1173897-86-3Relevant academic research and scientific papers
Lysophosphatidic acid receptor antagonists and preparation method thereof
-
Paragraph 0584-0585; 0586-0588, (2020/07/29)
The invention belongs to the technical field of medicinal chemistry, and particularly relates to lysophosphatidic acid receptor antagonists and a preparation method thereof. The applicant surprisinglyfinds that compounds provided by the invention have high LPAR1 antagonistic activity and selectivity, low toxicity, good metabolic stability and good drug development prospect, and can be used for preventing or treating diseases or symptoms related to LPAR1. The applicant also accidentally finds that the IC50 value of part of the compounds can be as low as 300 nM or below and even 50 nM or below.Moreover, the compounds disclosed by the invention have better safety, and the CC50 range of the compounds can reach 200 [mu]M or above. In addition, the compounds of the present invention have goodmetabolic stability in humans, rats, and mice, such excellent inhibitory activity being very desirable for their use as LPAR1 inhibitors in the above diseases or disorders. In addition, the preparation method of the compounds is simple, mild in reaction condition, high in product yield and suitable for industrial production.
TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
-
Page/Page column 75, (2016/05/02)
The present invention is directed to substituted indole compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, adisease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
Povarov reaction, scope and limitations: Preparation of diversely heterocyclic tetrahydro-1H-cyclopenta[c]quinolines
Ni?o, Patricia,Caba, Marta,Aguilar, Nuria,Terricabras, Emma,Albericio, Fernando,Fernàndez, Joan-Carles
, p. 1117 - 1130 (2017/04/28)
Parallel synthesis of diverse heterocyclic-tetrahydro-1H-cyclopenta[c]quinolines in excellent yields and high endo diastereoselectivity has been described hereia These compounds are highly functionalized natural product-like tricyclic systems, which may be useful as biologically relevant targets. Fine tuning of the reaction conditions need to be performed depending on the nature and molecular structure of the heterocyclic aromatic carbaldehyde, as well as the choice of the Lewis acid catalyst. Synthesis of the heterocyclic aromatic aldehyde precursors of the Povarov Reaction is also described.
Discovery of Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor CC-223
Mortensen, Deborah S.,Perrin-Ninkovic, Sophie M.,Shevlin, Graziella,Zhao, Jingjing,Packard, Garrick,Bahmanyar, Sogole,Correa, Matthew,Elsner, Jan,Harris, Roy,Lee, Branden G. S.,Papa, Patrick,Parnes, Jason S.,Riggs, Jennifer R.,Sapienza, John,Tehrani, Lida,Whitefield, Brandon,Apuy, Julius,Bisonette, René R.,Gamez, James C.,Hickman, Matt,Khambatta, Godrej,Leisten, Jim,Peng, Sophie X.,Richardson, Samantha J.,Cathers, Brian E.,Canan, Stacie S.,Moghaddam, Mehran F.,Raymon, Heather K.,Worland, Peter,Narla, Rama Krishna,Fultz, Kimberly E.,Sankar, Sabita
supporting information, p. 5323 - 5333 (2015/08/03)
We report here the synthesis and structure-activity relationship (SAR) of a novel series of mammalian target of rapamycin (mTOR) kinase inhibitors. A series of 4,6- or 1,7-disubstituted-3,4-dihydropyrazino[2,3-b]pyrazine-2(1H)-ones were optimized for in v
BICYCLIC UREAS AND THIADIAZOLIDINE-1,1-DIOXIDES AS CETP INHIBITORS
-
, (2015/02/25)
Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, wherein X is -C(=O) or -S(O)2-, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
PHARMACEUTICAL FORMULATIONS, PROCESSES, SOLID FORMS AND METHODS OF USE RELATING TO 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL)PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO[2,3-b]PYRAZIN-2(1H)-ONE
-
, (2014/10/29)
Provided herein are formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one.
PYRIDINE-2-AMIDES USEFUL AS CB2 AGONISTS
-
Page/Page column 49, (2014/06/24)
The invention relates to CB2 agonists of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
-
, (2013/10/22)
The present invention belongs to the field of EPl receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EPl receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EPl receptor as well as to pharmaceutical compositions comprising them.
SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
-
, (2013/10/22)
The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
NOVEL PYRIDINE DERIVATIVES
-
Page/Page column 92-93, (2013/02/27)
The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
