Nitrogen Of The Hetero Ring Is Shared By An Additional Cyclo Of The Tricyclo Ring System Patents (Class 540/496)
-
Patent number: 7186828Abstract: A method for preparing cyclic urea compounds from at least an activated carbamic acid derivative containing an unprotected primary or secondary amine function, includes a cyclization step which consists in a reaction between the primary or secondary amine function and the carbamic acid function of the carbamic acid derivative(s).Type: GrantFiled: June 13, 2001Date of Patent: March 6, 2007Assignee: ImmuPharma (France) SAInventors: Gilles Guichard, Marie-Christine Galas-Rodriguez, legal representative, Pierre Rodriguez, legal representative, Elisa Rodriguez, legal representative, Romain Rodriguez, legal representative, Serge Plaue, Vincent Semetey, Arnaud-Pierre Schaffner, Jean-Paul Briand, Marc Rodriguez, deceased
-
Patent number: 7173026Abstract: The present invention relates to synthesis of pyrrolo[2,1-c][1,4]benzodiazepine-anthraquinone hybrids (V) wherein n=3,4; R=H, OH and to their use as antitumour agents.Type: GrantFiled: December 27, 2004Date of Patent: February 6, 2007Assignee: Council of Scientific and Industrial ResearchInventors: Ahmed Kamal, Gollapalli B. Khanna Ramesh, Ramu Rondla
-
Patent number: 7067511Abstract: Compounds of the formulae Ia and Ib: wherein: A is CH2, or a single bond; R2 is selected from: R, OH, OR, CO2H, CO2R, COH, COR, SO2R, CN; R6, R7 and R9 are independently selected from H, R, OH, OR, halo, amino, NHR, nitro, Me3Sn; and R8 is selected from H, R, OH, OR, halo, amino, NHR, nitro, Me3Sn, where R is as defined above, or the compound is a dimer with each monomer being the same or different and being of formula Ia or Ib, where the R8 groups of the monomers form together a bridge having the formula —X—R?—X— linking the monomers, where R? is an alkylene chain containing from 3 to 12 carbon atoms, which chain may be interrupted by one or more hetero-atoms and/or aromatic rings and may contain one or more carbon-carbon double or triple bonds, and each X is independently selected from O, S, or N; except that in a compound of formula Ia when A is a single bond, then R2 is not CH?CH(CONH2) or CH?CH(CONMe2). Other related compounds are also disclosed.Type: GrantFiled: December 12, 2001Date of Patent: June 27, 2006Assignee: Spirogen LimitedInventors: David Edwin Thurston, Philip Wilson Howard
-
Patent number: 7064121Abstract: Compounds of structural Formula (I) where A is a lipophilic group including an aliphatic bridging group, B is a lipophilic group, D is a group having at least one amino or substituted amino group and R is hydrogen, alkyl or cycloalkyl, and pharmaceutically acceptable salts and individual isomers thereof, which have growth hormone releasing activity in humans or animalsType: GrantFiled: October 13, 2004Date of Patent: June 20, 2006Assignees: Kaken Pharmaceutical Co., Ltd., Molecular Research InstituteInventors: Hidenori Funamizu, Nobuo Ishiyama, Satoru Ikegami, Tadashi Okuno, Kiyoshi Inoguchi, Ping Huang, Gilda Loew
-
Patent number: 7056913Abstract: The present invention provides novel pyrrolo-[2,1-c][1,4]benzodiazepine hybrids useful as anti-tumour agents and a process for the preparation thereof.Type: GrantFiled: March 30, 2004Date of Patent: June 6, 2006Assignee: Council of Scientific and Industrial ResearchInventors: Ahmed Kamal, Srinivas Olepu, Ramulu Poddutoori, Ramesh Gujjar, Praveen Kumar Pogula
-
