184368-70-5Relevant articles and documents
4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-3,6-DIHYDROPYRIDINE-1-(2H)-CARBOXAMIDE DERIVATIVES AS LIMK AND/OR ROCK KINASES INHIBITORS FOR USE IN THE TREATMENT OF CANCER
-
Paragraph 0157; 0160, (2021/12/07)
The present invention concerns a compound of formula (I), in particular as LIMK and/or ROCK kinases inhibitors. The present invention also concerns these new inhibitors for use for the treatment of a condition selected in the group consisting of: cancers, virion infections, ocular hypertension and glaucoma formation, Neurofibromatosis type 1 and 2, psoriatic lesions, inflammatory diseases and hyperalgesia, central sensitization and chronic pain, reproduction erectile dysfunction, and neuronal diseases. The present description discloses the syntheses and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 32 to 127; examples 1 to 96; families 1 to 8; compounds; biological studies; tables). An exemplary compound is e.g. 4-(5-m ethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-N-phenyl-3,6-dihydropyridine-1-(2H)-carboxamide (example 1; compound 5).
3-(1-OXO-5-(PIPERIDIN-4-YL)ISOINDOLIN-2-YL)PIPERIDINE-2,6-DIONE DERIVATIVES AND USES THEREOF
-
Page/Page column 307-308, (2020/08/28)
The present disclosure provides a compound of Formula (I), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein R1, R2, R3, Rx, and n are as defined herein, and methods of making and using same.
AMINOPYRIMIDINES AS ALK INHIBITORS
-
, (2018/03/25)
The present disclosure provides compounds represented by Formula (I): and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, and R7 are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I) for use to treat a condition or disorder responsive to inhibition of ALK such as cancer.
5,6-DIHYDRO-11H-INDOLO[2,3-B]QUINOLIN-11-ONES AS ALK INHIBITORS
-
, (2018/06/06)
The present disclosure provides compounds represented by Formula( I), and the pharmaceutically acceptable salts and solvates thereof, wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7, E and (B) are as defined as set forth in the specification. The present disclosure also provides compounds of Formula ( I) for use to treat a condition or disorder responsive to inhibition of ALK such as cancer.
SPIRO[CYCLOBUTANE-1,3'-INDOLIN]-2'-ONE DERIVATIVES AS BROMODOMAIN INHIBITORS
-
Page/Page column 62; 63, (2017/01/02)
The present invention provides novel spiro[cyclobutane-1,3'-indolin]-2'- derivatives of formula (I) in which Cy R1, R2, R4, L and 'm' are have the meaning given in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful as bromodomain inhibitors in the treatment or prevention of diseases or disorders where bromodomain inhibition is desired.
COMPOUNDS FOR THE MODULATION OF MYC ACTIVITY
-
Paragraph 301; 302, (2017/05/31)
The present invention provides novel compounds of Formulas (I) and (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases, e.g., cancers (e.g., breast cancer, prostate cancer, lymphoma, lung cancer, pancreatic cancer, ovarian cancer, neuroblastoma, or colorectal cancer), benign neoplasms, angio genesis, inflammatory diseases, fibrosis (e.g., polycystic kidney disease), autoinflammatory diseases, and autoimmune diseases in a subject.
Novel kinase inhibitors
-
Paragraph 0333-0335, (2017/08/02)
The present invention relates to a novel kinase inhibitor useful as a medicine for tumor, nerve disorder and mental illness. The purpose of the present invention is to provide a compound having improved blood-aqueous barrier penetrability to neurodegenerative diseases that cancer spreads to brain or progresses in brain. To this end, provided is a compound represented by chemical formula 1 or a pharmaceutically allowable salt thereof.COPYRIGHT KIPO 2017
TRPA1 MODULATORS
-
Paragraph 0359-0360, (2015/07/16)
This disclosure relates to polycyclic heteroaromatic compounds useful as TRPA1 modulators, as well as compositions and methods of treating pain that include the compounds.
ORGANIC COMPOUNDS
-
Page/Page column 64-65, (2009/05/28)
The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R5, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.
METHOD OF INHIBITING C-KIT KINASE
-
Page/Page column 65, (2008/06/13)
A method of reducing or inhibiting kinase activity of C-KIT in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to C-KIT using a compound of the present invention: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.