Chalcogen Bonded Directly At 2- And 4-positions Patents (Class 544/285)
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Patent number: 7232902Abstract: The invention relates to a process for the preparation of certain pyrimidinone compounds.Type: GrantFiled: August 13, 2002Date of Patent: June 19, 2007Assignee: SmithKline Beecham p.l.c.Inventors: Keith Raymond Mulholland, Andrew R Ross, Graham Ralph Slater, Gillian Elizabeth Smith
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Patent number: 7205309Abstract: Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3 and A have the significance given in the specification are provided. The compounds can be used for the treatment or prevention of obesity.Type: GrantFiled: July 3, 2003Date of Patent: April 17, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Patrizio Mattei, Werner Mueller, Werner Neidhart, Matthias Heinrich Nettekoven, Philippe Pflieger
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Patent number: 7160874Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.Type: GrantFiled: November 15, 2004Date of Patent: January 9, 2007Assignee: Ajinomoto Co., Inc.Inventors: Yasuhiro Tanaka, Toshihiko Yoshimura, Hiroyuki Izawa, Chieko Ejima, Mitsuhiko Kojima, Yuko Satake, Eiji Nakanishi, Nobuyasu Suzuki, Shingo Makino, Manabu Suzuki, Masahiro Murata
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Substituted amidoalkyl uracils and their use as inhibitors of the poly(adp-ribose) synthetase (PARS)
Patent number: 7125995Abstract: This application relates to compounds of formula (I) below in which the several variable groups are as defined in the specification and claims, to methods of preparing these materials, to pharmaceutical compositions containing these materials, and to methods of using these materials to treat ischaemia or reperfusion damage.Type: GrantFiled: November 2, 2001Date of Patent: October 24, 2006Assignee: Bayer AktiengesellschaftInventors: Barbara Albrecht, Michael Gerisch, Gabriele Handke-Ergüden, Axel Jensen, Thomas Krahn, Werner Nickl, Felix Oehme, Karl-Heinz Schlemmer, Henning Steinhagen -
Patent number: 7109332Abstract: 2,4-Dioxo-3-quinazolinylaryl sulfonylurea compounds having the formula: wherein R is a member selected from the group consisting of H and C1-6 alkyl; R1 is a member selected from the group consisting of H, C1-6 alkyl, C1-6 haloalkyl, C3-5 cycloalkyl and C3-5 cycloalkyl-alkyl; R2 is a member selected from the group consisting of H, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C1-6 alkoxy, cyano and —C(O)R2a, wherein R2a is a member selected from the group consisting of C1-6 alkoxy and (C1-6 alkyl)0-2 amino; L is a 1 to 3 carbon linking group selected from the group consisting of —CH2—, —CH(CH3)—, —CH2CH2—, —CH2CH(CH3)— and —CH2CH2CH2—; L1 is a linking group selected from the group consisting of a bond and —CH2—; L2 is a linking group selected from the group consisting of a bond, —NH— and —CH2—; and Ar1 is an aromatic ring selected from the group consisting of benzene, pyridine and pyrimidine; are provided.Type: GrantFiled: September 29, 2004Date of Patent: September 19, 2006Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Wolin Huang, Anjali Pandey, Shawn M. Bauer, Xiaoming Zhang, Zhaozhong J. Jia
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Patent number: 7094780Abstract: Antibacterial 3-aminoquinazolin-2,4-diones have formula (I) wherein: R1 and R3 include alkyl, alkenyl, cycloalkyl, aryl, hetero-cyclic, and heteroaryl; R5, R6, and R8 include H, alkyl, alkoxy, halo, NO2, CN, NH2, alkyl and dialkylamino; R7 includes hydrogen, alkyl, cycloalkyl, hetero-cyclic, fused heterocyclic, aryl and fused aryl; J and K are C or N; and pharmaceutically acceptable salts thereof.Type: GrantFiled: December 12, 2000Date of Patent: August 22, 2006Assignee: Warner Lambert Company LLCInventors: Paul Bird, Edmund Lee Ellsworth, Dai Quoc Nguyen, Joseph Peter Sanchez, Howard Daniel Hollis Showalter, Rajeshwar Singh, Michael Andrew Stier, Tuan Phong Tran, Brian Morgan Watson, Judy Yip
