СПОСОБ ПОЛУЧЕНИЯ АРОМАТИЧЕСКИХ ПРОИЗВОДНЫХ ИЛИ ИХ СОЛЕЙ С ОРГАНИЧЕСКИМИ ИЛИ НЕОРГАНИЧЕСКИМИ КИСЛОТАМИ ИЛИ ИХ РАЦЕМАТОВ

Использование: в фармацевтической промышленности. Сущность изобретения: получение ароматических соединений общей формулы I (см. описание изобретения), где m - 2, 3; Ar и Ar1 имеют различные значения, выбранные из тиенила, замещенного или незамещенного фенила, бензотиенила, нафтила, бифенила, индолила; X, X' различные и означают водород, а другие - водород, гидроксил или образуют с X'' углерод-углеродную связь, либо вместе X и X' образуют оксо- или диалкиламиноалкилоксиминогруппу; Y - N или C(X''); Q, R, T, Z, M имеют различные значения. Реагент I - соединение формулы II, реагент II -соединение III HOCOZ или соединение IV' W=C=N-Z с получением соединения IV, от которого отщепляют мягким гидролизом кислотным тетрапиранилоксигруппу, обработкой полученного N-защищенного алканоламина формулы V метансульфонилхлоридом, с получением мезилата формулы VI, который обрабатывают вторичным амином VII, отщепляют защитные группы и при желании переводят в соль. 4 з.п. ф-лы, 11 табл.

ПЕСТИЦИДНЫЕ КОМПОЗИЦИИ И СВЯЗАННЫЕ С НИМ СПОСОБЫ

СЕЛЕКТИВНЫЕ К BCL-2 АГЕНТЫ, ВЫЗЫВАЮЩИЕ АПОПТОЗ, ДЛЯ ЛЕЧЕНИЯ РАКА И ИММУННЫХ ЗАБОЛЕВАНИЙ

... 1. Соединение формулы Iили его терапевтически приемлемая соль, пролекарство или соль пролекарства,где Аявляется N или С(А);один, или два, или три, или каждый из А, В, Dи Eнезависимо выбраны из R, OR, SR, S(O)R, SOR, C(O)R, C(O)OR, OC(O)R, NHR, N(R), C(O)NHR, C(O)N(R), NHC(O)R, NHC(O)OR, NRC(O)NHR, NRC(O)N(R), SONHR, SON(R), NHSOR, NHSONHRили N(CH)SON(CH)R, а остальные независимо выбраны из H, F, Cl, Br, I, CN, CF, C(O)OH, C(O)NHили C(O)ORиYпредставляет собой H, CN, NO, C(O)OH, F, Cl, Br, I, CF, OCF, CFCF, OCFCF, R, OR, C(O)R, C(O)OR, SR, NH, NHR, N(R), NHC(O)R, C(O)NH, C(O)NHR, C(O)N(R), NHS(O)Rили NHSOR;или Ви Yвместе с атомами, с которыми они связаны, образуют имидазол или триазол иодин, или два, или каждый из А, Dи Eнезависимо выбраны из R, OR, SR, S(O)R, SOR, C(O)R, C(O)OR, OC(O)R, NHR, N(R), C(O)NHR, C(O)N(R), NHC(O)R, NHC(O)OR, NHC(O)NHR, N(CH)C(O)N(CH)R, SONHR, SON(R), NHSOR, NHSONHRили N(CH)SON(CH)R, а остальные независимо выбраны из H, F, Cl, Br,I, CF, C(O)OH, C(O)NHили C(O)OR; ...

Фунгицидный состав

Verfahren zur Herstellung von Aminocarbonsaeureamiden, welche die Atomgruppierung ? enthalten

Verfahren zur Herstellung von ungesaettigten Acylaminomethyl-aminen

"NEUE BENZOESAEUREN, IHRE HERSTELLUNG UND IHRE VERWENDUNG ALS ARZNEIMITTEL"

Verfahren zur Herstellung von Enaminen

Dibenzocycloheptene compounds and their preparation

Novel 3 - halosulphonyl - 7 - halo - 10,11 - dihydro - 5H - dibenzo[a,d]cyclohepten - 5 - ones, having no further substituents, are prepared by reacting a 3-halo-10,11-dihydro-5H-dibenzo[a,d] cyclohepten-5-one, having no further substituents, with a halosulphonic acid.

Dibenzocycloheptene compounds and their preparation

Novel compounds of the Formula I wherein the dotted line indicates the presence of an optional double-bond in the 10(11)-position, X represents a hydrogen or halogen atom, each of R and R1 represents a C1- 4 alkyl radical, and each of R11 and R111 represents a C1- 6 alkyl radical or R11 and R111 are linked through a carbon, nitrogen or oxygen atom so that -NR11R111 represents a heterocyclic group containing 5 or 6 atoms and salts thereof are prepared by reacting a ketone of the Formula II with a Grignard reagent of the formula HalMgCH2CH2CH2NR11R111, wherein Hal represents a halogen atom and hydrolysing the resulting Grignard adduct. ...

New nitrogen-containing polymers and process of preparation

The invention comprises polymers of formula where R is an aliphatic hydrocarbon radical containing at least 3 carbon atoms or an aromatic or cycloaliphatic hydrocarbon radical and n is an integer. The polymers are obtained by polycondensation of N,N1-bis-b -hydroxyethyl diamines of formula HO.CH2.CH2.NH.R.NH. -CH2.CH2.OH by heating in an inert atmosphere at above 250 DEG C. The starting material may be heated with a catalyst, e.g. orthophosphoric acid, pyrophosphoric acid, iodine, aluminium chloride or boron phosphate. Low molecular weight polymers may be obtained and may be converted to higher molecular weight products by further heating, e.g. at above 300 DEG C., and under reduced pressure, e.g. at below 0.5 mm. Hg. In examples polymers are obtained from N,N1 - bis - (b - hydroxyethyl) - dodecamethylene diamine, from N,N1-bis(b -hydroxyethyl)-m-phenylene diamine, from N,N1-bis-(b -hydroxyethyl)-1, 4-diaminocyclohexane, and from N,N1-bis-(b -hydroxyethyl) hexamethylenediamine.ALSO ...

Monoquaternary ammonium salts endowed with neurotropic spasmolytic activity

The invention comprises quaternary compounds of the formula (wherein R is methyl or ethyl, -NR1R11 is dialkylamino, each alkyl group containing at most 3 carbon atoms, pyrrolidino, morpholino or piperidino, X is one equivalent of a non-toxic anion, and Y is phenyl or cyclohexyl). They may be prepared by quaternization of the corresponding tertiary base, which in turn is prepared by condensing a compound of the formula with a secondary amine; or by directly condensing a halogen compound of the above formula with a tertiary amine. Examples are given.

BIS (BENZAMIDO)-BENZENE DERIVATIVES AND PROCESS FOR PREPARING THE SAME

SUBSTITUTED OXIMES PROCESSES FOR THEIR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS

... 1323453 Analgesic medicines CHOAY SA 7 Aug 1970 [8 Aug 1969] 38147/70 Heading A5B [Also in Division C2] Pharmaceutical compositions having analgesic activity, for oral, parenteral or rectal administration, comprise a compound of formula I: in which R 1 represents one or more substituents each attached at any available position on the phenyl nucleus and selected from -NO 2 , -OH, carbomethoxy, methyl-sulfonyl, halogen and alkyl groups containing one to three carbon atoms, two chlorine or methyl radicals not simultaneously occupying the 2 and 6 positions on the phenyl nucleus, or, except when R 2 is hydrogen and R 3 and R 4 are both ethyl groups, R 1 represents a hydrogen atom; R 2 is hydrogen or a methyl group; R 3 and R 4 are alkyl radicals containing from two to four carbon atoms, or together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heterocyclic group; and Y is an aliphatic divalent hydrocarbon group containing from two to four carbon atoms ...

N (tertiary amino-alkyl) - 2-alkylene (or alkinyle) oxy-benzamides and their method of preparation.

3- or 4-monosubstituted phenol and thiophenol derivatives useful as H3 ligands.

New carbonylated (AZA) cyclohexanes as dopamine D3receptor ligands

3-OR 4-Monosubstituted phenol and thiophenolderivatives useful as H3 ligands

New carbonylated (AZA) cyclohexanes as dopamine D3 receptor ligands

New substituted benzamides and their method of preparation.

3-OR 4-Monosubstituted phenol and thiophenolderivatives useful as H3 ligands

3-OR 4-Monosubstituted phenol and thiophenolderivatives useful as H3 ligands

N-ARYL-N' ARYLCYCLOALKYL UREA AS MCH ANTAGONIST FOR the TREATMENT OF OBESITY

Procedure for the production of new n (1-Aryloxy-2-hydroxypropyl) - amino acids and their derivatives

USE OF OMEGA CARBOXYARYL SUBSTITUTING DIPHENYLHARNSTOFFEN AS RAF KINASE INHIBITORS

AS H3-LIGANDEN APTITUDE 3ODER 4MONOSUBSTITUIERTE PHENOLUND of THIOPHENOL DERIVATIVES

NEW n (2-AMINOPHENYL) BENZAMIDDERIVATE WITH UREA STRUCTURE

PHARMACEUTICAL COMPOSITIONS CONTAINING 1BENZYL-1HYDROXY-2,3-DIAMINO-PROPYLAMINE, 3BENZYL-3 HYDROXY-2-AMINO-PROPIONSÄUREAMIDE AND USED CONNECTIONS AS ANALGESICS

ARYL AND HETEROARYL PIPERAZINYLCARBOXAMIDE ONE WITH EFFECT ON THE CENTER THE NERVOUS SYSTEM

- G (V) - CARBOXYARYL SUBSTITUTED DIPHENYL UREA AS RAF KINASE INHIBITORS

PROCEDURE FOR the PRODUCTION OF HALOGENIERTEN 2-AMINOBENZYLAMINEN AND THEIR SOUR ADDITION SALTS

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

As well as procedures for the production of new Amino dihalogenphenyl äthylaminen from their acid addition salts

Procedures for the production of new Dibenzocyloheptenen and of them acid addition salt

Procedure for the production of new α-6-Deoxy-5-oxytetracyclinen

N-ARYL-N' ARYLCYCLOALKYL UREA AS MCH ANTAGONIST FOR the TREATMENT OF OBESITY

N-ARYL-N' ARYLCYCLOALKYL UREA AS MCH ANTAGONIST FOR the TREATMENT OF OBESITY

N-ARYL-N' ARYLCYCLOALKYL UREA AS MCH ANTAGONIST FOR the TREATMENT OF OBESITY

N-ARYL-N' ARYLCYCLOALKYL UREA AS MCH ANTAGONIST FOR the TREATMENT OF OBESITY

N-ARYL-N' ARYLCYCLOALKYL UREA AS MCH ANTAGONIST FOR the TREATMENT OF OBESITY

N-ARYL-N' ARYLCYCLOALKYL UREA AS MCH ANTAGONIST FOR the TREATMENT OF OBESITY

N-ARYL-N' ARYLCYCLOALKYL UREA AS MCH ANTAGONIST FOR the TREATMENT OF OBESITY

N-ARYL-N' ARYLCYCLOALKYL UREA AS MCH ANTAGONIST FOR the TREATMENT OF OBESITY

N-ARYL-N' ARYLCYCLOALKYL UREA AS MCH ANTAGONIST FOR the TREATMENT OF OBESITY

N-ARYL-N' ARYLCYCLOALKYL UREA AS MCH ANTAGONIST FOR the TREATMENT OF OBESITY

N-ARYL-N' ARYLCYCLOALKYL UREA AS MCH ANTAGONIST FOR the TREATMENT OF OBESITY

Amine derivative having NPY Y5 receptor antagonist activity

Novel vanilloid receptor ligands and their use for producing medicaments

The invention relates to novel vanilloid receptor ligands, methods for the production thereof, medicaments containing these compounds, and to the use of these compounds for producing medicaments.

IMPROVEMENT IN THE STORAGE STABILITY OF PHOTOINITIATORS

Use of 1-benzyl-1-hydr0xy-2, 3-diamino-propyl amines, 3-benzyl-3-hydroxy-2-amino-propionic acid amides and related compounds as analgesics

BIS %BENZAMIDO<-BENZENE DERIVATIVES

N-ARYL-N'-ARYLCYCLOALKYL-UREA DERIVATIVES AS MCH ANTAGONISTS FOR THE TREATMENT OF OBESITY

BENZAMIDE DERIVATIVES AND PROCESSES FOR THEIR MANUFACTURE

BENZAMIDE DERIVATIVES AND PROCESSES FOR THEIR MANUFACTURE

COMPOUNDS

The present invention relates to a compound of formula (Ia), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X-Y is -NHSO2- or -SO2NH-; R1 is H or alkyl; R2 is selected from COOH and a tetrazolyl group; R3 is selected from H, Cl and alkyl; R4 is selected from H, Cl and F; R5 is selected from H, alkyl, alkynyl, alkenyl, haloalkyl, SO2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R6 is H; R7 is selected from H, CN, haloalkyl, Cl, F, SO2-alkyl, SO2NR13R14, optionally substituted heteroaryl and alkyl; R8 is selected from H, alkyl, haloalkyl and halo; R9 is H, C1-C3-alkyl, or halo; R10 and R11, together with the nitrogen to which they are attached, form an azepanyl group, wherein (a) said azepanyl group is substituted by one or more substituents, or (b) one or two carbons in said azepanyl group are replaced by a group selected from O, NH, S and CO, and said azepanyl group is optionally further substituted ...

AMINO ACID DERIVATIVES

METHODS OF USING AS ANALGESICS 1-BENZYL-1-HYDROXY-2,3-DIAMINO-PROPYL AMINES, 3-BENZYL-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES AND RELATED COMPOUNDS

... ²²²The compounds shown by the structural formulas below have analgesic effect and ²are used in compositions for treating a mammal in need of such treatment.² ...

PROCESS FOR PREPARING LINEZOLID

The present invention relates to a new process for preparing the oxazolid inone antibacterial agent linezolid which comprises the reaction of an (S)-I -chloro-3- (benzyIidenylamino)-propan-2-ol with a morpholinyl fluorophenyl carbamate to afford a protected imine intermediate which, upon hydrolysis an d acylation, yields linezolid in high yield.

SULFONAMIDE COMPOUND OR SALT THEREOF

Disclosed is a sulfonamide compound having a chemical structure character ized in that the compound has an amide structure wherein a carbon atom in th e amide binds to a nitrogen atom in a sulfonamide through a lower alkylene, or a salt of the compound. The compound or the salt has a potent antagonisti c activity against an EP1 receptor and is therefore useful as a therapeutic agent for a disease associated with an EP1 receptor, particularly lower urin ary tract symptom.

AZULENE HYDROXAMIC ACID DERIVATIVES AS METALLOPROTEIN INHIBITORS

The invention provides novel azulene derivatives of general formula (I) wherein R1 to R6 have the significance given in the description, as well as their tautomers, enantiomers, diastereomers, racemates and physiologically compatible salts or esters and substances which are hydrolyzed or metabolised in vivo to compounds of formula (I). The invention is also concerned with a process and intermediates for the manufacture of the above compounds, medicaments which contain such compounds as well as the use of these compounds in the production of medicaments having metalloprotein-inhibiting activity.

Verfahren zur Herstellung eines kapillaraktiven Mittels.

Procédé de préparation d'un nouveau dérivé sulfamidé.

