Oxygen Hetero Ring Attached Directly Or Indirectly To The 1,3-diazine Ring By Nonionic Bonding Patents (Class 514/252.2)
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Publication number: 20110118266Abstract: The present invention relates to derivatives of general formula I wherein: —W represents nitrogen, —R1 represents: •a hydrogen or a linear or branched C1-C5 alkyl radical or, •a C1-C3 alkyl radical substituted with groups such as trifluoromethyl, nitrile, hydroxy, C1-C3 alcoxy, C3-C6 alkoxyalkoxy, indolyl, thiophenyl, oxothiophenyl, C1-C3 N-alkylcarbamoyl groups or, •a phenyl or pyridyl or naphthyl, or thiophenyl group optionally substituted with one or more groups such as halogen atoms, nitro, nitrile, trifluoromethyl, vinyl, methylsulfanyl, linear branched C1-C4 alkyl, linear or branched C1-C3 alkoxy groups, •a C6 2-oxocycloalkyl radical—R2 represents a methyl or heptyl, —m, n are equal to 1, —V represents CH2, —X—Y represents —N— (C?O)—, —CH—O—, —Z represents a phenyl group substituted with one or more trifluoromethyl groups, halogen atoms or linear C1-C4 alkyl groups.Type: ApplicationFiled: July 7, 2009Publication date: May 19, 2011Applicant: PIERRE FABRE MEDICAMENTInventors: Isabelle Leroy, Elisabeth Dupont-Passelaigue, Karine Valeille, Yves Rival, Didier Junquero
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Publication number: 20110092474Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: ApplicationFiled: June 11, 2009Publication date: April 21, 2011Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xiaohu Zhang
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Publication number: 20110065706Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as GPR119 modulators, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus, and pharmaceutical compositions containing them.Type: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Applicant: AstraZeneca ABInventors: Alan Martin Birch, Roger John Butlin, David Stephen Clarke, Andrew Leach, Philip Alexander MacFaul, Charles John O'Donnell, James Stewart Scott, Paul Robert Owen Whittamore, Dan Anders Broo, Öjvind Percy Davidsson, Kjell Erik Johansson, Hanna De La Motte
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Publication number: 20110046108Abstract: The invention concerns benzamide compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, ring A, n, R3, and R4 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of EphB4, and/or EphA2 and/or Src kinases.Type: ApplicationFiled: January 25, 2007Publication date: February 24, 2011Applicant: AstraZeneca ABInventors: Jason Grant Kettle, Jon Read, Andrew Leach, Bernard Christophe Barlaam, Richard Ducray, Christine Marie Paul Lambert-Van Der Brempt
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Publication number: 20110028484Abstract: The present invention relates to 2-phenyl-4-cyclopropyl-pyrimidine derivatives and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.Type: ApplicationFiled: April 9, 2009Publication date: February 3, 2011Inventors: Eva Caroff, Emmanuel Meyer
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Patent number: 7879853Abstract: The invention relates to novel pyrimidine derivatives of Formula (1) which are efficacious inhibitors of protein kinases, in particular of one or more isoforms of the protein kinase B/Akt.Type: GrantFiled: June 28, 2005Date of Patent: February 1, 2011Assignee: Bayer Schering Pharma AGInventors: Josef Stadlwieser, Thomas Baer, Thomas Maier, Thomas Beckers, Thomas Ciossek, Armin Zuelch, Ulrich Graedler
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Publication number: 20100324010Abstract: A renin inhibitor comprising a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof. The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.Type: ApplicationFiled: October 14, 2008Publication date: December 23, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Yasuhiro Imaeda, Takanobu Kuroita, Yoshiyuki Fukase, Shinkichi Suzuki, Michiko Amano
