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MONOESTER MONOCHLORIDES OF 2-CHLOROMALONIC ACID (Wed, 16 Mar 1977)
1467687 Monoester monochlorides of chloromalonic acids UCB 25 Nov 1975 [25 Nov 1974] 50869/74 Heading C2C Novel monoester monochlorides of 2-chloromalonic acid of the general formula wherein R is benzyl or C 1-5 straight or branched alkyl, are prepared by reacting a compound of general formula where Z is H or an alkali metal, with (COCl) 2 when Z is alkali metal and with an -chlorenamine of formula in which X, X1, Y and Y1, same or different, are each alkyl, aryl, alkaryl or aralkyl or Y and Y1 together with the N atom to which they are attached form a heterocyclic radical which is optionally substituted, when Z is H. Alternatively those esters other than where R = t-butyl are obtained by reacting N 2 = CH-COOR with COCl 2 in organic solution to give the corresponding product and then treating with HCl. In the examples the methyl, ethyl, t-butyl and benzyl derivatives are prepared. 3 - Chloro - 2 - oxo - 1,4 - diphenyl - azetidine- 3-carboxylate (I) is obtained from ethyl 2-chloromalonate acid chloride and benzaniline. The 1,4,4-diphenyl derivative is similarly prepared using N-(diphenylmethylene) aniline instead of benzaniline. 6 - Chloro - 3,3 - dimethyl - 7 - oxo - 4 - thia - 1- azabicyclo[3,2,0]heptane- 2,6 - dicarboxylate (II) is prepared from methyl 2-chloromalonate acid chloride and 5,5-dimethyl-4-methoxycarbonyl- #2-thiazoline. 7 - Chloro - 7 - methoxycarbonyl - [3,2,0] bicyclohepten-6-one (III) is obtained from methyl- 2-chloromalonate acid chloride and cyclopentadiene. Methyl - 5 - methoxycarbonyl - - chloro - 2- cyclopentene - 1 - acetate is prepared by treating product (III) above with methanol.
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2-hydroxy-3-[1-(1H-imidazol-4-yl)alkyl]-benzenecarboximidamides (Tue, 26 Sep 1995)
These are substituted 2-hydroxy-3-[1-(1H-imidazol-4-yl)-alkyl]benzenecarboximidamide derivatives of the formula wherein R1 represents a hydrogen atom or C1-4 alkyl, R2 represents a hydrogen atom, a hydroxyl group, an amino group or a C1-4 alkyl, and R3 is a hydrogen atom, or R2 and R3 taken together represent an ethylene group; and non-toxic ophthalmologically acceptable acid addition salts thereof. Such derivatives are reported to be useful in lowering intraocular pressure.
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2-oxo-1-pyrrolidine derivatives, process for preparing them and their uses (Fri, 19 Dec 2003)
Patent 520493 A compound of formula (A), where: X is ���CONR5R6, ���COOR7, -CO-R8 or CN; R1 is H, alkyl, aryl, heterocycloalkyl, heteroaryl, halogen, hydroxy, amino, nitro, or cyano; R2 and R4 are independently hydrogen, halogen, hydroxy, amino, nitro, cyano, acyl, acyloxy, sulfonyl, sulfinyl, alkylamino, carboxy, ester, ether, amido, sulfonic acid, sulfonamide, alkylsulfonyl, arylsulfonyl, alkoxycarbonyl, alkylsulfinyl, arylsulfinyl, alkylthio, arylthio, alkyl, alkoxy, oxyester, oxyamido, aryl, arylamino, aryloxy, heterocycloalkyl, heteroaryl or vinyl; R3 is hydrogen, halogen, hydroxy, amino, nitro, cyano, acyl, acyloxy, sulfonyl, sulfinyl, alkylamino, carboxy, ester, ether, amido, sulfonic acid, sulfonamide, alkylsulfonyl, arylsulfonyl, alkoxycarbonyl, alkylsulfinyl, arylsulfinyl, alkylthio, arylthio, alkyl, alkoxy, oxyester, oxyamido, aryl, arylamino, aryloxy, heterocycloalkyl, heteroaryl, alkenyl, alkynyl, azido or phenylsulfonyloxy; R5, R6 and R7 are independently hydrogen, hydroxy, alkyl, aryl, heterocycloalkyl, heteroaryl, alkoxy or aryloxy; R8 is hydrogen, hydroxy, thiol, halogen, alkyl, aryl, heterocycloalkyl, heteroaryl, alkylthio, arylthio; with the proviso that the compound is not methyl 2-(4R,S-isopropyl-2-oxo-pyrrolidin-1-yl) acrylate, methyl 2-(3R,S-chloro-4R,S-isopropyl-2-oxopyrrolidin-1-yl) acrylate or methyl-2-(2-oxo-pyrrolidin-1-yl) acrylate...
