СИНТЕЗ КИСЛОРОДЗАМЕЩЕННЫХ БЕНЗОЦИКЛОГЕПТЕНОВ В КАЧЕСТВЕ ЦЕННЫХ ПРОМЕЖУТОЧНЫХ ПРОДУКТОВ ДЛЯ ПОЛУЧЕНИЯ ТКАНЕСЕЛЕКТИВНЫХ ЭСТРОГЕНОВ

Изобретение относится к новым промежуточным продуктам и усовершенствованному способу получения соединения С: Предлагаемый в изобретении способ получения основан на использовании недорогих исходных материалов, позволяет получать промежуточные продукты с высоким выходом и высокой степенью чистоты без необходимости проводить операции по хроматографической очистке и может быть реализован в условиях крупномасштабного промышленного производства. Изобретение относится к усовершенствованным способам получения соединения формулы I: соединения формулы II: соединения формулы III: соединения формулы VIII: соединения формулы IX: а также к реагенту, состоящему из трибромида бора и 2,6-диметилпиридина, для щадящего и селективного отщепления метильной группы в ароматических простых метиловых эфирах. 11 н. и 1 з.п. ф-лы.

ЦИС-2,4,5-ТРИФЕНИЛИМИДАЗОЛИНЫ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ

Изобретение относится к новым соединениям формулы I, где R означает -C(O)R1, где R1 выбирают из ряда C1-С6алкил, -C=CHCOOH,-NHCH2CH2R2, -N(CH2CH2OH)CH2CH2OH, -N(CH3)CH2CH2 NHCH3, -N(СН3)СН2СН2N(СН3)СН3, насыщенные 4-, 5- и 6-членные циклы и насыщенные и ненасыщенные 5- и 6-членные циклы, содержащие по меньшей мере один гетероатом, выбранный из ряда S, N и О, и необязательно замещенные группой, выбранной из ряда C1-С6алкил, -C=O-R5, -ОН, C1-С6 алкил, необязательно замещенный гидроксигруппой, C1-С6алкил, необязательно замещенный группой ряда -NH2, -N-(C1-С6)алкил, -SO2СН3, =O, и 5- и 6-членные насыщенные циклы, содержащие по меньшей мере один гетероатом, выбранный из ряда N и О, где R5 выбирают из ряда Н, C1-С6алкил, C1-С6алкил, необязательно замещенный гидроксигруппой, и C1-С6алкил, необязательно замещенный группой -NH2, R2 выбирают из ряда -N(СН3)СН3, -NH2, морфолинил и пиперазинил, X1, Х2 и Х3 независимо выбирают из ряда -ОН, С1-С2алкил, C1-С6алкокси, -Cl, -Br, -F, -СН2OCH3 и -СН2OCH2СН3 ...

Способ получения производных тризамещенных имидазолов или их солей

... 1. Способ получения производных тризамещенных имидазолов общей формулы (I) J XV-H Н2 -N Н где R, и R - каждьй, замещенный низшим, алкокси фенил; А - низший алкилен или низший алкилиден; Rg - карбокси, низший алкоксикарбонил или кар- бамоил, или один из остатков R, и Rg - пиридил или 1-окси- допиридил, а другой - фенил или замещенный низшим алкокси, окси или галогеном фенил, А - низший алкилен. низший алкилиден, низший алкенилиден или моноциклический цик- лоалкилиден с 3-8 членами, а R.-карбокси , низший алкокси- карбонил или низший алканоилоксинизший алкоксикарбонил, или один КЗ остатков R и R - пиридил или 1-оксидопиридил, а другой - тиенил, А - низший алкилиден, а R J - низший алкоксикарбонил , или их солей, при условии, что, если А - этилиден, а Rj - карбокси или соответственно карбамоил, то оба остатка R, и Rj не могут одно- в ременно означать п -метоксифенил, отличающийся тем, что соединение общей формулы (П) «, R :хУf Нз § (Л с в гЗ о ел ч Од 4 Н где R,-R,. и А имеют указанные значе ...

Verfahren zur Aufhebung des durch optische Aufheller erzielten Aufhelleffektes

Angiotensin II receptor blocking imidazolinone derivatives

Cyclic amidines and compositions containing them

A liquid hydrocarbon fuel has dissolved therein at least one cyclic amidine of the general formula wherein R1 is C1-C24 alkyl, phenyl, naphthyl, benzyl, or said aryl groups substituted with one or more alkyl groups contributing a total of not more than 16 carbon atoms; R2 is hydrogen or C1-C24 alkyl; or R1 and R2 together with the nitrogen atom to which they are joined represent a morpholino, thiamorpholino, piperidino or pyrrolidinyl group; X represents ethylene, ethenylene, trimethylene, alkyl- or alkenyl-substituted ethylene having a total of up to 20 carbon atoms, 1,2-cyclohexylene or alkyl-substituted 1,2-cyclohexylene having a total of up to 16 carbon atoms, 1,2-cyclohexenylen or alkyl-substituted 1,2-cyclohexenylene having a total of up to 16 carbon atoms, 3,6-methano-1,2 - cyclohexylene and 3,6 - methano - 1,2 - cyclohexenylene; R3 represents hydrogen, 2-hydroxyethyl, 2 - amino - ethyl, 2- or 3-hydroxypropyl, 2- or 3-aminopropyl, 2- or 3-(2-aminoethyl) aminopropyl ...

PRODUCTION OF 1,3-DIAZA-HETEROCYCLES

CIS IMIDAZOLINE ONE AS MDM2-HEMMER

PRODUCTION OF ALPHA - HYDROXY CARBOXY ACID BY A COUPLED ENZYME SYSTEM

TRICYCLI STEROIDHORMONKERNREZEPTOR MODULATORS

PROCEDURES FOR THE PRODUCTION OF ARYL ETHANOL DIAMINES THE WHEN AGONISTEN THE BETA-3-ADRENOCEPTORS USEFUL ARE

PROCEDURE FOR the PRODUCTION OF NEW ONE 6-ARYL-2,3, 6,7-TETRAHYDRO-5H-PYRROLO (1,2-A) IMIDAZOLEN AND OF THEIR SAEUREADDITONSSALZEN

NEW TRISUBSTITUTED IMIDAZOLDERIVATE, PROCEDURES FOR YOUR PRODUCTION, THESE CONTAINING PHARMACEUTICAL PREPARATIONS AND YOUR USE.

N-CYANOMETHYLAMIDE ONE AS PROTEASE INHIBITORS

AS WELL AS AZOVERBINDUNGEN PROCEDURES FOR THE PRODUCTION THE SAME

PROCEDURE FOR THE PRODUCTION OF FACIAL METAL TRICARBONYL CONNECTIONS AND YOUR APPLICATION TO THE MARKING OF BIO SUBSTRATES

STABLE POLYMORPH OF FLIBANSERIN, INDUSTRIALIST PROCEDURE FOR ITS PRODUCTION AND ITS USE FOR THE PRODUCTION OF MEDICINES

AMINOALKYLAMINOCARBONYL AMINODIOL AMINO ACID DERIVATIVES AS ANTI-HYPERTENSIVE AGENTS

Benzamidine derivatives

2,4,5-triphenyl imidazoline derivatives as inhibitors of the interaction between P53 and MDM2 proteins for use as anticancer agents

There is provided a compound of formula (I) and the pharmaceutically acceptable salts and esters thereof wherein X , X, R , R, R, R, R and R are herein described. The compounds exhibit activity as anticancer agents.

Use of lamotrigine for treating aids-related neural disorders

Pesticidal heterocycles

Neprilysin inhibitors

In one aspect, the invention relates to compounds having the formula: where R ...

Novel imidazoline compounds

CIS-2,4,5- TRIPHENYL-IMIDAZOLINES AND THEIR USE IN THE TREATMENT OF TUMORS

The present invention provides compounds according to formula I and formula II and pharmaceutically acceptable salts ad esters thereof, having the designations provides herein and which inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activity. Formula (I).

