VERFAHREN ZUR HERSTELLUNG VON PHENYLESSIGSAEURE-DERIVATEN

3-acyl-acrylic acids prepn - from a ketone and glyoxylic acid (deriv)

... 3-Acyl-acrylic acids of formula (I):- (in which A is aryl or heteroaryl opt. substd. by lower alkyl; R1 and R2 same or different, are H, lower alkyl, opt. substd. aroyl, halogen, NO2, acetylamino, CN, carbamoyl opt. substd. by one or more alkyl, carboalkoxy, OH, alkoxy, alkylthio, or alkylsulphenyl, or one of R1 and R2 may be cycloalkyl or cycloalkenyl opt. substd. by CN or alkyl, allyloxy, dialkylaminoalkyl, heteroaryl opt. hydrated, aryl opt. substd. by lower alkyl, halogen, NO2, acetylamino, CN, carbamoyl which may be substd. by one or more alkyl, carboalkoxy, OH, alkoxy, alkylthio or alkylsulphenyl, and R3 is H or lower alkyl) comprises reacting a ketone of formula (II): with a glyoxylic acid or its deriv. of formula (III): (in which R4 is H or lower alkyl; R5 and R6, same or different, are H, lower alkyl, or together form alkylene) in presence of acid condensation agent at 50 - 200 degrees C. Cpds. (I) are inters. for antiinflammatory and antitussive crotonic acid cpds.

UNGESAETTIGTE KAMPFERDERIVATE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG AUF DEM GEBIET DER PHARMAZIE UND DER KOSMETIK

Indane compounds with smooth muscle relaxing and/or mast cell stabilising and/or anti-inflammatory activity

3-Benzylidene camphor derivatives

The invention relates to new 3-benzylidene-camphor derivatives of the formula: (I) in which R1 denotes H or SO3(-)M(+), with M=H, an alkali metal or N(+)(R3)4, with R3=H or C1-C4 alkyl or hydroxyalkyl; R2 denotes C1-C4 alkyl or C1-C4 alkoxy and n=0-4; and Z denotes in which R4 has the same meaning as R1 and can be identical or different, or alternatively in which R5 denotes H, optionally substituted aryl, C1-C4 alkyl, -CN, -COOR7 or and R6 denotes -COOR8 or in which R7 and R8, which are identical or different, denote alkyl, alkenyl, cycloalkyl or aralkyl and R9 and R10, which are identical or different, denote H, alkyl, alkenyl or cycloalkyl; if R5=H, alkyl or aryl, R6 can represent -COO(-)M(+); the methylidene-camphor radical, on the one hand, and the radical Z, on the other hand, are in the meta or para position. These derivatives act as sun filters.

Anti-inflammatory phenylacetic acid derivatives

Anti-inflammatory agents for external use comprise a compound of formula: wherein: n=1 or 2; R<1> is hydrogen or lower alkyl, preferably methyl; R<2> is hydrogen, lower alkyl, aralkyl or pyridylmethyl; and ...

PROSTAGLANDINS

New phenylacetic acid derivatives

Phenylacetic acid derivatives of the formula wherein n is an integer of 2 to 5; R1 is hydrogen, halogen, trifluoromethyl, nitro or amino; R2 and R3 each independently is hydrogen or lower alkyl; or together form an ethylene group; X1 represents two hydrogen atoms or an oxo group; and Y1 is cyano, hydroxyamidocarbonyl, carbamoyl, 5-tetrazolyl or carboxyl; and for derivatives wherein Y is carboxyl, salts thereof with physiologically compatible bases, esters thereof from physiologically acceptable alcohols and amides thereof from physiologically acceptable amines have valuable pharmacological activity, e.g., as antiinflammatory agents.

New derivatives of the dibenzo [has, D] cycloheptene, their salts and their preparation.

Method of preparation of new hydro compounds aromatic bicyclic.

VERFAHREN ZUM HERSTELLEN VON NEUEN 3-BENZYLIDEN- CAMPHER-VERBINDUNGEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN SUBSTITUIERTEN PHENYLESSIGSAEUREN, DEREN NIEDEREN ALKYLESTERN UNDSALZEN

(ETHYLENEDIOXO-3,3 ZYCLOHEXYL) - 4 AKETOPHENON AND DERIVATIVES OF IT, PROCEDURES FOR THEIR PRODUCTION AND USE OF THESE CONNECTIONS.

CONNECTIONS USABLE AS INTERMEDIATE PRODUCTS TO THE PRODUCTION OF PIPERIDINDERIVATE

Piperidine derivatives and process for their production

Phenylketone carboxylate compounds and pharmaceutical compositions for the prevention and treatment of osteoporosis

The present invention concerns the use of compounds for preventing and/or treating osteoporosis, for stimulating bone formation, for stimulating the differentiation and mineralization of osteoblasts, or for inhibiting bone resorption in a subject. These novel uses have been found for compounds represented by Formula I and pharmaceutically acceptable salts thereof. wherein: R ...

UNSATURATED CAMPHOR DERIVATIVES

OXYBENZYLIDIENE-BORNANONES

COMPOSES HYDRO AROMATIQUES BICYCLIQUES, LEUR PREPARATION ET LEUR APPLICATION COMME MEDICAMENTS

FLUORENE-2-ACETIC ACIDS AND DERIVATIVES, PROCESS AND METHOD OF USING

COMPOSES HYDRO AROMATIQUES BICYCLIQUES, LEUR PREPARATION ET LEUR APPLICATION COMME MEDICAMENTS

THERAPEUTIC COMPOUNDS

Compounds having a structure are disclosed herein (Formula I). Compositions, methods, and medicaments related to the therapeutic use of these compounds a re also disclosed.

SPIRO COMPOUNDS AND PHARMACEUTICAL USE THEREOF

Disclosed is a spiro-ring compound represented by the general formula [Ia], a pharmaceutically acceptable salt thereof, or a solvate of the compound or the pharmaceutically acceptable salt thereof.

PHENYLACETIC ACID DERIVATIVES

THERAPEUTIC AGENT FOR DIABETES

A therapeutic agent for diabetes comprising a compound represented by general formula (I) [wherein X represents (a), (b) or (c)] [wherein R4 and R5, which may be the same or different, represent a hydrogen atom, or an optionally substituted alkyl group having 1 to 5 carbon atoms and R6 represents a hydrogen atom or an amino protective group; R1 represents an optionally substituted alkyl group having 1 to 5 carbon atoms or an optionally substituted alkenyl group having 2 to 6 carbon atoms; R2 represents a hydrogen atom or an optionally substituted alkyl group having 1 to 5 carbon atoms; R2' represents a hydrogen atom; and R3 represents an optionally substituted alkyl group having 1 to 5 carbon atoms], a prodrug compound thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof, or a solvate thereof. The agent has an excellent blood sugar lowering activity in the case of a high blood sugar level, does not influence the blood sugar in the case of a normal blood sugar level, that is, does not cause any severe side effect, such as hypoglycemia, and is useful not only as a therapeutic agent but also as a prophylactic for chronic complications of diabetes.

INDANE DIMER COMPOUNDS AND THEIR PHARMACEUTICAL USE

Indame dimer compounds and their pharmaceutical use particularly to achieve smooth muscle relaxing activity and/or mast cell stabilising activity and/or anti-inflammatory activity are described. ...

Phenanthrene compounds anti-androgens

Phenanthrene compounds of general formula (I), of which the left hand side corresponds to parts 2-4 and the right hand side to parts 5-7, and their salts and quaternary compounds. R1=H-, C1-4 alkyl, alkenyl- or alkynyl- R2=H-, methyl- R3=H-, C1-4 alkyl-, alkenyl- or alkynyl- X=presence or absence of -CH2- R4=H-, acyl- or O, N-group next to ketone e.g oxime ketal or R5 = C1-4 alkyl-, alkenyl-, alkynyl- Z=tert.amino-, acyloxy-, C1-4 alkyloxy- dotted line = presence or absence of a double bond (R1)=absence of R1 if there is a double bond at 4a for instance compound Anti-androgen, anti-myogen, anti-thymolytic without other hormone activity. For treatment of hirsutism.

Procédé de préparation de nouveaux acides spiro benzocyclane acétiques

Procédé de préparation de nouveaux acides spiro benzocyclane acétiques

Anti-inflammatory and analygesic spiro

Anti-inflammatory and analgesic spiro-benzocyclane acetic acids Spiro-benzocyclane acetic acids (I) (where R is H or opt. branched 1-4C alkyl; R3 is H, Cl, 1-4C alkoxy or CF3; Y is -CH2-, -O- or -S- and n is 2, 3 or 4) and their esters and salts with an (in)organic non-toxic base, for treatment of rheumatic ailments, arthritis, lumbago, neuralgia, toothache and post operation pains, can be given by mouth, parenterally, as suppositories or per-mucously. - Pref. synthesis includes reaction of cyanoalkyl acetate with a ketal of 2-R3-4-acetylphenyl MgBr to form a ketal which is hydrolysed and decarboxylated, converted to a thiocarbonyl deriv. which is converted to an acid deriv., cyclised reduced, esterified and alkylated.

Procédé de préparation de nouveaux acides spiro benzocyclane acétiques

PROCEDE DE PREPARATION D'ACIDES FLUORENE-2-ACETIQUES ET DE LEURS DERIVES.

