PATENTSCOPE: EN_ALL:nmr AND PA:sanofi

NOVEL CONJUGATES OF A PHARMACEUTICAL AGENT AND A MOIETY CAPABLE OF BINDING TO A GLUCOSE SENSING PROTEIN (Fri, 07 Jun 2019)
The invention describes novel conjugates of formula (I) of a pharmaceutical agent and a moiety capable of binding to a glucose sensing protein allowing a reversible release of the pharmaceutical agent depending on the glucose concentration.
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ANTIBACTERIAL COMPOUNDS PRODUCED BY THE MICROORGANISM STRAIN CORALLOCOCCUS CORALLOIDES ST201330 (DSM 24989) (Fri, 22 Mar 2019)
The present invention relates to novel compounds of the formula (I), in which R is is hydrogen or hydroxy, that can be obtained by fermentation of the microorganism strain Corallococcus coralloides ST201330 (DSM 24989).
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SEQUANAMYCIN MACROLIDES USEFUL IN THE TREATMENT OF TUBERCULOSIS (Fri, 01 Feb 2019)
The present invention relates to compounds of formula (I), their process of preparation and the therapeutic use thereof. These sequanamycin macrolides are useful in the treatment of tuberculosis.
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COMBINATION COMPRISING PALBOCICLIB AND 6-(2,4-DICHLOROPHENYL)-5-[4-[(3S)-1-(3-FLUOROPROPYL)PYRROLIDIN-3-YL]OXYPHENYL]-8,9-DIHYDRO-7H-BENZO[7] ANNULENE-2-CARBOXYLIC ACID AND ITS USE FOR THE TREATMENT OF CANCER (Fri, 01 Feb 2019)
Herein are provided a combination of palbociclib and of 6-(2,4-dichlorophenyl)-5-[4-[(3S)-1 -(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2- carboxylic acid or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing such a combination, and the therapeutic uses thereof, in particular for the treatment of cancer, including breast cancer.
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SEQUANAMYCIN MACROLIDES USEFUL IN THE TREATMENT OF TUBERCULOSIS (Fri, 01 Feb 2019)
The present application relates to compounds of formula (I), their process of preparation and the therapeutic uses thereof. These sequanamycin macrolides are useful in the treatment of tuberculosis.
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SEQUANAMYCIN MACROLIDES USEFUL IN THE TREATMENT OF TUBERCULOSIS (Fri, 01 Feb 2019)
The present invention relates to the compounds of formula (I), this process of preparation, and the therapeutic uses thereof. These macrolides of formula (I) are useful in the treatment of tuberculosis.
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ETHYNYL COMPOUNDS, THEIR PREPARATION AND THEIR THERAPEUTIC USE FOR THE TREATMENT OF MALARIA (Fri, 11 Jan 2019)
The present disclosure relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein R1 means a fluorine atom or a perhalogeno linear alkyl radical containing 1, 2 or 3 carbon atoms; R2 means a chlorine atom, a linear alkyl radical containing 1, 2 or 3 carbon atoms or a perhalogeno linear alkyl radical containing 1, 2 or 3 carbon atoms, and R means a hydrogen atom or a radical of formula (la). The present disclosure also relates to processes for their preparation as well their therapeutic uses, in particular such as for use in the treatment of malaria.
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PEPTIDIC LINKERS AND CRYPTOPHYCIN CONJUGATES, USEFUL IN THERAPY, AND THEIR PREPARATION (Fri, 16 Nov 2018)
The present disclosure relates to compounds of formula (I): RCG1-L-P (I) wherein RCG1 represents a reactive chemical group being reactive towards a chemical group present on a polypeptide such as an antibody; P represents H, OH or an activated O; and L represents a specific linker. The disclosure also relates to cryptophycin payloads, as well as to cryptophycin conjugates, to compositions containing them and to their therapeutic use, especially as anticancer agents. The disclosure also relates to the process for preparing these conjugates.
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FUSED PENTACYCLIC IMIDAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY (Fri, 02 Nov 2018)
A compound of formula (I) as defined herein, or a pharmaceutically acceptable salt thereof, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
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FUSED PENTACYCLIC IMIDAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY (Fri, 21 Sep 2018)
A series of substituted fused pentacyclic imidazopyridine and imidazopyridazine derivatives, and analogues thereof, being potent modulators of human TNFα activiy, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
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AZETIDINE COMPOUNDS AS GPR119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS (Fri, 31 Aug 2018)
The present invention relates to azetidine compounds. The azetidine compounds are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of azetidine compounds as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
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ROR gamma (RORy) modulators (Fri, 15 Jun 2018)
The present application relates to compounds according to (Formula IA) or (Formula IB): (Formula IA) (Formula IB) or a pharmaceutically acceptable salt thereof. The compounds can be used as inhibitors of RORγ and are useful for the treatment of RORγ mediated diseases.
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CONJUGATES COMPRISING AN GLP-1/GLUCAGON DUAL AGONIST, A LINKER AND HYALURONIC ACID (Fri, 08 Jun 2018)
