145218-19-5Relevant articles and documents
COMPOUND FOR INHIBITING PGE2/EP4 SIGNALING TRANSDUCTION INHIBITING, PREPARATION METHOD THEREFOR, AND MEDICAL USES THEREOF
-
, (2022/03/14)
A compound of formula (I), a preparation method therefor, a pharmaceutical composition containing a derivative thereof, and the therapeutic uses thereof, especially inhibiting PGE2/EP4 signalling transduction and the uses thereof for treating cancer, acute or chronic pain, migraine, osteoarthritis, rheumatoid arthritis, gout, bursitis, ankylosing spondylitis, primary dysmenorrhea, tumour or arteriosclerosis.
1,5,7-TRISUBSTITUTED ISOQUINOLINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES
-
Paragraph 0250-0251; 0286-0287, (2020/08/30)
The present disclosure relates to 1,5,7-trisubstituted isoquinoline derivatives, their preparation and pharmaceutical use. In particular, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof. The definitions of the groups in the formula can be found in the specification and claims.
COMPOUNDS, COMPOSITIONS, AND METHODS OF USE
-
Paragraph 0295, (2020/12/11)
Described herein are compounds that act as CYP46A1 inhibitors, compositions comprising these compounds, and methods of their use into treating neurodegenerative diseases and the like, or a pharmaceutically active salt thereof. The present invention relates to compounds represented by the formula wherein each symbol is as defined in the specification, or a pharmaceutically active salt thereof.
PqsR INVERSE AGONISTS
-
Page/Page column 67, (2020/01/31)
The present invention relates to a compound according to general formula (I), which acts as an inhibitor of PqsR (the currently only known receptor for the Pseudomonas Quinolone Signal (PQS)); to a pharmaceutical composition containing one or more of the compound(s) of the invention; to a combination preparation containing at least one compound of the invention and at least one further active pharmaceutical ingredient; and to uses of said compound(s), including the use as a medicament, e.g. the use in the treatment or prophylaxis of a bacterial infection, especially a Pseudomonas aeruginosa or Burkholderia infection.
5-(PYRIMIDIN-4-YL)-2-(PYRROLIDIN-1-YL)NICOTINONITRILE COMPOUNDS AS IKKE, TBK1 AND/OR SIK2 KINASES INHIBITORS
-
Page/Page column 19-20, (2018/09/19)
The invention provides compounds of formula (I) wherein R is ?CH3 or ?CH2CH3 and pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful in the treatment of diseases or disorders mediated by IKKE, TBK1 and/or SIK2 mechanisms in a subject, for example cancer and inflammatory and tissue repair disorders. The invention also provides uses of the compounds of formula (I) and compositions containing them. (Formula (I))
3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
-
Paragraph 00602-00604, (2017/10/06)
The present invention provides compounds, compositions thereof, and methods of using the same.
Design of Potent and Orally Active GPR119 Agonists for the Treatment of Type II Diabetes
Liu, Ping,Hu, Zhiyong,Dubois, Byron G.,Moyes, Christopher R.,Hunter, David N.,Zhu, Cheng,Kar, Nam Fung,Zhu, Yuping,Garfunkle, Joie,Kang, Ling,Chicchi, Gary,Ehrhardt, Anka,Woods, Andrea,Seo, Toru,Woods, Morgan,Van Heek, Margaret,Dingley, Karen H.,Pang, Jianmei,Salituro, Gino M.,Powell, Joyce,Terebetski, Jenna L.,Hornak, Viktor,Campeau, Louis-Charles,Lamberson, Joe,Ujjainwalla, Fez,Miller, Michael,Stamford, Andrew,Wood, Harold B.,Kowalski, Timothy,Nargund, Ravi P.,Edmondson, Scott D.
supporting information, p. 936 - 941 (2015/08/24)
We report herein the design and synthesis of a series of potent and selective GPR119 agonists. Our objective was to develop a GPR119 agonist with properties that were suitable for fixed-dose combination with a DPP4 inhibitor. Starting from a phenoxy analo
BETA-TETRAZOLYL-PROPIONIC ACIDS AS METALLO-BETA-LACTAMASE INHIBITORS
-
Page/Page column 63, (2015/11/27)
The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
FATTY ACID SYNTHASE INHIBITORS
-
Page/Page column 105, (2014/01/18)
This invention relates to novel spirocyclic piperidines according to Formula (I) which are inhibitors of fatty acid synthase (FAS), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
SUBSTITUTED CYCLOPROPYL COMPOUNDS
-
Page/Page column 47; 48, (2014/04/17)
Substituted cyclopropyl piperidinyl compounds and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-1 19. Pharmaceutical compositions and methods of treatment are also included.