Patent number: 7049311Abstract: Compounds of formula (Ia) and (Ib) wherein A is CH2, or a single bond; R2 is selected from: R, OH, OR, CO2H, CO2R, COH, COR, SO2R, CN; R6, R7 and R9 are independently selected from H, R, OH, OR, halo, amino, NHR, nitro, Me3Sn; and R8 is selected from H, R, OH, OR, halo, amino, NHR, nitro, Me3Sn, where R is as defined above, or the compound is a dimer with each monomer being the same or different and being of formula (Ia) or (Ib), where the R8 groups of the monomers form together a bridge having the formula —X—R?—X— linking the monomers, where R? is an alkylene chain containing from 3 to 12 carbon atoms, which chain may be interrupted by one or more hetero-atoms and/or aromatic rings and may contain one or more carbon—carbon double or triple bonds, and each X is independently selected from O, S, or N; except that in a compound of formula (Ia) when A is a single bond, then R2 is not CH?CH(CONH2) or CH?CH(CONMe2).Type: GrantFiled: August 27, 1999Date of Patent: May 23, 2006Assignee: Spirogen LimitedInventors: David Edwin Thurston, Philip Wilson Howard
-
Patent number: 7015215Abstract: The present invention provides Analogues of 1,1?-{[(bisalkane-1,N-diyl)piperazine]dioxy}bis(11aS)-7-methoxy-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one] of formula (VI) where n=2 to 10; a pharmaceutical composition comprising the above analogs and a process of preparing these analogues.Type: GrantFiled: March 31, 2003Date of Patent: March 21, 2006Assignee: Council of Scientific and Industrial ResearchInventors: Ahmed Kamal, Peram Surakattula Murali Mohan Reddy, Depatla Rajasekhar Reddy
-
Patent number: 6979684Abstract: The present invention relates to novel pyrrolo[2,1-c][1,4]benzodiazepine-napthalimide hybrids linked through piperazine moiety as potential antitumour agents. The present invention also relates to a process for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine-napthalimide hybrids linked through piperazine moiety useful as potential antitumour agents.Type: GrantFiled: June 30, 2004Date of Patent: December 27, 2005Assignee: Council of Scientific and Industrial ResearchInventors: Ahmed Kamal, Ramu Rondla, Gollpalli Bhasker Ramesh Khanna
-
Patent number: 6951853Abstract: Novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids as well as processes for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids are dislcosed. More particularly, present invention relates to a process for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine hybrids as DNA sequence selective agents which are useful as potential antitumour agents. In particular, the present invention relates to a process for the preparation of new pyrrolo[2,1-c][1,4]benzodiazepine hybrids as potential antitumour agents.Type: GrantFiled: March 30, 2004Date of Patent: October 4, 2005Assignee: Council of Scientific and Industrial ResearchInventors: Ahmed Kamal, Ramulu Poddutoori, Srinivas Olepu
-
Patent number: 6939869Abstract: Disclosed herein are novel pyrrolo[2,1-c][1,4]benzodiazepine-indole derivatives of formula (I): wherein each of the substituents is given the definition as set forth in the Specification and claims. Also disclosed are the preparation process of these derivatives and their uses in the manufacture of pharmaceutical compositions.Type: GrantFiled: September 12, 2002Date of Patent: September 6, 2005Assignee: Kaohsiung Medical UniversityInventor: Jeh-Jeng Wang
-
Patent number: 6838455Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: December 23, 2002Date of Patent: January 4, 2005Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: James E. Audia, Warren J. Porter, Richard C. Thompson, Stephen C. Wilkie, Douglas R. Stack, Qing Shi
-
Publication number: 20040198722Abstract: A compound of formula (I), wherein: R2 and R3 are independently selected from H, R, OH, OR, ═O, ═CH—R, ═CH2, CH2—CO2R, CH2—CO2H, CH2—SO2R, O—SO2R, CO2R, COR and CN, and there is optionally a double bond between C1 and C2 or C2 and C3; R6, R7, R8 and R9 are independently selected from H, R, OH, OR, halo, nitro, amino, Me3Sn; R11 is either H or R; Q is S, O or NH; L is a linking group, or a single bond; O is a solid support; or where one or more of R2, R3, R6, R7 and R8 are independently: H—(T)n—X—Y—A— where: X is CO, NH, S or O; T is a combinatorial unit; Y is a divalent group such that HY═R; A is O, S, NH, or a single bond and n is a positive integer.Type: ApplicationFiled: April 15, 2004Publication date: October 7, 2004Applicant: Spirogen LimitedInventors: David Edwin Thurston, Philip Wilson Howard
