ОКСАЗОЛИДИНОНЫ, ИХ СОЛИ, СПОСОБ ИХ ПОЛУЧЕНИЯ, ФАРМАЦЕВТИЧЕСКИЙ ПРЕПАРАТ И СПОСОБ ЕГО ПОЛУЧЕНИЯ

Изобретение относится к новым производным оксазолидинонов общей формулы (I), приведенной в описании, а также их соли. Способ получения соединения общей формулы (I) заключается в том, что соединения формулы (I), где R1 - фенил, замещенный CN-группой, превращают в соединения формулы (I), где R1 - фенил, замещенный амидиновой группой, Y имеет значения, указанные в п. 1. Фармацевтический препарат, обладающий ингибирующей активностью связывания фибриногена, содержащий соединения формулы (I) и фармацевтически приемлемый носитель, а также способ его получения. Данные соединения могут использоваться для лечения тромбозов, инфаркта миакарда, воспалений, опухолей. 4 с. и 1 з.п. ф-лы, 1 табл.

Fused benzoxazepinones as ion modulators

Fused benzoxazepinones as ion modulators

Fused benzoxazepinones as ion modulators

HETERO-CYCLIC CONNECTIONS.

4(3)SUBSTITUTED-4(3)-AMINOMETHYL-(THIO)PYRAN OR -PIPERIDINE DERIVATIVES (=GABAPENTIN ANALOGUES), THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

Novel amines of formulas (1D) and (1E), or a pharmaceutically acceptable salt thereof, wherein: n is an integer of from 0 to 2; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; and X is -O-, -S-, -S(O)-, -S(O)2-, or NR'1 wherein R'1 is hydrogen, straight or branched alkyl of from 1 to 6 carbons, or benzyl, -C(O)R'2 wherein R'2 is straight or branched alkyl of 1 to 6 carbons, benzyl or phenyl or -CO2R'3 wherein R'3 is straight or branched alkyl of from 1 to 6 carbons, or benzyl wherein the benzyl or phenyl groups can be unsubstituted or substituted by from 1 to 3 substituents selected from halogen, trifluoromethyl, and nitro, are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS.

КОНДЕНСИРОВАННЫЕ ГЕТЕРОЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ МОДУЛЯТОРОВ ИОННЫХ КАНАЛОВ

Изобретение относится к соединениям, представляющим собой ингибиторы натриевого канала, и к их применению в лечении различных болезненных состояний, включая сердечно-сосудистые заболевания и диабет. Согласно конкретным вариантам реализации структура соединений согласно настоящему изобретению представлена формулой II где R2, R3, R4, R10, R17, n и m такие, как описано в настоящем документе, а также к способам получения и применения соединений согласно настоящему изобретению и к фармацевтическим композициям, содержащим указанные соединения.

CEPHEM COMPOUNDS, THEIR PRODUCTION AND USE

CONDENSED HETEROCYCLIC COMPOUNDS AS MODULATORS OF ION CHANNELS

Конденсированные соединения бензоксазепинонов в качестве модуляторов ионных каналов

Настоящее изобретение относится к новым соединениям, которые являются ингибиторами натриевых каналов и к их использованию в лечении различных болезненных состояний, в том числе сердечно-сосудистых заболеваний и диабета. В конкретных вариантах осуществления структура соединений представлена формулой I: I где Z1, Z2, Z3, Z4, X, Y, R2, R3 и R4 таковы, как определены в описании, для способов получения и использования соединений и для фармацевтических композиций их содержащих. П. формулы: 67 ...

FUSED BENZOXAZEPINONES AS ION CHANNEL MODULATORS

HETEROAROMATIC COMPOUNDS, PROCESS FOR PREPARING THE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, USES AND METHOD OF TREATING THE ACUTE CHRONIC PAIN

Insecticidal heterocyclic compounds

Insecticidal heterocyclic compounds of the formulaered or six-membered heteroaryl group containing one to three hetero atoms selected from the group consisting of S, O and N, said heteroaryl group being unsubstituted or substituted by a halogen atom or C1-4 alkyl group, Z represents a three-membered straight chain, each member being selected from the group consisting of CH2-, O, S and N-R2 with at least one of said three members being O, S or N-R2, E represents CH2, O, S or N-R2, wherein R2 represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group or the group wherein R3 represents a hydrogen atom or halogen atom, X represents CH or N, Y represents a nitro group or cyano group, and R1 represents a hydrogen atom or methyl group.