CIS-2,4,5-TRIPHENYL-IMIDAZOLINES AND THEIR USE IN THE TREATMENT OF TUMORS

The present invention provides compounds according to formula I and formula II and pharmaceutically acceptable salts ad esters thereof, having the designations provides herein and which inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activity. Formula (I).

SALT FREE PHOSPHOBETAINES

1,3-DIAMINOCYCLOPENTANE CARBOXAMIDE DERIVATIVES

Disclosed herein are 1,3-diaminocyclopentane carboxamide derivatives of the general formula I, pharmaceutical compositions comprising them, and processes for their preparation. The disclosed compounds inhibit the activity of fatty acid synthase and can be employed for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.

.ALPHA.-ARYL-.ALPHA.-HYDROXY-.BETA.-IMIDAZOLINYL-PROPIONAMIDES

.alpha.-Ary-.alpha.-hydroxy-.beta.-imidazolinyl-propionamides Abstract The present invention relates to novel .alpha.-aryl-.alpha.-hydroxy-.beta.-imidazolinyl-propionamides of the general formula (I) (I)

USE OF LAMOTRIGINE FOR THE TREATMENT OF NEURO-SIDA

L'invention concerne l'application de la lamotrigine ou les sels pharmaceutiquement de ce composé dans le traitement du neuro SIDA.

NOVEL N-(ARYLSULPHONYL)AMINO ACID DERIVATIVES, THEIR PREPARATION PROCESS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

L'invention concerne des composés de formule (I) dans laquelle R1 à R9, R16 et R17 sont tels que définis à la revendication (1). Ces composés sont pharmacologiquement actifs.

AZO COMPOUNDS AND PROCESS FOR PRODUCING THE SAME

Azo compounds represented by formula (I), which are diamide type azo compounds derived from 2-hydroxynaphthalene-3,6-dicarboxylic acid and in which at least one of the amides is aliphatic. Various uses of the compounds are also provided.

Verfahren zur Herstellung oligomerer bzw. polymerer Amine

Procédé de préparation d'isothiourées

Procédé de préparation de thiourées

PROCEDURE FOR THE PRODUCTION OF NEW OF SUBSTITUTING BETA AMINOPROPIONSAEURE ONES AND THEIR ESTER.

PROCEDURE FOR the PRODUCTION of NEW 6-ARYL AND/OR 6-HETEROARYL-2,3,6,7-TETRAHYDRO-5H-PYRROLO (1,2-A) - IMIDAZOLE.

PROCEDURE FOR the PRODUCTION of NEW 6-ARYL AND/OR 6-HETEROARYL-2,3,6,7-TETRAHYDRO-5H-PYRROLO (1,2-A) - IMIDAZOLE.

PROCEDURE FOR the PRODUCTION of NEW 6-ARYL AND/OR 6-HETEROARYL-2,3,6,7-TETRAHYDRO-5H-PYRROLO (1,2-A) - IMIDAZOLE.

PREPARATION METHOD [...]-AMINO AMIDE.

PREPARATION METHOD [...]-AMINO ACIDS.

СТАБІЛЬНА ПОЛІМОРФНА МОДИФІКАЦІЯ ФЛІБАНСЕРИНУ, СПОСІБ ЇЇ ПРОМИСЛОВОГО ОДЕРЖАННЯ ТА ЇЇ ЗАСТОСУВАННЯ ДЛЯ ОДЕРЖАННЯ ЛІКАРСЬКИХ ЗАСОБІВ

У заявці описані поліморфна модифікація А флібансерину, спосіб її промислового одержання, а також її застосування для одержання лікарських засобів.

НОВЫЕ СОЕДИНЕНИЯ И КОМПОЗИЦИИ В КАЧЕСТВЕ ИНГИБИТОРОВ ПРОТЕАЗЫ

Настоящее изобретение относится к новым N-цианометиламидам, которые являются ингибиторами цистеиновой протеазы, к их фармацевтически приемлемым солям и их N-оксидам, а также к их применению в качестве терапевтических агентов и к способам получения указанных соединений.

МЕТА-АЗАЦИКЛІЧНІ СПОЛУКИ АМІНОБЕНЗОЙНОЇ КИСЛОТИ ТА ЇХ ПОХІДНІ, ЩО Є ІНГІБІТОРАМИ ІНТЕГРИНУ

Даний винахід відноситься до сполук формули (І) і фармацевтично прийнятних солей і ізомерів таких сполук, застосовних як антагоністи -інтегрину (І).

STABLE POLYMORPH MODIFICATION OF FLIBANSERIN, METHOD FOR INDUSTRIAL PRODUCTION THEREOF AND USE THEREOF FOR PREPARING MEDICAMENTS

Method for synthesizing heterocyclic ketenes amine condensation derivatives

The invention discloses a synthesizing method of heterocyclic ketene amine derivant, which comprises the following steps: 1) reacting acryloyl chloride and Wang resin to obtain resin connected by alpha, beta-unsaturated acid ester; reacting with diamine compound to obtain fix-carrying diamine; 2) reacting the fix-carrying diamine and S, S-ketene acetal to produce the product; filtering; washing; drying; separating; realizing the diversity of product.

ISOTHIOUREAS

Derives d'alcools n-heterocycliques a action therapeutique

Composes repondant a la formule :X-CH2-CH-C-NH-CH-C-NH-CH-CH-R1 Ces composes sont des inhibiteurs de la renine et sont par consequent utilisables comme agents cardiovasculaires.

derivados de 2,4,5-trifenil imidazolina, composição farmacêutica que os compreende, uso e processo para a sìntese dos mesmos

NEW LH-RH-ANTAGONISTS OF IMPROVED EFFECT

The invention relates to new LH-RH antagonists, in particularof protomimetics and peptides modified in a side chain, to theirsalts with pharmaceutically acceptable acids and to method fortheir preparation. The peptides are analogues of the hormonreleasing the luteinization hormone (LH-RH). The compounds havehigh antagonistic activity and have no unwanted side effects, inparticular edematogenous ones.18 claims, 6 figures ...

IMIDAZOLES AND THEIR USE CCK-1 RECEPTOR MODULATORS

Certain imidazole compounds of formula (i) wherein R1, R2 and Ar are specified ring systems, m is 0, 1, or 2, and R4 is COOR5 or CONR6R7, are CCK1 modulators useful in the treatment of CCK1 mediated diseases.

IMIDAZOLE DERIVATIVES FOR THE TREATMENT OF DEMENTIA AND RELATED DISORDERS

This invention relates to imidazole derivatives which are useful in treating dementia and related disorders.

PROCESS FOR THE PREPARATION OF ARYLETHANOLDIAMINES USEFUL AS AGONISTS OF THE BETA-3-ADRENOCEPTOR

An improved process for preparing arylethanoldiamines is described. Compounds of this type are known to be useful as agonists at atypical beta-adrenoceptors (also known as beta-3-adrenoceptors).

USE OF RILUZOLE FOR TREATING AIDS-RELATED NEURAL DISORDERS

The use of riluzole or pharmaceutically acceptable salts thereof for treating AIDS-related neural disorders is disclosed.

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.

NOVEL IMIDAZOLINE COMPOUNDS

Compounds represented by the general formula (I): (wherein Ar1 and Ar2 are each aryl or heteroaryl; R1 is lower cycloalkyl, -Ar3, or a group of the general formula (a), (b) or (c): and R2and R3 are each hydrogen, lower cycloalkyl, lower alkenyl, or optionally substituted lower alkyl (with the proviso that when R2 and R3are simultaneously hydrogen, Ar1, Ar2 and R1do not simultaneously represent unsubstituted phenyl). The compounds are useful as treating agents for various NPY-related diseases, for example, circulatory diseases including hypertension, kidney diseases, cardiac diseases, vasospasm and arteriosclerosis; central nervous system diseases including hyperphagia, depression, anxiety, convulsion, epilepsy, dementia, pain, alcohol dependence, and withdrawal symptoms due to abstinence from drugs; metabolic diseases including obesity, diabetes, hormonal disorders, hypercholesterolemia, and hyperlipidemia; sexual dysfunction and reproductive function disorders; digestive diseases including ...