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Publication number: 20100286124Abstract: The present invention relates to new prop-2-yn-1-amine inhibitors of monoamine oxidase type B activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 9, 2010Publication date: November 11, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Patent number: 7807671Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with diketo piperazine and piperadine derivatives that possess unique antiviral activity useful for the treatment of HIV and AIDS.Type: GrantFiled: April 10, 2007Date of Patent: October 5, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, John F. Kadow, Zhongxing Zhang, Zhiwei Yin, Nicholas A. Meanwell, Alicia Regueiro-Ren, Jacob Swidorski, Ying Han, David J. Carini
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Publication number: 20100240636Abstract: The present invention disclosed compounds of Structural Formula (I), and enantiomer, racemic body, pharmaceutically acceptable salts, solvates or hydrates thereof, wherein variable groups are as defined within, as well as methods for preparing such compounds. The compounds are useful as PPAR? agonist, through activating PPAR-RXR heterodimers that intereacts with specific DNA response elements within promoter regions of target gene, particularly in the treatment and prevention of polycystic kidney and cancer.Type: ApplicationFiled: October 11, 2007Publication date: September 23, 2010Inventors: Jianhua Shen, Changlin Mei, Hualiang Jiang, Bin Dai, Yangliang Ye, Xishan Xiong, Jing Tang, Lili Fu
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Publication number: 20100152182Abstract: Disclosed are pyrimidine derivatives of formula wherein R0, R1, R3 to R9, and Z have a signification as indicated in claim 1, which have interesting pharmaceutical properties.Type: ApplicationFiled: January 13, 2010Publication date: June 17, 2010Inventors: Rolf Baenteli, Marie Claude Bernhard, Peter Buehlmayer, Nigel Graham Cooke, Rudolf Duthaler, Klaus Hinterding, Gebhard Thoma, Maurice Van Eis, Anette Von Matt, Louis Walliser, Gerhard Zenke
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Patent number: 7718653Abstract: A compound of formula (I) where one of A1, A2 or A3 is N, and the others are independently selected from CH or N; ring B is a fused 5 or 6-membered carbocyclic or heterocyclic ring which is optionally substituted as defined in the specification, and R1, R2, R3, R4, and n are as defined in the specification. The compounds are inhibitors of EphB4 or EphA2 and therefore may be useful in pharmaceutical compositions for the treatment of conditions such as cancer.Type: GrantFiled: July 16, 2008Date of Patent: May 18, 2010Assignee: AstraZeneca ABInventors: Bernard Christophe Barlaam, Richard Ducray, Jason Grant Kettle
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Publication number: 20100119503Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.Type: ApplicationFiled: September 25, 2008Publication date: May 13, 2010Applicant: INCYTE CORPORATIONInventors: Chu-Biao Xue, Changsheng Zheng, Hao Feng, Michael Xia, Joseph Glenn, Ganfeng Cao, Brian W. Metcalf
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Publication number: 20100056512Abstract: Pyrimidine compounds of the following formula: wherein R1, R2, R3, R4, R5, X, Q1, Q2, and Q3 are defined herein. Also disclosed is a method of treating cancer with one of these compounds.Type: ApplicationFiled: August 29, 2008Publication date: March 4, 2010Applicant: Hutchison MediPharma Enterprises LimitedInventors: Wei-Guo Su, Hong Jia, Rick B. Ye, Yang Sai
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Patent number: 7655661Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytotoxic drugs in a targeted fashion.Type: GrantFiled: June 23, 2008Date of Patent: February 2, 2010Assignee: ImmunoGen Inc.Inventors: Robert Yongxin Zhao, Ravi V. J. Chari
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Patent number: 7655660Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.Type: GrantFiled: January 5, 2007Date of Patent: February 2, 2010Assignee: Immunogen Inc.Inventors: Robert Yongxin Zhao, Ravi V. J. Chari
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Publication number: 20090291962Abstract: The invention relates to 2-phenyl-6-aminbcarbonyl-pyrimidinc derivatives and their use as P2Y12 receptor antagonists in the treatment and/or prevention and/or treatment of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals. Formula (1).Type: ApplicationFiled: October 24, 2007Publication date: November 26, 2009Applicant: Actelion Pharmaceuticals Ltd.Inventors: Eva Caroff, Kurt Hilpert, Emmanuel Meyer
