Abstract: The invention provides a pharmaceutical composition for the treatment of dementia or Alzheimer's disease in which the active therapeutical agent is donepezil hydrochloride in an amorphous state.
Type:
Grant
Filed:
August 1, 2002
Date of Patent:
May 11, 2004
Assignee:
Chemagis Ltd.
Inventors:
Alexander Weisman, Chalil Abu Gnim, Rina Uzan, Joseph Kaspi
Abstract: The invention provides a process for the preparation of a compound of the formula 6 comprising the hydrolysis and decarboxylation of a compound of the formula 5 according to the reaction: 1
Type:
Application
Filed:
June 11, 2003
Publication date:
March 11, 2004
Applicant:
CHEMAGIS LTD
Inventors:
Ori Lerman, Joseph Kaspi, Oded Arad, Mohammed Alnabari, Yana Sery
Abstract: The invention provides a pharmaceutical composition for the treatment of dementia or Alzheimer's disease in which the active therapeutical agent is donepezil hydrochloride in an amorphous state.
Type:
Application
Filed:
August 1, 2002
Publication date:
January 1, 2004
Applicant:
Chemagis Ltd.
Inventors:
Alexander Weisman, Chalil Abu Gnim, Rina Uzan, Joseph Kaspi
Abstract: The invention provides a process for the preparation of diphenylmethylthioacetamide (I) as described in Scheme 4 comprising reacting of the isothiouronium salt or its corresponding base of the formula IV with an acetamide of the formula XCH2CONH2, wherein X represents a halogen, M represents an alkali metal and A represents an anion, in a protic medium at a temperature of less than 100° C.
Type:
Grant
Filed:
April 2, 2002
Date of Patent:
November 18, 2003
Assignee:
Chemagis, Ltd.
Inventors:
Vladimir Naddaka, Naim Menashe, Jael Lexner, Shadi Saeed, Joseph Kaspi, Ori Lerman
Abstract: The invention provides a process for the preparation of 2-amino-N-[2-(2,5-dimethoxyphenyl)-2-hydroxyethyl]acetamide of the formula 1 by hydrogenolysis of substituted 2-dibenzylamino-N-[2-(2′,5′-dimethoxyphenyl)-2-hydroxy-ethyl]acetamide having the formula (5), wherein Ar and Ar′ are aryl groups.
Type:
Grant
Filed:
July 30, 2002
Date of Patent:
August 26, 2003
Assignee:
Chemagis Ltd.
Inventors:
Michael Brand, Ronit Chen, Deby Yigal, Joseph Kaspi
Abstract: The invention provides a process for the preparation of 6,6-dimethylhept-1-en-4-yn-3-ol comprising of reacting t-butylacetylene with a proton-extracting agent selected from the group consisting of an organometallic compound and metallic lithium to form a t-butylacetylide, reacting the acetylide with acrolein at temperatures between −40° C. to +20° C., quenching the reaction mixture and isolating the product.
Type:
Grant
Filed:
July 17, 2001
Date of Patent:
May 27, 2003
Assignee:
Chemagis Ltd.
Inventors:
Joseph Kaspi, Oded Friedman, Edna Danon
Abstract: The invention provides a process for the preparation of 2-amino-N-[2-(2,5-dimethoxyphenyl)-2-hydroxyethyl]acetamide of the formula 1 by hydrogenolysis of substituted 2-dibenzylamino-N-[2-(2′,5′-dimethoxyphenyl)-2-hydroxy-ethyl]acetamide having the formula (5), wherein Ar and Ar′are aryl groups.
Type:
Application
Filed:
July 30, 2002
Publication date:
December 19, 2002
Applicant:
Chemagis Ltd.
Inventors:
Michael Brand, Ronit Chen, Deby Yigal, Joseph Kaspi
Abstract: The invention provides a process for the preparation of diphenylmethylthioacetamide (I) as described in Scheme 4 comprising reacting of the isothiouronium salt or its corresponding base of the formula IV with an acetamide of the formula XCH2CONH2, wherein X represents a halogen, M represents an alkali metal and A represents an anion, in a protic medium at a temperature of less than 100° C.
Type:
Application
Filed:
April 2, 2002
Publication date:
December 5, 2002
Applicant:
CHEMAGIS LTD.