-
Patent number: 6800622Abstract: The present invention relates to a process for the preparation of novel pyrrolo [2,1-c][1,4]benzodiazepine hybrids useful as antitumour agents. This invention also relates to a process for the preparation of new pyrrolo[2,1-c][1,4]benzodiazepine hybrids as potential antitumour agents. More particularly, it provides a process for the preparation of 7-methoxy-8-[N-(1″-pyrenyl)-alkane-3′-carboxamide]-oxy-(11aS)-1,2,3,11a-tetraydro 5H-pyrrolo[2,1-c][1,4]benzodiazepine-5-one, with aliphatic chain length variation of these compounds and it also describes the DNA binding, anticancer (antitumour) activity.Type: GrantFiled: March 25, 2003Date of Patent: October 5, 2004Assignee: Council of Scientific and Industrial ResearchInventors: Ahmed Kamal, Ramesh Gujjar, Ramulu Poddutoori, Srinivas Olepu
-
Publication number: 20040192678Abstract: The present invention provides Analogues of 1,1′-{[(bisalkane-1,N-diyl)piperazine]dioxy}bis(11aS)-7-methoxy-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one] of formula (VI) 1Type: ApplicationFiled: March 31, 2003Publication date: September 30, 2004Inventors: Ahmed Kamal, Peram Surakattula Murali Mohan Reddy, Depatla Rajasekhar Reddy
-
Publication number: 20040192679Abstract: The present invention relates to novel pyrrolo[2,1-c][1,4]benzodiazepines compounds of general formula V as shown below, which are useful as potential antitumour agents and a process of preparing these compounds; particularly the present invention provides a process for the preparation of 7-methoxy-8-{n-[7-methoxy-(11aS)-1,2,3,10,11,11a-hexahydro-5H-pyrrolo[2,1-c][1,4]ben-zodiazepine-5-one-8-yloxy]alkyloxy}-(11aS)-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one, with varying aliphatic chain length and its 2-hydroxy derivatives.Type: ApplicationFiled: March 31, 2003Publication date: September 30, 2004Inventors: Ahmed Kamal, Gujjar Ramesh, Olepu Srinivas, Poddutoori Ramulu
-
Publication number: 20040192677Abstract: The present invention relates to a process for the preparation of novel pyrrolo [2,1 -c][1,4]benzodiazepine hybrids useful as antitumour agents. This invention also relates to a process for the preparation of new pyrrolo[2,1-c][1,4]benzodiazepine hybrids as potential antitumour agents. More particularly, it provides a process for the preparation of 7-methoxy-8-[N-(1″-pyrenyl)-alkane-3′-carboxamide]-oxy-(11aS)-1,2,3,11a-tetraydro 5H-pyrrolo[2,1 -c][1,4]benzodiazepin-5-one, with aliphatic chain length variation of these compounds and it also describes the DNA binding, aticancer (antitumour) activity.Type: ApplicationFiled: March 25, 2003Publication date: September 30, 2004Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCHInventors: Ahmed Kamal, Ramesh Gujjar, Ramulu Poddutoori, Srinivas Olepu
-
Publication number: 20040176591Abstract: The present invention is directed to methods for the preparation of piperazine ring-containing compounds, particularly mirtazapine. According to the present invention, the mirtazapine intermediate 1-(3-carboxypyridyl-2)-4-methyl-2-phenyl-piperazine is made by hydrolyzing 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine with a base where the base is present in a ratio of up to about 12 moles of the base per one mole of 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine. The mirtazapine intermediate 1-(3-carboxypyridyl-2)-4-methyl-2-phenyl-piperazine may be made by hydrolyzing 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine with potassium hydroxide at a temperature of at least about 130° C.Type: ApplicationFiled: March 16, 2004Publication date: September 9, 2004Inventors: Claude Singer, Anita Liberman, Nina Finkelstein
-
Patent number: 6774125Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: October 7, 2002Date of Patent: August 10, 2004Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: James E. Audia, Richard C. Thompson, Stephen C. Wilkie, Thomas C. Britton, Warren J. Porter, George W. Huffman, Lee H. Latimer
