The Additional Hetero Ring Is Five-membered Consisting Of Carbon And Plural Nitrogens As The Only Ring Members Patents (Class 514/266.23)
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Patent number: 8835458Abstract: Provided is a pharmaceutical composition comprising, as an active ingredient, a quinoline or quinazoline derivative of formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof, which is effective in the prevention and treatment of a cancer, inflammation, autoimmune diseases or neurodegenerative disorders which are induced by the overexpression of inhibitor of apoptosis proteins (IAPs).Type: GrantFiled: August 31, 2011Date of Patent: September 16, 2014Assignee: Hanmi Science Co., LtdInventors: In Hwan Bae, Eun Young Byun, Hae Kyoung Ju, Ji Young Song, Seung Hyun Jung, Seung Ah Jun, Ho Seok Kim, Young Hee Jung, Mi Yon Shim, Young Gil Ahn, Maeng Sup Kim
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Publication number: 20140249129Abstract: This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: February 20, 2014Publication date: September 4, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Christian GNAMM, Thorsten OOST, Stefan PETERS, Klaus RUDOLF
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Patent number: 8815849Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.Type: GrantFiled: July 26, 2011Date of Patent: August 26, 2014Assignee: Janssen R&D IrelandInventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
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Publication number: 20140228367Abstract: The present disclosure relates to compounds of the Formula (I): and pharmaceutically acceptable salts, as kinase modulators, compatible with the Type-II inhibition of kinases.Type: ApplicationFiled: February 5, 2014Publication date: August 14, 2014Inventor: Gary A. Flynn
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Publication number: 20140228362Abstract: The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of neuropathic pain, including mechanical hyperalgesia, thermal or mechanical allodynia, diabetic pain and entrapment pain, in vertebrate animals and particularly in human subjects. The AT2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of neuropathic conditions.Type: ApplicationFiled: March 28, 2014Publication date: August 14, 2014Applicant: Spinifex Pharmaceuticals Pty LtdInventors: Maree Therese Smith, Bruce Douglas Wyse
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Patent number: 8796263Abstract: Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.Type: GrantFiled: August 12, 2011Date of Patent: August 5, 2014Assignee: Janssen Pharmaceutica NVInventors: Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
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Patent number: 8796259Abstract: N3-Heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: October 4, 2012Date of Patent: August 5, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Pingyu Ding, Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Joane Litvak
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Publication number: 20140206688Abstract: Disclosed are compounds having the formula (Formula I)): wherein R1, R2, R3 and Z are as defined herein, and methods of making and using the same.Type: ApplicationFiled: August 17, 2012Publication date: July 24, 2014Inventors: Michael Jonathan Bury, Linda N. Casillas, Adam K. Charnley, Michael P. Demartino, Xiaoyang Dong, Patrick M. Eidam, Pamela A. Haile, Robert W. Marquis, JR., Joshi M. Ramanjulu, Joseph J. Romano, Ami Lakdawala Shah, Robert R. Singhaus, JR., Gren Wang
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Publication number: 20140206676Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: January 12, 2013Publication date: July 24, 2014Applicant: Vanderbilt UniversityInventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
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Publication number: 20140206706Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: March 19, 2014Publication date: July 24, 2014Inventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
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Patent number: 8785459Abstract: A compound for treating protein kinase-related disease or disorder having a structure of formula (A): wherein X is N or CH; Y is NH, O, or CH2; Z is an aryl or a heteroaryl; and R1, R2, R3, and R4 are independently H, halo, nitro, cyano, aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, —ORa, —C(O)Ra, —C(O)NRaRb, —NRaC(O)Rb, —NRaRb, —S(O)2Ra, —S(O)2NRaRb, —NRaS(O)2Rb, —N?CRaRb, or —NRaC(O)NHRb, wherein each of Ra and Rb, independently, is H, alkyl, alkenyl, alkynyl, aryl, aryloxy, alkoxy, hydroxy, heteroaryl, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl, or Ra and Rb, together with the nitrogen atom to which they are bonded, form heteroaryl, heterocycloalkyl, or heterocycloalkenyl; or R3 and R4 are as defined above, and R1 and R2 together with the carbons, to which they are attached, form a heterocycloalkenyl or heteroaryl.Type: GrantFiled: December 27, 2011Date of Patent: July 22, 2014Assignee: Development Center for BiotechnologyInventors: Jiann-Jyh Huang, Chu-Bin Liao, Pao-Nien Chen
