ЗАМЕЩЕННЫЕ АМИДЫ ФЕНИЛЦИКЛОГЕКСАНКАРБОНОВОЙ КИСЛОТЫ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ И ЛЕКАРСТВЕННОЕ СРЕДСТВО НА ИХ ОСНОВЕ

Изобретение относится к замещённым амидам фенилциклогексанкарбоновой кислоты формулы (I) в которой A, D, Е и G одинаковы или различны и означают группу СН или атом азота, R1 означает группу СН2-ОН или остаток формулы CO-NH2, R2 означает алкил, содержащий 1-8 атомов углерода, который может быть прерван атомом кислорода, или пиперизин, содержащий остаток формулы NR4, где R4 означает водород, алкил, содержащий 1-6 атомов углерода, или циклоалкил, содержащий 3-7 атомов углерода, причем алкил, содержащий 1-8 атомов углерода, который может быть прерван атомом кислорода, замещен 1-3 гидроксильными группами или остатком формулы –NR5R6, где R5 и R6 означают водород, или вместе с атомом азота образуют кольцо морфолина, R3 означает фенильное кольцо, и их соли. Изобретение также относится к лекарственному средству, обладающему ингибирующим поглощением аденозина, на основе этих соединений. Технический результат – получение новых соединений и лекарственного средства на их основе в целях лечения ишемических ...

БЕНЗИМИДАЗОЛЬНЫЕ ПРОИЗВОДНЫЕ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

Настоящее изобретение относится к новым производным бензимидазола общей формулы (I) или к его фармакологически приемлемым солям, где R' представляет собой С6-арильную группу, которая может быть замещенной 1-3 группами, независимо выбранными из группы заместителей (а), или гетероциклическую группу, которая представляет пиридил, дигидробензофуранил, 1,3-бензодиоксолил, тетрагидропиранил, тетрагидрофуранил, которая может быть замещенной 1-3 группами, независимо выбранными из группы заместителей (а), R2 представляет собой C1-С6 алкильную группу, R3 представляет собой С6-арильную группу, которая может быть замещенной 1-2 группами, независимо выбранными из группы заместителей (a), Q представляет собой группу, представленную формулой =СН-, или атом азота и группа заместителей (а) представляет собой группу, состоящую из атома галогена, C1-С6 алкильной группы, C1-С6 галогенированной алкильной группы, карбоксильной группы, C1-C7 алкилкарбонильной группы, C2-C7 алкоксикарбонильной группы, C1-С6 алкоксигруппы ...

НОВЫЕ ПРОИЗВОДНЫЕ БЕНЗИМИДАЗОЛА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ЛЕКАРСТВЕННЫХ СРЕДСТВ

Настоящее изобретение относится к новым производным бензимидазола, имеющих общую формулу (I), где А обозначает -CH2-, -C(O), -C(O)-C(Ra)(Rb)-, Х обозначает -CH-радикал; Ra и Rb обозначают, независимо, атом водорода или (C1-C6)алкильный радикал; ! R1 обозначает атом водорода или (C1-C8)алкильный радикал; R2 обозначает ! (C1-С8)алкильный радикал; R3 обозначает -(CH2)p-Z3, -C(O)-Z'3 или -C(O)-NH-Z''3; Z3 обозначает (C1-C6)алкильный, (C2-C6)алкенильный, (C1-C6)алкокси, (C1-C6)алкилкарбонильный, (C1-C6)алкоксикарбонильный, ! (C1-C6)алкил-N(RN)карбонильный, (C3-C7)циклоалкильный, арильный, арилтио или гетероарильный радикал, Z3 присоединен к радикалу -(CH2)р- через атом углерода, гетероарильный радикал, представляющий собой 5-10-членный гетероарил, включающий 1-2 одинаковых или разных гетероатомов, выбранных из серы, азота или кислорода, и необязательно замещен одним или несколькими одинаковыми или разными заместителями, выбранными из галогена, нитрогруппы или -(CH2)p'-V30-Y3; арильный радикал ...

КОНДЕНСИРОВАННЫЕ 5-ЧЛЕННЫЕ ГЕТЕРОЦИКЛЫ ИЛИ ИХ СОЛИ, ПРОЯВЛЯЮЩИЕ АКТИВНОСТЬ ПО ТОРМОЖЕНИЮ АГРЕГАЦИИ

Использование: в качестве препаратов, проявляющих активность по торможению агрегации. Сущность изобретения: конденсированные 5-членные гетероциклы ф лы (1) с определенными буквенными значениями, проявляющие активность по торможению агрегации. 1 табл. (I).

АМИДО- ИЛИ КАРБАМИДО- ПРОИЗВОДНЫЕ, ИЛИ ИХ ФАРМАЦЕВТИЧЕСКИЕ СОЛИ И КОМПОЗИЦИЯ, ОБЛАДАЮЩАЯ ИНГИБИРУЮЩЕЙ АКТИВНОСТЬЮ В ОТНОШЕНИИ АЦИЛ-СОА:ХОЛЕСТЕРИН АЦИЛТРАНСФЕРАЗЫ

Предложены соединения формулы (I): где R1 означает алкильную группу; или группу формулы (II), (III), (IY) или (Y): и где R2, R3, R4 и R5 являются водородом или различными оорганическими группами; и их фармацевтически приемлемые соли; а также способы их получения и их использование при лечении и профилактике гиперхолестеремии и атеросклероза. 3 с. и 29 з.п. ф-лы, 32 ил., 12 табл.

НОВЫЕ ПРОИЗВОДНЫЕ БЕНЗИМИДАЗОЛА И ИМИДАЗОПИРИДИНАИ ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ЛЕКАРСТВЕННЫХ СРЕДСТВ

Соединение общей формулы (I) в рацемической, энантиомерной форме или в виде любых сочетаний указанных форм, где А обозначает -CH2-, -C(O)-, -C(O)-C(Ra)(Rb)-; X обозначает -CH-радикал или атом азота; Ra и Rb обозначают, независимо, атом водорода или (C1-C6)алкильный радикал; R1 обозначает атом водорода или (C1-C8)алкильный радикал; R2 обозначает (C1-C8)алкильный радикал; или R1 и R2 вместе с атомом азота, к которому они присоединяются, образуют гетеробициклоалкил или гетероциклоалкил, необязательно замещенный одним или несколькими идентичными или разными (C1-C6)алкильными заместителями; R3 обозначает -(CH2)p-Z3, -C(O)-Z'3, -CH(OH)-Z'3 или -C(O)-NH-Z"3; Z3 обозначает (С1-C6)алкильный, (С2-C6)алкенильный, (С1-C6)алкокси, (С1-C6)алкилкарбонильный, (С1-C6)алкоксикарбонильный, (С1-C6)алкил-N(RN)карбонильный, (С3-C7 )циклоалкильный, гетероциклоалкильный, арильный, арилтио или гетероарильный радикал, Z3 присоединен к радикалу -(CH2)p- через атом углерода, (C3-C7)циклоалкильный и гетероциклоалкильный ...

α-замещенные производные карбоновых кислот

... 1. α-Замещенное производное карбоновой кислоты общей формулы (II) где R1, R2 и R3 являются одинаковыми или различными, и каждый представляет собой (i) атом водорода, (ii) (C1-C6)-алкильную группу, (iii) (С6-С10)-арильную группу (необязательно содержащую 1-5 заместителей α1, имеющих значения, указанные далее), (iv) (C7-C16 )-аралкильную группу (необязательно содержащую в своей арильной части 1-5 заместителей α1, имеющих значения, указанные далее), (v) (C1-C6)-алкилсульфонильную группу, (vi) (C1-C6)-галогеналкилсульфонильную группу, (vii) (С6-С10)-арилсульфонильную группу (необязательно содержащую 1-5 заместителей α1, имеющих значения, указанные далее) или (viii) (C7-C16)-аралкилсульфонильную группу (необязательно содержащую в своей арильной части 1-5 заместителей α1, имеющих значения, указанные далее); А представляет собой атом азота или =СН-группу; В представляет собой атом кислорода или атом серы; W1 представляет собой (C1-С8)-алкиленовую группу; W2 представляет собой простую связь или ...

Способ получения производных бензимидазола или их солей

Способ получения производных ацилимидазола

Способ получения 2-замещенных производных 1-циннамилбензимидазола

Verfahren zur Herstellung von Benzimidazolylidenverbindungen

Verfahren zur Herstellung von 1-(tert.-Aminoaethyl)-2-(p-alkoxy-benzyl)-benzimidazolen

BENZIMIDAZOLDERIVATE MIT EINER WIRKUNG ALS ULKUSMITTEL.

AROYLPYRIDINONE

A Photographic Material containing a Colour Coupler

... 1,160,628. Benzimidazoles. AGFA-GEVAERT A.G. 20 Nov., 1967 [25 Nov., 1966], No. 52576/67. Heading C2C. [Also in Division G2] Benzimidazole colour couplers of formula (in which R is alkyleneoxy, alkylene or alkenylene; R 1 and R 2 are each H, alkyl, alkoxy or halogen; R 3 is aryl or aromatic heterocyclic, optionally substituted by alkyl, alkoxy, aryl, aryloxy, halogen, sulpho, halogen sulphonyl, organo-sulphonyl or acylamino; R 4 is alkyl optionally substituted by alkoxy, amino or hydroxyalkyl; R 5 is H, sulpho, alkyl, alkoxy, optionally substituted amido-sulphonyl, organosulphonyl or opt. esterified carboxyl; and n is 0 or 1) are prepared by reacting a (1-R 4 ), (4-R 5 )-ophenylene diamine with a p-(Cl-CO-R)- nitrobenzene and reducing the NO 2 group to give a compound of formula which is then reacted with either (i) an ester of formula C 2 H 5 OOC-CH 2 -COR 3 , (ii) a sulphonyl chloride of formula or (iii) a nitro substituted sulphonyl chloride to give a compound of formula which is then ...

Substituted 2-benzylbenzimidazole

The invention comprises 2-(2-hydroxybenzyl)-benzimidazole and its acid addition salts and the preparation thereof by reaction of 1,2-phenylenediamine with 2-hydroxyphenylacetic acid under acid conditions. Pharmaceutical formulations comprise the above compound and salts and a carrier. Tablets, capsules, cachets, ampoules, suppositories, solutions, suspensions and ointments are mentioned. The compound is antiviral.

IMPROVEMENTS IN OR RELATING TO BENZIMIDAZOLES

Improvements in or relating to benzimidazoles

Certain N-substituted benzimidazoles are disclosed. The compounds are potent antiviral agents. Pharmaceutical formulations containing such compounds and a method of treating viral infections are provided.

Trifluoroacetoxy-alkenyl benzimidazoles

The invention comprises compounds of the general formula and the CF3COOH addition salts of compounds of the general formula wherein each of R1 and R2 is H, CF3 or a C1- 5 alkyl or alkoxy radical, R3 is H or a C1- 5 alkyl radical and R5 is H or CF3CO-. The compounds are prepared by treating a compound of the formula with (CF3CO)2O in the presence of a catalytic amount of a sulphonic acid to produce a compound of the formula which compound may be subsequently hydrolysed to give a compound of the formula or hydrolysed and neutralized to give a compound of the formula ...

ACYLIMIDAZOLES

... 1291614 Acylimidazoles FARBENFABRIKEN BAYER AG 14 May 1970 [22 May 1969 12 Nov 1969] 23408/70 Heading C2C Novel acylimidazoles of the general formula wherein R is a tertiary alkyl, halo-, nitro- or amino-alkyl, alkoxy, alkylthio, dialkylamino, aryloxy, arylthio, phenyl, halo-, nitro-, amino-, alkoxy-, or hydroxy-phenyl, naphthyl, cycloalkyl, pyridyl, pyrazolyl, oxazolyl, thiadiazolyl, furyl or thienyl radical, or a group of the formula wherein A is a direct bond or a -CO-, -COCH 2 - or -COC 6 H 4 - group, R1 is an alkyl, aralyl or aryl radical which may be substituted by halogen, nitro, cyano or alkyl groups, X and Y are halogen, hydrogen, alkyl, haloalkyl, phenyl or halophenyl or, together with the -CH=CH- group between them, represent a benzene ring, are prepared by reacting an imidazole derivative of the general formula with a compound of the formula R11-CO-Z, wherein R11 is a halogen, halocarbonyl, halocarbonylmethyl or halocarbonylphenyl, or is the same as ...