Indolyl amino acids useful as antihypertensive agents

A compound of the formula possesses antihypertensive activity. Also provided are methods for the preparation of the compounds as well as pharmaceutical formulations and methods for their use as antihypertensive agents.

Melanocortin-4 receptor binding compounds and methods of use thereof

Provided are MC4-R binding compounds of the formula XVII: wherein L₂ is a linker group, and P¹, P², P³, P⁴, Z¹, Z², Z³, Z⁴, Z⁵, t, s, and R are as described in the specification. Methods of using the compounds to treat MC4-R associated disorders, such as disorders associated with weight loss, are also provided.

Tri-substituted imidazole derivatives, pharmaceutical preparations containing them, and their use

The invention relates to novel tri-substituted imidazole derivatives, especially compounds of the general formula I (I) in which R1 and R2 represent, independently of each other, carbocyclic aryl and heteroaryl, A represents a divalent hydrocarbon radical, and R3 represents carboxy, esterified carboxy or amidated carboxy, their isomers and their salts, especially pharmaceutically acceptable salts, with the proviso that, if A represents methylene or ethylidene and R3 represents ethoxycarbonyl, at least one of the radicals R1 and R2 is different from phenyl, and the further proviso that, if A represents ethylidene and R3 represents carboxy, at least one of the radicals R1 and R2 is different from phenyl, p-methoxyphenyl and p-chlorophenyl, processes for their manufacture, pharmaceutical preparations containing such compounds, and their use, for example as active substances in medicaments. The compounds of the formula I can be used as skin phlogistatics, sun-screening agents and antiviral ...

Subtype-selective NMDA receptor ligands and the use thereof

The invention relates to subtype-selective NMDA receptor ligands and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, Parkinson's disease, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.

Способ получения тризамещенных производных имидазола

СПОСОБ ПОЛУЧЕНИЯ ТРИЗАМЕЩЕННЫХ ПРОИЗВОДНЫХ ИМИДАЗОЛА общей формулы (1) N V-A-R. R R N Н 2. где R, и Rj - каждый замещенный низшим алкокси фенил; А низший алкилен или низший алкилиден; карбокси, низщий алкоксикарбоНИЛ или карбамоил, или один из остатков R и R2 - пйридил или 1-оксидопиридил, а другой фенил или замещенный нижгаим алкоКси, окси или галогеном фенил; А - низший алкилен, низший алкилиден, низший алкенилиден или моноциклический циклоалкилиден с 3-8 членами, R карбокси , низший алкоксикарбоиил или низший алканоилоксинизший алкоксикарбонил, или один из остатков Я, и Rg пиридил или 1-оксидопиридил, а другой - тиенил; А - низший алкилиден, з низший алкоксикарбонил , с тем условием, что если А - этилиден, а R j - карбокси или соответственно карбамоил, то оба остатка К, и Rj не могут одновременно означать п -метоксифенил , отличающийся СО тем, что соединения формулы (II) R RZ N где R, и Rj имеют указанные значения, или их таутомеры подвергают взаимодействию с соединениями формулы , N ...

OXIME DERIVATIVES AND THEIR USE IN THE PROTECTION OF CULTIVATED PLANTS

VERFAHREN ZUR HERSTELLUNG NEUER TRISUBSTITUIERTER OXAZOLDERIVATE

HERSTELLUNG VON ALPHA -HYDROXY-CARBOXY SÄURE MIT HILFE VON EINEM GEKOPPELTEN ENZYM SYSTEM

Nitrogenous Compounds

... 1,172,734. Lubricants; fuels. ROHM & HAAS CO. 20 Feb., 1967 [2 March, 1966], No. 7992/67. Headings C5F and C5G. [Also in Division C3] Natural and synthetic lubricant and liquid hydrocarbon fuel compositions comprise detergent and dispersant additives of formula where one R is an alkenyl or substituted alkenyl group of 30 to 200 carbon atoms and the other R is hydrogen; R 1 is C 1-24 alkyl, phenyl, naphthyl, benzyl or a alkyl-substituted phenyl, naphthyl or benzyl in which the alkyl substituents have a total of up to 24 carbon atoms, and R 2 is hydrogen or C 1-24 alkyl, or R 1 and R 2 together with the nitrogen atom to which they are attached form a morpholino, thiamorpholino, piperidino or pyrrolidinyl group; R 3 is hydrogen, hydroxyethyl, aminoethyl, hydroxypropyl, aminopropyl or aminoethylaminopropyl; and D is a divalent saturated chain of 2 or 3 carbon atoms, optionally substituted by alkyl groups containing up to 12 carbon atoms, or a 1,2-cyclohexylene group. The fuel may be a gasoline ...

HERBICIDES VINYLAMINDERIVATE.

ALPHA ARYL ALPHA HYDRAULIC XY BETA IMIDAZOLINYLPROPIONSÄUREAMIDE

ADMINISTRATION FROM RILUZOL TO THE TREATMENT OF NEURO AIDS

IMIDAZOLIN CONNECTIONS

SALT-FREE PHOSPHORUS BETAINES.

DERIVATIVES OF AMINO ACIDS, IT ABSTENTIONS PHARMACEUTICAL COMPOSITIONS AS WELL AS THEIR HERSTELLUNSGVERFAHREN

PREPARATIONS FOR THE INHIBITION OF THE BY OSTEOKLASTEN OBTAINED BONE ABSORPTION

AMINO ACID ANALOGS AS CCK ANTAGONISTS

Novel CIS-imidazolines

Melanocortin-4 receptor binding compounds and methods of use thereof

CIS-2,4,5- TRIPHENYL-IMIDAZOLINES AND THEIR USE IN THE TREATMENT OF TUMORS

Use of riluzole for treating aids-related neural disorders

ANGIOTENSIN II RECEPTOR BLOCKING IMIDAZOLINONE DERIVATIVES

ANGIOTENSIN II RECEPTOR BLOCKING IMIDAZOLINONE DERIVATIVES

Novel imidazoline compounds

Neprilysin inhibitors

In one aspect, the invention relates to compounds having the formula: where R ...

IMIDAZOLIDINE DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS

AGENTS FOR PROTECTING PLANT CROPS

NITROGENOUS CONDENSATION PRODUCTS

CIS-2,4,5-TRIARYL-IMIDAZOLINES AND THEIR USE AS ANTI-CANCER MEDICAMENTS

There are presented compounds of the formula (I), or pharmaceutically acceptable salts thereof, wherein Y1,Y2, X1 ,X2, X3 and R are as described in this application. These compounds are believed to inhibit MDM2-p53 interaction and as such the compounds will have anti-hyperproliferative cellular activity.

NEPRILYSIN INHIBITORS

In one aspect, the invention relates to compounds having the formula: (see formula I) or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

NEW IMIDAZOLINE DERIVATIVES, PREPARATION PROCESS AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Composés de formule (I): (voir fig. I) dans laquelle R est tel que défini dans la description, ainsi que leurs isomères et leurs sels d'addition à un acide, pharmaceutiquement acceptables, utiles dans le traitement des pathologies liées aux récepteurs aux imidazolines.

AMINO ACID DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS AND PROCESSES FOR PREPARING THEM

The invention relates to new amino acid derivatives of general formula (I), wherein B, T, Z, Y, V and n are defined as in claim 1, the tautomers, diastereomers and enantiomers thereof, the mixtures thereof and the salts thereof, particularly their physiologically acceptable salts with inorganic or organic acids or bases which have valuable pharmacological properties, particularly selective NPY-antagonist properties, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.