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Publication number: 20140200136Abstract: The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one pesticidal active 3-arylquinazolin-4-one compound I of formula (I): wherein R1, R2, R3, R4, k and n are defined in the description; and 2) at least one fungicidal compounds II selected from azoles, strobilurins, carboxamides, carbamates, heterocyclic and various other compounds as defined in the description, in synergistically effective amounts. The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes and harmful fungis in and on plants, and for protecting such plants being infested with pests, especially also for protecting seeds.Type: ApplicationFiled: August 31, 2012Publication date: July 17, 2014Applicant: BASF SEInventors: Florian Kaiser, Steffen Gross, Egon Haden, Arun Narine
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Publication number: 20140194449Abstract: Provided herein is an optically active pyrozolylaminoquinazaline, and pharmaceutical compositions thereof. Also provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a JAK-mediated condition, disorder, or disease. Further provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a proliferative disease, inflammatory disease, or renal disease.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicant: Ambit Biosciences Corp.Inventors: Mark W. HOLLADAY, Eduardo SETTI
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Patent number: 8772298Abstract: The present invention relates to spirocyclic heterocycles of general formula (I) the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways, and the preparation thereof.Type: GrantFiled: June 18, 2013Date of Patent: July 8, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Birgit Jung, Ralf Lotz
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Publication number: 20140187550Abstract: A compound of formula (I): in free or salt form, wherein R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.Type: ApplicationFiled: December 16, 2013Publication date: July 3, 2014Applicant: Novartis AGInventor: Roger John Taylor
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Publication number: 20140179673Abstract: The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts thereof, in which R1, R2, n, R3, R4, R5 and R6 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3K?. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3K?.Type: ApplicationFiled: December 20, 2013Publication date: June 26, 2014Applicant: GILEAD CALISTOGA LLCInventors: Jerry EVARTS, Leena PATEL, Jennifer A. TREIBERG, Stephane PERREAULT, Arthur YEUNG, Lafe J. PURVIS, II, Musong KIM
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Patent number: 8759363Abstract: Quinazoline derivatives are provided that specifically inhibit proliferation of T cells without affecting the level of IL-2 secreted from said T cells. These compounds as well as pharmaceutical composition comprising them are useful for the treatment of indications mediated by T cell proliferation.Type: GrantFiled: January 27, 2011Date of Patent: June 24, 2014Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.Inventors: Alexander Levitzki, Idit Sagiv
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Publication number: 20140163050Abstract: The invention concerns the use of competitive AMPA receptor antagonists for the treatment or prevention of photosensitive epilepsy.Type: ApplicationFiled: February 12, 2014Publication date: June 12, 2014Inventors: Donald JOHNS, Georges IMBERT, Klaus KUCHER
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Publication number: 20140161801Abstract: The invention relates to a quinazoline derivative represented by the general formula (I), a pharmaceutical acceptable salt and a stereoisomer thereof as tyrosine kinase inhibitor, wherein R1, R2, R3, R3?, R4, R5, R6, X, L, T, Z and q are as defined in the specification. The invention also relates to a process for preparing the same, a pharmaceutical composition and a pharmaceutical formulation containing the derivative, use of the derivative for treating excessive proliferative diseases and chronic obstructive pulmonary disease and use of the derivative in the manufacture of a medicament for treating excessive proliferative diseases and chronic obstructive pulmonary disease.Type: ApplicationFiled: May 28, 2012Publication date: June 12, 2014Applicant: XUANZHU PHARMA CO., LTD.Inventors: Frank Wu, Aichen Wang
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BRIDGED BICYCLIC ARYL AND BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
Publication number: 20140155386Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: December 2, 2013Publication date: June 5, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak -
Patent number: 8716492Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.Type: GrantFiled: December 15, 2011Date of Patent: May 6, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
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Publication number: 20140107138Abstract: A fungicidal composition containing, as active ingredients, (a) a benzoylpyridine derivative represented by the following formula or its salt: wherein X is a halogen atom, a nitro group, a substitutable hydrocarbon group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group, a hydroxyl group, a substitutable alkylthio group, a cyano group, a carboxyl group which may be esterified or amidated, or a substitutable amino group, n is 1, 2, 3 or 4; R1 is a substitutable alkyl group, R2? is a substitutable alkyl group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group or a hydroxyl group, p is 1, 2 or 3, and R2? is a substitutable alkoxy group or a hydroxyl group, provided that at least two of R2? and R2? optionally form a condensed ring containing an oxygen atom and (b) at least one other fungicide.Type: ApplicationFiled: December 20, 2013Publication date: April 17, 2014Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Hisaya Nishide, Shigeyuki Nishimura, Shigeru Mitani, Koji Minamida, Fumio Kanamori, Munekazu Ogawa, Shigehisa Kanbayashi, Toyoshi Tanimura, Koji Higuchi, Hidemasa Kominami, Tomohiro Okamoto, Akihiro Nishimura
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Publication number: 20140100213Abstract: This invention relates to the use of triazolone derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer.Type: ApplicationFiled: November 4, 2013Publication date: April 10, 2014Applicant: GlaxoSmithKline LLCInventors: Nicholas David Adams, Christopher Joseph Aquino, Amita M. Chaudhari, Jonathan Michael Chergurovich, Terence John Kiesow, Cynthia Ann Parrish, Alexander Joseph Reif, Kenneth Wiggall
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Publication number: 20140073642Abstract: This invention relates to quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy of disorders in which the modulation of toll-like-receptors is involved.Type: ApplicationFiled: May 18, 2012Publication date: March 13, 2014Applicant: Janssen R&D IrelandInventors: David McGowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers, Stefaan Julien Last, Werner Embrechts, Serge Maria Aloysius Pieters
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Patent number: 8653077Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.Type: GrantFiled: September 28, 2011Date of Patent: February 18, 2014Assignee: ICOS CorporationInventors: Chanchal Sadhu, Kennith O. Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
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Publication number: 20140037561Abstract: A composition is provided that capitalizes on the biological activity of trichloroacetic acid, but effectively reduces or eliminates TCA induced irritation allowing the composition to be used as a wrinkle effacer or stimulant of skin cell turnover; uses previously thought as commercially impossible with TCA. Also provided are processes of effacing wrinkles or stimulating skin cell turnover including applying the inventive composition to the skin of a subject.Type: ApplicationFiled: February 3, 2011Publication date: February 6, 2014Inventors: John E. Kulesza, Mark Rubin
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Publication number: 20140031358Abstract: The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts or prodrugs thereof, which inhibit the poly(ADP-ribose) polymerases (PARP) and therefore are useful for treating diseases, disorders, and conditions related to PARP. The present invention also discloses pharmaceutical compositions comprising a compound of formula (I), and methods of using such compounds to inhibit PARP enzymes, and to treat diseases, disorders, and conditions related to PARP.Type: ApplicationFiled: March 12, 2012Publication date: January 30, 2014Applicant: Eternity Bioscience Inc.Inventors: Dong Liu, Minsheng Zhang, Kan He, Lianshan Zhang
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Publication number: 20140024657Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: ApplicationFiled: September 20, 2013Publication date: January 23, 2014Applicant: President and Fellows of Harvard CollegeInventors: Junying YUAN, Emily S. Hsu
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Patent number: 8633210Abstract: This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.Type: GrantFiled: April 26, 2011Date of Patent: January 21, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Pan Li, Ronald Knegtel, Julian Marian Charles Golec, David Bebbington, Hayley Marie Binch