Improvements relating to the production of benzimidazolylidene compounds and the resulting products

Benzimidazolylidene compounds are prepared by condensing a benzimidazole-2-aldehyde, unsubstituted in the benzene ring, with an organic compound containing an activated methyl or methylene group and having the general formula X-CH2-Y as hereinafter defined, if necessary in the presence of an acid or basic condensation catalyst, with splitting off of water. The organic compounds containing an activated methyl or methylene group are those in which X represents an electrophilic group such as a carbonyl, carboxyl, carboxylic ester, carboxylic amide, cyano, nitro or organic ammonium group, an aromatic-heterocyclic containing tertiary nitrogen, or a negatively substituted-aromatic isocyclic radical, and Y represents hydrogen, an inert organic group or an electrophilic group. Specified compounds include acetophenone, phenylacetic acid, benzyl cyanide, cyano acetic esters and amides, open and cyclic 1:3-diketones, malonic esters and amides including cyclic amides such as 1:3-diketo pyrazolidines ...

Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents

Benzoheterocycles and their use mek inhibitors

ARYL AND HETEROARYL ETHER COMPOUNDS AS ROR GAMMA MODULATORS

Substituted 4-hydroxy-phenylalcanoic acid derivatives with agonist activity to ppar-gamma

Substituted 4-hydroxy-phenylalcanoic acid derivatives with agonist to PPAR-gamma.

A compound having formula (I), wherein A is selected from the group consisting of: (i) phenyl, wherein said phenyl is optionally substituted by one or more halogen atoms, C1-6alkyl, C1-3alkoxy, C1-3fluoroalkoxy, nitrile, or -NR7R8 where R7 and R8 are independently hydrogen or C1-3alkyl; (ii) a 5- or 6-membered heterocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur; and (iii) a fused bicyclic ring (a), wherein ring C represents a heterocyclic group as defined in point (ii) above, which bicyclic ring is attached to group B via a ring atom of ring C; B is selected from the group consisting of: (iv) C1-6alkylene; (v) -MC1-6alkyiene or C1-6alkyleneMC1-6alkylene, wherein M is O, S, or-NR2 wherein R2 represents hydrogen or C1-3 alkyi; (vi) a 5-or 6-membered heterocyclic group containing at least one nitrogen heteroatom and optionally at least one further heteroatom selected from oxygen, nitrogen and sulfur and optionally substituted by C1-3 alkyl; and ( ...

Benzimidazole compounds.

A range is disclosed of benzimidazole-4-carboxamide compounds (I) which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DMA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. In formula (I), R and R' may each be selected independently from hydrogen, alkyl, hydroxyalkyl (e.g. CH2CH2OH), acyl (e.g. acetyl or benzoyl) or an optionally substituted aryl (e.g. phenyl) or aralkyl (e.g. benzyl or carboxybenzyl) group. R is generally a substituted phenyl group in the most preferred compounds. The compounds may also be used in the form of pharmaceutically acceptable salts or pro-drugs.

ARYL AND HETEROARYL ETHER COMPOUNDS AS ROR GAMMA MODULATORS

Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents.

This invention provides a compound of the formula (i); or the pharmaceutically acceptable salts thereof, wherein y1, y2, y3, and y4 are independently selected from n, ch, etc., r1 is h, c1-8 alkyl, etc., q1 is 5-12 membered monocyclic or bicyclic aromatic ring optonally containing up to 4 heteroatoms selected from o,n and s,etc., a is a 5-6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected from o,n and s,etc.;B is c1-6 alkylene optionally substituted with an oxo group, etc.; w is nh, o, etc.; r2 is h,c1-4 alkyl, etc.; z is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected from o,n and s, etc.; l is halo, c1-4 alkyl,,etc.; m is0, 1 or 2; r3 and r4 are independently selected from o,n and s, etc.; l is halo, c1-4 alkyl ; r5 is h, c1-4 alkyl, etc.; q2 is a 5-12 membered monocyclic or bicyclic aromatic ring ortricyclic ring optionally containing up to 3 heteroatoms selected from o, n and s, etc. These compounds ...

Chemical compounds

Benzimidazole compounds

EP4 receptor inhibitors to treat rheumatoid arthritis.

The invention features a method of treating rheumatoid arthritis in a mammal comprising administering an agent that inhibits prostaglandin ep4 receptor (EP4) activity. Also featured is a method of identifying agents that selectively inhibit EP4 activity in vivo.

Benzoheterocycles and their use as MEK inhibitors.

The invention provides compounds having formula (I), wherein W is OH, or derivatives of the carboxylic acid, and Q is a heterocyclo-condensed ortho-phenylene residue. These compounds are useful as MEK inhibitors, particularly in the treatment of proliferative diseases such as cancer.

Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents

Benzimidazole compounds

Ep-4 receptor inhibitors to treat rheumatoid arthritis.

Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents.

Derived from hétérocyclyl-carboxylic acids acylés and proceeded for their preparation.

Benzoheterocycles and their use as MEK inhibitors.

System of adjustment of the tension of an alternator.

Method of preparation of isothiocyano-benzazoles.

3Ep4 receptor inhibitors to treat rheumatoid arthritis

Chemical compounds

Benzimidazole compounds

ARYL AND HETEROARYL ETHER COMPOUNDS AS ROR GAMMA MODULATORS

3Ep4 receptor inhibitors to treat rheumatoid arthritis

Benzoheterocycles and their use mek inhibitors

BIARYLSULFONAMIDE AS MMP INHIBITORS

PROCEDURE FOR THE PRODUCTION OF NEW BENZ-ACYLBENZIMIDAZOL-2-DERIVATE AND YOUR SALTS

VERFAHREN ZUR HERSTELLUNG VON NEUEN IMIDAZOLYL- (2) -CARBINOLEN UND IHREN SALZEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN PYRIMIDINVERBINDUNGEN UND DEREN SAEUREADDITIONSSALZEN

DIAMINOCYCLOHEXANUND DIAMINOCYCLOPENTANDERIVATE

4-ARYL SUBSTITUTED CHINOLE AND ANALOGUES AS THERAPEUTIC ACTIVE SUBSTANCES

MONOUND BICYCLI AZOLDERIVATE THE INTERACTION OF LIGANDS WITH RISES UP RESTRAINING

REGIOSELEKTIVE, PALLADIUM-CATALYZED SYNTHESIS OF BENZIMIDAZOLEN AND AZABENZIMIDAZOLEN

PROCEDURE FOR THE PRODUCTION OF NEW BENZIMIDAZOLDERIVATE

PROCEDURE FOR THE PRODUCTION OF NEW BENZIMIDAZOLDERIVATE

PROCEDURE FOR the PRODUCTION OF NEW ONE 2-CARBOXAMIDO-SUBSTITUIERTEN TETRACYCLINEN

PROCEDURE FOR THE PRODUCTION OF NEW BENZIMIDAZOL-2 - DERIVATIVES AND YOUR SALTS

HETEROZYCLI KETONEN AS NPY Y5 ANTAGONIST

BENZEN, PYRIDIN, PYRIMIDINDERIVAT

BENZIMIDAZOLE, THESE CONNECTIONS CONTAINING DRUGS AND PROCEDURES FOR YOUR PRODUCTION

SUBSTITUTED ACETOPHENONE, THEIR PRODUCTION AND PHARMACEUTICAL PREPARATIONS, IT CONTAINING.

NAPHTHYLPROPIONSAEUREDERIVATE.

MORE ARYLARALKYLETHER, PROCEDURES FOR THEIR PRODUCTION AND THIS CONTAINING PHARMACEUTICAL COMPOSITION.

PROCEDURE FOR THE PRODUCTION OF NEW BENZ-ACYLBENZIMIDAZOL-2-DERIVATE AND YOUR SALTS

IMIDAZOPYRIDINDERIVATE, PROCEDURE FOR THEIR PRODUCTION AND THEIR APPLICATION

BENZIMIDAZOL PHOSPHONO AMINO ACID

VERFAHREN ZUR HERSTELLUNG NEUER BENZIMIDAZOLDERIVATE

SUBSTITUTED PHENOXIALKANCARBONSAEUREDERIVATE, PROCEDURES FOR YOUR PRODUCTION AND YOUR USE AS HERBICIDES.

GALLIUM III COMPLEXES, PROCEDURE FOR YOUR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS, IT CONTAINING

USE OF 4-HYDROXY OR 4-AMINOBENZIMIDAZOL OR ITS DERIVATIVES AS SUCH AS KUPPLER SUBSTANCES IN OXIDATION COLOURING COMPOSITIONS, AS WELL AS COMPOSITIONS AND PROCEDURES FOR THEIR APPLICATION

PROPAN-1,3-DION-DERIVATE

HETERO-CYCLIC OXIMDERIVATE, PROCEDURES FOR YOUR PRODUCTION AND USE IN THE TREATMENT OF TYPE [...] DIABETES

TRISUBSTITUTED PHENYLDERIVATE AS PHOSPHODIESTERASEINHIBITOREN

FLUORINE COMPOUNDS AS FLAVORS SE INHIBITORS

BENZIMIDAZOLDERIVATE

INTEGRIN RECEPTOR ANTAGONIST

Procedure for the production of new Acylimidazolen and their salts

DISUBSTITUIERTE BICYCLI HETEROCYCLEN WITH IN PARTICULAR A THROMBINHEMMENDE EFFECT

PROCEDURE FOR THE PRODUCTION OF 2 - ARYLBENZIMIDAZOLSULFONSÄUREN

ANGIOTENSIN II ANTAGONIST

New heterocyclic oxime compounds, a process for their preparation and pharmaceutical compositions containing them

TRANSCRIPTION FACTOR MODULATING COMPOUNDS AND METHODS OF USE THEREOF

NOVEL COMPOUNDS

Medicinal composition for inhibiting amyloid-beta protein deposition

Use of substituted 2-amidobenzimidazoles, 2-amidobenzoxazoles and 2-amidobenzothiazoles or salts thereof as active substances against abiotic plant stress

The invention relates to the use of substituted 2-amidobenzimidazoles, 2-amidobenzoxazoles and 2-amidobenzothiazoles of general formula (I) or the salts thereof, the groups in general formula (I) corresponding to the definitions cited in the description, for increasing the stress tolerance of plants to abiotic stress, for strengthening plant growth and/or for increasing the plant yield. The invention also relates to specific methods for producing said compounds.

5-(4-(DIARYLMETHYL)-1-PIPERAZINYL-ALKYL)BENZIMIDAZOLE DERIVATIVES

Benzimidazole derivatives as inhibitors of smooth muscle cell proliferation

Symmetrical bis-heteroarylmethoxyphenylalkyl carboxylates as inhibitors of leukotriene biosynthesis

Bioreductive cytotoxic agents

FURAN DERIVATIVES

New benzimidazole, benzoxazole and benzothiazole compounds, aprocess for their preparation and pharmaceutical compositions containing them

HETEROCYCLIC COMPOUNDS

PROCESS FOR THE PREPARATION OF NOVEL 5-ALKYL-BENZ- IMIDAZOLE-DERIVATIVES

Novel benzimidazole-2 derivatives of the formula (I) wherein R1 denotes alkyl containing 1 to 7 carbon atoms, R2 denotes hydrogen or alkyl containing 1 to 4 carbon atoms, R3 denotes hydrogen or alkyl containing 1 to 4 carbon atoms and R denotes carboxy, alkoxycarbonyl, wherein alkoxy contains 1 to 4 carbon atoms, with the proviso that R1 differs from methyl or R3 differs from 6-methyl, when R is carboxyl or hydroxymethyl and R2 is hydrogen and pharmaceutically usable salts of compounds of the formula I with salt-forming properties are disclosed as medicaments. Pharmaceutical preparations containing these compounds and their use as anti-allergic agents are also disclosed. The novel compounds can be manufactured by methods known per se and suitable such methods are described.