SUBSTITUTED 5 (2 ((2-ARYL-2 HYDROXYETHYL) AMINO) PROPYL>-1,3-BENZODIOXOLE

((CYCLO) ALKYL SUBSTITUTED) - .GAMMA. - AMINOBUTYRIC ACID OF DERIVATIVES (=GABA ANALOGUES), THEIR PRODUCTION AND THEIR USE WITH THE TREATMENT OF NEUROLOGICAL ILLNESSES

SYNTHESIS OF EPOTHILONEN, INTERMEDIATE PRODUCTS OF IT, ANALOGUES AND YOUR USE

Fused benzoxazepinones as ion channel modulators

The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula 1: wherein Z1, Z2 , Z3, Z4 , X, Y, R2' R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

BENZOIC ACID COMPOUND AND USE THEREOF AS MEDICINE

Benzoic acid compounds of the formula (I) wherein each symbol is as defined in the specification, optical isomers thereof and pharmaceutically acceptable salts thereof; pharmaceutical composition comprising this compound and pharmaceutically acceptable additive; and serotonin 4 receptor agonists, gastrointestinal prokinetic agents and therapeutic agents for various gastrointestinal diseases, which comprise this compound as active ingredient. The compounds of the present invention selectively activate serotonin 4 receptor, and are useful medications for the prophylaxis and treatment of various gastrointestinal diseases (e.g., delayed gastric emptying, indigestion, meteorism, reflux esophagitis, abdominal indefinite complaint, intestinal pseudoileus constipation, acute or chronic gastritis, gastric or duodenal ulcer, Crohn's disease, non-ulcer dyspepsia, ulcerative colitis, postgastrectomy syndrome, postoperative digestive function failure, gastrointestinal injury due to gastric neurosis ...

Производные бензо[f][1,4]оксазепин-5-онов в качестве модуляторов ионных каналов

Настоящее изобретение относится к новым соединениям, которые являются ингибиторами натриевых каналов и к их использованию в лечении различных болезненных состояний, в том числе сердечно-сосудистых заболеваний и диабета. Структура заявленных соединений представлена формулой II: где R2, R3, R4, R10, R17 , m и n определены в описании. Соединения функционируют как блокаторы натриевых каналов позднего тока. П. формулы: 16 ...

CONDENSED HETEROCYCLIC COMPOUNDS AS MODULATORS OF ION CHANNELS

Производные бензо[f][1,4]оксазепин-5-онов в качестве модуляторов ионных каналов

Настоящее изобретение относится к новым соединениям, которые являются ингибиторами натриевых каналов и к их использованию в лечении различных болезненных состояний, в том числе сердечно-сосудистых заболеваний и диабета. Структура заявленных соединений представлена формулой II: где R2, R3, R4, R10, R17 , m и n определены в описании. Соединения функционируют как блокаторы натриевых каналов позднего тока. П. формулы: 16 ...

SYNTHESIS OF EPOTHILONES INTERMEDIATES THERETO AND ANALOGUES THEREOF

The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula(I).

Insecticidal heterocyclic compounds

Insecticidal heterocyclic compounds of the formula см. иллюстрацию в PDF-документе wherein A represents a five-membered or six-membered heteroaryl group containing one to three hetero atoms selected from the group consisting of S, O and N, said heteroaryl group being unsubstituted or substituted by a halogen atom or C1-4 alkyl group, Z represents a three-membered straight chain, each member being selected from the group consisting of CH2 --, O, S and N--R2 with at least one of said three members being O, S or N--R2, E represents CH2, O, S or N--R2 wherein R2 represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group or the group см. иллюстрацию в PDF-документе wherein R3 represents a hydrogen atom or halogen atom, X represents CH or N, Y represents a nitro group or cyano group, and R1 represents a hydrogen atom or methyl group.