-
Patent number: 6747144Abstract: A compound of formula (I), wherein: R2 and R3 are independently selected from H, R, OH, OR, ═O, ═CH—R, ═CH2, CH2—CO2R, CH2—CO2H, CH2—SO2R, O—SO2R, CO2R, COR and CN, and there is optionally a double bond between C1 and C2 or C2 and C3; R6, R7, R8 and R9 are independently selected from H, R, OH, OR, halo, nitro, amino, Me3Sn; R11 is either H or R; Q is S, O or NH; L is a linking group, or a single bond; O is a solid support; or where one or more of R2, R3, R6, R7 and R8 are independently: H—(T)n—X—Y—A— where: X is CO, NH, S or O; T is a combinatorial unit; Y is a divalent group such that HY=R; A is O, S, NH, or a single bond and n is a positive integerType: GrantFiled: February 26, 2001Date of Patent: June 8, 2004Assignee: Spirogen LimitedInventors: David Edwin Thurston, Philip Wilson Howard
-
Publication number: 20040097490Abstract: The invention relates to novel heterocyclic compounds of general formula (I) and to their salts with a base or an acid: 1Type: ApplicationFiled: September 4, 2003Publication date: May 20, 2004Applicant: AVENTIS PHARMA S.A.Inventor: Branislav Musicki
-
Publication number: 20040054168Abstract: Disclosed herein are novel pyrrolo[2,1-c][1,4]benzodiazepine-indole derivatives of formula (I): 1Type: ApplicationFiled: September 12, 2002Publication date: March 18, 2004Applicant: Kaohsiung Medical UniversityInventor: Jeh-Jeng Wang
-
Publication number: 20040043977Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: January 6, 2003Publication date: March 4, 2004Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
-
Patent number: 6696438Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: December 12, 2002Date of Patent: February 24, 2004Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: James E. Audia, Bruce A. Dressman, Qing Shi
-
Patent number: 6689881Abstract: Method for the preparation of enantiomerically pure diazepino-indolone of formula which comprises the intramolecular cyclization of a product of formula where A, B, X1, X2, Z, Z1, Z2 and R are as defined in the description, in the presence of a weak Lewis acid catalyst.Type: GrantFiled: April 3, 2002Date of Patent: February 10, 2004Assignee: Warner-Lambert LLCInventor: Patrick Bernardelli
-
Patent number: 6683073Abstract: The present invention relates to a process for the preparation of novel pyrrolo [2,1-c][1,4]benzodiazepines useful as potential antitumour agents. This invention also relates to a process for the preparation of new pyrrolo[2,1-c][1,4]benzodiazepines as potential antitumour agents. More particularly, it provides a process for the preparation of 7-methoxy-8-[6′-(4″-fluorophenyl)-2′-methylpyrimidine-4′-yloxy]alkoxy-(11aS)-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1,c][1,4]benzodiazepin-5-one with aliphatic chain length variations for the compounds and it also describes the anticancer (antitumour) activity. The structural formula of novel pyrrolo[2,1-c][1,4]benzodiazepine is as follows.Type: GrantFiled: March 25, 2003Date of Patent: January 27, 2004Assignee: Council of Scientific and Industrial ResearchInventors: Ahmed Kamal, Karnati Laxma Reddy
-
Patent number: 6683075Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: January 6, 2003Date of Patent: January 27, 2004Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
-
Publication number: 20040002603Abstract: A process for making nevirapine, comprising the following steps:Type: ApplicationFiled: June 5, 2003Publication date: January 1, 2004Applicant: Boehringer ingelheim Chemicals, Inc.Inventors: Robert Frederick Boswell, Bernard Franklin Gupton, Young Sek Lo
-
Patent number: 6660856Abstract: The present invention provides an efficient process for the preparation of pyrrolo [2,1-c][1,4]benzodiazepines (PBDs) represented by the formula (I): which starts from a subsituted 2-amino benzoic acid compound, and involves a step of an intermediate MOM-protected dilactam compound in the presence of LiBH4. The process enables a practital and large scale (e.g. ca. 10 g) synthesis of PBD analogue.Type: GrantFiled: March 8, 2002Date of Patent: December 9, 2003Assignee: Kaohsiung Medical UniversityInventor: Jeh-Jeng Wang
