Produits et services

Pharmaceutical preparations and substances containing small molecule active pharmaceutical ingredients for the treatment of bacterial infections

Produits et services

Diagnostic preparations for clinical or medical laboratory use; Diagnostic reagents for clinical or medical laboratory use Pharmaceutical and veterinary preparations for the treatment or prevention of dermatological conditions, namely, eczema, inflammation, infection, warts, psoriasis, aging of the skin, ultra violet radiation and cancer; Pharmaceutical and veterinary preparations for the treatment of infections caused by bacteria, fungi, viruses and rheumatoid arthritis; Pharmaceutical and veterinary preparations for the treatment of diseases, disorders and conditions in the area of oncology

Produits et services

Diagnostic preparations for clinical or medical laboratory use; Diagnostic reagents for clinical or medical laboratory use Pharmaceutical and veterinary preparations for the treatment or prevention of dermatological conditions, namely, eczema, inflammation, infection, warts, psoriasis, aging of the skin, ultra violet radiation and cancer; Pharmaceutical and veterinary preparations for the treatment of infections caused by bacteria, fungi, viruses and rheumatoid arthritis; Pharmaceutical and veterinary preparations for the treatment of diseases, disorders and conditions in the area of oncology

Produits et services

Chemical substances for use in the manufacture of pharmaceutical preparations for the treatment of dermatological conditions and for the treatment of infections and diseases; chemical substances for use in research and development of pharmaceuticals for the treatment of dermatological conditions and for the treatment of infections and diseases; diagnostic preparations for scientific clinical use; diagnostic reagents for clinical or medical laboratory use Pharmaceutical and veterinary products and preparations for the treatment and prevention of dermatological conditions, namely, eczema, inflammation, infection, warts, psoriasis, aging of the skin, ultra violet radiation and cancer; Pharmaceutical and veterinary products and preparations for the treatment and prevention of infections caused by bacteria, fungi, viruses, and rheumatoid arthritis; Pharmaceutical and veterinary products and preparations for the treatment and prevention of diseases, disorders and conditions in the area of oncology; Pharmaceutical and veterinary products and preparations for the treatment and prevention of diseases, disorders and conditions in the area of gastroenterology; Pharmaceutical and veterinary products and preparations for the treatment and prevention of diseases, disorders and conditions in the area of neurology; Pharmaceutical and veterinary products and preparations for the treatment and prevention of diseases, disorders and conditions in the area of gynecology; Pharmaceutical and veterinary products and preparations for the treatment and prevention of diseases, disorders and conditions in the area of urology; Pharmaceutical and veterinary products and preparations for the treatment and prevention of diseases, disorders and conditions in the area of cardiology; Pharmaceutical and veterinary products and preparations for the treatment and prevention of diseases, disorders and conditions in the area of endocrinology; Pharmaceutical and veterinary products and preparations for the treatment and prevention of diseases, disorders and conditions in the area of nephrology; Pharmaceutical and veterinary products and preparations for the treatment and prevention of diseases, disorders and conditions in the area of hematology; Pharmaceutical and veterinary products and preparations for the treatment and prevention of diseases, disorders and conditions in the area of allergy; Pharmaceutical and veterinary products and preparations for the treatment and prevention of diseases, disorders and conditions in the area of immunology; Pharmaceutical and veterinary products and preparations for the treatment and prevention of diseases, disorders and conditions in the area of psychiatry; Pharmaceutical and veterinary products and preparations for the treatment and prevention of diseases, disorders and conditions in the area of anesthesiology; Pharmaceutical and veterinary products and preparations for the treatment and prevention of diseases, disorders and conditions in the area of rheumatology; all of the aforesaid for prescription only Research and development services for third parties in the field of chemical substances, pharmaceutical and veterinary products and preparations

Produits et services

Pharmaceutical preparations and substances for the treatment of infectious diseases, for the treatment of dermatological disorders, for the treatment of gastrointestinal diseases, for the treatment of neurological diseases, for the treatment of cardiovascular diseases, and for the treatment of gynecological diseases

Abrégé

The invention relates to a process for the manufacture of diastereomerically and enantiomerically enriched triazole compounds isavuconazole and ravuconazole, comprising a Reformatsky reaction between a ketone and a 2-halozincpropionate ester, followed by a resolution step, preferably an enzymatic resolution with an esterase enzyme.

Classes IPC  ?

• C07D 249/08 - Triazoles-1, 2, 4Triazoles-1, 2, 4 hydrogénés

Abrégé

5 together represent methylenedioxy; and pharmaceutically acceptable derivatives thereof. Methods of treatment of neoplastic and autoimmune diseases with these compounds we also disclosed.

Classes IPC  ?

• A61K 31/4245 - Oxadiazoles
• A61K 31/4439 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. oméprazole
• C12Q 1/48 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir une transférase
• G01N 33/574 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour le cancer
• C07D 413/04 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
• C07D 413/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles

Produits et services

(1) Pharmaceutical preparations for the prevention and/or treatment of: dermatological conditions, namely, skin pigmentation diseases, acne, infection, warts, psoriasis, aging of the skin, ultra violet radiation, cancer, and infectious diseases and disorders caused by bacteria, fungi and viruses, namely, skin infections, skin structure infections, diabetic foot infections, eye infections, respiratory tract infections, soft tissue infections, urinary tract infections, biliary infections, intra-abdominal infections, genital infections, bone infections, joint infections, nail infections, osteomyelitis, septicemia, pneumonia, bacterial endocarditis, meningitis, otitis media; pharmaceutical preparations for the prevention and treatment of rheumatoid arthritis; pharmaceutical preparations for the prevention and treatment of cancer; pharmaceutical preparations for use in oncology; antibiotic preparations; anti-inflammatory preparations; anti-fungal pharmaceutical preparations; Chemical, biological and diagnostic reagents for medical laboratory use and clinical laboratory use (1) Manufacturing of chemicals, pharmaceutical preparations, and veterinary products to the order and specification of others (2) The provision of research and development services to others in the area of chemicals, pharmaceutical and veterinary products and preparations (3) Operation of a pharmaceutical company

