- HETEROCYCLIC COMPOUND INTERMEDIATE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
-
Disclosed by the invention is a heterocyclic compound, an intermediate, and a preparation method therefor and an application thereof. Provided by the invention are a heterocyclic compound as shown in formula I, and a stereoisomer, a geometric isomer, a tautomer, a nitrogen oxide, a hydrate, a solvate, a metabolite, an ester, a pharmaceutically acceptable salt or a prodrug thereof. The heterocyclic compound hasa high P2X3 antagonistic activity, and has good selectivity, low toxicity, good metabolic stability and little taste influence.
- -
-
Paragraph 0439-0441
(2021/10/07)
-
- HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
-
The present invention provides a heterocyclic compound of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof or a hydrate thereof, wherein A, A′ B, D, R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising a compound of formula (I) as an active ingredient, methods of production, and methods of use thereof. Particularly, the present invention provides a compound of formula (I) useful for treating or preventing a disease, condition or disorder associated with protein kinases, preferably Janus Kinase family.
- -
-
Paragraph 0413
(2014/06/23)
-
- HETEROCYCLYL PYRIMIDINE ANALOGUES AS TYK2 INHIBITORS
-
The present invention relates to compounds of formula (I), wherein R, R1, X1 to X5 have the meaning as cited in the description and the claims. Said compounds are useful as TYK2 inhibitors for the treatment or prophylaxis
- -
-
Page/Page column 66
(2014/01/07)
-
- HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
-
The present invention provides a heterocyclic compound of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof or a hydrate thereof, wherein A, A' B, D, R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising a compound of formula (I) as an active ingredient, methods of production, and methods of use thereof. Particularly, the present invention provides a compound of formula (I) useful for treating or preventing a disease, condition or disorder associated with protein kinases, preferably Janus Kinase family.
- -
-
Page/Page column 68
(2012/12/13)
-
- A fluorine scan of the phenylamidinium needle of tricyclic thrombin inhibitors: Effects of fluorine substitution on pKa and binding affinity and evidence for intermolecular C-F...CN interactions
-
The H-atoms of the phenylamidinium needle of tricyclic thrombin inhibitors, which interacts with Asp189 at the bottom of the selectivity pocket S1 of the enzyme, were systematically exchanged with F-atoms in an attempt to improve the pharmacokinetic prope
- Olsen, Jacob,Seiler, Paul,Wagner, Bjoern,Fischer, Holger,Tschopp, Thomas,Obst-Sander, Ulrike,Banner, David W.,Kansy, Manfred,Mueller, Klaus,Diederich, Francois
-
p. 1339 - 1352
(2007/10/03)
-
- SAR and pharmacokinetic studies on phenethylamide inhibitors of the hepatitis C virus NS3/NS4A serine protease
-
SAR on the phenethylamide 1 (Ki 1.2μM) in the P2- and the P′-position led to potent inhibitors, one of which showed good exposure and low clearance when administered intramuscularly to rat.
- Malancona, Savina,Colarusso, Stefania,Ontoria, Jesus M.,Marchetti, Antonella,Poma, Marco,Stansfield, Ian,Laufer, Ralph,Di Marco, Annalise,Taliani, Marina,Verdirame, Maria,Gonzalez-Paz, Odalys,Matassa, Victor G.,Narjes, Frank
-
p. 4575 - 4579
(2007/10/03)
-
- IMMEDIATE RELEASE PHARMACEUTICAL FORMULATION
-
According to the present invention there is provided an immediate release pharmaceutical formulation comprising, as active ingredient, a compound of formula (I), wherein R1 represents C?1-2#191 alkyl substituted by one or more fluoro substituen
- -
-
-
- MODIFIED RELEASE PHARMACEUTICAL FORMULATION
-
A modified release pharmaceutical composition comprising, as active ingredient, a compound of formula (I), wherein R1 represents C?1-2#191 alkyl substituted by one or more fluoro substituents;R2 represents hydrogen, hydroxy, methoxy
- -
-
-
- PHARMACEUTICAL COMBINATION
-
There is provided a combination product comprising: (1) a compound of claim 1 in WO 02/44145 or a compound of claim 20 in WO 02/44145 (or derivative thereof)or a pharmaceutically-acceptable derivative thereof; and (1) a compound as defined in claim 1 of WO 01/28992 or (2) a compound of Claim 34 of WO 01/28992 or (3) Compound A or B or C or D (or pharmaceutically-acceptable salts thereof) for use in treating arrhythmia or a coagulation controlled complication thereof.
- -
-
-
- NEW SALTS
-
There is provided pharmaceutically-acceptable acid addition salts of compounds of formula (I), wherein R1 represents C1-2 alkyl substituted by one or more fluoro substituents; R2 represents C1-2 alkyl; and n rep
- -
-
-