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Publication number: 20090170836Abstract: This invention comprises the novel compounds of formula (I) wherein n, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: February 18, 2009Publication date: July 2, 2009Inventors: Patrick Rene Angibaud, Isabelle Noelle Constance Pilatte, Sven Franciscus Anna Van Brandt, Bruno Roux, Peter Ten Holte, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Alexey Borisovich Dyatkin
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Publication number: 20090149466Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity.Type: ApplicationFiled: December 5, 2008Publication date: June 11, 2009Inventors: Paul Gillespie, Robert Alan Goodnow, JR., Shawn David Erickson, Richard Jones
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Patent number: 7511044Abstract: Pyrimidine ethers and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea,Type: GrantFiled: February 11, 2005Date of Patent: March 31, 2009Assignee: Amgen Inc.Inventors: Hui-Ling Wang, Chenera Balan, Elizabeth M. Doherty, James R. Falsey, Vijay Keshav Gore, Jodie Katon, Mark H. Norman
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Publication number: 20090054449Abstract: The invention relates to substituted N-heterocyclic compounds of general formula (I.A) and to the tautomers of the compounds the physiologically acceptable salts of the compounds and the physiologically acceptable salts of the tautomers of the compounds. The invention also relates to the use of these compounds and their pharmacologically acceptable salts in the production of a pharmaceutical agent for treating diseases that respond to the influence exerted by dopamine D3 receptor ligands, especially for treating diseases of the central nervous system, especially schizophrenia and/or depression.Type: ApplicationFiled: December 20, 2005Publication date: February 26, 2009Applicant: Abbott GmbH & Co. KGInventors: Herve Geneste, Daryl R. Sauer
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Publication number: 20090030009Abstract: The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and to the use of a compound of formula (I) for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.Type: ApplicationFiled: March 9, 2007Publication date: January 29, 2009Inventors: Guido Bold, Andrea Vaupel, Marc Lang
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Publication number: 20090023719Abstract: A compound of formula (I) where one of A1, A2 or A3 is N, and the others are independently selected from CH or N; ring B is a fused 5 or 6-membered carbocyclic or heterocyclic which is optionally substituted as defined in the specification, and R1, R2, R3, R4, and n are as defined in the specification. The compounds are inhibitors of EphB4 or EphA2 and therefore may be useful in pharmaceutical compositions for the treatment of conditions such as cancer.Type: ApplicationFiled: July 16, 2008Publication date: January 22, 2009Applicant: Astrazeneca ABInventors: Bernard Christophe Barlaam, Richard Ducray, Jason Grant Kettle
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Publication number: 20090012094Abstract: Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.Type: ApplicationFiled: October 31, 2007Publication date: January 8, 2009Applicants: IRM LLC, A DELAWARE LIMITED LIABILITY COMAPNY, NOVARTIS, AGInventors: Valentina Molteni, Xiaolin Li, Donatella Chianelli, Jon Loren, Juliet Nabakka, Xiaodong Liu, Shifeng Pan, Yi Liu, Donald S. Karanewsky, Pascal Furet, Vito Guagnano, Shuli You
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Patent number: 7470722Abstract: Disclosed herein are carbonyl compounds of Formula I as described herein. Methods and compositions are disclosed for treating disease states including, but not limited to cancers, autoimmune diseases, tissue damage, central nervous system disorders, neurodegenerative disorders, fibrosis, bone disorders, polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, cardiovascular conditions, and disorders in which angiogenesis play a role in pathogenesis, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.Type: GrantFiled: June 9, 2005Date of Patent: December 30, 2008Assignee: Kalypsys, Inc.Inventors: James William Malecha, Stewart Alwyn Noble, Christian Andreus Hassig, Paul L. Wash, Brandon M. Wiley, Charles Maxwell Lawrence, Timothy Z. Hoffman
