[EN] PYRIDINONE- AND PYRIDAZINONE-BASED COMPOUNDS AND MEDICAL USES THEREOF<br/>[FR] COMPOSÉS À BASE DE PYRIDINONE ET DE PYRIDAZINONE ET UTILISATIONS MÉDICALES ASSOCIÉES
申请人:HLA TIMOTHY
公开号:WO2019173790A1
公开(公告)日:2019-09-12
The various examples presented herein are directed to compounds of the formula A-L1-Het1-L2-Cy1 or a pharmaceutical acceptable salt, polymorph, prodrug, solvate or clathrate thereof, wherein: A is cycloalkyl, aryl, arylalkyl or heterocyclyl; Het1 is heterocyclyl containing at least two heteroatoms; Cy1 is a heterocyclyl; L1 is a bond, alkyl, alkenyl or alkynyl linker; L2 is an acyl or alkyl linker; and A and Cy1 are different. The compounds are useful in the treatment of fibrotic diseases, abnormal vascular leak and pathological angiogenesis.
The invention relates to new piperidino-dihydrothienopyrimidines of formula 1, as well as pharmacologically acceptable salts thereof,
wherein X is SO or SO
2
, but preferably SO, and wherein R
1
, R
2
, R
3
and R
4
may have the meanings given in claim
1
, as well as pharmaceutical compositions which contain these compounds.
These new piperidino-dihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers.
DRUG COMBINATIONS CONTAINING PDE4 INHIBITORS AND NSAIDS
申请人:Nickolaus Peter
公开号:US20120035143A1
公开(公告)日:2012-02-09
The present invention relates to new drug combinations which contain in addition to one or more PDE4-inhibitors at least one NSAID (=non-steroidal anti-inflammatory drug) (2), processes for preparing them and their use in treating in particular respiratory complaints such as for example COPD, chronic sinusitis and asthma.
The invention particularly relates to those drug combinations which contain, in addition to one or more, preferably one PDE4 inhibitor of general formula 1
wherein X is SO or SO
2
, but preferably SO, and wherein
R
1
, R
2
, R
3
and R
4
have the meanings given in claim
1,
at least one NSAID (2), the preparation thereof and the use thereof for the treatment of respiratory complaints.
COMBINATIONS OF MEDICAMENTS, CONTAINING PDE4-INHIBITORS AND EP4-RECEPTOR-ANTAGONISTS
申请人:Nickolaus Peter
公开号:US20130225609A1
公开(公告)日:2013-08-29
The present invention relates to new medicament combinations which contain in addition to one or more PDE4-inhibitors (1) at least one EP4 receptor antagonist (2), as well as the use thereof for the treatment of preferably respiratory complaints such as particularly COPD, chronic sinusitis and asthma.
The invention relates in particular to those medicament combinations which contain, in addition to one or more, preferably one, PDE4 inhibitor of general formula 1
wherein X is SO or SO
2
, but preferably SO, and wherein
R
1
, R
2
, R
3
and R
4
have the meanings given in claim
1,
at least one EP4 receptor antagonist (2), the preparation thereof and the use thereof for the treatment of respiratory complaints.
[EN] BICYCLIC PYRIDAZINE COMPOUNDS AS PIM INHIBITORS<br/>[FR] COMPOSÉS PYRIDAZINES BICYCLIQUES EN TANT QU'INHIBITEURS DE PIM
申请人:AMGEN INC
公开号:WO2012148775A1
公开(公告)日:2012-11-01
The invention relates to bicyclic compounds of formulas I and I', and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.