PROCEDE DE PREPARATION D'ACIDES FLUORENE-2-ACETIQUES ET DE LEURS DERIVES.

PROCEDE DE PREPARATION D'ACIDES FLUORENE-2-ACETIQUES ET DE LEURS DERIVES.

PROCEDE DE PREPARATION D'ESTERS D'ACIDES FLUORENE-2-GLYOXYLIQUES.

Verfahren zur Herstellung von Phenylessigsäuren

Process for the preparation of novel indanacetic acids and their esters

The acids and esters correspond to the formula I. In this formula, R1 denotes lower alkyl, R2 denotes hydrogen or lower alkyl, R3 denotes hydrogen or lower alkyl, R4 denotes hydrogen or lower alkyl, R5 denotes hydrogen, chlorine or lower alkyl and R6 and R7 each denote a hydrogen atom or, if R5 represents hydrogen, also denote chlorine or lower alkyl. The compounds of the formula I are obtained by reduction of the corresponding alpha -oxo- or alpha -hydroxyacetic acids. They and their salts have interesting pharmacodynamic properties, in particular anti-inflammatory and anti-arthritic actions. ...

SUBSTITUTED NAPHTHYL-1 ACETIC ACID DERIVATIVES, METHODS FOR THEIR PREPARATION AND MEDICINE CONTAINING THEM.

[...][...], THEIR METHODS OF PREPARATION, AND COSMETIC COMPOSITIONS CONTAINING THEM.

2,3-Dihydroindene derivative

The 2,3-dihydroindene derivatives of formula: in which R<1> and R<2> each represent a hydrogen atom, a halogen atom, a nitro group, a lower alkyl group or a lower alkyloxy group, provided that R<1> and R<2> are not a hydrogen atom at the same time, and provided that n is an integer between 2 and 4, are described. This 2,3-dihydroindene derivative can be used as an anti-inflammatory medicament.

DIHYDROXY 1.8 SUBSTITUTED ANTHRONES AND 9 10 AND COMPOSITIONS FOR HUMAN OR VETERINARY MEDICINE AND THE COSMETIC CONTAINING THEM.

DIBENZO (A, D) CYCLOHEPTEN DERIVATIVES AND PROCEDURES FOR THEIR PRODUCTION.

ANTIINFLAMMATORI MEANS FOR AEUSSERLICHE APPLICATION.

CAMPHOR UNSATURATED DERIVATIVES, METHODS FOR THEIR PREPARATION AND PHARMACEUTICAL AND COSMETIC COMPOSITIONS CONTAINING THEM.

3 A-BENZYLIDENE-CAMPHOR DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE FOR PROTECTION AGAINST UV RAYS.

PREPARING THE (ETHYLENEDIOXO-TO-3.3 THE CYCLOHEXYL) ACETOPHENONE AND -4 DERIVATIVES.

COMPOSITION ANTI-INFLAMMATOIRE CONTENANT A TITRE DE PRINCIPE ACTIF DES DERIVES DE L'ACIDE PHENYL-ACETIQUE OU PHENYL-PROPIONIQUE

L'INVENTION A POUR OBJET DES AGENTS ANTI-INFLAMMATOIRES POUR USAGE EXTERNE COMPRENANT UN COMPOSE REPONDANT A LA FORMULE: (CF DESSIN DANS BOPI) DANS LAQUELLE: N1 OU 2; RH OU UN GROUPE ALCOYLE INFERIEUR, DE PREFERENCE METHYLE; RH OU UN GROUPE ALCOYLE INFERIEUR, ARALCOYLE OU PYRIDYLMETHYLE; ET A-B- REPRESENTE UN GROUPE CH-CH- OU CCH-.

INDANYL OXY OR THIO METHYL TETRAZOLES AND INDANYL OSY OR THIO- TETRAZOLES THEIR PREPARATION AND COMPOSITIONS CONTAINING THEM

NOUVEAUX ANALOGUES 5,6-DIHYDRO DE PROSTAGLANDINE -I2, LEUR PROCEDE DE PRODUCTION ET MEDICAMENT LES CONTENANT

L'INVENTION A TRAIT AU DOMAINE DE LA CHIMIE PHARMACEUTIQUE. ELLE CONCERNE DE NOUVEAUX ANALOGUES, 5,6-DIHYDRO DE PROSTAGLANDINE I ET UN PROCEDE PERMETTANT DE LES OBTENIR. LES COMPOSES DE L'INVENTION INHIBENT L'AGREGATION DES PLAQUETTES OU L'ACIDITE GASTRIQUE CHEZ LES PATIENTS DONT L'ETAT NECESSITE CE TYPE DE TRAITEMENT.

DERIVES DU DIBENZO (A,D) CYCLOHEPTENE, LEUR PREPARATION ET MEDICAMENTS CONTENANT CES SUBSTANCES

Dérivés du dibenzooa,dÁocycloheptène et leur préparation. Ils sont caractérisés par la formule générale ...

([...]-TO-3.3 THE CYCLOHEXYL) -4 ACETOPHENONE AND DERIVATIVES THEREOF, METHODS FOR THEIR PREPARATION AND THEIR USE

DERIVES D'ACIDES PHENYLACETIQUES ET MEDICAMENTS QUI EN CONTIENNENT

Dérivés d'acides phényl-acétiques. Ils répondent à la formule : ...

Use of aroyl-alkanoic acid in cosmetics - for reducing secretion of sebaceous glands

NOVEL BICYCLIC AROMATIC, PROCESS FOR THEIR PREPARATION AND THEIR USE IN HUMAN AND VETERINARY MEDICINE AND IN COSMETICS

DIHYDROXY-1,8 ANTHRONES-9 SUBSTITUEES EN POSITION 10 ET LEUR UTILISATION EN MEDECINE HUMAINE OU VETERINAIRE ET EN COSMETIQUE

L'INVENTION CONCERNE LES DIHYDROXY-1,8 ANTHRONES-9 SUBSTITUEES EN POSITION 10 DE FORMULE: (CF DESSIN DANS BOPI) DANS LAQUELLE: R REPRESENTE UN RADICAL PRIS DANS LE GROUPE CONSTITUE PAR: (CF DESSIN DANS BOPI) R REPRESENTANT H, ALKYLE DE 1 - 8C, MONO OU POLYHYDROXYALKYLE DE 1 - 3C, CARBAMOYLE OU PHENYLE, R, R ET R REPRESENTANT H, ALKYLE DE 1 - 8C, MONO OU POLYHYDROXYALKYLE DE 3 - 8C EVENTUELLEMENT INTERROMPU PAR UN OXYGENE, CYCLOALKYLE DE 3 - 6C, OU R ET R FORMENT UN RADICAL DIVALENT: -(CH) -(CH)-O-(CH) OU -(CH)N(R)-(CH)-, R ETANT H, -CH OU -CH-CHOH R REPRESENTANT -COR, -CN, -CHO, -CONH OU -CONH-CHOH, ET R ET R ETANT H OU -CH, ET LEURS ISOMERES OPTIQUES. UTILISATION DES COMPOSES I EN MEDECINE HUMAINE OU VETERINAIRE, EN PARTICULIER DANS LE TRAITEMENT DU PSORIASIS ET EN COSMETIQUE.

[...]

MODULATORS OF MOLECULES WITH PHOSPHOTYROSINE RECOGNITION UNITS

The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, micro-organisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of general formula (I) wherein (L)n, n, Ar1 and R1 are defined as defined in the application.

2-aryl-cyclopentane-1,3-dione derivatives

The present invention relates to novel 2-aryl-3-hydroxy-cyclopent-2-en-1-one derivatives of the formula (I) in which X represents halogen, nitro, cyano, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl or halogenoalkoxy, Y represents hydrogen, halogen, nitro, cyano, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl or halogenoalkoxy, Z represents halogen, nitro, cyano, alkyl, alkoxy or halogenoalkoxy and A, B, D1, D2, G and n have the meaning given in the description, several processes for their preparation and their use as compositions for controlling pests and as herbicides.

9-HYDROXYFLUORENE-2-ALKANOIC ACIDS AND ESTERS THEREOF

Prostaglandins

PCT No. PCT/GB80/00001 Sec. 371 Date Sep. 3, 1980 Sec. 102(e) Date Sep. 3, 1980 PCT Filed Jan. 4, 1980 PCT Pub. No. WO80/01381 PCT Pub. Date Jul. 10, 1980.Novel bicyclo [2,2,1] heptanes and hept-2Z-enes are substituted at the 5-position by a 6-carboxyhex-2-enyl group or a modification thereof, and at the 6-position by an aldoxime or ketoxime group which is O-substituted by an aliphatic hydrocarbon residue, an aromatic residue, or an aliphatic hydrocarbon residue substituted directly or through an oxygen or sulphur atom by an aromatic residue. Such compounds may be prepared by the action of an oximating agent on an intermediate which is substituted at the 6-position by an aldehydic or ketonic carbonyl group. The compounds are of value for use in pharmaceutical compositions particularly in the context of the inhibition of thromboxane activity.

