ЗАМЕЩЕННЫЕ АЗЕПИНО[4,3-b]ИНДОЛЫ, ФАРМАЦЕВТИЧЕСКАЯКОМПОЗИЦИЯ, СПОСОБ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ

Изобретение относится к новым гидрированным азепино[4,3-b]индолам общей формулы 1, их рацематам, оптическим изомерам, геометрическим изомерам, их фармацевтически приемлемым солям и/или гидратам, которые обладают нейропротекторными, когнитивно-стимулирующими и антигистаминными свойствами и могут найти применение при лечении различных неврологических расстройств, аллергических и аутоиммунных заболеваний, например, для улучшения памяти. В общей формуле 1 пунктирная линия с сопровождающей ее сплошной линией представляет собой одинарную или двойную связь; R1 и R2 независимо друг от друга представляют собой заместители аминогруппы, выбранные из водорода; возможно замещенного C1-C8-алкила, возможно замещенного арилом, 5-6-членным азагетероциклилом; C1-C8-алкоксикарбонила; возможно замещенного фенила; возможно замещенных карбониламино или тиокарбониламино; замещенного ацила; C1-C8-алкилсульфонила; возможно замещенного арилсульфонила; при этом заместители в указанных R1 и R2 независимо выбираются ...

ПРОИЗВОДНЫЕ ГАЛАНТАМИНА И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

Описываются производные галантамина как ингибиторы ацетилхолинэстеразы. В частности, описываются соединения формулы, приведенной в описании, для лечения нарушения памяти, характеризующегося пониженной холинэргической функцией, фармацевтические композиции, содержащие эти соединения, и способы получения и применения этих соединений.

Galanthamin Derivate, ein Verfahren zu ihrer Herstellung und ihre Verwendung als Medikamente

2-amino-4,5,7,8-tetrahydro-6h-thiazolo-or oxazolo(5,4-d) - azepines - as hypotensive, antiphlogistic, sedative and bechic agents

Cpds (I) and their salts. (where R1 is H, 1-4C alkyl opt. substd. by OH, allyl, cycloalkyl, hexahydrobenzyl, phenyl, phenethyl or benzyl opt. substd by 1 or 2 halogen, 1-3-MeO, Cf3 or 1-3C alkyl, R2 is (when X is S) H, 1-5C alkyl, allyl, cycloalkyl, phenyl, benzyl, or phenethyl, and (when X is O) H) are prepd by reacting a hexahydroazepin-4-one with a urea or thiourea in the presence of halogen or a halo hydroazepin-4-one with a urea or thiourea or a 4-alkoxy-tetrahydroazepine with a thiourea in the presence of a halogen or by reducing (I R1 or R2= acyl) by hydroxyalkylating (I R1=He with an epoxide or by diacylating a 6-acylamino deriv. of (I). Thus 1-benzyl-5-bromohexahydro-1H-azepinone-(4)-and thiourea gave (I R1=benzyl R2=N, X=S).

VERFAHREN ZUM HERSTELLEN VON DERIVATEN DES 4a,5,9,10,11,12,-HEXAHYDRO-6H-BENZOFURO[3a,3,2-ef][2]BENZAZEPINS

5-SUBSTITUIERTE 9-CYANMETHYLENDITHIENO (3,4-B:4' 3'-E) -AZEPINE

1,3-DISUBSTITUIERTE HARNSTOFFE UND 2-THIOHARNSTOFFE

VITRONEKTINREZEPTORANTAGONISTEN

PYRAZINE DERIVATIVES

Tricyclic inhibitors of ply (adp-robose) polymerases

Tricyclic inhibitors of poly(adp-ribose)polymerases.

8-substituted benzoazepines as toll-like receptor modulators

Compounds compositions and methods for stimulating neuronal growth and elongation

Tricyclic inhibitors of poly (adp-ribose) polymerases.

Tartrate salts of 5,8,14-triazatetracyclo{10.3.1.0 .0] hexadeca2(11),3,5,7.9-pentaene and pharmaceutical compositions thereof.

