ГЕТЕРОПОЛИЦИКЛИЧЕСКОЕ СОЕДИНЕНИЕ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ОБЛАДАЮЩАЯ АНТАГОНИСТИЧЕСКОЙ АКТИВНОСТЬЮ В ОТНОШЕНИИ МЕТАБОТРОПНЫХ ГЛЮТАМАТНЫХ РЕЦЕПТОРОВ mGluR ГРУППЫ I

Изобретение относится к области медицинской химии и касается соединений и фармацевтических композиций, которые действуют в качестве антагонистов метаботропных глютаматных рецепторов. 3 н. и 4 з.п. ф-лы, 3 табл.

ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ МЕК И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

Изобретение относится к новым соединениям, включая его разделенные энантиомеры, диастереоизомеры, сольваты, и к фармацевтически приемлемым солям, имеющим формулу: ! ! где Х представляет собой N или CR10; Y представляет собой NR3; R1, R2, R8, R9 и R10 независимо представляют собой водород, гидрокси, галоген, -SR11, -OR3, -NR3R4, C1-С10алкил, С3-С10циклоалкил, С3-С10циклоалкилалкил, арил, арилалкил, гетероарил, гетероарилалкил, гетероциклил или гетероциклилалкил; R7 представляет собой водород, C1-С10алкил, С3-С10циклоалкил, С3-С10циклоалкилалкил, арил, арилалкил, гетероарил, гетероарилалкил, гетероциклил или гетероциклилалкил, где любые из указанных алкильных, циклоалкильных, арильных, арилалкильных, гетероарильных, гетероарилалкильных, гетероциклильных и гетероциклилалкильных фрагментов возможно замещены одной или более чем одной группой, независимо выбранной из оксо (при условии, что она не замещена на ариле или гетероариле), галогена, циано, нитро, SO2NR11R12, -C(O)R11, C(O)OR11, -C(O) ...

ПРОИЗВОДНЫЕ 1,3,4-ОКСАДИАЗОЛСУЛЬФОНАМИДА В КАЧЕСТВЕ ИНГИБИТОРОВ ДЕАЦЕТИЛАЗЫ ГИСТОНОВ 6 И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ИХ

Изобретение относится к новым соединениям формулы I, их стереоизомерам или их фармацевтически приемлемым солям, к их применению для получения терапевтических средств, к фармацевтическим композициям, содержащим их, и к способу лечения опосредованных HDAC6 заболеваний. Технический результат: получены новые соединения, обладающие активностью ингибирования деацетилазы гистонов 6 (HDAC6), которые являются эффективными для предупреждения или лечения заболеваний, опосредуемых HDAC6. 4 н. и 6 з.п. ф-лы, 2 табл., 339 пр.Формула I ...

СПОСОБЫ ПОЛУЧЕНИЯ ЛИНЕЗОЛИДА

... 1. Способ получения линезолида или его фармацевтически приемлемой соли, включающий стадию, выбранную из группы, состоящей из(a) смешивания 4-хлорнитробензола с фтором с получением 3-фтор-4-хлорнитробензола;(b) смешивания 3-фтор-4-галогеннитробензола с морфолином с получением 3-фтор-4-(1-морфолино)нитробензола или его соли;(c) смешивания 3-фтор-4-(1-морфолино)нитробензола с восстановителем с получением 3-фтор-4-(1-морфолино)анилина или его соли;(d) смешивания 3-фтор-4-(1-морфолино)анилина с ацилирующим средством с получением 3-фтор-4-(1-морфолино)фенилизоцианата;(e) смешивания 3-фтор-4-(1-морфолино)фенилизоцианата с оксираном формулыс получением соединения формулыили его соли; где Rпредставляет собой галоген или защищенную аминогруппу; и Rпредставляет собой галоген, аминогруппу или защищенную аминогруппу; и(f) смешивания соединения формулыс CHC(O)SH с получением соединения формулыили его соли;и их комбинацию.2. Способ по п.1, где 3-фтор-4-галогеннитробензол представляет собой 3,4-дифторнитробензол ...

НОВЫЕ СУЛЬФОНИЛАМИНОПИРИМИДИНЫ

Соединения общей формулыгде R- R, R, R, X, Y, Z, m и n имеют указанное в описании значение, могут применяться в качестве лечебных средств, прежде всего для лечения и профилактики состояний, связанных с активностью эндотелия.

