公开(公告)号：US20220388991A1

公开(公告)日：2022-12-08

申请号：US17766051

申请日：2020-09-30

Applicant: IDEMITSU KOSAN CO.,LTD.

Inventor： Shota SAWANO ,  Keiichi YASUKAWA ,  Takushi SHIOMI ,  Kazuki TERADA

IPC: C07D403/14 ,  C07D211/82 ,  C07D519/00 ,  C07D495/04 ,  C07D491/048 ,  C07F5/02 ,  C07D493/04 ,  H01L51/00 ,  H01L51/50

Abstract: A compound is represented by a formula (1) below. D is a group represented by a formula (11), (12) or (13) below; at least one D is a group represented by the formula (12) or (13); at least one R is a substituent; and a sum of the number of R serving as a substituent and the number of a group represented by the formula (12) or (13) is 3 or 4.

公开(公告)号：US10532976B2

公开(公告)日：2020-01-14

申请号：US15853653

申请日：2017-12-22

Applicant: National Institute of Biological Sciences, Beijing

Inventor： Niu Huang ,  Shiming Peng

IPC: C07C255/34 ,  A61P25/28 ,  A61P3/04 ,  C07D277/30 ,  C07D277/46 ,  C07D213/57 ,  C07D237/14 ,  C07D239/36 ,  C07D241/24 ,  C07D251/16 ,  C07D241/52 ,  C07D471/04 ,  C07D213/80 ,  C07D241/20 ,  C07D285/08 ,  C07D295/185 ,  C07D241/12 ,  C07D249/08 ,  C07D261/12 ,  C07D239/42 ,  C07D215/233 ,  C07D277/56 ,  C07D249/12 ,  C07D211/82 ,  C07D487/04 ,  C07D235/08 ,  C07D231/14 ,  C07D209/08 ,  C07D239/26 ,  C07D233/56 ,  C07D277/24 ,  C07D261/08 ,  C07D307/46 ,  C07D257/04 ,  C07D213/75 ,  C07D277/64 ,  C07C255/43

Abstract: The invention provides compounds that inhibit FTO (fat mass and obesity), including pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof, particularly obesity, with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

公开(公告)号：US10315994B2

公开(公告)日：2019-06-11

申请号：US15518743

申请日：2016-11-28

Applicant: Commonwealth Scientific and Industrial Research Organisation

Inventor： John Ryan ,  Mark York

IPC: C07D211/70 ,  C07D211/82 ,  C07D401/10 ,  A61K8/49 ,  C09D5/32 ,  A61Q17/04 ,  C07C49/543 ,  C07C49/792 ,  C07C49/807 ,  C09K15/30

Abstract: The present invention describes compounds and uses thereof in applications relating to absorption of electromagnetic energy. Preferred compounds are double bond-containing cyclic compounds capable of absorbing electromagnetic radiation energy and having improved photostability due to the presence and location of one or more fluorine groups in relation to the double bond of the ring.

公开(公告)号：US09890121B2

公开(公告)日：2018-02-13

申请号：US14767054

申请日：2014-02-12

Applicant: Cipla Limited

Inventor： Rajendra Narayanrao Kankan ,  Srinivas Laxminarayan Pathi ,  Venugopalarao Chinimilli

IPC: C07D211/70 ,  C07D211/82 ,  C07D213/06 ,  C07D213/58 ,  C07D213/42

CPC classification number: C07D213/58 ,  C07D213/42

Abstract: The present invention relates to a process for the preparation of Compound (A): wherein the process comprises contacting atazanavir base (Compound (II)) with sulphuric acid in a combination of two or more solvents and isolating compound (A). The present invention also relates to substantially pure Compound (A), and to Compound (A) devoid of mesityl oxide impurity. Mesityl oxide has the following formula:

公开(公告)号：US20160376229A1

公开(公告)日：2016-12-29

申请号：US15191511

申请日：2016-06-23

Applicant: Nitto Denko Corporation

Inventor： Roger Adami ,  Hao Bai ,  John Gaudette ,  Bharat Majeti ,  Seiji Nukui ,  Kwok Yin Tsang ,  Hai Wang ,  Haiqing Ying ,  Wenbin Ying

IPC: C07C271/16 ,  A61K47/22 ,  C07D207/12 ,  A61K47/16 ,  C07C237/16 ,  A61K31/713 ,  C07D211/86 ,  C07D211/82 ,  C07D211/74 ,  C07F9/06 ,  A61K47/24 ,  C07D205/04 ,  C07D207/09