Produits et services

(1) Pharmaceutical preparations for the prevention and/or treatment of: dermatological conditions, namely, skin pigmentation diseases, acne, infection, warts, psoriasis, aging of the skin, ultra violet radiation, cancer, and infectious diseases and disorders caused by bacteria, fungi and viruses, namely, skin infections, skin structure infections, diabetic foot infections, eye infections, respiratory tract infections, soft tissue infections, urinary tract infections, biliary infections, intra-abdominal infections, genital infections, bone infections, joint infections, nail infections, osteomyelitis, septicemia, pneumonia, bacterial endocarditis, meningitis, otitis media; pharmaceutical preparations for the prevention and treatment of rheumatoid arthritis; pharmaceutical preparations for the prevention and treatment of cancer; pharmaceutical preparations for use in oncology; antibiotic preparations; anti-inflammatory preparations; anti-fungal pharmaceutical preparations; Chemical, biological and diagnostic reagents for medical laboratory use, clinical laboratory use and medical research use (1) Manufacturing of chemicals, pharmaceutical preparations, and veterinary products to the order and specification of others (2) The provision of research and development services to others in the area of chemicals, pharmaceutical and veterinary products and preparations (3) Operation of a pharmaceutical company

Abrégé

Use of BUBR1 as a biomarker for predicting the response to a compound, preferably resistance of a disease such as cancer in a subject, wherein the compound is a compound of general formula I and pharmaceutically acceptable derivatives thereof. Methods of treatment of neoplastic and autoimmune diseases with these compounds are also disclosed.

Classes IPC  ?

• G01N 33/574 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour le cancer
• A61K 31/4245 - Oxadiazoles
• G01N 33/50 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique
• A61K 31/4439 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. oméprazole
• C12Q 1/68 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques

Produits et services

Pharmaceutical products and preparations, namely, for the treatment and prevention of infections caused by bacteria

Abrégé

Disclosed is a novel principle for dosing a specific anti-cancer drug compound of formula (I), a prodrug thereof or a pharmaceutically acceptable salt of said drug compound or prodrug thereof as described, wherein said drug compound, prodrug thereof or pharmaceutically acceptable salt of said drug compound or prodrug thereof is intravenously administered to a cancer patient according to a specific dosage frequency and a specific treatment cycle at a dose being below the maximum tolerated dose (MTD) defined for said dosage frequency and treatment cycle of said drug, prodrug thereof or pharmaceutically acceptable salt of said drug compound or prodrug thereof but providing at least the same exposure of the tissue of the cancer from which said cancer patient is suffering, to said drug as provided by the MTD at the same dosage frequency and treatment cycle.

Classes IPC  ?

• A61K 31/4439 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. oméprazole

Abrégé

The invention relates to a process for the manufacture of diastereomerically and enantiomerically enriched triazole compounds isavuconazole and ravuconazole, comprising a Reformatsky reaction between a ketone and a 2-halozincpropionate ester, followed by a resolution step, preferably an enzymatic resolution with an esterase enzyme.

Classes IPC  ?

• C07D 249/08 - Triazoles-1, 2, 4Triazoles-1, 2, 4 hydrogénés

Abrégé

The antibacterial compound of formula I X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.

Classes IPC  ?

• C07D 513/04 - Systèmes condensés en ortho
• C07D 417/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
• C07D 498/04 - Systèmes condensés en ortho
• C07D 413/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
• C07D 413/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
• C07D 405/14 - Composés hétérocycliques contenant à la fois un ou plusieurs hétérocycles comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle et un ou plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
• C07D 409/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
• C07D 495/04 - Systèmes condensés en ortho
• C07D 215/20 - Atomes d'oxygène
• C07D 405/12 - Composés hétérocycliques contenant à la fois un ou plusieurs hétérocycles comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle et un ou plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
• C07D 409/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
• C07D 417/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
• C07D 471/04 - Systèmes condensés en ortho
• C07D 519/00 - Composés hétérocycliques contenant plusieurs systèmes de plusieurs hétérocycles déterminants condensés entre eux ou condensés avec un système carbocyclique commun non prévus dans les groupes ou
• C07D 401/12 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons

Abrégé

The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.

Classes IPC  ?

• C07D 513/04 - Systèmes condensés en ortho
• C07D 491/04 - Systèmes condensés en ortho
• C07D 495/04 - Systèmes condensés en ortho
• C07D 491/052 - Systèmes condensés en ortho avec un seul atome d'oxygène comme hétéro-atome du cycle contenant de l'oxygène le cycle contenant de l'oxygène étant à six chaînons
• C07D 491/147 - Systèmes condensés en ortho le système condensé contenant un cycle avec l'oxygène comme hétéro-atome du cycle et deux cycles avec l'azote comme hétéro-atome du cycle
• C07D 498/04 - Systèmes condensés en ortho
• C07D 498/14 - Systèmes condensés en ortho

Abrégé

A solid DMSO solvate of a compound of formula (I) is described, which is a useful intermediate for preparing the broad spectrum antibiotics Ceftobiprole and Ceftobiprole Medocaril.

