Amino- and amido-aminotetralin derivatives and related compounds as mu opioid receptor antagonists

The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

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

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

Fatty Acid Inhibitors

Fatty acid inhibitors, pharmaceutical compositions including fatty acid inhibitors, methods for using fatty acid inhibitors to treat a variety of diseases, and methods for preparing fatty acid inhibitors are provided herein. 2. The compound of claim 1 , wherein the unsaturated or polyunsaturated fatty acid comprises an aliphatic chain having 5 to 23 carbons.3. The compound of claim 1 , wherein the unsaturated or polyunsaturated fatty acid is selected from a glycolipid claim 1 , a glycerolipid claim 1 , a phospholipid and a cholesterol ester.4. The compound of claim 1 , wherein Ris nitro (—NO).5. The compound of claim 1 , wherein the one or more electron withdrawing group is positioned on an alpha carbon of a carbon-carbon double bond of the non-naturally occurring claim 1 , unsaturated or polyunsaturated fatty acid.6. The compound of claim 1 , wherein a carbon-carbon double bond associated with Ris in cis configuration.7. The compound of claim 1 , wherein a carbon-carbon double bond associated with Ris in trans configuration.8. The compound of claim 1 , wherein the unsaturated or polyunsaturated fatty acid comprises two or more conjugated carbon-carbon double bonds.9. The compound of claim 8 , wherein Ris at any carbon in the two or more conjugated carbon-carbon double bonds.10. The compound of claim 1 , wherein at least Ris positioned at C-9 claim 1 , C-10 claim 1 , C-12 claim 1 , C-13 or a combination thereof.11. The compound of claim 1 , further comprising one or more non-carbon-carbon linkage selected from an ester linkage claim 1 , an ether linkage claim 1 , and a vinyl ether linkage.12. The compound of claim 1 , further comprising one or more functional group other than an electron withdrawing group positioned at any carbon of the unsaturated or polyunsaturated fatty acid.13. The compound of claim 1 , further comprising a pharmaceutically acceptable carrier claim 1 , excipient claim 1 , or combination thereof.14. The compound of claim 13 , further comprising ...

INTERMEDIATES OF SITAGLIPTIN AND PREPARATION PROCESS THEREOF

Disclosed are intermediates of Sitagliptin, a preparation process thereof, and a process for synthesizing Sitagliptin using these intermediates. Sitagliptin is synthesized by using chiral amino compounds as a raw material, without having to build a chiral center with a chiral asymmetric catalytic hydrogenation, and high-pressure hydrogenation is avoided. 2. The aziridine compound (I) with absolute configuration R according to claim 1 , wherein claim 1 ,{'sup': 1', '3', '3', '1', '4', '4, 'sub': 2', '2, 'Ris —CHSR, wherein Ris methyl; or Ris —CHOR, wherein Ris selected from the group consisting of hydrogen, methoxymethyl, benzyl, p-nitrobenzyl, tert-butyldimethylsilyl and tert-butyldiphenylsilyl; and'}{'sup': '2', 'Ris selected from the group consisting of formate group, acyl, sulfonyl, benzyl and 4-methoxybenzyl, wherein the formate group is selected from the group consisting of methoxycarbonyl, tert-butoxycarbonyl, benzyloxycarbonyl and allyloxycarbonyl; the acyl is benzoyl; the sulfonyl is benzenesulfonyl or trifluoromethylsulfonyl.'}3. The aziridine compound (I) with absolute configuration R according to claim 1 , wherein claim 1 , Ris —CHSR claim 1 , wherein Ris methyl claim 1 , or Ris —CHOR claim 1 , wherein Ris selected from the group consisting of hydrogen claim 1 , benzyl and tert-butyldimethylsilyl; and Ris selected from the group consisting of tert-butoxycarbonyl claim 1 , benzyl and benzenesulfonyl.5. The process according to claim 4 , wherein claim 4 , Ris —CHSR claim 4 , wherein Ris methyl claim 4 , or Ris —CHOR claim 4 , wherein Ris selected from the group consisting of hydrogen claim 4 , benzyl and tert-butyldimethylsilyl; Ris selected from the group consisting of tert-butoxycarbonyl claim 4 , benzyl and benzenesulfonyl; Ris methanesulfonate or p-toluenesulfonate.6. The process according to claim 4 , wherein the alkali is organic alkali or inorganic alkali;wherein the inorganic alkali is one or more alkalis selected from the group consisting of sodium ...

JOINT PRODUCTION METHOD AND DEVICE FOR AZIRIDINE, PIPERAZINE AND TRIETHYLENEDIAMINE

Disclosed are a joint production method and device for aziridine, piperazine and triethylenediamine. The method comprises: reaction 1, preparing piperazine and triethylenediamine by taking ethanol amine as a raw material under the existence of a cyclamine catalyst; reaction 2, preparing aziridine by taking the ethanol amine as the raw material under the existence of a catalyst B; and taking heat released in the reaction 1 as a heat source of heat absorption in the reaction 2. The device comprises a reactor 1 for carrying out the reaction 1 and the heat exchange between reaction materials of the reaction 1 and the raw material of the reaction 2 and a reactor 2 for carrying out the reaction 2. According to the present invention, the same raw material, namely the ethanol amine is adopted, aziridine, piperazine and triethylenediamine can be produced in a joint manner, the heat released in the reaction 1 is used for preheating materials in the reaction 2, so that heat coupling between the reactions is implemented, energy conservation is facilitated and competitiveness of the device is improved. 1. A joint production method for aziridine , piperazine and triethylenediamine , characterized in that , the method comprises:reaction 1, preparing piperazine and triethylenediamine by taking ethanol amine as a raw material in the presence of a cyclamine catalyst; andreaction 2, preparing aziridine by taking the ethanol amine as a raw material in the presence of a catalyst B;{'sub': a', 'b', 'c', 'd', 'e', 'f, 'wherein the catalyst B is TiPBXYO, wherein: X is an alkaline earth metal, Y is an alkaline metal, 0 is an oxygen element; a, b, c, d, e, and f are the mole ratios of each element atom, and a=1, b=0.02˜0.2, c=0.002˜0.02, d=0.01˜0.1, e=0.001˜0.01, and f is dependent on a, b, c, d, and e;'}the heat released in the reaction 1 is used as a heat source for the reaction 2.2. The joint production method for aziridine claim 1 , piperazine and triethylenediamine of claim 1 , ...

PYRIDONE COMPOUNDS AND AGRICULTURAL AND HORTICULTURAL FUNGICIDES CONTAINING THE SAME AS ACTIVE INGREDIENTS

Pyridine compounds of Formula (1) are provided: 2. The compound or a salt thereof according to claim 1 , whereinHet representsa pyridyl group, a pyridazinyl group, a pyrimidinyl group, a pyrazinyl group, a triazinyl group, a tetrazinyl group, a thienyl group, a thiazolyl group, an isothiazolyl group, a thiadiazolyl group, a thiatriazolyl group, a pyrrolyl group, a pyrazolyl group, an imidazolyl group, a triazolyl group, a tetrazolyl group, a pentazolyl group, a furyl group, an oxazolyl group, an indolyl group, an isoindolyl group, an indazolyl group, a benzimidazolyl group, a benzotriazolyl group, a benzofuryl group, an isobenzofuryl group, a benzoxazolyl group, a benzothienyl group, benzothiazolyl group, a benzisothiazolyl group, a benzothiadiazolyl group, an indolidinyl group, an imidazopyridyl group, a pyrazolopyridyl group, a triazolopyridyl group, a pyrrolopyrimidinyl group, an imidazopyrimidinyl group, a pyrazolopyrimidinyl group, a triazolopyrimidinyl group, a pyrrolopyrazinyl group, an imidazopyrazinyl group, a pyrazolopyrazinyl group, a triazolopyrazinyl group, a quinolyl group, an isoquinolyl group, a cinnolyl group, a phthalazinyl group, a quinoxalynyl group, a quinazolynyl group, a naphthylidinyl group or a 3 to 6-membered ring group containing 1 to 2 oxygen atoms,the pyridyl group, the pyridazinyl group, the pyrimidinyl group, the pyrazinyl group, the triazinyl group or the tetrazinyl group is optionally substituted with 0 to 4 substituents R3 (with the proviso that when two or more substituents R3 are present, each R3 represents an independent substituent),the thienyl group, the thiazolyl group, the isothiazolyl group, the thiadiazolyl group or the thiatriazolyl group is optionally substituted with 0 to 3 substituents R3 (with the proviso that when two or more substituents R3 are present, each R3 represents an independent substituent),the pyrrolyl group, the pyrazolyl group, the imidazolyl group, the triazolyl group, the tetrazolyl group or the ...

WATER-SOLUBLE PROPOFOL DERIVATIVES AND USES THEREOF

The present invention discloses a class of water-soluble propofol derivatives, preparation method thereof, anesthetization method using the same, use thereof as prodrugs and use thereof in the preparation of intravenous anesthetics. The water-soluble propofol derivatives have the general formula (I); wherein X is H or F, Y is F or alkyl substituted by one or more F, n is 1, 2, 3, 4, 5 or 6, W is Wor W; Wis NRR.A or 6. The water soluble propofol derivative according to claim 1 , characterized in that the metal ion is an alkali metal ion claim 1 , an alkaline earth metal ion or a trivalent metal ion.7. The water soluble propofol derivative according to claim 6 , characterized in that the metal ion is a lithium ion claim 6 , a sodium ion or a potassium ion.8. The water soluble propofol derivative according to claim 6 , characterized in that the alkaline earth metal ion is a magnesium ion claim 6 , a zinc ion or a calcium ion.9. The water soluble propofol derivative according to claim 6 , characterized in that the trivalent metal ion is an aluminum ion.11. The water soluble propofol derivative according to claim 10 , characterized in that the alkyl is Calkyl.12. The water soluble propofol derivative according to claim 11 , characterized in that the Calkyl is methyl claim 11 , ethyl claim 11 , propyl claim 11 , isopropyl claim 11 , butyl or isobutyl.13. The water soluble propofol derivative according to claim 10 , characterized in that the cycloalkyl is Ccycloalkyl.14. The water soluble propofol derivative according to claim 13 , characterized in that the Ccycloalkyl is cyclopropyl claim 13 , cyclobutyl claim 13 , cyclopentyl or cyclohexyl.15. The water soluble propofol derivative according to claim 10 , characterized in that R claim 10 , R claim 10 , Rand Rare each independently H claim 10 , methyl claim 10 , ethyl claim 10 , propyl claim 10 , isopropyl claim 10 , butyl claim 10 , isobutyl claim 10 , benzyl claim 10 , cyclopropyl claim 10 , cyclobutyl claim 10 , ...

High-throughput method to rapidly add chemical moieties to a small molecule library

Organic compounds for target identification, drug discovery, chemical library production, high-throughput screening, fluorophore conjugation, chemiluminescent compound conjugation, creation of proximity induced modulators (e.g., protein degraders)/chimeric molecules, or a combination thereof are described. The compounds can contain small molecule moieties for identification of their potential targets; an isocyanate, photoactivatable groups; chemical moieties for enrichment and detection of target-small molecule moiety interactions; proximity induced modulator element; fluorophores; chemiluminescent groups; or combinations thereof.