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Patent number: 7060825Abstract: The invention claimed herein relates to an improvement in a process for synthesizing a compound of formula Ib: wherein R1 and R2 are each individually amino or N-alkyl substituted amino; hydroxy; alkoxy; keto; lower alkyl; or a nitrogen or oxygen protecting group; R3 is hydrogen; hydroxy; alkoxy; trifluoromethyl alkoxy; halo; sulfhydryl or alkylthio; R4 is —C(O)—X; X is hydroxy; alkoxy; or an amino acid residue; in which process a 2-amino-5-nitro-benzonitrile starting reagent is cyclized to form 2,4-diamino-6-nitro-quinazoline, which is converted to 2,4,6-triamino-quinazoline, which is converted to 2,4-diamino-6-cyano-quinazoline, which is converted to 2,4-diamino-6-formyl-quinazoline; in which the improvement includes: reacting an R4-p-benzoic acid alkylene moiety with triethyl phosphite to form a 4-R4-carbonyloxyalkyl-phenyl-alkyldiethylphosphite; and reacting the 2,4-diamino-6-formyl-quinazoline with the 4-R4-carbonyloxyalkyl-phenyl-alkyldiethylphosphite to form the compound of formula Ib.Type: GrantFiled: July 25, 2003Date of Patent: June 13, 2006Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Ye Wu, Harry Kochat
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Patent number: 7056926Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 13, 2004Date of Patent: June 6, 2006Assignee: Portola Pharmaceuticals Inc.Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-Maguire
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Patent number: 7049438Abstract: The invention concerns quinazoline derivatives of Formula (I) wherein each of Q1, Z, m, R1, R2, R3 and Q2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour diseaseType: GrantFiled: June 1, 2001Date of Patent: May 23, 2006Assignee: AstraZeneca ABInventors: Laurent François André Hennequin, Patrick Ple
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Patent number: 7037880Abstract: Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent such as a cyano group; A is a substituent such as a 4-pyrazolyl or thiazolyl group; and B is a substituent such as an alkylcarbonyl group. Agricultural chemicals and agents for preventing the attachment of aquatic organisms containing one or more such ethylene derivatives.Type: GrantFiled: August 8, 2002Date of Patent: May 2, 2006Assignee: Nissan Chemical Industries, Ltd.Inventors: Tomoyuki Ogura, Hiroshi Murakami, Akira Numata, Rika Miyachi, Toshiro Miyake, Norihiko Mimori, Shinji Takii
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Patent number: 6921766Abstract: There is provided a preventive or therapeutic agent for diseases accompanied by abnormal vascular function in which lipid deposition in the blood vessel is involved, said agent comprising a chymase inhibitor as an active ingredient. As the chymase inhibitor, a quinazoline derivative represented by the following formula is used. In the above formula, the ring A represents an aromatic ring.Type: GrantFiled: November 1, 2000Date of Patent: July 26, 2005Assignee: Daiichi Suntory Pharma Co., Ltd.Inventors: Harukazu Fukami, Hidenori Urata
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Patent number: 6900222Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is aType: GrantFiled: May 23, 2000Date of Patent: May 31, 2005Assignee: Janssen Pharmaceutica N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Patent number: 6872727Abstract: Polycyclic pyrimidine-2,4(1H,3H)-diones with functionalized alkyl residues at the 1-, the 3-, or both position(s); methods for their synthesis, production, and pharmaceutical preparation. The invention concerns the synthesis of the above-described compounds, their chemical and structural characterization, and the analysis of their physiological/pharmacological activities in vitro and in vivo. These goals have been attained by the specification of routes of synthesis, methods for the production of the compounds, and the presentation of compound-specific characteristics. The substances encompassed by the present invention demonstrate pharmacologically significant collangenase/matrix metalloproteinase inhibitory activities. The specific example 1-(3-mercaptoprop-1-yl)-3-methyl-chinazolin-2,4(1H,3H)-dione will be presented in detail.Type: GrantFiled: August 21, 2000Date of Patent: March 29, 2005Assignee: Privates Institut fur Biomedizinische Forschung und BeratungInventors: Konrad Herrmann, Siegfried Leistner, Petra Wippich
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Patent number: 6867214Abstract: A quinazoline derivative having formula (1) and a pharmaceutically acceptable salt thereof: wherein the ring A represents an aryl group, which derivative has a chymase inhibitory activity and suppresses the exacerbation of vascular permeability induced by chymase, and a pharmaceutical composition containing the same as an essential ingredient. These compounds are useful for treatment of allergic diseases, rheumatic diseases, and cardiac and circulatory system diseases which are due to the abnormal exacerbation of Angiotensin II production.Type: GrantFiled: August 20, 1999Date of Patent: March 15, 2005Assignee: Daiichi Suntory Pharma Co., Ltd.Inventors: Harukazu Fukami, Akiko Ito, Seiichi Imajo