Classes IPC  ?

• C07D 501/12 - SéparationPurification
• C07D 501/54 - Radicaux méthylène, substitués par des hétérocycles avec le radical amino-7 acylé par un acide carboxylique araliphatique, lequel est substitué sur le radical aliphatique par des hétéro-atomes

Abrégé

The application relates to the macrolide compound of the formula (I): wherein * indicates a stereocentre which is in (R) or (S) configuration, or a pharmaceutically acceptable salt or ester thereof and their use as PDE4 inhibitors.

Classes IPC  ?

• C07H 17/08 - Hétérocycles d'au moins huit chaînons, p. ex. érythromycines
• A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p. ex. leucoglucosane, hespéridine, érythromycine, nystatine
• A61P 11/06 - Antiasthmatiques

Abrégé

Use of BUBR1 as a biomarker for predicting the response to a compound, preferably resistance of a disease such as cancer in a subject, wherein the compound is a furazanobenzimidazole compound of general formula (I).

Classes IPC  ?

• G01N 33/50 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique
• C12Q 1/6886 - Produits d’acides nucléiques utilisés dans l’analyse d’acides nucléiques, p. ex. amorces ou sondes pour les maladies provoquées par des altérations du matériel génétique pour le cancer
• G01N 33/574 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour le cancer
• A61K 31/4245 - Oxadiazoles
• A61K 31/4439 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. oméprazole
• A61K 31/44 - Pyridines non condenséesLeurs dérivés hydrogénés
• A61K 31/41 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec plusieurs hétéro-atomes cycliques, l'un au moins étant l'azote, p. ex. tétrazole
• C12Q 1/68 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir des acides nucléiques
• G01N 33/00 - Recherche ou analyse des matériaux par des méthodes spécifiques non couvertes par les groupes

Abrégé

The invention relates to a process for the manufacture of diastereomerically and enantiomerically enriched triazole compounds isavuconazole and ravuconazole, comprising a Reformatsky reaction between a ketone and a 2-halozincpropionate ester, followed by a resolution step, preferably an enzymatic resolution with an esterase enzyme.

Classes IPC  ?

• C07D 249/08 - Triazoles-1, 2, 4Triazoles-1, 2, 4 hydrogénés

Abrégé

Use of glu-tubulin as a biomarker for predicting the response to a compound, preferably resistance of a disease such as cancer in a subject to said compound, wherein the compound is a furazanobenzimidazole compound of general formula (I).

Classes IPC  ?

• G01N 33/68 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique faisant intervenir des protéines, peptides ou amino-acides
• A61K 31/4245 - Oxadiazoles
• G01N 33/50 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique

Abrégé

The invention relates to novel Rauwolfia alkaloid derivatives of formula (I) combinations of Rauwolfia alkaloid derivatives and a mitochondrial inhibitor, e.g. metformin, and the use of Rauwolfia alkaloid derivatives in combination with mitochondrial inhibitor for the treatment of cancer and for achieving clinical immunosuppression. The invention also relates to a fluorescence-based method for predicting the sensitivity of a cancer cell towards a compound of formula (I).

Classes IPC  ?

• C07D 459/00 - Composés hétérocycliques contenant des systèmes cycliques benz [g] indolo [2, 3-a] quinolizine, p. ex. yohimbineLeurs lactones en 16, 18, p. ex. lactone de l'acide réserpique
• A61K 31/475 - QuinoléinesIsoquinoléines ayant un cycle indole, p. ex. yohimbine, réserpine, strychnine, vinblastine
• A61P 35/00 - Agents anticancéreux
• A61P 37/06 - Immunosuppresseurs, p. ex. médicaments pour le traitement du rejet de greffe

Produits et services

(1) Chemical preparations for use in the pharmaceutical industry as well as chemical preparations for research and development of pharmaceutical preparations; pharmaceutical preparations for the prevention and / or treatment of: dermatological conditions, namely, dermatitis, skin pigmentation diseases, acne, eczema, inflammation, infection, warts, psoriasis, aging of the skin, ultra violet radiation and cancer; infectious diseases and disorders, namely, rheumatoid arthritis and infectious diseases and disorders caused by bacteria, fungi, and viruses; diseases, disorders and conditions in the area of oncology; antibiotic preparations; anti-inflammatory preparations; anti-fungal pharmaceutical preparations; anti-microbial pharmaceutical preparations. (1) The provision of scientific and technological research services and scientific and technological development services to others in the area of chemicals, pharmaceutical and veterinary products and preparations.

Abrégé

Use of acetylated tubulin as a biomarker for predicting the response to a compound, preferably resistance of a disease such as cancer in a subject to said compound, wherein the compound is a furazanobenzimidazoles compound of general formula (I).

Classes IPC  ?

• A61K 31/415 - 1,2-Diazoles
• A61K 31/41 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec plusieurs hétéro-atomes cycliques, l'un au moins étant l'azote, p. ex. tétrazole
• G01N 33/68 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique faisant intervenir des protéines, peptides ou amino-acides
• A61K 31/4245 - Oxadiazoles
• G01N 33/50 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique
• A61K 31/4184 - 1,3-Diazoles condensés avec des carbocycles, p. ex. benzimidazoles
• A61K 31/42 - Oxazoles
• A61K 38/00 - Préparations médicinales contenant des peptides

Produits et services

Pharmaceutical preparations and substances.