NOVEL ARYL ETHENE DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT

The present invention relates to an aryl ethene derivative, for inhibiting an estrogen-related receptor gamma (ERRγ) activity, a prodrug of same, a solvate of same, a stereoisomer of same or pharmaceutically acceptable salts of same, and a pharmaceutical composition containing same as an active ingredient. 2. The method of claim 1 , wherein the thyroid cancer is analpastic thyroid cancer.4. The method of claim 1 ,wherein{'sup': 1', '11', '12', '13', '14', '16', '17', '15, 'sub': 2', 'm', '2', 'm', '2', 'm', '2', 'n', '2', 'm, 'Ris (C3-C10)heterocycloalkyl, (C3-C10)heteroaryl, —O—(CH)—R, —(CH)—R, —NH—(CH)—R, —NHCO—(CH)—R, or —SiRR—(CH)—R;'}{'sup': 11', '15, 'Rto Rare independently of one another (C3-C10)heterocycloalkyl;'}{'sup': 16', '17, 'Rand Rare independently of each other (C1-C10)alkyl;'}m is an integer of 1 to 3;n is an integer of 0 or 1;Ar is (C6-C12)aryl or (C3-C12)heteroaryl, in which the aryl or heteroaryl of Ar may be further substituted by one or more selected from the group consisting of hydroxy, halogen, (C1-C10)alkyl, halo(C1-C10)alkyl, (C1-C10)alkoxy, nitro, cyano, amino, (C1-C10)alkylsulfonylamino, (C3-C10)cycloalkylsulfonylamino, di((C1-C10)alkyl sulfonyl)amino, (C1-C10)alkylcarbonyloxy, (C1-C10)alkylcarbonylamino, guanidino, (C1-C10)alkyl sulfonyl, (C1-C10)alkylsulfonyloxy, halo(C1-C10)alkylsulfonyloxy, and (C3-C10)cycloalkylsulfonyloxy;{'sup': '2', 'Ris hydroxy, fluoro, (C1-C10)alkylcarbonyloxy, or (C1-C10)alkylsulfonyloxy; and'}{'sup': 1', '11', '15, 'the heterocycloalkyl or heteroaryl of Rand the heterocycloalkyl of Rto Rmay be further substituted by one or more selected from the group consisting of (C1-C10)alkyl, (C3-C10)cycloalkyl, (C2-C10)alkenyl, amidino, (C1-C10)alkoxycarbonyl, hydroxy(C1-C10)alkyl, and di(C1-C10)alkylamino(C1-C10)alkyl.'}5. The method of claim 4 , wherein{'sup': 1', '11', '11', '1', '11, 'sub': 2', 'm, 'Ris (C3-C10)heterocycloalkyl or —O—(CH)—R; Ris (C3-C10)heterocycloalkyl; m is an integer of 1 to 3; and the ...

JOINT PRODUCTION METHOD AND DEVICE FOR AZIRIDINE, PIPERAZINE AND TRIETHYLENEDIAMINE

Disclosed are a joint production method and device for aziridine, piperazine and triethylenediamine. The method comprises: reaction 1, preparing piperazine and triethylenediamine by taking ethanol amine as a raw material under the existence of a cyclamine catalyst; reaction 2, preparing aziridine by taking the ethanol amine as the raw material under the existence of a catalyst B; and taking heat released in the reaction 1 as a heat source of heat absorption in the reaction 2. The device comprises a reactor for carrying out the reaction 1 and the heat exchange between reaction materials of the reaction 1 and the raw material of the reaction 2 and a reactor for carrying out the reaction 2. According to the present invention, the same raw material, namely the ethanol amine is adopted, aziridine, piperazine and triethylenediamine can be produced in a joint manner, the heat released in the reaction 1 is used for preheating materials in the reaction 2, so that heat coupling between the reactions is implemented, energy conservation is facilitated and competitiveness of the device is improved. 15-. (canceled)6. A device for production of aziridine , piperazine and triethylenediamine , the device comprising:a first reactor, for carrying out a first reaction and for heat exchange between reaction materials of the first reaction and raw materials of a second reaction;a second reactor, for carrying out the second reaction; anda combination separation unit, comprising a flash unit, an aziridine separation unit, and a polyamine separation unit connected successively, wherein the flash unit is configured for separating nitrogen, the aziridine separation unit is configured for separating aziridine, and the polyamine separation unit is configured for separating piperazine and triethylenediamine.7. The device of claim 6 , wherein the flash unit is a flash tower having a theoretical plate number of 1 to 3 claim 6 , and is configured for operation at a temperature in a range of 0° C. ...

Compliant hydrophilic coatings for medical devices

Example compliant hydrophilic coatings including a base coat and a lubricious top coat for coating a medical device including a flexible substrate. The coatings exhibit reduced cracking and peeling in response to deformation or expansion of the flexible substrate. Example techniques for coating a medical device including a flexible substrate with compliant hydrophilic coatings.

Biosourced compound having epoxide functions, method for the synthesis of such a compound, and use thereof for producing epoxy resin

A compound has at least one epoxide function which can be synthesized by an epoxidation reaction of a compound having at least one hydroxyl function obtained by depolymerization of condensed tannins by a nucleophile selected from furan and the derivatives thereof. The compound having at least one epoxide function has properties that are useful in the production of epoxy resins, as a synthon precursor and/or as a starting material for forming a polyamine hardener.

Method and catalyst for synthesising aziridine

The present invention relates to methods of synthesising aziridines including isotopically labelled aziridines, said methods comprising contacting an imine or one or more precursors thereof with a diazo compound in the presence of a phosphoramide or a phosphoramide-derived catalyst. The present invention also relates to aziridines, modified aziridines and aziridine-derived compounds preparable by the aforementioned methods, and to phosphoramide or phosphoramide-derived catalysts suitable for use in such methods.

METHOD AND CATALYST FOR SYNTHESISING AZIRIDINE

The present invention relates to methods of synthesising aziridines including isotopically labelled aziridines, said methods comprising contacting an imine or one or more precursors thereof with a diazo compound in the presence of a phosphoramide or a phosphoramide-derived catalyst. The present invention also relates to aziridines, modified aziridines and aziridine-derived compounds preparable by the aforementioned methods, and to phosphoramide or phosphoramide-derived catalysts suitable for use in such methods. 138-. (canceled)40. A method as claimed in claim 39 , wherein:(i) the imine (I), one or more precursors thereof, and/or the diazo compound (II) are isotopically labelled such that the resultant aziridine (III) is also isotopically labelled; and/or(ii) the imine (I) or the salt or the one or more precursors thereof are contacted with the diazo compound (II) or the salt thereof in a solvent comprising a mixture of halocarbons.41. A method as claimed in claim 39 , wherein the catalyst is:(i) a chiral compound of formula (IV) or a salt thereof, or a chiral compound of formula (V) or a salt thereof; and/or(ii) a compound of formula (IV) or a salt thereof.42. A method as claimed in claim 39 , wherein:the method comprises contacting the imine (I) or the salt thereof with the diazo compound (II) or the salt thereof; or{'sub': '2', 'sup': 3', '1', '2, '(ii) the method comprises contacting the imine (I) or the salt thereof with the diazo compound (II) or the salt thereof, and wherein the method further comprises the step of synthesising the imine (I) or the salt thereof from an amine HNRor a salt or protected derivative thereof, and a carbonyl compound RCORor a salt or protected derivative thereof; or'}{'sub': '2', 'sup': 3', '1', '2, '(iii) the method comprises contacting the imine (I) or the salt thereof with the diazo compound (III) or the salt thereof, and wherein the method further comprises the step of synthesising the imine (I) or the salt thereof from an amine ...

Carboxylic Branched Chain-Cutting Agent for Golf Ball-Covering Ionomer Resin, Golf Ball Coating Composition, and Method for Manufacturing Golf Ball

The present invention relates to a carboxylic branched chain-cutting agent for a golf ball-covering ionomer resin, a golf ball coating composition, and a method for manufacturing a golf ball. The present invention can provide a coating composition containing within an appropriate range, a specific compound for use as a carboxylic branched chain-cutting agent for a golf ball-covering ionomer resin, and thus can provide a golf ball on which a bridge is formed between a golf ball covering resin and a coating resin. By providing the coating composition containing a specific composition for use as a carboxylic branched chain-cutting agent for a golf ball-covering ionomer resin, the present invention is appropriate for ensuring the physical properties of the golf ball, such as yellowing resistance, and workability, such as pot life, even eliminating an adhesion pretreatment step, thereby reducing side effects due to the existing pretreatment step while providing a golf ball having excellent physical properties. 3. The carboxylic branched chain cleavage agent of claim 1 , wherein the golf ball cover ionomer resin is one or more selected from the group consisting of a hard ionomer which is a magnesium claim 1 , lithium claim 1 , sodium or zinc salt of a copolymer of a C-Colefin with a C-Cunsaturated monocarboxylic acid and has a modulus of 30 claim 1 ,000 to 55 claim 1 ,000 P.S.I. claim 1 , and a soft ionomer which is a magnesium claim 1 , lithium claim 1 , sodium or zinc salt of a copolymer of a C-Colefin with a C-Cacrylate ester-based unsaturated monomer and has a modulus of 3 claim 1 ,000 to 7 claim 1 ,000 P.S.I.4. The carboxylic branched chain cleavage agent of claim 3 , wherein the golf ball cover ionomer resin is one or more selected from the group consisting of a hard ionomer which is a magnesium claim 3 , lithium claim 3 , sodium or zinc salt of a copolymer of ethylene with methacrylic acid claim 3 , and a soft ionomer which is a sodium salt of a terpolymer of n- ...

NOVEL ARYL ETHENE DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT

The present invention relates to an aryl ethene derivative, for inhibiting an estrogen-related receptor gamma (ERRγ) activity, a prodrug of same, a solvate of same, a stereoisomer of same or pharmaceutically acceptable salts of same, and a pharmaceutical composition containing same as an active ingredient. 3. The arylethene derivative claim 1 , or the prodrug claim 1 , solvate claim 1 , stereoisomer claim 1 , or pharmaceutically acceptable salt thereof claim 1 , of claim 1 , wherein{'sup': 1', '11', '12', '13', '14', '16', '17', '15, 'sub': 2', 'm', '2', 'm', '2', 'm', '2', 'n', '2', 'm, 'Ris (C3-C10)heterocycloalkyl, (C3-C10)heteroaryl, —O—(CH)—R, —(CH)—R, —NH—(CH)—R, —NHCO—(CH)—R, or —SiRR—(CH)—R;'}{'sup': 11', '15, 'Rto Rare independently of one another (C3-C10)heterocycloalkyl;'}{'sup': 16', '17, 'Rand Rare independently of each other (C1-C10)alkyl;'}m is an integer of 1 to 3;n is an integer of 0 or 1;Ar is (C6-C12)aryl or (C3-C12)heteroaryl, in which the aryl or heteroaryl of Ar may be further substituted by one or more selected from the group consisting of hydroxy, halogen, (C1-C10)alkyl, halo(C1-C10)alkyl, (C1-C10)alkoxy, nitro, cyano, amino, (C1-C10)alkylsulfonylamino, (C3-C10)cycloalkylsulfonylamino, di((C1-C10)alkylsulfonyl)amino, (C1-C10)alkylcarbonyloxy, (C1-C10)alkylcarbonylamino, guanidino, (C1-C10)alkylsulfonyl, (C1-C10)alkylsulfonyloxy, halo(C1-C10)alkylsulfonyloxy, and (C3-C10)cycloalkylsulfonyloxy;{'sup': '2', 'Ris hydroxy, fluoro, (C1-C10)alkylcarbonyloxy, or (C1-C10)alkylsulfonyloxy; and'}{'sup': 1', '11', '15, 'the heterocycloalkyl or heteroaryl of Rand the heterocycloalkyl of Rto Rmay be further substituted by one or more selected from the group consisting of (C1-C10)alkyl, (C3-C10)cycloalkyl, (C2-C10)alkenyl, amidino, (C1-C10)alkoxycarbonyl, hydroxy(C1-C10)alkyl, and di(C1-C10)alkylamino(C1-C10)alkyl.'}4. The arylethene derivative claim 3 , or the prodrug claim 3 , solvate claim 3 , stereoisomer claim 3 , or pharmaceutically acceptable salt ...