CEPHEM COMPOUNDS, THEIR PRODUCTION AND USE

HYDROXYISOXAZOLINES AND DERIVATIVES THEREOF

((CYCLO)ALKYL SUBSTITUIERTE)-.GAMMA.-AMINOBUTTERSÄURE DERIVATE (=GABA ANALOGA), DEREN HERSTELLUNG UND DEREN VERWENDUNG BEI DER BEHANDLUNG VON NEUROLOGISCHEN ERKRANKUNGEN

SUBSTITUTED 1-PHENYL-OXAZOLIDIN-2-ON DERIVATIVES, THEIR PRODUCTION AND THEIR USE AS an ADHESION RECEPTOR ANTAGONIST

1-SUBSTITUIERTE-1-AMINOMETHYL-CYCLOALKAN of DERIVATIVES (= GABAPENTIN ANALOGUES), THEIR PRODUCTION AND THEIR USE WITH the TREATMENT OF NEUROLOGICAL ILLNESSES

SYNTHESIS OF EPOTHILONES, INTERMEDIATES THERETO, ANALOGUES AND USES THEREOF

... ²²²The present invention provides compounds of formula (I): as described ²generally and in classes and subclasses herein. The present invention ²additionally provides pharmaceutical compositions comprising compounds of ²formula (I) and provides methods of treating cancer comprising administering a ²compound of formula (I).² ...

SUBSTITUTED 5-(2-((2-ARYL-2-HYDROXYETHYL)AMINO)PROPYL)-1,3-BENZODIOXOLES

... 30,725 Title: SUBSTITUTED 5-(2-((2-ARYL-2-HYDROXYETHYL) AMINO)PROPYL)-1,3-HENZODIOXOLES The present invention relates to novel 1,3-benzodioxole compounds which have antidiabetic and/or anti-hyperglycemic properties in mammals. More particularly it relates to novel substituted 5-(2-((2-aryl-2-hydroxyethyl)amino)propyl)-1,3-benzodi-oxoles. The present invention also relates to pharmaceutical compositions comprising these compounds, methods for the preparation of these compounds, as well as methods for the use of these compounds in treating diabetes and/or hyperglycemia and/or obesity in mammals.

SYNTHESIS OF EPOTHILONES, INTERMEDIATES THERETO, ANALOGUES AND USES THEREOF

BENZOIC ACID COMPOUND AND USE THEREOF AS MEDICINE

A benzoic acid compound represented by general formula (I) (wherein each symbol is as defined in the specification); an optical isomer or pharmaceutically acceptable salt thereof; a medicinal composition comprising the compound and pharmaceutically acceptable excipients; and a serotonin 4 receptor agonist, digestive function ameliorant, and digestive disease remedy, each containing the compound as the active ingredient. This compound has a selective agonism against serotonin 4 receptors and is useful as medicines for preventing and treating digestive diseases (e.g., delayed gastric excretion, maldigestion, tympanism, reflux esophagitis, abdominal unidentified complaint, pseudoileus, constipation, acute and chronic gastrites, gastroduodenal ulcer, Crohn's disease, nonulcer dyspepsia, ulcerous colitis, postgastrectomy syndrome, postanesthetic dysfunction of digestive system, gastroptosis, gastrointestinal disorder caused by diabetes or the like, and irritable bowel syndrome), central nervous ...

Adhesion-receptor antagonists

Novel compounds of the formula I in which R1, X and Y have the meanings given in Patent Claim 1, and their salts inhibit the binding of fibrinogen to the fibrinogen receptor and can be used for the treatment of thromboses, apoplexy, cardiac infarcts, inflammations, arteriosclerosis, osteoporosis and tumours.

Способ получения диглицидилбензимидазолидонов

Heterocyclische Verbindungen.

PIPERAZINYLMETHYL-1,2,4-TRIAZOLYLMETHYLCARBINOLE.

