МОДУЛЯТОРЫ 5НТ2С РЕЦЕПТОРА

... 1. Соединение, представленное формулой (I) где R1 является Н или С1-8 алкилом; R2 является С1-8 алкилом, -СН2 -О-С1-8 алкилом, -С(=О)-О-С1-8 алкилом, -С(=О)-NH-С1-8 алкилом или СН2ОН; R2a является Н; или R2 и R2a вместе образуют –СН2-СН2-; R3 является галогеном, пергалогеналкилом, CN, SR5, NHR5, N(R5)2, арилом или гетероарилом, где указанный арил может необязательно иметь до двух заместителей, выбранных из С1-8 алкила, галогена пергалогеналкила и алкокси, и указанный гетероарил может необязательно иметь до двух заместителей, выбранных из галогена и С1-8 алкила; R4 является Н, галогеном, пергалогеналкилом, CN, SR5, NHR5, N(R5)2, арилом или гетероарилом, где указанный арил может необязательно иметь до двух заместителей, выбранных из С1-8 алкила, галогена, пергалогеналкила и алкокси, и указанный гетероарил может необязательно иметь до двух заместителей, выбранных из галогена и С1-8 алкила; или R3 и R4 вместе с атомами, к которым они присоединены, могут образовывать 5- или 6-членное гетероциклическое ...

СПОСОБ ПОЛУЧЕНИЯ БЕНАЗЕПРИЛА СПОСОБ ПОЛУЧЕНИЯ БЕНАЗЕПРИЛА

... 1. Способ получения трифторметансульфоната этилового эфира (R)-2-гидрокси-4-фенилмасляной кислоты формулы (I), включающий взаимодействие этилового эфира (R)-2-гидрокси-4-фенилмасляной кислоты формулы (III) с ангидридом трифторметансульфоновой кислоты формулы (IV) в инертном растворителе в присутствии основания и его очистку путем пропускания через колонку. 2. Способ по п.1, отличающийся тем, что инертный растворитель выбирают из группы, состоящей из метиленхлорида, хлороформа, четыреххлористого углерода, толуола, бензола и гексана. 3. Способ по п.1, отличающийся тем, что основание выбирают из группы, состоящей из карбоната калия, карбоната натрия, бикарбоната натрия, триэтиламина и пиридина. 4. Способ по п.3, отличающийся тем, что основание представляет собой пиридин. 5. Способ получения гидрохлорида беназеприла формулы (II) включающий стадии: (i) обработки этилового эфира (R)-2-гидрокси-4-фенилмасляной кислоты формулы (III) ангидридом трифторметансульфоновой кислоты формулы (IV) в инертном ...

SS-LACTAM-ANTIBIOTIKA, VERFAHREN ZUR HERSTELLUNG UND IHRE VERWENDUNG ALS ARZNEIMITTEL

PIPERIDINYL COMPOUNDS

PSYCHOTROPIC POLYCYCLIC IMIDES

Thiazolo(2,3-b)benzo (and azobenzo) thiazole derivatives, process for their preparation and pharmaceutical compositions containing them

Novel 2-substituted-3-hydroxythiazolo?2,3-b!benzo-(and azabenzo)thiazolium salts, the mesoionic didehydro derivatives thereof and related compounds are disclosed, as well as the use thereof as modulators of the immune response.

PENICILLIN COMPOUNDS AND A METHOD OF SYNTHESISING SAME

... 1312030 Penicillin compounds INSTYTUT PRZEMYSLU FARMACEUTYZNEGO 17 Dec 1971 [22 Dec 1970] 58618/71 Heading C2A [Also in Division C3] The invention comprises penicillin compounds of the general Formula I wherein R represents a substituted or an unsubstituted alkyl group, a cycloalkyl group, an aryl group, an aralkyl group, a heterocyclic group or a hydrogen atom; R1 and R2, the same or different, represent a substituted or an unsubstituted alkyl group, a cycloalkyl group, an aryl group, an aralkyl group or a hydrogen atom or R1 and E2 together form a heterocyclic group; and X represents an hydroxyl group or an OR3 group wherein R3 represents a substituted silyl group, a substituted or an unsubstituted alkyl group, an aryl group, an aralkyl group or a cycloalkyl group. The group R3 may be selected from trimethylsilyl, substituted dimethylsilyl, methyl, ethyl, propyl, butyl, benzyl, #,#,#-trichlorethyl, methoxymethyl, phenacyl, ...

