The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/510)
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Publication number: 20110060024Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: April 26, 2010Publication date: March 10, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Peter D.J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Djamel Numa
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Patent number: 7888336Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as spingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.Type: GrantFiled: September 18, 2008Date of Patent: February 15, 2011Assignee: Allergan, Inc.Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello
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Publication number: 20100324039Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.Type: ApplicationFiled: August 30, 2010Publication date: December 23, 2010Inventors: Michael Jones, David Gunn, John Howard Jones, Michael Van Zandt
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Publication number: 20100324105Abstract: Disclosed are methods of reducing serum glucose and triglyceride levels and for inhibiting angiogenesis, the methods comprising administration of substituted indolealkanoic acids to patients in need of such treatment. Also disclosed are such compounds useful in the treatment of angiogenesis, hyperglycemia, hyperlipidemia and chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds.Type: ApplicationFiled: August 30, 2010Publication date: December 23, 2010Inventors: Janet Sredy, Jorge Jacot
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Patent number: 7851625Abstract: Disclosed are processes for making 2, 3 disubstituted indole compounds such as compounds of general formula I comprised of the steps of a) reacting a bromoindole compound (i) with a dialkoxyl C1-5 borane in the presence of a ligand, a palladium catalyst and a base to make a compound of general formula (ii); or alternatively reacting compound (i) with a trialkyl magnesiate reagent, followed by treatment with a borate; b) reacting the product of step a with a R2-Hal where R2-Hal is defined herein.Type: GrantFiled: June 19, 2009Date of Patent: December 14, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Ahmad Khodabocus, Zhi-Hui Lu, Chris Hugh Senanayake, Hanxun Wei, Yongda Zhang
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Publication number: 20100280034Abstract: The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;Type: ApplicationFiled: December 28, 2007Publication date: November 4, 2010Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20100273850Abstract: Compounds of Formula I: I in which D1, D2, R1, R2, R7, R8 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.Type: ApplicationFiled: November 4, 2008Publication date: October 28, 2010Inventor: George A. Doherty
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Publication number: 20100240614Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as spingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.Type: ApplicationFiled: September 18, 2008Publication date: September 23, 2010Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello
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Patent number: 7799933Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R1, R2, R3, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: GrantFiled: December 6, 2007Date of Patent: September 21, 2010Assignee: Hoffman-La Roche Inc.Inventors: Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander
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Patent number: 7786146Abstract: This invention provides compounds of formula I where the dashed line represents an optional double bond; where R1 is phenyl, naphthyl, pyridyl, pyrimidyl, pyrrolyl, imidazolyl, pyrazyl, furyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, or isothiazolyl, optionally substituted, and other substituents are defined herein. Such compounds are potassium channel modulators.Type: GrantFiled: August 11, 2008Date of Patent: August 31, 2010Assignee: Valeant Pharmaceuticals InternationalInventors: Jean-Michel Vernier, Huanming Chen, Jianlan Song
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Patent number: 7781598Abstract: The invention relates to a novel process for the preparation of substituted indoles which are useful as therapeutic agents.Type: GrantFiled: January 9, 2006Date of Patent: August 24, 2010Assignee: AstraZeneca ABInventors: Philip Keegan, Eric Merifield, Duncan Gill