Состав для уничтожения нежелательных и регулирования роста полезных растений

DELTA 6, 7-TAXOLEN, ANTINEOPLASTISCHE VERWENDUNG UND DIESE ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSTELLUNGEN

PIPERIDINYL COMPOUNDS

AZOLE DERIVATIVES

Method for recovery of copper from sulfide ore materials using super-fine grinding and medium temperature pressure leaching

Process and intermediates for preparing anti-cancer compounds

Metalloproteinaise inhibitors pharmaceutical compositions containing them and their pharmaceeutical uses and methods and intermediates useful for their preparation

Piperidinyl compounds

Substituted isoquinoline derivatives and their use as anticonvulsants

PYRROLIDINONES

Dibenzyl amine derivatives as CEPT inhibitors

Substituted1-yl)-azolin-2-aryl-1-hetaryl-ethane

Aminopyridine derivatives as selective dopamine D3agonists

Indazole and indolone derivatives and their use aspharmaceuticals

New benzoyl urea derivatives

Piperidine acetic acid derivatives and their use in the treatment of thrombotic disorders

Novel compounds of amino sulfonyl derivatives

Substituted oxazoles and thiozoles derivatives as hppar gamma amd hppar alpha activators

Bicyclic [3.1.0] heteroaryl amides as type I glycine transport inhibitors

An oxindole oxazolidinone as antibacterial agent

Insecticidal 5-substituted-2,4-diaminopyrimidine derivatives.

An insecticidal composition comprising, in admixture with an agriculturally acceptable carrier, an insecticidally effective amount of compound of the formula: whereinr is (a)hydrogen, straight or branched chain alkyl, cycloalkyl,polycycloalkyl, cyano, morpholinly, alkylsilane, arylsilane, phenyl, or substituted-phenyl-phenyl of the formula: ...

Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses, and methods and intermediates useful for their preparation.

The invention relates to compounds of formula (1) wherein: Z is O or S; V is a divalent radical which together wtih C* and N forms a ring having six ring atoms, where each of said ring atoms other than C* and N independently is unsubstituted or substituted by a suitable substituent, and at least one of said other ring atoms is a heteroatom selected from O, N and S and the remainder is carbon atoms; and Ar is an aryl or heteroaryl group; and pharmaceutically acceptable prodrugs, salts and solvates thereof. The invention further relates to pharmaceutically acceptable prodrugs, salts and solvates of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases by administering a compound of formula (1)or a prodrug, salt or solvate therof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, solvates.The invetion still further relates to methods and intermediates useful for ...

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 ...

Metalloproteinase inhibitors, pharmaceutical compositisions containing them and their pharmaceutical uses, and methods and intermediates useful for their preparations.

The invention relates to compounds of formula (1)wherein: z is o or s; v is a divalent radical which together with c* and n forms a ring having six ring atoms, where each of said ring atoms other than c* and n independently is unsubstituted or substituted by a suitable substituent, and at least one of said other ring atoms is a heteroatom selected from o, n and s, and the remainder is carbon atoms; and ar is an aryl or heteroaryl group; and pharmaceutically acceptable prodrugs, salts and solvates thereof. The invention further relates to pharmaceutically acceptable prodrugs, salts and solvates of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases by administering a compound of formula (1)or a prodrug, salt or solvate thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts and solvates. The invention still further relates to methods and intermediates useful ...

Certain 1, 4, 5-Tri-substituted imidazole compounds useful as cytokine.

This invention relates to certain 5-(optionally substituted aryl or heteroaryl)-4-(optionally substituted heteroaryl)-1-(optionally substituted heterocyclyl or heterocyclylalkyl)or -1- optionally substituted alkyl or alkenyl - imidazoles and derivatives thereof. Synthetic processes for the preparation of said tri-substituted imidazoles is described. The aforementioned imidazoles are useful for treating cytokine mediated diseases. The compounds of the invention are incorporated into pharmaceutical compositions for use in treating cytokine related diseases.

Method for recovery of copper from sulfidic ore materials using super-fine grinding and medium temperature pressure leaching

The present invention relates generally to a process for recovering copper and other metal values from metal-containing materials using controlled, super-fine grinding reducing the particle size to less than 25 micrometer and medium temperature (140 -180 °C) pressure leaching. Processes embodying aspects of the present invention may be beneficial for recovering a variety of metals such as copper, gold, silver, nickel, cobalt, molybdenum, rhenium, zinc, uranium, and platinum group metals, from metal-bearing materials, and find particular utility in connection with the extraction of copper from copper sulfide ores and concentrates.

A method of preparing quinazoline derivatives useful as anti-cancer compounds.

A method of preparing quinazoline derivatives useful as anti-cancer compounds.

The present invention relates to methods and intermediates for preparing compounds of the formula 1 and the pharmaceutically acceptable salts and solvates thereof, as well as structurally related compounds, whereinR1, R2 and R15 are as defined herein. The foregoing compounds are useful in the treatment of hyperproliferative disorders, such as cancers, in mammals.