1-substituted-1-aminomethyl-cycloalkane derivatives (=gabapentin analogues), their preparation and their use in the treatment of neurological disorders

LINKED HETEROCYCLIC COMPOUNDS

PIPERAZINYLMETHYL-1,2,4-TRIAZOLYLMETHYL CARBINOLS

1,2-benzoxathiin and thiepin 2,2-dioxide herbicides

HYDROXYISOXAZOLINES AND DERIVATIVES THEREOF

The present disclosure relates to the use of hydroxyisoxazolines and derivatives thereof as fungicide. It also relates to new hydroxyisoxazolines derivatives, their use as fungicide and compositions comprising thereof.

ADHESION RECEPTOR ANTAGONISTS

Novel compounds of the formula I I in which R1, X and Y have the meanings given in Patent Claim 1, and their salts, inhibit the binding of fibrinogen to the fibrinogen receptor and can be used for treating thromboses, stroke, cardiac infarction, inflammations, arteriosclerosis, osteoporosis and tumours.

ADHESION RECEPTOR ANTAGONISTS

Novel compounds of the formula I (see formula I) in which R1, X and Y have the meanings given in Patent Claim 1, and their salts, inhibit the binding of fibrinogen to the fibrinogen receptor and can be used for treating thromboses, stroke, cardiac infarction, inflam- mations, arteriosclerosis, osteoporosis and tumours.

4(3)SUBSTITUTED-4(3)-AMINOMETHYL-(THIO)PYRAN OR -PIPERIDINE DERIVATIVES (=GABAPENTIN ANALOGUES), THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

Novel amines of formulas (1D) and (1E), or a pharmaceutically acceptable sal t thereof, wherein: n is an integer of from 0 to 2; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; and X is -O-, -S-, -S(O)-, -S(O)2-, or NR'1 wherein R'1 is hydrogen, straight or branched alkyl of from 1 to 6 carbons, or benzyl, -C(O)R'2 wherein R'2 is straight or branched alkyl of 1 to 6 carbons, benzyl or phenyl or -CO2R'3 wherein R'3 is straight or branched alkyl of from 1 to 6 carbons, or benzyl wherein the benzyl or phenyl groups can be unsubstituted or substituted by from 1 to 3 substituents selected from halogen, trifluoromethyl, and nitro, are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS.

FUSED BENZOXAZEPINONES AS ION CHANNEL MODULATORS

The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

Heterocyclic compounds

Novel insecticides of the formula см. иллюстрацию в PDF-документе in which n is 0 or 1, X is S, O, см. иллюстрацию в PDF-документе Y is N or см. иллюстрацию в PDF-документе Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R9 variously represent hydrogen or specified organic radicals.

((CYCLO)ALKYL SUBSTITUIERTE)-.GAMMA.-AMINOBUTTERSÄURE DERIVATE (=GABA ANALOGA), DEREN HERSTELLUNG UND DEREN VERWENDUNG BEI DER BEHANDLUNG VON NEUROLOGISCHEN ERKRANKUNGEN

SYNTHESIS OF EPOTHILONES INTERMEDIATES THERETO AND ANALOGUES THEREOF

SUBSTITUTED 5-(2-((2-ARYL-2-HYDROXYETHYL)AMINO)PROPYL)-1,3-BENZODIOXOLES

((CYCLO)ALKYL SUBSTITUTED)-GAMMA-AMINOBUTYRIC ACID DERIVATIVES (=GABA ANALOGUES), THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

Novel amines of formulas (1A) and (1B) are disclosed and are useful as agent s in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS. Processes for the preparation and intermediates useful in the preparation are also disclosed.

METHOD OF INCREASING LEAN MEAT IN EDIBLE ANIMALS

DERIVATIVES OF 1-SUBSTITUÍDO-1-AMINOMETIL-CICLOALCANO (=ANÁLOGOS OF GABAPENTINA), ITS PREPARATION AND ITS USE IN the TREATMENT OF NEUROLOGICAL RIOTS

NOVEL LAPACHONE COMPOUNDS AND METHODS OF USE THEREOF

The invention provides lapachone analogs and derivatives as well as methods of use thereof. These compounds can be used in pharmaceutical compositions for the treatment or prevention of cell proliferation disorders. These compounds can also be used in the treatment or prevention of cancer or precancerous conditions.

ГЕТЕРОЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ, ОБЛАДАЮЩИЕ ИНГИБИРУЮЩЕЙ АКТИВНОСТЬЮ ПО ОТНОШЕНИЮ К 11β-ГИДРОКСИСТЕРОИДДЕГИДРОГЕНАЗЕ 1 ТИПА

Изобретение относится к соединению, представленному формулой (I), его фармацевтически приемлемым солям или сольватам, в которой R1 представляет собой необязательно замещенный алкил или тому подобное, R2 представляет собой группу формулы: -Y-R5, где Y представляет собой -O- или S; R5 представляет собой замещенный алкил (заместитель представляет собой необязательно замещенный циклоалкил или тому подобное), разветвленный алкил или тому подобное; R4 представляет собой водород или С1-10алкил; R3 представляет собой группу формулы: -C(=O)-Z-R6, где Z представляет собой -NR7- или -NR7-W-; R6 представляет собой необязательно замещенный циклоалкил или тому подобное; R7 представляет собой водород или С1-10алкил, W представляет собой C1-10алкилен; Х представляет собой =N- при условии, что исключаются соединения, в которых R2 представляет собой 2-(4-морфолино)этокси, 2-, 3- или 4-пиридилметокси, 1-метилпиперидинил-2-метокси, бензилокси или 4-замещенный бензилокси; и R3 представляет собой N-(1-адамантил ...

Fused benzoxazepinones as ion channel modulators

The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula 1: wherein Z1, Z2 , Z3, Z4 , X, Y, R2' R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

CEPHEM COMPOUNDS, THEIR PRODUCTION AND USE

HUMAN RIGHTS AND FUNDAMENTAL FREEDOMS

La presente descripción se refiere al uso de hidroxiisoxalinas y derivados de estos como fungicida. También se refiere a derivados de hidroxiisoxalinas, su uso como fungicida y composiciones que comprenden los mismos. Reivindicación 1: Un compuesto de fórmula (1), donde: R¹ representa un sustituyente que se selecciona del grupo que consiste en hidrógeno, C₁₋₆-alquilo y -C(=O)Rᵃ, donde el propio sustituyente C₁₋₆-alquilo esta opcionalmente sustituido, una o más veces, del mismo modo o de modo diferente, con R⁵; R² y R³ independientemente uno del otro, representan un sustituyente que se selecciona del grupo que consiste en hidrógeno, halógeno y C₁₋₆-alquilo; o, juntos, forman un C₃₋₁₀-carbociclilo; A representa arilo o heteroarilo; R⁶ representa CX₃ donde X representa, independientemente uno de otro, un sustituyente que se selecciona del grupo que consiste en un átomo de hidrogeno, flúor cloro, bromo, y yodo, donde al menos un sustituyente X es un átomo de flúor; R⁴ representa independientemente ...

THIOXOTHIAZOLIDINE DERIVATIVE HAVING RAS FUNCTION INHIBITORY EFFECT

Provided is an anticancer agent which has an Ras function inhibitory effect. The present invention provides an Ras function inhibitor which contains a compound represented by formula (I') (wherein the symbols are as defined in the description) or a salt thereof.

NOVEL LAPACHONE COMPOUNDS AND METHODS OF USE THEREOF

The invention provides lapachone analogs and derivatives as well as methods of use thereof. These compounds can be used in pharmaceutical compositions for the treatment or prevention of cell proliferation disorders. These compounds can also be used in the treatment or prevention of cancer or precancerous conditions.

Nitroimino-nitromethylene-azole or-azine heterocyclic compounds, insecticidal compositions containing them, and insecticidal methods of using them

Insecticides of the formulain whichn is 0 or 1,X is S, O,orY is N orZ is a 5- or 6-membered nitrogen-containing heterocyclic ring, andR to R9 variously represent hydrogen or specified organic radicals.