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Publication number: 20080312245Abstract: The present invention provides a composition comprising metronidazole, ketoconazole, and lincomycin and methods of treating infectious skin diseases such as acne by topically administering the composition.Type: ApplicationFiled: October 9, 2007Publication date: December 18, 2008Inventor: Longyan Xiao
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Patent number: 7393845Abstract: A heteroaryl derivative having the formula (I).Type: GrantFiled: June 5, 2007Date of Patent: July 1, 2008Assignee: H. Lundbeck A/SInventors: Mario Rottländer, Ejner Knud Moltzen, Ivan Mikkelsen, Thomas Ruhland, Kim Andersen, Christian Krog-Jensen
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Patent number: 7388026Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.Type: GrantFiled: September 2, 2005Date of Patent: June 17, 2008Assignee: Immunogen, Inc.Inventors: Robert Yongxin Zhao, Ravi V. J. Chari
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Publication number: 20080025972Abstract: Sex steroid potentiated disorders including, prostate cancer and breast cancer, in a patient in need of treatment thereof, are treated with an amount of nitric oxide donating compound and/or nitrosoglutathione reductase inhibitor and/or cysteine binder different from that provided by nitric oxide donating compound effective to inhibit activation of steroid receptor. Variations include using only nitric oxide donating agent as treating agent; using only nitrosoglutathione reductase inhibitors as treating agent, using nitric oxide donating agent plus nitrosoglutathione reductase inhibiting agent; for prostate cancer treatment using prostate cancer drug modified to contain nitric oxide donating moiety or FDA approved nitric oxide donating agent and FDA approved prostate cancer treating agent. Also disclosed is an assay for assessing mutagenic potential of prostate cancer in a patient.Type: ApplicationFiled: May 21, 2007Publication date: January 31, 2008Applicant: Duke UniversityInventors: Yehia Daaka, Jonathan S. Stamler
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Patent number: 7300937Abstract: New derivatives of cyanoaryl (or cyanoheteroaryl)-carbonyl-piperazinyl-pyrimidines (I), where R1 represents an OR3 radical, where R3 represents a radical derived from a saturated hydrocarbon, with a linear or branched chain of 1 to 4 carbon atoms, and R2 represents a phenyl radical substituted at least by one cyan radical (—C?N), or a radical of a heteroaromatic ring of 5 or 6 members substituted at least by one cyan radical (—C?N); and their physiologically acceptable salts, are useful for application in human and/or veterinary therapeutics as sedatives, anticonvulsants, hypnotics and general anaestheticsType: GrantFiled: October 10, 2001Date of Patent: November 27, 2007Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Jordi Corbera-Arjona, David Vano-Domenech, Maria Neus Mesquida-Estevez, Jordi Frigola-Constansa
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Patent number: 7208495Abstract: A compound represented by the formula: (wherein, R1 and R2 are the same or different and each represents a hydrogen atom, hydrocarbon group or heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3–8 membered iso- or heterocyclic group, R3 represents a cyclic group, a hydroxy group, a mercapto group that may have oxo, or an amino group, R4 represents a hydrogen atom, a hydrocarbon group, a hydroxy group, a mercapto group which may have oxo, or an amino group, or R2 and R4 may link together to form a double bond, X represents a bond or a linear hydrocarbon group, W represents an oxygen atom or a sulfur atom, ring B represents a 5–8 membered nitrogen-containing heterocyclic group, ring C represents a benzene ring, and— represents a single bond or a double bond), or a salt or a prodrug thereof that has excellent neurodegenerative inhibitory activity and brain penetrability, and is useful as an agent for preventing/treating neurodegenerative diseases.Type: GrantFiled: July 4, 2002Date of Patent: April 24, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Shigenori Ohkawa, Masaomi Miyamoto, Masahiro Okura, Tetsuya Tsukamoto