Abrégé

Compounds of formula (I), wherein A1 represents -0-, -S- or -CH2-; A2 represents -CH2- or -0-; A3 represents C3-C8cycloalkylene; saturated or unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen or oxygen, which group A3 is unsubstituted or substituted; A4 represents C1-C4alkylene, -C(=0)-; G represents aryl or heteroaryl, which is unsubstituted or substituted; X1 represents a nitrogen atom or CR1; R1 represents a hydrogen atom or a halogen atom; R2 represents a hydrogen atom; m is 0 or 1; n is 1; the -(CH2)n- group is unsubstituted or substituted; p is 0 or 1; or pharmaceutically acceptable salts thereof are valuable for use as a medicament for the treatment of bacterial infections.

Classes IPC  ?

• C07D 491/14 - Systèmes condensés en ortho
• C07D 491/147 - Systèmes condensés en ortho le système condensé contenant un cycle avec l'oxygène comme hétéro-atome du cycle et deux cycles avec l'azote comme hétéro-atome du cycle

Abrégé

A compound of formula II 2 is a group selected from (b), (c), and (d):

Classes IPC  ?

• A61K 31/44 - Pyridines non condenséesLeurs dérivés hydrogénés
• C07D 413/04 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique

Abrégé

Use of phospho-Akt as a biomarker for predicting the response, such as resistance, to a compound, wherein phospho-Akt is Akt that has been phosphorylated on one or more residues, with the proviso that for Akt1, Akt2, and Akt3 the designation phospho-Akt is used to indicate phosphorylation at a site other than T308, T309 or T305 respectively, wherein the compound is a compound of general formula (I) wherein R represents phenyl, thienyl or pyridinyl wherein phenyl is optionally substituted by one or two substituents independently selected from alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, monoalkylamino, dialkylamino, lower alkoxycarbonylamino, lower alkylcarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower alkoxycarbonyl, cyano, halogen, and nitro; and wherein two adjacent substituents are methylenedioxy; and wherein pyridinyl is optionally substituted by lower alkoxy, amino or halogen; X represents a group C=Y, wherein Y stands for oxygen or nitrogen substituted by hydroxy or lower alkoxy; R1 represents hydrogen, lower alkylcarbonyl, hydroxy-lower alkyl or cyano-lower alkyl; R2, R3 and R6 represent hydrogen; R4 and R5, independently of each other, represent hydrogen, lower alkyi or lower alkoxy; or R4 and R5 together represent methylenedioxy; and pharmaceutically acceptable derivatives thereof; or wherein R represents phenyl or pyridinyl wherein phenyl is optionally substituted by one or two substituents independently selected from alkyi, halo-lower alkyi, hydroxy-lower alkyi, lower alkoxy-lower alkyi, acyloxy-lower alkyi, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, monoalkylamino, dialkylamino, lower alkoxycarbonylamino, lower alkylcarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower alkoxycarbonyl, formyl, cyano, halogen, and nitro; and wherein two adjacent substituents are methylenedioxy; and wherein pyridinyl is optionally substituted by lower alkoxy, amino or halogen; X represents oxygen; R1 represents hydrogen, lower alkylcarbonyl, hydroxy-lower alkyi or cyano-lower alkyi; R2, R3 and R6 represent hydrogen; R4 and R5, independently of each other, represent hydrogen, lower alkyi or lower alkoxy; or R4 and R5 together represent methylenedioxy; and pharmaceutically acceptable derivatives thereof. Methods of treatment of neoplastic and autoimmune diseases with these compounds are also disclosed.

Classes IPC  ?

• C12Q 1/48 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir une transférase
• G01N 33/68 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique faisant intervenir des protéines, peptides ou amino-acides
• G01N 33/574 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour le cancer

Abrégé

Use of acetylated tubulin as a biomarker for predicting the response to a compound, preferably resistance of a disease such as cancer in a subject to said compound, wherein the compound is a furazanobenzimidazoles compound of general formula (I).

Classes IPC  ?

• G01N 33/50 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique
• A61K 31/00 - Préparations médicinales contenant des ingrédients actifs organiques
• A61K 38/00 - Préparations médicinales contenant des peptides

Abrégé

Use of stathmin as a biomarker for predicting the response, such as resistance, to a compound, wherein the compound is a furazanobenzimidazole compound of general formula (I).

Classes IPC  ?

• G01N 33/50 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique
• A61K 31/00 - Préparations médicinales contenant des ingrédients actifs organiques

Abrégé

Use of glu-tubulin as a biomarker for predicting the response to a compound, preferably resistance of a disease such as cancer in a subject to said compound, wherein the compound is a furazanobenzimidazole compound of general formula (I).

Classes IPC  ?

• G01N 33/50 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique
• A61K 31/00 - Préparations médicinales contenant des ingrédients actifs organiques
• A61K 38/00 - Préparations médicinales contenant des peptides

Abrégé

Use of BUBR1 as a biomarker for predicting the response to a compound, preferably resistance of a disease such as cancer in a subject, wherein the compound is a furazanobenzimidazole compound of general formula (I).

Classes IPC  ?

• G01N 33/50 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique
• A61K 31/00 - Préparations médicinales contenant des ingrédients actifs organiques

Abrégé

3 are independently of one another hydrogen, F or Cl; or a pharmaceutically acceptable acid addition salt thereof, and (b) a carrier comprising a solubilizer component for the antifungally effective component (a).

Classes IPC  ?