Verfahren zur Herstellung neuer Anilide

Verfahren zur Herstellung neuer Amide

Verfahren zur Herstellung neuer Amide

Verfahren zur Herstellung neuer Amide

Verfahren zur Herstellung therapeutisch wirksamer Sulfonylharnstoffe

Verfahren zur Herstellung neuer Diazaverbindungen

Procédé de fabrication d'un dérivé nouveau de la tétracycline

Verfahren zur Herstellung von neuen Sulfonylharnstoffen

Verfahren zur Herstellung von neuen Sulfonylharnstoffen

Verfahren zur Herstellung von neuen Sulfonylharnstoffen

Verfahren zur Herstellung neuer Diazaverbindungen

Verfahren zur Herstellung neuer Diazaverbindungen

Verfahren zur Herstellung neuer Diazaverbindungen

Verfahren zur Herstellung von N,N'-tetrasubstituierten 3-Amino-2-azaprop-2-en-1-ylidenammoniumhalogeniden

Verfahren zur Herstellung von basischen Amiden

Verfahren zur Herstellung von basischen Amiden

Préparation des N-(tertiaire-aminoalkyl) benzamides substitués

Verfahren zur Herstellung von disubstituierten Piperazin-Derivaten mit antibiotischer Wirkung

Procédé de préparation de N-tertiaire-aminoalkyl-2-hydroxy (ou alcoxy) 4-amino-5-halogéno benzamides

Verfahren zur Herstellung von neuen Amino-dihalogen-phenyläthylaminen

Verfahren zur Herstellung von neuen Amino-dihalogenphenyläthylaminen

Procédé de préparation de N-(tertiaire amino-alkyl)-2-alkényl-(ou alkinyle) oxy-benzamides

Aromatic ethers

Compds. (R1R2)C6H3-X-CH2-Y-CH2-Z-C6H3(R3R4) (where R1 is NH2, AlkylNH, AlkanoylNH, AlkanoylIN(Alkyl) or AlkylINHSO2; R2 is H or Halogen; R3 and R4 are H, OH, NH2, halogen, alkyl or Oalkyl, X is O or S; Y is CH2, CHOH, CHOOCalkyl, CHOSO2alkyl, CHOSO2aryl, or CO- and Z is 1,4-piperazinyl) esp. racemic and (+)-2'-/3-/4-(o-methoxyphenyl)-1-piperazinyl/-2-hydroxypropoxy/-a- cetanilide and racemic 3'-/3-(4-phenyl-1-piperazinyl)-2-hydroxypropoxy/acetanilide are useful hypotensive agents and are prepd. by standard methods.

Aromatic ethers

Compds. (R1R2)C6H3-X-CH2-Y-CH2-Z-C6H3(R3R4) (where R1 is NH2, AlkylNH, AlkanoylNH, AlkanoylIN(Alkyl) or AlkylINHSO2; R2 is H or Halogen; R3 and R4 are H, OH, NH2, halogen, alkyl or Oalkyl, X is O or S; Y is CH2, CHOH, CHOOCalkyl, CHOSO2alkyl, CHOSO2aryl, or CO- and Z is 1,4-piperazinyl) esp. racemic and (+)-2'-/3-/4-(o-methoxyphenyl)-1-piperazinyl/-2-hydroxypropoxy/-a- cetanilide and racemic 3'-/3-(4-phenyl-1-piperazinyl)-2-hydroxypropoxy/acetanilide are useful hypotensive agents and are prepd. by standard methods.

Aromatic ethers

Compds. (R1R2)C6H3-X-CH2-Y-CH2-Z-C6H3(R3R4) (where R1 is NH2, AlkylNH, AlkanoylNH, AlkanoylIN(Alkyl) or AlkylINHSO2; R2 is H or Halogen; R3 and R4 are H, OH, NH2, halogen, alkyl or Oalkyl, X is O or S; Y is CH2, CHOH, CHOOCalkyl, CHOSO2alkyl, CHOSO2aryl, or CO- and Z is 1,4-piperazinyl) esp. racemic and (+)-2'-/3-/4-(o-methoxyphenyl)-1-piperazinyl/-2-hydroxypropoxy/-a- cetanilide and racemic 3'-/3-(4-phenyl-1-piperazinyl)-2-hydroxypropoxy/acetanilide are useful hypotensive agents and are prepd. by standard methods.

Verfahren zur Herstellung von 5H-Dibenzo(a,d)cycloheptenen

Procédé de préparation de dérivés de la phloramine

Procédé de préparation de bases de Mannich de l'a-6-deoxy-5-oxy-tétracycline

Verfahren zur Herstellung von N-o-Cyanophenyl-N',N'-dialkylformamidiniumsalzen

Procédé de préparation de dibenzo-oxépine-spiro-dioxolannes substiués

Verfahren zur Herstellung von Enaminen

Verfahren zur Herstellung von Sulfamylbenzoesäure-Derivaten und deren Verwendung

VERFAHREN ZUR HERSTELLUNG VON AMINOSAEUREDERIVATEN.

Procédé de fabrication d'oximes O-substituées présentant des propriétés analgésiques et anti-inflammatoires

Phenoxy substituted phenylamidine derivatives and their use as fungicides

The present invention relates to 3-substituted phenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to a composition for this purpose, comprising the phenoxyamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.

Polymerizable composition, color filter, and method of producing the same, solid-state imaging device, and planographic printing plate precursor, and novel compound

Disclosed is a photopolymerizable composition which contains a photopolymerization initiator (A) that has a partial structure represented by the following Formula (1) and a polymerizable compound (B). In General formula (1), R 3 and R 4 each independently represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group or an alkoxy group; R 3 and R 4 may form a ring with each other; and X represents OR 5 , SR 6 , or NR 17 R 18 . The photopolymerizable composition is capable of forming a cured film that has high sensitivity, excellent intra-membrane curability and excellent adhesion to a support. The cured film is able to maintain a patterned shape even during post-heating after development and has good pattern formability, while coloring due to heating with passage of time being suppressed.

3-Arylamino Pyridine Derivatives

The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.

C7-Fluoro Substituted Tetracycline Compounds

The present invention is directed to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.

4-carboxybenzylamino derivatives as histone deacetylase inhibitors

The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the 4-carboxybenzylamino derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the 4-carboxybenzylamino derivatives in vivo.

SUBSTITUTED CYCLOPENTYL-AZINES AS CASR-ACTIVE COMPOUNDS

Compounds of general formula I, (formula [I)], their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds. 3. A compound according to claim 1 , wherein Rrepresents methyl.4. A compound according to claim 1 , wherein X represents —CH—.5. A compound according to claim 1 , wherein X represents a nitrogen atom.6. A compound according to claim 1 , wherein Ar represents phenyl substituted with one or more claim 1 , same or different substituents independently selected from fluoro claim 1 , chloro claim 1 , methoxy or ethoxy.7. A compound according to claim 6 , wherein Ar represents 4-fluoro-3-methoxyphenyl.8. A compound according to claim 1 , wherein Ar represents naphthyl or benzodioxolyl.9. A compound according to claim 1 , wherein Rrepresents hydrogen.10. A compound according to claim 1 , wherein Rand Rtogether with the adjacent nitrogen atom to which they are attached forms a 6-membered Cheterocycloalkyl comprising 1 or 2 heteroatoms selected from the group consisting of O and N claim 1 , said Cheterocycloalkyl being optionally substituted by oxo claim 1 , —NH claim 1 , —S(O)NH claim 1 , —S(O)CH claim 1 , hydroxy claim 1 , halogen claim 1 , trifluoromethyl claim 1 , Calkyl claim 1 , Calkylcarbonyl claim 1 , Calkoxy claim 1 , aminoCalkyl claim 1 , or Calkylamino.11. A compound according to wherein Rand Rtogether with the adjacent nitrogen to which they are attached forms a 6-membered Cheterocycloalkyl comprising 1 or 2 heteroatoms selected from the group consisting of O and N claim 10 , said Cheterocyclic ring being optionally substituted by oxo claim 10 , —NH claim 10 , hydroxyCalkyl claim 10 , —S(O)CHor methylcarbonyl.12. A compound according to claim 11 , wherein the heterocycloalkyl represents piperidyl claim 11 ...

Phenyl amino pyrimidine compounds and uses thereof

The present invention relates to phenyl amino pyrimidine compounds which are inhibitors of protein kinases including JAK kinases. In particular the compounds are selective for JAK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.

Inhibitors of PI3K-Delta and Methods of Their Use and Manufacture

The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds. 35-. (canceled)6. The compound of claim 1 , wherein Ris H or methyl.7. The compound of claim 6 , wherein Q is absent or is (C-C)alkylene and Z is absent or is NH claim 6 , N(C-C)alkyl claim 6 , —NH—(C═O)— claim 6 , —N(C-C)alkyl-(C═O)— claim 6 , O claim 6 , or S.8. (canceled)9. The compound of Formula I-g of claim 2 , wherein Y is optionally substituted (C-C)alkylene claim 2 , wherein up to two carbon atoms of the (C-C)alkylene are replaced by NH claim 2 , N(C-C)alkyl claim 2 , —NH—(C═O)— claim 2 , —N(C-C)alkyl-(C═O)— claim 2 , or —(C═O)—.10. The compound of claim 9 , wherein Q is CHor CH(CH).11. The compound of claim 10 , wherein Z is absent or is —NH— claim 10 , —NH—(C═O)— claim 10 , or S.12. (canceled)14. The compound of claim 13 , wherein Ris NH claim 13 , purinyl claim 13 , pyrazinyl claim 13 , pyrazolopyrimidinyl claim 13 , benzodioxinyl claim 13 , phenyl claim 13 , morpholinyl claim 13 , oxadiazolyl claim 13 , cyclopropyl claim 13 , or pyridinyl claim 13 , any of which may be optionally substituted.18. The compound of claim 17 , wherein Z is absent or is O claim 17 , S claim 17 , —NH— or —NH(C═O)—.19. A compound of which is:9-{[2-(2-methylphenyl)quinolin-3-yl]methyl}-9H-purin-6-amine;9-{[3-(2-methylphenyl)quinoxalin-2-yl]methyl}-9H-purin-6-amine;9-{[8-methyl-2-(2-methylphenyl)quinolin-3-yl]methyl}-9H-purin-6-amine;8-methyl-2-(2-methylphenyl)-3-[(9H-purin-6-ylthio)methyl]quinoline;9-{[2-(2-chlorophenyl)-8-methylquinolin-3-yl]methyl}-9H-purin-6-amine;9-({2-[2-(ethyloxy)phenyl]-8-methylquinolin-3-yl}methyl)-9H-purin-6-amine;9-({8-methyl-2-[3-(methyloxy)phenyl]quinolin-3-yl}methyl)-9H-purin-6-amine;9-{[8-methyl-2-(3-{[2-(methyloxy)ethyl]oxy}phenyl)quinolin-3-yl]methyl}-9H-purin-6-amine;9-{[8-methyl-2-(3-methylphenyl)quinolin-3-yl]methyl}-9H-purin-6-amine;9-({8-methyl-2-[2-(trifluoromethyl)phenyl] ...

3-Arylamino Pyridine Derivatives

The invention provides novel, substituted 3-arylamino pyridine compounds 2. The method according to claim 1 , wherein the disease is selected from the group consisting of cancer claim 1 , inflammation claim 1 , pancreatitis or kidney disease claim 1 , pain claim 1 , benign hyperplasia of the skin claim 1 , restenosis claim 1 , prostate claim 1 , diseases related to vasculogenesis or angiogenesis claim 1 , tumor angiogenesis claim 1 , skin diseases selected from psoriasis claim 1 , eczema claim 1 , and sclerodema claim 1 , diabetes claim 1 , diabetic retinopathy claim 1 , retinopathy of prematurity claim 1 , age-related macular degeneration claim 1 , hemangioma claim 1 , glioma claim 1 , melanoma and Kaposi's sarcoma.3. The method according to claim 2 , wherein the disease is cancer or inflammation.4. The method according to claim 2 , wherein the cancer is selected from the group consisting of ovarian claim 2 , breast claim 2 , lung claim 2 , pancreatic claim 2 , prostate claim 2 , colon and epidermoid cancer.5. The method according to claim 3 , wherein the inflammation is selected from the group consisting of rheumatoid arthritis claim 3 , inflammatory bowel disease and atherosclerosis. This application is a divisional of U.S. application Ser. No. 13/472,721 filed on May 16, 2012, which is a continuation of U.S. application Ser. No. 13/112,490, filed on May 20, 2011, which is a divisional of U.S. application Ser. No. 11/665,651, filed on Oct. 19, 2005, which is the U.S. National Stage of International Application No. PCT/EP2005/011257, filed on Oct. 19, 2005, published in English, which claims priority under 35 U.S.C. §119 or §365 to European Application No. 04024967.4, filed Oct. 20, 2004. The entire teachings of the above applications are incorporated herein by reference.The invention relates to a series of substituted 3-arylamino pyridine derivatives that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also ...

IRE-1alpha INHIBITORS

Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies. 2. The compound of claim 1 , wherein the compound is represented by structural formula (E).3. The compound of claim 1 , wherein the compound is represented by structural formula (X).8. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a compound of or a pharmaceutically acceptable salt thereof; and'}a pharmaceutically acceptable carrier.9. A method of inhibiting IRE-1α activity claim 1 , comprising administering to a subject a compound of or a pharmaceutically acceptable salt of the compound.10. The method of claim 1 , wherein the compound is a compound of .11. The method of claim 1 , wherein the compound is a compound of .12. The method of claim 1 , wherein the compound is a compound of .13. The method of claim 1 , wherein the compound is a compound of .14. The method of claim 1 , wherein the compound is a compound of15. The method of claim 1 , wherein the compound is a compound of .16. The method of wherein cells of the subject have an activated unfolded protein response.17. The method of claim 9 , wherein the subject has cancer.18. The method of claim 17 , wherein the cancer is myeloma.19. The method of claim 9 , further comprising administering to the subject an agent that induces or up-regulates IRE-1α expression.20. The method of claim 9 , further comprising administering to the subject a biotherapeutic agent claim 9 , a chemotherapeutic agent claim 9 , radiation claim 9 , or a proteasome inhibitor. This application is a division of Ser. No. 12/941,530 filed on Nov. 8, 2010, which is a continuation of Ser. No. 12/135,571 filed on Jun. 9, 2008, now U.S. Pat. No. 7,858,666, which claims the benefit of Ser. No. 60/942,743 filed Jun. 8, 2007. ...

C7-FLUORO SUBSTITUTED TETRACYCLINE COMPOUNDS

The present invention is directed to a compound represented by Structural Formula (A): 4. The compound of claim 3 , wherein Ris hydrogen or a (C-C)alkyl.5. The compound of claim 3 , wherein Ris selected from (C-C)alkyl claim 3 , (C-C)cycloalkyl(C-C)alkyl claim 3 , (C-C)alkoxy(C-C)alkyl claim 3 , phenyl claim 3 , phenyl(C-C)alkyl claim 3 , (C-C)cycloalkyl and halo(C-C)alkyl claim 3 , wherein each alkyl claim 3 , alkoxy and cycloalkyl moiety in the groups represented by Ris optionally substituted with one or more substituents independently selected from the group consisting of (C-C)alkyl and halo; and each phenyl moiety in the groups represented by Ris optionally substituted with one or more substituents independently selected from the group consisting of (C-C)alkyl claim 3 , halo claim 3 , (C-C)alkoxy claim 3 , (C-C)alkoxy(C-C)alkyl claim 3 , —CN claim 3 , halo(C-C)alkyl claim 3 , and halo(C-C)alkoxy.6. The compound of any one of claim 3 , wherein Ris selected from hydrogen claim 3 , methyl and ethyl.7. The compound of claim 6 , wherein Ris selected from the group consisting of cyclopropyl claim 6 , cyclobutyl claim 6 , cyclopentyl claim 6 , cyclopropylmethyl claim 6 , cyclobutylmethyl claim 6 , phenyl claim 6 , benzyl claim 6 , —(CH)—O—CH claim 6 , —(CH)—OCH claim 6 , —C(CH) claim 6 , —CH(CH) claim 6 , —CHC(CH) claim 6 , —CHCH(CH) claim 6 , —CH—CF claim 6 , —(CH)—CHF claim 6 , and —(CH)CH; n is 0 claim 6 , 1 claim 6 , 2 claim 6 , 3 claim 6 , 4 claim 6 , 5 or 6; and wherein the phenyl or benzyl group represented by Ris optionally substituted with one or two substituents independently selected from the group consisting of (C-C)alkyl claim 6 , halogen claim 6 , (C-C)alkoxy claim 6 , (C-C)alkoxy(C-C)alkyl claim 6 , —CN claim 6 , halo(C-C)alkyl claim 6 , and halo(C-C)alkoxy.8. The compound of claim 7 , wherein Ris selected from cyclopropyl claim 7 , cyclopropylmethyl claim 7 , cyclobutyl claim 7 , cyclopentyl claim 7 , cyclohexyl claim 7 , —(CH)—O—CH claim 7 , —C(CH) ...