Inventors:
Vladimir Naddaka, Naim Menashe, Jael Lexner, Shadi Saeed, Joseph Kaspi, Ori Lerman
Abstract: The invention provides a process for the preparation of 2-amino-N-[2-(2,5-dimethoxyphenyl)-2-hydroxyethyl]acetamide of the formula 1 by hydrogenolysis of substituted 2-dibenzylamino-N-[2-(2′,5′-dimethoxyphenyl)-2-hydroxy-ethyl]acetamide having the formula (5), wherein Ar and Ar′ are aryl groups.
Type:
Application
Filed:
January 9, 2002
Publication date:
September 12, 2002
Applicant:
Chemagis Ltd.
Inventors:
Michael Brand, Ronit Chen, Deby Yigal, Joseph Kaspi
Abstract: The invention provides a process for the preparation of 2-amino-N-[2-(2,5-dimethoxyphenyl)-2-hydroxyethyl]acetamide of the formula 1 by hydrogenolysis of substituted 2-dibenzylamino-N-[2-(2′,5′-dimethoxyphenyl)-2-hydroxy-ethyl]acetamide having the formula (5), wherein Ar and Ar′ are aryl groups,
Type:
Grant
Filed:
January 9, 2002
Date of Patent:
September 3, 2002
Assignee:
Chemagis Ltd.
Inventors:
Michael Brand, Ronit Chen, Deby Yigal, Joseph Kaspi
Abstract: The present invention provides a process for preparing a compound of the general formula (I):
wherein
R1 to R5 are independently selected from hydrogen, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or C1-6 alkoxy, all optionally substituted by one or more of halogen, hydroxy and aryl groups, as well as being independently selected from amino, mono- or disubstituted amino, alkenyloxy, acyl, acyloxy, cyano, nitro, aryl and alkylthio groups, which process comprises reacting a compound of the general formula (II):
wherein
R1 to R5 are as defined in formula (I), with aminoguanidine bicarbonate in a mixture of a water-soluble solvent and polyphosphoric acid.
Type:
Grant
Filed:
February 22, 2001
Date of Patent:
December 11, 2001
Assignee:
Chemagis, Ltd.
Inventors:
Vladimir Nadaka, Jael Lexmer, Joseph Kaspi
Abstract: The invention provides a process for the separation of (RR,SS) 2-dimethylaminomethyl-1-(3-methoxyphenyl) cyclohexanol hydrochloride ?(RR,SS)-Tramadol!, from a mixture consisting of (RR,SS) Tramadol and (RS,SR)-2-dimethylaminomethyl-1-(3-methoxyphenyl) cyclohexanol ?(RS,SR)-Tramadol!, which process includes combining the mixture with an electrophilic reagent, the reagent selectively reacting with the hydroxyl group of (RS,SR)-Tramadol, leaving most of the (RR,SS) Tramadol intact, and precipitating the remaining, practically pure (RR,SS) Tramadol from the mixture.
Abstract: The invention provides a process for the purification and isolation of (RR,SS)-2-dimethylaminomethyl-1-(3-methoxyphenyl)cyclohexanol from mixtures also containing the (RS,SR) isomer comprising reacting the above mixture in a solvent at elevated temperature under acidic conditions, whereby the (RS,SR) isomer is selectively converted to the (RR,SS) isomer, 1-(3-methoxyphenyl)-2-dimethylaminomethylcyclohex-6-ene, 1-(3-methoxyphenyl)-2-dimethyl-aminomethylcyclohex-1-ene or a mixture thereof, selectively precipitating the desired (RR,SS) isomer as an amine acid salt, and recrystallizing the purified product.
Type:
Grant
Filed:
November 14, 1996
Date of Patent:
September 30, 1997
Assignee:
Chemagis Ltd.
Inventors:
Ori Lerman, Michael Tennenbaum, Erez Gal, Joseph Kaspi
Abstract: A process for the improved purification and separation of trans 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol hydrochloride from a reaction mixture containing the trans isomer, the cis isomer and Grignard reaction side products, comprising combining the mixture with a solution of hydrochloric acid in a low molecular weight alcohol or with gaseous hydrogen chloride in the presence of an organic solvent selected from medium molecular weight alcohols, ketones, esters and ethers or aromatic ethers, to effect the selective precipitation of trans 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol hydrochloride.
Type:
Grant
Filed:
September 8, 1993
Date of Patent:
May 9, 1995
Assignee:
Chemagis, Ltd.
Inventors:
Stephen Cherkez, Ori Lerman, Michael Tennenbaum, Hasalia Avner, Tamar Kunyevski