REAGENT FOR MASS SPECTROMETRY

The present invention relates to reagents which are suitable to be used in mass spectrometry as well as methods of mass spectrometric determination of analyte molecules using said reagents. 1. Compound of formula A:{'br': None, 'X-L1-Y-L2-Z'}whereinX is a reactive unit, which is in particular capable of forming a covalent bond with an analyte molecule,L1 and L3 are independently of each other substituted or unsubstituted linker, in particular linear linkerY is a neutral loss unit,Z is a charged unit comprising at least one permanently charged moiety, in particular comprising one permanently charged moiety,including any salt thereof.2. Compound of claim 1 , wherein the reactive unit X is selected from the group consisting of carbonyl reactive unit claim 1 , diene reactive unit claim 1 , hydroxyl reactive unit claim 1 , amino reactive unit claim 1 , an imine reactive unit claim 1 , a thiol reactive unit claim 1 , a diol reactive unit claim 1 , a phenol reactive unit claim 1 , epoxide reactive unit claim 1 , a disulfide reactive unit claim 1 , and a azide reactive unit.3. Compound of any of the preceding claims claim 1 , wherein the reactive unit X is a carbonyl-reactive group claim 1 , in particular wherein X is selected from the group consisting of(i) a hydrazine unit, in particular a H2N—NH—, or H2N-NR1-unit, wherein R1 is aryl or C1-4 alkyl, particularly C1 or C2 alkyl, optionally substituted,(ii) a hydrazide unit, in particular a carbo-hydrazide or a sulfohydrazide, in particular a H2N—NH—C(O)—, or H2N-NR2-C(O)— unit, wherein R2 is aryl or C1-4 alkyl, particularly C1 or C2 alkyl, optionally substituted,(iii) a hydroxylamino unit, in particular a H2N—O— unit, and(iv) a dithiol unit, particularly a 1,2-dithiol or 1,3-dithiol unit.4. Compound of or claim 1 , wherein the reactive unit X is a thiol-reactive group or is an amino-reactive group such as an active ester group claim 1 , e.g. N-hydroxysuccinimide (NHS) ester or sulpho-NHS ester claim 1 , a ...

Benzoylglycine Derivatives and Methods of Making and Using Same

Disclosed are compounds of formulae: 3. The method of claim 1 , wherein Ris —CO(C-Calkyl) claim 1 , —C-Calkyl-CO(C-Calkyl) claim 1 , —C-Calkyl-COH claim 1 , C-Ccycloalkyl optionally substituted with R claim 1 , or (C-Ccycloalkyl)C-Calkyl- optionally substituted with R.4. The method of claim 1 , wherein Ris C-Ccycloalkyl optionally substituted with R; or Ris cyclopropyl claim 1 , cyclopentyl claim 1 , or cyclohexyl claim 1 , each optionally substituted with R.5. The method of claim 1 , wherein each Ris independently selected from the group consisting of halogen claim 1 , C-Calkyl claim 1 , C-Chaloalkyl claim 1 , —NH claim 1 , —NH(C-Calkyl) claim 1 , —N(C-Calkyl) claim 1 , —OH claim 1 , C-Calkoxy claim 1 , C-Chaloalkoxy claim 1 , —C-Calkyl-OH claim 1 , —C-Calkyl-(C-Calkoxy) claim 1 , —C-Calkyl-NH claim 1 , —C-Calkyl-NH—C-Calkyl) claim 1 , —C-Calkyl-N(C-Calkyl) claim 1 , —C-Calkyl-NH(SOC-Calkyl) claim 1 , —CONH claim 1 , —CON(C-Calkyl) claim 1 , —CON(C-Calkyl) claim 1 , —CO(C-Calkyl) claim 1 , —COH claim 1 , —CO(C-Calkyl) claim 1 , —C-Calkyl-CONH claim 1 , —C-Calkyl-CON(C-Calkyl) claim 1 , —C-Calkyl-CON(C-Calkyl) claim 1 , —C-Calkyl-CO(C-Calkyl) claim 1 , —C-Calkyl-COH claim 1 , and —C-Calkyl-CO(C-Calkyl).6. The method of claim 1 , wherein Ris C-Calkyl claim 1 , C-Chaloalkyl claim 1 , —CO(C-Calkyl) claim 1 , —C-Calkyl-CO(C-Calkyl) claim 1 , —C-Calkyl-COH claim 1 , C-Ccycloalkyl optionally substituted with R claim 1 , or heterocyclyl optionally substituted with R.7. The method of claim 1 , wherein Ris C-Ccycloalkyl optionally substituted with Ror (C-Ccycloalkyl)C-Calkyl- optionally substituted with R; or Ris C-Ccycloalkyl optionally substituted with R; or Ris cyclopropyl claim 1 , cyclopentyl claim 1 , or cyclohexyl claim 1 , each optionally substituted with R.8. The method of claim 1 , wherein each Ris independently selected from the group consisting of halogen claim 1 , C-Calkyl claim 1 , C-Chaloalkyl claim 1 , —NH claim 1 , —NH(C-Calkyl) claim 1 , —N(C-Calkyl) claim ...

Modifying Polymeric Materials By Amines

This invention relates to the modification of polymeric materials containing reactive carbon-to-carbon unsaturation and to amines, including aziridines, which are used in such modification. A polymeric material containing carbon-to-carbon bonds can be modified by crosslinking or to make it susceptible to crosslinking. 1. A process for modifying a polymeric material containing carbon-to-carbon unsaturation , characterised in that the polymeric material is treated with a compound (II) containing in its molecule at least two moieties of the formula —OC(O)-(Az)-J wherein Az represents an aziridine ring bonded to the group J through its nitrogen atom; and J represents a hydrocarbyl or substituted hydrocarbyl group having 1 to 20 carbon atoms.2. A process according to claim 1 , characterised in that the compound (II) has the formula Q(—OC(O)-(Az)-J)wherein x=2 to 6; and Q is the residue of a polyol having at least x hydroxyl groups.3. A process according to claim 1 , characterised in that the compound (II) has the formula M(—OC(O)-(Az)-J)wherein M represents a metal ion of valence m claim 1 , preferably a divalent metal ion.4. A process according to wherein the polymeric material and the compound (II) are heated together at a temperature of 120 to 200° C. claim 1 , whereby the polymeric material is crosslinked by the compound (II).5. A process according to wherein the polymeric material and the compound (II) are mixed at a temperature of 0 to 120° C. and subsequently heated at a temperature of 120 to 200° C. to crosslink the polymeric material.6. A process according to claim 1 , characterised in that the polymeric material is a diene rubber.7. A process according to claim 1 , characterised in that the polymeric material is an organopolysiloxane containing alkenyl groups.10. An aziridine compound having the formula M(—OC(O)-(Az)-J)wherein M represents a divalent metal ion; Az represents an aziridine ring bonded to the group J through its nitrogen atom; and J represents a ...

Method for the stereoselective preparation of amino acid derivatives

The invention relates to a process for the stereoselective preparation of amino acid derivatives, comprising a hydrogenation reaction of the compound of formula (III), alternatively its enantiomer, wherein R is (C 1 -C 8 )-alkyl; followed by a hydrolysis reaction to obtain L-mesityl alanine, alternatively its enantiomer D-mesityl alanine and, optionally, subjecting said compound to an amino group protection reaction, particularly as Fmoc. It also comprises Fmoc-L- or Fmoc-D- mesityl alanine as products per se, useful as intermediates in preparing peptides or peptide analogs with therapeutic or biological activity.

POST-CURABLE PRESSURE-SENSITIVE ADHESIVE

The present disclosure is directed to a curable precursor of a pressure sensitive adhesive comprising: 117-. (canceled)18. A cured pressure sensitive adhesive comprising a cured product of a curable precursor , wherein the cured product is an interpenetrating polymer network that is formed from a (meth)acrylate ester based (co)polymeric network and an aziridine polymeric network , wherein a (meth)acrylate ester monomer;', 'an optional co-monomer having an ethylenically unsaturated group, the co-monomer being a non-acid functional polar monomer;, 'a) the (meth)acrylate ester based (co)polymeric network comprising the reaction product of a (co)polymerizable material comprising'} a polyfunctional aziridine having at least two aziridine functional groups; and', 'an acid generating agent selected from the group consisting of thermal acid generating agents, photo acid generating agents, and any combinations or mixtures thereof., 'b) the azidine polymeric network resulting from acid-catalyzed cationic ring-opening polymerization of a reaction mixture comprising'}21. The cured pressure sensitive adhesive of claim 18 , wherein the acid generating agent is a thermal acid generating agent selected from the group consisting of quaternary blocked superacids claim 18 , amine blocked superacids claim 18 , and any combinations or mixtures thereof.22. The cured pressure sensitive adhesive of claim 18 , wherein the acid generating agent is a photo acid generating agent selected from the group consisting of ionic salts of organometallic complexes claim 18 , iodonium or sulfonium salts and any combinations or mixtures thereof.23. The cured pressure sensitive adhesive of claim 18 , wherein the non-acid functional polar monomer has a nitrogen-containing group or a salt thereof.24. The cured pressure sensitive adhesive of claim 23 , wherein the nitrogen-containing group is selected from secondary amido groups and tertiary amido groups.25. The cured pressure sensitive adhesive of claim 18 ...

KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF

Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity. 146.-. (canceled)48. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein X is —CRR—.49. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris hydrogen claim 47 , hydroxyl claim 47 , lower alkoxy claim 47 , amino optionally substituted with one or more alkyl groups claim 47 , or lower alkyl optionally substituted with one or more groups independently selected from halo claim 47 , hydroxyl claim 47 , lower alkoxy claim 47 , and amino optionally substituted with one or more alkyl groups.50. The compound of claim 49 , or a pharmaceutically acceptable salt thereof claim 49 , wherein Ris hydrogen claim 49 , amino claim 49 , methylamino claim 49 , dimethylamino claim 49 , hydroxyl claim 49 , methyl claim 49 , methoxy ...