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Publication number: 20140018376Abstract: The invention concerns the use of competitive AMPA receptor antagonists for the treatment, prevention or delay of progression of Rasmussen's encephalitis and/or certain forms of epilepsy.Type: ApplicationFiled: October 20, 2010Publication date: January 16, 2014Inventors: Hans Allgeier, Yves Auberson, Thomas Blaettler, David Carcache, Philipp Floersheim, Wolfgang Froestl, Christel Guibourdenche, Hans o Kalkman, Joerg Kallen, Manuel Koller, Kurt Lingenhohl, Henri Mattes, Joachim Nozulak, David Orain, Johanne Renaud, Christine Strohmaier
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Publication number: 20130345222Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.Type: ApplicationFiled: May 17, 2013Publication date: December 26, 2013Inventors: Donald S. Karanewsky, Joseph R. Fotsing, Catherine Tachdjian, Melissa Arellano
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Publication number: 20130296320Abstract: Provided is a novel bicyclic compound which has an HSP90 inhibitory effect and a carcinostatic effect. Also provided is a pharmaceutical agent which is based on the HSP90 inhibitory effect and is useful in the prevention and/or treatment of a disease involving HSP90, particularly, cancer. The present invention provides a compound represented by the following general formula (I) or a salt thereof wherein at least one of X1, X2, X3, and X4 represents N or N-oxide and the rest thereof are the same or different and each represent C—R2; any one or two of Y1, Y2, Y3, and Y4 represent C—R4 and the rest thereof are the same or different and each represent CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R2 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R3 represents a hydrogen atom, —CO—R5 etc.; R4 represents a hydrogen atom, —CO—R6, —N(R7)(R8) etc.Type: ApplicationFiled: January 6, 2012Publication date: November 7, 2013Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Makoto Kitade, Satoshi Yamashita, Shuichi Ohkubo
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Publication number: 20130296332Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.Type: ApplicationFiled: July 1, 2013Publication date: November 7, 2013Inventors: Hans ALLGEIER, Yves AUBERSON, David CARCACHE, Philipp FLOERSHEIM, Christel GUIBOURDENCHE, Wolfgang FROESTL, Jörg KALLEN, Manuel KOLLER, Henri MATTES, Joachim NOZULAK, David ORAIN, Johanne RENAUD
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Publication number: 20130289044Abstract: The invention relates to aryl substituted quinazolines of Formula I, and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, A, and R1-R4 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: October 5, 2011Publication date: October 31, 2013Applicant: Purdue Pharma L.P.Inventors: R. Richard Goehring, Laykea Tafesse, Jiangchao Yao
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Publication number: 20130281461Abstract: The present invention relates to spirocyclic heterocycles of general formula (I) the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways, and the preparation thereof.Type: ApplicationFiled: June 18, 2013Publication date: October 24, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Birgit JUNG, Ralf LOTZ
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Publication number: 20130281398Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor.Type: ApplicationFiled: March 15, 2013Publication date: October 24, 2013Applicant: RVX Therapeutics Inc.Inventors: Kevin G. McLure, Peter R. Young
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Publication number: 20130281399Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor.Type: ApplicationFiled: March 15, 2013Publication date: October 24, 2013Applicant: RVX Therapeutics Inc.Inventors: Kevin G. McLure, Peter R. Young
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Patent number: 8551992Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.Type: GrantFiled: May 23, 2012Date of Patent: October 8, 2013Assignee: Neosome Life Sciences, LLCInventors: Laxman S. Desai, Srinivas Chittaboina
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Publication number: 20130261123Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: ApplicationFiled: December 16, 2011Publication date: October 3, 2013Inventors: Xicheng Sun, Jian Qiu, Adam Stout
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Publication number: 20130245014Abstract: Provided herein are quinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: October 4, 2012Publication date: September 19, 2013Applicant: Ambit Biosciences Corp.Inventors: Sunny Abraham, Qi Chao, Michael J. Hadd, Mark W. Holladay, Liu Gang, Eduardo Setti
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Publication number: 20130225614Abstract: Provided herein are 4-azolylaminoquinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: August 31, 2011Publication date: August 29, 2013Applicant: Ambit Biosciences CorporationInventor: Michael J. Hadd
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Publication number: 20130225580Abstract: Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.Type: ApplicationFiled: February 28, 2013Publication date: August 29, 2013Applicant: CHEMOCENTRYX, INC.Inventor: ChemoCentryx, Inc.