The present invention is directed to the tartrate salts of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene: and pharmaceutical compositions thereof. The present invention in particular is directed to the L-tartrate salt, and further to the various polymorphs of the L-tartrate salt, including two distinct anhydrous polymorphs (referred to herein as Forms A and B) and a hydrate polymorph (referred to herein as Form C). In addition, the present invention is also directed to the D-tartrate salt of 5,8,14- triazatetracyclo[10.3.1.02,11.0 4,9]-hexadeca-2 (11),3,5,7,9-pentaene and the various polymorphs thereof; as well as the D,L-tartrate salt thereof and its polymorphs, and the meso-tartrate salt thereof and its polymorphs.

Citrate salt of 5,8,14-triazatetracyclo Ä10.3.02,11.04,9Ü-hexadeca-2 (11),3,5,7,9-pentaene and pharmacetical compositions thereof

Vitronectin receptor antagonists.

Compounds, compositions, and methods for stimulating neuronal growth and elongation

Compounds that inhibit the peptidyl-proly isomerase (rotamase)enzyme activity of the FK-506 binding protein (FKBP)and compositions comprising these compounds are described. The fkbp-inhibiting compounds have a bicyclic [3.3.1], [4.3.1]or polycyclic azaamide nucleus, pharmaceutical compositions containing such compounds help stimulate the outgrowth of neurites in nerve cells and augmenting nerve regeneration. Methods of treating nerve cells with such compositions are useful to promote repair of neuronal damage caused by disease and physical trauma.

Tartrate salts of 5,8,14-triazatetracyclo Ä10.3.1.02,11.04,9Ü-hexadeca-2(11),3,5,7,9-pentaene and pharmacetical compositions thereof

Tricyclic inhibitors of ply (adp-robose) polymerases

Vitronectin receptor antagonists

Use of ivabradine as diagnostic agent in the method of coronary angiography by multislice computed tomography

Citrate salt of 5,8,14-triazatetracycloÄ10.3.1.02,11.04,9Ü- hexadeca2(11),3,5,7,9-pentaene and pharmaceutical compositions thereof

Synthesis process, and crystalline form of 4-ä3-ÄCis-hexahydrocyclopentaÄCÜpyrrol-2(1H)-YLÜpropoxyübenzamide hydrochloride and pharmaceutical compositions containing it.

The citrate salt of 5,8,14-triazatetracyclo 10.3.1.o2,11.o49)-hexadeca-2(11)3,5,7,9-pentaene and pharmaceutical compositions thereof.

Compounds, compositions, and methods for stimulating neuronal growth and elongation.

Tricyclic inhibitors of poly(adp-ribose)polymerases.

(2-thio) ureas, 1,3-disubstituted.

New derivatives of S-alcoyl- (methyl-hexahydro-1-H-azépine) - 1-carbothiolates, their method of preparation.

"Fused benzazepines".

Tartrate salts of 5,8, 14-triazatetracyclo Ä10.3.1.o2,11.o4.9Ü-hexadeca2(11),3,5,7,9-pentaene and pharmaceutical compositions thereof.

Tartrate salts of 5,8,14-triazatetracyclo Ä10.3.1.02,11.04,9Ü-hexadeca-2(11),3,5,7,9-pentaene and pharmacetical compositions thereof

Citrate salt of 5,8,14-triazatetracyclo Ä10.3.02,11.04,9Ü-hexadeca-2 (11),3,5,7,9-pentaene and pharmacetical compositions thereof

Use of ivabradine as diagnostic agent in the method of coronary angiography by multislice computed tomography

Tartrate salts of 5,8,14-triazatetracyclo Ä10.3.1.02,11.04,9Ü-hexadeca-2(11),3,5,7,9-pentaene and pharmacetical compositions thereof

Synthesis process, and crystalline form of 4-ä3-ÄCis-hexahydrocyclopentaÄCÜpyrrol-2(1H)-YLÜpropoxyübenzamide hydrochloride and pharmaceutical compositions containing it.