KAPPA OPIOID AGONISTS AND USES THEREOF

Provided are compounds of Formula I: 2. The compound of claim 1 , wherein Ris a phenyl substituted with 1 claim 1 , 2 claim 1 , or 3 halogen atoms.3. The compound of claim 1 , wherein Ris methyl.4. The compound of claim 1 , wherein Ris phenyl substituted with —X-POLY.5. The compound of claim 1 , wherein Rand Rare taken together to form an optionally substituted pyrrolidinyl.6. The compound of claim 1 , wherein X is:{'sub': 2', '2', '2', '2', '2', '2', '2', '2, 'a covalent bond; —C(O)NH—; —C(O)NHCH—; —C(O)NHCHCH—; —OC(O)NH—; —C(O)NH—; —O—; —NHC(O)—; —NHC(O)CH—; —NHC(O)CHO—; —NHC(O)CHCH—; —NH—; or —NHS(O)—.'}7. The compound of claim 1 , wherein POLY is a poly(alkylene oxide) oligomer.8. The compound claim 1 , wherein POLY is a poly(ethylene oxide) oligomer.9. The compound of claim 1 , wherein POLY is end-capped with a hydroxyl group claim 1 , a lower alkoxy group claim 1 , or a trifluoromethoxy group.15. A pharmaceutical composition comprising a compound of and at least one pharmaceutically acceptable excipient.16. A method of treating pain or inflammation comprising administering a compound of to a patient in need thereof. This application a Continuation of U.S. application Ser. No. 14/900,039, filed 18 Dec. 2015, which is a 35 U.S.C. §371 application of International Application No. PCT/US2014/044535, filed 27 Jun. 2014, designating the United States, which claims the benefit of priority under 35 U.S.C. §119(e) to both U.S. Provisional Patent Application Ser. No. 61/929,685, filed 21 Jan. 2014, and U.S. Provisional Patent Application Ser. No. 61/841,042, filed 28 Jun. 2013, the disclosures of which are incorporated herein by reference in their entireties.The present disclosure relates to novel compounds and to their use as agonists of the kappa opioid receptor. The disclosure also relates to methods for preparation of the compounds and to pharmaceutical compositions containing such compounds. The compounds described herein relate to and/or have application(s) in ( ...

ANTI-FIBROTIC PYRIDINONES

Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders. 2. The compound of claim 1 , wherein{'sup': 2', '5', '6', '7', '8, 'Ris selected from the group consisting of halogen, —OR, —NRR, and —C(O)R;'}{'sup': 3', '9, 'sub': 2', 'n', '6-10', '2', 'n', '2', 'n', '3-10', '2', 'n, 'Ris selected from the group consisting of —(CH)—(Caryl), —(CH)-(5-10 membered heteroaryl), —(CH)—(Ccarbocyclyl), and —(CH)-(3-10 membered heterocyclyl), each optionally substituted with one or more R;'}{'sup': 9', '5', '14', '15', '8', '16, 'sub': 1-6', '2-6', '2-6', '1-6', '2-8', '3-10', '6-10', '2', '2, 'each Ris independently selected from the group consisting of halogen, optionally substituted Calkyl, optionally substituted Calkenyl, optionally substituted Calkynyl, optionally substituted Calkylthio, optionally substituted Calkoxyalkyl, optionally substituted Ccarbocyclyl, optionally substituted Caryl, —OR, —NRR, —C(O)R, —SOR, and —NO; and'}{'sup': '11', 'sub': 1-6', '2-6', '2-6', '1-6, 'each Ris independently selected from the group consisting of halogen, —CN, optionally substituted Calkyl, optionally substituted Calkenyl, optionally substituted Calkynyl, and optionally substituted Calkoxy.'}3. The compound of claim 1 , wherein Ris a Caryl optionally substituted with one or more R.4. The compound of claim 3 , wherein Ris a phenyl optionally substituted with one or more R.5. The compound of claim 1 , wherein Ris a 5-10 membered heteroaryl optionally substituted with one or more R.6. The compound of claim 5 , wherein Ris a pyrazolyl or 1-methylpyrazolyl optionally substituted with one or more R.7. The compound of claim 1 , wherein each Ris independently selected from halogen claim 1 , or optionally substituted Calkyl.8. (canceled)9. The compound of claim 7 , wherein Ris methyl.10. (canceled)11. (canceled)12. The compound of claim 1 , wherein Ris —CN.13. The compound of claim 1 , wherein Ris −OR.14. The compound of claim 13 , ...

BENZAMIDES AND RELATED INHIBITORS OF FACTOR XA

Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders. 172.-. (canceled)74. The method of claim 73 , wherein the salt is the maleate salt.75. The method of claim 73 , wherein the compound is administered to the mammal in the form of a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier.76. The method of claim 75 , wherein the pharmaceutical composition is in capsule form.78. The method of claim 77 , wherein the salt is the maleate salt.79. The method of claim 77 , wherein the compound is administered to the mammal in the form of a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier.80. The method of claim 79 , wherein the pharmaceutical composition is in capsule form.82. The method of claim 81 , wherein the salt is the maleate salt.83. The method of claim 81 , wherein the compound is administered to the mammal in the form of a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier.84. The method of claim 83 , wherein the pharmaceutical composition is in capsule form. This invention relates to novel compounds which are potent and highly selective inhibitors of isolated factor Xa or when assembled in the prothrombinase complex. These compounds show selectivity for factor Xa versus other proteases of the coagulation (e.g. thrombin, fVIIa, fIXa) or the fibrinolytic cascades (e.g. plasminogen activators, plasmin). In another aspect, the present invention relates to novel monoamidino-containing compounds, their pharmaceutically acceptable salts, and pharmaceutically acceptable compositions thereof which are useful as potent and specific inhibitors of blood ...

Compounds for treating viral infections

The present invention relates to small molecule compounds and their use in the treatment of diseases, in particular viral diseases, in particular hepatitis C virus (HCV).

MU OPIOID RECEPTOR MODULATORS

Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity. 141.-. (canceled)43. The method of claim 42 , wherein said method does not comprise an increased risk of respiratory depression or constipation.45. (canceled)48. The method of claim 47 , wherein said method does not comprise modulating arrestin function.49. The method of claim 42 , wherein Ring A is R-substituted or unsubstituted phenyl.50. The method of claim 42 , wherein Ris independently hydrogen claim 42 , —CF claim 42 , —CN claim 42 , —OH claim 42 , —NH claim 42 , —COOH claim 42 , —CONH claim 42 , —NO claim 42 , —SH claim 42 , —SOH claim 42 , —SOH claim 42 , —SONH claim 42 , —NHNH claim 42 , —ONH claim 42 , —NHC═(O)NHNH claim 42 , —NHC═(O)NH claim 42 , —NHSOH claim 42 , —NHC═(O)H claim 42 , —NHC(O)OH claim 42 , —NHOH claim 42 , —CHF claim 42 , —CHF claim 42 , —OCF claim 42 , —OCHF claim 42 , substituted or unsubstituted (C-C) alkyl claim 42 , or unsubstituted 2 to 5 membered heteroalkyl.53. The method of claim 52 , wherein Rand Rare independently an unsubstituted methyl.54. The method of claim 42 , wherein:Ring A is unsubstituted phenyl and Ring B is unsubstituted thienyl;Ring A is para-hydroxy substituted phenyl and Ring B is unsubstituted thienyl;Ring A is para-hydroxy substituted phenyl and Ring B is unsubstituted phenyl;Ring A is para-hydroxy substituted phenyl and Ring B is unsubstituted benzothienyl;Ring A is para-hydroxy substituted phenyl and Ring B is para-methyl substituted phenyl;Ring A is 2-hydroxy pyridin-4-yl and Ring B is unsubstituted thienyl;Ring A is 2-hydroxy pyridin-5-yl and Ring B is unsubstituted thienyl;Ring A is para-hydroxy substituted phenyl and Ring B is unsubstituted naphthyl; orRing A is para-hydroxy substituted phenyl and Ring B is unsubstituted 2,3-dihydro-1H-indenyl.55. The method of claim 42 , wherein Ring B is an unsubstituted phenyl or an unsubstituted 3-thienyl.56. The method of claim 42 , wherein:{'sup': '1', 'sub': 1', '5 ...

C7-fluoro substituted tetracycline compounds

The present invention is directed to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.

Anti-Fibrotic Pyridinones

Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders. 2. The compound of claim 1 , wherein{'sup': 2', '5', '6', '7', '8, 'Ris selected from the group consisting of halogen, —OR, —NRR, and —C(O)R;'}{'sup': 3', '9, 'sub': 2', 'n', '2', 'n', '3-10', '2', 'n, 'Ris selected from the group consisting of phenyl, —(CH)-(5-10 membered heteroaryl), —(CH)—(Ccarbocyclyl), and —(CH)-(3-10 membered heterocyclyl), each optionally substituted with one or more R;'}{'sup': 9', '5', '14', '15', '8', '16, 'sub': 1-6', '2-6', '2-6', '1-6', '2-8', '3-10', '6-10', '2', '2, 'each Ris independently selected from the group consisting of halogen, optionally substituted Calkyl, optionally substituted Calkenyl, optionally substituted Calkynyl, optionally substituted Calkylthio, optionally substituted Calkoxyalkyl, optionally substituted Ccarbocyclyl, optionally substituted Caryl, —OR, —NRR, —C(O)R, —SOR, and —NO; and'}{'sup': '11', 'sub': 1-6', '2-6', '2-6', '1-6, 'each Ris independently selected from the group consisting of halogen, —CN, optionally substituted Calkyl, optionally substituted Calkenyl, optionally substituted Calkynyl, and optionally substituted Calkoxy.'}3. The compound of claim 1 , wherein Ris a Caryl optionally substituted with one or more R.4. The compound of claim 3 , wherein Ris a phenyl optionally substituted with one or more R.5. The compound of claim 1 , wherein Ris a 5-10 membered heteroaryl optionally substituted with one or more R.6. The compound of claim 5 , wherein Ris a pyrazolyl or 1-methyl pyrazolyl optionally substituted with one or more R.7. The compound of claim 1 , wherein each Ris independently selected from halogen claim 1 , or optionally substituted Calkyl.8. (canceled)9. The compound of claim 7 , wherein Ris methyl.1011.-. (canceled)12. The compound of claim 1 , wherein Ris —CN.13. The compound of claim 1 , wherein Ris —OR.14. The compound of claim 13 , wherein Ris selected from hydrogen ...

COMPOUNDS AND METHODS OF TREATING INFECTIONS

The invention provides compounds of Formula I, and methods of treating or preventing a bacterial infection in a subject using a compound of Formula I. The invention also provides the use of a compound of Formula I in the manufacture of a medicament for the treatment of a bacterial infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a bacterial infection in a subject and to a medical device comprising the composition of the invention. 148.-. (canceled)49. A compound selected from the group consisting of:NCL178 4,6-bis(2-((E)-1-(4-chlorophenyl)ethylidene)hydrazinyl)pyrimidineNCL179 4,6-bis(2-((E)-4-chlorobenzylidene)hydrazinyl)pyrimidin-2-amineNCL180 (2Z,2′Z)-2,2′-(pyrimidine-4,6-diylbis(hydrazin-2-yl-1-ylidene))bis(2-(4-chlorophenyl)ethan-1-ol)NCL 181 4,6-bis(2-((E)-4-chlorobenzylidene)hydrazinyl)pyrimidineNCL183 N4,N6-bis(1-phenylethyl)pyrimidine-4,6-diamineNCL184 N4,N6-bis(1-phenylethyl)pyrimidine-2,4,6-triamineNCL185 4,6-bis(2-((E)-1-(4-chlorophenyl)ethylidene)hydrazinyl)pyrimidinehydrochlorideNCL 187 4,6-bis(2-((E)-4-chlorobenzylidene)hydrazinyl)pyrimidinehydrochlorideNCL189 (2Z,2′Z)-2,2′-(pyrimidine-4,6-diylbis(hydrazin-2-yl-1-ylidene))bis(2-(4-chlorophenyl)ethan-1-ol)hydrochlorideNCL193 4,6-bis(2-((E)-4-bromobenzylidene)hydrazinyl)pyrimidin-2-amineNCL194 N′,N′″-(2-aminopyrimidine-4,6-diyl)di(benzohydrazide)NCL195 4,6-bis(2-((E)-4-methylbenzylidene)hydrazinyl)pyrimidin-2-amineNCL 196 4,4′-((1E,1′E)-((2-aminopyrimidine-4,6-diyl)bis(hydrazin-2-yl-1-ylidene))bis(methanylylidene))diphenolNCL197 3,3′-((1E,1′E)-((2-aminopyrimidine-4,6-diyl)bis(hydrazin-2-yl-1-ylidene))bis(methanylylidene))diphenolNCL198 4,6-bis(2-((E)-4-(tert-butyl)benzylidene)hydrazinyl)pyrimidin-2-aminedihydrochlorideNCL199 4,6-bis(2-((E)-benzylidene)hydrazinyl)pyrimidin-2-amineNCL200 4,6-bis(2-((E)-4-(tert-butyl)benzylidene)hydrazinyl)pyrimidin-2-amineNCL201 4,4′-((1E,1′E)-((2-aminopyrimidine-4,6-diyl)bis(hydrazin-2-yl-1-ylidene)) ...

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

This document discloses molecules having the following formula (“Formula One”): 2. A molecule according to wherein R1 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.3. A molecule according to wherein R2 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.4. A molecule according to wherein R3 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , ...

2-Acylaminopropoanol-Type Glucosylceramide Synthase Inhibitors

A compound is represented by Structural Formula (I): 189-. (canceled)91. The compound of claim 90 , wherein Ris an optionally substituted aryl or arylalkyl group claim 90 , wherein aryl claim 90 , used alone or as in arylalkyl claim 90 , is a carbocyclic aromatic ring having 6 to 14 carbon atoms or an aromatic ring having 5 to 14 ring atoms selected from carbon and at least one heteroatom and arylalkyl includes straight and branched saturated chains.92. The compound of claim 90 , wherein the compound is a (1R claim 90 ,2R) stereoisomer.93. The compound of claim 90 , wherein Ris an aryl or lower arylalkyl group each optionally and independently substituted with one or more substituents selected from the group consisting of halogen claim 90 , C1-C10 alkyl claim 90 , C1-C10 haloalkyl claim 90 , Ar claim 90 , —OR claim 90 , —O(haloalkyl) claim 90 , —SR claim 90 , —NO claim 90 , —CN claim 90 , —N(R) claim 90 , —NRC(O)R claim 90 , —C(O)R claim 90 , —C(O)OR claim 90 , —OC(O)R claim 90 , —C(O)N(R) claim 90 , —V—Ar claim 90 , —V—OR claim 90 , —V—O(haloalkyl) claim 90 , —V—SR claim 90 , —V—NO claim 90 , —V—CN claim 90 , —V—N(R) claim 90 , —V—NRC(O)R claim 90 , —V—C(O)R claim 90 , —V—COR claim 90 , —V—OC(O)R claim 90 , —V—C(O)N(R)— claim 90 , —O—V—Ar claim 90 , —O—V—N(R) claim 90 , —S—V—Ar claim 90 , —S—V—N(R) claim 90 , —N(R)—V—Ar claim 90 , —N(R)—V—N(R) claim 90 , —NRC(O)—V—N(R) claim 90 , —NRC(O)—V—Ar claim 90 , —C(O)—V—N(R) claim 90 , —C(O)—V—Ar claim 90 , —C(O)O—V—N(R) claim 90 , —C(O)O—V—Ar claim 90 , —O—C(O)—V—N(R) claim 90 , —O—C(O)—V—Ar claim 90 , —C(O)N(R)—V—N(R) claim 90 , —C(O)N(R)—V—Ar claim 90 , —O—[CH]—O— and —[CH]— claim 90 , wherein lower arylalkyl includes straight and branched saturated chains containing one to six carbon atoms.96. The compound of claim 95 , wherein —N(RR) is an unsubstituted pyrrolidinyl claim 95 , azetidinyl claim 95 , piperidinyl claim 95 , piperazinyl or morpholinyl group.97. The compound of claim 96 , wherein each of rings A-Z5 is ...