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Patent number: 7084144Abstract: A compound having the general formula (I): wherein: X is N or C; R0 is H, a lower alkyl group, a lower O-alkyl group, lower alkyl group, a benzyl group, a phenyl group, a heterocyclic amine group, a cycloalkyl group, a cycloalkyl group substituted with O-alkyl or, a furyl group; R1 and R2 are, independently, H, an amine group, a lower alkyl group, a lower O-alkyl group, a lower S-alkyl group or a lower N-alkyl group, or R1 and R2 taken together with the carbon atoms to which they are attached form a five-membered carbocyclic or heterocyclic ring, where the heteroatoms of the heterocyclic ring are one or two oxygen atoms, and/or where any substituent on said carbocyclic or heterocyclic ring is chosen from O, S and N; n is 0,1,2,3 or 4; m is 0 or 1; and pharmaceutically acceptable salts thereof; with the proviso that said compound is not 1-[(4-methoxyphenyl)sulfonyl]piperazine or 1-(1,3-benzodioxol-5-ylsulfonyl)piperazine.Type: GrantFiled: May 19, 2004Date of Patent: August 1, 2006Assignee: The Jordanian Pharmaceutical MFG & Medical Equipment CO LTDInventor: Adnan Badwan
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Patent number: 7045519Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.Type: GrantFiled: September 6, 2001Date of Patent: May 16, 2006Assignee: Chiron CorporationInventors: John M. Nuss, Stephen D. Harrison, David B. Ring, Rustum S. Boyce, Kirk Johnson, Keith B. Pfister, Savithri Ramurthy, Lynn Seely, Allan S. Wagman, Manoj C. Desai, Barry H. Levine
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Patent number: 6995159Abstract: Compounds of Formula (IC) that act as 5-HT receptor ligands and their uses in the treatment of diseases linked to the activation of 5-HT2 receptors in animals are described herein .Type: GrantFiled: September 16, 2004Date of Patent: February 7, 2006Assignee: Pfizer Inc.Inventors: Phoebe Chiang, William A. Novomisle, Willard M. Welch, Jr.
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Patent number: 6953803Abstract: Pyrmidinone compounds of formula (I) are inhibitors of the enzyme Lp-PLA2 and of use in therapy, in particular for treating atherosclerosis.Type: GrantFiled: April 25, 2000Date of Patent: October 11, 2005Assignee: SmithKline Beecham p.l.c.Inventors: Deirdre Mary Bernadette Hickey, Colin Andrew Leach, Stephen Allan Smith
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Patent number: 6916804Abstract: The subject invention provides compounds having the structure: wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R2 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R3 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R2 and R3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R3 is oxygen; R4 and R5 are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R4NR5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl mType: GrantFiled: December 20, 2002Date of Patent: July 12, 2005Assignee: OSI Pharmaceuticals, Inc.Inventors: Arlindo Castelhano, Bryan McKibben, Arno Steinig, Eric Collington
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Patent number: 6908920Abstract: Compounds of formula (I), wherein R1, p, R2, q, R3 and R4 are defined within, and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described.Type: GrantFiled: July 6, 2001Date of Patent: June 21, 2005Assignee: AstraZeneca ABInventors: Andrew Peter Thomas, Nicholas John Newcombe, David William Heaton
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Patent number: 6867226Abstract: This invention provides a serotonin 5-HT3 receptor partial activator which has a serotonin 5-HT3 receptor activating action, in addition to its serotonin 5-HT3 receptor antagonism, and does not cause constipation as a side effect. Particularly, based on the finding that newly synthesized benzoxazole derivatives typified by the compounds of the following formula (2) have strong serotonin 5-HT3 receptor antagonism and serotonin 5-HT3 receptor activating action, this invention provides these benzoxazole derivatives as serotonin 5-HT3 receptor partial activators.Type: GrantFiled: August 16, 2002Date of Patent: March 15, 2005Assignee: Meiji Seika Kaisha, Ltd.Inventors: Yasuo Sato, Megumi Yamada, Kazuko Kobayashi, Katsuyoshi Iwamatsu, Fukio Konno, Koichi Shudo