Piperidinyl compounds

Dibenzyl amine derivatives as CEPT inhibitors

2-Methoxyphenylpi perazine derivatives

Piperidinyl compounds

Novel piperidinyl compounds of formula 1 in which x and y are independently selected from hydrogen, halogen and ci-6 alkoxy, r1 is selected from five- and six- membered heteroaryl rings containing fro 1-3 heteroatoms selected from nitrogen, oxygen, and sulfur, and benz derivatives thereof, which may bear 1-2 substituents selected from c1-6 alkyl, hydroxy, c1-6 alkoxy which may bear a trifluoromethyl group, c1-6 alkoxycarbonyl, c1-6 hydroxyalkyl, benzloxy, halo, c1-3 alkylaminocarbonylc1-3alkyl, aminocarbonyl having the formula: conrcrd wherein rc and rd are independently selected from hydrogen, 2-pyrrolidinyl, and c1-6 alkyl or wherein rc and rd together with the nitrogen atom to which each is attached form a 5- or 6- membered heterocyclic ring in which said nitrogen is the only heteroatom, res(o)n, rfnh, and fgs wherein re and rf are independently selected from hydrogen and c1-6 alkyl and n is 0, 1 or 2 and rg is selected from c1-3 alkylcarbonylaminophenyl and di(c1-3)alkylamino(c1-6)alkyl ...

New oxabispidine compounds useful in the treatmentof cardiac arrhythmias.

New oxabispidine compounds useful in the treatment of cardiac arrhythmias

Piperidinyl compounds

Pharmaceutical composition of isoniazid.

Stable copper(i) complexes and methods related thereto

New oxabispidine compounds useful in the treatmentof cardiac arrhythmias.

New oxabispidine compounds useful in the treatment of cardiac arrhythmias

Pharmaceutical composition of isoniazid.

New oxabispidine compounds useful in the treatment of cardiac arrhythmias

Bicyclic pyrazolyl and imidazolyl compounds and uses thereof.

Pharmaceutical composition of isoniazid.

DEALKYLIERTE DERIVATIVES OF PYRROLO (2.1 - B) BENZOTHIAZEPINEN WITH ATYPICAL ANTIPSYCHOTI EFFECT

PROCEDURE FOR THE PRODUCTION OF NEW DERIVATIVES OF

MEDICAL USE OF ZWITTERION CONNECTIONS AS MODULATORS OF THE CFTR - CHANNEL

PYRANO, PIPERIDINO, AND THIOPYRANO DERIVATIVES AND METHOD FOR USE

PYRIMIDIN-4-ONE OF DERIVATIVES, PROCEDURES FOR ITS PRODUCTION AND IT CONTAINING COMPOSITIONS

PHOTOGRAPHIC SILVER HALIDE MATERIAL CONTAINING A METHINFARBSTOFF

PROCEDURE FOR the PRODUCTION OF n (2-ACETYL-4,6DIMETHYLPHENYL) - 3-ÄÄ (3.4 DIMETHYL-5

NEUE TRICYCLISCHE LACTAME

NEUE TRICYCLISCHE LACTAME

PROCEDURE FOR THE PRODUCTION OF NEW SUBSTITUTED CEPH-3-EMEN AND CEPH-3-EM-SULFOXYDEN

PROCEDURE FOR THE PRODUCTION OF NEW ISOTHIAZOLO ISOCHINOLIN DERIVATIVES AND YOUR SALTS

PROCEDURE FOR the PRODUCTION of NEW 4 (4-PIPERIDYLIDEN) - 4H-BENZO (4,5) CYCLOHEPTA (1,2-B) THIOPHEN DERIVATIVES AND YOUR SOUR ADDITION SALTS

PROCEDURE FOR the PRODUCTION OF OXAZINO (5,6-C) - 1,2-BENZOTHIAZIN-6,6-DIOXID

ORGANIC COMPOUNDS

ORGANIC COMPOUNDS

PROCEDURE FOR THE PRODUCTION OF NEW ONE, TRICYCLI CONDENSED IMIDAZOL DERIVATIVES

PROCEDURE FOR THE PRODUCTION OF NEW THIADIA ZOLO AND THIAZOLO PYRIMIDIN CARBONIC ACIDS, - ESTERS AND - SALTS AND OF THEIR SALTS