9,10-Dihydro-1,8,9-trihydroxy-9,10-anthracene alpha , beta -endosuccinimide, alpha , beta -endosuccinic acid and alpha , beta -endomaleic acid and derivative thereof

The invention concerns adducts of 1,8-dihydroxy-9-anthrone, of formula: (I) in which: R1 and R2, taken together, form one of the following divalent residues: (i) (ii) (iii) R3, R4, R'4, R5 and R'5 representing H, an alkyl group having 1-8 C with the exception of R5=R'5=CH3, a monohydroxyalkyl group with 2-8 C, possibly interrupted by one or more oxygens, a cycloalkyl group having 4-6 C, a phenyl group, or a benzyl group. Utilization of the compounds (I) in human or veterinary medicine, in particular in the treatment of psoriasis and or warts, and in cosmetics.

Phenanthrenverbindungen

OXYBENZYLIDENEBORNANONES THEIR PREPARATION AND THEIR USE IN COSMETICS

INDANYL OXY OR THIO METHYL TETRAZOLES AND INDANYL OSY OR THIO- TETRAZOLES THEIR PREPARATION AND COMPOSITIONS CONTAINING THEM

... 1373318 5 - [Indanyloxy(or thio)-] and 5 - [indanyloxy(or thio)methyl-]tetrazoles MERCK & CO Inc 6 Nov 1972 [12 Nov 1971] 50989/72 Heading C2C Novel compounds I in which A is oxygen or sulphur, R is C 1-5 alkyl, cycloalkyl, mononuclear aralkyl optionally halogenated or trifluoro substituted-C 1-5 -alkyl, R1 is hydrogen or halogen, R2 is hydrogen, C 1-5 alkyl or phenyl, each X which may be the same or different is halogen, a C 1-5 alkyl, trihalomethyl or acylamino or two adjacent X's may form a hydrocarbon chain, n is 0 or 1 and m is 1 to 3 are prepared by reacting a compound III with a hydrazoic acid salt in an inert solvent at a temperature of 0‹ to 100‹ C. to form a compound I in which R1 is hydrogen which may be reacted with a halogenating agent to form a compound I in which R1 is halogen. R is preferably ethyl propyl, cyclopentyl or 2,2,2- trifluoroethyl, R1 is hydrogen or chlorine, R2 is hydrogen, methyl and X m is up to two substituents ...

CYCLOALKANE DERIVATIVES

PROCEDURE FOR THE PRODUCTION OF NEW SUBSTITUTED PHENYLESSIGSAEUREN, THEIR LOW ONE ALKYL STAR AND SALTS

VERFAHREN ZUR HERSTELLUNG VON NEUEN 10,11-DIHYDRO-5-OXODIBENZO (A,D)CYCLOHEPTEN-2-YLALKANSAUREAMIDEN

AROMATIC DERIVATIVES THE BUTYRSAEURE, PROCEDURES FOR YOUR PRODUCTION AND YOUR USE IN COSMETIC AND PHARMACEUTICAL PREPARATIONS.

CYCLOHEXANE DERIVATIVES.

BIZYKLI AROMATIC CONNECTIONS, PROCEDURES FOR YOUR PRODUCTION AND YOUR USE AS DRUGS.

AGAINST THE CEREBRAL INSUFFICIENCY EFFECTIVE CONNECTIONS.

VERFAHREN ZUR HERSTELLUNG VON NEUEN 1-NAPHTHYL- ESSIGSAEUREN SOWIE DEREN ESTERN, AMIDEN UND PHARMAZEUTISCH VERTRAEGLICHEN SALZEN

PROCEDURE FOR the PRODUCTION OF NEW ONE 1-NAPHTHYL ACETIC ACIDS AS WELL AS THEIR ESTERS, AMIDES AND PHARMACEUTICAL COMPATIBLE ONE SALTS

PROCEDURE FOR THE PRODUCTION OF CONNECTIONS SUITABLY AS INTERMEDIATE PRODUCTS

PROCEDURE FOR THE PRODUCTION OF NEW SPIROBENZOCYCLANESSIGSAUREN

PROCEDURE FOR THE PRODUCTION OF NEW SUBSTITUTED PHENYLESSIGSAEUREN AND THEIR NIED. ALKYL STAR AND SALTS

PROCEDURE FOR the PRODUCTION OF NEW ONE 10,11-DIHYDRO-5-OXODIBENZO (A, D) CYCLOHEPTEN-2-YLALKANSAUREAMIDEN

Novel intermediates useful for the preparation of antihistaminic piperidine derivatives

OXYBENZYLIDIENE-BORNANONES

Indane dimer compounds with smooth muscle relaxing and/or mast cell stabilising and/or antiinflammatory activity

Novel intermediates for the preparation of antihistaminic 4-diphenylmethyl/diphenylmethoxy piperidine derivatives

(ETHYLENEDIOXO-3,3 CYCLOHEXYL)-4 ACETOPHENONE AND DERIVATIVES THEREOF, PROCESSES FOR PREPARING THEM AND USE OF THESE COMPOUNDS

PHENYLACETIC ACID DERIVATIVES

CYCLODECAPENTAENE COMPOUNDS AND PROCESS FOR MAKING SAME

CYCLOHEXANE DERIVATIVES

A B s T R A C T CYCLOHEXANE DERIVATIVES This invention concerns novel (4-substituted-2-phenylcyclohexyl)alkenoic and alkanoic acid derivatives of the formula I wherein one of Ra and Rb is hydrogen, hydroxy, (1-6C)alkyl, (1-6C)alkoxy, (3-6C)alkenyloxy or phenyl(1-4C)alkoxy and the other of Ra and Rb is hydrogen, (1-6C)alkyl, (1-6C)alkoxy or (3-6C)alkenyloxy; or Ra and Rb together form a (2-4C)alkylanedioxy or oxo group; benzene ring X optionally bears a substituent selected from halogeno, (1-6C)alkyl, (1-6C)alkoxy, hydroxy, (2-6C)alkanoyloxy, (1-6C)alkanoylamino, trifluoromethyl and nitro; n is 3-5; Y is ethylene or vinylene; and in the cyclohexane ring, the substituents at positions 1 and 2 have cis- or trans- relative stereochemistry; and the pharmaceutically acceptable salts, (1-6C)alkyl esters and (1-6C)alkanesulphonamides thereof. The compounds of formula I possess valuable pharmacological properties of use in medicines. The invention also concerns processes for the manufacture of, ...

PROCESS FOR THE PREPARATION OF 1-NAPHTYL-ACETIC ACID DERIVATIVES

... . This invention relates to a process for the preparation of 1-naphthyl acetic acid derivatives having the general formula : (I) in which : R1 is a hydrogen atom or a straight- or branched-chain C1-6 alkyl group, R2 is a straight- or branched-chain alkyl group or a cycloalkyl group having 1-12 carbon atoms, A is a carbonyl or methylene group, R3 is a hydroxy group, a C1-6 straight- or branched-chain alkoxy group or a group of the formula NR4R5 in which R4 and R5 represent independently a hydrogen atom or, C1-6 straight- or branched-chain alkyl group or, together with the nitrogen atom to which they are attached, form a saturated or unsaturated heterocyclic radical, and their pharmaceutically acceptable salts. Said compounds have, in particular, anti-inflammatory, anti-pyretic and analgesic activities and are free from ulcerogenic activity under the administration conditions.

PROCESS FOR THE PREPARATION OF OXYBENZYLIDENE BORNANONES AND COSMETIC COMPOSITION THEREOF

L'invention est relative à de nouvelles oxy benzylidène bornanones. Ces composés répondent à la formule générale: dans laquelle Z et Z' désignent hydrogène ou un radical SO3H. l'un au moins des deux radicaux Z et Z' désignant hydrogène R1 désigne hydrogène ou un radical alkyle de 2 à 18 atomes de carbone, un radical alkenyle de 3 à 18 atomes de carbone un radical -(CH2CH2O)nH, , -CH2-CHOH-CH3, , -(CH2)mCO2R dans lequel R désigne H ou un radical alkyle. -(CH2)3SO3H ou un radical divalent -(CH2)m ou -CH2-CHOH-CH2-; m ayant les valeurs 1 à 10. n les valeurs 1 à 20 et p les valeurs 1 à 6: R3 et R4 représentant hydrogéne un radical alkyle éventuellement ramifié ou hydroxyle. ou bien formant un hétérocycle aminoaliphatique avec l'atome d'azote R2 désigne un atome d'hydrogène. un radical alcoxy ou un radical divalent - O - relié au radical R1 lorsque celui-ci est également divalent q désigne 1 ou 2, lorsque q a la valeur 2 R1 est un radical divalent et lorsque R1 désigne hydrogène ...

COMPOUND EFFECTIVE AS CEREBRAL INSUFFICIENCY IMPROVER

Compounds having the formula (I): (I) wherein A is -CH2-, -O-, or -S-; R1 is CH3 or OCH3; R2 is a hydroxy group or -CO-R4 wherein R4 is a hydroxy group, lower alkoxy group, benzyloxy group, morpholino group, thiomorpholino group, piperidino group or N-methylpiperazinyl group; R3 is H or a lower alkyl; and n is 0 or an integer of 1 to 6 or pharmaceutically acceptable salts thereof are useful in the treatment of cerebral insufficiency.