Modifying Polymeric Materials By Amines

This invention relates to the modification of polymeric materials containing reactive carbon-to-carbon unsaturation and to amines, including piperazines, which are used in such modification. A polymeric material containing carbon-to-carbon bonds can be modified by crosslinking or to make it susceptible to crosslinking.

DERIVATIVES OF EPA ENDOCANNABINOID EPOXIDES AS ANTI-INFLAMMATORY, ANTI-CANCEROUS, ANTI-ANGIOGENC AND ANTIPLATELET AGGREGATION COMPOUNDS

The present disclosure provides chemical compound derivatives of a class of biological lipid mediators known as endocannabinoids and methods of synthesizing the compositions. These compounds are useful for treating cancer, reducing inflammation, reducing platelet aggregation, and reducing angiogenesis. 3. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris hydrogen.4. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris Calkyl , or —Calkylene-R , -G , or —Calkylene-G.5. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris —Calkylene-R.6. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein{'sup': 2', '2', '2, 'sub': '1-6', 'Ris -Gor —Calkylene-G, and'}{'sup': 2', 'x2, 'sub': '3-8', 'Gis Ccycloalkyl optionally substituted with 1, 2, 3, or 4 R.'}8. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Rat each occurrence is independently —OH or —NH.11. A pharmaceutical composition comprising a therapeutically effective amount of a compound of any one of - , or a pharmaceutically acceptable salt thereof , and a pharmaceutically acceptable carrier.12. The compound of any one of - , or a pharmaceutically acceptable salt thereof , for use in treating cancer.13. The compound of any one of - , or a pharmaceutically acceptable salt thereof , for use in reducing inflammation in a subject.14. The compound of any one of - , or a pharmaceutically acceptable salt thereof , for use in reducing platelet aggregation in a subject.15. The compound of any one of - , or a pharmaceutically acceptable salt thereof , for use in reducing angiogenesis in a subject.16. The compound of any one of - , or a pharmaceutically acceptable salt thereof , for use in inducing vasoconstriction or vasodilation in a subject.17. Use of a compound of any one of - , or a pharmaceutically acceptable salt thereof , for ...

(METH)ACRYLATE COMPOUND, AND COPOLYMER AND HOMOPOLYMER COMPRISING REPEATING UNIT DERIVED FROM SAME

The present specification relates to a (meth)acrylate compound, and a copolymer and a homopolymer including a repeating unit derived therefrom. 2. The (meth)acrylate compound of claim 1 , wherein Chemical Formula 1 is obtained by a reaction of an aziridine compound; and (meth)acrylate including a (meth)acrylic acid or a hydroxy group (—OH) as a substituent group.7. A copolymer comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a repeating unit derived from the (meth)acrylate compound according to .'}8. A homopolymer comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a repeating unit derived from the (meth)acrylate compound according to .'}9. The homopolymer of claim 8 , wherein a glass transition temperature (Tg) of the homopolymer is 100° C. to 300° C.10. The homopolymer of claim 8 , wherein a storage modulus of the homopolymer measured by a DMA (dynamic mechanical analysis) method at 25° C. is 3000 to 30000 MPa.11. The homopolymer of claim 8 , wherein a gel fraction of the homopolymer is 85% to 100%.12. The homopolymer of claim 8 , wherein claim 8 , of an IR spectrum of the homopolymer claim 8 , a peak of a region band of 1408 cmwhich is a C═C band of a (meth)acrylate group of a repeating unit derived from the (meth)acrylate compound of the homopolymer is reduced as compared to a peak of an IR spectrum of the (meth)acrylate compound.13. The homopolymer of claim 8 , wherein claim 8 , of an IR spectrum of the homopolymer claim 8 , an integral value of peak areas of a region band of 1408 cmwhich is a C═C band of a (meth)acrylate group of a repeating unit derived from the (meth)acrylate compound of the homopolymer is reduced by 80% or more based on 100% of an integral value of peak areas of an IR spectrum of the (meth)acrylate compound. This application claims priority to and the benefit of Korean Patent Application No. 10-2014-0132135 filed in the Korean Intellectual Property Office on Sep. 30, 2014, the entire contents of which are incorporated ...

Polymeric Materials Modified By Silanes

This invention relates to a process for modifying a polymeric material having a carbon backbone containing carbon-to-carbon unsaturation by reaction with a hydrolysable silane. The polymeric material can for example be a diene elastomer, and the invention relates to a composition comprising a diene elastomer, a hydrolysable silane and a curing agent for the diene elastomer, and also to the use of a hydrolysable silane as a coupling agent for a diene elastomer composition containing a filler.

SMALL MOLECULE INHIBITORS OF THE MITOCHONDRIAL PERMEABILITY TRANSITION PORE (mtPTP)

The present technology relates to compounds of any one of Formula I, II, IIa, III, IV, and/or V as described herein and their tautomers and/or pharmaceutically acceptable salts, compositions, and methods of uses thereof. 3. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare independently at each occurrence hydrogen claim 1 , C-Calkyl claim 1 , C-Ccycloalkyl claim 1 , C-Calkenyl claim 1 , C-Calkynyl claim 1 , aryl claim 1 , cyano claim 1 , carboxyl claim 1 , carboxyl ester claim 1 , acyl claim 1 , formyl claim 1 , C-Cheteroaryl claim 1 , or C-Cheterocyclyl claim 1 , or two adjacent R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rtogether form an aryl claim 1 , heteroaryl claim 1 , or heterocyclyl ring.5. The compound of claim 4 , wherein Ris H claim 4 , F claim 4 , Cl claim 4 , or methoxy.6. The compound of claim 2 , wherein Yis O and Wis N or Yis NH and Wis N.7. The compound of claim 2 , wherein Zis CH.8. A composition comprising a compound of and a pharmaceutically acceptable excipient.1112-. (canceled)13. A method for treating a disease in a subject claim 1 , wherein the method comprises administering an effective amount of a compound of to the subject claim 1 , wherein the disease is multiple sclerosis claim 1 , amyotropic lateral sclerosis claim 1 , ischemic reperfusion injury claim 1 , Alzheimer's disease claim 1 , Huntington's disease claim 1 , Parkinson's disease claim 1 , insulin-induced hypoglycemia claim 1 , cerebral ischemia claim 1 , brain damage from epilepsy or experimental trauma claim 1 , Bethlem myopathy claim 1 , pancreatitis claim 1 , hepatitis (type A claim 1 , and/or B claim 1 , and/or C) claim 1 , type II diabetes claim 1 , diabetic retinopathy claim 1 , muscular dystrophy claim 1 , traumatic brain injury claim 1 , heart infarction claim 1 , and/or stroke.16. A method for inhibiting the mitochondrial permeability transition pore claim 1 , wherein the ...

CATALYST FOR SYNTHESIZING ETHYLENIMINE AS WELL AS PREPARATION METHOD AND APPLICATION THEREOF

The present invention relates to a catalyst for synthesizing ethylenimine as well as a preparation method and application thereof. The related catalyst comprises a carrier and metal ions loaded on the carrier; the carrier is a composite oxide comprising titanium, silicon and phosphorus elements; the metal ions are magnesium ions, iron ions and cesium ions; the molar ratio of the magnesium ions to the iron ions to the cesium ions is (1-10):1:0.1; the mass of all metal ions is 0.5-10 percent of that of the carrier. In the related preparation method, a catalyst precursor is roasted at the temperature of 350-650° C., so that the catalyst is obtained; the catalyst precursor is the mixture of the carrier, soluble salt of magnesium, soluble salt of iron and soluble salt of cesium. The present invention also provides the application of the catalyst to synthesis of the ethylenimine by using amino alcohol as the raw material. Compared with a common catalyst which has the requirement on the temperature of over 400° C., the catalyst of the present invention obviously reduces the reaction temperature. The prepared catalyst can catalyze the intramolecular dehydration reaction of the amino alcohol and has relatively excellent selectivity. 1. A catalyst for synthesizing ethylenimine , characterized in that , the catalyst comprises a carrier and metal ions loaded on the carrier; the carrier is a composite oxide comprising titanium , silicon and phosphorus elements; the metal ions are magnesium ion , iron ion and cesium ion; the molar ratio of the magnesium ion to the iron ion to the cesium ion is (1-10):1:0.1; and the total mass of all the metal ions is 0.5%-10% of that of the carrier.2. The catalyst for synthesizing ethylenimine of claim 1 , characterized in that claim 1 , the catalyst is prepared by a method comprising:{'sub': 2', '2', '2', '5, '(1) mixing silicon oxide, titanium oxide, and an ammonium phosphate salt in an amount of the weight ratio of 5-20:80:15-5 in the oxides ...

INHIBITORS OF HEPATITIS C VIRUS

Compounds of formula I: 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein M is —O— or a direct bond.3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein X is —OC(O)— claim 1 , —O— claim 1 , or a direct bond.4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein G is —COH or —CONHSOZ.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein is T claim 1 , T claim 1 , or T.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein is T claim 1 , and wherein Tis optionally substituted with 1-4 Zgroups.11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein J is —O— or —N(R)—.12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein J is selected from —CH— claim 1 , —CF— claim 1 , or —C(O)—.13. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein J is selected from —CH— or —CF—.34. The compound of claim 14 , or a pharmaceutically acceptable salt thereof claim 14 , wherein E is E.42. The compound of claim 41 , or a pharmaceutically acceptable salt thereof claim 41 , wherein J is —CH.43. The compound of claim 41 , or a pharmaceutically acceptable salt thereof claim 41 , wherein L is C-Calkylene claim 41 , C-Ccarbocyclylalkylene or C-Calkenylene claim 41 , wherein L is optionally substituted with up to two halogen atoms.48. The compound of claim 41 , or a pharmaceutically acceptable salt thereof claim 41 , wherein each W is Cl claim 41 , F claim 41 , −OCH claim 41 , —OCHF claim 41 , —OCFor —CN.49. The compound of claim 41 , or a pharmaceutically acceptable salt thereof claim 41 , wherein Q is C-Calkyl claim 41 , or C-Ccarbocyclyl.51. The compound of claim 41 , or a pharmaceutically acceptable salt thereof claim 41 , wherein E is C-Calkyl substituted with one or more halogen ...