Meta-Azacyclic Amino Benzoic Acid Compounds and Derivatives Thereof Being Integrin Inhibitors, Pharmaceutical Composition and Use Thereof

Мета-азациклические соединения аминобензокислоты и их производные, которые представляют собой ингибиторы интегрина, содержащая их фармацевтическая композиция и применение

... 1. Технический результат Увеличение ассортимента лечебных средств. 2. Суть Соединение формулы (1) значения (X, Y и R даны в описании), содержащая их фармацевтическая композиция и применение в качестве лечебного средства. 3. Область применения Медицина Пунк.: 13 незав. 2 зав.

TRICYCLIC MODULATORS OF STEROID HORMONE NUCLEAR RECEPTOR

НОВЫЕ СОЕДИНЕНИЯ И КОМПОЗИЦИИ В КАЧЕСТВЕ ИНГИБИТОРОВ ПРОТЕАЗЫ

Новые соединения и композиции в качестве ингибиторов протеазы. Настоящее изобретение относится к новым N-цианометиламидам, которые являются ингибиторами цистеиновой протеазы, к их фармацевтически приемлемым солям и их N-оксидам, а также к их применению в качестве терапевтических агентов и к способам получения указанных соединений. Отчет о международном поиске был опубликован 2001.04.26.

N-ЦІАНОМЕТИЛОВІ АМІДИ ЯК ІНГІБІТОРИ ПРОТЕАЗИ

Винахід стосується нових N-ціанометилових амідів, що є інгібіторами цистеїнових протеаз, їх фармацевтично прийнятних солей та N-оксидів, використання цих сполук як терапевтичних засобів та способів їх виготовлення.

МЕТА-АЗАЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ АМИНОБЕНЗОЙНОЙ КИСЛОТЫ И ИХ ПРОИЗВОДНЫЕ, ЯВЛЯЮЩИЕСЯ ИНГИБИТОРАМИ ИНТЕГРИНА

Настоящее изобретение относится к соединениям формулы (I) и фармацевтически приемлемым солям и изомерам таких соединений, применимым в качестве антагонистов αvβ3-интегрина. Международная заявка была опубликована вместе с отчетом о международном поиске.

ПРОИЗВОДНЫЕ 2,4,5-ТРИФЕНИЛИМИДАЗОЛИНА КАК ИНГИБИТОРЫ ВЗАИМОДЕЙСТВИЯ МЕЖДУ БЕЛКАМИ P53 И MDM2, ПРЕДНАЗНАЧЕННЫЕ ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ПРОТИВОРАКОВЫХ СРЕДСТВ

В заявке описано соединение формулы I (I) и его фармацевтически приемлемые соли и сложные эфиры, в котором Х1, Х2, R1, R2, R3, R4, R5 и R6 описаны в данной заявке. Соединения имеют активность как противораковые средства.

Biocide composition of agricultural use

ACYLAMINO-CEPHEM-CARBOXYLIC ACIDS AND PROCESS FOR THEIR PREPARATION

DERIVED FROM N (ARYLSULFONYL) the PHARMACEUTICAL AMINO ACIDS, THEIR PREPARATION, COMPOSITIONS WHILE CONTAINING

L'invention concerne des composés de formule: (CF DESSIN DANS BOPI) dans laquelle R1 , R2 , R3 , R4 , R5 , R6 , R7 , R8 et R9 sont tels que définis à la revendication 1. Ces composés sont utilisables comme médicaments.

AGENTS ANTI-HYPERTENSIFS

L'invention concerne des composés chimiques nouveaux. Il s'agit de nouveaux dérivés de phénylalanine. Ces composés sont utiles comme médicaments.

Solabegron Zwitterion and Uses Thereof

This application relates to solabegron zwitterion useful for the treatment of lower urinary tract symptoms such as, for example, overactive bladder and prostate disorders. Additionally, this application relates to pharmaceutical compositions and methods of treatment utilizing the solabegron zwitterion for treating lower urinary tract symptoms. This application also relates to methods of preparing solabegron hydrochloride from the solabegron zwitterion. 2. The solid compound according to claim 1 , wherein the compound is characterized by an x-ray powder diffraction pattern having peaks expressed in degrees 2θ (±2) at 6.3 claim 1 , 12.6; 18.6; 18.9; 20.9; 22.4; 25.3; and 25.5.3. The solid compound according to claim 1 , wherein the compound is characterized by an x-ray powder diffraction pattern having peaks expressed in degrees 2θ (±2) at 6.2 claim 1 , 12.5; 18.8; 20.6; and 25.2.4. The solid compound according to claim 1 , wherein the compound is characterized by an x-ray powder diffraction pattern having peaks expressed in degrees 2θ (±2) at 6.2 claim 1 , 12.5; 18.6; 18.8; 20.6; 22.3 claim 1 , and 25.2.5. The solid compound according to claim 1 , wherein the compound is characterized by an x-ray powder diffraction pattern having peaks expressed in degrees 2θ (±2) at 6.2 claim 1 , 12.5; 16.9 claim 1 , 18.6; 18.8; 20.6; 21.1 claim 1 , 21.5; 22.3 claim 1 , 25.2; 26.6 claim 1 , and 32.9.6. The solid compound according to claim 1 , wherein the compound is characterized by an x-ray powder diffraction pattern having peaks expressed in degrees 2θ (±2) at 17.6 claim 1 , 18.7 claim 1 , 19.6 claim 1 , 20.1 claim 1 , 20.5 claim 1 , 23.7 claim 1 , and 25.8.7. The solid compound according to claim 1 , wherein the compound is characterized by an x-ray powder diffraction pattern having peaks expressed in degrees 2θ (±2) at 9.4 claim 1 , 15.1 claim 1 , 16.2 claim 1 , 17.6 claim 1 , 18.7 claim 1 , 19.6 claim 1 , 20.1 claim 1 , 20.5 claim 1 , 21.8 claim 1 , 22.6 claim 1 , 23.7 claim 1 ...

Compounds for the treatment of hypertension and hypertensive end stage renal disease

This disclosure relates to compounds and compositions useful for the treatment of hypertension and hypertensive renal disease. 2. The compound of claim 1 , wherein Rand Rare independently selected from the group consisting of: H claim 1 , CH claim 1 , and —C(O)NH(CH).3. The compound of claim 1 , wherein X is O.45.-. (canceled)7. (canceled)9. (canceled)11. (canceled)13. (canceled)14. The compound of claim 12 , wherein X is S.15. The compound of claim 12 , wherein X is O.16. (canceled)17. (canceled)19. (canceled)21. (canceled)2328.-. (canceled)28. A method for treating hypertensive end stage renal disease (ESRD) in a patient in need thereof claim 1 , the method comprising administering to the patient a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.2938.-. (canceled)40. A method for treating hypertensive end stage renal disease (ESRD) in a patient in need thereof claim 12 , the method comprising administering to the patient a therapeutically effective amount of a compound of claim 12 , or a pharmaceutically acceptable salt thereof. This application claims priority to U.S. Provisional Application Ser. No. 61/828,083, filed on May 28, 2013, which is incorporated herein by reference in its entirety.This invention was made with Government support under Grant No. HL58120, DK awarded by the National Institutes of Health. The Government has certain rights in the invention.This disclosure relates to compounds and compositions useful for the treatment of hypertension and hypertensive end stage renal disease.Hypertension is the most common and lethal of cardiovascular risk factors, yet despite pharmacological advances, it remains only partially controlled by antihypertensive medications. The past 30 years have seen a remarkable rise in the number of people living with end-stage renal disease (ESRD) within the United States, from a population of about 40,000 in 1978 to more than 400,000 in the early 21st century. ...