CHLOROANILINE DERIVATIVES

CHLOROANILINE DERIVATIVES The invention provides compounds of the general formula (I) (I) and physiologically acceptable salts and solvates thereof, wherein Q represents a chlorine atom or a trifluoromethyl group; X represents a bond, or a C1-6alkylene, C2-6alkenylene or C2-6alkynylene chain, and Y represents a bond, or a C1-6alkylene, C2-6alkenylene or C2-6alkynylene chain with the proviso that the sum total or carbon atoms in the chains X and Y is not more than 10, and the chains XCH2 and CH2Y may each be optionally substituted by one or two C1-3alkyl groups, or, when one carbon atom is substituted by two alkyl groups, these may be linked to form an alkylene group; R represents a hydrogen atom or a C1-3alkyl group; R1 and R2 each represent a hydrogen atom or a C1-3alkyl group, with the proviso that the sum total of carbon atoms in R1 and R2 is not more than 4; and Het represents a benzoheteroaryl or a monocyclic heteroaryl group wherein the heteroaryl group is 5 or 6 membered and ...

2-BENZYL AND 2-HETEROARYL BENZIMIDAZOLE NMDA/NR2B ANTAGONISTS

Novel benzimidazoles, substituted in the 2-position by substituted benzyl groups or heteroaryl groups are effective as NMDA NR2B antagonists and are useful for relieving pain.

PREPARATION PROCESS OF NOVEL - MERCAPTOPROPANAMIDE DERIVATIVES AND DERIVATIVES THUS OBTAINED

NOVEL HETEROARYL DERIVATIVE

Disclosed are a heteroaryl derivative represented by the formula (1) below, a prodrug thereof, and their pharmaceutically acceptable salts. (1) (In the formula, ring Z represents a heteroaryl which may be substituted; R1 represents a carboxyl group, alkoxycarbonyl group or the like; W1 and W2 respectively represent a lower alkylene which may be substituted; Ar1 represents an arylene which may be substituted or a heteroarylene which may be substituted; W3 represents a single bond, a lower alkylene, a lower alkenylene or the like; W4 represents a single bond, -NR10- or the like; and Ar2 represents an aryl which may be substituted or a heteroaryl which may be substituted.) ...

2-(2-Hydroxybiphenyl-3-yl)-1H-Benzoimidazole-5-Carboxamidine Derivatives as Factor VIIA Inhibitors

The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.

NOVEL CANNABINOID RECEPTOR 2 (CB2) INVERSE AGONISTS AND THERAPEUTIC POTENTIAL FOR MULTIPLE MYELOMA AND OSTEOPOROSIS BONE DISEASES

Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: 3. The compound according to claim 2 , wherein R′″ is (C-C)heterocycloalkyl.4. The compound according to claim 3 , wherein R′″ is oxetanyl claim 3 , tetrahydrofuranyl claim 3 , tetrahydropyranyl claim 3 , oxepanyl claim 3 , tetrahydrothiophenyl claim 3 , tetrahydrothiopyranyl claim 3 , 1 claim 3 ,3-dioxanyl claim 3 , oxazolidinyl claim 3 , azetidinyl claim 3 , pyrrolidinyl claim 3 , piperidinyl claim 3 , azepinyl claim 3 , piperazinyl claim 3 , morpholinyl claim 3 , tetrahydrothiopyranyl-1-oxide claim 3 , tetrahydrothiopyranyl-1 claim 3 ,1-dioxide claim 3 , pyrrolidinonyl claim 3 , piperidinonyl claim 3 , azepinonyl claim 3 , piperazidinonyl claim 3 , oxazidilinonyl claim 3 , azetidinonyl claim 3 , or morpholinonyl.7. (canceled)8. The compound according to claim 1 , wherein the compound conforms to Formula I′ and whereinD is H;D′ is phenyl;{'sub': 1', '6, 'B and Q are independently (C-C)alkylene;'}e is 0 and each of f and g is 1; and{'sup': a′', 'a″', 'a′″, 'sub': 1', '6, 'each of R, R, and R is independently selected from the group consisting of H, and straight or branched chain (C-C)alkyl.'}10. (canceled)12. The compound according to claim 11 , wherein subscripts h and k independently are 0 and subscript j is 1.14. (canceled)16. The compound according to claim 15 , wherein substituent X is N claim 15 , T and R are each independently S(O)— and Q′ is (C-C)alkyl.17. The compound according to claim 15 , wherein substituent X is CH— and each of Q′ claim 15 , R and T are independently —O—(CH)—O— claim 15 , —OC(O)— or (CH)—OC(O)—.2022-. (canceled)23. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier.24. (canceled)25. A method for treating multiple myeloma or osteoporosis in a subject by ...

PROCESS FOR THE PREPARATION OF BENDAMUSTINE

The present invention relates to a method for preparation of alkyl 4-[5-[bis(2-hydroxyethyl)amino]-1-methyl-1H-benzimidazol-2-yl]butanoate (7) from 2-fluoro-5-nitroaniline, comprising the steps of: (a) conversion of 2-fluoro-5-nitroaniline to 5-(2-fluoro-5-nitroanilino)-5-oxopentanoic acid (1) using glutaric anhydride, conversion of compound (1) to methylammonium 5-[2-(methylamino)-5-nitroanilino]-5-oxopentanoate (2) using methylamine; conversion of compound (2) to 5-[2-(methylamino)-5-nitroanilino]-5-oxopentanoic acid (3) and condensation of compound (3) to 4-(1-methyl-5-nitro-1H-benzimidazol-2-yl)butanoic acid (4); (b) esterification of the product (4) of step a) to alkyl 4-(1-methyl-5-nitro1H-benzimidazol-2-yl)butanoate (5); (c) reduction of the product of step b) to alkyl 4-(5-amino-1-methyl-1H-benzimidazol-2-yl)butanoate (6), and (d) conversion of the product of step c) to alkyl 4-[5-[bis(2-hydroxyethyl)amino]-1-methyl-1H-benzimidazol-2-yl]butanoate (7) 2. The method according to claim 1 , wherein steps a) to d) are performed in a single process step without isolation of the reaction products.3. The method according to claim 1 , wherein tetrahydrofuran is used as solvent.5. The method according to claim 4 , wherein the amount of said strong acid in step e) is from 10-90% in relation to the amount of substance of the product 4-(1-methyl-5-nitro-1H-benzimidazol-2-yl)butanoic acid (4) of step d).6. The method according to claim 4 , wherein steps a) to e) are performed in a single process step without isolation of the reaction products.8. The method according to claim 7 , wherein said reduction is performed with hydrogen using an iron-doped palladium catalyst.9. The method according to claim 8 , wherein an iron (II) or iron (III) salt of an organic or inorganic acid is added to said iron-doped palladium catalyst.11. The method according to claim 10 , wherein the alkylation is performed with ethylene oxide or a 2-haloethanol12. The method according to claim 11 , ...

Methods of Synthesizing Substituted Purine Compounds

The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure. 2. The crystalline form of claim 1 , characterized by an X-ray powder diffraction (XRPD) pattern comprising peaks at about 16.5 claim 1 , 20.5 claim 1 , and 5.2° 2θ using Cu Kα radiation.3. The crystalline form of claim 2 , characterized by an XRPD pattern comprising peaks at about 16.5 claim 2 , 20.5 claim 2 , 5.2 claim 2 , and 14.2° 2θ using Cu Kα radiation.4. The crystalline form of claim 3 , characterized by an XRPD pattern comprising peaks at about 16.5 claim 3 , 20.5 claim 3 , 5.2 claim 3 , 14.2 claim 3 , 18.0 claim 3 , and 10.4° 2θ using Cu Kα radiation.5. The crystalline form of claim 1 , characterized by an XRPD pattern comprising at least three peaks selected from the group consisting of about 16.5 claim 1 , 20.5 claim 1 , 5.2 claim 1 , 14.2 claim 1 , 18.0 claim 1 , 10.4 claim 1 , 12.3 claim 1 , 10.0 claim 1 , 22.7 claim 1 , and 20.9° 2θ using Cu Kα radiation.612-. (canceled)13. The crystalline form of claim 1 , characterized by an XRPD pattern comprising peaks at about 5.5 claim 1 , 16.9 claim 1 , and 16.6° 2θ using Cu Ku radiation.14. The crystalline form of ...

BENZIMIDAZOLE DERIVATIVES AS SELECTIVE BLOCKERS OF PERSISTENT SODIUM CURRENT

The present invention is directed to a compound of Formula I 2. The compound of claim 1 , wherein R is and unsubstituted straight chain or branched Calkyl.3. The compound of claim 1 , wherein R is Calkyl which is substituted with a Caryloxy group.4. The compound of claim 3 , wherein the “aryl” portion of said Caryloxy group is unsubstituted or substituted with 1-2 Calkyl or Calkoxy substitutents.5. The compound of claim 1 , wherein R is Calkyl which is substituted with a heteroaryl substitutent claim 1 , wherein said heteroaryl group is five- to six-membered ring containing 1-2 ring N atoms claim 1 , and wherein when said five- to six-membered ring containing 1-2 ring N atoms has two substituents on adjacent carbon atoms claim 1 , said substituents together with the carbon atoms to which they are attached can optionally form a phenyl ring claim 1 , and wherein said six-membered ring containing 1-2 ring N atoms claim 1 , optionally with said phenyl ring is optionally further substituted with a ring system substituent.6. The compound of claim 5 , wherein said five- to six-membered ring containing 1-2 ring N atoms claim 5 , optionally with said phenyl ring is selected from the group consisting of pyrazolyl claim 5 , imidazolyl claim 5 , pyrimidinyl claim 5 , pyrazinyl claim 5 , and benzimidazolyl.7. The compound of claim 6 , wherein said five- to six-membered ring containing 1-2 ring N atoms claim 6 , optionally with said phenyl ring is selected from the group consisting of is imidazolyl and benzimidazolyl.8. The compound of claim 1 , wherein R is Calkyl which is substituted with a —N(Calkyl)substituent.10. The compound of claim 1 , wherein Rand Rare both H.11. The compound of claim 10 , wherein m is 1 or 2.12. The compound of claim 10 , wherein m is 1 claim 10 , and X is O.13. The compound of claim 10 , wherein m is 2 claim 10 , and X is a covalent bond.14. The compound of claim 10 , wherein m is 1 claim 10 , and X is —S(═O)—.15. The compound of claim 10 , wherein m ...

METHODS OF SYNTHESIZING SUBSTITUTED PURINE COMPOUNDS

The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning calorimetry profile, as well as a unique crystalline structure. 2. The crystalline form of claim 1 , characterized by an X-ray powder diffraction (XRPD) pattern comprising peaks at about 16.5 claim 1 , 20.5 claim 1 , and 5.2° 2θ using Cu Kα radiation.3. The crystalline form of claim 2 , characterized by an XRPD pattern comprising peaks at about 16.5 claim 2 , 20.5 claim 2 , 5.2 claim 2 , and 14.2° 2θ using Cu Kα radiation.4. The crystalline form of claim 3 , characterized by an XRPD pattern comprising peaks at about 16.5 claim 3 , 20.5 claim 3 , 5.2 claim 3 , 14.2 claim 3 , 18.0 claim 3 , and 10.4° 2θ using Cu Kα radiation.5. The crystalline form of claim 1 , characterized by an XRPD pattern comprising at least three peaks selected from the group consisting of about 16.5 claim 1 , 20.5 claim 1 , 5.2 claim 1 , 14.2 claim 1 , 18.0 claim 1 , 10.4 claim 1 , 12.3 claim 1 , 10.0 claim 1 , 22.7 claim 1 , and 20.9° 2θ using Cu Kα radiation.6. The crystalline form of claim 1 , characterized by an XRPD pattern comprising at least four peaks selected from the group consisting of about 16.5 claim 1 , 20.5 claim 1 , 5.2 claim 1 , 14.2 claim 1 , 18.0 ...