• A01N 43/78 - Thiazoles-1,3Thiazoles-1,3 hydrogénés
• A01N 55/02 - Biocides, produits repoussant ou attirant les animaux nuisibles ou régulateurs de croissance des végétaux, contenant des composés organiques comportant des éléments autres que le carbone, l'hydrogène, les halogènes, l'oxygène, l'azote et le soufre contenant des atomes de métal
• A01N 43/64 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec trois atomes d'azote comme uniques hétéro-atomes du cycle
• A61K 31/41 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec plusieurs hétéro-atomes cycliques, l'un au moins étant l'azote, p. ex. tétrazole
• A61K 31/555 - Composés hétérocycliques contenant des métaux lourds, p. ex. hémine, hématine, mélarsoprol

Produits et services

Pharmaceutical preparations and substances, namely antifungals.

Abrégé

Compound of formula (I): wherein A1 represents -O-, -S- or -N-R3; A2 represents -CH2-, -O-, -N-R4, -C(=O)- or -CH(O-R4)-; A3 represents C3-C8cycloalkylene; saturated and unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, which group A3 is unsubstituted or substituted; A4 represents C1-C4alkylene, C2-C4alkenylene, >C=O or a group selected from - C2H4NH-, -C2H4O-, and -C2H4S- being linked to the adjacent NR5-group via the carbon atom; and G represents aryl or heteroaryl, which is unsubstituted or substituted and R1 and R2 independently of one another, represent hydrogen or a substituent selected from hydroxy, halogen, mercapto, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylcarbonyloxy, C1-C6alkylsulfonyloxy, C1-C6heteroalkylcarbonyloxy, C5-C6heterocyclylcarbonyloxy, C1-C6heteroalkoxy, wherein heteroalkyl, heteroalkoxy groups or heterocyclyl comprise 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, in which substituents the alkyl moieties are unsubstituted or further substituted; R3, R4 and R5 independently of one another, represent hydrogen or C1-C6alkyl; X1 and X2 independently of one another, represent a nitrogen atom or CR2, with the proviso that at least one of Xl and X2 represents a nitrogen atom; m is 1; and the (CH2)m moiety is optionally substituted by C1-C4alkyl; halogen, carboxy, hydroxy, C1-C4alkoxy, C1-C4-alkylcarbonyloxy, amino, mono- or di-(C1-C4alkyl)amino or acylamino n is 0, 1 or 2 or pharmaceutically acceptable salt thereof are valuable for use as a medicament for the treatment of bacterial infections.

Classes IPC  ?

• C07D 491/04 - Systèmes condensés en ortho
• C07D 495/04 - Systèmes condensés en ortho
• A61K 31/4741 - QuinoléinesIsoquinoléines condensées en ortho ou en péri avec des systèmes hétérocycliques condensées avec des systèmes cycliques ayant l'oxygène comme hétéro-atome d'un cycle, p. ex. dérivés du tubocurarane, noscapine, bicuculline
• A61K 31/4743 - QuinoléinesIsoquinoléines condensées en ortho ou en péri avec des systèmes hétérocycliques condensées avec des systèmes cycliques ayant le soufre comme hétéro-atome d'un cycle
• A61P 31/04 - Agents antibactériens

Abrégé

A solid DMSO solvate of a compound of formula (I) is described, which is a useful intermediate for preparing the broad spectrum antibiotics Ceftobiprole and Ceftobiprole Medocaril.

Classes IPC  ?

• A61K 31/545 - Composés contenant des systèmes cycliques thia-5 aza-1 bicyclo [4.2.0] octane, c.-à-d. composés contenant un système cyclique de formule , p. ex. céphalosporines, céfaclor, céphalexine
• C07D 501/04 - Préparation à partir de composés contenant déjà les systèmes cycliques ou cycliques condensés, p. ex. par déshydrogénation du cycle, par introduction, élimination ou modification de substituants
• C07D 501/54 - Radicaux méthylène, substitués par des hétérocycles avec le radical amino-7 acylé par un acide carboxylique araliphatique, lequel est substitué sur le radical aliphatique par des hétéro-atomes
• C07D 501/12 - SéparationPurification

Abrégé

The invention relates to macrolide compounds of formula (I), the use of said compounds as medicaments, in particular for the treatment or prevention of inflammatory and allergic diseases, pharmaceutical compositions containing said compounds and to processes for their preparation. The invention relates in particular to macrolide compounds with antiinflammatory activity mediated primarily through inhibition of phosphodiesterase 4 (PDE4) which makes them useful for the treatment and/or prevention of inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, atopic dermatitis or inflammatory bowel disease or proliferative diseases such as cancer.

Classes IPC  ?

• C07D 498/04 - Systèmes condensés en ortho
• A61K 31/4433 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un cycle à six chaînons avec l'oxygène comme hétéro-atome du cycle
• A61P 11/06 - Antiasthmatiques
• A61P 35/00 - Agents anticancéreux
• A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
• C07H 17/08 - Hétérocycles d'au moins huit chaînons, p. ex. érythromycines

Abrégé

A compound of formula (II) wherein (a) represents a divalent benzene residue which is unsubstituted or substituted by one or two additional substituents independently selected from lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, mono(lower alkyl)amino, di(lower alkyl)amino, mono(lower alkenyl)amino, di(lower alkenyl)amino, lower alkoxycarbonylamino, lower alkylcarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower 15 alkoxycarbonyl, cyano, halogen, and nitro; or wherein two adjacent substituents can be methylenedioxy; or a divalent pyridine residue (Z = N) which is unsubstituted or substituted additionally by lower alkyl, lower alkoxy, lower alkoxy-lower alkoxy,amino, optionally substituted by one or two substituents selected from lower alkyl, lower alkenyl and alkylcarbonyl, halo-20 lower alkyl, lower alkoxy-lower alkyl, or halogen; R1 represents hydrogen, lower alkylcarbonyl, hydroxy-lower alkylor cyano-loweralkyl; and R2 represents a group selected from: (b), (c) and (d); or pharmaceutically acceptable salts thereof.