PROCESS FOR THE PREPARATION OF OXYBENZYLIDENE BORNANONES AND COSMETIC COMPOSITION THEREOF

10-SUBSTITUTED 1,8-DIHYDROXY-9-ANTHRONES AND THEIR USE AS THERAPEUTIC AGENTS IN HUMAN AND VETERINARY MEDICINES AND AS COSMETIC AGENTS

SUBSTITUTED 1,3-DIPHENYLPROPANE DERIVATIVES, PREPARATIONS AND USES THEREOF

La présente invention concerne des composés dérivés de 1,3-diphénylpropan e substitués, les compositions pharmaceutiques les comprenant ainsi que leur s applications thérapeutiques, notamment dans les domaines de la santé humai ne et animale.

NOVEL AND SPECIFIC INHIBITORS OF CYTOCHROME P450 26 RETINOIC ACID HYDROXYLASE

The present disclosure is generally directed to compositions and methods for treating diseases that are ameliorated by the inhibition of CYP26 mediated retinoic acid metabolism. The compositions comprise compounds of formula (I). A repreid50000060307390 IB/345 nullsents aryl optionally substituted with one, two, three, or four groups that are each independently halogen, cyano, nitro, Calkyl, Chaloalkyl, —NH, —NH(C-Calkyl), —N(C-Calkyl), —OH, C-Calkoxy, and C-Chaloalkoxy; X is a bond, —CH—, —CHR—, —C═CHR—, —NR—, —N═O—R—, —O—, —S—, —SO—, —SO—, —C(O)—, or —C(NR)—, or X is of formula (a), (b) or (c), wherein each n is independently 1, 2, or 3; each Ris independently hydrogen or Calkyl; Ris independently hydrogen, Calkyl, or —OR, where Ris selected from the group consisting of hydrogen, Calkyl, Calkenyl, CalkynyL Ccycloalkyl, heterocyclyl, aryl, arylCalkyl, heteroaryl, or heteroarylCalkyl; Y is Calkylene, Calkenylene, or Calkylylene moiety.

Spiro compounds and pharmaceutical use thereof

The Spiro compound represented by the following general formula [Ia], its pharmaceutically acceptable salt or a solvate thereof

Radiation-sensitive resin composition, resist pattern-forming method, polymer, and method for producing compound

A radiation-sensitive resin composition contains: a polymer having a structural unit that includes a group represented by formula (1); a radiation-sensitive acid generator; and an organic solvent. In the formula (1), R P represents a hydrogen atom or a monovalent organic group, and * denotes a binding site to a rest of the structural unit other than the group represented by the formula (1). It is preferred that R P in the formula (1) represents a monovalent organic group, and the monovalent organic group is an acid-nonlabile group. It is also preferred that R P in the formula (1) represents a monovalent organic group, and the monovalent organic group is an acid-labile group.

2-ARYL-ZINC-PROPIONATE CATALYST AND PREPARATION METHOD AND USE THEREOF

The present invention belongs to the technical field of chemical catalysts, and particularly relates to a zinc 2-arylpropionate catalyst, a preparation method therefor and use thereof The structural formula of the zinc 2-arylpropionate catalyst of the present invention is one of the following structures. The catalyst can be used for homogeneous catalysis of a 1,2-aryl rearrangement reaction of α-haloarylketal, and especially for synthesis of high yield and environmentally friendly 2-arylpropanonic acid non-steroidal anti-inflammatory analgesic drugs, such as, ibuprofen, ketoprofen, loxoprofen, flurbiprofen, fenoprofen, or naproxen and the like. 2. A method for preparing the zinc 2-arylpropionate catalyst in accordance with claim 1 , comprising the steps of:{'sub': 1', '4, '(1) an alkaline earth hydroxide is dissolved in a C-Calcohol, 2-arylpropionic acid is added, the reaction being for 0.5-2 h at room temperature to 100° C. to obtain a solution of alkaline earth 2-arylpropionate; said alkaline earth hydroxide is lithium hydroxide, sodium hydroxide, potassium hydroxide or calcium hydroxide, and the molar ratio of the 2-arylpropionic acid to the alkaline earth hydroxide is 1:0.8-1:1.5;'}(2) a zinc salt or zinc oxide is added into the above-mentioned alkaline earth 2-arylpropionate solution, the reaction being for 0.5-20 h at room temperature to 100° C. to obtain zinc 2-arylpropionate; said zinc salt is zinc chloride, zinc sulphate or zinc acetate; and the molar ratio of said zinc salt or zinc oxide to the alkaline earth 2-arylpropionate is 0.5:1-0.5:1.2.3. The method of claim 2 , characterized in that in step (1) claim 2 , the alkaline earth hydroxide is sodium hydroxide claim 2 , the C-Calcohol is methanol or ethanol claim 2 , the reaction temperature is 45-55° C. claim 2 , the reaction time is 0.5-2 h claim 2 , and the molar ratio of the 2-arylpropionic acid to the alkaline earth hydroxide is 1:1-1:1.1.4. The method of or claim 2 , characterized in that in step (2) ...

Indane dimer compounds and their pharmaceutical use

Indame dimer compounds and their pharmaceutical use particularly to achieve smooth muscle relaxing activity and/or mast cell stabilising activity and/or anti-inflammatory activity are described.

含芴结构的水性光引发剂及其制备方法和应用

本发明公开了一种含芴结构的水性光引发剂及其制备方法和应用。其中，该水性光引发剂具有如通式(Ⅰ)所示结构：

Patent FR2430938B1

Patent FR2528420B1

PHARMACEUTICAL COMPOSITIONS CONTAINING CAMPHO-METHYLIDENE CINNAMIC ACID DERIVATIVES

인단 다이머 화합물 및 그 약학적 용도

화합물 인단 다이머 화합물과 특별히 유연한 근육이완성 및/또는 마스트셀 안정성 및/또는 항염증성을 달성하기 위한 약학적 용도에 관한 것이다.

Novel oxybenzilidine bornanone compound*its manufacture and composition containing it

Therapeutic compounds and methods

本发明涉及式(I)化合物及其制备方法。还描述了包含式(I)化合物的药物组合物及其在治疗或预防与线粒体功能障碍相关的病症中的用途。式(I)

THERAPEUTIC COMPOUNDS AND METHODS

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2019 136 705 A (51) МПК C07C 50/12 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2019136705, 20.04.2018 (71) Заявитель(и): ЮНИВЕРСИТИ ОФ ТАСМАНИЯ (AU) Приоритет(ы): (30) Конвенционный приоритет: 21.04.2017 AU 2017901457 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 21.11.2019 R U (43) Дата публикации заявки: 21.05.2021 Бюл. № 15 (72) Автор(ы): ГЮВЕН, Нури (AU), СМИТ, Джейсон (AU), ВУЛЛИ, Кристел Ли (AU), НАДИКУДИ, Монила (AU) (86) Заявка PCT: (87) Публикация заявки PCT: WO 2018/191789 (25.10.2018) A Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр. 3, ООО "Юридическая фирма Городисский и Партнеры" R U (57) Формула изобретения 1. Соединение формулы (Ib): A 2 0 1 9 1 3 6 7 0 5 (54) ТЕРАПЕВТИЧЕСКИЕ СОЕДИНЕНИЯ И СПОСОБЫ 2 0 1 9 1 3 6 7 0 5 AU 2018/050360 (20.04.2018) Формула (Ib) или его фармацевтически приемлемая соль, в которой: R5 выбран из группы, включающей H и метил, R6 означает необязательно замещенный C5-C12 арил, R означает H или необязательно замещенный C1-C6 алкил; R13 в каждом случае независимо выбран из группы, включающей H, необязательно замещенный фенил и необязательно замещенный бензил, n означает целое число, выбранное из группы, включающей 1, 2, 3, 4 и 5, и m означает целое число, выбранное из группы, включающей 0, 1, 2 и 3. Стр.: 1 2. Соединение по п. 1, в котором R6 означает необязательно замещенный C6 арил. 3. Соединение по п. 1 или 2, в котором R6 означает диметоксифенил, предпочтительно 3,4-диметоксифенил. 4. Соединение по п. 1, в котором R5 означает H. 5. Соединение по п. 1, в котором R5 означает метил. 6. Соединение, выбранное из группы, включающей: Установленный № Структура R U R U A 2 0 1 9 1 3 6 7 0 5 A 2 0 1 9 1 3 6 7 0 5 Стр.: 2 A 2 0 1 9 1 3 6 7 0 5 A 2 0 1 9 1 3 6 7 0 5 R U R U Стр.: 3 A 2 0 1 9 1 3 6 7 0 5 A 2 0 1 9 1 3 6 7 0 5 R U R U Стр.: 4 A 2 0 1 9 1 3 6 7 0 5 A 2 0 1 9 1 3 6 7 0 5 R U R U Стр.: 5 R U R ...