-
Patent number: 6653303Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: January 6, 2003Date of Patent: November 25, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
-
Publication number: 20030195196Abstract: A compound with formula (I) 1Type: ApplicationFiled: March 4, 2003Publication date: October 16, 2003Applicant: Spirogen LimitedInventors: David Edwin Thurston, Philip Wilson Howard
-
Publication number: 20030187253Abstract: The present invention provides an efficient process for the preparation of pyrrolo[2,1-c][1,4]benzodiazepines (PBDS) represented by the formula (I): 1Type: ApplicationFiled: March 8, 2002Publication date: October 2, 2003Applicant: Kaohsiung Medical UniversityInventor: Jeh-Jeng Wang
-
Patent number: 6624159Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.Type: GrantFiled: June 22, 2001Date of Patent: September 23, 2003Assignee: Pharmacia & Upjohn CompanyInventors: David John Anderson, Gordon L. Bundy, Fred L. Ciske, David R. Graber, Michael J. Genin, Thomas M. Judge, Malcolm Wilson Moon, Mark E. Schnute, Joseph Walter Strohbach, Suvit Thaisrivongs, Atli Thorarensen, Steven Ronald Turner, Valerie A. Vaillancourt, Allison J. Wolf
-
Publication number: 20030162768Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: December 12, 2002Publication date: August 28, 2003Inventors: James E. Audia, Bruce A. Dressman, Qing Shi
-
Patent number: 6608192Abstract: A compound of formula (IV): O is a solid support; L is a linking group or a single bond; X′ is selected from CO, NH, S, or O; A is O, S, NH, or a single bond; R2 and R3 are independently selected from: H, R, OH, OR, ═O, ═CH—R, ═CH2, CH2—CO2R′, CH2—CO2H, CH2—SO2R, O—SO2R, CO2R, COR, CN and there is optionally a double bond between C1 and C2 or C2 and C3; R6, R7, and R9 are independently selected from H, R, OH, OR, halo, nitro, amino, Me3Sn; R11 is either H or R; Q is S, O or NH; R10 is a nitrogen protecting group; and Y is a divalent group such that HY=R, and other related compounds and collections of compounds.Type: GrantFiled: February 26, 2001Date of Patent: August 19, 2003Assignee: Spirogen LimitedInventors: David Edwin Thurston, Philip Wilson Howard
-
Publication number: 20030153550Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: October 7, 2002Publication date: August 14, 2003Inventors: James E. Audia, Richard C. Thompson, Stephen C. Wilkie, Thomas C. Britton, Warren J. Porter, George W. Huffman, Lee H. Latimer
-
Patent number: 6562806Abstract: A compound with formula (I) where R10 is a therapeutically removable nitrogen protecting group; R2 and R3 are independently selected from: H, R, OH, OR, ═O, ═CH—R, ═CH2, CH2—CO2R, CH2—CO2H, CH2—SO2R, O—SO2—R, CO2R, COR and CN; R6, R7 and R9 are independently selected from H, R, OH, OR, halo, amino, nitro, Me3Sn; X is S, O or NH; R11 is either H or R; and where there is optionally a double bond between C1 and C2 or C2 and C3; and R8 is selected from H, R, OH, OR, halo, amino, nitro, Me3Sn, or R7 and R8 together form a group —O—(CH2)p—O—, where p is 1 or 2. Such compounds may be used in methods of ADEPT, GDEPT, NPEPT or PDT.Type: GrantFiled: February 26, 2001Date of Patent: May 13, 2003Assignee: Spirogen LimitedInventors: David Edwin Thurston, Philip Wilson Howard
-
Patent number: 6548494Abstract: Compounds of the formula shown below are poly(ADP-ribosyl)transferase inhibitors: Such compounds are useful as therapeutics in treating cancers and in ameliorating the effects of stroke, head trauma, and neurodegenerative disease.Type: GrantFiled: August 31, 2000Date of Patent: April 15, 2003Assignee: Agouron Pharmaceuticals, Inc.Inventors: Stephen Evan Webber, Donald James Skalitzky, Jayashree Girish Tikhe, Robert Arnold Kumpf, Joseph Timothy Marakovits, Brian Walter Eastman