Heterocyclic compounds

1-SUBSTITUIERTE-1-AMINOMETHYL-CYCLOALKAN DERIVATE (= GABAPENTIN ANALOGA), DEREN HERSTELLUNG UND DEREN VERWENDUNG BEI DER BEHANDLUNG VON NEUROLOGISCHEN ERKRANKUNGEN

1-SUBSTITUTED-1-AMINOMETHYL-CYCLOALKANE DERIVATIVES (=GABAPENTIN ANALOGUES), THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

Novel amines of formulas (1), (1C), (1F), (1G) and (1H) or a pharmaceutical acceptable salt thereof wherein n is an integer of from 0 to 2; m is an integer of from 0 to 3; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; A' is a bridged ring selected from (1), (2), (3), (4), (5) wherein \Ablank; is the point of attachment; Z1 to Z4 are each independently selected from hydrogen and methyl; o is an integer of from 1 to 4; and p is an integer of from 0 to 2. In formula (1) above R cannot be sulfonic acid when m is 2 and n is 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially irritable bowel syndrome.

2-NITROMETHYLENE AND 2-NITROIMINE DERIVATIVES OF TRIAZOLIDINE, THIAZINE, OXAZOLIDINE, OXAZINE, IMIDAZOLIDINE, TETRAHYDROPYRIMIDINE, PYRROLIDINE AND PIPERIDINE AS INSECTICIDES

The present invention relates to novel heterocyclic compounds, to processes for their preparation and to their use as insecticides. The new heterocyclic compounds can be characterized by the formula (I) (I) wherein n represents 0 or 1, R1, R2, R5 and R6 independently represent a hydrogen atom or and alkyl group, R3 and R4 independently represent a hydrogen atom, a hydroxy group or an alkyl group, where n represents 1, then R2 may form a single bond together with R5, X represents a sulfur atom, an oxygen atom or the following groups: -N-R7 or -?H-R8, wherein R7 and R8 have the meanings indicated in the patent application, ? represents a hydrogen atom or an alkyl group, Y represents a nitrogen atom or the group =?-R wherein R9 has the meaning as defined in the patent application and wherein Z has the meaning as defined in the patent application.

-4(3)-İkameli -4(3)- aminometil-(tio) piran veya- piperidin türevleri (=Gabapentin analogları), hazırlanmaları ve nörolojik hastalıkların tedavisinde kullanımları

SYNTHESIS OF EPOTHILONES, INTERMEDIATES THERETO, ANALOGUES AND USES THEREOF

The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).

Heterocyclic compounds

Novel insecticides of the formula (* CHEMICAL STRUCTURE *) in which n is 1, X is (* CHEMICAL STRUCTURE *) Y is N or (* CHEMICAL STRUCTURE *) Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R9 variously represent hydrogen or specified organic radicals.

PIPERAZINYLMETHYL-1,2,4-TRIAZOLYL METHYL CARBINOLS

Hydroxyisoxazolines and derivatives thereof

The present disclosure relates to the use of hydroxyisoxazolines and derivatives thereof as fungicide. It also relates to new hydroxyisoxazolines derivatives, their use as fungicide and compositions comprising thereof.

HIGHLY SELECTIVE SIGMA RECEPTOR RADIOLIGANDS

Compounds having the general formula III, or IV wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y is S; Z can be either H, O, S, SR or NR where R groups can be either H, aryls, alkyls, or cycloalkyls; n can be 1 to 5 carbons in length and stereoisomers, functional analogs, and pharmaceutically acceptable salts thereof and wherein the moiety bridging R1 and N can be a substituted alkylene, optionally substituted alkenylene or optionally substituted alkynylene and where the alkylene group can include an inserted C3-C5 cycloalkyl group, aromatic, and ...