PROCEDURE FOR the PRODUCTION OF NEW ONE 1,3-THIAZOLOISOCHINOLIN-DERIVATEN AND YOUR SALTS

PROCEDURE FOR the PRODUCTION OF NEW ONE 1 (HYDROXYMETHYL) - 1,6,7,11B-TETRAHYDRO-2H, 4H (1,3) THIAZINO (4,3-A) ISOCHINO LINDERIVATEN AS WELL AS OF THEIR ACID ADDITION SALTS AND QUATERNAEREN SALTS

PROCEDURE FOR THE PRODUCTION OF THIAZOLINAZETIDINONEN

THIAZOLO (2,3-B) BENZO (AND AZABENZO) THIAZOLDERIVATE, PROCEDURE FOR YOUR PRODUCTION AND IT ABSTENTION PHARMACEUTICAL COMPOSITIONS.

TRICYCLI PYRIDONDERIVATE.

BETA LACTAM ANTIBIOTICS, PROCEDURES FOR THE PRODUCTION AND YOUR USE AS DRUGS.

NEW 4,5-G (A) EPOXYMORPHINAN-6-SPIRO-2' (4 ' KARBOXY-1',3' THIAZOLIDIN) - DESCENDANTS.

SUBSTITUTED HEXAHYDROARYLCHINOLIZINE.

PROCEDURE FOR THE ISOLATION OF LEVAMISOL OF TETRAMISOL.

UNTIL (2,5-DITHIO - 1,3,4-THIADIAZOL> AND PROCEDURE FOR ITS PRODUCTION.

CONDENSED PYRIMIDINDERIVATE, PROCEDURES AND INTERMEDIATE PRODUCTS TO YOUR PRODUCTION AND THESE CONTAINING PHARMACEUTICAL PREPARATIONS.

TRIAZOLOBENZAZEPINE, PROCEDURE AND INTERMEDIATE PRODUCTS FOR THEIR PRODUCTION AND THESE CONTAINING DRUGS.

CONDENSED HETERO-CYCLIC CONNECTIONS.

IMIDAZOTHIADIAZOLALKENCARBONSAEUREAMIDE, NEW INTERMEDIATE PRODUCTS TO YOUR PRODUCTION, YOUR PRODUCTION AND YOUR USE IN DRUGS.

5H-1,3,4-THIAZOL (3,2-A>PYRIMIDIN-5-ON-DERIVATE AND THIS CONTAINING FUNGICIDES PREPARATIONS.

PROCEDURE FOR THE PRODUCTION OF TETRAMISOL.

CONDENSED DIHYDROXYCHINOXALINE AND YOUR USE AS GLUTAMATANTAGONISTEN.

SPIRO ISOCHINOLIN PYRROLIDIN TETRONE AND SIMILAR ONE OF IT, USABLE AS ALDOSEREDUKTASEINHIBITOREN.

NEW TRICYCLIC AMINO AND NITRO CONNECTIONS WITH ACE RESTRAINING CHARACTERISTICS

2,3-DIHYDRO-1H-INDOL-DERIVATE AND INTERMEDIATE PRODUCTS FOR it, PROCEDURES FOR THEIR PRODUCTION, THESE DERIVATIVES ABSTENTIONS PHARMACEUTICAL COMPOSITIONS AND YOUR PRODUCTION.

THIAZASPIRANDERIVATE, PROCEDURE FOR YOUR PRODUCTION AND DRUG.

TRICYCLI BENZOTRIAZOLE, PROCEDURE FOR YOUR PRODUCTION AS WELL AS DRUG.

SPIRO PYRROLIDIN-2,5-DIONE AND PROCEDURE FOR YOUR PRODUCTION.

ASYMMETRICAL DIHYDRO DITHIAZINE ONES, PROCEDURES FOR YOUR PRODUCTION AND YOUR USE AS SMELLING AND TASTE MATERIALS.

CHINOLINE USEFUL AS ANTI-ALLERGY MEANS.

NEW N-ALKOXY NALKYLSULFONYLAMINOSULFONYLHARNSTOFFE, AND NEW ONE (PYRIMIDO) TRIAZINO THIATRIAZINOXIDE ONE AS PRE-PRODUCTS.

PROCEDURE FOR RINGOEFFNUNG OF IN ACCORDANCE WITH DICYANOEPOXYDEN AND CONNECTIONS, THE BY THIS PROCEDURE RECEIVING.