Tetrahydrobenzazepine derivatives useful as modulators of dopamine d3 receptors (antipsychotic agents)

Vitronectin receptor antagonists

Protease inhibitors

Tricyclic inhibitors of ply (adp-robose) polymerases

Citrate salt of 5,8,14-triazatetracyclo Ä10.3.02,11.04,9Ü-hexadeca-2 (11),3,5,7,9-pentaene and pharmacetical compositions thereof

Use of ivabradine as diagnostic agent in the method of coronary angiography by multislice computed tomography

Synthesis process, and crystalline form of 4-ä3-ÄCis-hexahydrocyclopentaÄCÜpyrrol-2(1H)-YLÜpropoxyübenzamide hydrochloride and pharmaceutical compositions containing it.

Compounds compositions and methods for stimulating neuronal growth and elongation

NEUE TRICYCLISCHE LACTAME

NEUE TRICYCLISCHE LACTAME

PROCEDURES FOR the PRODUCTION OF NEW ONES 2-OXO-HEXAHYDROAZEPIN, - PIPERIDIN AND - PYRROLIDINDERIVATEN

PROCEDURE FOR the PRODUCTION OF NEW DERIVATIVES of the 5-METHYL-11 (BETA ALKYLAMINOATHYL) - (5H) - DIBENZO (B, F) - AZEPINS AND OF ITS SALTS

PROCEDURE FOR the PRODUCTION OF NEW N-SUBSTITUTING 1-AMINO-3-PHENOXY-PROPANOLEN (2) AND YOUR SALTS

USE OF CARBAMAZEPINE AND OXCARBAZEPINE FOR THE TREATMENT OF PARKINSON AND THE PARK IN ON SYNDROMES

3H-2-BENZAZEPINE, INTERMEDIATE PRODUCTS AND PROCEDURES FOR YOUR PRODUCTION, AS WELL AS THESE CONTAINING PREPARATIONS.

NEW CYCLI AMINE DERIVATIVES, THESE CONNECTIONS CONTAINING DRUGS AND PROCEDURES FOR YOUR PRODUCTION.

SULFINYL AND 3BENZAZEPINE SULPHONYL-SUBSTITUTED.

1-SUBSTITUIERTE LAKTAME CONTAINING COMPOSITIONS.

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

6-CHLOR-3-METHYL-2,3,4,5-TETRAHYDRO-1H-3BENZAZEPIN, ITS ADDITION SALTS WITH ACIDS AND ITS USE AS INTERMEDIATE PRODUCT.

5,6-DIHYDRO-11-ALKYLEN-MORPHANTRIDIN-6-ONE, YOUR PRODUCTION AND THESE CONTAINING DRUGS.

PHARMACEUTICAL COMPOSITIONS WITH CONTENT OF 7,8-DIHYDROXY-1 (HYDROXY PHENYL) - 2,3,4,5TETRAHYDRO-1H-3-BENZAZEPIN-DERIVATEN AND OF an BETA-ADRENERGIC BLOCKER.

BENZAZEPINDERIVATE.

NEW INDOLDERIVATE, THEIR PRODUCTION AND USE FOR DRUGS.

2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPINE, PROCEDURE FOR YOUR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS WITH DOPAMINE RECEPTOR BLOCKER ACTIVITY.

PROCEDURE FOR THE PRODUCTION OF OXCARBAZEPIN

TRICYCLI INDOLDERIVATE, PRODUCTION AND APPLICATION AS DRUGS.

MONO BY SULFATES OF NITROGEN-CONTAINING HETERO-CYCLIC POLYPERCARBONSAEUREN.

FLUORINE-SUBSTITUTED DICARBONIC ACIDS AS WELL AS A PROCEDURE FOR YOUR PRODUCTION AND USE

USE OF RILUZOLE FOR THE TREATMENT OF TRAUMA TABLES NEUROLOGICAL DAMAGES

BENZAZEPINDERIVATE, YOUR PRODUCTION AND YOUR USE AS DRUGS.

ANTI-ARRHYTHMIC MEANS.

DOPAMINE SUPPL. EFFECT BENZAZEPINE.

POLYIODIERTE CONNECTIONS, PROCEDURE FOR THEIR PRODUCTION AND DIAGNOSTIC COMPOSITION

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

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

PROCEDURE FOR the PRODUCTION OF NEW N-SUBSTITUTING 1-AMINO-3-PHENOXY-PROPANOLEN (2) AND YOUR SALTS

PROCEDURE FOR THE PRODUCTION OF NEW ACYLAMINOALKYLBENZOLSULFONYLSEMICARBAZIDEN AND THEIR SALTS

Procedure for the production of a new Azepinderivats

Procedure for the production of new 1-Carbamoyl-3-carbamoyloximino-azacycloheptan-2-onen

PROCEDURE FOR THE PRODUCTION OF HYDROXYSAEUREN.