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Publication number: 20100189671Abstract: The present invention concerns the use of some indole amide derivatives as perfuming ingredients.Type: ApplicationFiled: July 29, 2008Publication date: July 29, 2010Inventor: Jean-Marc Gaudin
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Publication number: 20100179326Abstract: Compounds having high angiogenesis inhibiting activity useful as agents for effective treatment and prevention of diseases involving pathologic angiogenesis, e.g.Type: ApplicationFiled: March 23, 2010Publication date: July 15, 2010Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Hiroshi KOYANO, Atsushi Suda, Kousuke Aso, Kihito Hada, Miyuki Asai, Masami Hasegawa, Yasuko Sato
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Publication number: 20100167333Abstract: The present invention provides a metal chelator and methods that facilitate binding, detecting, monitoring and quantitating of heavy metal ions in a sample.Type: ApplicationFiled: December 11, 2009Publication date: July 1, 2010Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Kyle R. Gee, Jolene Bradford, Vladimir V. Martin
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Publication number: 20100144821Abstract: The invention is directed to compounds and methods for treating protein folder disorders. In certain embodiments the invention provides compounds and methods for treating neurodegenerative diseases such as Alzheimer's disease, tauopathy, cerebral amyloid angiopathy, Lewy body disease, dementia, Huntington's disease and prion-based spongiform encelopathy. The invention further provides compounds, methods and pharmaceutical compositions for inhibiting tau protein, A? protein or ?-synuclein protein aggregation.Type: ApplicationFiled: November 19, 2007Publication date: June 10, 2010Applicant: Queen's University at KingstonInventors: Michael D. Carter, Donald F. Weaver, Sheila Marie H. Jacobo, Erhu Lu, Fuye Gao
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Publication number: 20100137301Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.Type: ApplicationFiled: February 8, 2010Publication date: June 3, 2010Inventors: Michael Lee Jones, David Gunn, John Howard Jones, Michael C. Van Zandt
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Publication number: 20100137363Abstract: The present invention relates generally to substituted indoles and methods of using them.Type: ApplicationFiled: January 29, 2010Publication date: June 3, 2010Applicant: Wyeth LLCInventors: Baihua HU, James W. Jetter
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Publication number: 20100113777Abstract: A compound, or its salt, or a solvate thereof having a cPLA2 inhibiting activity having the formula (I): or a pharmaceutical composition, cPLA2 inhibitor and inhibitors of various lipid mediator production containing the same as active ingredients.Type: ApplicationFiled: March 28, 2008Publication date: May 6, 2010Applicant: Asubio Pharma Co., Ltd.Inventors: Toshiyuki Tomoo, Takashi Nakatsuka, Yasuhiro Hayashi, Toyoko Katayama
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Publication number: 20100087446Abstract: 2-Substituted indole derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: April 22, 2008Publication date: April 8, 2010Inventors: Prasun K. Chakravarty, Joseph L. Duffy, Min K. Park, Sriram Tyagarajan, Bishan Zhou
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Patent number: 7683091Abstract: The present invention relates generally to substituted indoles and methods of using them.Type: GrantFiled: August 16, 2006Date of Patent: March 23, 2010Assignee: WyethInventors: Baihua Hu, James W. Jetter
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Publication number: 20100069405Abstract: The present invention is directed to compounds and compositions for the treatment of neurological diseases that cause neurogenic and neuropathic pain, inflammatory diseases, renal ischaemia, cardiovascular disease and other pathologies caused by the presence of endogenous cannabinoids and or other substrates resulting from the metabolic activities of fatty acid amido hydrolase (FAAH). These compounds are represented by the formula (I): wherein A, n, R1, R7 and R8 are as defined herein.Type: ApplicationFiled: November 24, 2009Publication date: March 18, 2010Applicant: SANOFI-AVENTISInventors: Ahmed Abouabdellah, Regine Bartsch-Li, Christian Hoornaert, Antoine Ravet