OXODIAZINVERBINDUNGEN.

PHENYLETHYLTHIAZOLDERIVATE, YOUR PRODUCTION AND YOUR APPLICATION IN THE THERAPEUTIK.

OXAZINOBENZOTHIAZIN-6,6-DIOXIDEDERIVATE, YOUR PRODUCTION AND APPLICATION AS DRUGS.

Procedure for the production of new Azepin derivatives and their acid addition salts

Procedure for the production of new Thiazolinazetidinonen

Procedure for the production of new Azepin derivatives and their acid addition salts

Procedure for the production of new 2 (5-Nitro-2-furyl) - thieno [3,2-d] pyrimidinen and their acid addition salts

PROCEDURE FOR THE PRODUCTION OF NEW IMIDAZOLDERIVATE AND YOUR SALTS

TETRAHYDROPYRIDINYL SUBSTITUTED TRICYCLI DERIVATIVES WITH DOPAMINE OF ANTAGONISTIC EFFECT.

Procedure for the production of new Benzodiazepinverbindungen

5HT2C-REZEPTOR-MODULATOREN

DEALKYLIERTE DERIVATIVES OF PYRROLO (2.1 - B) BENZOTHIAZEPINEN WITH ATYPICAL ANTIPSYCHOTI EFFECT

DEALKYLIERTE DERIVATIVES OF PYRROLO (2.1 - B) BENZOTHIAZEPINEN WITH ATYPICAL ANTIPSYCHOTI EFFECT

DEALKYLIERTE DERIVATIVES OF PYRROLO (2.1 - B) BENZOTHIAZEPINEN WITH ATYPICAL ANTIPSYCHOTI EFFECT

DEALKYLIERTE DERIVATIVES OF PYRROLO (2.1 - B) BENZOTHIAZEPINEN WITH ATYPICAL ANTIPSYCHOTI EFFECT

DEALKYLIERTE DERIVATIVES OF PYRROLO (2.1 - B) BENZOTHIAZEPINEN WITH ATYPICAL ANTIPSYCHOTI EFFECT

DEALKYLIERTE DERIVATIVES OF PYRROLO (2.1 - B) BENZOTHIAZEPINEN WITH ATYPICAL ANTIPSYCHOTI EFFECT

DEALKYLIERTE DERIVATIVES OF PYRROLO (2.1 - B) BENZOTHIAZEPINEN WITH ATYPICAL ANTIPSYCHOTI EFFECT

DEALKYLIERTE DERIVATIVES OF PYRROLO (2.1 - B) BENZOTHIAZEPINEN WITH ATYPICAL ANTIPSYCHOTI EFFECT

DEALKYLIERTE DERIVATIVES OF PYRROLO (2.1 - B) BENZOTHIAZEPINEN WITH ATYPICAL ANTIPSYCHOTI EFFECT

DEALKYLIERTE DERIVATIVES OF PYRROLO (2.1 - B) BENZOTHIAZEPINEN WITH ATYPICAL ANTIPSYCHOTI EFFECT

DEALKYLIERTE DERIVATIVES OF PYRROLO (2.1 - B) BENZOTHIAZEPINEN WITH ATYPICAL ANTIPSYCHOTI EFFECT

SPIROTETRATHIOCARBAMATES AND SPIROOXOTHIOCARBAMATES

Dealkylated derivatives of pyrrolo[2,1-b]benzothiazepines with atypical antipsychotic activity

Tricyclic compounds and methds of making and using same

The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

Gamma secretase modulators

TRIAZINE DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS

... [0183] The invention provides for Triazine derivatives and their use to modulate protein kinase activity in a variety of conditions and diseases.

CYCLIC PRODRUGS OF ANTI-INFLAMMATORY OXICAMS WHICH ARE 1,3-OXAZINO 5,6-C 1,2-BENZOTHIAZINES

1,4-DIHYDRO-4-OXO-1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACIDS

BICYCLIC BENZENOID ALKYLENE AMINO THIENO(3,4-D)ISOTHIAZOLE ETHERS AND THIO-ETHERS, AND THEIR PHARMACEUTICAL USES

BICYCLIC PYRIMIDIN-5-ONE DERIVATIVES

PROCEDURE FOR MANUFACTURING NEW ONE 1,3-THIAZOLOISOCHINOLINDERIVATEN.