ARYL AND HETEROARYL ETHER COMPOUNDS AS ROR GAMMA MODULATORS

The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein Ring A, Ring B, R, R, R, n, and p are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (RORγt). These compounds prevent, inhibit, or suppress the action of RORγt and are therefore useful in the treatment of RORγt mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer. 157-. (canceled)59. The compound according to claim 58 , wherein R is —CH.60. The compound according to claim 58 , wherein ‘p’ is 0.63. The compound according to claim 58 , wherein Ris —F claim 58 , —Cl claim 58 , —CH claim 58 , —CHCH claim 58 , —CH(CH) claim 58 , —CF claim 58 , —OCF claim 58 , —OCF claim 58 , —CN or 4-chlorophenyl; and ‘n’ is 1 claim 58 , 2 or 3.71. The compound according to claim 70 , wherein Ris —F claim 70 , —Cl claim 70 , —CH claim 70 , —CHCH claim 70 , —CH(CH) claim 70 , —CF claim 70 , —OCF claim 70 , —OCF claim 70 , —CN or 4-chlorophenyl; and ‘n’ is 1 claim 70 , 2 or 3.74. The compound according to claim 73 , wherein{'sup': '1', 'Xis N, CH or CF;'}Ring B is phenyl;{'sup': '2', 'sub': 3', '2', '3, 'Ris —F, —Cl, —CF, —OCF, —OCFor —CN;'}‘n’ is 1, 2 or 3; and{'sup': c', 'd, 'Rand Rare independently selected from hydrogen and methyl.'}76. The compound according to claim 58 , selected from2-[4-(Ethylsulfonyl)phenyl]-N-(1-methyl-2-{2-[4-(trifluoromethyl) phenoxy]propan-2-yl}-1H-benzimidazol-5-yl)acetamide;N-{2-[2-(3,4-Difluorophenoxy)propan-2-yl]-1-methyl-1H-benzimidazol-5-yl}-2-[4-(ethylsulfonyl)phenyl]acetamide;N-{2-[1-(4-Chloro-2-fluoro-phenoxy)-1-methyl-ethyl]-1-methyl-1H-benzoimidazol-5-yl}-2-(4-ethanesulfonyl-phenyl)-acetamide;N-{2-[2-(2,4-Dichlorophenoxy)propan-2-yl]-1-methyl-1H-benzimidazol-5-yl}-2-[4-(ethylsulfonyl)phenyl]acetamide;N-{2-[2-(3,4-Dichlorophenoxy)propan-2-yl ...

METHODS OF TREATING A FLAVIVIRIDAE FAMILY VIRAL INFECTION, COMPOSITIONS FOR TREATING A FLAVIVIRIDAE FAMILY VIRAL INFECTION, AND SCREENING ASSAYS FOR IDENTIFYING COMPOSITIONS FOR TREATING A FLAVIVIRIDAE FAMILY VIRAL INFECTION

Briefly described, embodiments of this disclosure include compositions, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of identifying a candidate agent for the treatment of hepatitis C virus (HCV) infection, and the like. 1. A method of treating a host infected with a virus from the Flaviviridae family of viruses , the method comprising administering to the host a therapeutically effective amount of an inhibiting agent to reduce the viral load in the host.2. The method of claim 1 , wherein the Flaviviridae family of viruses includes viruses selected from the group consisting of: a flavivirus claim 1 , a pestivirus claim 1 , a Hepatitis C virus claim 1 , a yellow fever virus (YFV); a Dengue virus; a Japanese Encephalitis virus; a Murray Valley Encephalitis virus; a St. Louis Encephalitis virus; a West Nile virus; a tick-borne encephalitis virus; a Hepatitis C virus; a Kunjin virus; a Central European encephalitis virus; a Russian spring-summer encephalitis virus; a Powassan virus; a Kyasanur Forest disease virus; and a Omsk hemorrhagic fever virus.3. The method of claim 1 , wherein the virus is Hepatitis C virus.4. The method of claim 1 , wherein the inhibiting agent is selected from the group consisting of: clemizole claim 1 , a clemizole analog claim 1 , and a compound having a clemizole scaffold; an H1 antagonist claim 1 , an H1 receptor antagonist that share structural similarity with clemizole; cinoxacin claim 1 , a cinoxacin analog claim 1 , and a compound having a cinoxacin scaffold; norepinephrine claim 1 , a norepinephrine analog claim 1 , and a compound having a norepinephrine scaffold; glybenclamide claim 1 , a glybenclamide analog claim 1 , and a compound having a glybenclamide scaffold; spiradoline claim 1 , a spiradoline analog claim 1 , and a compound having a spiradoline scaffold; tropicamide claim 1 , a tropicamide analog claim 1 , and a compound having a tropicamide ...

Organometallic compound and organic light-emitting device including same

Provided are an organometallic compound represented by Formula 1 and an organic light-emitting device including the organometallic compound. The organic light-emitting device includes; a first electrode; a second electrode facing the first electrode; an organic layer between the first electrode and the second electrode and comprising an emission layer; and at least one of the organometallic compound represented by Formula 1.

BENZIMIDAZOLE DERIVATIVES AND USES THEREOF

Benzimidazole derivatives of Formula I, that modulate the activity of ACSS2 are disclosed for therapeutic use. The fused imidazole ring of the compounds disclosed has a diarylmethyl or diarylmethanol moiety attached at the 2-position and the as compounds have at least one other substituent at the 5 or 6 position of the benzimidazole. Also disclosed are methods of using the benzimidazole compounds for the treatment of diseases or disorders, such as cancer. 2. The compound of claim 1 , wherein Ris alkyl claim 1 , cycloalkyl claim 1 , heteroalkyl claim 1 , heterocycloalkyl claim 1 , alkoxy claim 1 , aryl claim 1 , heteroaryl claim 1 , cyano claim 1 , —(CH)NRC(═O)R claim 1 , —C(═O)OR claim 1 , —C(═O)NRR claim 1 , —S(═O)R claim 1 , or —S(═O)NRR claim 1 , and Ris hydrogen claim 1 , halo claim 1 , or alkyl.3. The compound of or claim 1 , wherein Ris hydrogen claim 1 , halo claim 1 , or alkyl claim 1 , and Ris alkyl claim 1 , cycloalkyl claim 1 , heteroalkyl claim 1 , heterocycloalkyl claim 1 , alkoxy claim 1 , aryl claim 1 , heteroaryl claim 1 , cyano claim 1 , —(CH)NRC(═O)R claim 1 , —C(═O)OR claim 1 , —C(═O)NRR claim 1 , S(═O)R claim 1 , or S(═O)NRR.4. The compound of any one of - claim 1 , wherein Rand Rare independently selected from phenyl and pyridyl claim 1 , and each of Rand Ris optionally substituted with one or more substituents selected from halo claim 1 , alkyl claim 1 , cyano claim 1 , and alkoxy.5. The compound of any one of - claim 1 , wherein Ris phenyl claim 1 , optionally substituted with one or more substituents selected from halo claim 1 , alkyl claim 1 , cyano claim 1 , and alkoxy.6. The compound of any one of - claim 1 , wherein Ris phenyl claim 1 , optionally substituted with one or more substituents selected from halo claim 1 , alkyl claim 1 , cyano claim 1 , and alkoxy.7. The compound of any one of - claim 1 , wherein Ris hydroxy.9. The compound of claim 8 , wherein Wis CR claim 8 , and Ris hydrogen claim 8 , halo claim 8 , or C-Calkyl.10. The ...

LABELLING AGENT, AND COMPOSITION FOR LABELLING A PROTEIN, METHOD FOR LABELLING A PROTEIN, AND METHOD FOR DETECTING A PROTEIN

Provided are a labelling agent including a compound of the following Formula 1, a labelling composition, a method of labelling a protein with the labelling agent, and a method of detecting the protein using the labelling agent: 2. The labelling agent of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare independently H claim 1 , substituted or unsubstituted —C-alkyl- claim 1 ,{'sub': 7', '9', '10', '9', '10', '1-10, 'Ris H or —NRR, Rand Rare independently H, substituted or unsubstituted —C-alkyl-,'}{'sub': 11', '1-10, 'Ris H, substituted or unsubstituted —C-alkyl-,'}{'sub': 12', '1-10, 'Ris H, substituted or unsubstituted —C-alkyl-, and'}{'sub': 13', '14', '1-10, 'Rand Ris independently H, substituted or unsubstituted —C-alkyl-.'}6. The composition of claim 4 , wherein the compound is covalently linked to the protein.8. The method of claim 7 , wherein the irradiating light causes a radical reaction of the labelling agent to form a complex of the labelling agent and the protein. This application claims the benefit of Korean Patent Application No. 10-2014-0150621, filed on Oct. 31, 2014, in the Korean Intellectual Property Office, the disclosure of which is incorporated herein in its entirety by reference.1. FieldThe present disclosure relates to a labelling agent, a composition for labelling a protein, a method of labelling a protein using the labelling agent, and a method of detecting a protein.2. Description of the Related ArtA technology of labelling in vivo proteins is one of fields which are of great importance in molecular biology, since development of green fluorescence protein (GFP). This technology is used to monitor protein migration according to cell proliferation and signal transduction as well as location of proteins present in an organism, and thus has a great function to overcome resolution of the existing microscopes and to find out a new mechanism.To label proteins with GFP, transfection using virus is ...

NOVEL ONE-POT HOMOGENEOUS PROCESS FOR THE LARGE SCALE MANUFACTURE OF 2-SUBSTITUTED BENZIMIDAZOLES

2-substituted benzimidazoles and methods of preparing the same are disclosed. The compositions may include a compound or salt thereof, an acid, and a polar aprotic solvent. The compositions may be used to inhibit corrosion of a metal surface in contact with an aqueous system, and provide enhanced protection against corrosion of metals in the aqueous system. 2. The composition of claim 1 , further comprising water.3. The composition of claim 1 , whereinX is independently hydrogen or halogen;{'sup': '1', 'Ris hydrogen;'}{'sup': '2', 'Ris absent; and'}{'sup': 3', '4, 'Ris CHR.'}4. The composition of claim 1 , wherein at least one Z is nitrogen.5. The composition of claim 1 , wherein Ris a bond and at least one Z is nitrogen.7. The composition of claim 1 , wherein the acid is selected from sulfuric acid claim 1 , hydrochloric acid claim 1 , nitric acid claim 1 , methanesulfonic acid claim 1 , phosphoric acid claim 1 , sulfamic acid claim 1 , aminomethylphosphonic acid claim 1 , p-toluenesulfonic acid claim 1 , and any combination thereof.8. The composition of claim 1 , wherein the polar aprotic solvent is selected from acetonitrile claim 1 , N claim 1 ,N-dimethylformamide claim 1 , acetone claim 1 , dimethylsulfoxide claim 1 , sulfolane claim 1 , N-methylpyrrolidinone claim 1 , methylsulfonylmethane claim 1 , chlorobenzene claim 1 , o-dichlorobenzene claim 1 , nitromethane claim 1 , an ionic liquid claim 1 , and any combination thereof.9. The composition of claim 1 , wherein the composition is homogenous liquid.10. The composition of claim 1 , further comprising a high temperature stable phase transfer catalyst.11. The composition of claim 10 , wherein the high temperature stable phase transfer catalyst is selected from the group consisting of an alkyl guanidinium salt claim 10 , an aryl guanidinium salt claim 10 , an alkyl phosphonium salt claim 10 , an aryl phosphonium salt claim 10 , a peralkylated phosphazenium salt claim 10 , and any combination thereof.13. The ...

Crystals containing unsaturated carboxylic acid amide compound and method for producing same

Provided is a crystal of an unsaturated carboxylic acid amide. The crystal is useful as or for fine chemicals such as pharmaceuticals, agricultural chemicals, polymeric materials, functional materials, and intermediates of them, has a high purity, still is not bulky, and can be handled excellently. The crystal includes an unsaturated carboxylic acid amide represented by Formula (1) in an amount of 95 percent by area or more and has a bulk density of 0.2 to 0.7 g/mL. In the formula, R 1 to R 5 are independently selected from hydrogen, alkyl, hydroxyl, alkoxy, and nitro. At least two of R 1 to R 5 may be linked to form a ring together with carbon atoms constituting the specified aromatic ring. R 6 , R 7 , and R 8 are independently selected from hydrogen, alkyl, and aryl. R 7 and R 8 may be linked to form a ring together with carbon atoms constituting the specified imidazole ring.