Synthesis of Triethylenetetramines

Methods and intermediates for synthesizing triethylenetetramine and salts thereof, as well as novel triethylenetetramine salts and their crystal structure, and triethylenetetramine salts of high purity. 1. A method of treating a cardiovascular disorder in a subject in need thereof , the method comprising administering a triethylenetetramine salt that has a purity of greater than about 95% pure.2. The method of wherein the cardiovascular disorder is selected from the group comprising atherosclerosis; peripheral vascular disease; cardiovascular disease; heart disease; coronary heart disease; restenosis; angina; ischemia; heart failure; stroke; cardiomyopathy; pre-hypertension claim 1 , hypertension claim 1 , secondary hypertension claim 1 , malignant hypertension claim 1 , isolated systolic hypertension claim 1 , and portal hypertension; acute coronary syndromes claim 1 , including myocardial infarction; and vascular occlusive disorders.3. The method of wherein the cardiovascular disorder is cardiomyopathy.4. The method of wherein the cardiovascular disorder is selected from the group comprising diseases or disorders associated with a hypercoagulable state or protein C deficiency claim 1 , including but not limited to arterial thrombosis claim 1 , arterial embolism claim 1 , pulmonary embolism claim 1 , deep venous thrombosis claim 1 , venous thrombosis claim 1 , renal vein thrombosis claim 1 , mesenteric vein thrombosis claim 1 , atheroembolic renal disease claim 1 , thrombophlebitis claim 1 , heart attack or angina claim 1 , viral hemorrhagic fever claim 1 , disseminated intravascular coagulation claim 1 , purpura fulminans claim 1 , bone marrow and other transplantations claim 1 , severe burns claim 1 , major surgery claim 1 , severe trauma claim 1 , adult respiratory distress syndrome claim 1 , postphlebic syndrome claim 1 , coumarin-induced skin necrosis; thrombotic diseases claim 1 , disorders or conditions; sepsis and related diseases claim 1 , disorders or ...

SOLABEGRON ZWITTERION AND USES THEREOF

This application relates to solabegron zwitterion useful for the treatment of lower urinary tract symptoms such as, for example, overactive bladder and prostate disorders. Additionally, this application relates to pharmaceutical compositions and methods of treatment utilizing the solabegron zwitterion for treating lower urinary tract symptoms. This application also relates to methods of preparing solabegron hydrochloride from the solabegron zwitterion. 140-. (canceled)42. The isolated compound according to claim 41 , wherein the isolated compound is a crystalline solid.43. The isolated compound according to claim 42 , wherein the crystalline solid is a single polymorph.44. The isolated compound according to claim 42 , wherein the crystalline solid is an anhydrous crystalline solid.45. The isolated compound according to claim 42 , wherein the crystalline solid is a hydrate of isopropanol solvate.46. The isolated compound according to claim 41 , wherein the compound is at least about 97.0% by weight pure.47. The isolated compound according to claim 41 , wherein the compound is at least about 99.0% by weight pure.48. The isolated compound according to claim 41 , wherein the compound is at least about 99.5% by weigh pure.49. The isolated compound according to claim 41 , wherein the compound is at least about 99.9% by weight pure.50. The isolated compound according to claim 41 , wherein no single impurity is present in an amount greater than about 0.5% by weight.51. The isolated compound according to claim 41 , wherein no single impurity is present in an amount greater than about 0.25% by weight.52. The isolated compound according to claim 41 , wherein no single impurity is present in an amount greater than about 0.10% by weight.54. The composition according to claim 53 , further comprising one or more additional therapeutic agents selected from the group consisting of: antimuscarinic agents; alpha adrenoceptor blockers; 5-alpha reductases; and phosphdiesterases-5 ...

TYPE III SECRETION INHIBITORS, ANALOGS AND USES THEREOF

The invention, in some aspects, relates to compounds and compositions useful for inhibiting Type III secretion systems in pathogenic bacteria, such as . In some aspects, the invention relates to methods for discovering inhibitors of the Type III secretion system and uses of such inhibitors in the treatment and prevention of disease. 3Yersinia. The method of claim 1 , wherein the bacterium is a species.4YersiniaYersinia pestis, Yersinia pseudotuberculosisYersinia enterocolitica.. The method of claim 3 , wherein the species is claim 3 , or5Yersinia pestis, Yersinia enterocolitica, Yersinia pseudotuberculosis, Salmonella enterica, Escherichia coli, Shigella dysenteriae, Shigella flexneri, Shigella boydii, Shigella sonnei, Bordetella pertussis, Bordetella parapertussis, Bordetella bronchiseptica, Pseudomonas aeruginosa, Burkholderia pseudomallei, Vibrio parahaemolyticus, Vibrio cholerae, Chlamydia trachomatis, Chlamydia pneumoniaeChlamydia psittaci.. The method of claim 1 , wherein the bacterium is selected from the group consisting of: claim 1 , and6. The method of claim 1 , wherein the bacterium is in a subject.7. The method of claim 6 , wherein the subject has a disease claim 6 , or is at risk of a disease claim 6 , caused by the bacterium.8. The method of claim 7 , wherein the disease is selected from the group consisting of: bubonic plague claim 7 , pneumonic plague claim 7 , septicemic plague claim 7 , enterocolitis claim 7 , mesenteric lymphadenitis claim 7 , typhlitis claim 7 , typhoid-like disease claim 7 , enteric fever claim 7 , intestinal inflammation claim 7 , bacteremia claim 7 , septicemia claim 7 , bloody diarrhea claim 7 , renal failure claim 7 , septic shock claim 7 , bacillary dysentery (shigellosis) claim 7 , sporadic dysentery claim 7 , whooping cough claim 7 , kennel cough claim 7 , atrophic rhinitis claim 7 , respiratory illness claim 7 , pneumonia claim 7 , chronic airway infection claim 7 , urinary tract infection claim 7 , clinical infections ...

SOLABEGRON ZWITTERION AND USES THEREOF

This application relates to solabegron zwitterion useful for the treatment of lower urinary tract symptoms such as, for example, overactive bladder and prostate disorders. Additionally, this application relates to pharmaceutical compositions and methods of treatment utilizing the solabegron zwitterion for treating lower urinary tract symptoms. This application also relates to methods of preparing solabegron hydrochloride from the solabegron zwitterion. 125-. (canceled)27. The process according to wherein the reaction vessel additionally contains isopropyl alcohol.32. The process according to further comprising coupling 3-nitrophenyl)boronic acid and methyl 3-bromobenzoate to form the biphenyl amine according to Formula V.3338.-. (canceled)40. A process for the preparation of solabegron hydrochloride comprising:a. coupling (3-nitrophenyl)boronic acid and methyl 3-bromobenzoate with a coupling agent to form 3′-amino-[1,1′-biphenyl]-3-carboxylate;b. contacting the 3′-amino-[1,1′-biphenyl]-3-carboxylate from step a. with (Z)-N-(2-chloroethyl)acetimidoyl chloride dichlorophosphate to form methyl (E)-3′-N-(2-chloroethyl)acetimiamido-[1,1′-biphenyl]-3-carboxylate hydrochloride;c. contacting the methyl (E)-3′-N-(2-chloroethyl)acetimiamido-[1,1′-biphenyl]-3-carboxylate hydrochloride of step b. with an saturated aqueous base to form 3′-(2′methl-4,5-dihydro-1H-imidazol-1-yl)-[1,1′]biphenyl-3-carboxylate;d. coupling the 3′-(2′methl-4,5-dihydro-1H-imidazol-1-yl)-[1,1′]biphenyl-3-carboxylate of step c. with (R)-3-chlorostyrene oxide to form methyl 3′-((2R)-2-(3-chlorophenyl)-7a-methyltetrahydroimidazo[2,1-b]oxazol-7(7aH)-yl)-[1,1′-biphenyl]-3-carboxylate;e. contacting the methyl 3′-((2R)-2-(3-chlorophenyl)-7a-methyltetrahydroimidazo[2,1-b]oxazol-7(7aH)-yl)-[1,1′-biphenyl]-3-carboxylate from step d with aqueous sodium hydroxide to form a sodium salt of solabegron;f. contacting the sodium salt of solabegron from step e. with hydrochloric acid to make a solabegron zwitterion as a ...