Classes IPC  ?

• C07D 413/04 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
• A61K 31/4245 - Oxadiazoles
• A61P 35/00 - Agents anticancéreux

Abrégé

Compounds of formula (I) wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C-H, C-(C1-C6alkyl), C-(C1-C6alkoxy), C-halogen, C-COOH; X5 represents C-H or C-(C1-C6alkyl), C-halogen; R1 and R2, independently of one another, represent hydrogen or a substituent selected from hydroxy, halogen, carboxy, amino, C1-C6alkylamino, di(C1-C6alkyl)amino, mercapto, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylamino- carbonyloxy, C2-C6alkenyl, C2-C6alkynyl, C1-C6alkylcarbonyloxy, C1-C6alkyl- sulfonyloxy, C1 -C6heteroalkylcarbonyloxy, C5-C6heterocyclylcarbonyloxy, C1-C6heteroalkyl, C1-C6heteroalkoxy, wherein heteroalkyl, heteroalkoxy groups or heterocyclyl comprise 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, in which substituents the alkyl moieties are unsubstituted or further substituted by halogeno, cyano, hydroxy, C1-C4alkoxy, C1-C4alkylcarbonyl, C1-C4alkoxycarbonyl, unsubstituted or substituted phenoxy or phenylcarbonyl, unsubstituted or substituted C5-C6heterocyclyl or carboxy; A1 represents a divalent group of one of the formulae -O-(CH2)m-(CH2)-, -S-(CH2)m-(CH2)- or -(C=O)O-(CH2)m-(CH2)-, wherein the (CH2)m moiety is optionally substituted by C1-C4alkyl, C2-C4alkenyl, C3-C6cycloalkyl, C3-C6cycloalkylmethyl, morpholinomethyl, halogen, carboxy, hydroxy, C1-C4alkoxy; C1 -C4alkoxyC1 -C4alkyl, C1 -C4alkoxy(C1 -C4alkylenoxy)C1 -C4alkyl, benzyloxyC1 - C4alkyl, amino, mono- or di-(C1-C4alkyl)amino or acylamino, in which substituents the alkyl moieties can be further substituted by 1 or more fluoro atoms m is 0, 1 or 2, provided that the number of atoms in the direct chain between the two terminal valencies of A1 is at least 3, which group A1 is linked to A2 via the terminal (CH2)-moiety; A2 is a group selected from C3-C8cycloalkylene; saturated and unsaturated 4 to 8- membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, which group A2 is unsubstituted or substituted; R4 represents hydrogen or C1 -C4alkyl; A3 represents C1-C4alkylene, C2-C4alkenylene, >C=O, -C(O)C1-C3alkylene-, -C(=O)NH-, or a group selected from -C2H4NH-, -C2H4O-, and -C2H4S- being linked to the adjacent NR4-group via the carbon atom; and G represents aryl or heteroaryl, which is unsubstituted or substituted and n is 0, 1 or 2; or a pharmaceutically acceptable salts, hydrates or solvates thereof are valuable antibacterial agents.

Classes IPC  ?

• C07D 405/12 - Composés hétérocycliques contenant à la fois un ou plusieurs hétérocycles comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle et un ou plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
• C07D 409/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
• C07D 409/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
• C07D 413/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
• C07D 413/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
• C07D 417/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
• A61K 31/4375 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à six chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. quinolizines, naphtyridines, berbérine, vincamine
• A61K 31/47 - QuinoléinesIsoquinoléines
• A61P 33/00 - Agents antiparasitaires

Abrégé

A compound of formula (I) in a crystalline form, which has a X-ray diffraction pattern comprising, when measured using Cu- Kα1 radiation, a diffraction line, having a relative intensity (rl) of 100 percent at about 11.6, 12.9, 14.7, 22.0, 23.1 or 24.5, given in degrees 2 Theta [2θ]. Five corresponding polymorphic crystal forms (Polymorph A; B; C; D or E) have been characterized by means of their XRPD and have been isolated.

Classes IPC  ?

• C07D 501/00 - Composés hétérocycliques contenant des systèmes cycliques thia-5 aza-1 bicyclo [4.2.0] octane, c.-à-d. des composés contenant un système cyclique de formule , p. ex. céphalosporinesCes systèmes cycliques étant ultérieurement condensés, p. ex. condensés en positions 2, 3 avec des hétérocycles contenant de l'oxygène, de l'azote ou du soufre
• A61K 31/549 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec au moins un azote et au moins un soufre comme hétéro-atomes d'un cycle, p. ex. sulthiame ayant plusieurs atomes d'azote dans le même cycle, p. ex. hydrochlorothiazide
• A61P 31/04 - Agents antibactériens

Abrégé

Disclosed is a process for the manufacture of a compound of formula (I) 2 represent, independently from one another, hydrogen or Hal; in which process a compound of formula (II) is converted to a corresponding alkyl, fluoroalkyl or aryl sulfonic acid ester, which is then reacted with an alkali metal nitrite in the presence of a suitable crown ether in a polar non-nucleophilic solvent at a temperature of −10 to 50° C. to give the compound of formula (I).

Classes IPC  ?