CPC classification number: C07C271/16 ,  A61K9/127 ,  A61K9/5123 ,  A61K31/7105 ,  A61K31/713 ,  C07C237/08 ,  C07C237/16 ,  C07C237/50 ,  C07D205/04 ,  C07D207/09 ,  C07D207/12 ,  C07D211/74 ,  C07D211/82 ,  C07D211/86 ,  C07F9/06 ,  C07F9/106 ,  A61K2300/00

Abstract: This invention includes ionizable compounds, and compositions and methods of use thereof. The ionizable compounds can be used for making nanoparticle compositions for use in biopharmaceuticals and therapeutics. More particularly, this invention relates to compounds, compositions and methods for providing nanoparticles to encapsulate active agents, such as nucleic acid agents, and to deliver and distribute the active agents to cells, tissues, organs, and subjects.

Abstract translation: 本发明包括可离子化的化合物及其组合物及其使用方法。 可电离化合物可用于制备用于生物药物和治疗剂的纳米颗粒组合物。 更具体地说，本发明涉及用于提供纳米颗粒以包封活性剂（例如核酸试剂）的化合物，组合物和方法，并将活性剂递送和分配到细胞，组织，器官和受试者中。

公开(公告)号：US09452164B2

公开(公告)日：2016-09-27

申请号：US14267272

申请日：2014-05-01

Applicant: SANOFI

Inventor： Chantal Alcouffe ,  Reinhard Kirsch ,  Corentin Herbert ,  Gilbert Lassalle

IPC: A01N43/32 ,  A61K31/44 ,  A61K31/517 ,  A61K31/437 ,  A61K9/20 ,  C07D211/82 ,  C07D211/90 ,  C07D233/64 ,  C07D233/88 ,  C07D233/90 ,  C07D471/04 ,  A61K31/5377 ,  A61K45/06

CPC classification number: A61K31/517 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2059 ,  A61K31/437 ,  A61K31/5377 ,  A61K45/06 ,  C07D211/82 ,  C07D211/90 ,  C07D233/64 ,  C07D233/88 ,  C07D233/90 ,  C07D471/04

Abstract: The invention relates to compounds corresponding to formula (I): in which R2 and R3 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below: in which the wavy lines represent the phenyl nucleus to which R2 and R3 are attached. Preparation process and therapeutic use.

Abstract translation: 制备过程和治疗用途。

公开(公告)号：US09266982B2

公开(公告)日：2016-02-23

申请号：US13991044

申请日：2011-12-01

Applicant: Jun Liu ,  Mingfang Zheng ,  Weizhen Li ,  Haiying Zhang ,  Huaijie Wang ,  Yu Zhou ,  Tonglin Li ,  Lan Zhao ,  Hongfei Wu ,  Mingjun Xie ,  Chunhong Wu ,  Zhiguang Jia ,  Yanping Qi ,  Jilong Wang

Inventor： Jun Liu ,  Mingfang Zheng ,  Weizhen Li ,  Haiying Zhang ,  Huaijie Wang ,  Yu Zhou ,  Tonglin Li ,  Lan Zhao ,  Hongfei Wu ,  Mingjun Xie ,  Chunhong Wu ,  Zhiguang Jia ,  Yanping Qi ,  Jilong Wang

IPC: C07D471/04 ,  C07D211/70 ,  C07D211/82 ,  C07D213/46 ,  C08F110/02 ,  B01J31/18 ,  C07C2/32 ,  C07D213/127 ,  C07F15/02

CPC classification number: C08F110/02 ,  B01J31/183 ,  B01J2231/20 ,  B01J2531/0241 ,  B01J2531/842 ,  C07C2/32 ,  C07D213/127 ,  C07D471/04 ,  C07F15/025 ,  C07C11/02

Abstract: Provided are a process for preparing an N ortho acyl substituted nitrogen-containing heterocyclic compound and an aminal iron (II) complex thereof, and the use of the complexes obtained by the process in an olefin oligomerization catalyst. The N ortho acyl substituted nitrogen-containing heterocyclic compound in the present invention is for example 2-acyl-1,10-phenanthroline or 2,6-diacetyl pyridine as shown in formula b, and the N ortho acyl substituted nitrogen-containing heterocyclic compound in the present invention is produced by a reaction of a precursor thereof in a substituted or unsubstituted nitrobenzene. Preferably the precursor shown in formula I in the present invention is produced by 1,10-phenanthroline reacting with trialkyl aluminum, or a halogenoalkyl aluminum RnAIXm, or a substituted or unsubstituted benzyl lithium Ph′CH2Li, followed by hydrolysis. The preparation method provided in the present invention has a few synthetic steps, an easy process, a low toxic effect, and reduces the preparation costs of the catalyst, and has a promising outlook in the industrial application.

