PATENTSCOPE: EN_ALL:nmr AND PA:servier

NEW CRYSTALLINE FORM OF A BCL-2 INHIBITOR, A PROCESS FOR ITS PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING IT (Fri, 11 Jan 2019)
Crystalline form II of Compound A. HC1: (Formula) characterised by its X-ray powder diffraction diagram and solid-state 13C NMR spectrum, and pharmaceutical compositions containing it.
>> Read More

5-[3-[PIPERAZIN-1-YL]-3-OXO-PROPYL]-IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS ADAMTS 4 AND 5 INHIBITORS FOR TREATING E.G. OSTEOARTHRITIS (Fri, 15 Dec 2017)
The present invention discloses 5-[3-[piperazin-l-yl]-3-oxo-propyl]-imidazolidine-2,4-dione derivatives according to Formula (I), wherein R1, R2, R3a, R3b, R6a, R6b, the subscript n and Cy are as defined herein. The present invention relates to compounds inhibiting ADAMTS 4 and 5 for the prophylaxis or treatment of inflammatory diseases or diseases involving degradation of cartilage or disruption of cartilage homeostasis, such as e.g. osteoarthritis.
>> Read More

NEW PIPERIDINYL DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM (Fri, 15 Dec 2017)
Compounds of formula (I) wherein R1, R2, R3, n and W are as defined in the description. Medicaments.
>> Read More

5-[3-[PIPERIDIN-1-YL]-3-OXO-PROPYL]-IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS ADAMTS 4 AND 5 INHIBITORS FOR TREATING E.G. OSTEOARTHRITIS (Fri, 15 Dec 2017)
The present invention discloses 5-[3-[piperazin-l-yl]-3-oxo-propyl]-imidazolidine-2,4-dione derivatives according to Formula (I), wherein R1, R2, R3a, R3b, R6a, R6b, the subscript n and Cy are as defined herein. The present invention relates to compounds inhibiting ADAMTS 4 and 5 for the prophylaxis or treatment of inflammatory diseases or diseases involving degradation of cartilage or disruption of cartilage homeostasis, such as e.g. osteoarthritis.
>> Read More

(5R)-5-[3-[(3S)-4-(4-CHLORO-3-METHOXY-5-METHYL-PHENYL)-3-METHYL-PIPERAZIN-1-YL]- 3-OXO-PROPYL]-5-METHYL-IMIDAZOLIDINE-2,4-DIONE AS ADAMTS 4 AND 5 INHIBITOR FOR TREATING E.G. OSTEOARTHRITIS (Fri, 15 Dec 2017)
The present invention discloses (5R)-5-[3-[(3S)-4-(4-chloro-3-methoxy-5-methyl-phenyl)-3-methyl-piperazin-l-yl]-3-oxo-propyl]-5-methyl-imidazolidine-2,4-dione according to Formula (I). The present invention relates to the compound of formula (I) inhibiting ADAMTS 4 and 5 for the prophylaxis or treatment of inflammatory diseases or diseases involving degradation of cartilage or disruption of cartilage homeostasis, such as e.g. osteoarthritis.
>> Read More

NEW AMMONIUM DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM (Fri, 28 Jul 2017)
Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6 and Y are as defined in the description. Medicaments.
>> Read More

NEW IMIDAZO[4,5-B]PYRIDINE DERIVATIVES AS DUAL DYRK1/CLK1 INHIBITORS (Fri, 07 Apr 2017)
(Formula I) Compounds of formula (I) usefull for the treatment of cancer, neurodegenerative disorders and metabolic disorders.
>> Read More

NEW PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES AS DUAL DYRK1/CLK1 INHIBITORS (Fri, 07 Apr 2017)
(Formula I) Compounds of formula (I) usefull for the treatment of cancer, neurodegenerative disorders and metabolic disorders.
>> Read More

NEW HYDROXYACID DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM (Fri, 30 Dec 2016)
Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R14, A and n are as defined in the description. Medicaments.
>> Read More

NEW BICYCLIC DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM (Fri, 30 Dec 2016)
Compounds of formula (I); wherein R1, R2, R3, R4, R5, R6, R7, R8, R14, W, A and n are as defined in the description. Medicaments.
>> Read More

NEW AMINOACID DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM (Fri, 30 Dec 2016)
Compounds of formula (I): wherein R1, R2, R5, R6, R7, R12, X, Y, A, E and n are as defined in the description. Medicaments.
>> Read More