4(3)substituted-4(3)-aminomethyl-(thio)pyran or -piperidine derivatives (=gabapentin analogues), their preparation and their use in the treatment of neurological disorders

Cephem compounds, their production and use

Cephem compounds, pharmaceutically acceptable salts thereof, and methods of using same, wherein the compound has a bicyclic nitrogen-containing aromatic heterocyclic ring as the quaternary ammoniomethyl group at the 3-position and one or both of a terminal amidine residue (substituted or unsubstituted) attached to an aryl or a 5- or 6- membered heteroaryl group (substituted or unsubstituted) which is further attached through a spacer to the free N-atom of the quaternary nitrogen-containing bicyclic ring at the 3-side chain, or a terminal guanidine residue attached to an aryl or a 5- or 6- membered heteroaryl group (substituted or unsubstituted) which is further attached through a spacer to the free N-atom of the quaternary nitrogen-containing bicyclic ring at the 3-side chain.

Heterocyclic inhibitors of MEK and methods of use thereof

Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Synthesis of epothilones, intermediates thereto, analogues and uses thereof

The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).

1-SUBSTITUIERTE-1-AMINOMETHYL-CYCLOALKAN DERIVATE (= GABAPENTIN ANALOGA), DEREN HERSTELLUNG UND DEREN VERWENDUNG BEI DER BEHANDLUNG VON NEUROLOGISCHEN ERKRANKUNGEN

Adhesion receptor antagonists

Cephem compounds, their production and use

Cephem compounds, pharmaceutically acceptable salts thereof, and methods of using same, wherein the compound has a bicyclic nitrogen-containing aromatic heterocyclic ring as the quaternary ammoniomethyl group at the 3-position and one or both of a terminal amidine residue (substituted or unsubstituted) attached to an aryl or a 5- or 6- membered heteroaryl group (substituted or unsubstituted) which is further attached through a spacer to the free N-atom of the quaternary nitrogen-containing bicyclic ring at the 3-side chain, or a terminal guanidine residue attached to an aryl or a 5- or 6- membered heteroaryl group (substituted or unsubstituted) which is further attached through a spacer to the free N-atom of the quaternary nitrogen-containing bicyclic ring at the 3-side chain.

Novel amines as pharmaceutical agents

MEDICINAL IMIDAZOLE DERIVATIVES

LINKED HETEROCYCLIC COMPOUNDS

1-SUBSTITUTED-1-AMINOMETHYL-CYCLOALKANE DERIVATIVES (=GABAPENTIN ANALOGUES), THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

Novel amines of formulas (1), (1C), (1F), (1G) and (1H) or a pharmaceutical acceptable salt thereof wherein n is an integer of from 0 to 2; m is an integer of from 0 to 3; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; A' is a bridged ring selected from (1), (2), (3), (4), (5) wherein is the point of attachment; Z1 to Z4 are each independently selected from hydrogen and methyl; o is an integer of from 1 to 4; and p is an integer of from 0 to 2. In formula (1) above R cannot be sulfonic acid when m is 2 and n is 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially irritable bowel syndrome.

((CYCLO)ALKYL SUBSTITUTED)-GAMMA-AMINOBUTYRIC ACID DERIVATIVES (=GABA ANALOGUES), THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

Novel amines of formulas (1A) and (1B) or a pharmaceutically acceptable salt thereof wherein: n is an integer of from 0 to 2; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; A is hydrogen or methyl; and B is (a), straight or branched alkyl of from 1 to 11 carbons, or -(CH2)1-4-Y-(CH2)0-4-phenyl wherein Y is -O-, -S-, -NR'3 wherein R'3 is alkyl of from 1 to 6 carbons, cycloalkyl of from 3 to 8 carbons, benzyl or phenyl wherein benzyl or phenyl can be unsubstituted or substituted with from 1 to 3 substituents each independently selected from alkyl, alkoxy, halogen, hydroxy, carboxy, carboalkoxy, trifluoromethyl, and nitro are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS. Processes for the preparation and intermediates ...