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Publication number: 20040229876Abstract: An object of the present invention is to provide compounds having potent antitumor activity.Type: ApplicationFiled: June 7, 2004Publication date: November 18, 2004Applicant: KIRIN BEER KABUSHIKI KAISHAInventors: Kazuo Kubo, Teruyuki Sakai, Rika Nagao, Yasunari Fujiwara, Toshiyuki Isoe, Kazumasa Hasegawa
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Publication number: 20040214819Abstract: The present invention relates to modified amino acids of general formula 1Type: ApplicationFiled: April 29, 2004Publication date: October 28, 2004Applicant: Dr. Karl Thomae GmbHInventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Helmut Pieper, Henri Doods, Gerhard Hallermayer, Michael Entzeroth, Wolfgang Wienen
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Patent number: 6806274Abstract: The invention concerns quinazoline derivatives of Formula (I) wherein Q1 includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3 includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2 and R3 is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal.Type: GrantFiled: January 7, 2002Date of Patent: October 19, 2004Assignee: AstraZeneca UK LimitedInventors: Graham C Crawley, Laurent F A Hennequin, Darren McKerrecher, Patrick Ple, Jeffrey Philip Poyser, Christine M P Lambert
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Publication number: 20040127500Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented.Type: ApplicationFiled: December 12, 2003Publication date: July 1, 2004Applicant: Bayer Pharmaceuticals CorporationInventors: Michael C. VanZandt, David R. Brittelli, Brian R. Dixon
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Publication number: 20040122030Abstract: The present invention is directed to novel thalidomide derivative compounds that have activity as anti-angiogenic compounds. More particularly the compounds have the general structure: where R1 is selected from the group consisting of H, halo, alkyl, haloalkyl, —NH2, hydroxy and alkoxy; R2 is selected from the group consisting of optionally substituted bicyclic, optionally substituted aryl, and R6 is H, or C1-C8 alkyl; R19 is optionally substituted aryl; and m is 0-6.Type: ApplicationFiled: October 21, 2003Publication date: June 24, 2004Inventor: Milton L. Brown
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Publication number: 20040097525Abstract: Pyrimidone compounds of formula (I): 1Type: ApplicationFiled: October 27, 2003Publication date: May 20, 2004Applicant: SmithKline Beecham plcInventors: Deirdre Mary Bernadette Hickey, Robert John Ife, Colin Andrew Leach, Ivan Leo Pinto, Stephen Allan Smith, Steven James Stanway
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Publication number: 20040067969Abstract: The present invention provides intermediates, synthetic methods and novel quinazolinone compositions of matter.Type: ApplicationFiled: February 14, 2003Publication date: April 8, 2004Inventors: Gustave Bergnes, Edward Ha, George Yiannikouros, Panos Kalaritis, Brandon E. Yonce, Kurt Alan Welday
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Publication number: 20040044013Abstract: It is the object of this invention to discover and study new chemical substances of non-proteinogenic structure which have a matrix metalloproteinase (MMP)-inhibitory effect.Type: ApplicationFiled: October 22, 2003Publication date: March 4, 2004Inventors: Jochen Heinicke, Uwe Klausmeier, Christoph Arkona, Siegfried Leistner
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Patent number: 6689786Abstract: Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 23, 2003Date of Patent: February 10, 2004Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Wolin Huang
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Publication number: 20040019049Abstract: A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure IA, IB, or IC where the values of the variable are defined herein.Type: ApplicationFiled: May 23, 2003Publication date: January 29, 2004Applicant: CHIRON CORPORATIONInventors: Rustum S. Boyce, Natalia Aurrecoechea, Daniel Chu, Aaron Smith
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Patent number: 6683101Abstract: Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof.Type: GrantFiled: December 3, 2002Date of Patent: January 27, 2004Assignee: Warner-Lambert CompanyInventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