C7-FLUORO SUBSTITUTED TETRACYCLINE COMPOUNDS

The present invention is directed to a compound represented by Structural Formula (A): 4. The compound of claim 3 , wherein Ris hydrogen or a (C-C)alkyl.5. The compound of claim 3 , wherein Ris selected from (C-C)alkyl claim 3 , (C-C)cycloalkyl(C-C)alkyl claim 3 , (C-C)alkoxy(C-C)alkyl claim 3 , phenyl claim 3 , phenyl(C-C)alkyl claim 3 , (C-C)cycloalkyl and halo(C-C)alkyl claim 3 , wherein each alkyl claim 3 , alkoxy and cycloalkyl moiety in the groups represented by Ris optionally substituted with one or more substituents independently selected from the group consisting of (C-C)alkyl and halo; and each phenyl moiety in the groups represented by Ris optionally substituted with one or more substituents independently selected from the group consisting of (C-C)alkyl claim 3 , halo claim 3 , (C-C)alkoxy claim 3 , (C-C)alkoxy(C-C)alkyl claim 3 , —CN claim 3 , halo(C-C)alkyl claim 3 , and halo(C-C)alkoxy.6. The compound of claim 3 , wherein Ris selected from hydrogen claim 3 , methyl and ethyl.7. The compound of claim 6 , wherein Ris selected from the group consisting of cyclopropyl claim 6 , cyclobutyl claim 6 , cyclopentyl claim 6 , cyclopropylmethyl claim 6 , cyclobutylmethyl claim 6 , phenyl claim 6 , benzyl claim 6 , —(CH)—O—CH claim 6 , —(CH)—OCH claim 6 , —C(CH) claim 6 , —CH(CH) claim 6 , —CHC(CH) claim 6 , —CHCH(CH) claim 6 , —CH—CF claim 6 , —(CH)—CHF claim 6 , and —(CH)CH; n is 0 claim 6 , 1 claim 6 , 2 claim 6 , 3 claim 6 , 4 claim 6 , 5 or 6; and wherein the phenyl or benzyl group represented by Ris optionally substituted with one or two substituents independently selected from the group consisting of (C-C)alkyl claim 6 , halogen claim 6 , (C-C)alkoxy claim 6 , (C-C)alkoxy(C-C)alkyl claim 6 , —CN claim 6 , halo(C-C)alkyl claim 6 , and halo(C-C)alkoxy.8. The compound of claim 7 , wherein Ris selected from cyclopropyl claim 7 , cyclopropylmethyl claim 7 , cyclobutyl claim 7 , cyclopentyl claim 7 , cyclohexyl claim 7 , —(CH)—O—CH claim 7 , —C(CH) claim 7 , —CH( ...

BIODEGRADABLE LIPIDS FOR THE DELIVERY OF ACTIVE AGENTS

The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid. 119-. (canceled)21. The lipid particle of claim 20 , wherein the biodegradable group is an ester.22. The lipid particle of claim 20 , wherein the head group comprises an aliphatic group and a hydroxyl group.23. The lipid particle of claim 20 , wherein the head group consists of a saturated aliphatic group and a hydroxyl group.24. The lipid particle of claim 20 , wherein the hydrophobic tails have different chemical formulas.25. The lipid particle of claim 20 , wherein claim 20 , in each hydrophobic tail claim 20 , Ris a saturated claim 20 , straight-chain C-Calkyl group.26. The lipid particle of claim 20 , wherein claim 20 , in each hydrophobic tail claim 20 , Ris n-hexyl.27. The lipid particle of claim 20 , wherein claim 20 , in each hydrophobic tail claim 20 , Ris branched.28. The lipid particle of claim 21 , wherein the ester group in each hydrophobic tail is —OC(O)—.29. The lipid particle of claim 21 , wherein the ester group in each hydrophobic tail is —C(O)O—.30. The lipid particle of claim 20 , wherein claim 20 , in each hydrophobic tail claim 20 , Ris a saturated claim 20 , branched C-Calkyl group claim 20 , where the branching occurs at the α-position relative to the biodegradable group claim 20 , and where the total carbon atom content of the tail is 21 to 26.31. The lipid particle of claim 20 , wherein claim 20 , in the at least one hydrophobic tail claim 20 , the biodegradable group is separated from a ...

BIODEGRADABLE LIPIDS FOR THE DELIVERY OF ACTIVE AGENTS

The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid. 119-. (canceled)20. A pharmaceutical composition comprising a lipid particle and a pharmaceutically acceptable diluent , wherein the lipid particle comprises:(i) a nucleic acid;(ii) 35-65 mol % of a lipid compound;(iii) 3-12 mol % of distearoylphosphatidylcholine (DSPC);(iv) 15-45 mol % of cholesterol; and(v) 0.5-10 mol % of 1-(monomethoxy-polyethylene glycol)-2,3-dimyristoyl glycerol (PEG-DMG) having an average molecular weight of 2,000 Da, wherein the lipid compound comprises a head group, two hydrophobic tails, and a central moiety to which the head group and the two hydrophobic tails are directly bonded, wherein:the central moiety is a nitrogen atom;{'sup': 12', '1', '13', '12', '1', '13, 'sub': 4', '14', '10', '20, 'each of the two hydrophobic tails independently has the formula —R-M-R, wherein Ris a C-Calkyl group, Mis a biodegradable group, and Ris a C-Calkyl group;'}in each hydrophobic tail, the biodegradable group is separated from a terminus of the hydrophobic tail by from 8 to 12 carbon atoms; and{'sup': '13', 'in at least one hydrophobic tail, Ris branched, where the branching occurs at the α-position relative to the biodegradable group, and where the total carbon atom content of the at least one tail is 21 to 26.'}21. The pharmaceutical composition of claim 20 , wherein the nucleic acid comprises RNA.22. The pharmaceutical composition of claim 20 , further comprising sodium acetate.23. The pharmaceutical ...

BIODEGRADABLE LIPIDS FOR THE DELIVERY OF ACTIVE AGENTS

The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid. 119-. (canceled)20. A pharmaceutical composition comprising a lipid particle and a pharmaceutically acceptable diluent , wherein the lipid particle comprises:(i) a nucleic acid;(ii) 35-65 mol % of a lipid compound;(iii) 3-12 mol % of distearoylphosphatidylcholine (DSPC);(iv) 15-45 mol % of cholesterol; and(v) 0.5-10 mol % of a PEG-modified lipid, whereinthe lipid compound comprises a head group, two hydrophobic tails, and a central moiety to which the head group and the two hydrophobic tails are directly bonded, wherein:the central moiety is a nitrogen atom;{'sup': 12', '1', '13', '12', '1', '13, 'sub': 4', '14', '10', '20, 'each of the two hydrophobic tails independently has the formula —R-M-R, wherein Ris a C-Calkyl group, Mis a biodegradable group, and Ris a C-Calkyl group;'}in each hydrophobic tail, the biodegradable group is separated from a terminus of the hydrophobic tail by from 8 to 12 carbon atoms; and{'sup': '13', 'in at least one hydrophobic tail, Ris branched, where the branching occurs at the α-position relative to the biodegradable group, and where the total carbon atom content of the at least one tail is 21 to 26.'}21. The pharmaceutical composition of claim 20 , wherein the nucleic acid comprises RNA.22. The pharmaceutical composition of claim 20 , wherein the pharmaceutical composition is a vaccine.23. The pharmaceutical composition of claim 20 , further comprising sodium chloride.24. The pharmaceutical ...

PHENYL CARBAMATES AND THEIR USE AS INHIBITORS OF THE FATTY ACID AMIDE HYDROLASE (FAAH) ENZYME AND MODULATORS OF THE D3 DOPAMINE RECEPTOR (D3DR)

The invention provides compounds of Formula (I) or pharmaceutically acceptable salts thereof 2. A compound of Formula (I) according to wherein:Ar′ is a benzene, indole, naphthyl or pyridine ring;{'sub': 1', '2', '1-6', '3, 'Rand Rare, independently, hydrogen, halogen, Calkoxy, CF;'}X is N or CH;{'sub': 2', '2', 'n', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'Y is CH—(CH)—, —CH, where n is 0 or an integer from 1 to 2, or a group CH—CH═CH—CH, CHCH(OH)CHCH, CHCH(F)CH, CHCH(F)CHCH, CHCH(OH)CH, CH(CHF)CH, CH(CHF) CHCH, CH(CHOH)CH;'}{'sub': 3', '5', '5', '1-6', '2', '3', '3, 'Ris a phenyl, benzyl, benzoyl or a pyridine ring attached to phenyl ring in the meta or para position and optionally substituted by up to two same or different substituents R, wherein Ris halogen, Calkyl or a group CONHor CONHCHattached to Rin the meta or para position;'}{'sub': 3', '6', '6', '3, 'or Ris a 5- to 7-membered heterocyclic ring comprising up to 2 heteroatoms attached to the phenyl ring in the meta or para position and optionally substituted by up to two same or different substituents R, wherein Ris gem-difluoro, gem-dimethyl, COMe, attached to Rin any position of the ring;'}{'sub': 4', '1-6', '1-6', '3', '4, 'Ris hydrogen, halogen, Calkyl, Calkoxy, CF; the group Rcan be attached to the phenyl ring in any position of the ring;'}{'sub': 3', '4, 'or Rand Rtogether with the phenyl ring to which they are connected may form a 9H-carbazole ring.'}3. A compound of Formula (I) according to claim 2 , wherein:Ar′ is a benzene ring;{'sub': 1', '2', '3, 'Rand Rare, independently, H, Cl, or OMe, Me, CF;'}X is N or CH;{'sub': 2', '2', 'n', '2', '2', '2', '2', '2', '2', '2', '2, 'Y is CH—(CH)—CH, where n is 0 or an integer from 1 to 2, or a group CH—CH═CH—CH, a group CH(CHF)CH, or a group CHCH(F)CHCH;'}{'sub': 3', '2', '3', '3, 'Ris a phenyl, benzyl, benzoyl or pyridine ring attached to the phenyl ring in the meta or para position and optionally ...

Inhibitors of PI3K-Delta and Methods of Their Use and Manufacture

The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds. 35-. (canceled)6. The compound of claim 1 , wherein Ris H or methyl.7. The compound of claim 6 , wherein Q is absent or is (C-C)alkylene and Z is absent or is NH claim 6 , N(C-C)alkyl claim 6 , —NH—(C═O)— claim 6 , —N(C-C)alkyl-(C═O)— claim 6 , O claim 6 , or S.8. (canceled)9. The compound of Formula I-g of claim 2 , wherein Y is optionally substituted (C-C)alkylene claim 2 , wherein up to two carbon atoms of the (C-C)alkylene are replaced by NH claim 2 , N(C-C)alkyl claim 2 , —NH—(C═O)— claim 2 , —N(C-C)alkyl-(C═O)— claim 2 , or —(C═O)—.10. The compound of claim 9 , wherein Q is CHor CH(CH).11. The compound of claim 10 , wherein Z is absent or is —NH— claim 10 , —NH—(C═O)— claim 10 , or S.12. (canceled)14. The compound of claim 13 , wherein Ris NH claim 13 , purinyl claim 13 , pyrazinyl claim 13 , pyrazolopyrimidinyl claim 13 , benzodioxinyl claim 13 , phenyl claim 13 , morpholinyl claim 13 , oxadiazolyl claim 13 , cyclopropyl claim 13 , or pyridinyl claim 13 , any of which may be optionally substituted.18. The compound of claim 17 , wherein Z is absent or is O claim 17 , S claim 17 , —NH— or —NH(C═O)—.19. A compound of which is:9-{[2-(2-methylphenyl)quinolin-3-yl]methyl}-9H-purin-6-amine;9-{[3-(2-methylphenyl)quinoxalin-2-yl]methyl}-9H-purin-6-amine;9-{[8-methyl-2-(2-methylphenyl)quinolin-3-yl]methyl}-9H-purin-6-amine;8-methyl-2-(2-methylphenyl)-3-[(9H-purin-6-ylthio)methyl]quinoline;9-{[2-(2-chlorophenyl)-8-methylquinolin-3-yl]methyl}-9H-purin-6-amine;9-({2-[2-(ethyloxy)phenyl]-8-methylquinolin-3-yl}methyl)-9H-purin-6-amine;9-({8-methyl-2-[3-(methyloxy)phenyl]quinolin-3-yl}methyl)-9H-purin-6-amine;9-{[8-methyl-2-(3-{[2-(methyloxy)ethyl]oxy}phenyl)quinolin-3-yl]methyl}-9H-purin-6-amine;9-{[8-methyl-2-(3-methylphenyl)quinolin-3-yl]methyl}-9H-purin-6-amine;9-({8-methyl-2-[2-(trifluoromethyl)phenyl] ...

PHENYL AMINO PYRIMIDINE COMPOUNDS AND USES THEREOF

The present invention relates to phenyl amino pyrimidine compounds which are inhibitors of protein kinases including JAK kinases. In particular the compounds are selective for JAK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.

BCL-3 INHIBITORS

The present application relates to compounds of any one of Formulae I, Ia, Ib, Ic, Id, Ie, and If. Compounds of Formula I have the structure: 10. A method for the treatment of cancer claim 1 , the method comprising administering to a subject in need of such treatment an effective amount of a compound according to .11. The method of claim 10 , wherein the cancer is leukaemia or lymphoma.12. The method of claim 11 , wherein the cancer is anaplastic large cell lymphoma (ALCL) claim 11 , Classic Hodgkin lymphoma (cHL) claim 11 , non-Hodgkin's lymphoma; or a solid tumour cancer.13. The method of claim 12 , wherein the solid tumour cancer is breast cancer claim 12 , melanoma claim 12 , lung cancer claim 12 , pancreatic cancer claim 12 , oesophageal cancer claim 12 , colorectal cancer claim 12 , nasopharyngeal carcinoma claim 12 , or hepatocarcinoma.14. A method according to claim 10 , wherein the treatment comprises the treatment or prevention of metastasis in cancer.15. A method according to wherein the cancer is breast cancer.16. A method according to wherein the cancer is triple negative breast cancer or HER2 enriched breast cancer.17. A method according to wherein the compound is to be used in combination with one or more additional active agents which are useful in the treatment of cancer.18. A method according to claim 17 , wherein the one or more additional active agents are selected from:anti-HER2 agents;standard adjuvant therapy regimens; andanti-angiogenic/antimetastatic agents.19. A pharmaceutical composition comprising a compound according to and a pharmaceutically or veterinarily acceptable excipient or carrier.2087. A process for the preparation of a pharmaceutical composition according to claim claim 1 , the process comprising bringing the compound according to into association with a pharmaceutically or veterinarily acceptable excipient or carrier. This application is a continuation of U.S. application Ser. No. 15/500,016 filed on Jan. 27, 2017, which ...

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

This document discloses molecules having the following formula (“Formula One”):

C7-Fluoro Substituted Tetracycline Compounds

The present invention is directed to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.

GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES

Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS). 3. (canceled)4. The compound of claim 1 , wherein Rand Rtogether with the nitrogen to which they are attached form a 4-5 membered monocyclic heterocycloalkyl ring or a 7-8 membered bicyclic heterocycloalkyl; each of which is optionally substituted with 1 or 2 R; optionally as a tautomer claim 1 , a single stereoisomer or mixture of stereoisomers thereof and additionally optionally as a pharmaceutically acceptable salt thereof.5. (canceled)6. The compound of claim 1 , wherein Ris aryl which is optionally substituted with 1 claim 1 , 2 claim 1 , or 3 Rgroups; optionally as a tautomer claim 1 , a single stereoisomer or mixture of stereoisomers thereof and additionally optionally as a pharmaceutically acceptable salt thereof.7. The compound of claim 6 , wherein each R claim 6 , when present claim 6 , is independently halo claim 6 , alkoxy claim 6 , alkenyloxy claim 6 , hydroxyalkyloxy claim 6 , haloalkoxy claim 6 , cycloalkylthio claim 6 , cycloalkyloxy claim 6 , cycloalkylalkyloxy claim 6 , heterocycloalkyloxy claim 6 , or heterocycloalkylalkyloxy; optionally as a tautomer claim 6 , a single stereoisomer or mixture of stereoisomers thereof and additionally optionally as a pharmaceutically acceptable salt thereof.8. (canceled)9. The compound of claim 1 , wherein Ris heteroaryl which is optionally substituted with 1 claim 1 , 2 claim 1 , or 3 Rgroups; optionally as a tautomer claim 1 , a single stereoisomer or mixture of stereoisomers thereof and additionally optionally as a pharmaceutically acceptable salt thereof.10. The compound of claim 9 , wherein Ris 2 claim 9 ,3-dihydrobenzo[b][1 claim 9 ,4]dioxin-6-yl optionally substituted with a halo; optionally as a tautomer claim 9 , a single ...