The present invention relates to a conjugate or a pharmaceutically acceptable salt thereof comprising an GLP-1/Glucagon receptor agonist, a linker and a hyaluronic acid hydrogel bearing - L1 −L2 - L - Y - R20 groups, wherein Y represents an GLP-1/Glucagon receptor agonist moiety; and -L is a linker moiety - by formula (la), wherein the dashed line indicates the attachment to one of the amino groups of the GLP-1/Glucagon receptor agonist moiety by forming an amide bond. The invention further relates to pharmaceutical compositions comprising said conjugates as well as their use as a medicament for treating or preventing diseases or disorders which can be treated by GLP-1/Glucagon receptor agonist.
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NOVEL SUBSTITUTED N-(3-FLUOROPROPYL)-PYRROLIDINE COMPOUNDS, PROCESSES FOR THEIR PREPARATION AND THERAPEUTIC USES THEREOF (Fri, 25 May 2018)
The present invention relates to novel substituted N-(3-fluoropropyl)-pyrrolidine compounds of formula (l-A): wherein R1 and R2 represent independently a hydrogen atom or a deuterium atom; A represents an oxygen or nitrogen atom; and SERM-F represents a selective estrogen receptor modulator fragment comprising an aryl or heteroaryl group linked to the adjacent "A" group. The invention also relates to the preparation and to the therapeutic uses of the compounds of formula (l-A) as inhibitors and degraders of estrogen receptors.
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SUBSTITUTED PYRIDO[3,4-B]INDOLES FOR THE TREATMENT OF CARTILAGE DISORDERS (Sat, 12 May 2018)
The present invention relates to 8-aryl-substituted and 8-heteroaryl-substituted 9H-pyrido[3,4-b]indoles of the formula (I), in which A, E, G, R1 to R6 and R10 are as defined in the claims, which stimulate chondrogenesis and cartilage matrix synthesis and can be used in the treatment of cartilage disorders and conditions in which a regeneration of damaged cartilage is desired, for example joint diseases such as osteoarthritis. The invention furthermore relates to processes for the synthesis of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
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MULTIVALENT PNEUMOCOCCAL POLYSACCHARIDE-PROTEIN CONJUGATE COMPOSITION (Fri, 09 Feb 2018)
Provided are mixed carrier, multivalent pneumococcal conjugate compositions comprising 20 different pneumococcal capsular polysaccharide-protein conjugates, wherein each of the conjugates includes a capsular polysaccharide from a different serotype of Streptococcus pneumoniae conjugated to either tetanus toxoid or CRM197, wherein the Streptococcus pneumoniae serotypes are selected from 1, 3, 4, 5, 6A, 6B, 7F, 8, 9V, 10A, 11A, 12F, 14, 15B, 18C, 19A, 19F, 22F, 23F, and 33F, wherein two of the capsular polysaccharides are conjugated to tetanus toxoid and the remaining capsular polysaccharides are conjugated to CRMig7, and wherein the two capsular polysaccharides that are conjugated to tetanus toxoid are selected from the group consisting of serotypes 1, 3, and 5. Also provided are methods of producing the mixed carrier, multivalent pneumococcal conjugate compositions and methods of using the same for prophylaxis against Streptococcus pneumoniae infection or disease in a subject.
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MULTIVALENT PNEUMOCOCCAL POLYSACCHARIDE-PROTEIN CONJUGATE COMPOSITION (Fri, 09 Feb 2018)
Provided are mixed carrier, multivalent pneumococcal conjugate compositions comprising 16 different pneumococcal capsular polysaccharide-protein conjugates, wherein each of the conjugates includes a capsular polysaccharide from a different serotype of Streptococcus pneumoniae conjugated to either tetanus toxoid or CRM197, wherein the Streptococcus pneumoniae serotypes are selected from 1, 3, 4, 5, 6A, 6B, 7F, 9V, 12F, 14, 18C, 19A, 19F, 22F, 23F, and 33F, wherein two of the capsular polysaccharides are conjugated to tetanus toxoid and the remaining capsular polysaccharides are conjugated to CRM197, and wherein the two capsular polysaccharides that are conjugated to tetanus toxoid are selected from the group consisting of serotypes 1, 3, and 5. Also provided are methods of producing the mixed carrier, multivalent pneumococcal conjugate compositions and methods of using the same for prophylaxis against Streptococcus pneumoniae infection or disease in a subject.
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CONJUGATES OF A PHARMACEUTICAL AGENT AND A MOIETY CAPABLE OF BINDING TO A GLUCOSE SENSING PROTEIN (Fri, 08 Dec 2017)
The invention describes novel conjugates of formula (I) of a pharmaceutical agent and a moiety capable of binding to a glucose sensing protein allowing a reversible release of the pharmaceutical agent depending on the glucose concentration.
>> Read More

FUSED PENTACYCLIC IMIDAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY (Fri, 06 Oct 2017)
A series of substituted fused pentacyclic benzimidazole derivatives,and analogues thereof,being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
>> Read More

FUSED PENTACYCLIC IMIDAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY (Fri, 06 Oct 2017)
A series of substituted fused pentacyclic benzimidazole derivatives,and analogues thereof,being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
>> Read More