Compounds and methods for treatment of hedgehog pathway associated conditions

Provided herein is novel compounds of formula (I), (II), (III), (IV), and (V) as described in the specification, and pharmaceutically acceptable salts, solvates, and prodrugs and compositions thereof, and methods of measuring hedgehog pathway activation in tumor cells, examining tumor cell proliferation, differentiation and apoptosis and using the compounds and pharmaceutical compositions disclosed for treatment of diseases and disorders associated with the hedgehog signaling pathway.

CHIRAL DIAMINE COMPOUNDS FOR THE PREPARATION OF CHIRAL ALCOHOLS AND CHIRAL AMINES

A process for the stereoselective preparation of a chiral alcohol or a chiral amine, the process comprising reacting a first prochiral reactant selected from the group consisting of a ketone, an aldehyde, and an imine, with a second reactant comprising a Grignard reagent, in the presence of a chiral trans-diamine of formula (1) as defined herein: 2. The process according to claim 1 , wherein the ketone claim 1 , aldehyde or imine is formed in-situ.3. The process according to claim 1 , wherein Ra and Rb together define a C-Ccycloalkyl group.4. The process according to claim 3 , wherein the cycloalkyl group is cyclohexane or cyclopentane.5. The process according to claim 1 , wherein Ra and Rb are each independently an alkyl or an aryl group.6. The process according to claim 5 , wherein Ra and Rb are each independently phenyl claim 5 , methyl or tert-butyl.7. The process according to claim 1 , wherein Rc is a Calkyl group.8. The process according to claim 1 , wherein Rd is a Calkyl group.9. The process according to claim 1 , wherein Rd and Re together define an imidazolidine ring with the two N atoms.10. The process according to claim 1 , wherein Re is a Calkyl group.11. The process according to claim 1 , wherein n is 1.12. The process according to claim 1 , wherein Rf is an alkyl or aryl group.13. The process according to claim 12 , wherein Rf is a tert-butyl group.14. The process according to claim 12 , wherein Rf is an aryl group which is substituted by at least one substituent selected from hydroxy claim 12 , alkoxy claim 12 , amino claim 12 , aminoalkyl claim 12 , thiol claim 12 , halo claim 12 , haloalkyl claim 12 , haloalkoxy claim 12 , alkyl claim 12 , cycloalkyl claim 12 , alkenyl claim 12 , cycloalkenyl claim 12 , alkynyl claim 12 , aryl claim 12 , heterocyclyl claim 12 , cyano claim 12 , nitro claim 12 , silyl claim 12 , sulfanyl claim 12 , phosphanyl and CF.16. The process according to claim 15 , wherein Rii and Riv are both hydrogen.17. The process ...

PROCESS AND METHOD FOR REDUCING METAL CORROSION IN WATER

This disclosure relates to compositions and methods of reducing corrosion using benzimidazoles. The method may include adding a benzimidazole and a halogen to an aqueous system that is in contact with a metal surface. The halogen may be bromine, iodine, or any combination thereof. In some cases, adding the halogen may be optional depending on the substituents on the benzimidazole ring. Compositions are also disclosed that include a benzimidazole, optionally a halogen depending on the substituents on the benzimidazole ring, and optionally a halogen stabilizer. 1. A method of reducing corrosion of a metal surface in an aqueous system , comprising:adding a benzimidazole to an aqueous system comprising a metal surface; andadding a halogen selected from bromine, iodine, and any combination thereof to the aqueous system.4. The method of claim 1 , wherein the halogen is a bromine precursor claim 1 , an iodine precursor claim 1 , or any combination thereof.5. The method of claim 3 , wherein Z is CRand Ris hydrogen.6. The method of claim 1 , further comprising adding a halogen stabilizer that is an isocyanate claim 1 , a hydantoin claim 1 , sulfamic acid claim 1 , ammonia claim 1 , urea claim 1 , an amine claim 1 , or any combination thereof.7. The method of claim 1 , further comprising measuring a corrosion rate of a metal surface in the aqueous system.8. The method of claim 7 , wherein the metal surface is copper or a copper alloy.9. The method of claim 1 , further comprising adjusting a dosage of the compound of formula (I) or salt thereof to achieve a predetermined corrosion rate.10. The method of claim 1 , further comprising adjusting a dosage of the halogen to achieve a predetermined corrosion rate.11. The method of claim 1 , wherein a dosage of the benzimidazole ranges from about 0.01 ppm to about 100 ppm.12. The method of claim 1 , wherein a dosage of the halogen ranges from about 0.01 ppm to about 100 ppm.13. The method of claim 1 , wherein the aqueous system ...

NOVEL 2-SUBSTITUTED BENZIMIDAZOLES AS SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMS)

The present invention is directed to a novel 2-substituted benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor. 121-. (canceled)23. The method of claim 22 , comprising treating the subject with a pharmaceutical composition comprising a pharmaceutically acceptable carrier and the compound of formula (I).25. The method of claim 24 , wherein{'sup': '1', 'sub': 2', '2', '2-4', '2', '2-4', '3', '2, 'Ris selected from the group consisting of -(lower alkyl)-CN, —(CH)-heteroaryl, —(CH)—(Calkenyl), —(CH)—(Calkynyl), -(lower alkyl)-C(O)O-(lower alkyl) and -(lower alkyl)-O—Si(CH)(t-butyl);'}{'sup': 2', '3, 'Rand Rare each independently selected from the group consisting of halogen, cyano and halogen substituted lower alkyl;'}{'sup': '4', 'Ris selected from the group consisting of alkenyl, alkynyl and aryl; wherein the alkenyl is optionally substituted with a substituent selected from the group consisting of hydroxy, carboxy and phenyl;'}{'sup': '5', 'Ris OH;'}{'sup': 4', '5, 'claim-text': {'sub': '1-2', 'wherein the ring structure is optionally substituted with one to two substituents independently selected from the group consisting of methyl, ethyl, hydroxymethyl, hydroxyethyl, and —(Calkyl)-halogen;'}, 'alternatively, Rand Rare taken together with the atom to which they are bound to form a ring structure selected from the group consisting of 2,5-dihydro-furanyl, 2-tetrahydrofuranyl, 2-[1,3]-dioxolanyl, 2-[1,3]dioxanyl, 2-imidazolyl and 2-oxazolidinyl;'}or a pharmaceutically acceptable salt thereof.26. The method of claim 25 , wherein{'sup': '1', 'Ris selected from the group consisting of cyano-methyl-, 2-pyridyl-methyl-, allyl, 1-propyn-3-yl, methoxy-carbonyl-methyl- and t-butyl-dimethyl-silyloxy-ethyl-;'}{'sup': '2', 'Ris selected from the group consisting of chloro and trifluoromethyl;'}{'sup': '3', 'Ris selected from the group consisting of chloro and cyano ...

METHOD FOR PRODUCING SULFONYL AMIDINE COMPOUND

Provided are a method for producing a sulfonyl amidine compound, which has an excellent gonadotropin releasing hormone receptor antagonism and is useful as a therapeutic agent for gonadotropin-dependent diseases (for example, prostate cancer, breast cancer, endometriosis, uterine fibroid, prostatic hyperplasia, or the like) or a salt thereof, and a synthesis intermediate useful in the production method. The production method of the present invention controls formation of a by-product which is hardly removed unless column purification is conducted and racemization of a target compound, thereby obtaining the target compound with a high purity, and therefore, the production method is suitable for industrial production. 34-. (canceled)5. (2R)-2-(Tetrahydro-2H-pyran-2-yloxy)propanimidamide or a salt , hydrate , or solvate thereof.6. (2R)—N-({5-[3-(2 ,5-Difluorophenyl)-2-(1 ,3-dihydro-2H-benzoimidazol-2-ylidene)-3-oxopropanoyl]-2-fluorophenyl}sulfonyl)-2-(tetrahydro-2H-pyran-2-yloxy)propanimidamide or a salt , hydrate , or solvate thereof.11. The method of claim 1 , wherein a free compound of formula (I) is obtained from the deprotecting.12. The method of claim 1 , wherein a salt of the compound of formula (I) is obtained from the deprotecting.13. The method of claim 1 , wherein a purity of the compound of formula 1 or the salt claim 1 , hydrate claim 1 , or solvate thereof is at least 93.72%.15. The crystal of claim 7 , wherein a purity of the compound of formula (I) or the salt claim 7 , hydrate claim 7 , or solvate thereof is at least 97.76%.16. The crystal of claim 8 , wherein a purity of the compound of formula (I) or the salt claim 8 , hydrate claim 8 , or solvate thereof is at least 98.28%. The present invention relates to a method for producing (2R)—N-({5-[3-(2,5-difluorophenyl)-2-(1,3-dihydro-2H-benzoimidazol-2-ylidene)-3-oxopropanoyl]-2-fluorophenyl}sulfonyl)-2-hydroxypropanimidamide (hereinafter referred to as a “compound A” or “a compound of the formula (I)” ...

FUSED RING ANALOGUES OF ANTI-FIBROTIC AGENTS

The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders. 237-. (canceled)3973-. (canceled)75135-. (canceled) The present invention relates to compounds that may be useful in the treatment of medical conditions associated with tissue fibrosis. More particularly, the present invention relates to fused ring derivatives of 2-{[(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]amino}benzoic acid, pharmaceutical compositions containing these derivative compounds, and uses of the derivative compounds in the treatment of certain conditions associated with tissue fibrosis.Fibrosis occurs when excess fibrous connective tissue forms or develops in an organ or tissue. Fibrosis can occur as a part of the wound-healing process following tissue damage resulting from physical injury, inflammation, infection, exposure to toxins, and other causes. Examples of conditions associated with tissue fibrosis include dermal scar formation, keloids, liver fibrosis, kidney fibrosis (including diabetic nephropathy), hepatic cirrhosis, pulmonary interstitial fibrosis, glomerulonephritis, heart failure (ischaemic and non-ischaemic), diabetic nephropathy, scleroderma, excessive scar tissue post surgery or device insertion, progressive kidney disease, hypertension, heart failure due to ischaemic heart disease, valvular heart disease, hypertensive heart disease, and hypertrophic scars.The elaboration of extracellular matrix also has a role in fibroproliferative tumor progression and metastasis. Accordingly, strategies that reduce the accumulation of extracellular matrix have been advocated as potential therapies for the treatment and prevention of heart failure in both diabetic and nondiabetic states.At present the pathogenic mechanism of fibrosis is not ...

BENZO-HETEROCYCLIC COMPOUND AND COMPOSITION FOR PREVENTING OR TREATING CANCER DISEASE, CONTAINING SAME AS ACTIVE INGREDIENT

A novel benzoheterocycle compound or a pharmaceutically acceptable salt thereof showed a high anti-proliferative effect against cancer cell lines. Using this, a pharmaceutical composition for preventing or treating cancer disease can comprise the compound or a pharmaceutically acceptable salt thereof as an active ingredient. In addition, a health functional food composition for preventing or improving cancer disease can include the compound or a pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutical composition or health functional food composition can effectively prevent or treat various cancer diseases. 2. The compound or a pharmaceutically acceptable salt thereof of claim 1 , wherein in Chemical Formula 1 claim 1 , the R is O claim 1 , S or NR claim 1 , and the Ris hydrogen or C1-C4 alkyl.3. The compound or a pharmaceutically acceptable salt thereof of claim 1 , wherein the compound is selected from the group consisting of 4-(1H-benzo[d]imidazol-2-yl)-N-hydroxybenzamide claim 1 , N-hydroxy-4-(1-methyl-1H-benzo[d]imidazole-2-yl)benzamide claim 1 , 4-(1-ethyl-1H-benzo[d]imidazol-2-yl)-N-hydroxybenzamide claim 1 , N-hydroxy-4-(1-propyl-1H-benzo[d]imidazol-2-yl)benzamide claim 1 , 4-(1-butyl-1H-benzo[d]imidazol-2-yl)-N-hydroxybenzamide claim 1 , 4-(benzo[d]oxazole-2-yl)-N-hydroxybenzamide claim 1 , 4-(benzo[d]thiazol-2-yl)-N-hydroxybenzamide claim 1 , 3-(1H-benzo[d]amidazol-2-yl)-N-hydroxybenzamide claim 1 , N-hydroxy-3-(1-methyl-1H-benzo[d]imidazol-2-yl)benzamide claim 1 , 3-(1-ethyl-1H-benzo[d]imidazole-2-yl)-N-hydroxybenzamide claim 1 , N-hydroxy-3-(1-propyl-1H-benzo[d]imidazol-2-yl)benzamide claim 1 , 3-(1-butyl-1H-benzo[d]imidazol-2-yl)-N-hydroxybenzamide claim 1 , 3-(benzo[d]oxazol-2-yl)-N-hydroxybenzamide and 3-(benzo[d]thiazol-2-yl)-N-hydroxybenzamide.4. A pharmaceutical composition for preventing or treating cancer disease comprising the compound or a pharmaceutically acceptable salt thereof of as an active ingredient.5. A ...