Dihydrazone compounds having high affinity to a beta protein and tau protein, derivatives thereof and use thereof

The present disclosure provides dihydrazone compounds having high affinity to Aβ protein and Tau protein and derivatives thereof. The structure of the compounds is shown by formula (I)

Anti-Fibrotic Pyridinones

Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders. 2. The compound of claim 1 , wherein{'sup': 2', '5', '6', '7', '8, 'Ris selected from the group consisting of halogen, —OR, —NRR, and —C(O)R;'}{'sup': 3', '9, 'sub': 2', 'n', '6-10', '2', 'n', '2', 'n', '3-10', '2', 'n, 'Ris selected from the group consisting of —(CH)—(Caryl), —(CH)-(5-10 membered heteroaryl), —(CH)—(Ccarbocyclyl), and —(CH)-(3-10 membered heterocyclyl), each optionally substituted with one or more R;'}{'sup': 9', '5', '14', '15', '8', '16, 'sub': 1-6', '2-6', '2-6', '1-6', '2-8', '3-10', '6-10', '2', '2, 'each Ris independently selected from the group consisting of halogen, optionally substituted Calkyl, optionally substituted Calkenyl, optionally substituted Calkynyl, optionally substituted Calkylthio, optionally substituted Calkoxyalkyl, optionally substituted Ccarbocyclyl, optionally substituted Caryl, —OR, —NRR, —C(O)R, —SOR, and —NO; and'}{'sup': '11', 'sub': 1-6', '2-6', '2-6', '1-6, 'each Ris independently selected from the group consisting of halogen, —CN, optionally substituted Calkyl, optionally substituted Calkenyl, optionally substituted Calkynyl, and optionally substituted Calkoxy.'}3. The compound of or claim 1 , wherein Ris a Caryl optionally substituted with one or more R.4. The compound of claim 3 , wherein Ris a phenyl optionally substituted with one or more R.5. The compound of or claim 3 , wherein Ris a 5-10 membered heteroaryl optionally substituted with one or more R.6. The compound of claim 5 , wherein Ris a pyrazolyl or 1-methyl pyrazolyl optionally substituted with one or more R.7. The compound of any one of to claim 5 , wherein each Ris independently selected from halogen claim 5 , or optionally substituted Calkyl.8. The compound of claim 7 , wherein Ris fluoro.9. The compound of claim 7 , wherein Ris methyl.10. The compound of any one of to claim 7 , wherein Ris halogen.11. The compound of claim 10 , ...

KAPPA OPIOID AGONISTS AND USES THEREOF

Provided are compounds of Formula I; and pharmaceutically acceptable salts and solvates thereof. The compounds of Formula I described herein relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry. 2. The compound of claim 1 , wherein Ris an optionally substituted phenyl.3. The compound of any one of the proceeding claims claim 1 , wherein Ris selected from phenyl claim 1 , phenyl substituted with 1 to 3 halogens claim 1 , and phenyl substituted with ˜X-POLY.4. The compound of any one of the proceeding claims claim 1 , wherein Ris optionally substituted amino.5. The compound of any one of the proceeding claims claim 1 , wherein Ris amino substituted with an optionally substituted aryl.6. The compound of any one of the proceeding claims claim 1 , wherein Ris amino substituted with an optionally substituted phenyl.7. The compound of any one of the proceeding claims claim 1 , wherein Ris amino substituted with a phenyl group.8. The compound of any one of the proceeding claims claim 1 , wherein Ris hydrogen.9. The compound of any one of the proceeding claims claim 1 , wherein Ris ˜X-POLY.10. The compound of any one of the proceeding claims claim 1 , wherein Ris an optionally substituted aryl.11. The compound of any one of the proceeding claims claim 1 , wherein Ris an optionally substituted phenyl.12. The compound of any one of the proceeding claims claim 1 , wherein Ris phenyl.13. The compound of any one of the proceeding claims claim 1 , wherein Ris hydrogen.14. The compound of any one of the proceeding claims claim 1 , wherein Ris an optionally substituted lower alkyl.15. The compound of any one of the proceeding claims claim 1 , wherein Ris methyl.16. The compound of any one of the proceeding claims claim 1 , wherein Ris selected from an optionally substituted phenyl.17. The compound of any one of the proceeding claims claim 1 , wherein Ris selected from phenyl and ...

Microbiocidal phenylamidine derivatives

Compounds of the formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and X are as defined in claim 1. Furthermore, the present invention relates to agrochemical compositions which comprise compounds of formula (I), to preparation of these compositions, and to the use of the compounds or compositions in agriculture or horticulture for combating, preventing or controlling infestation of plants, harvested food crops, seeds or non-living materials by phytopathogenic microorganisms, in particular fungi.

BIODEGRADABLE LIPIDS FOR THE DELIVERY OF ACTIVE AGENTS

The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid. 134-. (Canceled)42. The process of claim 39 , wherein the reaction is performed in dichloromethane.43. The process of claim 40 , wherein the reaction is performed in dichloromethane.44. The process of claim 41 , wherein the reaction is performed in dichloromethane. This application is a continuation of U.S. patent application Ser. No. 13/708,383, filed Dec. 7, 2012, which claims the benefit of U.S. Provisional Application No. 61/568,133, filed Dec. 7, 2011, and U.S. Provisional Application No. 61/623,274, filed Apr. 12, 2012, each of which is hereby incorporated by reference.The present invention relates to biodegradable lipids and to their use for the delivery of active agents such as nucleic acids.Therapeutic nucleic acids include, e.g., small interfering RNA (siRNA), micro RNA (miRNA), antisense oligonucleotides, ribozymes, plasmids, immune stimulating nucleic acids, antisense, antagomir, antimir, microRNA mimic, supermir, U1 adaptor, and aptamer. In the case of siRNA or miRNA, these nucleic acids can down-regulate intracellular levels of specific proteins through a process termed RNA interference (RNAi). The therapeutic applications of RNAi are extremely broad, since siRNA and miRNA constructs can be synthesized with any nucleotide sequence directed against a target protein. To date, siRNA constructs have shown the ability to specifically down-regulate target proteins in both in vitro and in vivo models. In addition, ...

Omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors

This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.

Piperazine derivative

A piperazine derivative represented by the formula (1):    wherein n is an integer of 1 to 8; R 1 represents hydrogen or C 1-10 alkyl; A represents CH or nitrogen; Ar 1 represents phenyl or substituted phenyl; and Y represents a group represented by the formula Y 1 -Y 2 -Ar 2 or Y 3 -Y 4 (Ar 5 )-Ar 6 or a pharmaceutically acceptable salt of the derivative. The novel piperazine derivative has MC4 receptor antagonistic activity.

Remedial agent for anxiety neurosis or depression and piperazine derivative

There are provided a therapeutic preparation for anxiety neurosis or depression which comprises a MC 4 receptor antagonist as an effective ingredient; and a piperazine derivative represented by Formula [1]: [wherein Ar 1 is a phenyl group, a substituted phenyl group, a naphthyl group or a substituted naphthyl group; Ar 2 is a naphthyl group, a substituted naphthyl group, a quinolyl group, a group represented by the formula: (wherein R 4 is a hydrogen atom or a halogen atom; and X-Y is CH-NH, CH-O, CH-S or N-O) or a group represented by the formula: (wherein R 5 is a hydrogen atom, a hydroxyl group or a C 1-10 alkoxy group); R 1 is a hydrogen atom, a C 1-10 alkyl group, a C 3-8 cycloalkyl group, a C 3-10 alkenyl group, a phenyl group, a 1-cyanoethyl group, a pyrimidin-2-yl group or an amidyl group; R 2 and R 3 are the same or different, and are each a hydrogen atom or a C 1-10 alkyl group; A-B is N-CH 2 , CH-CH 2, C(OH)-CH 2 or C=CH; T 1 is a single bond, -N(R 6 )- (wherein R 6 is a hydrogen atom or a C 1-10 alkyl group), -O-, -CH=CH- or -C(=O)-; n is an integer of from 1 to 10 and when T 1 is a single bond, -CH=CH- or -C(=O)-, n is an integer of from 2 to 10 when T 1 is -N(R 6 )- or -O-], or a pharmaceutically acceptable salt thereof.

Phenyl- and phenylalkyl-substituted ethanolamines and ethylenediamines

The invention relates to compounds of the general formula (1), wherein A, R?1, R2, R3, R4, R5 and R6¿ are defined as in the description and the claims. The invention further relates to a method for producing said compounds and to their use as medicaments. The compounds of formula (1) are used as blockers of the voltage-dependent sodium channel and can be used for diseases that are associated with a functional disorder caused by hyperexcitability.

2,3-dihydro-1h-indene-2-ylurea derivative and pharmaceutical application of same

In order to provide a low molecular weight compound that has p38MAPK inhibitory activity and the accompanying TNF α production suppression activity and that has a favorable pharmacokinetic profile as a pharmaceutical and decreased hepatotoxicity, and to provide a pharmaceutical application of same, disclosed is a 2,3-dihydro-1H-indene-2-ylurea derivative represented below, a pharmacologically acceptable salt thereof, and a therapeutic agent or preventative agent that contains same as an active ingredient and that is for allergic dermatitis, inflammatory bowel disease, and pain.

BIODEGRADABLE LIPIDS FOR THE DELIVERY OF ACTIVE AGENTS

The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid. 1. A cationic lipid comprising a primary group and two biodegradable hydrophobic tails , wherein (a) the primary group comprises a protonatable group having a pKof from about 4 to about 13 , (b) the cationic lipid has an in vivo half life (t) of less than about 3 hours , and (c) at least one of the hydrophobic tails has the formula -(hydrophobic chain)-(biodegradable group)-(hydrophobic chain) where the terminal hydrophobic chain in the hydrophobic tail is a branched alkyl group. where the branching occurs at the α-position relative to the biodegradable group.2. The cationic lipid of claim 1 , wherein the primary group includes (i) a head group claim 1 , and (ii) a central moiety to which both the biodegradable hydrophobic tails are directly bonded.3. The cationic lipid of claim 2 , wherein the central moiety is selected from the group consisting of a central carbon atom claim 2 , a central nitrogen atom claim 2 , a central carbocyclic group claim 2 , a central aryl group claim 2 , a central heterocyclic and a central heteroaryl group.4. The cationic lipid of claim 1 , wherein at least one biodegradable hydrophobic tail has the formula —R-M-R claim 1 , where Ris a C-Calkylene or C-Calkenylene claim 1 , Mis a biodegradable group claim 1 , and Ris a branched alkyl or branched alkenyl.5. The cationic lipid of claim 4 , wherein Ris a branched C-Calkyl or C-Calkenyl.6. The cationic lipid of claim 4 , wherein the chain length ...

N-Arylamidine-substituted trifluoroethylsulfide derivatives as acaricides and insecticides

N-arylamidine substituted trifluoroethyl sulfide derivatives (I) are new. N-arylamidine substituted trifluoroethyl sulfide derivatives of formula (I) are new. n : 0-2; either X1-X4 : cycloalkylalkyl, cycloalkyloxy, cycloalkyl-alkoxy, cycloalkylthio, cycloalkyl-alkylthio, cycloalkylsulfinyl, cycloalkyl-alkylsulfinyl, cycloalkylsulfonyl or cycloalkyl-alkylsulfonyl (all optionally saturated), phenylalkyl, phenoxy, phenyl-alkyloxy, phenoxy-alkyl, phenylthio, phenyl-thioalkyl, phenylsulfinyl, phenylsulfonyl, heteroarylalkyl, heteroaryloxy, heteroaryl-thio, heteroaryl-alkyloxy, heteroaryl-sulfinyl or heteroaryl-sulfonyl (all optionally substituted), H, halo, OH, NH 2, OCN, SCN, SF 5, trialkylsilyl, (halo)alkyl, cyanoalkyl, hydroxyalkyl, alkoxycarbonylalkyl, alkoxyalkyl, (halo)alkenyl, cyano-alkenyl, (halo)alkynyl, cyano-alkynyl, (halo)alkoxy, cyanoalkoxy, hydroxycarbonyl-alkoxy, alkoxycarbonyl-alkoxy, alkoxy-alkoxy, alkyl-hydroxyimino, alkoxyimino, (halo)alkyl-alkoxyimino, (halo)alkylthio, alkoxy-alkylthio, alkylthioalkyl, (halo)alkylsulfinyl, alkoxy-alkylsulfinyl, alkylsulfinyl-alkyl, (halo)alkylsulfonyl, alkoxy-alkylsulfonyl, alkylsulfonyl-alkyl, alkyl-sulfonyloxy, (halo)alkylcarbonyl, carboxy, alkylcarbonyloxy, (halo)alkoxycarbonyl, alkoxycarbonylalkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, alkenylaminocarbonyl, dialkenyl-aminocarbonyl, cycloalkylaminocarbonyl, alkylsulfonylamino, aminosulfonyl, alkyl-aminosulfonyl, dialkylamino-sulfonyl, alkylsulfoximino, aminothiocarbonyl, alkyl-aminothiocarbonyl, dialkylamino-thiocarbonyl, NR4R5 or saturated, partially saturated or aromatic 3-6-membered ring (optionally containing 1-3 O, S or N and optionally mono- or polysubstituted by G1); or X2+X3+C, X3+X4+C : 5-6-membered ring (optionally substituted and optionally interrupted by O, S, N or CO); either R4, R5 : H, CN, (halo)alkyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, (halo)alkenyl, cyano-alkenyl, (halo)alkynyl, cyano-alkynyl, acyl or ...

Synthesis of deuterated morpholine derivatives

The present invention is directed to a process for preparing a 2,26,6- d 4 -morpholine derivative represented by Structural Formula (I), or a salt thereof.

Improving the storage stability of photoinitiators

<omega>-karboksyarylsubstituerte difenylureaforbindelser som raf-kinaseinhibitorer

Lipoic acid derivatives for pharmaceutical use

Therapeutically-effective amounts of novel analogs or derivatives of alkyl fatty acids, such as but not limited to lipoic acid, and pharmaceutical formulations comprising such analogs or derivatives and pharmaceutically-acceptable carriers therefor, are useful for the treatment, prevention, imaging, and/or diagnosis of medical disorders.

Замещенные циклопентилазины в качестве casr-активных соединений

1. Соединение общей формулы I:[I]гдеAr представляет собой Cарил, Cгетероарил или Cгетероциклоалкиларил, где указанный Cарил, Cгетероарил или Cгетероциклоалкиларил необязательно замещен одним или более одинаковыми или различными заместителями, независимо выбранными из галогена, гидрокси, Cалкила, трифторметила или Cалкокси;X представляет собой -CH- или атом азота;Rпредставляет собой Cалкил, Cалкенил, Cалкинил, гидроксиСалкил, галогенСалкил или Cциклоалкил;Rпредставляет собой водород или выбран из группы, состоящей из аминоСалкила, Cалкила, Cалкенила, гидроксиСалкила, CалкиламиноСалкила, гидроксиСалкиламиноСалкила, CалкилсульфониламиноСалкила, Cалкилкарбонила, Cалкиламинокарбонила, CалкилсульфонилСгетероциклоалкила, аминосульфонилСалкила, Cгегетероциклоалкила, Cгетероциклоалкилкарбонила, где указанный Cалкил, Cалкенил, гидроксиСалкил, CалкиламиноСалкил, гидроксиСалкиламиноСалкил, Cалкилкарбонил, Cалкиламинокарбонил, Cгетероциклоалкил или Cгетероциклоалкилкарбонил необязательно дополнительно замещен одним или более заместителями, выбранными из галогена, гидрокси, трифторметила, -S(O)NH, -S(O)CHили -NH;Rпредставляет собой водород или выбран из группы, состоящей из Cалкила, Cалкенила, Cалкокси, аминоСалкила, Cциклоалкила или Cгетероциклоалкила;или Rи Rвместе с соседним атомом, к которому они присоединены, образуют 4-, 5-, 6- или 7-членный Cгетероциклоалкил, содержащий один или более гетероатомов, выбранных из группы, состоящей из O, S и N, причем указанный Cгетероциклоалкил необязательно замещен оксо, гидрокси, атомом галогена, трифторметилом, Cалкилом, -NH, -S(O)NH, -S(O)CH, Cалкилкарбонилом, гидроксиСалкилом, Cалкокси, аминоСалкилом, Cалкил� РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 213/61 (13) 2013 128 950 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2013128950/04, 21.11.2011 (71) Заявитель(и): ЛЕО ФАРМА А/С (DK) Приоритет(ы): (30) Конвенционный приоритет: 26.11.2010 US 61/417,369 (85) Дата начала ...