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Patent number: 6849660Abstract: Provided are antibacterial compounds having Formula I: In such compositions, X is O or S; Y is CH2; n is 0 or 1. One of R1 and R1? is —C(O)NR5R5?, —C(O)—Q—NR5R5?, —CH2NR5R5? or —S(O)2NR5R5? and the other is H or R3. One of R2 and R2? is —NHC(O)R6 or —NHS(O)2R6 and the other is H or R4. Q is an amino acid or peptide. R3 is H, halogen, —NR5R5? or —NHC(O)R6; and R4 is selected from the group consisting of H, halogen, hydroxyl, amino, carboxyl, alkyl, alkenyl and alkynyl. R5 is selected from the group consisting of H, alkyl, alkenyl or alkynyl optionally substituted with halogen, OH, amino, amidinyl, guanidinyl, urea, alkyl, carboxyl, oxo, carboxamide; R5? is H or R5 and R5? together form a 5-16 member heterocycle optionally substituted with halogen, OH, amino, alkyl, carboxyl, carbonyl or carboxamide.Type: GrantFiled: August 1, 2000Date of Patent: February 1, 2005Assignee: ISIS Pharmaceuticals, Inc.Inventors: Elizabeth Jefferson, Eric Swayze
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Publication number: 20040180880Abstract: The present invention relates to piperazine and piperidine derivatives, which are especially useful for treating or preventing neuronal damage, particularly damage associated with neurological diseases. These compounds are also useful for stimulating nerve growth. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage or for stimulating nerve growth.Type: ApplicationFiled: October 2, 2003Publication date: September 16, 2004Inventors: David J. Lauffer, Martyn C. Botfield, Eckard Ottow
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Patent number: 6767907Abstract: 4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH2 and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9 is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10 and R11 are hydrogen, alkyl or aryl, or R10 and R11 are linked to form a ring; R2 is hydrogen, alkyl, cykcloalkyl or cycloalkylalkyl; or R1 and R2 are linked to form a ring; R3-R5 are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6 and R7 are hydrogen or alkyl or they are linked to constitute 3-7 membered ring; R8 is hydrogen or alkyl; have effects at cType: GrantFiled: April 14, 2000Date of Patent: July 27, 2004Assignee: H. Lundbeck A/SInventors: Jens Kristian Perregaard, John Willie Stenberg, Bitten Hansen
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Publication number: 20040142926Abstract: Compounds of the formula I: 1Type: ApplicationFiled: September 10, 2003Publication date: July 22, 2004Inventors: Deborah Ann Evrard, Dahui Zhou, Gary Paul Stack, Aranapakam Madumbai Venkatesan, Amedeo A. Failli, Susan Christman Croce
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Patent number: 6756380Abstract: Compounds of the general formula are described: wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R3 is halogen, trifluoromethyl, lower alkoxy or lower alkyl; R4/R4′are each independently hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, hydroxy, hydroxy-lower alkyl, —(CH2)n-piperazinyl, optionally substituted by lower alkyl, —(CH2)n-morpholinyl, —(CH2)n+1-imidazolyl, —O—(CH2)n+1-morpholinyl, —O—(CH2)n+1-piperidinyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, —NH—(CH2)n+1N(R4″)2, —(CH2)n—NH—(CH2)n+1N(R4″)2, —(CH2)n+1N(R4″)2, or —O—(CH2)n+1N(R4″)2, wherein R4″ is hydrogen or lower alkyl; R6 is hydrogen; R2 and R6 or R1 and R6 may together be —CH═CH—CH═CH—, wherein R2 and R6 or R1 and R6, respectively, together with the two carbon rinType: GrantFiled: May 22, 2000Date of Patent: June 29, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bös, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler
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Patent number: 6713474Abstract: Chemical compounds having structural formula I and physiologically acceptable salts and metabolites thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the kinases, whose activity is inhibited by these chemical compounds, are involved in immunologic, hyperproliferative, or angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferation is a factor. These compounds can be used to treat cancer and hyper proliferative disorders, rheumatiod arthritis, disorders of the immune system, trasplant rejections and imflammatory disorders.Type: GrantFiled: March 29, 2000Date of Patent: March 30, 2004Assignee: Abbott GmbH & Co. KGInventors: Gavin C. Hirst, David Calderwood, Rainer Munschauer, Lee D. Arnold, David N. Johnston, Paul Rafferty
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Publication number: 20040058931Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure 1Type: ApplicationFiled: November 15, 2002Publication date: March 25, 2004Inventors: John Lloyd, Heather J. Finlay, Wayne Vaccaro, Karnail S. Atwal, Michael F. Gross, Kerry L. Spear
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Patent number: 6602874Abstract: A compound of the formula wherein X, Y, Z, R2 and R3 are as defined above, useful in treating or preventing migraine, depression and other disorders for which a 5-HT1, agonist or antagonist is indicated.Type: GrantFiled: May 22, 2001Date of Patent: August 5, 2003Assignee: Pfizer Inc.Inventor: Harry R. Howard
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Patent number: 6552057Abstract: This invention provides a serotonin 5-HT3 receptor partial activator which has a serotonin 5-HT3 receptor activating action, in addition to its serotonin 5-HT3 receptor antagonism, and does not cause constipation as a side effect. Particularly, based on the finding that newly synthesized benzoxazole derivatives typified by the compounds of the following formula (2) have strong serotonin 5-HT3 receptor antagonism and serotonin 5-HT3 receptor activating action, this invention provides these benzoxazole derivatives as serotonin 5-HT3 receptor partial activators.Type: GrantFiled: March 2, 2001Date of Patent: April 22, 2003Assignee: Meiji Seika Kaisha, Ltd.Inventors: Yasuo Sato, Megumi Yamada, Kazuko Kobayashi, Katsuyoshi Iwamatsu, Fukio Konno, Koichi Shudo
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Patent number: 6537995Abstract: A method is provided for treating or preventing a disorder or condition selected from hypertension, depression, generalized anxiety disorder, phobias, posttraumatic stress syndrome, avoidant personality disorder, premature ejaculation, eating disorders, obesity, cluster headache, migraine, pain, obsessive-compulsive disorder, panic disorder, endocrine disorders, vasospasm, cerebellar ataxia, gastrointestinal tract disorders, premenstrual syndrome, fibromyalgia syndrome, stress incontinence, chronic paroxysmal hemicrania and headache in a mammal, comprising administering to a mammal in need of such treatment or prevention an amount of a compound of the formula (I) or the pharmaceutically acceptable salt thereof; wherein X, Y, Z, R2 and R3 are as defined herein.Type: GrantFiled: May 22, 2001Date of Patent: March 25, 2003Assignee: Pfizer Inc.Inventor: Harry R. Howard
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Patent number: 6440965Abstract: The present invention relates to novel derivatives of a series of substituted pyrimidines, to pharmaceutical compositions which contain them, to methods for their preparation and to their use in therapy, particularly in the treatment of neurodegenerative or other neurological disorders of the central and peripheral systems.Type: GrantFiled: April 14, 2000Date of Patent: August 27, 2002Assignee: Krenitsky Pharmaceuticals, Inc.Inventors: James L. Kelley, Thomas A. Krenitsky, Lilia M. Beauchamp
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Publication number: 20020037900Abstract: The invention encompasses novel compounds which are inhibitors of matrix metalloproteinase, ADAM or ADAM-TS enzymes, and which are useful for the treatment of diseases mediated by those enzymes, including degenerative diseases and certain cancers.Type: ApplicationFiled: May 15, 2001Publication date: March 28, 2002Inventors: Duncan Robert Hannah, Hazel Joan Dyke, Andrew Sharpe, Andrew Douglas Baxter