ANNELIERTE AZEPINON AND AZOCINON DERIVATIVES, PROCEDURE FOR YOUR PRODUCTION, THESE CONTAINING MEANS AND YOUR USE, AS WELL AS INTERMEDIATE PRODUCTS WHEN YOUR PRODUCTION.

Procedure for the production of new 5-basisch of substituted 5,6-Dihydro-6-oxomorphanthridine, as well as of acid addition salts of it

Procedure for the production of new 5-basisch more substituted 5.6 Dihydro 6 oxomorphanthridine, as well as of acid addition salts of it

Procedure for the production of new o-substituted 2-Phenyl-imino-1-azacycloheptanen and of their salts

Procedure for the production of new Azepinderivaten and their acid addition salts

Procedure for the production of new 6,11-Diamino-morphanthridinen and their salts

INDOLE DERIVATIVES

CONDENSED PYRAZINE DERIVATIVES

Stabilized protease composition

A composition is provided, which comprises a serine protease; a reversible inhibitor of said serine protease; and a stabilizing agent M having the formula (I): Also provided are uses of the composition as a medicament, and other uses and methods employing its various properties .

Vitronectin receptor antagonists

1,3-DISUBSTITUTED (2-THIO) UREAS

Novel 1,3-disubstituted ureas and 2-thioureas having the formula wherein R1, R2, R3, R6, R7 and R8 represent independently a hydrogen atom, an alkyl radical containing 1 to 4 carbon atoms, an alkenyl radical containing 2 to 4 carbon atoms, an alkylene radical forming together with the carbon atom to which it is attached a cycloalkane ring having 5 or 6 carbon atoms, an aryl radical or a substituted aryl radical, R4 and R5 represent independently a hydrogen atom, an alkyl radical containing 1 or 2 carbon atoms or a phenyl radical, n and q are independently a whole number of from 3 to 7, m and p are independently 0, 1 or 2 and X is an oxygen or a sulfur atom, possess particularly valuable pharmaceutical properties. In particular, the compounds of the invention display a beneficial activity on mnemic processes and a protective activity against aggressions of the hypoxie type; they also display an interesting activity in the field of blood platelet aggregation.

DIBENZOIMIDAZOAZEPINES, -OXAZEPINES AND -THIAZEPINES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

The invention relates to compounds of formula I (I) ¢wherein R1, R2, R3 and R4, which may be the same or different, each represents a hydrogen or halogen atom or a C1 to C6 alkyl or C1 to C6 alkoxy group; R5 and R6, which may be the same or different, each represents a hydrogen atom or a C1 to C6 alkyl or C3 to C6 alkenyl group; or R5 and R6, together with the nitrogen atom to which they are attached, represent a pyrrolidino, piperidino or morpholino group; and X represents an oxygen or sulfur atom or a methylene group! and the tautomeric forms (where R6 represents a hydrogen atom) of formula Ia (Ia) as well as to acid adition salts of compounds of formulae I and Ia and processes for their preparation. The compounds of formulae I and Ia and their physiologically acceptable acid addition salts possess antiallergic, antihistaminic and antiserotonic activity and the invention also releates to pharmaceutical preparations containing these compounds or salts.

1,3-DISUBSTITUTED (2-THIO) UREAS

CHOLINERGIC ENHANCERS WITH IMPROVED BLOOD-BRAIN BARRIER PERMEABILITY FOR THE TREATMENT OF DISEASES ACCOMPANIED BY COGNITIVE IMPAIRMENT

The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g. galanthamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as "pro-drugs", in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. Compounds of this invention may be used as medicaments.

MDM2-BASED MODULATORS OF PROTEOLYSIS AND ASSOCIATED METHODS OF USE

The description relates to MDM2 binding compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the MDM2 E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.

PROCEDURE FOR THE PRODUCTION OF CYCLOHEXANONOXIM.