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Publication number: 20030236252Abstract: Described are bicycle-substituted cyclohexylamines of Formula (I) and their pharmaceutically acceptable salts thereof. The compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's specification. disease. The substituents are defined in the specification.Type: ApplicationFiled: November 12, 2002Publication date: December 25, 2003Inventors: Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
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Publication number: 20030232810Abstract: Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof. The compounds of formula (I) are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease.Type: ApplicationFiled: December 3, 2002Publication date: December 18, 2003Inventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
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Publication number: 20030216396Abstract: This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders.Type: ApplicationFiled: February 11, 2003Publication date: November 20, 2003Applicant: BAYER CORPORATIONInventors: Jacques Dumas, William J. Scott, Bernd Riedl
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Publication number: 20030153584Abstract: Methods and compounds useful for the inhibition of convulsive disorders, including epilepsy, are disclosed. The methods and compounds of the invention inhibit or prevent ictogenesis and/or epileptogenesis. Methods for preparing the compounds of the invention are also described.Type: ApplicationFiled: April 11, 2002Publication date: August 14, 2003Applicant: Queen's UniversityInventors: Donald F. Weaver, Buhendwa Musole Guillain, John R. Carran, Kathryn Jones
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Publication number: 20030149037Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: December 20, 2002Publication date: August 7, 2003Inventors: Francesco Salituro, Guy Bemis, John Cochran
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Publication number: 20030142462Abstract: A conductive polymer material can exhibit good heat resistance and good moisture resistance, in which the conductive polymer comprises as a dopant at least one of aromatic sulfonic acid derivatives represented by general formula 1: 1Type: ApplicationFiled: December 31, 2002Publication date: July 31, 2003Inventor: Masahiro Kuwahara
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Publication number: 20030130278Abstract: A compound selected from those of formula (I): 1Type: ApplicationFiled: October 11, 2002Publication date: July 10, 2003Inventors: Bernard Gaudilliere, Henri Jacobelli, Joseph Armand Picard, Michael William Wilson
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Publication number: 20030114666Abstract: The present invention provides compounds of formula (I): 1Type: ApplicationFiled: June 18, 2002Publication date: June 19, 2003Inventors: Edmund Lee Ellsworth, James Alan Kerschen, Sharon Anne Powell, Joseph Peter Sanchez, Howard Daniel Hollis Showalter, Michael Andrew Stier, Tuan Phong Tran
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Publication number: 20030092712Abstract: Compounds described by the chemical formula (I) or a pharmaceutically acceptable salt thereof: 1Type: ApplicationFiled: December 17, 2001Publication date: May 15, 2003Inventors: James B. Doherty, John E. Stelmach, Meng-Hsin Chen, Luping Liu, Julianne A. Hunt, Rowena D. Ruzck, Joung L. Goulet, David D. Wisnoski, Swaminathan Ravi Natarajan, Kathleen M. Rupprecht, Jianming Bao, Shouwu Miao, Xingfang Hong, Peter J. Sinclair, Florida Kallashi
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Patent number: 6521630Abstract: The present invention relates to tetrahydroquinazoline-2,4-diones derivatives of the formula (I): pharmaceutically acceptable salts thereof, wherein A is (CH2)n where n is equal to 0, 1 or 2; U is CH2, NH, or NR3, R1 and R2 are selected independently from H, (C1-C6)alkyl, Cl, F, CN, nitro, CF3, —NHC(O)R6 and —OR7, or R1 and R2, together with the atoms to which they are attached, form a carbocyclic or heterocyclic five- or six-membered ring, R3 is selected from the group consisting of H, (C1-C6)malkyl, C(═O)—(C1-C6)alkyl, where m=1 or 2; R4 and R5 are selected from H, (C1-C6)alkyl, Cl, F, —CF3, —CN, —NHC(═O)R6, —OR7, a 5-to 7-membered aryl or heteroaryl ring, where m, R6 and R7 are as defined above; and R6 and R7 are selected independently from H, (C1-C6)alkyl or a 5- to 7-membered aryl or heteroaryl ring; V is CH, CR3, or N; W is CH2, C(O), or S(O)2; X is C or N; and Y is CH, CR1,CR2, or N.Type: GrantFiled: August 29, 2000Date of Patent: February 18, 2003Assignee: Pfizer Inc.Inventors: Anton Franz Joseph Fliri, Todd William Butler, Randall James Gallaschun, John Anthony Ragan, Brian Patrick Jones