Novel cis-imidazolines

Formula (I) and the pharmaceutically acceptable salts and esters thereof, wherein X1, X2, X3,Y1, Y2 and R are described herein inhibit the interaction of MDM2 protein with a p53-like peptide and hence have anti proiferative activity.

Cis-imidazolines as inhibitors of mdm2

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to novel compounds of the formulae (I) and (II) and their pharmaceutically acceptable salts and esters wherein each Z 1 , Z 2 and Z 3 is chosen from series of (C 1 -C 6 )-alkoxy-group, -CH 2 OCH 3 and -CH 2 OCH 2 CH 3 , or one Z 1 , Z 2 or Z 3 means hydrogen atom, and each of two others is chosen independently from series (C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkoxy-group, -Cl, -Br, -F, -CF 3 , -CH 2 OCH 3 , -CH 2 OCH 2 CH 3 , -OCH 2 CH 2 R 1 , -CH 2 -morpholino, -OR 2 , -OCH 2 CF 3 , -OCH(CH 3 )CH 2 OH and -COOQ wherein Q is chosen from series hydrogen atom and (C 1 -C 6 )-alkyl, or one of Z 1 , Z 2 or Z 3 means hydrogen atom, and two others in common with carbon atoms and in combination with bonds between them and benzene cycle to which they are bound for a cycle chosen from 5- and 6-membered unsaturated cycles and 5- and 6-membered saturated cycles that comprise at least one oxygen atom as heteroatom, and wherein R 1 is chosen from series -F, -OCH 3 , -N(CH 3 ) 2 and unsaturated 5-membered cycles comprising at least one nitrogen or oxygen atom as heteroatom, and wherein R 2 means 3-6-membered saturated cycle, and each Y 1 and Y 2 is chosen independently from series -Cl, -Br, -NO 2 , -C≡N and -C≡CH, and their pharmaceutically acceptable salts and esters and wherein Z 4 is chosen from series (C 1 -C 2 )-alkyl, (C 1 -C 6 )-alkoxy-group, -OH, -SCH 3 , -CF 3 , -NO 2 , -COOQ 2 , -N(CH 3 ) 2 , -OCH 2 -phenyl, -Cl, -Br, -F, -OCH 2 COQ 1 , saturated 5- and 6-membered cycles comprising at least one heteroatom wherein heteroatom is chosen from nitrogen (N) and oxygen (O) atom, and wherein Q 1 is chosen from series, -OH, -NH 2 and -O(C 1 -C 6 )-alkyl; Q 2 is chosen from series hydrogen atom and (C 1 -C 6 )-alkyl; Y 1 and Y 2 are chosen independently from series -Cl, -Br, -NO 2 , -C≡N and -C≡CH under condition that if both Y 1 and Y 2 means -Cl then Z 4 doesn't means -Cl, and if both Y 1 and Y 2 mean -NO ...

Cis-imidazolines as mdm2 inhibitors

본 발명은 본원에 제공되는 의미를 가지며, MDM2 단백질과 p53 유사 펩티드의 상호작용을 저해하고 항증식 활성을 갖는, 화학식 I 및 화학식 II 에 따른 화합물 및 이들의 약학적으로 허용가능한 염 및 에스테르를 제공한다: The present invention provides compounds according to Formulas (I) and (II) and pharmaceutically acceptable salts and esters thereof having the meanings provided herein and inhibiting the interaction of MDM2 protein with p53-like peptide and having antiproliferative activity do: [화학식 I] [Formula I] [화학식 II] [Formula II] . . 이미다졸린, MDM2 저해제 Imidazolines, MDM2 inhibitors

Cis-imidazolines as mdm2 inhibitors

The present invention provides compounds according to formula I and formula II and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction of MDM2 prote in with a p53-like peptide and have antiproliferative activity (I) (II).</SDOAB >

Novel cis-imidazolines

화학식 I (식 중, X 1 , X 2 , X 3 , Y 1 , Y 2 및 R 은 본원에 기재됨) 및 이의 약학적으로 허용되는 염 및 에스테르는, MDM2 단백질과 p53-유사 펩타이드의 상호작용을 억제하고, 따라서 항증식 활성을 가진다. Formula I (wherein X 1 , X 2 , X 3 , Y 1 , Y 2 and R are described herein), and pharmaceutically acceptable salts and esters thereof, interacts with a MDM2 protein and a p53-like peptide. And therefore have antiproliferative activity.

Derivatives of 1, 4-bismethylene cyclohexane and 1, 4-bismethylene cyclohexadiene and processes of preparation

Aryl-substd. methylene-bis-imidazoline cpds. and analogues - useful as antimicrobial agents effective against Gram negative and positive bacteria

Heterocyclic cpds. of formula (I) (where X is O, S or alkylene; R1 is a phenyl, naphthyl or thienyl gp. with 0-3 substits, selected from halogen, CN, Ph, CF3, CF3O, CF3S, PhS, alkyl, alkoxy and divalent alkylene; Y is H or XR1, where the 2 XR1 gps. can be the same or different; R2 and R3 are H or alkyl opt. substd. by OH or halogen; A and B are alkylene or alkenylene, pref. CH2-CH2) are new. (I) are antimicrobial agents with high activity against Gram-positive and negative bacteria. They can be used as human or veterinary medicaments, disinfectants, preservatives, and animal growth promoters.

Ethereal N-terminal aminodiol amino acid derivatives as anti-hypertensive agents

Non-peptidyl compounds characterized generally as ethereal N-terminal aminodiol derivatives of amino acids are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein X is selected from oxygen atom and methylene; wherein R 1 is selected from methyl, ethyl, t-butyloxycarbonyl and 2-(N-piperidinyl)ethyl; wherein R 2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R 3 is selected from benzyl, phenethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R 4 and R 6 is independently selected from hydrido and methyl; wherein R 7 is cyclohexylmethyl; wherein R 8 is isobutyl; wherein each of R 9 and R 11 is hydrido; wherein m is zero or one and n is a number selected from zero through five; or a pharmaceutically-acceptable salt thereof; with the proviso that where m is zero, then R 5 is selected from imidazolemethyl, thiazolemethyl and isobutyl; and with the further proviso that when m is one, then R 5 is methyl or ethyl.

Acylamino-cephem-carboxylic acids and process for preparing them

IN WHICH R1, R2 and R3 represent hydrogen or lower alkyl groups and R1 and R2 may form together an alkylene group which may be substituted, R4 represents a linear or branched alkyl radical of 1 to 5 carbon atoms, a cyclo-alkyl radical of 3 to 7 carbon atoms which may be interrupted by heteroatoms, X represents a single bond or NH, A represents a phenylene or thienylene group which may be substituted and Y represents a single bond or oxygen, and their physiologically tolerated salts; the novel compounds have very good anti-bacterial properties. Acylamino-cephem-carboxylic acids of the general formula

Acylamino-cephem-carboxylic acids and process for preparing them

Imidazolidine compounds and their use as cxcr3 antagonists

Disclosed are novel compounds and a method of treating inflammatory diseases. The method comprises administering to an individual in need an effective amount of an imidazolidine compound represented by Structural Formula (1): and physiologically of pharmaceutically acceptable salts thereof.

New aminoamides and applications

Alpha-aryl-alpha-hydroxy-beta-imidazolinylpropionic acid amides, process for producing thereof, their use in medicaments and a pharmaceutical composition containing same

The present invention relates to novel alpha -aryl- alpha -hydroxy-ss-imidazolinylpropionamides of the general formula (I) <IMAGE> in which n, R<1> to R<4> and X have the meaning given in the description, a process for their preparation and their use in medicaments.