DIRECT STEREOSPECIFIC SYNTHESIS OF UNPROTECTED AZIRIDINES FROM OLEFINS

A method for the direct stereospecific conversion of structurally diverse mono-, di-, tri- and tetra-substituted olefins to N—H, N-alkyl, N-cycloalkyl, or N-aralkyl aziridines using a hydroxylamine amination agent with transition metal catalyst. The method is operationally simple (i.e., one-pot), scalable and fast at ambient temperature. 1. A process for making an aziridine , comprising: reacting an olefin with a hydroxylamine amination agent in the presence of a transition metal catalyst , wherein the aziridine product is an N—H , N-alkyl , N-cycloalkyl , or N-aralkyl aziridine.3. The process of claim 2 , wherein the hydroxylamine amination agent is of formula AA-1.4. The process of claim 2 , wherein the hydroxylamine amination agent is of formula AA-2.5. The process of claim 2 , wherein the hydroxylamine amination agent is of formula AA-3.6. The process of claim 2 , wherein the hydroxylamine amination agent is of formula AA-4.7. The process of claim 2 , wherein the hydroxylamine amination agent is of formula AA-5.8. The process of claim 2 , wherein the hydroxylamine amination agent is of formula AA-6.9. The process of claim 2 , wherein the hydroxylamine amination agent is of formula AA-7.10. The process of claim 2 , wherein the hydroxylamine amination agent is of formula AA-8.11. The process of claim 1 , wherein the transition metal catalyst is copper.12. The process of claim 1 , wherein the transition metal catalyst is rhodium.13. The process of claim 12 , wherein the catalyst is selected from:{'sub': 2', '4', '2', '4', '2', '2, 'Rh(OAc), Rh(octanoate), and Rh(esp).'}15. The process of claim 14 , wherein the olefin is of formula O-1.16. The process of claim 14 , wherein the olefin is of formula O-2.17. The process of claim 14 , wherein the olefin is of formula O-3.2034-. (canceled) This application claims the benefit of the filing date under 35 U.S.C. §119(e) of U.S. Provisional Patent Application No. 61/964,375 filed on Jan. 3, 2014, which is incorporated by ...

METHOD AND CATALYST FOR SYNTHESISING AZIRIDINE

The present invention relates to methods of synthesizing aziridines including isotopically labelled aziridines, said methods comprising contacting an imine or one or more precursors thereof with a diazo compound in the presence of a phosphoramide or a phosphoramide-derived catalyst. The present invention also relates to aziridines, modified aziridines and aziridine-derived compounds preparable by the aforementioned methods, and to phosphoramide or phosphoramide-derived catalysts suitable for use in such methods. 138-. (canceled)40. The method as claimed in claim 39 , wherein the imine (I) claim 39 , one or more precursors thereof claim 39 , and/or the diazo compound (II) are isotopically labelled such that the resultant aziridine (III) is also isotopically labelled.41. The method as claimed in claim 39 , wherein:(i) the method comprises contacting the imine (I) or the salt thereof with the diazo compound (II) or the salt thereof; or{'sub': '2', 'sup': 3', '1', '2, '(ii) the method comprises contacting the imine (I) or the salt thereof with the diazo compound (II) or the salt thereof, and wherein the method further comprises the step of synthesising the imine (I) or the salt thereof from an amine HNRor a salt or protected derivative thereof, and a carbonyl compound RCORor a salt or protected derivative thereof; or'}{'sub': '2', 'sup': 3', '1', '2, '(iii) the method comprises contacting the imine (I) or the salt thereof with the diazo compound (II) or the salt thereof, and wherein the method further comprises the step of synthesising the imine (I) or the salt thereof from an amine HNRor a salt or protected derivative thereof, and a carbonyl compound RCORor a salt or protected derivative thereof, wherein the imine (I) or the salt thereof is not isolated; or'}(iv) the method comprises contacting the precursors of the imine (I) with the diazo compound (II) or the salt thereof.42. The method as claimed in claim 39 , wherein R claim 39 , Rand Rare each independently ...

COMPOSITIONS AND METHODS FOR TREATMENT OF INFLAMMATORY DISEASES OF THE LUNG

Pharmaceutical compositions and methods are for treatment of an inflammatory disease of the lung caused by inhalation of a toxic agent or an irritant. In one example, chlorine inhalational lung injury can be treated using compounds useful in such compositions. 2. The compound of claim 1 , wherein Ris H claim 1 , —CO(C-C)alkyl claim 1 , —COO(C-C)alkyl claim 1 , or —CONH(C-C)alkyl.3. The compound of claim 1 , wherein Ris —OH claim 1 , or N(RR) claim 1 , wherein Rand Reach independently is H claim 1 , or (C-C)alkyl.4. The compound of claim 1 , wherein A is a 3 claim 1 , 4 claim 1 , 5 or 6 membered ring claim 1 , wherein each one of the carbon atoms in said ring may be substituted by oxo claim 1 , H claim 1 , halogen claim 1 , (C-C)alkyl claim 1 , NO claim 1 , N(RR) claim 1 , —OR claim 1 , —SR claim 1 , —SOR claim 1 , or —COR claim 1 , or two adjacent carbon atoms in said 3 claim 1 , 4 claim 1 , or 5 membered ring form a 3-6 membered saturated claim 1 , partially saturated claim 1 , or aromatic carbocyclic or heterocyclic ring claim 1 , or two adjacent carbon atoms in said 6 membered ring form a 3-6 membered saturated claim 1 , or partially saturated carbocyclic or heterocyclic ring; Rand Reach independently is H claim 1 , or (C-C)alkyl; and Ris OH claim 1 , NH claim 1 , or —O(C-C)alkyl.5. The compound of claim 4 , wherein A is a 3 claim 4 , 4 claim 4 , 5 or 6 membered ring claim 4 , wherein each one of the carbon atoms in said ring may be substituted by oxo claim 4 , H claim 4 , halogen claim 4 , methyl claim 4 , ethyl claim 4 , NO claim 4 , —NH claim 4 , OH claim 4 , —OCH claim 4 , —OCHCH claim 4 , —SH claim 4 , —SCH claim 4 , —SCHCH claim 4 , —SOH claim 4 , —SOCH claim 4 , —SOCHCH claim 4 , —COOH claim 4 , —COOCH claim 4 , —COOCHCH claim 4 , or —CONH claim 4 , or two adjacent carbon atoms in said 3 claim 4 , 4 or 5 membered ring form a 3-6 membered saturated claim 4 , partially saturated claim 4 , or aromatic carbocyclic or heterocyclic ring claim 4 , or two adjacent ...

Compliant hydrophilic coatings for medical devices

Example compliant hydrophilic coatings including a base coat and a lubricious top coat for coating a medical device including a flexible substrate. The coatings exhibit reduced cracking and peeling in response to deformation or expansion of the flexible substrate. Example techniques for coating a medical device including a flexible substrate with compliant hydrophilic coatings.

用于制备二肽基肽酶-iv抑制剂和中间体的改进方法

本发明涉及一种用于制备二肽基肽酶-IV抑制剂及中间体的改进方法。本发明通过采用低成本反应试剂能够降低制备成本，并通过提高产量而能够用于大量生产。

一种高纯度乙烯亚胺的制备方法

本发明涉及一种获得高纯度乙烯亚胺的方法，步骤如下：(1)向含有单乙醇胺和乙胺杂质的乙烯亚胺粗品中加入碱金属氢氧化物水溶液，在温度为10～30℃的条件下，搅拌均匀，得到混合液；(2)向混合液中加入芳磺酰氯，直至混合液里出现的沉淀不再溶解；(3)将混合液进行蒸馏，收集馏分，得到高纯度的乙烯亚胺产品。本发明方法利用伯胺、仲胺与芳磺酰氯反应现象上的巨大差异，实现了乙烯亚胺与杂质伯胺的高效分离，获得了含量大于99.9％的高纯度乙烯亚胺产品，且原料廉价易得、反应条件温和、操作过程简单。

Enhanced preparation method of dipeptidyl peptidase-Ⅳ inhibitor and intermediates thereof

본 발명은 디펩티딜 펩티다아제-Ⅳ 저해제 및 중간체의 개량된 제조방법에 관한 것으로, 본 발명에 따른 제조방법은 반응시 저가의 시약을 사용함으로써 제조 비용을 절감할 수 있으며, 수율 또한 향상되어 대량 생산에 유용하게 사용될 수 있다. The present invention relates to an improved method for preparing dipeptidyl peptidase-IV inhibitors and intermediates. The method according to the present invention can reduce production costs by using low-cost reagents during the reaction, and yields are also improved for mass production. It can be usefully used.

Optically active aziridine-2-carboxylate derivatives and a process for preparing them

아지리딘-2-카르복실산기와 멘톨기를 갖는 하기 구조식 (1) 화합물, 구조식(1)의 화합물을 제조하는 방법, 구조식(1)의 화합물을 광학 분할하여 광학적으로 활성인 형태의 아지리딘-2-카르복실산 유도체를 얻는 방법 및 상기 방법으로 제조한 광학적으로 활성인 형태의 아지리딘-2-카르복실산 유도체. Aziridine-2 in an optically active form by optically dividing the compound of formula (1), a compound of formula (1) having the aziridine-2-carboxylic acid group and a menthol group, and the compound of formula (1) A method for obtaining a carboxylic acid derivative and an aziridine-2-carboxylic acid derivative in an optically active form prepared by the method. 구조식 (1) Structural Formula (1) [이때, R 1 은 수소; 알킬; 시클로알킬; 4-클로로페닐; 4-메톡시페닐; s-트리아지닐 또는 피리디닐 아실; 벤질; 히드록시, 알콕시, 디알킬아미노, 페닐, 4-클로로페닐, 및 4-메톡시페닐로 이루어지는 군에서 선택된 치환기로 치환될 수 있는 탄화수소 잔기; 2,4-디메톡시페닐; 또는 (1R)-페닐에틸, (1S)-페닐에틸을 포함하는 치환된 페닐이다. 특히 바람직한 것으로는 (1R)-페닐에틸, (1S)-페닐에틸을 들 수 있다. 멘톨은 (+)-멘톨 또는 (-)-멘톨로 이루어진 군으로부터 선택된다] [Wherein R 1 is hydrogen; Alkyl; Cycloalkyl; 4-chlorophenyl; 4-methoxyphenyl; s-triazinyl or pyridinyl acyl; benzyl; Hydrocarbon residues which may be substituted with substituents selected from the group consisting of hydroxy, alkoxy, dialkylamino, phenyl, 4-chlorophenyl, and 4-methoxyphenyl; 2,4-dimethoxyphenyl; Or substituted phenyl comprising (1R) -phenylethyl, (1S) -phenylethyl. Particularly preferred examples thereof include (1R) -phenylethyl and (1S) -phenylethyl. Menthol is selected from the group consisting of (+)-menthol or (-)-menthol]

Method for synthesizing an n-unsubstituted or n-substituted aziridine

本发明涉及合成式(III)的N－未取代或N－取代氮丙啶的方法，其中在碘或溴存在下使式I的烯烃与氨或式R 5 NH 2 的伯胺反应，其中R 1 －R 5 彼此独立代表氢，具有1－16个碳原子的直链或支链烷基，具有1－4个碳原子的羟基烷基，具有5－7个碳原子的环烷基，可在苯基的邻位、间位或对位被甲氧基、羟基、氯或具有1－4个碳原子的烷基取代的苄基和苯基，基团R 1 和R 2 与基团R 3 和R 4 可为闭合的5－12元环。

Novel process and catalyst

A method of synthesising aziridines of formula (III) or a salt thereof including isotopically labelled aziridines, the method comprising contacting an imine (I), or one or more precursors thereof, with a diazo compound (II) or a salt thereof in the presence of a phosphoramide or a phosphoramide-derived catalyst of formulae (IV) or (V): wherein R1-R9 are any atom or group; and X is O, S or NR9. Preferred diazo compounds include tert-butyl diazoacetate, deuterated tert-butyl diazoacetate, deuterated allyl diazoacetate and ethyl diazoacetate. Preferred catalysts are chiral 1,1-bi-2-naphthol (BINOL) based phosphoramides with (S)-3,3-bis(9-anthracenyl)-[1,1]-binaphthalen-2,2-yl-N-triflyl-phosphoramide being particularly preferred. Certain phosphoramide or phosphoramide-derived catalysts of formulae (IV) and (V) are also claimed.