Intermediates for the synthesis of bicyclo (2,2,1) heptanes and bicyclo (2,2,1) hept-2z-enes

Spirocompounds and pharmaceutical application thereof

FIELD: medicine, pharmaceutics. SUBSTANCE: invention refers to new compounds of the following general formula [1a], wherein R 1 represents (1) a hydrogen atom, (2) C 1 -C 6 alkyl group, (3) C 2 -C 6 alkenyl group, (4) C 2 -C 6 alkynyl group, (5) C 1 -C 6 alkoxygroup, (6) hydroxyC 1 -C 6 alkyl group, (7) C 1 -C 6 alkoxy(C 1 -C 6 )alkyl group, (8) -CONR 11 R 12 , wherein R 11 and R 12 are identical or different, and each represents a hydrogen atom or C 1 -C 6 alkyl group, (9) phenyl group or (10) a five-member heteroaryl group which contains at least one heteroatom specified in a group consisting of a nitrogen atom and oxygen atom, and which may be substituted by C 1 -C 6 alkyl group; R 2 represents (1) a halogen atom, (2) C 1 -C 6 alkyl group, (3) hydroxy group or (4) C 1 -C 6 alkoxy group; p is equal to 0, 1, 2 or 3; X represents a carbon atom or nitrogen atom; m1 is equal to 0, 1 or 2; m2 is equal to 0 or 1; the spiro ring AB may be substituted by 1-5 identical or different, specified in a group consisting of (1) hydroxy group, (2) C 1 -C 6 alkyl group, (3) C 1 -C 6 alkoxygroup and (4) oxo group; n1 is equal to 0, 1, 2, 3 or 4; n2 is equal to 1, 2, 3 or 4; n3 is equal to 0, 1 or 2, provided n2+n3 is equal to 2, 3 or 4; and a bond presented by the symbol means a single bond or a double bond, provided the three adjoining carbon atoms forms no allene bond presented by formula: C=C=C, or a pharmaceutically acceptable salt thereof. EFFECT: invention refers to a pharmaceutical composition possessing GPR40 agonist activity, to a GPR40 agonist drugs; to a hypoglycemic agent stimulating insulin secretion on the basis of the above compounds. 45 cl, 42 tbl, 120 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 490 250 (13) C2 (51) МПК C07C C07C C07D C07D C07D C07D C07D ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИC07C C07C C07C 59/72 (2006.01) 235/34 (2006.01) 213/64 (2006.01) 257/04 (2006.01) 263/32 (2006.01) 277/20 (2006.01) 277/34 (2006.01) 59/68 (2006.01) 229/26 (2006.01) 59/ ...

Method of preparing derivatives of dibezo (a,d) cycloheptene or their salts

Compound effective as cerebral insufficiency improver

내용없음. None.

S-loxoprofen derivative and preparation method, pharmaceutical composition and application thereof

本发明公开了一种S‑洛索洛芬衍生物及其制备方法、药物组合物和用途。所述的S‑洛索洛芬衍生物由S‑洛索洛芬与胺或氨基酸形成的衍生物、立体异构体、水合物、溶剂化物、或其药学上可接受盐；所述S‑洛索洛芬衍生物如式(I)所示，其中各基团的定义详见说明书；该衍生物在提高疗效，进而降低给药剂量、降低不良反应方面取得良好的效果。

Patent JPS6347700B2

Patent RU2019136705A3

ВУ“? 2019136705” АЗ Дата публикации: 04.08.2021 Форма № 18 ИЗПМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение 5 «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2019136705/04(072492) 20.04.2018 РСТ/АЧ2018/050360 20.04.2018 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 2017901457 21.04.2017 АО Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) ТЕРАПЕВТИЧЕСКИЕ СОЕДИНЕНИЯ И СПОСОБЫ Заявитель: ЮНИВЕРСИТИ ОФ ТАСМАНИЯ, АЧ 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. Примечания) [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) С07С 50/12 (2006.01) С07С 53/136 (2006.01) Аб/1К 31/192 (2006.01) С07С 233/48 (2006.01) С07С 323/61 (2006.01) Аб/1К 31/4015 (2006.01) С07С 233/13 (2006.01) (070 209/14 (2006.01) Аб1Р 39/06 (2006.01) С07С 233/10 (2006.01) Аб1К 31/198 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) 5.2 Другая проверенная документация в той мере, в какой она включена в поисковые подборки: 5.3 Электронные базы данных, использованные при поиске (название базы, и если, возможно, поисковые термины): Езрасепеь Рабеагсп, Кеахуз 6. ДОКУМЕНТЫ, ОТНОСЯЩИЕСЯ К ...

The method of obtaining oxaspirobenzocyclan acetic acid

METHOD FOR CONTROLLING MUSHROOMS

SUBSTITUTED 1,3-DIPHENYLPROPANE DERIVATIVES, PREPARATIONS AND USES

La présente invention concerne des composés dérivés de 1,3-diphénylpropane substitués, les compositions pharmaceutiques les comprenant ainsi que leurs applications thérapeutiques, notamment dans les domaines de la santé humaine et animale.

Intermediates useful for the preparation of antihistaminic piperidine derivatives

The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R 1 represents hydrogen or hydroxy; R 2 represents hydrogen; R 1 and R 2 taken together form a second bond between the carbon atoms bearing R 1 and R 2 ; n is an integer of from 1 to 5; m is an integer 0 or 1; R 3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R 1 and R 2 are taken together to form a second bond between the carbon atoms bearing R 1 and R 2 or where R 1 represented hydroxy, m is an integer 0.

Patent FR2300551B2

PHENYLACETIC ACID DERIVATIVES AND MEDICINAL PRODUCTS CONTAINING IT

Dérivés d'acides phényl-acétiques. Ils répondent à la formule : Derivatives of phenyl-acetic acids. They answer the formula:

ANTI-INFLAMMATORY COMPOSITION CONTAINING, AS ACTIVE INGREDIENT, PHENYL ACETIC OR PHENYL PROPIONIC ACID DERIVATIVES

L'INVENTION A POUR OBJET DES AGENTS ANTI-INFLAMMATOIRES POUR USAGE EXTERNE COMPRENANT UN COMPOSE REPONDANT A LA FORMULE: (CF DESSIN DANS BOPI) DANS LAQUELLE: N1 OU 2; RH OU UN GROUPE ALCOYLE INFERIEUR, DE PREFERENCE METHYLE; RH OU UN GROUPE ALCOYLE INFERIEUR, ARALCOYLE OU PYRIDYLMETHYLE; ET A-B- REPRESENTE UN GROUPE CH-CH- OU CCH-. THE SUBJECT OF THE INVENTION IS ANTI-INFLAMMATORY AGENTS FOR EXTERNAL USE COMPRISING A COMPONENT RESPONDING TO THE FORMULA: (CF DRAWING IN BOPI) IN WHICH: N1 OR 2; RH OR A LOWER ALCOHYL GROUP, PREFERABLY METHYL; RH OR A LOWER ALCOHYL, ARALCOYL OR PYRIDYLMETHYL GROUP; AND A-B- REPRESENTS A CH-CH- OR CCH- GROUP.

NOVEL 3-BENZYLIDENE CAMPHERS, PROCESS FOR THEIR PREPARATION AND USE THEREOF FOR PROTECTION AGAINST UV RAYS

L'INVENTION CONCERNE DE NOUVEAUX DERIVES DU 3-BENZYLIDENE CAMPHRE DE FORMULE : (CF DESSIN DANS BOPI) OU R DESIGNE H, SOM AVEC M OU ALCALIN OU N(R) AVEC R H, ALKYLE OU HYDROXYALKYLE EN C-C;R DESIGNE C-C ALKYLE OU C-C ALCOXY,N 0-4;Z DESIGNEOU R A LA MEME SIGNIFICATION QUE R ET PEUT ETRE IDENTIQUE OU DIFFERENT OU BIEN (CF DESSIN DANS BOPI) OU R ET R, IDENTIQUES OU DIFFERENTS, DESIGNENT ALKYLE, ALCENYLE, CYCLOALKYLE OU ARALKYLE ET R ET R, IDENTIQUES OU DIFFERENTS, DESIGNENT H, ALKYLE, ALCENYLE OU CYCLOALKYLE, LORSQUE R H, R PEUT REPRESENTER -COOM; LES DEUX RADICAUX METHYLIDENE CAMPHRE D'UNE PART ET Z D'AUTRE PART ETANT EN META OU PARA. APPLICATION : EN COSMETIQUE POUR LA PROTECTION CONTRE LES RAYONS UV. THE INVENTION CONCERNS NEW DERIVATIVES OF 3-BENZYLIDENE CAMPHOR OF FORMULA: (CF DRAWING IN BOPI) OR R DESIGNATES H, SOM WITH M OR ALKALINE OR N (R) WITH RH, ALKYL OR HYDROXYALKYL IN CC; R DESIGNATES CC ALKYL OR CC ALCOXY, N 0-4; Z DESIGNATED OR RA THE SAME MEANING AS R AND MAY BE THE SAME OR DIFFERENT OR GOOD (CF DRAWING IN BOPI) OR R AND R, IDENTICAL OR DIFFERENT, DESIGNATE ALKYL, ALKENYL, CYCLOALKYL OR ARALKYL AND R AND R, IDENTICAL OR DIFFERENT, DESIGNATE H, ALKYL, ALCENYL OR CYCLOALKYL, WHEN RH, R MAY REPRESENT -COOM; THE TWO METHYLIDENE CAMPHOR RADICALS ON THE ONE HAND AND Z ON THE OTHER HAND BEING IN META OR PARA. APPLICATION: IN COSMETICS FOR PROTECTION AGAINST UV RAYS.