Difenilureias substituidas com (.)-carboxiarilo como inibidores de raf-quinase

Антагонисты vii рецептора ccr-3

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (51) ÌÏÊ 7 (11) 2004 120 065 (13) A C 07 D 211/18 ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2004120065/04, 20.11.2002 (71) Çà âèòåëü(è): Ô.ÕÎÔÔÌÀÍÍ-Ëß ÐÎØ Àà (CH) (30) Ïðèîðèòåò: 30.11.2001 US 60/334,819 (43) Äàòà ïóáëèêàöèè çà âêè: 27.05.2005 Áþë. ¹ 15 (74) Ïàòåíòíûé ïîâåðåííûé: Âåñåëèöêà Èðèíà Àëåêñàíäðîâíà (86) Çà âêà PCT: EP 02/12997 (20.11.2002) Àäðåñ äë ïåðåïèñêè: 101000, Ìîñêâà, Ì.Çëàòîóñòèíñêèé ïåð., 10, êâ.15, "ÅÂÐÎÌÀÐÊÏÀÒ", È.À.Âåñåëè êîé (54) ÀÍÒÀÃÎÍÈÑÒÛ VII ÐÅÖÅÏÒÎÐÀ CCR-3 Ôîðìóëà èçîáðåòåíè R U A 2 0 0 4 1 2 0 0 6 5 A 1. Ñîåäèíåíèå ôîðìóëû (I) ãäå R 1 îçíà÷àåò Ñ1-Ñ2àëêèëåí; R 2 îçíà÷àåò íåîá çàòåëüíî çàìåùåííûé ôåíèë; R 3 îçíà÷àåò âîäîðîä, C1-Ñ6àëêèë, àöèë, àðèë èëè àðèë(C1-Ñ6)àëêèë; öèêë À îçíà÷àåò Ñ3-Ñ7öèêëîàëêèë, ãåòåðîöèêëèë èëè íåîá çàòåëüíî çàìåùåííûé ôåíèë; D îçíà÷àåò N èëè C-R b; L îçíà÷àåò -Ñ(O)-, -C(=S)-, -SO2-, -C(=O)N(R a)-, -C(=S)N(R a)-, -SO2N(R a)-, -Ñ(=O)O-, -C(= S)O-, -S(=O)2O-; R 4 îçíà÷àåò C1-Ñ6àëêèë, Ñ3-Ñ7öèêëîàëêèë, Ñ2-Ñ6àëêåíèë, C2-Ñ6àëêèíèë, ãåòåðîàëêèë èëè àöèë(C1-Ñ6)àëêèë; Ñòðàíèöà: 1 RU 2 0 0 4 1 2 0 0 6 5 (87) Ïóáëèêàöè PCT: WO 03/045917 (05.06.2003) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 30.06.2004 (72) Àâòîð(û): ÄÞ-ÁÓÀ Äåéñè Äæî (US), ÂÀÍ Áýéõàíü (US) A 2 0 0 4 1 2 0 0 6 5 A R U 2 0 0 4 1 2 0 0 6 5 Ñòðàíèöà: 2 R U R à îçíà÷àåò âîäîðîä, C1-Ñ6àëêèë, àöèë, àðèë, àðèë(C1-Ñ6)àëêèë, C1-Ñ6àëêîêñèêàðáîíèë èëè áåíçèëîêñèêàðáîíèë; R b îçíà÷àåò âîäîðîä èëè C1-Ñ6àëêèë, è åãî ïðîëåêàðñòâà, èíäèâèäóàëüíûå èçîìåðû, ðàöåìè÷åñêèå è íåðàöåìè÷åñêèå ñìåñè èçîìåðîâ è ôàðìàöåòè÷åñêè ïðèåìëåìûå ñîëè, ãäå òåðìèí "íåîá çàòåëüíî çàìåùåííûé ôåíèë" îçíà÷àåò ôåíèëüíóþ ãðóïïó, êîòîðà íåîá çàòåëüíî çàìåùåíà îäíèì èëè áîëåå çàìåñòèòåë ìè, âûáðàííûìè èç ãðóïïû, âêëþ÷àþùåé C1-Ñ6àëêèë, ãàëîãåí(C1-Ñ6)àëêèë, ãèäðîêñè(Ñ1-Ñ6)àëêèë, ãåòåðîàëêèë, àöèë, àöèëàìèíî, àìèíî, C1-Ñ6àëêèëàìèíî, äè(Ñ 1-Ñ6)àëêèëàìèíî, C1-Ñ6àëêèëòèî, C1-Ñ6 ...

Blc-2 selective agents causing apoptosis for treating cancer and immune diseases

FIELD: medicine, pharmaceutics. SUBSTANCE: invention refers to compounds of formula I and formula IV wherein the radical values are such as specified in cl. 1 and 4 of the patent claim, as well as to their therapeutically acceptable salts. Besides, the invention refers to a composition for treating cancer on the basis of the compounds of formula I, to using the compounds of formula I for preparing the therapeutic agent for treating cancer, as well as to using it for treating cancer. EFFECT: there are prepared and described the new compounds which inhibit anti-apoptotic Bcl-2 and Bcl-x protein activity. 17 cl, 481 ex

Bridged spiro[2,4]heptane derivatives as alx and/or fprl2 receptor agonists

FIELD: medicine, pharmaceutics. SUBSTANCE: invention refers to bridged spiro[2.4]heptane derivatives of formula (I), wherein W means -CH 2 CH 2 - or -CH=CH-; Z means -C(O)NR 3 -* or -CH 2 NR 4 C(O)-*, Y means a bond or (C 1 -C 4 )alkane diyl group, R 1 -R 4 are those as specified in the description, to preparing and using them as ALX and/or FPRL2 receptor agonists applicable for treating inflammatory and obstructive respiratory diseases. EFFECT: preparing the compositions for treating the inflammatory and obstructive respiratory diseases. 14 cl, 1 tbl, 422 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07C 233/58 C07C 233/60 C07C 233/63 C07D 211/26 C07D 207/09 C07D 213/40 ФЕДЕРАЛЬНАЯ СЛУЖБА C07D 231/12 ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07D 233/64 C07D 235/14 C07D 239/30 (12) ОПИСАНИЕ (21)(22) Заявка: (13) 2 540 274 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) C07D C07D C07D C07D C07D A61K A61K A61K A61K A61P 249/08 277/28 277/62 307/52 319/12 31/44 31/40 31/426 31/427 11/00 C2 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2011151277/04, 17.05.2010 (24) Дата начала отсчета срока действия патента: 17.05.2010 18.05.2009 IB PCT/IB2009/052056 (45) Опубликовано: 10.02.2015 Бюл. № 4 (73) Патентообладатель(и): АКТЕЛИОН ФАРМАСЬЮТИКЛЗ ЛТД (CH) 2 5 4 0 2 7 4 R U 2005047899 A2, 26.05.2005 . BANNENBERG G L: "Anti-inflammatory actions of lipoxins" EXPERT OPINION ON THERAPEUTIC PATENTS 2007, vol. 17, no. 6, pages 591-605. BURLI R W ET AL: "Potent hFPRL1 (ALXR) agonists as potential anti-inflammatory agents" BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, 2006, vol. 16, no. 14, pages 3713-3718 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 19.12.2011 (86) Заявка PCT: IB 2010/052170 (17.05.2010) (87) Публикация заявки PCT: WO 2010/134014 (25.11.2010) Адрес для переписки: 105082, Москва, Спартаковский пер., д. 2, стр. 1, секция 1, ...

APOPTOSIS INDUCING AGENTS SELECTIVE FOR Bcl-2 FOR CANCER AND IMMUNE DISEASES TREATMENT

FIELD: pharmacy. SUBSTANCE: invention relates to specific heterocyclic compounds containing the sulphonyl amino carbonyl group. The invention also relates to a pharmaceutical composition based on this compound. EFFECT: new heterocyclic compounds with inhibitory activity in terms of anti-apoptotic Bcl-2 proteins are obtained. 2 cl, 3 tbl, 481 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 621 052 C2 (51) МПК C07D 295/14 (2006.01) C07D 405/12 (2006.01) C07D 405/14 (2006.01) A61K 31/453 (2006.01) A61K 31/46 (2006.01) A61K 31/496 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА A61K 31/5377 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ A61P 35/00 (2006.01) (12) ФОРМУЛА (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ 2013133800, 19.07.2013 (24) Дата начала отсчета срока действия патента: 04.12.2009 Дата регистрации: Приоритет(ы): (30) Конвенционный приоритет: (43) Дата публикации заявки: 27.01.2015 Бюл. № 3 2 6 2 1 0 5 2 R U Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, строение 3, ООО "Юридическая фирма Городисский и Партнеры" (73) Патентообладатель(и): ЭББВИ ИНК. (US) (56) Список документов, цитированных в отчете о поиске: US 2007/072860 A1, 29.03.2007. US 2005/159427 A1, 21.07.2005. EA 9201 B1, 28.12.2007. (54) СЕЛЕКТИВНЫЕ К BCL-2 АГЕНТЫ, ВЫЗЫВАЮЩИЕ АПОПТОЗ, ДЛЯ ЛЕЧЕНИЯ РАКА И ИММУННЫХ ЗАБОЛЕВАНИЙ (57) Формула изобретения 1. Соединение, выбранное из: 2-(бензилокси)-4-(4-((4'-хлор-1,1'-дифенил-2-ил)метил)пиперазин-1-ил)-N-((3-нитро4-((тетрагидро-2Н-пиран-4-илметил)амино)фенил)сульфонил)бензамида; 4-(4-((4'-хлор-1,1'-дифенил-2-ил)метил)пиперазин-1-ил)-N-((3-нитро-4-((тетрагидро2Н-пиран-4-илметил)амино)фенил)сульфонил)-2-(2-фенилэтокси)бензамида; 2-бензил-4-(4-((4'-хлор-1,1'-дифенил-2-ил)метил)пиперазин-1-ил)-N-((3-нитро-4-( (тетрагидро-2Н-пиран-4-илметил)амино)фенил)сульфонил)бензамида; 2-бензил-4-(4-((4'-хлор-1,1'-дифенил-2-ил)метил)пиперазин-1-ил)-N-((4-((тетрагидро2Н-пиран-4-илметил)амино)фенил)сульфонил)бензамида; Стр.: 1 C 2 C 2 (45) Опубликовано: 31.05.2017 Бюл. № ...

适用作h3配体的3－或4－单取代酚及苯硫酚衍生物

本发明涉及式(1)的3－或4－单取代酚及苯硫酚衍生物，并涉及制备该衍生物的方法、制备该衍生物中使用的中间体、含有该衍生物的组合物和该衍生物的用途。所述3－或4－单取代酚及苯硫酚衍生物为H 3 配体且适用于多种疾病、障碍及病况，尤其适用于炎性、过敏性及呼吸疾病、障碍及病况。

3- or 4-monosubstituted phenol and thiophenol derivatives useful as h3 ligands

본 발명은 화학식 1의 3- 또는 4-단일치환된 페놀 및 싸이오페놀 유도체 및 이러한 유도체의 제조 방법, 이러한 제조에 유용한 중간체, 이것을 함유한 조성물 및 이것의 용도에 관한 것이다. The present invention relates to 3- or 4-monosubstituted phenol and thiophenol derivatives of formula (1) and to methods of preparing such derivatives, intermediates useful for such preparations, compositions containing them and the use thereof. 화학식 1 Formula 1 3- 또는 4-단일치환된 페놀 및 싸이오페놀 유도체는 H 3 리간드이며, 많은 질병, 질환 및 증상, 특히 염증성, 알러지성 및 호흡기 질병, 질환 및 증상에 유용하다. 3- or 4-monosubstituted phenols and thiophenol derivatives are H 3 ligands and are useful for many diseases, conditions and symptoms, in particular inflammatory, allergic and respiratory diseases, diseases and conditions.

Dpp-iv inhibitors

FIELD: chemistry, pharmaceutics. SUBSTANCE: claimed invention relates to novel compounds of general formula (I) Z-C(R 1 R 2 )-C(R 3 NH 2 )-C(R 4 R 5 )-X-N(R 6 R 7 ) (I), or its pharmaceutically acceptable salt which is different because Z represents phenyl; where Z can be substituted with one or more R 8 , where R 8 represents halogen; R 1 , R 4 represent H; R 2 , R 5 represent H; R 3 represents H; X is selected from group consisting of S(O) 2 and C(O); R 6 , R 7 are independently selected from group consisting of H, (C(R 29 R 30 )) m -X 1 -Z 1 and (C(R 31 R 32 )) n -X 2 -X 3 -Z 2 and C 1-4 alkyl, which carries substitution with one or more R 29a , where R 29a is independently selected from group consisting of R 29b and Z 1 , on condition that R 6 and R 7 are selected in such way that R 6 and R 7 were not simultaneously independently selected from group consisting of H, CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3 and CH(CH 3 ) 2 ; R 29 R 29b , R 30 , R 31 , R 32 are independently selected from group consisting of H, C 1-6 alkyl and N(R 32a )-C 1-6 alkyl; R 32a represents C 1-6 alkyl; m is 0, 1 or 2; n is 2; X 1 is independently selected from group consisting of covalent bond, -C 1-6 alkyl and -C 1-6 alkyl-N(R 33 )-; X 2 represents -N(R 35 )-; X 3 represents -C(O)-; R 33 represents C 1-6 alkyl; R 35 represents H; Z 1 , Z 2 are independently selected from group consisting of Z 3 and -C(R 37a )Z 3a Z 3b ; R 37a represents H; Z 3 , Z 3a , Z 3b are independently selected from group consisting of T 1 , T 2 , C 1-6 alkyl, C 1-6 alkyl-T 1 and C 1-6 alkyl-T 2 ; T 1 represents phenyl; where T 1 is optionally substituted with one or more R 38 ; R 38 being independently selected from group consisting of halogen, CN, R 39 , C(O)NH 2 , S(O) 2 NH 2 , OT 3 , C(O)N(R 40 )T 3 and T 3 , T 2 is selected from group consisting of C 3-7 cycloalkyl, indanyl, tetralinyl, heterocycle and heterobicycle, T 2 optionally carries substitution with one or more R 41 , where R 41 is independently selected ...

作为用于治疗癌症和免疫疾病的bcl-2-选择性诱发细胞凋亡药剂的磺酰胺衍生物

作为用于治疗癌症和免疫疾病的BCL‑2‑选择性诱发细胞凋亡药剂的磺酰胺衍生物。公开了抑制抗细胞凋亡Bcl‑2或Bcl‑xL蛋白活性的化合物，含该化合物的组合物和治疗在其期间表达抗细胞凋亡Bcl‑2蛋白的疾病的方法。

Anti-fibrotic pyridinones

피리디논 화합물, 이들 화합물을 제조하는 방법, 그리고 섬유증 장애를 치료하기 위한 방법이 개시되어 있다. Pyridinone compounds, methods of making these compounds, and methods for treating fibrotic disorders are disclosed.