• C07D 301/32 - SéparationPurification
• C07D 303/14 - Composés contenant des cycles oxirane avec des radicaux hydrocarbonés, substitués par des atomes d'oxygène liés par des liaisons simples ou doubles par des radicaux hydroxyle libres
• C07D 249/08 - Triazoles-1, 2, 4Triazoles-1, 2, 4 hydrogénés
• C07D 277/24 - Radicaux substitués par des atomes d'oxygène

Abrégé

A solid DMSO solvate of a compound of formula (I) is described, which is a useful intermediate for preparing the broad spectrum antibiotics Ceftobiprole and Ceftobiprole Medocaril.

Classes IPC  ?

• C07D 501/12 - SéparationPurification
• C07D 501/54 - Radicaux méthylène, substitués par des hétérocycles avec le radical amino-7 acylé par un acide carboxylique araliphatique, lequel est substitué sur le radical aliphatique par des hétéro-atomes
• A61P 31/00 - Agents anti-infectieux, c.-à-d. antibiotiques, antiseptiques, chimiothérapeutiques
• A61K 31/546 - Composés contenant des systèmes cycliques thia-5 aza-1 bicyclo [4.2.0] octane, c.-à-d. composés contenant un système cyclique de formule , p. ex. céphalosporines, céfaclor, céphalexine contenant d'autres hétérocycles, p. ex. céphalotine

Abrégé

The invention relates to macrolide compounds of formula (I),the use of said compounds as medicaments, in particular for the treatment or prevention of inflammatory and allergic diseases, pharmaceutical compositions containing said compounds and to processes for their preparation. The invention relates in particular to macrolide compounds with anti-inflammatory activity mediated primarily through inhibition of phosphodiesterase 4 (PDE4) which makes them useful for the treatment and/or prevention of inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, atopic dermatitis or inflammatory bowel disease or proliferative diseases such as cancer.

Classes IPC  ?

• C07H 17/08 - Hétérocycles d'au moins huit chaînons, p. ex. érythromycines
• A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p. ex. leucoglucosane, hespéridine, érythromycine, nystatine
• A61P 11/06 - Antiasthmatiques
• A61P 17/06 - Antipsoriasiques
• A61P 25/02 - Médicaments pour le traitement des troubles du système nerveux des neuropathies périphériques

Abrégé

Macrolides of Formula (I) or (I-A): and wherein the residues R1, R2, R3, R4, R12, R13 and R14 have certain meanings defined in this application are useful for treating or preventing inflammatory or allergic diseases or. cancer in animals and humans.

Classes IPC  ?

• A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p. ex. leucoglucosane, hespéridine, érythromycine, nystatine
• A61P 31/04 - Agents antibactériens
• A61P 11/06 - Antiasthmatiques
• A61P 17/06 - Antipsoriasiques
• A61P 25/02 - Médicaments pour le traitement des troubles du système nerveux des neuropathies périphériques
• A61P 37/08 - Agents antiallergiques

Abrégé

A process for the production of a compound of formula (I) wherein ALINKERB represents a linker moiety of formula (V): A[G1 - G2*- G3]B; wherein A and B indicate the orientation of the group of formula (V) in formula (I); G1, G2 and G3 have specific meanings described herein and may be present or absent, with the proviso that at least one of G1 or G3 is present; which linker group may furthermore optionally contain one or more groups of formula (VI); and/or other substituents; and R1 represents hydrogen or a C1-C4-alkyl group; R2 represents hydrogen or a C1-C4-alkyl group; R3 independently at each occurrence, represents hydrogen or a C1-C4-alkyl group; x is 0 or 1; y is 0 or 1; z independently at each occurrence, is 0 or 1; and (- -) represents a single bond between a primary, secondary or tertiary carbon atom of the moiety ALINKERB and the adjacent nitrogen atom; in which process (A) a compound of formula (II) is reacted with a compound of formula (III) wherein Pr represents an amino protecting group selected from t-butyloxy carbonyl (t-Boc), 1-methyl-1-(4-biphenylyl)ethyloxy carbonyl (Bpoc), 1-(1-adamantyl)-1-methylethyloxy carbonyl (Adpoc), 1-(3,5-di-t-butylphenyl)-1-methylethyloxy carbonyl (t-Bumeoc), 1-adamantyloxy carbonyl (Adoc), p-methoxybenzyloxy carbonyl (Moz), o,p-dimethoxybenzyloxy carbonyl, ALINKERB has the same meaning as in formula (I) with the exception that one or more of the optional groups of formula (VII) may be replaced by a group of formula (VII) and R1; R2; R3; x; y; z and (--), at each occurrence, have the same meaning as in formula (I) and Pr is as defined above; in a dipolar aprotic solvent in the presence of a base to obtain a compound of formula (IV) wherein Pr; ALINKERB; R1; R2; R3; x; y; z; and (- -), at each occurrence, have the same meaning as in formula (III); which compound is then (B) deprotected by reaction with formic acid or a mixture of formic acid or acetic acid with hydrochloric acid or hydrobromic acid, to give the compound of formula (I) as well as the compounds of the aforementioned formula (IV).

Classes IPC  ?