2-BENZYL-BENZIMIDAZOLE COMPLEMENT FACTOR B INHIBITORS AND USES THEREOF

The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. 2. The compound of claim 1 , wherein X is N and Y is N(H) or O.3. The compound of wherein X is N and Y is N(H).4. The compound of claim 1 , wherein Ris absent.5. The compound of claim 1 , wherein Ris hydrogen claim 1 , C-Calkyl or C-Calkoxy.6. The compound of claim 1 , wherein Ris C-Calkyl or C-Calkoxy.8. The compound of claim 1 , wherein Ris hydrogen claim 1 , C-Calkyl claim 1 , halo C-Calkyl claim 1 , or C-Ccycloalkyl.9. The compound of claim 1 , wherein Ris hydroxyl claim 1 , amino claim 1 , C-Calkyl claim 1 , methoxy claim 1 , trifluoromethoxy claim 1 , mono- and di-C-Calkyl amino claim 1 , or CHC(O)NH.10. The compound of claim 1 , whereinX is N;Y is N(H);One occurrence of R is cyano and the other occurrence of R is hydrogen;{'sup': '1', 'Ris hydrogen, methyl, methoxy, ethyl or ethyoxy;'}{'sup': '2', 'Ris methyl, methoxy, ethyl or ethyoxy;'}{'sup': '3', 'Ris hydrogen or methyl;'}{'sup': '4', 'Ris absent;'}{'sup': '5', 'sub': 2', '2, 'Ris hydroxyl, amino, methoxy, trifluoromethoxy, methylamino or CHC(O)NH;'}{'sup': '6', 'Ris hydrogen, methyl, cyclopropyl or trifluoromethyl; and'}{'sup': '10', 'Ris hydrogen, chloro or bromo.'}11. The compound of claim 1 , or a salt or tautomer thereof claim 1 , which compound is selected from the group consisting of (±)-2-(Hydroxy(2-methoxy-4 claim 1 ,6-dimethylphenyl)methyl)-1H-benzo[d]imidazole-5-carbonitrile;(±)-2-(1-Hydroxy-1-(2-methoxy-4,6-dimethylphenyl)ethyl)-1H-benzo[d]imidazole-5-carbonitrile;(±)-2-(2,2,2-Trifluoro-1-hydroxy-1-(2-methoxy-4,6-dimethylphenyl)ethyl)-1H-benzo[d]imidazole-5-carbonitrile;(±)-2-(1-(3-bromo-6-methoxy-2,4-dimethylphenyl)-2,2,2-trifluoro-1-hydroxyethyl)-1H-benzo[d]imidazole-5-carbonitrile;(+) or (−)-2-(2,2,2-Trifluoro-1-(2-methoxy-4,6- ...

2-Substituted Imidazole and Benzimidazole Corrosion Inhibitors

Disclosed are methods of using nitrogen-containing compounds as corrosion inhibitors. The present method is used to inhibit corrosion of a metal surface in contact with an aqueous system using 2-substituted imidazoles and 2-substituted benzimidazoles, and provides enhanced protection against corrosion of metals in the aqueous system. The method comprises the use of corrosion inhibitors that are generally resistant to halogen attack and provide good corrosion resistance in the presence of oxidizing halogen-based biocides. Formulations comprising 2-substituted imidazoles and 2-substituted benzimidazoles are also disclosed. 2. The method of claim 1 , wherein Z is carbon.5. The method of claim 1 , wherein the metal surface comprises copper or a copper alloy.6. The method of claim 1 , wherein the aqueous system comprises an oxidizing halogen compound.7. The method of claim 1 , wherein the aqueous system is a cooling water system.8. The method of claim 1 , wherein the metal has a corrosion rate of less than about 0.1 mpy.14. The method of claim 9 , wherein the metal surface comprises copper or a copper alloy.15. The method of claim 9 , wherein the aqueous system is a cooling water system.16. The method of claim 9 , wherein the compound of formula (II) is added to the aqueous system at a dosage of from about 0.01 ppm to about 100 ppm.17. The method of claim 9 , wherein the metal has a corrosion rate of about 0.1 mpy car less.18. A formulation for inhibiting corrosion of a metal surface in contact with an aqueous system claim 9 , the formulation comprising a compound of formula (I) or (II) claim 9 , a phosphoric acid claim 9 , and a phosphinosuccinic oligomer.19. The formulation of claim 18 , wherein the formulation further comprises a fluorescent organic compound.20. The formulation of claim 19 , wherein the fluorescent organic compound is selected from the group consisting of Rhodamine claim 19 , a derivative of Rhodamine claim 19 , all acridine dye claim 19 , fluorescein ...

BENZIMIDAZOLE DERIVATIVES AS SELECTIVE BLOCKERS OF PERSISTENT SODIUM CURRENT

The present invention is directed to a compound of Formula I 2. The compound of claim 1 , wherein R is and unsubstituted straight chain or branched Calkyl.3. The compound of claim 1 , wherein R is Calkyl which is substituted with a Caryloxy group.4. The compound of claim 3 , wherein the “aryl” portion of said Caryloxy group is unsubstituted or substituted with 1-2 Calkyl or Calkoxy substitutents.5. The compound of claim 1 , wherein R is Calkyl which is substituted with a heteroaryl substitutent claim 1 , wherein said heteroaryl group is five- to six-membered ring containing 1-2 ring N atoms claim 1 , and wherein when said five- to six-membered ring containing 1-2 ring N atoms has two substituents on adjacent carbon atoms claim 1 , said substituents together with the carbon atoms to which they are attached can optionally form a phenyl ring claim 1 , and wherein said six-membered ring containing 1-2 ring N atoms claim 1 , optionally with said phenyl ring is optionally further substituted with a ring system substituent.6. The compound of claim 5 , wherein said five- to six-membered ring containing 1-2 ring N atoms claim 5 , optionally with said phenyl ring is selected from the group consisting of pyrazolyl claim 5 , imidazolyl claim 5 , pyrimidinyl claim 5 , pyrazinyl claim 5 , and benzimidazolyl.7. The compound of claim 6 , wherein said five- to six-membered ring containing 1-2 ring N atoms claim 6 , optionally with said phenyl ring is selected from the group consisting of is imidazolyl and benzimidazolyl.8. The compound of claim 1 , wherein R is Calkyl which is substituted with a —N(Calkyl)substituent.10. The compound of claim 1 , wherein Rand Rare both H.11. The compound of claim 10 , wherein m is 1 or 2.12. The compound of claim 10 , wherein m is 1 claim 10 , and X is O.13. The compound of claim 10 , wherein m is 2 claim 10 , and X is a covalent bond.14. The compound of claim 10 , wherein m is 1 claim 10 , and X is —S(═O)—.15. The compound of claim 10 , wherein m ...

cancer treatment compounds

Penicillanic acid and cephalosporanic acid derivs. - are antibiotics esp. effective against Gram negative microorganisms e.g. Pseudomonas and Proteus

Beta-Lactam cpds. of formula (I) and their acceptable salts and esters are new. In (I) X is of formula (H) or (J) R1 is H, opt. substd. alkyl, aryl or heterocyclic gp; R2 and R4 are H or lower alkyl; R3 and R5 are H, halogen, lower alkyl or alkoxy; A is CH or N; B is a single bond or methyleneoxy; C is a single bond, or phenylene; D is a single bond, lower alkylene or oxyalkylene; Y is opt. substd. Ph, opt. substd. monocyclic aromatic heterocyclic gp. or dihydrophenyl; and Z is of formula (K) or (L) E is H, acetoxy of S-G; G is an opt. substd. heterocyclic gp.). Typical cpds. are 6 D-2-(4-(benzimidazol-2-yl)phenoxyacetylamino-2-phenyl-acetylami- no -penicillanic acid and 7 D-2-(2-(4-fluorophenyl)-benzimidazol-5-yl-carbonylamino)-2-phen- ylacetyl-amino -cephalosporanic acid.

Process for preparing benzoic acid esters

提供了工业上更有利的用于制备期望用作药物的新型吡啶的衍生物的工艺。用于以高质量、较短步骤和较高收率制备作为制备工艺中的中间体的3-(6-羟基-1-甲基-1H-苯并咪唑-2-基)安息香酸酯的方法，以及作为其前体的新型安息香酸酯及其制备方法。

Compounds for treating cancer

Compounds of general formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterised by abnormal cell growth and/or dysregulated apoptosis.

Compounds for treating cancer

Compounds of general formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterized by abnormal cell growth and/or dysregulated apoptosis.

Compounds for treating cancer

Compounds for treating cancer

本发明涉及通式(I)化合物：其中R 1 、R 2 、R 3 、R 4 、R 5 、R 6 、X和Y如本文所定义，其作为Bcl-2的抑制剂且可用于治疗特征为异常的细胞生长和/或失调的细胞凋亡的疾病。

Compounds for treating cancer

Compounds of general formula (I): wherein R, R, R, R, R, R, X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterised by abnormal cell growth and/or dysregulated apoptosis.

Compounds for treating cancer

Compounds of general formula (I): wherein R1, R2, R3, R4, R5, R6, X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterised by abnormal cell growth and/or dysregulated apoptosis.

COMPOUNDS FOR CANCER TREATMENT

В заявке описаны соединения общей формулы (I)в которой R, R, R, R, R, R, X и Y являются такими, как определено в настоящем изобретении, которые являются ингибиторами Bcl-2 и применимы для лечения заболеваний, характеризующихся аномальным ростом клеток и/или нарушенной регуляцией апоптоза. The application describes compounds of general formula (I) in which R, R, R, R, R, R, X, and Y are as defined herein, which are Bcl-2 inhibitors and are useful in treating diseases characterized by abnormal growth. cells and / or impaired regulation of apoptosis.

Compounds for treating cancer.

Los compuestos de la fórmula general (I): (ver fórmula (I)) en donde R1, R2, R3, R4, R5, R6, X e Y son tal como se definen en la presente son inhibidores de Bcl-2 y son de utilidad para tratar enfermedades caracterizadas por un crecimiento celular anormal y/o una apoptosis desregulada.

Compounds for treating cancer

Compounds of general formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterised by abnormal cell growth and/or dysregulated apoptosis.

Compounds for treating cancer

Compounds of general formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterised by abnormal cell growth and/or dysregulated apoptosis.