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Patent number: 6498172Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: August 20, 1999Date of Patent: December 24, 2002Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Bruce A. Lefker, Robert L. Rosati
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Publication number: 20020193377Abstract: A compound selected from those of formula (I): 1Type: ApplicationFiled: February 13, 2002Publication date: December 19, 2002Inventors: Charles Andrianjara, Nicole Chantel Barvian, Bernard Gaudilliere, Henri Jacobelli, Daniel Fred Ortwine, William Chester Patt, Ly Pham, Catherine Rose Kostlan, Michael William Wilson
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Patent number: 6495547Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula —NR6—Alk2— (b-1), or —Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen.Type: GrantFiled: August 18, 2000Date of Patent: December 17, 2002Assignee: Janssen Pharmaceutica, N.V.Inventors: Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren, Marc Francis Josephine Schroven, Marcel Frans Leopold De Bruyn
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Publication number: 20020161226Abstract: Novel substituted quinozaline compounds and conjugates useful to inhibit the growth of brain tumor cells and to inhibit adhesion and migration of brain tumor cells. The compounds of the invention include 4-(3′-bromo-4′-hydroxy phenyl)-amino-6,7-dimethoxyquinazoline and this compound covalently bound to EGF.Type: ApplicationFiled: July 11, 2001Publication date: October 31, 2002Applicant: Parker Hughes InstituteInventors: Fatih M. Uckun, Rama Krishna Narla, Xing-Ping Liu
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Publication number: 20020156050Abstract: A compound of formula I: 1Type: ApplicationFiled: April 1, 2002Publication date: October 24, 2002Applicant: Guilford Pharmaceuticals Inc.Inventors: Jia-He Li, Jie Zhang
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Patent number: 6448270Abstract: Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using the 4-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as cerebral ischemia, central nervous system trauma, hypoglycemia, neurodegenerative disorders, anxiety, migraine headaches, convulsions, aminoglycoside antibiotics-induced hearing loss, chronic pain, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, urinary incontinence and neurodegenerative disorders such as lathyrism, Alzheimers' Disease, Parkinsonism, and Huntington's Disease are described. Also described are novel methods for preparing 4-substituted piperidine analogs and novel intermediates of the 4-substituted piperidine analogs.Type: GrantFiled: June 13, 2000Date of Patent: September 10, 2002Assignees: Warner-Lambert Company, Cocensys, IncorporatedInventors: Christopher F. Bigge, Jonathan Wright, Sui Xiong Cai, Eckard Weber, Richard Woodward, Nancy C. Lan, Zhang-Lin Zhou, John F.W. Keana
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Publication number: 20020115674Abstract: The invention is a series of 7-substituted quinazolin-2,4-diones useful as antibacterial agents, processes for the preparation of the compounds, and a pharmaceutical composition containing one or more of the compounds.Type: ApplicationFiled: October 4, 2001Publication date: August 22, 2002Inventors: John Michael Domagala, Edmund Lee Ellsworth, Liren Huang, Thomas Eric Renau, Rajeshwar Singh, Michael Andrew Stier
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Patent number: 6436925Abstract: Benzamides of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: R1—C1-C6-alkyl, branched or unbranched, where one of the C atoms in this chain may be substituted by a phenyl ring, cyclohexyl ring, indolyl ring and an SCH3 group, and the phenyl ring in turn is substituted by by [sic] a maximum of two R4 radicals, where R4 [lacuna] hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, and R2 can be NR5CO—R6 and NHR5SO2—R6, and R3 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl, CN, COOH, CONH2, COO—C1-C4-alkyl, SO2—C1-C4-alkyl, —SO2Ph, SO2NH—C1-C4-alkyl, iodine, SO2NH2 and NH2, and A can be aromType: GrantFiled: October 3, 2000Date of Patent: August 20, 2002Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