Azole derivatives.

... 2-(2-furyl)-5-[2-(morpholino)ethylamino][1,2,4]triazolo[1,5-a][1,3,5]triazine-7-amine and the pharmaceutically acceptable salts thereof, which are selective a2a adenosine antagonists. Also disclosed are pharmaceutical compositions comprising the compounds and processes for their preparation.

Inhibitors of human immunodeficiency virus replication

Novel compounds

Process and intermediates for preparing anti-cancer compounds

Meta lopro ei na e inh bitor pharmaceutical compositions containing them and their pharmaceutical uses and methods and intermediates useful for their preparation

Method for recovery of copper from sulfide ore materials using super-fine grinding and medium temperature pressure leaching

Intecticidal 5-substituted-2, 4-diaminopyrimidine derivatives

Metalloproteinaise inhibitors pharmaceutical compositions containing them and their pharmaceeutical uses and methods and intermediates useful for their preparation

Piperidinyl compounds

Process and intermediates for preparing anticancer compounds

Aminoheteroaryl compounds as protein kinase inhibitors.

Inhibitors of human immunodeficiency virus replication.

Aminoheteroaryl compounds as protein kinase inhibitors

Manufactoring process of cyclic news imides.

Insecticidal 5-substituted-2, 4-diaminopyrimidine derivatives

Processes and intermediates for preparing anti-cancer compounds.

Oxazolidinone derivatives as antimicrobials.

"Method for preparation of taxol using oxazinone".

Method of preparation of compositions for the treatment of chronic infections of trypanosomiasis.

Dihydropyridylimidates cyclic.

Method for recovery of copper from sulfidic ore materials using super-fine grinding and medium temperature pressure leaching.

Caspase inhibitors containing isoxazoline ring.

Hetero biaryl derivatives as matrix metalloproteinase inhibitors.

Benzimidazolone coumpounds having 5-HT4 receptor agonistic activity.

Certain 1, 4, 5-tri-substituted imidazole compounds useful as cytokine

Aminoheteroaryl compounds as protein kinase inhibitors.

Metalloproteinase inhibitors pharmaceutical compositions containing them and their pharmaceutical uses and methods and intermediates useful for their preparation

Pyridine compounds for the treatment of prostaglandin mediated diseases

Inhibitors of human immunodeficiency virus replication.

Process and intermediates for preparing anticancer compounds

Pyrazine derivatives as sodium channel modulators for the treatment of pain

Estrogen modulators

Oxazolidinones containing oxindoles as antibacterial agents

Indo e com ounds as an i-inf ammatory/an algesic agents

Vitronectin receptor antagonists

Compounds and methods for the treatment or prevention of flavivirus infections

HIV replication inhibiting pyrimidines and triazines.

Compounds having a potentiating effect on the activity of ethoionamide and uses thereof

Heterocyclic compounds as inhibitors of rotamase enyzmes

Intecticidal 5-substituted-2, 4-diaminopyrimidine derivatives

Process and intermediates for preparing anticancer compounds

3-Heterocyclylpropanohydroxamic acid pcp inhibitors

2,4-Diaminopyrimidine compounds useful as immunosupressants

Morpholine derivatives for use as dopamine agonists in the treatment of I.A. sexual dysfunction

3-Heterocyclyl propanohydroxamic acid pcp inhibitors

Cyclopentapyridine and tetrahydroquinoline derivatives

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

Benzoamide derivatives compounds as substance antagonists

Pyrazole derivatives

Azole derivatives

Metalloproteinaise inhibitors pharmaceutical compositions containing them and their pharmaceeutical uses and methods and intermediates useful for their preparation

Novel compounds

Protease inhibitors

Therapeutic amides

5-Substituted-2-arylpyridines as CRF 1 modulators.

Method for recovery of copper from sulfide ore materials using super-fine grinding and medium temperature pressure leaching

Meta lopro ei na e inh bitor pharmaceutical compositions containing them and their pharmaceutical uses and methods and intermediates useful for their preparation

Herbicidal isoyazoline compounds

Process and intermediates for preparing anti-cancer compounds

Substituted morpholine compounds for the treatmentof central nervous system disorders

NPY antagonists, preparation and use

Hydroxamates as histone deacetylase inhibitors and pharmaceutical formulations containing them

7-Fluro-1,3-dihydro-indol-2-one oxazolidinones as antibacterial agents

Aminoheteroaryl compounds as protein kinase inhibitors.

Aminoheteroaryl compounds as protein kinase inhibitors.