Catalytic process for the production of aziridines

Preparation method of ((2S)-2-aziridinyl) benzhydrol

本发明公开了一种（（2S）-2-氮丙啶基）二苯基甲醇的制备方法，以2-三苯基甲胺基-3-羟基丙酸甲酯为原料，初始原料与三乙胺和甲基磺酰氯反应，得到中间产物2-（（2S）-N-三苯甲基-2-氮丙啶基）乙酸甲酯，该中间产物与格氏试剂作用生成N-三苯甲基氮丙啶基二苯基甲醇，N-三苯甲基氮丙啶基二苯基甲醇经酸性水解，生成目标产物（（2S）-2-氮丙啶基）二苯基甲醇。本发明合成步骤简短，合成方法简单，反应条件易实现，适合工业化生产，合成出的（（2S）-2-氮丙啶基）二苯基甲醇催化效果好，值得推广。

Improved method of producing dipeptidyl peptidase-iv inhibitor and intermediate compound

FIELD: chemistry. SUBSTANCE: invention relates to an improved method of producing protected (R)-3-amino-4-(2,4,5-trifluorophenyl)butanoic acid of formula 2, as shown on dwg 1, and a dipeptidyl peptidase-IV inhibitor intermediate compound. The method involves: (step a) obtaining a compound of formula 6 by opening the epoxide ring in compound 5, using Grignard reagent; (step b) obtaining a compound of formula 7 by reacting the compound of formula 6 with sodium azide; (step c) obtaining a compound of formula 8 by reacting the compound of formula 7 with triphenyl phosphine and adding an amine protective group (PG); (step d) obtaining a compound of formula 9 by opening the aziridine ring in compound 8 using a cyanogens-based reagent; and (step e) obtaining a compound of formula 2 by hydrolysis of the compound of formula 9 using a base; [Reaction scheme 1] , where X denotes a halogen and PG denotes a protective group. Novel intermediate compounds are described. EFFECT: improved method. 12 cl, 3 dwg, 4 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 499 792 (13) C2 (51) МПК C07D C07D C07D C07C C07C 203/16 (2006.01) 203/24 (2006.01) 241/08 (2006.01) 213/02 (2006.01) 219/18 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2011141208/04, 30.03.2010 (24) Дата начала отсчета срока действия патента: 30.03.2010 (43) Дата публикации заявки: 10.05.2013 Бюл. № 13 2 4 9 9 7 9 2 R U (85) Дата начала рассмотрения заявки PCT на национальной фазе: 31.10.2011 C 2 C 2 (56) Список документов, цитированных в отчете о поиске: WO 2006/098342 A1, 21.09.2006. KR 20080094604, 23.10.2008. Bioorganic & Medicinal Chemistry Letters, (2007), 17(1), 49-52. Bulletin of the Korean Chemical Society (2008), 29(11), 2129-2134. US 2008-0280913 A1, 13.11.2008. EA 007434 B1, 27.10.2006. (86) Заявка PCT: KR 2010/001947 (30.03.2010) (87) Публикация заявки РСТ: WO 2010/114291 (07.10.2010) Адрес для переписки: 191036, Санкт-Петербург, а/я 24, "НЕВИНПАТ" (54 ...

CONTROLLED RELEASE REGULAR PEPTIDES MICROCAPSULES, PRODUCTION METHOD AND INJECTION PREPARATIONS

The method of obtaining 2-aminobutanol

compound

[과제] 파장 400nm 부근의 장파 자외선∼근자외선 영역에 대한 높은 흡수 선택성을 가지며, 또한 내후성이 높은, 메로시아닌 골격을 가지는 신규 화합물을 제공한다. 또한, 본 발명의 화합물을 포함하는 조성물로부터 형성된 층은, 조성물에 대한 첨가량을 늘린 경우라 하더라도 화합물이 블리딩되는 일 없이, 상기 영역의 광흡수성이 우수한 박막층을 제공할 수 있다. [해결 수단] 중합성기와 하기 식 (X)로 나타내어지는 부분 구조를 가지는 화합물. [식 (X) 중, 고리 W 1 은, 고리의 구성 요소로서 이중 결합을 가지고, 또한 방향족성을 가지지 않는 고리 구조를 나타내며, 고리 W 1 은 치환기를 가지고 있어도 된다. R 3 은, 1가의 치환기를 나타낸다.]

Organic compound and electroluminescent device comprising the same

본 발명은 유기발광소자에 구비되는 광효율 개선층에 채용되어 소자의 저전압 구동과 우수한 색순도, 발광 효율 등의 발광 특성을 구현할 수 있는 하기 [화학식 Ⅰ]로 표시되는 화합물 및 이를 포함하는 유기발광소자에 관한 것이다. [화학식 Ⅰ] The present invention is a compound represented by the following [Formula I] which is employed in a light efficiency improvement layer provided in an organic light emitting device to realize light emitting characteristics such as low voltage driving, excellent color purity, and luminous efficiency of the device, and an organic light emitting device comprising the same it's about [Formula Ⅰ]

Process for preparing iso-serine and its derivatives from aziridine-2-carboxylates

본 발명은 아지리딘-2-카르복시산 에스테르를 아실 할라이드와 반응시켜 β-아미노-α-히드록시산 에스테르의 작용기를 가지는 중간체를 제조하고 이들로부터 이소세린 및 이소세린올을 제조하는 방법에 관한 것이다. The present invention relates to a process for reacting aziridine-2-carboxylic acid esters with acyl halides to prepare intermediates having functional groups of β-amino-α-hydroxy acid esters and to prepare isocerin and isoselinol from them. 본 발명은 상기 구조식 (1)의 아지리딘-2-카르복시산 에스테르를 알킬, 아릴 클로로포메이트, 보다 바람직하게는 메틸, 에틸, 또는 벤질클로로포메이트와 반응시켜 구조식 (2)의 화합물을 제조하거나 또는 아세틸클로라이드와 반응시켜 구조식(3)의 화합물을 제조한 후, 이들의 작용기 변환을 통해 구조식 (4)의 이소세린 및 구조식 (5)의 이소세린올을 제조하는 방법에 관한 것이다. 이때 구조식 (1), (2) 및 (3)의 R 1 은 (R)-페닐에틸, 또는 (S)-페닐에틸이고, R 2 는 에틸 또는 멘톨일을 포함한다. The present invention provides a compound of formula (2) by reacting the aziridine-2-carboxylic acid ester of formula (1) with alkyl, aryl chloroformate, more preferably methyl, ethyl, or benzylchloroformate, or After reacting with acetyl chloride to prepare a compound of formula (3), and through the functional group conversion of the isoserine of formula (4) and isoselinol of formula (5). Wherein R 1 in the formulas (1), (2) and (3) is (R) -phenylethyl, or (S) -phenylethyl, and R 2 comprises ethyl or mentholyl.

Oxylan, aziridine or cyclopropane production method

본발명은 (i) 알킬금속을 식 CHR 3 X'X" 의 메탄 유도체 (식중 R 3 은 수소, 알킬, 아릴, 헤테로방항족, CO 2 R 8 , R 8 3 Sn, CONR 8 R 9 또는 트리메틸실릴이며, X' 및 X" 는 각각 독립적으로 이탈 그룹임) 와 반응시킴으로써 얻을 수 있는 금속탄소 (metallocarbon) 와, 또는 (ii) 하기 식 (III) 의 화합물을 적당한 유기금속 시약 또는 무기 시약과 반응시킴으로써 얻을 수 있는 금속탄소와, 하기 식 (II) 화합물 및 식 SR 6 R 7 의 설파이드 (식중, R 6 및 R 7 은 각각 독립적으로 알킬, 아릴 또는 헤테로방향족이거나, R 6 과 R 7 이 서로 결합하여 임의로 추가의 헤테로원자를 포함하는 싸이클로알킬 링을 형성함) 혼합물을 반응시킴으로써 하기 식 (I) 의 옥시란, 아지리딘 또는 싸이클로프로판을 제조하는 방법에 관한다. [식중, R 1 , R 2 및 X 는 상기에서 정의한 바와 같음. [식중, R 3 은 수소가 아님.

Stabilised compositions containing polyfunctional aziridine compounds as hardening constituents

本发明涉及含有至少一种多官能氮丙啶化合物和1，4-二氮杂二环[2.2.2]辛烷的组合物及其制备方法。本发明还涉及该组合物用作皮革处理领域、涂料领域、织物印花领域和表面涂料领域中配制物的固化组分的用途。

Kynurenin-3-monooxygenase inhibitor, pharmaceutical composition thereof, and method of use thereof

For the preparation of improving one's methods of the intermediate of dipeptidyl peptidase-iv inhibitor

本发明涉及一种用于制备二肽基肽酶-IV抑制剂的中间体的改进方法。本发明通过采用低成本反应试剂能够降低制备成本，并通过提高产量而能够用于大量生产。

Fungicidic agent

1524599 Dressing seeds CIBA-GEIGY AG 29 Sept 1976 [30 Sept 1975 (2)] 40477/76 Heading A2Q [Also in Divisions C2 and C3] Seeds are dressed with compounds of the formula: wherein R 1 is halogen or (C 1 -C 4 ) alkyl or alkoxy, R 2 is H, halogen. (C 1 -C 3 ) alkyl or (C 1 -C 4 ) alkoxy, R 3 is H, halogen or (C 1 -C 3 ) alkyl, R 4 is H or CH 3 ; with the proviso that the total number of C atoms in R 1 , R 2 , R 3 and R 4 does not exceed 8. X is -CH 2 - or CH 3 | -CH-, R 5 is -COOR', -COSR' or R" | -CON-R"' wherein each of R', R" and R"' independently represents CH 3 or C 2 H 5 , R 6 is H or is R 7 , R 7 is (C 1 -C 6 ) alkyl which may be substituted by CN, OH or (C 1 -C 3 ) alkoxy, (C 3 -C 6 ) alkenyl which may be substituted by halogen, (C 3 -C 6 ) alkynyl or (C 3 -C 7 ) cycloalkyl, or R 6 and R together represent a (C 2 -C 6 ) alkylene or alkenylene which may be substituted by halogen or (C 1 -C 3 ) alkyl and may contain one or two heteroatoms; and salts thereof with inorganic or organic acids; to protect them from fungal attack.