Method of obtaining alkyl ester of bendamustine, bendamustine, and its derivatives

FIELD: chemistry. SUBSTANCE: invention relates to method of obtaining compound, described by formula (I) or its salt, where X stands for halogen residue, and R 1 and R 2 together stand for residue, described by formula (II), where R 4 and R 5 independently on each other represent alkyl residue and n represents number in the range 0-12. In accordance with claimed method compound of formula (III) is introduced into reaction with mixture, containing compound (i), selected from group, consisting of compound of formula (IV), where R 6 represents H or alkyl residue, and R 7 and R 8 independently on each other represent alkyl residue, and compound of formula (V) where R 9 and R 10 independently on each other represent alkyl residue, and compound (ii), which is described by formula (VI). R 1 and R 2 in compound of formula (III) and X in compound of formula (VI) are determined above for compound of formula (I). Invention also relates to method of obtaining respective acids by hydrolysis of ester group in compound of formula (I). EFFECT: claimed methods make it possible to obtain desired compounds with reproducible high outputs and can be applied in synthesis of bendamustine derivatives, used in chemical therapy of various cancer diseases. 14 cl, 3 ex (19) РОССИЙСКАЯ ФЕДЕРАЦИЯ RU (11) 2 505 533 (13) C2 (51) МПК C07D 235/16 (2006.01) C07C 227/16 (2006.01) C07C 227/18 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2011152372/04, 21.12.2011 (24) Дата начала отсчета срока действия патента: 21.12.2011 (73) Патентообладатель(и): ХЕРАЕУС ПРЕШИС МЕТАЛС ГМБХ ЭНД КО.КГ (DE) R U Приоритет(ы): (30) Конвенционный приоритет: 22.12.2010 DE 102010055499.5 22.12.2010 US 61/426,098 (72) Автор(ы): ГРО Кай (DE), РАУТЕР Хольгер (DE), БОРН Дирк (DE) (43) Дата публикации заявки: 27.06.2013 Бюл. № 18 2 5 0 5 5 3 3 Адрес для переписки: 129090, Москва, ул. Большая Спасская, 25, стр. 3, ООО "Юридическая фирма Городисский и Партнеры" ( ...

Fluoroalkyl-substituted 2-amidobenzimidazoles and the use thereof for boosting stress tolerance in plants

The invention relates to the use of fluoroalkyl-substituted 2-amidobenzimidazoles of formula (I), or the salts (I) thereof, for boosting stress tolerance in plants to abiotic stress, in particular for strengthening plant growth and/or for increasing plant yield, and to select methods for producing such fluoroalkyl-substituted 2-amidobenzimidazoles of formula (I).

5-Trifluoromethyl-7-nitrobenzimidazoles

Benzimidazoles of the formula ##SPC1## Wherein R 1 and R 2 represent at least one alkyl group which may optionally be substituted and X is lower alkoxy or halo, R 1 may also be dialkyl amino and R 2 may be halo. The compounds are useful as intermediates for preparation of herbicides.

Process for the production of bendamustine alkyl ester, bendamustine, and derivatives thereof

본 발명은 벤다무스틴 알킬 에스테르, 벤다무스틴과 이의 유도체의 제조 방법에 관한 것이다. 본 발명에 따른 방법을 이용하여 이들 화합물을 재현가능하게 높은 수율로 제조할 수 있다. 이를 위해서, 하이드록실기가 간단한 방법으로 할로겐 기로 치환되는 출발 물질로서 하이드록실기 함유 에스테르가 사용된다. 이러한 치환은 (i) 옥살릴 클로라이드 및 (ii) 디알킬포름아미드, 디알킬 아세트아미드 또는 디메틸 설폭시드의 존재 하에 가능하다. 후속 반응에서, 생성되는 에스테르를 가수분해하여 산을 형성할 수 있다.

Process for the preparation of furanyl-benzazoles

Ester derivatives of dimethylpropionic acid and pharmaceutical compositions containing them

The present invention relates to esters of 2,2-dimethylpropionic acid having the general formula (I)

2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors for the treatment of thromboembolic disorders

The present invention relates to 2-(2-hydroxybiphenyl-3-yl)-1H-benzoimidazole-5-carboxamidine derivatives as factor VIIa inhibitors for the treatment of thromboembolic disorders, cancers and rheumatoid arthritis. Processes for preparing these inhibitors and intermediates thereof are also disclosed.

Fluoroalkyl-substituted 2-amidobenzimidazoles and the use thereof for boosting stress tolerance in plants

式(1)的氟烷基取代的2-氨基苯并咪唑或其盐用于提高植物对非生物胁迫的耐受性，尤其用于增强植物生长和/或提高植物产率的用途，以及经选择的制备这种式(1)的氟烷基取代的2-氨基苯并咪唑的方法。 其中

Benzimidazole compounds

A range is disclosed of benzimidazole-4-carboxamide compounds (I) which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. In formula (I), R and R' may each be selected independently from hydrogen, alkyl, hydroxyalkyl (e.g. CH2CH2OH), acyl (e.g. acetyl or benzoyl) or an optionally substituted aryl (e.g. phenyl) or aralkyl (e.g. benzyl or carboxybenzyl) group. R is generally a substituted phenyl group in the most preferred compounds. The compounds may also be used in the form of pharmaceutically acceptable salts or pro-drugs.

Benzimidazole compounds, pharmaceutical preparation in which the compounds are comprised and use of the compounds as chemotherapeutic agents

A range is disclosed of benzimidazole-4-carboxamide compounds (I) which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. In formula (I), R and R' may each be selected independently from hydrogen, alkyl, hydroxyalkyl (e.g. CH2CH2OH), acyl (e.g. acetyl or benzoyl) or an optionally substituted aryl (e.g. phenyl) or aralkyl (e.g. benzyl or carboxybenzyl) group. R is generally a substituted phenyl group in the most preferred compounds. The compounds may also be used in the form of pharmaceutically acceptable salts or pro-drugs.

Fluoroalkyl-substituted 2-amidobenzimidazoles and the use thereof for boosting stress tolerance in plants

式(1)的氟烷基取代的2-氨基苯并咪唑或其盐用于提高植物对非生物胁迫的耐受性，尤其用于增强植物生长和/或提高植物产率的用途，以及经选择的制备这种式(1)的氟烷基取代的2-氨基苯并咪唑的方法。 其中

The manufacture method of sulphonyl amidine compound

本发明提供具有优良的促性腺激素释放激素受体拮抗作用、作为性激素依赖性疾病(例如，前列腺癌、乳腺癌、子宫内膜异位症、子宫肌瘤、前列腺肥大症等)的治疗剂有用的磺酰脒化合物或其盐的制造方法以及该制造方法中有用的合成中间体。本发明的制造方法能够抑制除非进行柱纯化否则难以除去的副产物的生成和目标化合物的外消旋化，能够纯度良好地得到目标化合物，因此适合于工业生产。

Benzimidazole compounds

1-benzoyl ethyl-2-carbamoyl methyl benzimidazoles - analgesics, antiinfl-ammatories, hypotensives, vasodilators, respiratory analeptics, anticholinergics, anti-histamines and diuretics

Title cpds of formula (I): (where Ar = phenyl, opt. subst. by Cl or F or by >=1 1-4C alkyl or alkoxy gps. and R = H or 1-3C alkyl may be prepd. by the reaction of a 1-benzoyl ethyl-2-hydroxy methyl benzimidazole (II) with an isocyanate RNCO (III), or by reaction of a phenoxy carbonyl deriv. of (II) with an amine RNH2.

New derivatives of aryl heteroaryl ketones, process for preparing them as well as their application as medicinal product

The present invention relates to new derivatives of aryl heteroaryl ketones, to the process for preparing them as well as to their application as medicinal products. The new aryl heteroaryl ketone derivatives which are the subject of the present invention correspond to the general formula I: in which: R1 to R3, which are identical or different, represent a hydrogen atom, a halogen, an alkyl radical, an aryl group, an alkoxy radical, a nitro radical, an amino radical or a cyano radical; Het represents an azole.

BENZIMIDAZOLE DERIVATIVES

LES DERIVES DE BENZIMIDAZOLE DE L'INVENTION REPONDENT A LA FORMULE GENERALE CI-DESSOUS, ET LEURS SELS PHYSIOLOGIQUEMENT ACCEPTABLES: (CF DESSIN DANS BOPI) DANS LAQUELLE R EST L'HYDROGENE OU UN GROUPE ALKYLE INFERIEUR, R EST (CF DESSIN DANS BOPI) (OU AR EST UN GROUPE PHENYLE SUBSTITUE OU NON SUBSTITUE; R, R, R ET R SONT IDENTIQUES OU DIFFERENTS ET SONT L'HYDROGENE OU UN GROUPE ALKYLE INFERIEUR, Y COMPRIS LES CAS SUIVANTS OU UNE DOUBLE LIAISON EST FORMEE EN COMBINANT R AVEC R, UNE TRIPLE LIAISON EST FORMEE PAR UNE AUTRE COMBINAISON DE R ET R ET UN CYCLE CYCLOPROPANE EST FORME EN COMBINANT R AVEC R ET LES ATOMES DE CARBONE ADJACENTS); ET R EST L'HYDROGENE UN GROUPE ALKYLE INFERIEUR, ACYLE OU ALKYLSULFONYLE. THE BENZIMIDAZOLE DERIVATIVES OF THE INVENTION MEET THE GENERAL FORMULA BELOW, AND THEIR PHYSIOLOGICALLY ACCEPTABLE SALTS: (CF DRAWING IN BOPI) IN WHICH R IS HYDROGEN OR A LOWER ALKYL GROUP, R IS (CF DRAWING IN BOPI) (WHERE AR IS A SUBSTITUTED OR NON-SUBSTITUTED PHENYL GROUP; R, R, R AND R ARE THE SAME OR DIFFERENT AND ARE HYDROGEN OR A LOWER ALKYL GROUP, INCLUDING THE FOLLOWING CASES WHERE A DOUBLE LINK IS FORMED BY COMBINING R WITH R , A TRIPLE LINK IS FORMED BY ANOTHER COMBINATION OF R AND R AND A CYCLOPROPANE CYCLE IS FORMED BY COMBINING R WITH R AND THE ADJACENT CARBON ATOMS); AND R IS HYDROGEN A LOWER ALKYL, ACYL OR ALKYLSULFONYL GROUP.

NOVEL ARYL-HETEROARYL CETONES DERIVATIVES, THEIR PREPARATION PROCESS AND THEIR APPLICATION AS MEDICAMENTS

2-Benzyl-benz-imidazoles - used as antioxidants for amines, phenols and oils

Benzimidazoles of formula (I) are new (where hal is halogen, especially F or Cl) Specif. claimed is 2-(4-chloro-alpha-hydroxybenzyl)-benzimidazole. (I) may be used to protect isoprenaline, dopamine, phenol, diphenolo, amino-phenolo and amines against oxidation.

New 5-substituted dialkylaminoalkyl-1 p-alkoxyphenyl-2-alkylbenzimidazoles

Patent FR2152799A1

Patent FR2292706B3

Patent FR2070090A1

2-cinnamoyl-1-(2-hydroxyethyl) benzimidazoles - with vasodilator , hypotensive respiratory analeptic, diuretic and analgesic activity

Cpds. of formula: (where Ar is phenyl, opt. substd. by >=1 halogen, 1-4C alkoxy, -NMe2, 2-furyl or 2-thienyl). The cpds. have vasodilator, respiratory analeptic, hypotensive, diuretic and analgesic activity. They are prepd. by treating 2-acetyl-1-(2-hydroxyethyl)benzimidazole with opt. substd. benzaldehydes.

2-4-thiazolyl benzimidazole derivs anthelmintics

(A) Cpds. of general formula (I) R = (1-10C)O-alkyl, Ph, or p-F.C6H4-and is pref. at posns. 5 (6). (B) Salts of I. Anthelmintics. Dose 5-125 mg/kg.

Oxazino-(1,4)(4,3-a) benzimidazole derivs. and related cpds. - have cardiovascular esp. antiarrhythmic and diuretic activity and CNS activity esp. antidepressant

Oxazino(1,4)(4,3-a)benzimidazole and related cpds. of formula (I) are new. In (I) -NR1R2 = mono-1-4C alkylamino, 3-6C cycloalkylamino, benzylamino, allylamino, dimethylproparglyamino, di(1-3C alkyl)amino, pyrrolidino, piperidino, morpholino, 4-methyl-piperazino,4-(2-hydroxyethel)-piperazino or 4-phenyl-piperazino and R3, X, Y, m is one of the combinations(a)H, CH2,0,1, CH3,0,1,1, CH3, 0,S, 1 or phenyl, 0,0,1 with n = 2 or 3, (b) phenyl, 0,0,2, phenyl, 5,5,1 or phenyl, 0,5,1 with n = 3 or (c) phenyl, 0, CH2, 1 with n = 1 or 2. (I) have cardiovascular activity, esp. as antiarrhythmics and diuretics, and CNS activity, esp. as antidepressants. They may be administered orally (10-300 mg doses 2-6 times daily) or parenterally (2-100 mg doses 1-4 times daily).

