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1. WO2018138293 - TYROSINE AMIDE DERIVATIVES AS RHO- KINASE INHIBITORS

Publication Number WO/2018/138293
Publication Date 02.08.2018
International Application No. PCT/EP2018/052009
International Filing Date 26.01.2018
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
4353
ortho- or peri-condensed with heterocyclic ring systems
437
the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
519
Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/ or C07D455/257
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11
Drugs for disorders of the respiratory system
06
Antiasthmatics
C07D 471/04 (2006.01)
A61K 31/437 (2006.01)
A61K 31/519 (2006.01)
C07D 487/04 (2006.01)
C07D 519/00 (2006.01)
A61P 11/06 (2006.01)
CPC
A61K 31/437
A61K 31/4375
A61K 31/439
A61K 31/444
A61K 31/4725
A61K 31/496
Applicants
  • CHIESI FARMACEUTICI S.P.A. [IT/IT]; Via Palermo, 26/A 43122 PARMA, IT
Inventors
  • ACCETTA, Alessandro; IT
  • RANCATI, Fabio; IT
  • CAPELLI, Anna Maria; IT
  • CLARK, David Edward; IT
  • TISSELLI, Patrizia; IT
  • EDWARDS, Christine; IT
  • CHEGUILLAUME, Arnaud Jean Francois Auguste; IT
  • BHALAY, Gurdip; IT
Agents
  • MINOJA, Fabrizio; IT
Priority Data
17153785.530.01.2017EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) TYROSINE AMIDE DERIVATIVES AS RHO- KINASE INHIBITORS
(FR) DÉRIVÉS DE TYROSINE AMIDE UTILISÉS EN TANT QU'INHIBITEURS DE LA RHO-KINASE
Abstract
(EN)
The invention relates to compounds of formula (I) inhibiting Rho Kinase that are bicyclic dihydropyrimidine-carboxamide derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
(FR)
L'invention concerne des composés de formule (I) inhibant la Rho Kinase, qui sont des dérivés bicycliques de dihydropyrimidine-carboxamide, des procédés de préparation de ces composés, des compositions pharmaceutiques les contenant et leur utilisation thérapeutique. En particulier, les composés de l'invention peuvent être utiles dans le traitement de nombreux troubles associés à des mécanismes enzymatiques de ROCK, tels que les maladies pulmonaires comprenant l'asthme, la bronchopneumopathie chronique obstructive (BPCO), la fibrose pulmonaire idiopathique (IPF) et l'hypertension artérielle pulmonaire (HTAP).
Also published as
EA201991793
GE15169/1
IR139850140003003446
JP2019535289
PH12019501572
UAa201907753
Latest bibliographic data on file with the International Bureau