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Patent number: 6429311Abstract: The present invention is directed to certain N-amino- and N-hydroxy-quinazolinone compounds and synthetic methods for synthesis thereof, which compounds may find use in combinatorial libraries. More specifically, the invention is directed to the synthesis of 3-hydroxy- and 3-amino-4 (1H)-quinazolinones via the reaction of an appropriate 2-aminobenzamide compound with a carboxylic acid or acyl halide at ambient temperature performed on a solid support or in solution.Type: GrantFiled: February 1, 2001Date of Patent: August 6, 2002Assignee: Sepracor Inc.Inventor: Yun Gao
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Patent number: 6413724Abstract: The invention provides chemistry libraries containing fused 2,4-pyrimidinediones. The invention also provides methods for the construction of fused 2,4-pyrimidinedione containing libraries. The invention further provides methods for the identification of bioactive, fused 2,4-pyrimidinediones from those libraries.Type: GrantFiled: February 4, 1997Date of Patent: July 2, 2002Assignee: Versicor, Inc.Inventors: Mikhail F. Gordeev, Dinesh V. Patel
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Patent number: 6407116Abstract: A compound represented by the formula: [wherein ring A represents a homocycle optionally having substituents or a nitrogen-containing heterocycle optionally having substituents; D and E are O or S; one of R1 and R2 represents a group represented by the formula: (wherein Ar1 and Ar2 represent an aromatic group optionally having substituents; Ar1 and Ar2 may form a condensed cyclic group optionally having substituents together with an adjacent carbon atom; ring B represents a nitrogen-containing heterocycle optionally having substituents; X and Y are a bond, O, S(O)p (p is an integer of 0 to 2), NR4 (R4 is H or a lower alkyl group) or a bivalent straight-chained lower hydrocarbon group, which may contain 1 to 3 hetero atoms, optionally having substituents; and R3 represents H, a hydroxy group optionally having substituents or an optionally esterified carboxyl group); and the other is a hydrogen atom, a cyano group or a hydrocarbon group optionally having substituents&rsqType: GrantFiled: February 25, 2000Date of Patent: June 18, 2002Assignee: Takeda Chemical Industries, Inc.Inventors: Masahiro Kajino, Shinji Morimoto, Atsuhiro Inaba, Hideaki Nagaya
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Publication number: 20020052355Abstract: The present invention is directed to a compound of the formula (I): 1Type: ApplicationFiled: August 1, 2001Publication date: May 2, 2002Inventors: Anton Franz Joseph Fliri, Todd William Butler, Randall James Gallaschun
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Patent number: 6376667Abstract: Methods and compounds for the synthesis of heterocycles, including pyrimidine-2,4-diones, are disclosed. Also disclosed are solid supports useful for solid phase synthesis, and methods for making the solid supports.Type: GrantFiled: November 24, 1998Date of Patent: April 23, 2002Assignee: OSI Pharmaceuticals, Inc.Inventors: Arlindo L. Castelhano, Hui Shao
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Patent number: 6369002Abstract: Compounds of formula 1 wherein R1 is hydrogen, fluorine, chlorine, bromine or methyl; R2 is C1-C4alkyl, C1-C4halogenalkyl, halogen, hydroxy, C1-C4alkoxy, C1-C4halogenalkoxy, nitro, amino or cyano; R3, R15 to R39 and X6 to X19 are as defined in claim 1, and the agrochemically acceptable salts and stereoisomers of these compounds of formula I are suitable for use as herbicides.Type: GrantFiled: October 30, 2000Date of Patent: April 9, 2002Assignee: Syngenta Crop Properties, Inc.Inventors: Walter Kunz, Kurt Nebel
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Patent number: 6344559Abstract: This invention provides an industrially useful process for producing a quinazoline derivative (I) of the general formula: [wherein R1 is hydrogen or halogen; R2 is carboxy or protected carboxy; A is lower alkylene] or its salt on a commercial scale which comprises reacting a compound of the general formula: [wherein R1 is hydrogen or halogen] or its salt with a silylating agent and then with a compound of the general formula: Cl—A—R2 (III) [wherein R2 is carboxy or protected carboxy; A is lower alkylene] or its salt, optionally followed by desilylation.Type: GrantFiled: October 13, 1999Date of Patent: February 5, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroki Omori, Shunsuke Goto, Hiroyuki Tsuboi, Masayasu Fukagawa, Kooji Kagara