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Pyroglutamate salts and their use in the optical resolution of intermediates for the synthesis of dextrocetirizine and levocetirizine (Fri, 28 Aug 2009)
Patent 556580 The disclosure relates to (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt; (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt; (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(R)-pyrrolidone-5-carboxylic acid salt; or (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxycetamide-(R)-pyrrolidone-5-carboxylic salt. The disclosure also relates to a process for preparing (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide (I) and (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide (II) by chemical resolution of a mixture. These compounds are respectively intermediates for the synthesis of dextrocetirizine and levocetirizine.
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Compounds and methods for treatment of asthma, allergy and inflammatory disorders (Thu, 21 Dec 2000)
The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted,4-alkylidenyl piperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferably asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.
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SUBSTITUTED 1-(1H-IMIDAZOL-4-YL)ALKYL-BENZAMIDES (Wed, 31 Jan 1990)
Substituted l-(lH-imidazol-4-yl)alkyl-benzamides and their salts. processes for the preparation thereof and pharmaceutical compositions. These compounds have the formula wherein — Ri , R» - hydrogen or Ci-C»-alkyl, R» - hydrogen, amino, hydroxy!, Ci-C_.-alkyl or Ci-C-hydroxyalkyl, Ri - hydrogen or Ci-C*-alkyl , or R»R-N - pyrrolidine piperidino or morpholino, Rs and R. - hydrogen, hydroxy1, Ci-C.-alkyl or d-C.-alkox , at least one of R≤ and Hg being other than hydrogen. These compounds are prepared either by reacting a nitrogen compound with an alkyl l-(lH-imidazol-4-yl)alkyl-benzoate or with a l-<�£',-adrenoceptor agonist activities.
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2-hydroxy-3-(1-(1H-imidazol-4-yl)alkyl)- benzenecarboximidamides (Thu, 07 Nov 1996)

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Novel substituted (2-(1-piperazinyl)ethoxy)methyl compounds (Thu, 08 Jan 1998)
Novel substituted [2-(1-piperazinyl)ethoxy]methyl compounds of formula (I), wherein R¿1? is a -CONH¿2?, -CN, -COOH, -COOM or -COOR¿3? group, where M is an alkali metal, R¿3? is a C¿1-4? alkyl radical; and R¿2? is a hydrogen atom or a -COR¿4? or -R¿5? group where R¿4? is selected from -OR¿6? or -R¿7? groups, wherein R¿5? is an allyl or alkylaryl radical, R¿6? is a straight or branched C¿1-4? alkyl radical, a haloalkyl radical, alkylaryl, alkylnitroaryl or alkylhaloaryl, and R¿7? is haloalkyl; a method for preparing said compounds, as well as the use thereof for preparing compounds that are themselves valuable intermediates for the preparation of 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic acid or 2-[2-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]ethoxy]acetic acid and/or pharmaceutically acceptable salts thereof, are disclosed.
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SUBSTITUTED 1H-IMIDAZOLES (Wed, 26 Jul 1989)
New substituted lH-imidazoles and their salts, processes for the preparation thereof and pharmaceutical compositions. These compounds have the formula wherein Ri, R», R» and R» - hydrogen or C -C»-alkyl ; R» " hydrogen, C.-0»-alkyl or C.-C-alkox : Y> - hydrogen and Ya - OZa or the reverse; Zx - Zi - hydrogen or Ci-C»-alkyl or Zi and Za - -CHa- or -C(CH«)a-. These compounds are prepared either by reducing a corresponding imidazole compound having a hydroxyl or alkoxy group on the methyl bridge between the imidazole and phenyl rings, or by hydrolyzing a - ( [2, 2-dimethyl-4H-l , 3-benzodioxin-6(or S)-yl Jmethyl J -lH-imidazole , or yet by reducing an alkyl 3-[(lH-inu.dazol-4-yl)methyl)-2-hydroxybenzoate. These compounds have cardiac, cerebral and tissular anti-ischemic activities.
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2-oxo-1-pyrrolidine derivatives, processes for preparing them and their uses (Thu, 11 Aug 2005)
The invention concerns compound (2S)-2-[4-(2,2-difluorovinyl)-2-oxopyrrolidin-1-Cyl]butanoic acid and stereoisomers thereof used as synthesis intermediate to obtain pharmaceutical active substances of formula wherein the substituents are as defined in the specification
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Compounds and methods for treatment of asthma, allergy and inflammatory disorders (Wed, 15 May 2002)
The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted,4-alkylidenyl piperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferably asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.