• C07D 487/04 - Systèmes condensés en ortho

Abrégé

A process for manufacturing a compound of Formula (I) which has cis-conformation and wherein R1 represents a 1-phenyl-C1-C4alkyl or 1-naphthyl-C1-C4alkyl group, wherein the phenyl or naphthyl moiety of R1 is unsubstituted or substituted with one or more C1-C4alkoxy groups and the carbon atoms in 2-, 3-, and/or 4-position of the alkyl part of R1 are, independently of the phenyl or naphthyl moiety of R1 and independently of one another, unsubstituted or substituted with C1-C4alkoxy and/or silyloxy or, preferably, are unsubstituted or substituted with one C1-C4alkoxy group and/or silyloxy group per carbon atom, and R2 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, in which process a compound of Formula (II) wherein R3 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, and R1 and R2 have the same meaning as in formula (I); is treated with a base at a temperature of 0°C or less in a liquid aprotic solvent for a time period sufficient to obtain the compound of formula (I).

Classes IPC  ?

• C07D 487/04 - Systèmes condensés en ortho
• C07C 237/20 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant les atomes de carbone des groupes carboxamide liés à des atomes de carbone acycliques du squelette carboné le squelette carboné contenant des cycles aromatiques à six chaînons

Abrégé

A pharmaceutical composition for oral administration which is self-emulsifying on contact with an aqueous phase, in particular gastrointestinal fluids, and which comprises: (a)an antifungally active compound of formula (I) wherein R1, R2 and R3 are independently of one another hydrogen, F or Cl; or a pharmaceutically acceptable acid addition salt thereof, and (b)a carrier comprising a solubilizer component for the antifungally effective component (a).

Classes IPC  ?

• A61K 9/107 - Émulsions
• A61K 31/427 - Thiazoles non condensés et contenant d'autres hétérocycles
• A61K 47/14 - Esters d’acides carboxyliques, p. ex. acides gras monoglycérides, triglycérides à chaine moyenne, parabènes ou esters d’acide gras de PEG

Abrégé

Use of a monobactam antibiotic of formula (I) wherein the oxyimino group i.e. ᡶC=N-O- has Z-orientation, or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of a bacterial infection in combination with a carbapenem antibiotic or a pharmaceutically acceptable salt thereof.

Classes IPC  ?

• A61K 31/427 - Thiazoles non condensés et contenant d'autres hétérocycles
• A61K 31/4436 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle
• A61P 31/04 - Agents antibactériens

Produits et services

Chemical preparations (for use in the pharmaceutical industry as well as chemical preparations for research and development of pharmaceutical preparations). Pharmaceutical preparations. Scientific and technological research services and scientific and technological development services.

Produits et services

Chemicals used in industry; chemicals used in science (except for medical or veterinary use). Pharmaceutical preparations; chemical preparations for pharmaceutical use; chemical-pharmaceutical preparations; chemical preparations for the investigation and the development of pharmaceutical preparations. Scientific and technical research services as well as scientific and technical development services.

Abrégé

Macrolide compounds of formula I: with PDF4 inhibiting activity are described, wherein R1 is a residue -Y-X-Q; Y is S, SO or SO2; X is a bond or a linear group consisting of hydrogen atoms and with up to 9 atoms selected from C, N, O and/or S, of which up to 2 atoms can be N and one atom can be O or S, one carbon atom can appear as a CO group and the sulphur atom can appear as an SO2 group and two adjacent C atoms can be present as - CH=CH- or -C≡C- and which group X is unsubstituted or is substituted with - COO-W or -CONH-W; Q is a residue -V-A1-L- A2-W or, if X does not represent a bond, may also be -NR6R7; V is a divalent aromatic or heterocyclic group; W is aryl or heterocyclyl; or in a group -V-A1-L- A2-W, wherein at least one of the groups A1; L or A2 is present, can also be a monovalent substituted or unsubstituted, saturated or unsaturated linear group with up to 5 atoms consisting of C, N, O and/or S of which one carbon can appear as a CO group one sulphur atom can appear as an SO2 group, A1, A2 are independently of each other either absent or a C1-C4alkylene group; L is -0-, -S-, -SO2-, -NH-, -CO-, -(CO)O-, -O(OC)-, -(CO)NH-, -NH(CO)-, -(SO2)NH-, -HN(SO2)-, -HN(CO)NH-, -0(CO)NH-, -NH(CO)O-, or can also be absent if Al and/or A2 are present; R2 is hydrogen and R3 is and 0R4 or R2, R3 taken together form a C=O group; R4 is hydrogen or an saturated or unsaturated aliphatic group with 1 to 6 carbon atoms; R6, R7 are independently selected from aryl; aralkyl; heterocyclyl and heterocyclylalkyl; and one of R6 and R7 can also be a group -L-W; and * indicates a chiral centre which is in the (R) or (S) form.

Classes IPC  ?

• C07H 17/08 - Hétérocycles d'au moins huit chaînons, p. ex. érythromycines
• A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p. ex. leucoglucosane, hespéridine, érythromycine, nystatine

Produits et services

(1) Pharmaceutical preparations for the prevention and/or treatment of: dermatological conditions, namely, dermatitis, eczema and inflammation.

Produits et services

(1) Pharmaceutical preparations for the prevention and/or treatment of: dermatological conditions, namely, dermatitis, eczema and inflammation.

Produits et services

Chemical substances for use in the pharmaceutical industry and in research and development of pharmaceuticals. Prescription only pharmaceutical and veterinary preparations; sanitary preparations for medical purposes; dietetic substances adapted for medical use, food for babies; plasters, materials for dressings; material for stopping teeth, dental wax; disinfectants; preparations for destroying vermin; fungicides, herbicides. Research and development services for third in the field of chemical substances, pharmaceutical and veterinary products and preparations.

Produits et services

Pharmaceutical products and substances.

Produits et services

Pharmaceutical products and substances.

Produits et services

Pharmaceutical products and substances.

Produits et services

Pharmaceutical preparations.