4-Oxo-4-phenyl-2-methyl(ene)-butyric acid derivs. - analgesics, antiinflammatories and hypocholesterolemiants

DIBENZO (A, D) CYCLOHEPTENE DERIVATIVES, THEIR PREPARATION AND MEDICINES CONTAINING THESE SUBSTANCES

Dérivés du dibenzoØa,dõcycloheptène et leur préparation. Ils sont caractérisés par la formule générale DibenzoØa and cycloheptene derivatives and their preparation. They are characterized by the general formula

NEW

Patent FR2062864A1

5-oxo dibenzo(a,d)cycloheptene derivs - with analgesic, antipyretic and anti-inflamm- atory activity

Novel cpds. of formula (I): (where X is H, halogen, 1-4C alkyl(thio) or alkoxy or CF3; R1 and R2 are H or 1-4C alkyl; R3 is OH, 1-4C alkoxy, 2,2-dimethyl-1,3-dioxolan-4-ylmethoxy or NR4R5; R4 and R5 are H, 1-4C (hydroxy)alkyl or Ph or NR4R5 is a 5- or 6-membered heterocycle opt. contg. a 2nd heteroatom selected from O S and NR; and R is H or 1-4C alkyl) are prepd. by (a) cyclisn and partial hydrolysis of a cpd. (II): (where Y is OH or Cl) to give (I; R3=NH2); (b) hydrolysis of (I; R3=NH2) or the corresp. nitrile to give (I; R3=OH); or (c) reacting R3H with the corresp. acid halide to form other esters and amides (I).

DERIVATIVES OF NAPHTHYL-1 ACETIC ACID, THEIR METHOD OF PREPARATION AND THEIR THERAPEUTIC APPLICATION

La présente invention est relative à des dérivés d'acide naphtyl-1 acétique répondant à la formule générale : The present invention relates to 1-naphthylacetic acid derivatives corresponding to the general formula:

Compounds

5-oxo dibenzo(a,d)cycloheptene derivs - with analgesic, antipyretic and anti-inflamm- atory activity

Novel cpds. of formula (I): (where X is H, halogen, 1-4C alkyl(thio) or alkoxy or CF3; R1 and R2 are H or 1-4C alkyl; R3 is OH, 1-4C alkoxy, 2,2-dimethyl-1,3-dioxolan-4-ylmethoxy or NR4R5; R4 and R5 are H, 1-4C (hydroxy)alkyl or Ph or NR4R5 is a 5- or 6-membered heterocycle opt. contg. a 2nd heteroatom selected from O S and NR; and R is H or 1-4C alkyl) are prepd. by (a) cyclisn and partial hydrolysis of a cpd. (II): (where Y is OH or Cl) to give (I; R3=NH2); (b) hydrolysis of (I; R3=NH2) or the corresp. nitrile to give (I; R3=OH); or (c) reacting R3H with the corresp. acid halide to form other esters and amides (I).

Patent FR2492372B1

ANTI-INFLAMMATORY COMPOSITION CONTAINING AS ACTIVE INGREDIENT DERIVATIVES OF PHENYL-ACETIC OR PHENYL-PROPIONIC ACID

NOVEL 2,3-DIHYDRO-INDENE DERIVATIVES, PREPARATION METHODS THEREOF AND THERAPEUTIC APPLICATION THEREOF

Pharmaceutical compositions containing camphormethylidenecinnamic acid derivatives

The present invention relates to a pharmaceutical composition containing, by way of active ingredient, a camphormethylidenecinnamic acid derivative of formula: in which: R1 denotes a linear or branched C1-C4 alkyl, or a C1-C4 alkoxy, n being an integer ranging from 0 to 4; when n is equal to or greater than 2, the radicals R1 may be identical or different, R2 denotes H, a C1-C4 alkyl, an aryl which is optionally substituted by halogen atoms or by: a C1-C4 alkyl or alkoxy, a radical -CN, -COOR4 or and R3 denotes -COOR5, , -CHO, -CH(OR9)2 or -CH2OR9, R4 and R5, which are identical or different, being alkyl, alkenyl, cycloalkyl or aralkyl containing at most 20 C, which are optionally substituted by hydroxyl, alkoxy, amine or quaternary ammonium groups, R6 and R7, which are identical or different, denoting H or alkyl, alkenyl, cycloalkyl or aralkyl containing at most 20 C, which are optionally substituted by hydroxyl, alkoxy, amine or quaternary ammonium groups, R9 denotes H or an alkyl, cycloalkyl or aralkyl containing at most 20 C, or alternatively, when R2 denotes H, an alkyl or aryl which is optionally substituted, R3 may represent COO<6>M<4> where M is H, an alkali metal or N<4)<R8)4, R8 denoting H or a C1-C4 alkyl or hydroxyalkyl, both radicals and methylidenecamphor being in the para or meta position relative to each other on the aromatic nucleus, in a nontoxic carrier or excipient. Application for the treatment and prophylaxis of neoplasias and dermatological and rheumatic disorders.

Phenylketone carboxylate compounds and pharmaceutical compositions for the prevention and treatment of osteoporosis

The present invention concerns the use of compounds for preventing and/or treating osteoporosis, for stimulating bone formation, for stimulating the differentiation and mineralization of osteoblasts, or for inhibiting bone resorption in a subject. These novel uses have been found for compounds represented by Formula I and pharmaceutically acceptable salts thereof. wherein: R1and R2 are independently equal to H, F or OH; A is (CH2)mCOOH, W(CH2)mCOOH, or Y-CH(COOH)-(CH2)p-CH3 when B is H; or B is (CH2)mCOOH, W(CH2)mCOOH, or Y-CH(COOH)-(CH2)p-CH3 when A is H; or A and B are covalently bonded to form a five (5), six (6), or seven (7)-membered cycloalkyl substituted with COOH; where: Y is O, S, HN or CH2; W is 0, S or NH; m is 0-2; and p is 3-7; D is CO(CH2)nCH3 or CHOH(CH2)nCH3 or 0(CH2)nCH3 where n is 2-6; and E is H or F.

Patent FR2409997A1

L'INVENTION A TRAIT AU DOMAINE DE LA CHIMIE PHARMACEUTIQUE. ELLE CONCERNE DE NOUVEAUX ANALOGUES, 5,6-DIHYDRO DE PROSTAGLANDINE I ET UN PROCEDE PERMETTANT DE LES OBTENIR. LES COMPOSES DE L'INVENTION INHIBENT L'AGREGATION DES PLAQUETTES OU L'ACIDITE GASTRIQUE CHEZ LES PATIENTS DONT L'ETAT NECESSITE CE TYPE DE TRAITEMENT. THE INVENTION RELATES TO THE FIELD OF PHARMACEUTICAL CHEMISTRY. IT CONCERNS NEW ANALOGUES, 5,6-DIHYDRO OF PROSTAGLANDIN I AND A PROCESS FOR OBTAINING THEM. THE COMPOUNDS OF THE INVENTION INHIBIT PLATELET AGGREGATION OR GASTRIC ACIDITY IN PATIENTS WHOSE CONDITION REQUIRES THIS TYPE OF TREATMENT.

Spiro ring compounds and pharmaceutical use thereof

【課題】 ＧＰＲ４０機能を調節する薬剤、特にＧＰＲ４０作動薬（アゴニスト）として糖尿病、高血糖、耐糖能異常、空腹時血糖異常等の治療剤又は予防剤を提供する。 【解決手段】 下記一般式［Ｉａ］で表されるスピロ環化合物又はその医薬上許容される塩、或いはその溶媒和物。 【選択図】なし

Indanyloxytetrazoles

Tricyclic compounds

1374491 Dibenzocyclo-heptenes and -octenes and benzo-cyclohepta-thiophenes ROUSSEL UCLAF 22 May 1972 [21 May 1971] 24020/72 Headings C2C and C2P Novel compounds (IA) and (IB) (including salts thereof), where X is H, halogen or CF 3 , Y is H or C 1 to C 3 alkyl, Z is H, alkyl (optionally substituted by one or more hydroxy groups or by an acetonide group derived from two such hydroxy groups), dialkylaminoalkyl or N-heterocyclic-alkyl, n<SP>1</SP> is 2 or 3 and n is 0, 1 or 2, are made, e.g. by chain lengthening corresponding -CO 2 Z compounds {sequentially via the corresponding acid chlorides and diazoketones, i.e. containing the grouping -CO.C(Y)N 2 } which are themselves obtained from the corresponding nitriles; a product (IA) or (IB) can be further chain lengthened to give higher homologues (IA) and (IB) and esterification and hydrolysis may also be effected. The following compounds are also prepared; 3-nitro-, -amino- and -cyano-5-oxo-8-chloro-10, 11- dihydro - 5H - dibenzo - [a,d] - cycloheptenes, the diazonium chloride salt of said amine, diethyl - 4 - (2 - ethoxycarbonyl) - thenyl phosphonate (prepared from triethyl phosphite and 2 - ethoxycarbonyl - 4 - bromomethylthiophene), 4 - [# - (2 - carboxy - phenyl) - vinyl and -ethyl]- thiophene - 2 - carboxylic acids, 3 - phenethyl - 6- bromo - isobenzofuran - 1 - one, 2 - (γ - phenylpropyl) - 5 - bromo - benzoic acid and 2 - bromo- 12 - oxo - 5,6,7,12 - tetrahydro - dibenzo - [a, d]- cyclooctene. Pharmaceutical preparations showing analgesic and anti-inflammatory actions contain (IA) and/or (IB) as active ingredient. Administration may be orally or by injection.