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Patent number: 7678803Abstract: The current invention is directed toward compounds and pharmaceutically acceptable salts of Formula I wherein Q1 is CR1, Q2 is N, Q4 and Q5 are each CR1, Q3 is CR2, X1 is N or CRc, Y is CRc, X2 and X3 are each C(R5)(R6), R7 is O. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer The current invention is also directed toward pharmaceutical compositions comprising compounds of the invention.Type: GrantFiled: August 24, 2007Date of Patent: March 16, 2010Assignee: Serenex, Inc.Inventors: Kenneth He Huang, James Veal, Thomas Barta, Emilie D. Smith, Wei Ma, Andy Ommen
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Publication number: 20100056544Abstract: The potassium, sodium, ammonium, lysine, diethylamine, tromethamine (TRIS), piperazine, ethylenediamine and ethanolamine salt of a compound of general formula (I): wherein R1 is halo or cyano; R2 is C1-C4 alkyl; and R3 is quinolyl or phenyl substituted with methane sulfonyl; can be synthesised by a novel method and are substantially more soluble than the parent free acids in a range of solvents.Type: ApplicationFiled: March 22, 2007Publication date: March 4, 2010Applicant: Oxagen LimitedInventor: James Matthew Lovell
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Publication number: 20100035956Abstract: Compounds of general formula (I) wherein R is phenyl optionally substituted with one or more halo substituents; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.Type: ApplicationFiled: July 20, 2007Publication date: February 11, 2010Applicant: Oxagen LimitedInventors: Richard Edward Armer, Graham Michael Wynne, Colin Richard Dorgan, Peter David Johnson
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Patent number: 7632956Abstract: The use of indole carbamates as fragrance ingredients and fragrance applications comprising indole carbamates in an effective amount.Type: GrantFiled: September 29, 2005Date of Patent: December 15, 2009Assignee: Givaudan SAInventors: Felix Flachsmann, Jean-Pierre Bachmann
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Publication number: 20090275142Abstract: The invention provides compositions and methods for the detection of biological targets, (e.g. nucleic acids and proteins) by nucleic acid-templated chemistry, for example, by generating fluorescent polymethine dyes.Type: ApplicationFiled: February 24, 2009Publication date: November 5, 2009Inventors: Yumei Huang, James M. Coull
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Publication number: 20090247766Abstract: The invention relates to a nitrogen heterocycle compound of formula 1: Also disclosed are a method of synthesizing the compound and use of the compound for treating various diseases and conditions.Type: ApplicationFiled: March 27, 2009Publication date: October 1, 2009Applicant: University of Southern CaliforniaInventors: Nicos A. Petasis, Malgorzata Myslinska
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Patent number: 7592373Abstract: Compounds of formula (I) wherein A, B, b, W, X, Y, Z, R1, R2, and R3 have the meanings given in claim 1, pharmaceutical compositions these compounds, and methods of preventing or treating metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia, and diabetes using these compounds.Type: GrantFiled: December 23, 2004Date of Patent: September 22, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Thorsten Lehmann-Lintz, Ralf R. H. Lotz, Philipp Lustenberger, Stephan Georg Mueller, Gerald Juergen Roth, Klaus Rudolf, Marcus Schindler, Dirk Stenkamp, Leo Thomas
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Publication number: 20090192319Abstract: Methods for treating cognitive/attention deficit disorders in general using tetrahydroindolone derivatives and analogues, particularly tetrahydroindolone derivatives or analogues in which the tetrahydroindolone derivative or analogue is covalently linked to another moiety to form a bifunctional conjugate are disclosed. More specifically, methods and compositions for treating attention deficit disorder and attention deficit hyperactivity disorders in adults and children as well as mild cognitive impairment and dementia are provided.Type: ApplicationFiled: March 30, 2009Publication date: July 30, 2009Applicant: Spectrum Pharmaceuticals, Inc.Inventors: Alvin J. Glasky, David B. Fick, David Helton
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Publication number: 20090192195Abstract: Compounds of general formula (I) wherein W is chloro or fluoro; Z is a group SO2R1; wherein R1 is —C3-C8 cycloalkyl or heterocyclyl optionally substituted with one or more substituents chosen from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, and —O(CH2)p—O—(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.Type: ApplicationFiled: January 22, 2009Publication date: July 30, 2009Applicant: Oxagen LimitedInventors: Richard Edward Armer, Carole Eliane Andree Maillol, Colin Richard Dorgan, Graham Michael Wynne, Julia Vile