NEW HYDROXYESTER DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM (Fri, 30 Dec 2016)
Compounds of formula (1) wherein R1, R2, R3, R4, R5, R6, R7, R13, Ra, Rb, A and n are as defined in the description. Medicaments containing them for use in the treatment of cancers.
>> Read More

TGR5 MODULATORS AND METHODS OF USE THEREOF (Fri, 23 Dec 2016)
The application relates to compounds of formula (A): or a salt, solvate, ester, tautomer, amino acide conjugate, or metabolite thereof. The compounds of formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.
>> Read More

5-[(PIPERAZIN-1-YL)-3-OXO-PROPYL]-IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS ADAMTS INHIBITORS FOR THE TREATMENT OF OSTEOARTHRITIS (Fri, 01 Jul 2016)
The present invention discloses compounds according to Formula (I), wherein R, R2, R3a, R3b, and Cy are as defined herein. The present invention discloses compounds inhibiting ADAMTS, methods for their production, pharmaceutical compositions comprising the same and methods for the prophylaxis and/or treatment of inflammatory conditions and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis.
>> Read More

NEW THIENOPYRIMIDINE DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM (Fri, 03 Jul 2015)
Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R12, X, A and n are as defined in the description.
>> Read More

NEW ISOINDOLINE OR ISOQUINOLINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM (Fri, 30 Jan 2015)
Compounds of formula (I): (I) wherein Het, R3, R4, R5, R7, R8, R9, T, p, p', q, and q' are as defined in the description are pro-apoptotic agents useful in the treatment of cancers and of auto-immune and immune system diseases.
>> Read More

AGENTS FOR TREATING DISORDERS INVOLVING MODULATION OF RYANODINE RECEPTORS (Fri, 25 Oct 2013)
The present invention relates to 1,4-benzothiazepine derivatives and their use to treat conditions, disorders and diseases associated with ryanodine receptors (RyRs) that regulate calcium channel functioning in cells. The invention also discloses pharmaceutical compositions comprising the compounds and uses thereof to treat diseases and conditions associated with RyRs, in particular cardiac, musculoskeletal and central nervous system (CNS) disorders.
>> Read More

PROCESS FOR PREPARING BENZOTHIAZEPINES FROM GAMMA-AMINOALKYLBENZENES (Sat, 12 Sep 2009)
The invention provides a process for preparing a 2,3,4,5-tetrahydro[1,4]benzothiazepine of formula: [I] by reacting a [2-(acylaminoethyl)thio]arene of formula [II] with an aldehyde or a multimer thereof, and with an acid. The invention also provides for first reacting the [2-(acylaminoethyl)thio]arene with the aldehyde or multimer thereof and a base to form an [N-hydroxymethyl-2-[acylaminoethyl)thio]arene of formula [III]; then treating the [N-hydroxymethyl-2-(acylaminoethyl)thio]arene with the acid to form the 2,3,4,5-tetrahydro[1,4]benzothiazepine.
>> Read More

3-SUBSTITUTED-[1,2,3]-BENZOTRIAZINONE COMPOUND FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES (Fri, 18 Jul 2008)
This invention relates to the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for higher order behaviors. These brain networks are involved in cognitive abilities related to memory impairment, such as is observed in a variety of dementias, and in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia and affective disorders. In a particular aspect, the present invention relates to a compound useful for treatment of such conditions, and methods of using this compound for such treatment.
>> Read More

PROCESS FOR THE PREPARATION OF HIGH PURITY PERINDOPRIL AND INTERMEDIATES USEFUL IN THE SYNTHESIS (Fri, 08 Aug 2003)
The invention relates to 1ᇁ2࿈S)ᇁ⏧1࿈S)ᇁ࿈ethoxycarbonyl)butylamino]propionyl}ᇁ࿈3aS,7aS)octahydroindolᇁ2࿈S)ᇁcarboxylic acid of the Formula I and the tᇁbutylamine salt of the Formula I' thereof free of contaminations derivable from dicyclohexyl carbodiimide, and a process for the preparation thereof. The invention also relates to new intermediates of the general Formula III ࿈wherein R stands for lower alkyl or aryl lower alkyl). The compound of the Formula I ᇁ perindopril ᇁ is a known ACE inhibitor.
>> Read More