Hew phenylacetic acid derivatives

Spiro-ring compound and use thereof for medical purposes

Method for preparing phenylpropionic acid derivatives or salts thereof

본 발명은 소염 진통제로서 유용한 페닐프로피온산 유도체 또는 그의 염의 신규한 제조방법에 관한 것으로, 더욱 상세하게는 화학식 2의 2-(4-할로메틸페닐)프로피온산과 화학식 3의 알킬 2-옥소사이클로펜타논카르복실레이트를 반응시킨 후, 산 존재하에서 가수분해 및 탈탄산시키는 공정을 포함하는 것을 특징으로 하는 화학식 1의 2-(4-(2-옥소사이클로펜탄-1-일메틸)페닐)프로피온산 또는 그의 약제학적으로 허용가능한 염의 제조방법에 관한 것이다. (상기 구조식에서 X는 염소, 브롬 또는 요오드이고, R은 메틸 또는 에틸을 나타낸다.)

Ppar modulators

The present invention is directed to a compound of formula I, or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomer thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.

Patent FR2219777B1

Patent SU379082A3

UNSATURATED CAMPHOR DERIVATIVES, THEIR PREPARATION PROCESSES AND THEIR APPLICATION IN THE PHARMACEUTICAL AND THERAPEUTIC FIELDS

Intermediates useful for the preparation of antihistaminic piperidine derivatives

The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R 1 represents hydrogen or hydroxy; R 2 represents hydrogen; R 1 and R 2 taken together form a second bond between the carbon atoms bearing R 1 and R 2 ; n is an integer of from 1 to 5; m is an integer 0 to 1; R 3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R 1 and R 2 are taken together to form a second bond between the carbon atoms bearing R 1 and R 2 or where R 1 represented hydroxy, m is an integer 0.

2-ARYLCYCLOPENTAN-1,3-DION DERIVATIVES

NOVEL BORNANONE OXYBENZYLIDENES, PROCESS FOR THEIR PREPARATION, AND COSMETIC COMPOSITIONS CONTAINING THEM

L'invention est relative à de nouvelles oxybenzylidènes bornanones. Ces composés répondent à la formule gènerale : The invention relates to novel oxybenzylidene bornanones. These compounds correspond to the general formula:

Patent RU2017116154A3

ВУ” 2017116154” АЗ Дата публикации: 06.05.2019 Форма № 18 ИЗПМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение ж 5 «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2017116154/04(027965) 08.10.2015 РСТ/СА2015/000530 08.10.2015 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 62/062,660 10.10.2014 05 Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) СОЕДИНЕНИЯ ФЕНИЛКЕТОНКАРБОКСИЛАТА И ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ ДЛЯ ПРЕДОТВРАЩЕНИЯ И ЛЕЧЕНИЯ ОСТЕОПОРОЗА Заявитель: ПРОМЕТИК ФАРМА СМТ ЛИМИТЕД, СВ 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. п см. Примечания [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) Аб/1К 31/192 (2006.01) Аб1К 31/196 (2006.01) Аб/1К 31/235 (2006.01) Аб1К 31/20 (2006.01) Аб/1К 31/222 (2006.01) Аб1Р 19/10 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) Аб1КЗ1/192,31/196,31/20,31/222,31/235 Аб1К45/00, Аб1Р19/10, 19/02, 29/00 5.2 Другая проверенная документация в той мере, в какой она включена в поисковые подборки: 5.3 Электронные базы данных, использованные при поиске (название базы, и если, возможно, поисковые термины): РУ/РТ, ЕАРАТГУ, ...

Substituted 1,3-diphenylpropane derivatives, preparations and uses thereof

The present invention relates to substituted 1,3-diphenylpropane derivatives, to the pharmaceutical compositions containing them and to the therapeutic uses thereof, in particular in the fields of human and animal health.

Novel 11-hydroxy-9-keto-5,6-cis-13,14-cis-prostadienoic acid derivatives

This disclosure describes certain 11-hydroxy and 11-deoxy-9-keto(or hydroxy)-prostanoic acid derivatives useful as bronchodilators, hypotensive agents, anti-ulcer agents, or as intermediates.

AGAINST CONNECTIONS EFFECTIVE AGAINST CEREBRAL INSUFFICIENCY.

Phenylacetic acid derivatives

Intermediates for the synthesis of bicyclo (2,2,1) heptanes and bicyclo (2,2,1) hept-2Z-enes

Novel bicyclo[2,2,1]heptanes and hept-2Z-enes are substituted at the 5-position by a 6-carboxyhex-2-enyl group or a modification thereof as defined herein, and at the 6-position by a group in which R 1 represents an aliphatic hydrocarbon residue or an aliphatic hydrocarbon residue substituted directly or through an oxygen or sulphur atom by an aromatic residue, R2 represents hydrogen and R 3 represents a hydroxy group, or R 2 and R 3 together represent the oxygen atom of a carboxyl group. These compounds are of value for use in the synthesis of certain biologically active 5,6-disubstituted bicyclo[2,2,1]heptanes and hept-2Z-enes.

Patent JPS50135050A

Indane dimer compounds and their pharmaceutical use

Indane dimer compounds of general formula 5, 6 or 9 and their pharma- ceutical use, particularly to achieve smooth muscle relaxing activity and/or mast cell stabilising activity and/or antiinflammatory activity are described, wherein in formulae 5 and 9, R1 and R3 to R15, and in formula 6, R1, R2 and R4 to R15, are selected from one or more of the same or different of H, halo, h y- droxy, alkoxy, aryloxy acetoxy, carboxy, alkyl carbonyl, hydro carbonyl, amino, amido, alkylamino hydroxylamino, amine oxide groups, azo groups, cyano, hy- drazino groups, hydrazide groups, hydrazone groups, imide groups, iminoether groups, ureyl groups, oxime, nitro, nitrate, nitrite, nitroso groups, nitril e, hete- rocyclic groups containing one or more heteroatoms selected from N, O or S, aralkyl groups, mono and polybenzoid aryl groups, substituted aryl groups, thiol, thioureyl, phenylthiol groups, sulphonic acid groups, sulphoxide groups, sulphone groups, alkyl containing 1 to 10 carbon atoms or cycloalkyl groups containin g 3 to 8 carbon atoms which may be saturated or unsaturated, substituted alkyl or cycloalkyl groups which may be saturated or unsaturated. In formulae 5, 6 an d 9, X is O, NR (wherein R is acyl, alkyl or sulphonate groups), S, SO or SO2. In formulae 5, 6 and 9, any one or more of R1, 1R1; R2,1R2; R3 1R3; R9 1R9; R10 , 1R10 and R14, 1R14 may together represent oxo.

Naphryl-1-acetic acid derivatives, processes for their preparation and compositions containing them

Spirocyclic compounds and pharmaceutical uses thereof

UNSATURATED CAMPHOR DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THEIR APPLICATION IN THE PHARMACEUTICAL AND THERAPEUTIC FIELDS

COMPOSES DERIVES DU CAMPHRE DE FORMULE: (CF DESSIN DANS BOPI) DANS LAQUELLE : -R A R REPRESENTENT H, ALKYLE OU TRIFLUOROMETHYLE; -R EST H, ALKYLE, ALCOXY, ARYLE, -CN, OXAZOLINYLE OU UN RADICAL DES FORMULES SUIVANTES: (CF DESSIN DANS BOPI) DANS LESQUELLES : -R EST H, ALKYLE OU LE COMPOUNDS DERIVED FROM CAMPHOR OF THE FORMULA: (CF DRAWING IN BOPI) IN WHICH: -R A R REPRESENT H, ALKYL OR TRIFLUOROMETHYL; -R IS H, ALKYL, ALCOXY, ARYL, -CN, OXAZOLINYL OR A RADICAL OF THE FOLLOWING FORMULAS: (CF DRAWING IN BOPI) IN WHICH: -R IS H, ALKYL OR THE

Preparation process of loxoprofen sodium

本发明涉及有机合成技术领域，具体为一种洛索洛芬钠的制备工艺，本发明提供了一种具有式5结构的化合物并提供了其制备方法和用途，

Bicyclo(2,2,1)heptane and bicyclo(2,2,1)hepta-2z-ene compound

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

NEW DIBENZO SQUARE BRACKET ON A, SQUARE BRACKET FOR CYCLOHEPTEN DERIVATIVES, THEIR PRODUCTION AND COMPOSITIONS THEREOF

Patent FR2138257A1

The method of obtaining spiro-benzocyclan acetic acid

Biaromatic compounds, pharmaceutical and cosmetic compositions containing them and uses thereof

The invention relates to novel biaromatic compounds having general formula Iand their use in pharmaceutical compositions for use in human and veterinary medicine, in particular for treating dermatological, rheumatic, respiratory, cardiovascular, and ophthalmological disorders, and for use in cosmetic compositions.

Method of obtaining dibenzo(a,d)cycloheptene derivatives

Analogous process for the preparation of alpha-alkyl substituted fluoren-2-acetic acids.

Patent FR2265409B1

Novel 2,3-dihydro-indene derivatives

Novel 2,3-dihydro-indene derivatives having remarkable anti-inflammatory effects and represented by the following formula <IMAGE> wherein R<1> and R<2> are each a hydrogen atom, halogen atom, nitro group, lower alkyl group or lower alkoxy group with the proviso that R<1> and R<2> do not take a hydrogen atom at the same time, and n is an integer of 2-4.