1-Propiophenone-2-phenyl propanol benzimidazoles - e.g. for use as vasodilators, respiratory analeptics, analgesics and hypotensives

Benzimidazole derivs. of formula (I):- (where R1-4 are H, F, 1-4C alkyl or CH3O), are useful for the treatment of anxiety, nervousness, pain, circulatory insufficiency, hypertension, oedema, gastro-duodenal ulcers, respiratory insufficiency, and asthenia.

NOVEL BENZIMIDAZOLE DERIVATIVES, THEIR PREPARATION AND THE MEDICINES THAT CONTAIN THEM

NOUVEAUX DERIVES DU BENZIMIDAZOLE DE FORMULEI DANS LAQUELLE R REPRESENTE UN ATOME D'HYDROGENE, UN RADICAL NITRO OU UN RESTE HYDROCARBONE OU UN RADICAL -OR DANS LEQUEL R REPRESENTE UN RESTE HYDROCARBONE ET R REPRESENTE UN RADICAL ALCOYLE 1 A 8C EN CHAINE DROITE OU RAMIFIEE, OU UN ATOME D'HALOGENE. CES DERIVES SONT PARTICULIEREMENT UTILES DANS LE TRAITEMENT DE L'ARTHRITE. NEW DERIVATIVES OF BENZIMIDAZOLE OF FORMULA I IN WHICH R REPRESENTS A HYDROGEN ATOM, A RADICAL NITRO OR A HYDROCARBON REMAINDER OR A -OR RADICAL IN WHICH R REPRESENTS A HYDROCARBON REMAINDER AND R REPRESENTS A RADICAL ALCOHYL CHAIN 1 TO 8C, OR RIGHT OR A HALOGEN ATOM. THESE DERIVATIVES ARE PARTICULARLY USEFUL IN THE TREATMENT OF ARTHRITIS.

Patent FR2115067A1

Benzimidazolylidene compounds and their preparation

Patent FR2152799B1

Alternator voltage adjustment system

Patent FR2032828A5

Patent FR2186246B1

Process for preparing benzoic acid esters

There is provided a more industrially advantageous process for preparing novel pyridine derivatives expected to be used as medicines. A process for preparing 3-[(6-hydroxy-1-methyl-1H-benzimidazol-2-yl)methoxy]benzoic acid esters as intermediates with high quality, in short steps and in a high yield, as well as novel benzoic acid esters as their precursors and a process for preparing the same.

2-(Alpha-hydroxy-halobenzyl) benzimidazoles - and their salts, with antihypertensive activity

New 2-(alpha-Hydroxy-halobenzyl)benzimidazoles of formula (I): (where Hal is halogen, esp. F and Cl) and their acid addn salts specif. 2-(alpha-hydroxy-2-chlorobenzyl)benzimidazole and its hydrochloride, are antihypertensive agents.

HERBICIDAL AGENTS

Benzimidazole Derivatives

Benzimidazole derivatives of the following formula, ##STR1## wherein R 1 indicates hydrogen atom, lower alkyl group having carbon atoms of 1 to 6 or dimethylaminopropyl group, R 2 indicates hydrogen atom or lower alkanoyl group having carbon atoms of 1 to 3, R 3 indicates hydrogen atom, lower alkyl group having carbon atoms of 1 to 3 or lower alkanoyl group having carbon atoms of 1 to 3, X indicates sulfur atom, sulfinyl group, sulfonyl group, amino group or methylene group, A indicates alkylene group having carbon atoms of 1 to 12, which alkylene group may optionally be substituted by hydroxy group or lower alkyl group having carbon atoms of 1 to 3, --(CHR')N--CR"═CR"--(CHR')M--, ##STR2## (in which R' and R" are each independently hydrogen atom, lower alkyl group having carbon atoms of 1 to 3 or hydroxy group, and n and m are equal to 0, 1, 2 or 3) and Y indicates oxygen atom or sulfur atom; their acid or alkali salts and hydrate thereof are useful as antiallergic agents.

2-Imidazolylcarbonylbenzoic acid compounds

Certain novel 2-imidazolylcabonylbenzoic acid compounds of the formula:

Pharmaceutical preparation containing benzimidazole 2-derivatives

4-12227/= Pharmaceutical preparation containing benzimidazole 2-derivatives Abstract of the Disclosure Benzimidazole 2-derivatives that are acylated in the nucleus and have the formula (I)

Acylated 2-benzimidazole derivatives

Acylated 2-benzimidazole derivatives of the formula <IMAGE> in which R denotes an optionally esterified or amidated carboxyl group or an optionally etherified or esterified hydroxymethyl group, R1 represents an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclic-aliphatic radical, R2 represents hydrogen or an aliphatic radical, and Ph represents a 1,2-phenylene group containing the radical R1-C(=O)-, have antiallergic properties and can be used as antiallergic pharmaceutical active compounds. They were prepared, for example, by reacting an appropriate 1,2-phenylenediamine, which is substituted by the acyl radical of the formula R1-C(=O) and can optionally also contain further substituents, or an acid addition salt thereof, e.g. its hydrochloride, with an acid of the formula R-COOH or a suitable reactive derivative thereof.

Ester derivatives of dimethylpropionic acid and pharmacetuical compositions containing them

Patent JPS4834880A

Process for the production of bendamustine alkyl ester, bendamustine, and derivatives thereof

The invention relates to a method for the production of bendamustine alkyl ester, bendamustine, as well as derivatives thereof. With the method according to the invention, the production of these compounds is possible in reproducibly high yields. To this end, hydroxyl-group-containing esters are used as the starting material whose hydroxyl groups are substituted in a simple way by halogen groups. This substitution is possible in the presence of (i) oxalyl chloride and (ii) dialkylformamide, dialkyl acetamide or dimethyl sulfoxide. In a subsequent reaction, the resulting esters can be hydrolyzed to form acid.

Benzimidazole derivatives and process for their preparations

S P E C I F I C A T I O N Title of the invention : Benzimidazole derivatives and process for their preparations Abstract of the invention : Benzimidazole derivatives of the following formula, wherein R1 indicates hydrogen atom, lower alkyl group having carbon atoms of 1 to 6 or dimethylaminopropyl group, R2 indicates hydrogen atom or lower alkanoyl group having carbon atoms of 1 to 3, R3 indicates hydrogen atom, lower alkyl group having carbon atoms of 1 to 3 or lower alkanoyl group having carbon atoms of 1 to 3, X indicates sulfur atom, sulfinyl group, sulfonyl group, amino group or methylene group, A indicates alkylene group having carbon atoms of 1 to 12, which alkylene group may optionally be substituted by hydroxy group or lower alkyl group having carbon atoms of 1 to 3, -(CHR')n-CR"=CR"-(CHR')m-, -(CHR')n

Heterocyclic compounds

A B S T R A C T HETEROCYCLIC COMPOUNDS Compounds of formula I

Method for producing 1,3-hydroxymethylene morpholino (4,3-a) benzimidazoles

Process and method for reducing metal corrosion in water

This disclosure relates to compositions and methods of reducing corrosion using benzimidazoles. The method may include adding a benzimidazole and a halogen to an aqueous system that is in contact with a metal surface. The halogen may be bromine, iodine, or any combination thereof. In some cases, adding the halogen may be optional depending on the substituents on the benzimidazole ring. Compositions are also disclosed that include a benzimidazole, optionally a halogen depending on the substituents on the benzimidazole ring, and optionally a halogen stabilizer.

2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors

The present invention relates to novel compound of Formula I inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.

METHOD FOR PRODUCING NEW BENZIMIDAZOLE DERIVATIVES

Color photographic recording material containing color couplers

Yellow couplers corresponding to the formula ##STR1## wherein Y represents an aromatic, aliphatic or cycloaliphatic group, X represents hydrogen or a releasable group, R 1 represents halogen, and R 2 and R 3 each represent an alkyl group having 1 to 20 carbon atoms, are readily soluble in oil formers and undergo coupling with a high color yield. They are resistant to heat and moisture and undergo color development to yield stable yellow dyes with an absorption maximum below 450 nm. They have a high absorption capacity in the near UV region and are virtually unaffected by fluctuations in the pH during processing.

Substituted phenylmercapto-benzimidazoles

1454469 Substituted 5-(6)-phenylmercaptobenzimidazoles HOECHST AG 27 May 1975 [28 May 1974] 23147/75 Heading C2C Novel substituted 5-(6-) phenylmercaptobenzimidazoles of the general formula in which R 1 is an alkyl group having from 1 to 4 carbon atoms, and R is a radical of the general formula in which R 2 is an alkyl or alkoxy group having from 1 to 4 carbon atoms, or an alkoxyalkyl or alkoxyalkoxy group having from 2 to 4 carbon atoms, in which the alkyl groups may be substituted by 1, 2, 3 or 4 halogen atoms; or R 2 is a phenyl, phenoxy, phenoxyalkyl, cyclohexyl, cyclohexyloxy or cyclohexyloxyalkyl group in which the alkyl groups have from 1 to 4 carbon atoms and in which the phenyl and cyclohexyl rings may carry one or more substituents selected from alkyl, haloalkyl, alkoxy, and haloalkoxy groups having 1 or 2 carbon atoms, and halogen atoms, or R 2 is a radical of the formula in which each of R 3 and R 4 is an alkyl group having from 1 to 4 carbon atoms or R 3 and R 4 together with the carbon atom carrying them from a cyclopentane or cyclohexane ring, or in which R is a radical of the general formula in which R 5 is a hydrogen atom, an alkyl group having from 1 to 4 carbon atoms, a cycloalkyl group having 5 or 6 carbon atoms or a phenyl group which may carry one or more substituents selected from alkyl, haloalkyl, alkoxy, and haloalkoxy groups having 1 or 2 carbon atoms and halogen atoms, are prepared by reacting a 5-(6-)phenylmercaptobenzimidazole of the formula with a halide of the formula R 2 CO.Hal or of the formula wherein Hal is chlorine or bromine. The compounds of the invention possess pharmaceutical properties.

Ophthalmic compositions for treating ocular hypertension

This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.

Process for preparing substituted benzimidazols

Calixarene derivatives and use of such compounds for sequestration of metals

Bioreductive cytotoxic agents

Imidazolyl-(2)-carbinols having hypolipidemic action and process for preparing them

Pharmaceutical preparations having hypolipidemic activity, which contain in addition to a pharmaceutically acceptable carrier an effective amount of an imidazolyl-(2)-carbinol of the general formula I < IMAGE > (I) in which R represents hydrogen, lower alkyl, phenyl or benzyl, R1 and R2 each represent hydrogen or together the group -CH=CH-CH=CH-, R3 and R4 represent hydrogen, lower alkyl, phenyl, lower haloalkyl, lower alkylphenyl, lower alkoxyphenyl, lower haloalkoxyphenyl, mono- or dihalophenyl, imidazolyl or benzylimidazolyl or R3 and R4 are together fluoryl of the formula < IMAGE > or of a physiologically tolerable acid addition salt thereof, and process for preparing them.

Ester derivatives of dimethylpropionic acid and pharmacetuical compositions containing them

The present invnetion relates to esters of 2,2-dimethylpropionic acid having the general formula (I) or pharmacological acceptable salts thereof, as well as to pharmacetical ocmpositons containing said compounds and having an inhibitory activity of elastase.

Substituted 2-alkoxycarbonylamine-5-(6)-phenylmercapto-benzimidazoles

Substituted 2-alkoxycarbonylamine-5(6)-phenylmercapto-benzimidazoles are described as well as a process for their manufacture. The compounds are chemotherapeutics being especially suitable for the control of parasites of humans and animals, for example for controlling nematodes.

Azole compounds, processes for their manufacture and their use

Herbicidal compositions

Patent FR2166117A1

Process for the production of higher molecular weight alkylated benzimidazoles and their compounds