3- or 4-monosubstituted phenol and thiophenol derivatives useful as H3 ligands

Derivative of n-acylanthranilic acid or its salt

FIELD: medicine, pharmaceutics. SUBSTANCE: invention relates to a novel derivative of N-acylanthranilic acid, represented by the following general formula 1, or to its pharmaceutically acceptable salt, in which R 1 , R 2 , R 3 , X 1 , X 2 , X 3 , X 4 and A are determined in the invention formula. EFFECT: invention relates to an inhibitor of collagen production, a medication for treating diseases, associated with the excessive production of collagen, containing N-acylanthranilic acid derivative РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07C 235/58 C07D 207/337 C07D 211/14 C07D 211/34 C07D 211/44 C07D 211/46 ФЕДЕРАЛЬНАЯ СЛУЖБА C07D 211/58 ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07D 211/96 C07D 213/56 C07D 213/73 (12) ОПИСАНИЕ (24) Дата начала отсчета срока действия патента: 29.01.2010 213/85 231/12 233/61 239/26 263/32 265/30 267/08 271/10 295/08 295/12 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) 2009-020274; 2009-020424; 2009-020462; 2009-239188 (72) Автор(ы): ЙОКОТАНИ Дзунити (JP), ТАКАТОРИ Арихиро (JP), ТАДА Юкие (JP), ЯНАИ Минори (JP), КАТО Хироси (JP), ТАНИГУТИ Йоити (JP), ТАНАБЕ Тихару (JP) (73) Патентообладатель(и): ТОЯМА КЕМИКАЛ КО., ЛТД. (JP) (43) Дата публикации заявки: 10.03.2013 Бюл. № 7 (45) Опубликовано: 10.10.2014 Бюл. № 28 2004-067690 A, 04.03.2004. WO 2006/098308 A1, 21.09.2006. JP 2009-501157 A, 15.01.2009. JP 2001-089412 A, 03.04.2001. WO 03/004458 A1, 16.01.2003. RU 2006124794 A, 20.01.2008 2 5 2 9 8 6 0 (86) Заявка PCT: R U (85) Дата начала рассмотрения заявки PCT на национальной фазе: 30.08.2011 (54) ПРОИЗВОДНОЕ N-АЦИЛАНТРАНИЛОВОЙ КИСЛОТЫ ИЛИ ЕГО СОЛЬ (57) Реферат: Изобретение относится к новому относится к ингибитору продукции коллагена, производному N-ацилантраниловой кислоты, средству для лечения заболеваний, представленному следующей общей формулой 1, ассоциированных с избыточной продукцией или к его фармацевтически приемлемой соли, в коллагена, содержащим производное N1 2 3 1 2 3 4 ...

The way to combat unwanted vegetation

Новые пиперидиновые производные для лечения депрессии

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (11) 2007 105 968 (13) A (51) ÌÏÊ C07D 295/067 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2007105968/04, 27.07.2005 (71) Çà âèòåëü(è): ÀñòðàÇåíåêà ÀÁ (SE) (30) Êîíâåíöèîííûé ïðèîðèòåò: 02.08.2004 SE 0401969-1 (43) Äàòà ïóáëèêàöèè çà âêè: 10.09.2008 Áþë. ¹ 25 (87) Ïóáëèêàöè PCT: WO 2006/014134 (09.02.2006) Àäðåñ äë ïåðåïèñêè: 191036, Ñàíêò-Ïåòåðáóðã, à/ 24, "ÍÅÂÈÍÏÀÒ", ïàò.ïîâ. À.Â.Ïîëèêàðïîâó R U (57) Ôîðìóëà èçîáðåòåíè 1. Ñîåäèíåíèå ôîðìóëû I, åãî ôàðìàöåâòè÷åñêè ïðèåìëåìûå ñîëü, åãî äèàñòåðåîìåðû, ýíàíòèîìåðû èëè èõ ñìåñè: A 2 0 0 7 1 0 5 9 6 8 A (54) ÍÎÂÛÅ ÏÈÏÅÐÈÄÈÍÎÂÛÅ ÏÐÎÈÇÂÎÄÍÛÅ ÄËß ËÅ×ÅÍÈß ÄÅÏÐÅÑÑÈÈ ãäå Ar 1 âûáðàí èç Ñ6-10àðèëà è Ñ2-9ãåòåðîàðèëà, ãäå óêàçàííûå Ñ6-10àðèë è Ñ2-9ãåòåðîàðèë âîçìîæíî çàìåùåíû îäíîé èëè áîëåå ãðóïïàìè, âûáðàííûìè èç -R, -NO2, -OR, -Cl, -Br, -I, -F, -CF3, -OCF3, -C(=O)R, -C(= O)OH, -NH2, -SH, -NHR, -NR2, -SR, -SO3Í, -SO2R, -SO2NR, -S(=O)R, -CN, -ÎÍ, -C(= O)OR, -C(=O)NR2, -NRC(=O)R è -NRC(=O)-OR, ãäå R íåçàâèñèìî ïðåäñòàâë åò ñîáîé âîäîðîä, Ñ3-6öèêëîàëêèë, Ñ3-6ãåòåðîöèêëèë, ôåíèë, áåíçèë, C1-6àëêèë èëè Ñ2-6àëêåíèë è ãäå óêàçàííûé R äîïîëíèòåëüíî âîçìîæíî çàìåùåí îäíîé èëè áîëåå ãðóïïàìè, âûáðàííûìè èç ìåòèëà, ãèäðîêñè è ãàëîãåíà, ëèáî Ar 1 ïðåäñòàâë åò ñîáîé , Ñòðàíèöà: 1 RU 2 0 0 7 1 0 5 9 6 8 (86) Çà âêà PCT: SE 2005/001187 (27.07.2005) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 02.03.2007 (72) Àâòîð(û): ÔÎËÌÅÐ Äæåéìñ (US), ÕÀÍÒ Ñàéìîí Ôðåéçåð (GB), ÕÝÌËÈ Ïèòåð (DE), ÂÅÑÎËÎÂÑÊÈ Ñòèâåí (US) 2 0 0 7 1 0 5 9 6 8 R U Ñòðàíèöà: 2 ; A ; 2 0 0 7 1 0 5 9 6 8 ãäå Ar âûáðàí èç ôåíèëà, ïèðèäèëà, íàôòèëà, áåíçî[1,3]äèîêñîëèëà, õèíîëèëà, èíäîëèëà, áåíçîòðèàçîëèëà, áåíçèìèäàçîëèëà, 2,3-äèãèäðî-áåíçîôóðàíèëà, áåíçî[1,2,3] òèàäèàçîëèëà, áåíçîòèàçîëèëà è 4Í-áåíçî[1,4]îêñàçèí-3-îí-èëà; R 1, R 2 è R 3 íåçàâèñèìî âûáðàíû èç -R, -NO2, -OR, -Cl, -Br, -I, -F, -CF3, -C(=O)R, -C(= O)OH, -NH2, -SH, -NHR, -NR2, -SR, -SO3Í, ...

IRE-1A inhibitors

Un compuesto que inhibe directamente la actividad in vitro de la IRE-1α y que está representado por la fórmula estructural (B):**Fórmula** o una sal farmacéuticamente aceptable del mismo, en la que: R1 es hidrógeno, fenilo o un heterociclo de cinco o seis miembros opcionalmente benzocondensado, en la que el fenilo o el heterociclo de cinco o seis miembros opcionalmente benzocondensado está opcionalmente sustituido con**Fórmula** -CH2OH, -CHO, -OCH3, halógeno, -OH, -CH3,**Fórmula** R2 es fenilo o un heterociclo de cinco o seis miembros opcionalmente benzocondensado, en la que el fenilo o el heterociclo de cinco o seis miembros opcionalmente benzocondensado está opcionalmente sustituido con**Fórmula** -CH2OH, -CHO, -OCH3, halógeno, -OH, -CH3, R3 es hidrógeno, halógeno, -NO2, alquilo C1-C3 lineal o ramificado, alcoxi C1-C3 lineal o ramificado, hidroxil alquilo C1-C3 lineal o ramificado,**Fórmula** y R4 es hidrógeno,**Fórmula** A compound that directly inhibits the in vitro activity of IRE-1α and is represented by structural formula (B): ** Formula ** or a pharmaceutically acceptable salt thereof, in which: R1 is hydrogen, phenyl or a optionally benzo-condensed five or six-membered heterocycle, wherein the phenyl or optionally benzo-condensed five or six-membered heterocycle is optionally substituted with ** Formula ** -CH2OH, -CHO, -OCH3, halogen, -OH, -CH3, ** Formula ** R2 is phenyl or an optionally benzo-condensed five or six-membered heterocycle, in which the optionally benzo-condensed phenyl or five or six-membered heterocycle is optionally substituted with ** Formula ** -CH2OH, -CHO, - OCH3, halogen, -OH, -CH3, R3 is hydrogen, halogen, -NO2, linear or branched C1-C3 alkyl, linear or branched C1-C3 alkoxy, linear or branched C1-C3 alkyl hydroxy, ** Formula ** and R4 is hydrogen, ** Formula **

IRE-1α inhibitors

Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

IRE-1α inhibitors

Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

IRE-1α inhibitors

Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

IRE-1α inhibitors

Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

IRE-1α inhibitors

Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

Preparation of N-phenyl-2-pyrimidinamine derivatives

1. Соединение формулы II' ! ! в которой ! R1, R2, R4 и R5 независимо выбраны из группы, включающей водород, циано; низший алкил; гидрокси- или аминозамещенный низший алкил; трифторметил; свободную или этерифицированную гидроксигруппу; (низший)алкокси; (низший)алканоилокси; свободную, алкилированную или ацилированную аминогруппу; моно- или ди(низший)алкиламино; (низший)алканоиламино; бензоиламино; свободную или этерифицированную карбоксигруппу; (низший)алкоксикарбонил и галоген; ! R13 обозначает 4-метилпиперазин-1-ил-метил и его соль. ! 2. Соединение формулы II' по п.1, где R1, R2, R4 и R5 все представляют собой водород, a R13 обозначает 4-метилпиперазин-1-ил-метил и его соль. ! 3. Соединение по п.2, которое находится в форме дигидрохлоридной соли. ! 4. Способ получения соединения формулы V, включающий взаимодействие соединения формулы II' с соединением формулы III ! ! где R1, R2, R4 и R5 все представляют собой водород, один из радикалов R6, R7 и R8 обозначает галоген, NH2, NO2, NHC(O)CF3, NHC(O)СН3 или NHC(NH)NH2, а два другие радикала независимо выбраны из группы, включающей водород, низший алкил; низший фторалкил; бензил или фенил, a R13 обозначает 4-метилпиперазин-1-ил-метил или его соли в присутствии органического растворителя и основания. ! 5. Применение соединения формулы II' ! ! в которой R1, R2, R4 и R5 все представляют собой водород, a R13 обозначает 4-метилпиперазин-1-ил-метил или его соли для получения соединения формулы IV, ! ! которое представляет собой N-{5-[4-(4-метилпиперазинометил)бензоиламидо]-2-метилфенил}-4-(3-пиридил)-2-пиримидинамин или его фармацевтически приемлемую соль. (19) РОССИЙСКАЯ ФЕДЕРАЦИЯ RU (11) 2007 148 217 (13) A (51) МПК C07D 295/12 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21), (22) Заявка: 2007148217/04, 26.12.2007 (30) Конвенционный приоритет: 07.02.2002 GB 0202873.6 (71) Заявитель(и): НОВАРТИС АГ (CH) R U A 2 0 0 7 1 4 8 2 1 7 A (57) ...

Tetracycline compounds have been substituted for C7-fluorine

Phenyl amino pyrimidine compounds and uses thereof

The present disclosure relates to phenyl amino pyrimidine compounds comprising the following general formula: (See Formula I) which are inhibitors of JAK kinases. In particular the compounds are selective for JAK2 kinases as compared to JAK3.

Derivatives of urea (variants), pharmaceutical composition (variants) and method for treatment of diseases associated with cancer cells growth (variants)

FIELD: organic chemistry, medicine, oncology, pharmacy. SUBSTANCE: invention relates to novel compounds of the general formula: A-D-B (I) given in the invention description, or their pharmaceutically acceptable salts that possess property of raf kinase inhibitors and can be used in treatment of disease associated with growth of cancer cells mediated by effect of this kinase. In compounds of the general formula A-D-B (I) D value is represented by the formula -NH-C(O)-NH-; A means a substituted structure comprising up to 40 carbon atoms of the formula -L-(M-L 1 ) q wherein L represents pyridyl or phenyl substituted with halogen atom or (C 1 -C 4 )-alkyl, or 6-membered nitrogen-containing heterocyclic structure bound with D directly; L 1 comprises possibly substituted (C 5 -C 7 )-aryl or (C 5 -C 8 )-nitrogen-containing heterocyclic group; M is a bridge group comprising at least one atom chosen from -O-, -S-, -CO-NH-, -NH-CO-; q is a whole number = 1 or 2; B represents substituted or unsubstituted (C 6 -C 14 )-aryl group or 6-membered heteroaryl group comprising 1-4 heteroatoms chosen from nitrogen, oxygen and sulfur atoms, and wherein L 1 is substituted with at least one substitute chosen from group consisting of -SO 2 R x , -C(O)R x and -C(NR y )R z , and if L 1 means phenyl then -SO 2 R x can not represent -SO 3 H; R y means (C 1 -C 4 )-alkoxy group; R z means hydroxy group, (C 1 -C 4 )-alkyl or (C 1 -C 4 )-alkoxy group; R x means R z or NR a R b wherein R a and R b : (a) are represented by hydrogen atom, (C 1 -C)-alkyl group substituted possibly hydroxy group, (C 1 -C 4 )-alkoxy group or (C 5 -C 6 )-heterocyclic group comprising 1-2 heteroatoms chosen from nitrogen (N) and oxygen (O) atoms that can be substituted with (C 1 -C 4 )-alkyl or amino group substituted possibly with (C 1 -C 4 )-alkyl group, or phenyl, or -OSi(R f ) 3 wherein R f means (C 1 -C 4 )-alkyl group; phenyl substituted possibly with halogen atom, amino group that can be substituted with (C 1 -C 4 ...

2-acylaminopropanol-type glucosylceramide synthase inhibitors

Arylalkylamines and pharmaceutical composition based on thereof

FIELD: organic chemistry. SUBSTANCE: products: arylalkylamines of the formula (I) where Y - group Cy- where Cy - unsubstituted phenyl or phenyl substituted with hydroxyl, C 1 -C 4 -alkoxy-group, C 3 -C 6 -cycloalkyl, pyrimidyl; Ar' - unsubstituted or substituted phenyl; R - hydrogen, C 1 -C 3 -alkyl; T - group -CO- or -CONH; m = 2 or 3; Z - M or OM where M - C 1 -C 4 -alkyl. Reagent 1: compound of the formula (II) 9561020сС ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) (51) МПК 211/30, 211/44, 211/50, Аб1 К ВИ "” 2 070 196 ' 13) СЛ С 070 241/04, 239/42, 211/26, 31/445, 31/505 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 5001435/04, 04.09.1991 (30) Приоритет: 05.09.1990 ЕК 9011039 25.06.1991 ЕВ 9107824 (46) Дата публикации: 10.12.1996 (56) Ссылки: Вагпез Р... Агсп. т. Рпагтасоадуп, 1990, 303, р. 67 - 82. Патент ЕПВ М 0336230, кл. СОГК 7/06, 1989. (71) Заявитель: Санофи (ЕК) (72) Изобретатель: Ксавье Эмон-Альт [ЕК], Пьер ГуляуикЕК], Винченцо Проиетто[1Т], Дидье Ван Брук[ВЕ] (73) Патентообладатель: Санофи (ЕК) (54) АРИЛАЛКИЛАМИНЫ И ФАРМАЦЕВТИЧЕСКАЯ (57) Реферат: Использование: в медицине в качестве антагонистов рецепторов нейрокинина А. Сущность изобретения: Продукты арилалкиламины Ф-лы, где У - группа су-м( в которой С, - Фенил, незамещенный ИЛИ замещенный гидроксилом, алкоксигруппой С\-С4, циклоалкил Сз3-Св, пиримидил, Аг- незамещенный или замещенный фенил, ® - водород, С 1-Сз-алкил, Т - группа -СО- или -СОМН, т=2 КОМПОЗИЦИЯ НА ИХ ОСНОВЕ или 3, 2 - М или ОМ, где М - С.-Сд-алкил. Реагент 1: Соединение ф-лы 2. Реагент 2: НСО-Г или О=С=М-Г. 3 с. и 8 з.п.ф-лы, 13 табл. Соединение 1 | у, мАССН > и бносн,-н-т-2 Аг“ Е Соединение 2 Е-< СН_» -СН-СН -мнЕ 2 м | 2. г Аг 2070196 С1 КО 95610140с ПЧ Го КУЗЗАМ АСЕМСУ ГОК РАТЕМТ$ АМО ТКАОЕМАКК$ (19) (51) 1пЕ. С1.6 211/26, 211/30, 211/44, 211/50, А ВИ "” 2 070 196 ' 13) Сл С 070 241/04, 239/42, 61 К 31/445, 31/505 12) АВЗТКАСТ ОЕ 1МУЕМТОМ (21), (22) АррИсаНоп: 5001435/04, 04.09.1991 ( ...