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Publication number: 20090191183Abstract: Disclosed herein are substituted indole cysteinyl leukotriene receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: July 29, 2008Publication date: July 30, 2009Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20090149662Abstract: An improved process for the preparation of substantially pure zafirlukast and pharmaceutical compositions thereof.Type: ApplicationFiled: December 4, 2008Publication date: June 11, 2009Inventors: Raghupathi Reddy Anumula, Goverdhan Gilla, Sampath Alla, Sreenivasulu Kurella, Janardana Sarma Ramachandra Kopparapu, Rama Krishna Venkata Medisetti, Srinivasula Reddy Maddula
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Publication number: 20090105474Abstract: The anthranilic acid derivative or the salt thereof represented by the general formula wherein R1 and R2 are hydrogen atom, or the like; R3 is a phenyl, cycloalkyl or bicyclic heterocyclic group which may be substituted, or the like; R4 is a phenyl, cycloalkyl or pyridyl group which may be substituted, or the like; X1 is an alkylene or alkenylene group which may be substituted or a bond; X2 is the general formula -X3-X4- or -X4-X3-, wherein X3 is a sulfur atom, an imino group or a bond, or the like; X4 means an alkylene or alkenylene group which may be substituted or a bond; is useful for a remedy such as rheumatoid arthritis, osteoarthritis and carcinoma, because it shows MMP-13 production inhibitory effect.Type: ApplicationFiled: March 14, 2006Publication date: April 23, 2009Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Yoichi Taniguchi, Eiji Hara, Hitoshi Akitsu, Hidehiko Tanaka, Shuzo Anzai
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Publication number: 20090036690Abstract: The use of indole carbamates as fragrance ingredients and fragrance applications comprising indole carbamates in an effective amount.Type: ApplicationFiled: September 29, 2001Publication date: February 5, 2009Inventors: Felix Flachsmann, Jean-Pierre Bachmann
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Publication number: 20090018338Abstract: The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.Type: ApplicationFiled: September 17, 2008Publication date: January 15, 2009Applicant: Oxagen LimitedInventors: David Middlemiss, Mark Richard Ashton, Edward Andrew Boyd, Frederick Arthur Brookfield, Michael George Hunter, Mark Whittaker, Chris Palmer, Eric R. Pettipher
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Publication number: 20080300243Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: February 24, 2006Publication date: December 4, 2008Inventors: Michael G. Kelly, John Kincaid, Matthew Duncton, Kiran Sahasrabudhe, Satyanarayana Janagani, Ravindra B. Upasani, Guoxian Wu, YunFeng Fang, Zhi-Liang Wei, Carl Kaub, Jianhua He
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Publication number: 20080221337Abstract: The present invention provides a process for producing an aromatic unsaturated compound of the formula (4) wherein Ar represents an optionally substituted aromatic group or an optionally substituted heteroaromatic group, and Y represents an electron withdrawing group, which comprises reacting (a) a compound of the formula (1) Ar—H??(1) wherein Ar has the same meaning as defined above with (b) a compound of the formula (2) wherein Y has the same meaning as defined above, and Z represents a lower alkoxy, or a compound of the formula (3) wherein Y and Z have the same meanings as defined above, in the presence of (c) an acid or a compound which generates a mineral acid by its hydrolysis.Type: ApplicationFiled: August 25, 2004Publication date: September 11, 2008Inventors: Weiqi Wang, Tetsuya Ikemoto
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Patent number: 7405236Abstract: This invention is directed to compounds of the formula (I): wherein one of R6, R7, R8 and R9 is and X, R1 to R12, m, n and o are as defined in the description, and pharmaceutically acceptable salts and/or esters thereof. The invention is also directed to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPAR? and/or PPAR? agonists.Type: GrantFiled: August 2, 2005Date of Patent: July 29, 2008Assignee: Hoffman-La Roche Inc.Inventors: Jean Ackermann, Johannes Aebi, Alfred Binggeli, Uwe Grether, Bernd Kuhn, Hans-Peter Maerki, Markus Meyer
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Patent number: 7365061Abstract: Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer.Type: GrantFiled: November 14, 2005Date of Patent: April 29, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Philip M. Sher, Gang Wu, Wei Meng, Alexandra A. Nirschl, William N. Washburn, Terry Stouch