Synthetic method of 2H-azapropene derivative

本发明公开了一种合成2H‑氮杂丙烯啶衍生物的新方法。向Schlenk封管反应器中，依次加入式I所示的炔类化合物，式II所示的磺酸钠盐，再加入亚硝酸叔丁酯(t‑BuONO)和有机溶剂，在惰性气氛保护条件下，油浴加热搅拌反应，通过TLC或GC‑MS监测反应完成后，经后处理得式III所示的2H‑氮杂丙烯啶衍生物。该方法具有原料来源易得、工艺路线简单、反应条件温和、工艺成本低、底物适应范围广、收率高的优点。

Method of obtaining n-haloidketimines

Method for producing aziridines

Method of obtaining n-substituted derivatives of 2-cyanethyleneimine

СПОСОБ ПОЛУЧЕНИЯ N-ЗАМЕЩЕННЫХ ПРОИЗВОДНЫХ 2-ЦИАНАЗЙРИДИНОВ общей формулы -CN R 47 N R где RI водород или метилу R неразветвленный или разветвленньй С -С..-алкил, аллил, 2-метилмеркаптобензил7 3,4-диметоксибензил5 4-ме- тилбензил, 3-этоксикарбоншт-2-метилбензил , 4 гидроксибензил , трифторметилбензил , 2-хло 1 ензил, 5-ме тил-2-нитробензил, циклопропил , 2-метоксиэтил, 2,2-диметоксиэтил , феноксиэтил , 2-гидроксиэтил, 2,2-дкхлорэтил , 2-хлорэтил, циклогекс-1-эннлметил, 2-тенил 2-фурилметил, 2-ме .тилаллил,. 1-адамантил, фенил, Су-С -алкоксикарбонилэтшт , С -Cj -алкоксикарбонилметил , тетрагидропиран-4-ил , 5-метоксикарбонил-2-тенил , 5-метоксикарбонил-2-фурфурил , 2-бутенил, 5-метилпиримидин-4-ил-метил, 2-гидрокси-6-метилпиридин- -З-ил, метил-1,6-диметил-2-оксопиридин-З-ил , метил- -2-метокси 6-метилпиридин- 3-ил, метил-2,5-диметилпиридин-4-ил , метил-4-метил- С тиазол-2-ил-метил, 2-проп-инилтетрагидрофурфурил , /Л 3-метил-меркаптопропил, 2- j, -метилсульфонилэтил, цинна Сшш мил, 3-бутИНИЛ, 2-НОрборНШ1, ;:; пиримидин-2-ил-метил, 5-карбокси-2-тенил или 5-карбокси-2-фурфурил , отличающийс  тем, что 4 .оединение общей формулы сл со го HQh RI-CH-C-CN ч1 Hall L где R, - имеет указанные значени ; Hat и Halj - хлор или бром; L - водород или вместе с Hat имеют валентную св зь подвергают взаимодействию с амином общей формулы 1 имеет указанные значени , и образовавшее- METHOD FOR OBTAINING N-SUBSTITUTED 2-CYANASYRIDINES DERIVATIVES of the general formula -CN R 47 NR where RI is hydrogen or methyl R is unbranched or branched C -C ..- alkyl, allyl, 2-methylmercaptobenzyl7 3,4-dimethoxybenzyl5 4-m-allyl, 2-methylmercaptobenzyl7 3,4-dimethoxybenzyl 5 4-m -ethoxycarbonate-2-methylbenzyl, 4 hydroxybenzyl, trifluoromethylbenzyl, 2-chloro 1 enyl, 5-methyl-2-nitrobenzyl, cyclopropyl, 2-methoxyethyl, 2,2-dimethoxyethyl, phenoxyethyl, 2-hydroxyethyl, 2,2-dhloroethyl , 2-chloroethyl, cyclohex-1-ennemethyl, 2-tenyl 2-furylmethyl, 2-me. Ethylallyl ,. 1-adamantyl, phenyl, Su-C- ...

Use of bifunctional ethyleneimine compounds in the manufacture of dental models and tooth replacement parts

Catalyst for vapor-phase intermolecular dehydration reaction of alkanolamines

Improved method for preparing dipeptidyl peptidase-iv inhibitor and intermediate

本发明涉及一种用于制备二肽基肽酶-IV抑制剂及中间体的改进方法。本发明通过采用低成本反应试剂能够降低制备成本，并通过提高产量而能够用于大量生产。

A kind of catalyst for the synthesis of Ethylenimine, preparation method and application

本发明涉及用于合成乙撑亚胺的催化剂、制备方法及应用。所涉及的催化剂包括载体和负载在载体上的金属离子，所述载体为含钛、硅和磷元素的复合氧化物；所述金属离子为镁离子、铁离子和铯离子，且镁离子、铁离子、铯离子的摩尔比为：1～10:1:0.1，所有金属离子的质量为载体质量的0.5%～10%。所涉及的制备方法是将催化剂前驱体在350℃～650℃下，焙烧制得催化剂，所述催化剂前驱体为载体、镁的可溶性盐、铁的可溶性盐与铯的可溶性盐的混合物。本发明还提供了上述催化剂用于以氨基醇为原料合成乙撑亚胺中的应用。本发明的催化剂，与一般要求温度高于400℃相比降低显著降低了反应温度。制得的催化剂能够催化氨基醇分子内脱水反应，并具有较优的选择性。

Novel quinolinedione derivatives, process for preparing thereof and pharmaceutical compositions containing them

본 발명은 우수한 항암활성을 갖는 퀴놀린디온 유도체, 이의 제조방법 및 이를 포함하는 약학적 조성물에 관한 것으로, 구체적으로 하기 화학식 1로 표시되는 퀴놀린디온 유도체는 DNA에 킬레이트화제 (Intercalator agents), 알킬화제 (Alkylating agents) 및 DNA 절단제 (Cutting agents)로 작용하여 우수한 항암 효과를 나타낼 뿐만 아니라 독성이 낮아 암 질환의 치료제 및 예방제로 유용하게 사용될 수 있다. 상기 식에서, R 1 , R 2 , R 3 , R 4 및 R 5 는 명세서 내에 기재된 바와 같다.

New ethyl arizidine derivatives and their preparation methods

본 발명은 하기 일반식(I)로 표시되는 신규의 에틸 아지리딘 유도체 및 그 제조방법에 관한 것이다. The present invention relates to a novel ethyl aziridine derivative represented by the following general formula (I) and a preparation method thereof. (I) (I) 상기식에서, R 1 과 R 2 는 각각 H, 알킬, 알릴, 알알킬 및 헤테로 원자 중에서 선택되고, 헤테로 원자는 알킬, 알릴 또는 알알킬에 연결되어있다. R 3 는 H, 알킬, 알릴, 알알킬 및 아미노 보호기 중에서 선택되고, 아미노 보호기의 질소원자는 탄소 수 5-7개의 단 고리 헤테로 고리 또는 7-11개의 두 고리 헤테로 고리로 구성된다. X와 Y는 각각 H, C 1 ~C 4 의 저급 알킬, 알알킬, 알릴 또는 헤테로 원자 중에서 선택되고, 헤테로 원자는 알킬, 알릴 또는 알알킬에 연결되어있다. R 4 는 같거나 다른 알킬 치환기를 갖는 실일기 및 알코올 보호기에서 선택되고, 알코올 보호기는 알콕시카르보닐, 아릴옥시카르보닐, 메톡시메틸, 테트라히드로퓨란, 메틸에톡시메틸, 또는 에톡시비닐에틸이다. Z는 F, Cl, Br, I,-OR 5 에서 선택된다. R 5 는 SOnR 6 이며, n = 0,1,2로 정의되고, R 6 는 알킬 또는 알릴기 중에서 선택된다. Wherein R 1 and R 2 are each selected from H, alkyl, allyl, alalkyl and hetero atoms, and the hetero atoms are linked to alkyl, allyl or alalkyl. R 3 is selected from H, alkyl, allyl, alalkyl and amino protecting groups, wherein the nitrogen atom of the amino protecting group consists of 5-7 monocyclic hetero rings or 7-11 two ring hetero rings. X and Y are each selected from H, C 1 to C 4 lower alkyl, alalkyl, allyl or hetero atoms, and the hetero atoms are linked to alkyl, allyl or alalkyl. R 4 is selected from silyl and alcohol protecting groups having the same or different alkyl substituents, and the alcohol protecting group is alkoxycarbonyl, aryloxycarbonyl, methoxymethyl, tetrahydrofuran, methylethoxymethyl, or ethoxyvinylethyl . Z is selected from F, Cl, Br, I, -OR 5 . R 5 is SOnR 6 , defined as n = 0,1,2, and R 6 is selected from alkyl or allyl groups.

Production of dental models and tooth replacement parts

Novel bromine-containing compounds of the formula ##STR1## in which R is an alkylidene radical having 1 to 6 carbon atoms, a cycloalkylidene radical or a SO 2 radical, R' is an alkylene radical having 2 to 6 carbon atoms or a cycloalkylene radical and Y is an acyl radical of a carboxylic acid having 2 to 6 carbon atoms and optionally bearing an aromatic substituent, and x is 1 or 2 and y is 0, 1 or 2, which are particularly useful for the preparation of dental replacement parts and dental models when mixed with a substance that catalyzes the polymerization of the compounds.

Patent DE3324917C2

Improvement in the preparation processes of aziridines

Pharmaceutical composition possessing antitumor activity

PHARMACEUTICAL COMPOSITION POSSESSING ANTITUMOR ACTIVITY ABSTRACT The pharmaceutical composition possessing antitumor activity which consists of a therapeutically efficaceous quantity of 1-H-2-aziridine-carbonic acid derivative having the formula

Preparation of 1-4 3-substituted thiamorpholines

Process for obtaining secondary n-aryl-beta-haloalkylamines

DERIVATIVES 1- (N-ACYLCARBAMOYL) 2-CYANO-AZIRIDINES HAVING A CANCEROSTATIC AND IMMUNOSTIMULATING ACTION AND PROCESS FOR THEIR PREPARATION

L'invention est relative à la 1-(N-acyl-carbamoyl) 2-cyano-aziridine répondant à la formule générale: The invention relates to 1- (N-acyl-carbamoyl) 2-cyano-aziridine corresponding to the general formula:

NOVEL N-SUBSTITUTED DERIVATIVES OF AZIRIDINYL 2-CARBOXYLIC ACID WITH IMMUNOSTIMULANT ACTIVITY, PROCESS FOR THEIR PREPARATION AND THERAPEUTIC APPLICATIONS

L'invention est relative à des dérivés de l'acide aziridinyl 2-carboxylique substitués sur l'atome d'azote du noyau de formule : The invention relates to derivatives of aziridinyl 2-carboxylic acid substituted on the nitrogen atom of the nucleus of formula:

Esters of aziridino-carboxylic acids and their preparation

Process for preparing nu-substituted ethylene-imine-carboxylic acid esters and products conforming to those thus obtained

Patent FR2445316B1

Process for the production of esters of carboxylic acids

NOVEL N-SUBSTITUTED DERIVATIVES OF AZIRIDINYL 2-CARBOXYLIC ACID WITH IMMUNOSTIMULANT ACTIVITY, PROCESS FOR THEIR PREPARATION AND THERAPEUTIC APPLICATIONS