Abstract translation: 提供了制备N-邻酰基取代的含氮杂环化合物和其亚胺铁（II）络合物的方法，以及通过该方法在烯烃低聚催化剂中获得的络合物的用途。 本发明中的N-邻酰基取代的含氮杂环化合物例如如式b所示的2-酰基-1,10-菲咯啉或2,6-二乙酰基吡啶，并且N-邻酰基取代的含氮杂环化合物 在本发明中通过其前体在取代或未取代的硝基苯中的反应来制备。 优选地，本发明中式I所示的前体是通过与三烷基铝或卤代烷基铝RnAIXm或取代或未取代的苄基锂Ph'CH2Li反应的1,10-菲咯啉然后水解制备的。 本发明提供的制备方法具有几个合成步骤，易操作，低毒性，降低催化剂的制备成本，在工业应用前景看好。

公开(公告)号：US08859778B2

公开(公告)日：2014-10-14

申请号：US14108731

申请日：2013-12-17

Applicant: Chiesi Farmaceutici S.p.A.

Inventor： Gabriele Amari ,  Elisabetta Armani ,  Maurizio Delcanale

IPC: A61K31/435 ,  C07D211/82 ,  A61M16/14 ,  C07D213/89 ,  A61M15/00 ,  C07D213/30 ,  A61K45/06 ,  A61K31/44

CPC classification number: A61M15/0065 ,  A61K31/44 ,  A61K31/4704 ,  A61K45/06 ,  A61M16/14 ,  C07D213/30 ,  C07D213/61 ,  C07D213/89

Abstract: 1-Phenyl-2-pyridinyl alkyl alcohol compounds are effective as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and may be used to prevent and/or treat certain diseases or conditions.

公开(公告)号：US08853407B1

公开(公告)日：2014-10-07

申请号：US14099913

申请日：2013-12-07

Applicant: Muhammed Majeed ,  Rajendran Ramanujam ,  Kalyanam Nagabhushanam

Inventor： Muhammed Majeed ,  Rajendran Ramanujam ,  Kalyanam Nagabhushanam

IPC: C07D211/82 ,  C07D211/32

CPC classification number: C07D211/32 ,  C07D211/82

Abstract: A novel process for the synthesis of 4-aryl 4-acyl piperidine derivatives using indium metal is described. Specifically, a novel process for the synthesis of 4-acetyl 4-phenyl piperidine and its salts using indium metal is described.

Abstract translation: 描述了使用铟金属合成4-芳基4-酰基哌啶衍生物的新方法。 具体地说，描述了使用铟金属合成4-乙酰基4-苯基哌啶及其盐的新方法。

公开(公告)号：US08722895B2

公开(公告)日：2014-05-13

申请号：US13859574

申请日：2013-04-09

Applicant: Akebia Therapeutics Inc.

Inventor： Richard M. Kawamoto ,  Shengde Wu ,  Artem G. Evdokimov ,  Kenneth D. Greis ,  Angelique Sun Boyer ,  Namal C. Warshakoon

IPC: A01N43/40 ,  A61K31/44 ,  C07D213/62 ,  C07D213/78 ,  C07D211/70 ,  C07D211/82 ,  C07D213/46 ,  C07D213/90 ,  C07D213/00

CPC classification number: A61K31/4418 ,  A61K31/4433 ,  C07C235/60 ,  C07C237/42 ,  C07C255/57 ,  C07D213/65 ,  C07D213/81 ,  C07D295/192 ,  C07D401/04 ,  C07D401/10 ,  C07D405/04 ,  C07D405/10 ,  C07D417/04

Abstract: The present disclosure relates to HIF-1α prolyl hydroxylase inhibitors, compositions which comprise the HIF-1α prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.

Abstract translation: 本公开内容涉及HIF-1α脯氨酰羟化酶抑制剂，其包含本文所述的HIF-1α脯氨酰羟化酶抑制剂的组合物以及用于控制外周血管疾病（PVD），冠状动脉疾病（CAD），心力衰竭， 缺血和贫血。