ANTIHYPERTENSIVE, N-TERMINAL ETHERAMINODIOLAMINO SYRADERIVES.

Ethereal N-terminal aminodiol amino acid derivatives as anti-hypertensive agents

Aminoalkylaminocarbonyl aminodiol amino acid derivatives as anti-hypertensive agents

Non-peptidyl compounds characterized generally as aminoalkylaminocarbonyl aminodiol derivatives of amino acids are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are of the formula wherein X is selected from oxygen atom and methylene; wherein each of R 1 and R 9 is independently selected from hydrido, methyl, ethyl, t-butyloxycarbonyl; and methoxymethylcarbonyl; wherein R 2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R 3 is selected from benzyl, phenethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R 4 and R 6 is independently selected from hydrido and methyl; wherein R 7 is cyclohexylmethyl; wherein R 8 is isobutyl; wherein each of R 11 and R 12 is hydrido; wherein m is zero or one and n is a number selected from zero through five; or a pharmaceutically-acceptable salt thereof; with the proviso that where m is zero, then R s is selected from imidazolemethyl, thiazolemethyl and isobutyl; and with the further proviso that when m is one, then R s is methyl or ethyl.

Imidazoline compounds

The imidazoline compound represented by structural formula (I) or pharmacologically acceptable salts thereof, and the imidazoline compound represented by structural formula (II). The compound (I) has a highly selective antagonistic activity against muscarine M3 receptors, particularly against muscarine M3 receptors of the respiratory tract, and hence is useful particularly as a preventive or therapeutic agent for diseases wherein muscarine M3 receptors participate, particularly chronic obstructive pulmonary disease and asthma. The compound (II) is useful as an intermediate for the preparation of the compound (I).

CIS- IMIDAXOLINAS

L a presente invención proporciona compuestos de la fórmula I y de la fórmula II asi como sales y ésteres farmacéuticamente aceptable de los mismos, que tienen las designaciones indicadas en la descripción y que inhiben la interacción de la proteina MDM2 con un péptido similar a p53 y que presentan una actividad antiproferativa. The present invention provides compounds of formula I and formula II as well as pharmaceutically acceptable salts and esters thereof, which have the designations indicated in the description and that inhibit the interaction of the MDM2 protein with a peptide similar to p53 and that present an antiprofessional activity.

Cis-imidazolines

Patent TW232011B

Imidazolinyl-ethyl-dithiocarbamic acid esters and process for their manufacture

Alpha-aryl-alpha-hydroxy-beta-imidazolinyl propionsyreamider

The present invention relates to novel alpha -aryl- alpha -hydroxy-ss-imidazolinylpropionamides of the general formula (I) <IMAGE> in which n, R<1> to R<4> and X have the meaning given in the description, a process for their preparation and their use in medicaments.

Multifunctional corrosion inhibitors

Corrosion inhibitors for ferrous metals are provided which afford protection from general corrosion and cracking-type corrosion, which inhibitors are reaction products of acylated polyamines and phosphate esters.

Alpha-Aryl-Alpha-hydroxy-Beta-imidazolinyl-propionamides

Imidazolin Derivatives and a Method for Producing the Same and a Therapeutic Agent for Maintaining Blood Pressure

(1) The imidazoline derivative represented by the following general formula (1) (see fig. I) where R1 is a substituent endowed with water solubility or fat solubility, particularly carboxyl group or carboxymethoxy group or a pharmaceutically acceptable salt thereof, (2) The method for producing the above-mentioned compound, and (3) A therapeutic agent containing as its active ingredient the above-mentioned imidazoline derivative or an imidazoline derivative wherein R1 indicated in the formula (1) is hydrogen atom. The imidazoline derivative set forth under (1) above is a novel substance; and this compound itself and its derivative having R1 as indicated in the general formula (1) is hydrogen atom are useful as a therapeutic agent for treatment of shock from the fall in blood pressure by virtue of their ability to remove excess NO which is the vascular endothelium-derived relaxing factor (EDRF).

Patent FR2138091A1

Cis-imidazolines as mdm2 inhibitors

Azoverbindungen sowie verfahren zur herstellung derselben

헤테로사이클릭 아미노산의 제조방법 및 이 방법으로 제조한 헤테로사이클릭 아미노산

본 발명은 특정 구조의 헤테로사이클릭 아미노산 및/또는 이의 염을 제조하는 방법에 관한 것으로서, 좀 더 구체적으로는 L-아미노산을 출발물질로 하여, 프탈릭-L-아미노산을 제조한 후, 이를 호프만 재배열 반응 및 탈보호화 반응을 연속적 또는 단속적(batch)으로 수행하여 (S)-디아미노알킬카복실산을 제조한 후, 이를 고리화 반응을 수행하여 특정 구조의 헤테로사이클릭 아미노산 및/또는 이의 염을 제조하는 방법에 관한 발명으로서, 제조 공정상 부반응이 생기질 않아서 추가로 정제공정이 불필요하며, 연속공정시 중간체를 분리 및 건조를 수행하지 않아도 되는 바, 공정 단축, 제조 원가 절감의 장점이 있으며 대량생산에 적용하기에 적합하다.

Cis-imidazoline als mdm2-hemmer

Imidazoline derivatives having CB1-antagonistic activity

The present invention relates to 1,2,4-tri-substituted imidazoline derivatives, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazoline derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these imidazoline derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula. (I) wherein the symbols have the meanings given in the specification.

Neuartige cis-imidazoline

一种妥尔油基咪唑啉琥珀酸酯磺酸盐表面活性剂的制备方法

本发明公开了一种妥尔油基咪唑啉琥珀酸酯磺酸盐表面活性剂的制备方法，包括以下步骤：在氮气保护下，将妥尔油酸羟乙基咪唑啉和酸升温至80～130℃搅拌1～60分钟脱水，降温至50～120℃，再加入亚硫酸盐、马来酸酐和催化剂反应1～5h，马来酸酐残留含量小于0.5％，降温至40～90℃，再加入亚硫酸盐和去离子水，温度为40～90℃的条件下反应1～5h，得到所述妥尔油基咪唑啉琥珀酸酯磺酸盐表面活性剂。本发明制备的妥尔油基咪唑啉琥珀酸酯磺酸盐常温下粘度较小，流动性好，产品易于使用，妥尔油酸羟乙基咪唑啉转化率高达95％以上。

一种妥尔油基咪唑啉琥珀酸酯磺酸盐表面活性剂的制备方法

本发明公开了一种妥尔油基咪唑啉琥珀酸酯磺酸盐表面活性剂的制备方法，包括以下步骤：在氮气保护下，将妥尔油酸羟乙基咪唑啉和酸升温至80～130℃搅拌1～60分钟脱水，降温至50～120℃，再加入亚硫酸盐、马来酸酐和催化剂反应1～5h，马来酸酐残留含量小于0.5％，降温至40～90℃，再加入亚硫酸盐和去离子水，温度为40～90℃的条件下反应1～5h，得到所述妥尔油基咪唑啉琥珀酸酯磺酸盐表面活性剂。本发明制备的妥尔油基咪唑啉琥珀酸酯磺酸盐常温下粘度较小，流动性好，产品易于使用，妥尔油酸羟乙基咪唑啉转化率高达95％以上。

改性咪唑啉季铵盐型沥青温拌剂及其制备方法

一种改性咪唑啉季铵盐型沥青温拌剂及其制备方法，按摩尔比计，称取以下组分：将摩尔比为1:1‑2的妥尔油、有机多胺加入到反应器中，加入总质量20％‑40％的携水剂，搅拌升温回流，在回流温度下发生酰胺化反应，反应温度120‑160℃，反应2h‑10h；将携水剂蒸出，抽真空度为0.09‑0.1MPa升温至230‑250℃进行环化反应1‑10h，制得咪唑啉中间体；将与咪唑啉中间体摩尔比1:1‑1.5的季胺化试剂制备质量分数为50％的乙醇溶液，缓慢滴加到咪唑啉中间体中，30‑60℃搅拌条件下反应4‑24h后，减压蒸出乙醇和未反应的季胺化试剂，得到沥青温拌剂。本发明的沥青温拌剂不含水，在反应过程中无需催化剂，可通过内掺及外掺两种方法添加，具有添加量低并且能显著降低沥青混合料拌和及压实温度30‑50℃。

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Imidazoline derivatives having CB1-antagonistic activity

The present invention relates to 1,2,4-tri-substituted imidazoline derivatives, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazoline derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these imidazoline derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.