L'invention est relative à des dérivés de l'acide aziridinyl 2-carboxylique substitués sur l'atome d'azote du noyau, de formule : The invention relates to aziridinyl 2-carboxylic acid derivatives substituted on the nitrogen atom of the nucleus, of formula:

Novel cephalotaxane derivatives with a side chain

Asymmetric hemisynthesis of novel harringtonines and their analogues, cephalotaxus alkaloids useful in chemotherapy, especially for treating haematosarcomas, involves direct esterification of a natural cephalotaxine with an acylating compound.- DETAILED DESCRIPTION - The preparation of sidechain-bearing cephalotaxane of formula Omega -CO-O-CTX or a salt comprises reacting either a carboxylic acid of formula Omega -CO-OH or a salt, or an activated form of an acid of formula Omega -CO-A or a salt, with either a hydroxyl group bearing cephalotaxine or a salt of formula HOCTX, or a metallic alkoxide of formula MOCTX, or an activated form of its hydroxyl group of formula YOCTX, with the possible presence of one or more reaction additives. Omega = representative radical of the chain terminal moiety; - CO = carbonyl of the ester group bonded to cephalotaxane; Omega CO = substituted heterocycloalkane (I) or group (II) or (III).- n,m = 0-8; - Z = O, N or S; - R5, R6, R7 = H, hydrocarbon (saturated or unsaturated, linear or branched, or cyclic, optionally with heteroatoms, and especially alkyl, alkenyl, alkynyl, cyaloalkyl, cycloalkenyl, aryl, heterocycloalkyl), or O ether bearing one of the above radicals; R6 and R8 may be included in a cycle; - Q2 = C, Si or P; - R9, R10 = H, alkoxy, hydrocarbon (as above); or R9 and R10 are absent, or together = heteroatom with a multiple bond with Q1; or R9 and R11 are absent, giving a multiple bond between the two C atoms bearing them; and - R11 = H, arylcarbonyl, alkoxycarbonyl, aryloxycarbonyl or alkylcarbonyl; - OCTX = cepahlotaxine moiety of formula (IV); - p = 1-2; - A = cyclic anhydride (V) or a halide; - Y = leaving group to allow a negative charge on the O atom by cleavage between Y- and -OCTX.- INDEPENDENT CLAIMS include claims for the following compounds, in racemic or enantiomeric forms: - (1) metal alkoxides of cephalotaxine (X), where M = Li or Na; - (2) a sidechain-bearing cephalotaxane Omega COOCTX and/or a salt, where ...

PR

L'invention concerne les produits médicamenteux. La préparation faisant l'objet de l'invention est du type à base dune substance active constituée par un dérivé de l'aziridine, et est caractérisée en ce qu'elle contient en qualité de substance active un dérivé de l'acide 1-H-2-aziridine-carboxylique de formule générale : The invention relates to medicinal products. The preparation forming the subject of the invention is of the type based on an active substance consisting of a derivative of aziridine, and is characterized in that it contains as active substance a derivative of 1-H acid. -2-aziridine-carboxylic of general formula:

Aminomethyl-aziridines (or aminomethyl-ethylene-imines), their preparation and their applications

Process for the preparation of lubricant additives and lubricants

Post-curable pressure sensitive adhesive

Process for the preparation of reaction products of cyanogen azide and aliphatically saturated organic compounds and products obtained

The catalyst of alkanolamine vapour phase molecule inner dewatering reaction

一种可使链烷醇胺(通式I)汽相分子内脱水反应转化为环胺(通式II)的催化剂(通式III)。 通式I和II中R和R′各可以是氢、甲基和乙基，n是2到5的整数。通式III是一种复合氧化物，其中X是第IIIA族元素、IVA族元素、VA族元素、I到VIII族的过渡金属元素、镧系元素和锕系元素中的一种元素，O是氧，P是磷，Y至少是碱金属元素和碱土金属元素中的一种元素，下标a、b、c、d分别是X、P、Y和O的原子比。

Process for producing immunostimulating n-substituted-aziridine-2-carboxylic acid derivatives

Method for the preparation of 2,3-dimethyl aziridine

THIS INVENTION INVOLVES THE SYNTHESIS OF 2,3-DIMETHYL AZIRIDINE IN BOTH ITS CIS AND TRANS ISOMERIC FORMS. SYNTHESIS IS EFFECTED BY TREATING THE APPROPRIATE ISOMERIC FORM OF 2-BUTENE. TREATMENT IS CARRIED OUT BY A FOUR STEP PROCESS RESULTING IN THE FORMATION OF THE CORRESPONDING CIS-2,3DIMETHYL AZIRIDINE COMPOUND OR THE TRANS-2,3-DIMETHYL AZIRIDINE COMPOUND. IN THE FIRST STEP OF THE PROCESS, 2-BUTENE IS EPOXIDIZED WITH PERACETIC ACID. THE RESULTING EPOXIDE IS THEN CONVERTED TO AN AMINO ALCOHOL BY TREATMENT WITH AMMONIA. IN THE THIRD STEP, AN INNER SALT IS FORMED BY REACTING THE AMINO ALCOHOL WITH CHLOROSULFONIC ACID. FINALLY, THE INNER SALT IS TREATED WITH SODIUM HYDROXIDE TO PRODUCE THE AZIRIDINE COMPOUND OF THIS INVENTION.

ANALOGY PROCEDURE FOR THE PREPARATION OF N-SUBSTITUTED 2-CYANAZIRIDINES

Novel aryl ethane derivative and pharmaceutical composition containing same as active ingredient

The present invention relates to an aryl ethene derivative, for inhibiting an estrogen-related receptor gamma (ERR³) activity, a prodrug of same, a solvate of same, a stereoisomer of same or pharmaceutically acceptable salts of same, and a pharmaceutical composition containing same as an active ingredient.

Aziridines - by reacting ammonia and vicinal dihaloalkanes in presenc of alk metal hydroxide acid acceptor

A process for the prodn of azidirines (I), by reacting NH3 with a vicinal dihaloalkane (II) in the presence of an alkali metal hydroxide acid acceptor, added incrementally to he reacting mixture in an amount sufficient to substantially neutralise the hydrogen halide formed during the reaction, but insufficient to cause substantial dehydrohalogenation of (II). The intermittent or continuous addition of alkali metal hydroxide in the required quantity results in increased yields of (I).

Synthesis method of 1, 1-dibromo-2, 2-bis (chloromethyl) cyclopropane

本发明公开了1,1‑二溴‑2,2‑双(氯甲基)环丙烷的合成方法，包括以下步骤：2‑氨基‑2‑羟基甲基丙烷‑1,3‑二醇和二氯亚砜进行氯取代反应得到(1,3‑二氯‑2‑(氯甲基)丙烷‑2‑基)氨基砜酮；(1,3‑二氯‑2‑(氯甲基)丙烷‑2‑基)氨基砜酮通过浓硫酸水溶液进行水解得到1,3‑二氯‑2‑氯甲基丙‑2‑胺硫酸盐；1,3‑二氯‑2‑氯甲基丙‑2‑胺硫酸盐在碱性条件下进行解盐，并关环得到2,2‑双(氯甲基)氮杂环丙烷；2,2‑双(氯甲基)氮杂环丙烷与亚硝酸钠反应得到3‑氯‑2‑氯甲基丙‑1‑烯；3‑氯‑2‑氯甲基丙‑1‑烯与三溴甲烷在碱性条件下反应生成1,1‑二溴‑2,2‑双(氯甲基)环丙烷。本发明制备方法简单，可进行放大生产。

Cephalotaxane derivatives and process for their preparation

The present invention concerns a new general process for asymetric hemisynthesis of harringtonines and their analogs, that are alcaloids used in chimiotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constituted of a side chain precursor which backbone and fonctionalization are entirely preformed.

Microbicidal compositions

Abstract of the Disclosure Amino aceto anilides of the formula I shown hereinafter are effective microbicides. They may be used to control fungi on plants or parts of plants or to prevent them from fungi attack.

Method for preparing 2h-azirine carboxylic esters

The invention relates to a method for preparing 2H-azirine carboxylic esters. More specifically, the invention relates to a method for preparing 2H-azirine carboxylic esters starting from α-diazo-β-keto oxime ethers in the presence of a rhodium (II)-based catalyst.

Improved method for preparing dipeptidyl peptidase-iv inhibitor and intermediate

The present invention relates to an improved method for preparing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention is able to reduce preparation costs by using low cost reagents on reaction and is able to be used in mass production by improving yield.

improved method for preparing dipeptidyl dipeptidase-iv inhibitor and intermediate

Aziridine derivatives

1423360 Anorectic compositions JOHN WYETH & BRO Ltd 10 Dec 1973 [21 Dec 1972] 59139/72 Heading A5B [Also in Division C2] Pharmaceutical compositions having anorectic activity comprise, as active ingredient, an aziridine of the general formula: or a pharmaceutically acceptable acid addition salt thereof, wherein Ar is a phenyl group optionally substituted by one or more hydroxy, halo, C 1-6 alkyl, C 1-6 alkoxy, halo-C 1-6 alkyl, nitro, amino or mono- or di-C 1-6 alkylamnio radicals, R is hydrogen, C 1-6 alkyl, aryl-C 1-6 alkyl or acyl and R' is C 1-6 alkyl, with the proviso that when Ar is phenyl and R' is methyl then R is C 1-6 alkyl or aryl-C 1-6 alkyl, in association with a pharmaceutical carrier, and may be administered in the form of powders, tablets, capsules, solutions, suspensions, emulsions, syrups and elixirs.

Process for producing aziridine-2-carboxylic acid or its salts

Title of the Invention CARBOXYLIC ACID OR ITS SALTS Abstract of the Disclosure A process for producing aziridine-2-carboxylic acid or its salts is provided which comprises treating an alpha-halogeno-beta-aminopropionitrile or its mineral acid salt with an alkali or alkaline earth metal hydroxide in water or in a water-containing organic solvent. In a preferred embodiment, aziridine-2-carboxylic acid or its salt is produced by treating the reaction mixture containing an alpha-halogeno-beta-aminopropionitrile obtained by reacting an alpha,beta-dihalogenopropionitrile or an alpha- halogenoacrylonitrile with ammonia, with an alkali or alkaline earth metal hydroxide in the presence of water without isolating the alpha-halogeno-beta-aminopropionitrile from the reaction mixture beforehand.

Process for producing solutions of aziridine-2-carboxylic acid salt

Process for regenerating a catalyst for the production of aziridine compounds.

Improved method for preparing dipeptidyl peptidase-IV inhibitor and intermediate

The present invention relates to an improved method for preparing dipeptidyl peptidase-IV inhibitor which is able to reduce preparations costs by using low cost reagents in the reaction steps and is able to be used in mass production by improving yield.

Synthesis of ethyleneimine dimer

The invention provides a method to synthesizing ethyleneimine dimer. This method of synthesis provides several advantages over previous methods: (1) the starting compounds are all relatively inexpensive, (2) the yield of product is greater than 20 % of the theoretical yield; and (3) the steps of synthesis are easy, inexpensive and amenable to large-scale production. All of these advantages allow for less expensive production of ethyleneimine dimer.

New Cephalotaxan Derivatives and Methods for Preparing Them