi ,  Tomoyuki Nagayama ,  Ryutaro Shimono ,  Yujiro Uchino ,  Koichi Takayanagi

IPC分类号： A61K31/44 ,  A61K31/415 ,  C07D471/02 ,  C07D491/02 ,  C07D498/02 ,  C07D513/02 ,  C07D515/02 ,  C07D235/00 ,  C07D235/24 ,  C07D235/12 ,  C07D235/14 ,  C07D235/16 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D471/04 ,  C07D473/00

CPC分类号： C07D235/12 ,  C07D235/14 ,  C07D235/16 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D471/04 ,  C07D473/00

摘要： Provided is a novel compound which shows an antagonistic effect against T-type calcium channels, and is useful as a pharmaceutical product.A compound represented by general formula (I), and a pharmaceutical agent containing the same, are disclosed: wherein n represents the number of nitrogen atoms contained in the 6-membered fused aromatic ring, and is 0, 1 or 2; p represents the number of nitrogen atoms contained in the 6-membered aromatic ring, and is 0 or 1; X represents an oxygen atom, —SO2— or —N(R9)—; and R1 to R5 each represents a hydrogen atom or other substituents.

摘要翻译： 本发明提供了对T型钙通道具有拮抗作用的新化合物，作为药物有用。 公开了由通式（I）表示的化合物和含有该化合物的药剂，其中n表示6元稠合芳环中所含的氮原子数，为0,1或2; p表示6元芳香环中含有的氮原子数，为0或1; X表示氧原子，-SO 2 - 或-N（R 9） - ; 并且R 1至R 5各自表示氢原子或其它取代基。

公开(公告)号：US08987440B2

公开(公告)日：2015-03-24

申请号：US13139103

申请日：2009-12-15

申请人： Shinichiro Shoji ,  Hirotaka Suzuki

发明人： Shinichiro Shoji ,  Hirotaka Suzuki

IPC分类号： C07D498/02 ,  C07D498/10 ,  C07D273/08

CPC分类号： C07D273/08 ,  C07D498/10

摘要： A cyclic carbodiimide compound which is useful as an end-sealing agent for polymer compounds. The cyclic carbodiimide compound is represented by the following formula (i): In the above formula, X is a divalent group or a tetravalent group represented by the following formula (i-4). When X is divalent, q is 0 and when X is tetravalent, q is 1. Ar1 to Ar4 are each independently an aromatic group. They may be substituted by an alkyl group having 1 to 6 carbon atoms or phenyl group.

摘要翻译： 可用作聚合物化合物的端密封剂的环状碳二亚胺化合物。 环状碳二亚胺化合物由下式（i）表示：在上式中，X是由下式（i-4）表示的二价基团或四价基团。 当X为二价时，q为0，X为四价时，q为1. Ar 1〜Ar 4各自独立地为芳香族基团。 它们可以被具有1至6个碳原子的烷基或苯基取代。

公开(公告)号：US08980889B2

公开(公告)日：2015-03-17

申请号：US14477683

申请日：2014-09-04

申请人： Mochida Pharmaceutical Co., Ltd.

发明人： Akihiro Okano ,  Muneyoshi Makabe

IPC分类号： C07D498/02 ,  A61K31/535 ,  C07D471/04

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04

摘要： It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.

摘要翻译： 期望开发一种药物组合物，其用于预防和/或治疗与PDE10相关的各种疾病（例如精神障碍和神经变性障碍）的药剂中。 本发明提供：具有PDE10抑制作用的化合物，特别是具有下式（I）表示的4-杂芳基吡唑-5-羧酸酰胺结构的化合物或其药学上可接受的盐或其溶剂合物; 药物组合物包含作为活性成分的化合物或其药学上可接受的盐或其溶剂合物; 化合物或其药学上可接受的盐或其溶剂化物的医疗用途。

公开(公告)号：US08962618B2

公开(公告)日：2015-02-24

申请号：US13458452

申请日：2012-04-27

申请人： K. Raja Reddy ,  Jeff Stebbins ,  Serge H. Boyer ,  Mark D. Erion ,  Scott J. Hecker ,  Nicholas Brian Raffaele ,  Brett C. Bookser ,  Venkat Reddy Mali

发明人： K. Raja Reddy ,  Jeff Stebbins ,  Serge H. Boyer ,  Mark D. Erion ,  Scott J. Hecker ,  Nicholas Brian Raffaele ,  Brett C. Bookser ,  Venkat Reddy Mali

IPC分类号： A61K31/54 ,  A61K31/535 ,  C07D513/00 ,  C07D265/36 ,  C07D498/02 ,  C07F9/6561 ,  A61K31/52 ,  A61K31/662 ,  A61K31/665 ,  A61K31/675 ,  A61K45/06 ,  C07D473/16 ,  C07D473/34 ,  C07D473/40 ,  C07F9/30 ,  C07F9/32 ,  C07F9/653 ,  C07F9/6574

CPC分类号： A61K31/675 ,  A61K31/52 ,  A61K31/542 ,  A61K31/662 ,  A61K31/665 ,  A61K31/683 ,  A61K31/688 ,  A61K45/06 ,  A61P3/04 ,  A61P3/10 ,  C07D473/16 ,  C07D473/34 ,  C07D473/40 ,  C07F9/303 ,  C07F9/3229 ,  C07F9/40 ,  C07F9/48 ,  C07F9/65312 ,  C07F9/6552 ,  C07F9/6561 ,  C07F9/65616 ,  C07F9/65742 ,  A61K2300/00

摘要： The invention pertains to the use of fused bicyclo heterocyclic adducts of thiohdroxy pridines or primidines as diacylglycerol O-acyltransferase 1 DGAT-1 inhibitors to treat hyperlipidiemias and various diseases and disorders associated therewith. Other conditions also can be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease.

摘要翻译： 本发明涉及硫代二羟基吡啶或嘧啶的稠合双环杂环加合物作为二酰基甘油O-酰基转移酶1（DGAT-1）抑制剂用于治疗高脂血症和与其相关的各种疾病和病症的用途。 其他条件也可以被改善或避免，例如高餐后甘油三酸酯或饮食相关的高甘油三酯血症，与过量甘油三酯相关的心血管风险，以及超重患者，糖尿病患者或其他葡萄糖代谢紊乱如X综合征和胰岛素抵抗/葡萄糖不耐受 /或多囊卵巢疾病。