-
Patent number: 6525044Abstract: This invention relates to novel carbocycles and heterocycles having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: GrantFiled: February 16, 2001Date of Patent: February 25, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Richard E Olson, Thomas P Maduskuie, Lorin Andrew Thompson, Andrew J Tebben, Nenghui Wang, Wei Deng, Hong Liu
-
Publication number: 20030022883Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.Type: ApplicationFiled: November 30, 2001Publication date: January 30, 2003Inventors: Dana V. Ferraris, Jia-He Li, Vincent J. Kalish, Jie Zhang
-
Publication number: 20020045747Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: July 30, 2001Publication date: April 18, 2002Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
-
Patent number: 6365585Abstract: Metabolites of the products of formula (I) in which A and R are as defined in the description, which are phosphodiesterase 4 inhibitors.Type: GrantFiled: June 7, 2000Date of Patent: April 2, 2002Assignee: Warner-Lambert CompanyInventors: Henry Jacobelli, Christine Julien-Larose, Sylvie Marc
-
Publication number: 20020025959Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: June 22, 2001Publication date: February 28, 2002Inventors: David John Anderson, Thomas J. Beauchamp, Gordon L. Bundy, Fred L. Ciske, John R. Farrell, David R. Graber, Michael J. Genin, Thomas M. Judge, Malcolm Wilson Moon, Mark E. Schnute, Joseph Walter Strohbach, Suvit Thaisrivongs, Atli Thorarensen, Steven Robert Turner, Valerie A. Vaillancourt, Allison J. Wolf
-
Patent number: 6281353Abstract: The present invention relates to a process for manufacturing diazepine derivatives of the general formula I wherein R1 is lower alkyl and R2 is hydrogen, or R1 and R2 are together —(CH2)n— and n is 2 or 3; R3 is halogen, lower alkyl, lower alkoxy and m is 0, 1 or 2; R4 is hydrogen or lower alkyl. The compounds of general formula I are valuable intermediate products for the manufacture of imidazo [1,5-a][1,4]diazepine derivatives, like for instance 7-chloro-3-(5-dimethylaminomethyl-[1,2,4]oxadiazol-3-yl)-5-methyl-4,5-dihydro-imidazo[1,5-a][1,4]benzodiazepin-6-one, which diazepine derivatives show excellent psychopharmacological properties as agonists of the central benzodiazepine receptors.Type: GrantFiled: May 8, 2000Date of Patent: August 28, 2001Assignee: Hoffmann-la Roche Inc.Inventor: Fabienne Hoffmann-Emery
-
Patent number: 6239130Abstract: The present invention presents compounds that inhibit phosphodiesterase 4 having Formula (I). The present invention also provides methods of using the compounds of Formula (I) to prevent or treat asthma, atopic dermatitis, rheumatoid arthritis, inflammatory bowel disorders, pulmonary hypertension, liver injury, bone loss, septic shock, or multiple sclerosis, and to pharmaceutical compositions that contain the compounds of Formula (I).Type: GrantFiled: November 10, 1999Date of Patent: May 29, 2001Assignee: Warner-Lambert CompanyInventors: Yves Pascal, Catherine Burnouf, Bernard Gaudilliere, Henry Jacobelli, Alain Calvet, Adrian Payne, Svein Dahl
-
Patent number: 6225306Abstract: A biphenyl derivative represented by the following general formula (1) and a pharmaceutically acceptable salt thereof: [In the formula (1), A represents a single bond, —CH2—, —CO—, —CS— or —SO2—; B represents a single bond or —CH2—; R1 represents a hydrogen atom, —OH, —NR11R12 (wherein R11 and R12 each independently represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms), —OCOCH3, or a halogen atom; R2 represents a hydrogen atom or R1 and R2 form a group ═O together; R3 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; provided that in the formula, the absolute configuration of the position a may be either R or S]. The compound of the present invention has considerably high safety and efficacy and is useful as, in particular, a vasopressin receptor antagonist.Type: GrantFiled: September 30, 1999Date of Patent: May 1, 2001Assignee: Wakamoto Pharmaceutical Co., Ltd.Inventors: Yasuhiro Ohtake, Akira Naito, Kenji Naito, Hidehiko Matsukawa, Yoshiaki Saito, Hatsunori Toyofuku