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2-oxo-1-pyrrolidine derivatives, processes for preparing them and their uses (Thu, 11 Aug 2005)
SThe invention concerns (2S)-2-[(4S)-4-(2,2-difluorovinyl)-2-oxopyrrolidinyl] \O C butanamide or a pharmaceutically acceptable salt thereof as well as their use as pharmaceuticals. The compounds of the invention are particularly suited for treating neurological disorders such as epilepsy
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Process for preparing 2-oxo-1-pyrrolidine derivatives by intramolecular allylation (Thu, 11 Jan 2007)
The present invention relates to a new process for preparing 2-oxo-1-pyrrolidine derivatives of general formula (I), comprising the cyclisation of an intermediate of general formula (II) wherein the substituents are as defined in the specification.
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Pyrrolidinone derivatives (Thu, 13 Feb 2003)
The present invention provides pharmaceutical compositions and novel compounds useful in the treatment of conditions mediated by CCR2, MCP-1 or the interaction thereof. The compounds of the present invention are pyrrolidinones and pyrrolidine-thiones.
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BENZYLIDENE THIAZOLIDINEDIONES AND THEIR USE AS ANTIMYCOTIC AGENTS (Wed, 28 May 2003)
A compound of formula I or a salt thereof wherein, A is O or S, X and Y independently represent O, CH¿2? and may be the same or different, Q is (CH¿2?)¿m?-CH(R1)-(CH¿2?)¿n?, R is OR6, NHR8, R1 is hydrogen, or optionally substituted alkyl, R2 and R3 are independently hydrogen, or specific substituents, provided that R2 and R3 are not both H, and R4 and R5 are hydrogen or specific substituents, m is 0-3; n is 0-2; are useful in the treatment of fungal infections.
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α-arylethylpiperazine derivatives as neurokinin antagonists (Thu, 27 Nov 2003)
The invention relates to new α-arylethylpiperazine of the formula embedded image wherein Z represents 0 or S; n′ represents 1 or 2; R2 represents a hydrogen atom or a methyl group; W, Ar1 and Ar2 represent various substituents as defined herein; or non-toxic pharmaceutically acceptable salt, individual optical isomer, or individual diastereoisomer thereof, which are useful as neurokinin receptor antagonists (NK1 antagonists). It also relates to processes for their preparation and use in methods for treatment of asthma and/or allergic rhinitis.
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Alpha-arylethylpiperazine derivatives as neurokinin antagonists (Wed, 27 Jun 2001)
The invention relates to new alpha -arylethylpiperazine derivatives, which are useful as neurokinin receptor antagonists (NK1antagonists). It also relates to processes for the preparation of said alpha -arylethylpiperazine derivatives, to their use for the prevention and/or treatment of a condition associated with pathogical levels of substance P in a patient and to pharmaceutical compositions containing them.
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PHARMACEUTICAL COMPOSITIONS FOR ORAL ADMINISTRATION COMPRISING AN ACTIVE SUBSTANCE AND A CYCLODEXTRIN (Mon, 25 Jul 2005)

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THIAZOLIDINE DERIVATIVES AND ITS USE AS ANTIFUNGAL AGENT (Wed, 28 May 2003)
Compounds of formula (I) or salts thereof are provided wherein X is O or S, A and B are OR2 or Y-NR3R4 wherein when A is OR2, B is Y-NR3R4 and vice versa, or when one of A or B is OR2, then the other can be CO¿2?R7, Y is CH¿2? or C=Q, Q is (CH¿2?)¿m?-CH(R1)-(CH¿2?)¿n?, R is OR6 or NHR7, and with the other definitions as set out in claim 1, a process for its preparation and its use in the prophylaxis or treatment of fungal infections.
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LACTAM-N-ACETICS ACIDS AND THE PREPARATION THEREOF (Wed, 12 Dec 1979)
The present invention provides lactam-N-acetic acid compounds of the general formula:- wherein R1 and R2, which are the same or different, are hydrogen atoms, straight or branched chain alkyl radicals containing up to 4 carbon atoms, unsubstituted aryl radicals or aryl radicals substituted by halogen, R3 is a hydroxyl group or an -NR4R5 group, wherein R4 and R5 are the same or different and are hydrogen atoms, straight or branched chain alkyl radicals containing up to 4 carbon atoms or cycloalkyl or aralkyl radicals or R4 and R5, together with the nitrogen atom to which they are attached, form a heterocyclic radical containing at most 7 ring members, selected from alkyleneimino, oxa- alkyleneimino, aza-alkyleneimino and N-benzyl-aza-alkyleneimino radicals, m is 3, 4 or 5 and n is 0, 1 or 2; and the pharmaceutically-acceptable salts thereof. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.
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