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Patent number: 7355054Abstract: The invention relates to 1-(R1)-2-(R2)-3-(Y—X—NH-A- or Z-A-)-4,5,6,7-R)0-4-indoles, and their acid addition salts where the compounds are basic, wherein A is C1-4 alkylene, X is >CH2, >C?O or >C?S, and the other symbols have various defined values, and to pharmaceutical, skin-protective and cosmetic compositions which comprise them.Type: GrantFiled: January 11, 2005Date of Patent: April 8, 2008Assignee: Neurim Pharmaceuticals (1991) Ltd.Inventors: Nava Zisapel, Moshe Laudon
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Patent number: 7351719Abstract: The present invention relates to amide compounds of general formula I wherein the groups and residues A, B, b, W, X, Y, Z, R1, R2 and R3 have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one amide according to the invention. In view of the MCH receptor-antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.Type: GrantFiled: October 31, 2003Date of Patent: April 1, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Dirk Stenkamp, Stephan Georg Mueller, Gerald Juergen Roth, Philipp Lustenberger, Klaus Rudolf, Thorsten Lehmann-Lintz, Kirsten Arndt, Ralf Lotz, Martin Lenter, Heike-Andrea Wieland
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Publication number: 20070232682Abstract: The present invention provides novel compounds having the following general formula I wherein: A, B, X, Y, R1, R2, R3, R4, n, o and p are as defined in the specification. Such compounds are useful for treating a disease or condition selected from the group consisting of glaucoma, dry eye, angiogenesis, cardiovascular conditions or diseases and wound healing.Type: ApplicationFiled: March 23, 2007Publication date: October 4, 2007Applicant: ALLERGAN, INC.Inventors: Richard L. Beard, John E. Donello, Haiqing Yuan, Vidyasagar Vuligonda, Tien T. Duong
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Patent number: 7226942Abstract: Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer.Type: GrantFiled: November 14, 2005Date of Patent: June 5, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Philip M. Sher, Alexandra A. Nirschl, Wei Meng, Wllliam N. Washburn
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Patent number: 7223786Abstract: Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer.Type: GrantFiled: November 14, 2005Date of Patent: May 29, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Wei Meng, Philip M. Sher, Bruce A. Ellsworth, William N. Washburn
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Patent number: 7217706Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: May 15, 2007Assignee: Astellas Pharma Inc.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 7214704Abstract: Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer.Type: GrantFiled: November 14, 2005Date of Patent: May 8, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Gang Wu, Philip M. Sher
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Patent number: 7173129Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.Type: GrantFiled: June 7, 2004Date of Patent: February 6, 2007Assignee: Athero Genics, Inc.Inventors: Kimberly J. Worsencroft, Liming Ni, Zhihong Ye, Charles Q. Meng, M. David Weingarten, Jacob E. Simpson, James A. Sikorski
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Patent number: 7105564Abstract: The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them. A compound of the formula (I): wherein R1 is —CH2—CH?CH—CH2—CH2—CH2—COOR2 or —CH?CH—CH2—CH2—CH2—COOR2; R2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X1 and X3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, have a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor.Type: GrantFiled: March 2, 2000Date of Patent: September 12, 2006Assignee: Shionogi & Co., Ltd.Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu, Akinori Arimura
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Patent number: 7074782Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.Type: GrantFiled: August 21, 2003Date of Patent: July 11, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Ronald Knegtel, Michael Mortimore, David Kay, Julian M. C. Golec
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Patent number: RE41990Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.Type: GrantFiled: January 4, 2007Date of Patent: December 7, 2010Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, Dongfang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J. Sorensen, Aaron Balog, Kenneth A. Savin