FUSED BENZOXAZEPINONES AS ION CHANNEL MODULATORS

The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

4(3)SUBSTITUTED-4(3)-AMINOMETHYL-(THIO)PYRAN OR -PIPERIDINE DERIVATIVES (=GABAPENTIN ANALOGUES), THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

Novel amines of formulas (1D) and (1E), or a pharmaceutically acceptable salt thereof, wherein: n is an integer of from 0 to 2; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; and X is -O-, -S-, -S(O)-, -S(O)2-, or NR'1 wherein R'1 is hydrogen, straight or branched alkyl of from 1 to 6 carbons, or benzyl, -C(O)R'2 wherein R'2 is straight or branched alkyl of 1 to 6 carbons, benzyl or phenyl or -CO2R'3 wherein R'3 is straight or branched alkyl of from 1 to 6 carbons, or benzyl wherein the benzyl or phenyl groups can be unsubstituted or substituted by from 1 to 3 substituents selected from halogen, trifluoromethyl, and nitro, are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS.

Fused benzoxazepinones as ion channel modulators

The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z ...

Cephem compounds, their production and use

Cephem compounds, pharmaceutically acceptable salts thereof, and methods of using same, wherein the compound has a bicyclic nitrogen-containing aromatic heterocyclic ring as the quaternary ammoniomethyl group at the 3-position and one or both of a terminal amidine residue (substituted or unsubstituted) attached to an aryl or a 5- or 6- membered heteroaryl group (substituted or unsubstituted) which is further attached through a spacer to the free N-atom of the quaternary nitrogen-containing bicyclic ring at the 3-side chain, or a terminal guanidine residue attached to an aryl or a 5- or 6- membered heteroaryl group (substituted or unsubstituted) which is further attached through a spacer to the free N-atom of the quaternary nitrogen-containing bicyclic ring at the 3-side chain.

CEFÉM COMPOUNDS, THEIR PRODUCTION AND USE

COMPOSTOS HETEROCICLICOS,PROCESSO PARA SUA PREPARACAO,COMPOSICOES INSETICIDAS,PROCESSO PARA COMBATE A INSETOS DANINHOS,UTILIZACAO E PROCESSO PARA A PREPARACAO DE COMPOSICOES

SYNTHESIS OF EPOTHILONES, INTERMEDIATES THERETO, ANALOGUES AND USES THEREOF

MONOMETHINE DYES

Monomethine dyes that have no or minimal fluorescence in buffer or in the presence of single stranded DNA or RNA, but strongly fluoresce in the presence of double-stranded DNA. In one embodiment, the dye is useful in quantitative RT-PCR.

Processes for preparing oxathiazin-like compounds

Oxathiazin-like compounds, processes for making new oxathiazin-like compounds, compounds useful for making oxathiazin-like compounds, and their uses are disclosed. Processes of treating patients suffering from cancers, bacterial infections, fungal infections and/or viral infections by administering oxathiazin-like compounds are also disclosed. These compounds were found to have significantly longer half-life compared to taurolidine and taurultam.

1-substituted-1-aminomethyl-cycloalkane derivatives (= gabapentin analogues), their preparation and their use in the treatment of neurological disorders

Novel amines of formulas 1, 1C, 1F, 1G and 1H or a pharmaceutical acceptable salt thereof wherein n is an integer of from 0 to 2; m is an integer of from 0 to 3; R is sulfonamide, amide, heterocycle, sulfonic acid, or hydroxamic acid; A' is a bridged ring selected from wherein is the point of attachment; Z1 to Z4 are each independently selected from hydrogen and methyl; o is an integer of from 1 to 4; and p is an integer of from 0 to 2. In formula (1) above R cannot be sulfonic acid when m is 2 and n is 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially irritable bowel syndrome.

SUBSTITUTED 5-(2-((2-ARYL-2-HYDROXYETHYL)AMINO)PROPYL)-1,3-BENZODIOXOLES

1-substituted-1-aminomethyl-cycloalkane derivatives (=gabapentin analogues), their preparation and their use in the treatment of neurological disorders

PIPERAZINYLMETHYL-1,2,4-TRIAZOLYLMETHYL-CARBINOLE

Substituted isoxazoles as fungicides

The present invention provides compounds of formula I: (I) along with methods of making the same, compositions thereof, and methods of use thereof, particularly methods of use as fungicides.

Fused benzoxazepinones as ion channel modulators

The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula 1: wherein Z1, Z2, Z3 , Z4, X, Y, R2 R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.