-
Patent number: 5972927Abstract: Diazepinoindoles of formula (I), ##STR1## wherein A is mono- to trisubstituted aryl or heteroaryl, and B is an --OR.sub.1 or --NR.sub.2 R.sub.3 group where R.sub.1, R.sub.2 and R.sub.3 are particularly hydrogen, and racemic forms, enantiomers and pharmaceutically acceptable salts thereof, as phosphodiesterase IV inhibitors, are disclosed.Type: GrantFiled: October 20, 1998Date of Patent: October 26, 1999Assignee: JouveinalInventors: Yves Pascal, Henry Jacobelli, Alain Calvet, Adrian Payne, Svein G. Dahl
-
Patent number: 5962337Abstract: A method has now been found of synthesizing a combinatorial library of 1,4-benzodiazepin-2,5-diones on solid supports via an aza-Wittig ring closure, said compounds optionally encoded with tags, and to the use of this library in assays to discover biologically active compounds, and, optionally, to cleave 1,4-benzodiazepin-2,5-diones therefrom.Type: GrantFiled: December 23, 1997Date of Patent: October 5, 1999Assignee: Pharmacopeia, Inc.Inventor: Michael H. J. Ohlmeyer
-
Patent number: 5852190Abstract: The invention relates to diazepinoindoles of formula: ##STR1## in which R is hydrogen, lower alkyl or lower alkoxy; A is aryl or nitrogen-containing heteroaryl, each of which is optionally substituted by from one to three groups of halogen, lower alkyl, haloalkyl, lower alkoxy and acetamido, or their racemic forms, isomers or pharmaceutically acceptable salts, wherein for the racemic forms of the (S) configuration, A is not phenyl, haloalkyl, or 2-indolyl when R is hydrogen, and for the racemic forms of the (R) configuration, A is not 2-indolyl when R is hydrogen. Also, the invention relates to a method for inhibiting cyclic nucleotide phosphodiesterase activity by administering these compounds to a subject in an amount which is therapeutically effective to inhibit cyclic nucleotide phosphodiesterase activity.Type: GrantFiled: February 22, 1995Date of Patent: December 22, 1998Assignee: Institut de Recherche Jouveinal SAInventors: Yves Pascal, Indres Moodley, Alain Calvet, Jean-Louis Junien
-
Patent number: 5846969Abstract: A sulfonamide derivative or a sulfonic ester derivative represented by the following general formula (I): ##STR1## {G represents an aromatic 5- or 6-membered ring; L represents O or --N(R.sup.1)-- (R.sup.1 represents hydrogen or lower alkyl); and M represents ##STR2## rings A and B represent each an unsaturated 5- or 6-membered ring; Y represents O, S(O).sub.n, C(R.sup.3)(R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10)C(O), N.dbd.C(R.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15).Type: GrantFiled: June 11, 1997Date of Patent: December 8, 1998Assignee: Eisai Co., Ltd.Inventors: Hiroshi Yoshino, Norihiro Ueda, Jun Niijima, Toru Haneda, Yoshihiko Kotake, Kentaro Yoshimatsu, Tatsuo Watanabe, Takeshi Nagasu, Naoko Tsukahara, Nozomu Koyanagi, Kyosuke Kitoh
-
Patent number: 5834460Abstract: A serine derivative represented by the general formula (I) ##STR1## (symbols in the formula represent the following meanings; X: a sulfur atom or an oxygen atom,Y: a nitrogen atom or CH,R.sup.1 and R.sup.2 : the same or different from each other and each represents a hydrogen atom, a lower alkyl group or a protecting group for the amino group, or R.sup.1 and R.sup.2 may be combined together to form a four- to nine-membered nitrogen-containing cycloalkyl group,R.sup.3 : a hydrogen atom, a carboxyl group, a protected carboxyl group, an aralkyl group, or a lower alkyl group unsubstituted or substituted with a hydroxyl group,R.sup.4 : a hydrogen atom or a hydroxyl group,R.sup.Type: GrantFiled: October 12, 1995Date of Patent: November 10, 1998Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Ichio Noda, Masahiro Iwata, Shuichi Sakamoto, Kazuo Koshiya, Takuma Morita, Atsuyuki Kohara