Diamine compound, process for producing the same, and medicament containing the compound for treating hypertension and inflammation

1-phenyl-3-(1-piperazinyl)-1H-indazoles

Novel 1-phenyl-3-(1-piperazinyl)-1H-indazoles, intermediates and processes for the preparation thereof, and methods for alleviating pain, treating convulsions, and treating depression utilizing compounds or compositions thereof are disclosed.

Derivatives of urea (variants), pharmaceutical composition (variants) and method for treatment of diseases associated with cancer cells growth (variants)

FIELD: organic chemistry, medicine, oncology, pharmacy. SUBSTANCE: invention relates to novel compounds of the general formula: A-D-B (I) given in the invention description, or their pharmaceutically acceptable salts that possess property of raf kinase inhibitors and can be used in treatment of disease associated with growth of cancer cells mediated by effect of this kinase. In compounds of the general formula A-D-B (I) D value is represented by the formula -NH-C(O)-NH-; A means a substituted structure comprising up to 40 carbon atoms of the formula -L-(M-L 1 ) q wherein L represents pyridyl or phenyl substituted with halogen atom or (C 1 -C 4 )-alkyl, or 6-membered nitrogen-containing heterocyclic structure bound with D directly; L 1 comprises possibly substituted (C 5 -C 7 )-aryl or (C 5 -C 8 )-nitrogen-containing heterocyclic group; M is a bridge group comprising at least one atom chosen from -O-, -S-, -CO-NH-, -NH-CO-; q is a whole number = 1 or 2; B represents substituted or unsubstituted (C 6 -C 14 )-aryl group or 6-membered heteroaryl group comprising 1-4 heteroatoms chosen from nitrogen, oxygen and sulfur atoms, and wherein L 1 is substituted with at least one substitute chosen from group consisting of -SO 2 R x , -C(O)R x and -C(NR y )R z , and if L 1 means phenyl then -SO 2 R x can not represent -SO 3 H; R y means (C 1 -C 4 )-alkoxy group; R z means hydroxy group, (C 1 -C 4 )-alkyl or (C 1 -C 4 )-alkoxy group; R x means R z or NR a R b wherein R a and R b : (a) are represented by hydrogen atom, (C 1 -C)-alkyl group substituted possibly hydroxy group, (C 1 -C 4 )-alkoxy group or (C 5 -C 6 )-heterocyclic group comprising 1-2 heteroatoms chosen from nitrogen (N) and oxygen (O) atoms that can be substituted with (C 1 -C 4 )-alkyl or amino group substituted possibly with (C 1 -C 4 )-alkyl group, or phenyl, or -OSi(R f ) 3 wherein R f means (C 1 -C 4 )-alkyl group; phenyl substituted possibly with halogen atom, amino group that can be substituted with (C 1 -C 4 ...

Anti-fibrotic pyridinones

피리디논 화합물, 이들 화합물을 제조하는 방법, 그리고 섬유증 장애를 치료하기 위한 방법이 개시되어 있다. Pyridinone compounds, methods of making these compounds, and methods for treating fibrotic disorders are disclosed.

CCR-3 receptor antagonists VII

本发明涉及式(I)的化合物，其中R 1 -R 4 、A、D和L如说明书中所定义。该化合物用作CCR-3受体拮抗剂，因此，可以用于治疗CCR-3介导的疾病。

Bcl-2-selective apoptosis-inducing agents for treating caner and immune diseases

Настоящее изобретение относится к конкретным соединениям или к их терапевтически приемлемой соли, приведенным в формуле изобретения и представляющим производные сульфонилбензамида. Также изобретение относится к фармацевтической композиции, ингибирующей активность анти-апоптотических белков семейства Bcl-2, включающей эксципиент и эффективное количество конкретного производного сульфонилбензамида. Технический результат - производные сульфонилбензамида, которые ингибируют активность анти-апоптотических Bcl-2 белков. 2 н.п. ф-лы, 3 табл., 558 пр. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 405/12 C07D 405/14 C07D 401/12 C07D 403/12 C07D 403/14 C07D 211/96 ФЕДЕРАЛЬНАЯ СЛУЖБА C07D 213/64 ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07D 231/56 C07D 235/26 C07D 417/14 (12) ОПИСАНИЕ (21)(22) Заявка: 2012127760/04, 01.06.2010 01.06.2010 04.12.2009 US 12/631,404 (45) Опубликовано: 27.02.2015 Бюл. № 6 (56) Список документов, цитированных в отчете о поиске: US 2007/072860 A1, 29.03.2007. WO (85) Дата начала рассмотрения заявки PCT на национальной фазе: 04.07.2012 (73) Патентообладатель(и): ЭББВИ ИНК. (US) (86) Заявка PCT: US 2010/036919 (01.06.2010) (87) Публикация заявки PCT: WO 2011/068561 (09.06.2011) Адрес для переписки: 129090, Москва, ул. Большая Спасская, 25, стр. 3, ООО "Юридическая фирма "Городисский и Партнеры" (54) BCL-2-СЕЛЕКТИВНЫЕ АПОПТОЗ-ИНДУЦИРУЮЩИЕ СРЕДСТВА ДЛЯ ЛЕЧЕНИЯ РАКА И ИММУННЫХ ЗАБОЛЕВАНИЙ (57) Реферат: Настоящее изобретение относится к сульфонилбензамида. Также изобретение конкретным соединениям или к их терапевтически относится к фармацевтической композиции, приемлемой соли, приведенным в формуле ингибирующей активность анти-апоптотических изобретения и представляющим производные белков семейства Bcl-2, включающей эксципиент Стр.: 1 C 2 2008/030836 A2, 13.03.2008. US 2005/159427 A1, 21.07.2005. US 2007/015787 A1, 18.01.2007. CHEOL-MIN PARK et al.: "Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins", JOURNAL ...

The tetracycline compound that C7-fluorine replaces

本发明公开了一种C7-氟取代的四环素化合物，所述化合物为由下列结构式表示的化合物：

N-arylamidine-substituted trifluoroethylsulfide derivatives as acaricides and insecticides

Die vorliegende Erfindung betrifft neue N-Arylamidine-substituierte Trifluoroethylsulfid-Derivate der Formel (I), - in welcher X 1 , X 2 , X 3 , X 4 , R 1 , R 2 , R 3 , n die in der Beschreibung angegebenen Bedeutungen haben- deren Anwendung als Akarizide und Insektizide zur Bekämpfung tierischer Schädlinge und Verfahren sowie Zwischenprodukte zu ihrer Herstellung The present invention relates to novel N-arylamidine-substituted trifluoroethylsulfide derivatives of the formula (I) in which X 1, X 2, X 3, X 4, R 1, R 2, R 3, n have the meanings given in the description, their use as acaricides and insecticides for combating animal pests and processes and intermediates for their preparation

N-arylamidine-substituted trifluoroethyl sulfide derivatives as acaricides and insecticides

The present invention relates to novel N-arylamidine-substituted trifluoroethyl sulfide derivatives of the formula (I) in which X 1 , X 2 , X 3 , X 4 , R 1 , R 2 , R 3 , n are each defined as specified in the description, to the use thereof as acaricides and insecticides for control of animal pests, and to processes and intermediates for preparation thereof.

Method for producing a pyrazole-4-carboxylic acid derivative

The invention relates to a method of producing a pyrazole derivative represented by the following formula (6), which comprises reacting a compound represented by the following formula (5) with an oxidant;whereinRis a hydrogen atom or a halogen atom,Ris a Calkyl group,Ris a hydrogen atom or a Calkyl group,Xand Xare each independently a fluorine atom or a chlorine atom, andZis a hydrogen atom or a Calkyl group.

Method for producing pyrazole derivative

The invention relates to a production method of pyrazole derivative (6) by reacting compound (5) with an oxidant. wherein R 1 , R 2 , R 3 , X 1 , X 2 and Z 1 are as defined herein.

3, 4-disubstituted phenoxyphenylamidines and use thereof as fungicides

The present invention relates to 3,4-disubstituted phenoxyphenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to a composition for this purpose, comprising the phenoxyphenylamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.

Phenoxy substituted phenylamidine derivatives and their use as fungicides

3, 4-disubstituted phenoxyphenylamidines and use thereof as fungicides

The present invention relates to 3,4-disubstituted phenoxyphenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to a composition for this purpose, comprising the phenoxyphenylamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.

Novel biphenyl and phenyl-pyridine amides

本发明涉及式(I)化合物或其可药用盐，其中R 1 、R 2 、R 3 、R 4 、R 5 、R 6 、R 7 和R 8 如本文所定义。还公开了采用所述化合物治疗与P2X 3 和/或P2X 2/3 受体拮抗剂相关的疾病的方法以及制备所述化合物的方法。

2-acylaminopropoanol-type glucosylceramide synthase inhibitors

A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-α, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

Glucosylceramide synthase inhibitors for the treatment of diseases

Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).

2-acylaminopropoanol-type glucosylceramide synthase inhibitors

A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-α, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

2-acylaminopropoanol-type glucosylceramide synthase inhibitors

A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-α, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

Glucosylceramide synthase inhibitors for the treatment of diseases

Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).

IMPROVEMENT OF STABILITY OF PHOTO INITIATORS DURING STORAGE

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (11) 2005 116 302 (13) A (51) ÌÏÊ C07D 295/10 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2005116302/04, 17.10.2003 (71) Çà âèòåëü(è): ÖÈÁÀ ÑÏÅØÈÀËÒÈ ÊÅÌÈÊÝËÇ ÕÎËÄÈÍà ÈÍÊ. (CH) (30) Ïðèîðèòåò: 28.10.2002 CH 20021800/02 (43) Äàòà ïóáëèêàöèè çà âêè: 20.01.2006 Áþë. ¹ 02 (74) Ïàòåíòíûé ïîâåðåííûé: Âåñåëèöêà Èðèíà Àëåêñàíäðîâíà Àäðåñ äë ïåðåïèñêè: 101000, Ìîñêâà, Ì.Çëàòîóñòèíñêèé ïåð., 10, êâ.15, "ÅÂÐÎÌÀÐÊÏÀÒ", ïàò.ïîâ. È.À.Âåñåëèöêîé, ðåã. ¹ 11 A (54) ÓËÓ×ØÅÍÈÅ ÑÒÀÁÈËÜÍÎÑÒÈ ÔÎÒÎÈÍÈÖÈÀÒÎÐΠÏÐÈ ÕÐÀÍÅÍÈÈ Ôîðìóëà èçîáðåòåíè R U A 2 0 0 5 1 1 6 3 0 2 1. Ñîåäèíåíèå ôîðìóëû (I) â êîòîðîé R1 îáîçíà÷àåò âîäîðîä èëè àëêèë; R2 îáîçíà÷àåò Ñ1-Ñ4àëêîêñèë èëè ìîðôîëèíîâûé ðàäèêàë; è R3 îáîçíà÷àåò âîäîðîä èëè Ñ1-Ñ4àëêîêñèë. 2. Ñîåäèíåíèå ôîðìóëû (I) ïî ï.1, â êîòîðîé R1 îáîçíà÷àåò âîäîðîä èëè Ñ1-Ñ4àëêèë, ïðåäïî÷òèòåëüíî - ìåòèë; R2 îáîçíà÷àåò ìåòîêñè èëè ìîðôîëèíîâûé ðàäèêàë; è R3 îáîçíà÷àåò âîäîðîä èëè ìåòîêñèë. 3. Ñîåäèíåíèå ôîðìóëû (I) ïî ï.1 Ñòðàíèöà: 1 RU 2 0 0 5 1 1 6 3 0 2 (87) Ïóáëèêàöè PCT: WO 2004/037799 (06.05.2004) (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 30.05.2005 R U (86) Çà âêà PCT: EP 03/50729 (17.10.2003) (72) Àâòîð(û): ÓËÜÐÈÕ Òîìàñ (CH), ÁÎËËÅ Òîìàñ (DE), ÄÈÒËÈÊÅÐ Êóðò (CH), ÂÎËÜÔ Æàí-Ïüåð (CH), ÔÓÊÑ Àíäðå (DE) èëè 2 0 0 5 1 1 6 3 0 2 R U A Ñòðàíèöà: 2 2 0 0 5 1 1 6 3 0 2 â êîòîðîé R1, R2 è R3 âë þòñ òàêèìè, êàê îïðåäåëåíî â ï.1. 5. Ñìåñü ñîåäèíåíè ôîðìóëû (I) ñ ñîåäèíåíèåì ôîðìóëû (II) ïî ï.4, âêëþ÷àþùà ñîåäèíåíèå ôîðìóëû (I) è ñîåäèíåíèå ôîðìóëû (II), â êîòîðîé â êàæäîì ñëó÷àå R1 îáîçíà÷àåò ìåòèë, R2 îáîçíà÷àåò ìîðôîëèíîâûé ðàäèêàë è R3 îáîçíà÷àåò âîäîðîä; èëè âêëþ÷àþùà ñîåäèíåíèå ôîðìóëû (I) è ñîåäèíåíèå ôîðìóëû (II), â êîòîðîé â êàæäîì ñëó÷àå R1 îáîçíà÷àåò âîäîðîä, R2 îáîçíà÷àåò ìîðôîëèíîâûé ðàäèêàë è R3 îáîçíà÷àåò âîäîðîä; èëè âêëþ÷àþùà ñîåäèíåíèå ôîðìóëû (I) è ñîåäèíåíèå ôîðìóëû (II), â êîòîðîé â êàæäîì ñëó÷àå R1 îáîçíà÷àåò ...

Urea derivatives useful as calcium receptor modulators

The present invention provides compounds of formula (I): in which Y is oxygen or sulphur; R1 and R~1 are optionally substituted aryl, heteroaryl or a fused ring structure, R2 and R'2 are each H, or optionally substituted alkyl, alkylaminoalkyl or dialkylaminoalkyl, or R2 and R'2 and their N form a saturated or unsaturated optionally substituted heterocycle, R3 represents a group of formula -(CH2)P-Ar-Rn, wherein p is 0 or 1 and, when p is 1, is optionally substituted, Ar is aryl or heteroaryl, and each R is H, halogen; hydroxyl; trifiuoromethyl; linear and branched alkyl, alkenyl, alkynyl, and alkoxyl groups, all optionally further substituted by one or more of hydroxy groups, halogen atoms, alkoxy groups, amino groups, and alkylthio groups; linear and branched alkoxyl groups; linear and branched thioalkyl groups; aryl groups; aralkyl groups; aralkoxy groups; aryloxy groups; perfluoroalkyl; -CN; -NR4R5, -C(=X)NR4R5,-O-C(=X)NR4R5, -SO2NR4R5, - Alk-NR4R5, -NZC(=X)(NH)qR6, -Alk-NZC(=X)(NH)qR6, -C(=X)R6, -Alk-C(=X)(NH)qR6, -NHSO2R7, -SO2R7, -SOR7, -SR7, or is a saturated or unsaturated heterocyclyl group, and salts and esters thereof, are useful in the treatment of conditions susceptible to modulating ion channels, to a process for their preparation, their application by way of medicaments, and to pharmaceutical compositions containing them.

Process for the preparation of new amino-dihalogen-phenyl-ethylamines

Acyclic ethylenediamine derivatives as substance p receptor antagonists

The present invention relates to novel acyclic ethylenediamine derivatives of nitrogen containing heterocyclic compounds, and specifically, to compounds of formula (I) wherein R?1, R2, R3, R4, R5 and R6¿ are defined as in the specification. It also relates to novel intermediates used in the synthesis of such derivatives. Compounds of formula (I) and their pharmaceutically acceptable salts are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.

Substituted cyclopentyl - azines as casr- active compounds

Compounds of general formula I, (formula [I)], their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.