Herbizide vinylaminderivate.

Verfahren zur aufhebung des durch optische aufheller erzielten aufhelleffektes

Verfahren zur Aufhebung des durch optische Aufheller erzielten Aufhelleffektes

Vinylaminderivater

Un procedimiento para preparar un derivado de amida amidinade un anhidrido poliaquenilsuccinico.

Aminodiolaminosyrederivater med etherisk n-terminal eller farmaceutisk acceptable salte deraf samt deres anvendelse som renininhibitorer

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Processo para a preparacao de derivados aminodiol n-terminais etereos de amino--acidos, uteis como agentes anti-hipertensivos

Acides acylamino-cepheme-carboxyliques et leur procede de preparation

Azo comound and a process for preparing the same

一种二氢咪唑类化合物的合成方法

本发明公开了一种二氢咪唑类化合物的合成方法，包括以α,β‑不饱和酮肟酯类化合物I、苯胺类化合物II和多聚甲醛III为反应原料，加入催化剂和碱性添加物，利用微通道模块化反应装置制备二氢咪唑类化合物IV，反应式如下。与现有技术相比，本发明以α,β‑不饱和酮肟酯类化合物、多聚甲醛和苯胺类化合物为底物制备新的二氢咪唑类化合物，使用廉价金属催化剂快速高效的合成产物。 其中，其中，R 1 、R 2 独立的选自非取代或取代的苯基，或噻吩基，所述取代的苯基选自被卤素、硝基、C1‑C5烷基或C1‑C5烷氧基取代的苯基。

Derive d'imidazoline, sa production, et agent de retention de la tension arterielle

一种钙皂分散剂月桂基乙酸钠型咪唑啉生产装置

一种钙皂分散剂月桂基乙酸钠型咪唑啉生产装置，主要包括：羟乙基乙二胺储罐、原料泵、真空泵、真空缓冲罐、环化反应釜、输送泵、季铵化反应釜、配料罐、成品泵；其中，羟乙基乙二胺储罐与原料泵相连接，原料泵与环化反应釜相连接，真空泵与真空缓冲罐相连接，真空缓冲罐分别与环化反应釜和季铵化反应釜相连接，环化反应釜与输送泵相连接，输送泵与季铵化反应釜相连接，季铵化反应釜与成品泵相连接，季铵化反应釜与原料泵相连接，原料泵与配料罐相连接；其中，羟乙基乙二胺储罐公称容积17—19L，全容积17.5—19.5L，筒体直径1850—1950mm,长度4500—5500mm,封头厚度10.5—11.5mm。

Processo para a preparacao de derivados aminodiol n-terminais etereos de amino--acidos, uteis como agentes anti-hipertensivos

Processo para a preparacao de derivados alquilaminocarbonil-aminodiol de amino--acidos, uteis como agentes anti-hipertensivos

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Amid-Amidinderivate der Polyalkenylbernsteinsaeure als Zusatzmittel fuer Schmieroeleund Kraftstoffe

Processo para a preparacao de derivados aminodiol n-terminais etereos de amino--acidos, uteis como agentes anti-hipertensivos

항고혈압제로서의 에테르성 n-말단 아미노디올 아미노산 유도체

내용 없음

Aminodiolaminosyrederivater med etherisk n-terminal eller farmaceutisk acceptable salte deraf samt deres anvendelse som renininhibitorer

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Dithiocarbamates a activite anthelminthique

Processo para a preparacao de derivados alquilaminocarbonil-aminodiol de amino--acidos, uteis como agentes anti-hipertensivos

Aminoalkylaminocarbonyl aminodiol amino acid derivatives as anti-hypertensive agents

Processo para a preparacao de derivados alquilaminocarbonil-aminodiol de amino--acidos, uteis como agentes anti-hipertensivos

Phenyl esters of (1-methyl-2-imidazolidinylidene)nitroacetic acids

Insecticidal phenyl esters of (1-methyl-2-imidazolidinylidene)nitroacetic acids.

一种妥尔油基咪唑啉琥珀酸酯磺酸盐表面活性剂的制备方法

本发明公开了一种妥尔油基咪唑啉琥珀酸酯磺酸盐表面活性剂的制备方法，包括以下步骤：在氮气保护下，将妥尔油酸羟乙基咪唑啉和酸升温至80～130℃搅拌1～60分钟脱水，降温至50～120℃，再加入亚硫酸盐、马来酸酐和催化剂反应1～5h，马来酸酐残留含量小于0.5％，降温至40～90℃，再加入亚硫酸盐和去离子水，温度为40～90℃的条件下反应1～5h，得到所述妥尔油基咪唑啉琥珀酸酯磺酸盐表面活性剂。本发明制备的妥尔油基咪唑啉琥珀酸酯磺酸盐常温下粘度较小，流动性好，产品易于使用，妥尔油酸羟乙基咪唑啉转化率高达95％以上。

改性咪唑啉季铵盐型沥青温拌剂及其制备方法

一种改性咪唑啉季铵盐型沥青温拌剂及其制备方法，按摩尔比计，称取以下组分：将摩尔比为1:1‑2的妥尔油、有机多胺加入到反应器中，加入总质量20％‑40％的携水剂，搅拌升温回流，在回流温度下发生酰胺化反应，反应温度120‑160℃，反应2h‑10h；将携水剂蒸出，抽真空度为0.09‑0.1MPa升温至230‑250℃进行环化反应1‑10h，制得咪唑啉中间体；将与咪唑啉中间体摩尔比1:1‑1.5的季胺化试剂制备质量分数为50％的乙醇溶液，缓慢滴加到咪唑啉中间体中，30‑60℃搅拌条件下反应4‑24h后，减压蒸出乙醇和未反应的季胺化试剂，得到沥青温拌剂。本发明的沥青温拌剂不含水，在反应过程中无需催化剂，可通过内掺及外掺两种方法添加，具有添加量低并且能显著降低沥青混合料拌和及压实温度30‑50℃。

一种二氢咪唑类化合物的合成方法

本发明公开了一种二氢咪唑类化合物的合成方法，包括以α,β‑不饱和酮肟酯类化合物I、苯胺类化合物II和多聚甲醛III为反应原料，加入催化剂和碱性添加物，利用微通道模块化反应装置制备二氢咪唑类化合物IV，反应式如下。与现有技术相比，本发明以α,β‑不饱和酮肟酯类化合物、多聚甲醛和苯胺类化合物为底物制备新的二氢咪唑类化合物，使用廉价金属催化剂快速高效的合成产物。 其中，其中，R 1 、R 2 独立的选自非取代或取代的苯基，或噻吩基，所述取代的苯基选自被卤素、硝基、C1‑C5烷基或C1‑C5烷氧基取代的苯基。

一种环氧树脂固化剂及其制备方法与应用

本发明属于高分子化学领域，具体涉及一种环氧树脂固化剂及其制备方法与应用。该环氧树脂固化剂，具有如式(Ⅰ)所示的结构式： 本发明先由一元或多元伯胺与含有特定结构的含有氨基和羧基结构的化合物反应、再由二聚酸或其他含有羧基的化合物与其缩聚而得到一种新型的环氧树脂固化剂，由于反应体系中可以生成咪唑林，因而使得该环氧树脂固化剂在涂料或胶黏剂领域应用时具有明显的力学性能优势。