7-oxo-benzocycloheptene acetic acids

BENZOCYCLOHEPTENE ACETIC ACIDS, E.G. 7-OXO-7H-BENZOCYCLOHEPTENE-6,8-DIACETIC ACID, ARE PREPARED BY REACTING A PHTHALALDEHYDE WITH A KETO-CARBOXYLIC ACID. THE RESULTING PRODUCTS ARE USEFUL AS ANTI-DIABETIC AGENTS.

BISAROMATIC COMPOUNDS, PHARMACEUTICAL AND COSMETIC COMPOSITIONS AND USES THEREOF

COMPOUNDS OF PHENYL KETONE CARBOXYLATE AND PHARMACEUTICAL COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF OSTEOPOROSIS

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2017 116 154 A (51) МПК A61K 31/20 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2017116154, 08.10.2015 (71) Заявитель(и): ПРОМЕТИК ФАРМА СМТ ЛИМИТЕД (GB) Приоритет(ы): (30) Конвенционный приоритет: 10.10.2014 US 62/062,660 32 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 10.05.2017 CA 2015/000530 (08.10.2015) (87) Публикация заявки PCT: R U Адрес для переписки: 123242, Москва, пл. Кудринская, д. 1, а/я 35, "Михайлюк, Сороколат и партнеры патентные поверенные" (54) СОЕДИНЕНИЯ ФЕНИЛКЕТОНКАРБОКСИЛАТА И ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ ДЛЯ ПРЕДОТВРАЩЕНИЯ И ЛЕЧЕНИЯ ОСТЕОПОРОЗА (57) Формула изобретения 1. Применение соединения Формулы I или его фармацевтически приемлемой соли для получения лекарственного средства для предотвращения и/или лечения остеопороза, где формула I представляет собой: , где R1 и R2 независимо представляют собой H, F или OH; Стр.: 1 A 2 0 1 7 1 1 6 1 5 4 A WO 2016/054725 (14.04.2016) 2 0 1 7 1 1 6 1 5 4 (86) Заявка PCT: R U (43) Дата публикации заявки: 12.11.2018 Бюл. № (72) Автор(ы): ГАНЬОН Лин (CA), ГРУА Брижит (CA) A представляет собой H, (CH2)mCOOH, W(CH2)mCOOH или и B представляет собой H, (CH2)mCOOH, W(CH2)mCOOH или при условии, что A представляет собой (CH2)mCOOH, W(CH2)mCOOH или , когда B представляет собой H; и B A 2 0 1 7 1 1 6 1 5 4 представляет собой , где Y представляет собой O, и p равен 5-7. 6.Применение по п 1, отличающееся тем, что R1 и R2 представляют собой H; B представляет собой H; A представляет собой 5-7; Y представляет собой O; и E представляет собой H. Стр.: 2 , где p равен A когда A представляет собой H; или A и B ковалентно связаны с образованием пяти-(5), шести-(6) или семи-(7)-членного циклоалкила, замещенного COOH; где Y представляет собой O, S, NH или CH2; W представляет собой O, S или NH; m равен 0-2; и p равен 3-7; D представляет собой C(O)-(CH2)n-CH3 или CH(OH)-(CH2)n-CH3, или O-(CH2)n-CH3, где n равен 2- ...

New hydro-aromatic bicyclic compounds and processes for their preparation

Patent FR2106396B1

Unsaturated derivatives of camphor

Patent FR2138257B1

Spiro-ring compound and use thereof for medical purposes

Method for obtaining derivatives of dibenzo (a,d) cycloheptene or their salts

Therapeutic agent for diabetes

A therapeutic agent for diabetes, which comprises a compound of the formula [I] wherein X is a group of the formula wherein R 4 and R 5 are the same or different and each is a hydrogen atom, an optionally substituted alkyl having 1 to 5 carbon atoms and the like, and R 6 is a hydrogen atom or an amino-protecting group; R 1 is an optionally substituted alkyl having 1 to 5 carbon atoms, an optionally substituted alkenyl having 2 to 6 carbon atoms and the like, R 2 is a hydrogen atom, an optionally substituted alkyl having 1 to 5 carbon atoms and the like, R 2 ' is a hydrogen atom, and R 3 is an optionally substituted alkyl having 1 to 5 carbon atoms and the like, a prodrug thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof and a solvate thereof. The compound of the present invention shows superior blood sugar decreasing action on the state of hyperglycemia, but does not affect the blood sugar when it is in the normal range or in the hypoglycemic state, which means that it is free of serious side effects such as hypoglycemia. Therefore, the compound of the present invention is useful as a therapeutic drug for diabetes and also useful as a preventive of the chronic complications of diabetes.

Organic nitric oxide enhancing salts of nonsteroidal antiinflammatory compounds, compositions and methods of use

The invention describes novel organic nitric oxide enhancing salts of nonsteroidal antiinflammatory drugs (NSAIDs) and novel compositions comprising at least one organic nitric oxide enhancing salt of an NSAID, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one organic nitric oxide enhancing salt of an NSAID, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating inflammation, pain and fever; (b) treating gastrointestinal disorders; (c) facilitating wound healing; (d) treating gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; (e) treating inflammatory disease states and/or disorders; (f) treating ophthalmic disorders; (h) treating peripheral vascular diseases; (i) treating diseases resulting from oxidative stress; (j) treating endothelial dysfunctions; and (k) treating diseases caused by endothelial dysfunctions. The organic nitric oxide enhancing compounds that form salts with the NSAIDs are organic nitrates, organic nitrites, nitrosothiols, thionitrites, thionitrates, NONOates, heterocyclic nitric oxide donors and/or nitroxides. The heterocyclic nitric oxide donors are furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5- imines.

Tricyclic antiinflammatories and analgesics - of dibenzo cyclo octane and cyclopentane carboxylic acid derivs

Title cpds. are of formula (I): (where (1) m = 3; X = H; Y = H or 1-3C alkyl; Z = H, 1-5C alkyl, 2,3-dihydroxypropyl or its acetonide, dialkylaminoalkyl, alkyl subst. by N heterocycle, or alkali metal; and n = 0-2; or (2) m = 2; and (a) Y = CH3; n = 0; Z = H or and X = Cl; or (b) Y = H; n = 1 or 2, z = H; and X = H; or (c) Y = H; n = 0; X = Cl; and Z = 2,3-dihydroxypropyl).

Novel and specific inhibitors of cytochrome p450 26 retinoic acid hydrolase

The present disclosure is generally directed to compositions and methods for treating diseases that are ameliorated by the inhibition of CYP26 mediated retinoic acid metabolism.

Isoquinolineacetic acid

Substituted 1,3-diphenylpropane derivatives, preparations and uses thereof

The present invention concerns substituted 1,3-diphenylpropane derivatives, pharmaceutical compositions comprising them and the therapeutic uses thereof, particularly in the field of human and animal health.

{8 1-Oxo-2-halo(or hydrogen) indanyloxy{9 -alkanoic acid

[1-Oxo-2-halo(or hydrogen)indanyloxy(or thio)]-alkanoic acid products and salts, esters and amide derivatives where the indanyl ring may be further substituted with from 2 to 5 nuclear substituents. The [1-oxo-2-haloindanyloxy-(or thio)]alkanoic acids are prepared (1) via the halogenation of a [1-oxoindanyloxy(or thio)]alkanoic acid or (2) via the addition of halogen to a [1-oxoindenyloxy(or thio)]-alkanoic acid. The [1-oxoindanyloxy(or thio)]alkanoic acids are prepared (1) via cyclialkylation of a (2-alkylideneacyl)-phenoxy(or thio)alkanoic acid or (2) via etherification of a hydroxy(or mercapto)-2-alkyl-1-indanone. The [1-oxo-2-halo(or hydrogen)indanyloxy(or thio)]alkanoic acids are diuretics and saluretics. In addition, some of these compounds are also able to maintain the uric acid concentration in the body at pretreatment level or to cause a decrease in uric acid concentration.

Phenylketone carboxylate compounds and pharmaceutical compositions for the prevention and treatment of osteoporosis

The present invention concerns the use of compounds for preventing and/or treating osteoporosis, for stimulating bone formation, for stimulating the differentiation and mineralization of osteoblasts, or for inhibiting bone resorption in a subject. These novel uses have been found for compounds represented by Formula I and pharmaceutically acceptable salts thereof. wherein: R 1 and R 2 are independently equal to H, F or OH; A is (CH 2 ) m COOH, W(CH2)mCOOH, or Y-CH(COOH)-(CH2)p-CH3 when B is H; or B is (CH2)mCOOH, W(CH2)mCOOH, or Y-CH(COOH)-(CH 2 ) p -CH 3 when A is H; or A and B are covalently bonded to form a five (5), six (6), or seven (7)-membered cycloalkyl substituted with COOH; where: Y is O, S, HN or CH 2 ; W is 0, S or NH; m is 0-2; and p is 3-7; D is CO(CH 2 ) n CH 3 or CHOH(CH 2 )nCH 3 or 0(CH 2 ) n CH 3 where n is 2-6; and E is H or F.

Substituted 1,3-diphenylpropane derivatives, preparations and uses thereof

Phenylketone carboxylate compounds and pharmaceutical compositions for the prevention and treatment of osteoporosis