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Publication number: 20130225578Abstract: Provided herein are 7-cyclylquinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: August 31, 2011Publication date: August 29, 2013Applicant: AMBIT BIOSCIENCES CORPORATIONInventors: Michael J. Hadd, Mark W. Holladay, Martin W. Rowbottom
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Publication number: 20130225615Abstract: Provided herein are 2-cycloquinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: August 31, 2011Publication date: August 29, 2013Applicant: AMBIT BIOSCIENCES CORPORATIONInventor: Michael J. Hadd
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Publication number: 20130210805Abstract: This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.Type: ApplicationFiled: October 6, 2011Publication date: August 15, 2013Inventors: Robert G. Aslanian, Christopher W. Boyce, Robert D. Mazzola, JR., Brian A. McKittrick, Kevin D. McCormick, Anandan Palani, Jun Qin, Haiqun Tang, Dong Xiao, Younong Yu, John P. Caldwell, Elizabeth Helen Kelley, Hongjun Zhang, Phieng Siliphaivanh, Rachel N. MacCoss, Joey L. Methot, Jolicia Polivina Gauuan, Qin Jiang, Andrew J. Leyhane, Johny Biju, Li Dong, Xian Huang, Ning Shao, Wei Zhou, Pawan K. Dhondi
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Publication number: 20130203656Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: May 23, 2011Publication date: August 8, 2013Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Min Zhong, Leping Li
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Publication number: 20130178462Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.Type: ApplicationFiled: March 5, 2013Publication date: July 11, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Publication number: 20130172373Abstract: Provided are certain quinazoline compounds, compositions thereof and methods of use thereof. These quinazoline compounds can effectively inhibit the overexpression and/or overactivity of epidermal growth factor receptor (EGFR).Type: ApplicationFiled: May 25, 2011Publication date: July 4, 2013Applicant: Hutchison Medipharma LimitedInventors: Weihan Zhang, Wei-Guo Su, Haibin Yang, Yumin Cui, Yongxin Ren, Xiaoqiang Yan
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Publication number: 20130165458Abstract: A compound for treating protein kinase-related disease or disorder having a structure of formula (A): wherein X is N or CH; Y is NH, O, or CH2; Z is an aryl or a heteroaryl; and R1, R2, R3, and R4 are independently H, halo, nitro, cyano, aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, —ORa, —C(O)Ra, —C(O)NRaRb, —NRaC(O)Rb, —NRaRb, —S(O)2Ra, —S(O)2NRa Rb, —NRaS(O)2Rb, —N?CRaRb, or —NRaC(O)NHRb, wherein each of Ra and Rb, independently, is H, alkyl, alkenyl, alkynyl, aryl, aryloxy, alkoxy, hydroxy, heteroaryl, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl, or Ra and Rb, together with the nitrogen atom to which they are bonded, form heteroaryl, heterocycloalkyl, or heterocycloalkenyl; or R3 and R4 are as defined above, and R1 and R2 together with the carbons, to which they are attached, form a heterocycloalkenyl or heteroaryl.Type: ApplicationFiled: December 27, 2011Publication date: June 27, 2013Applicant: DEVELOPMENT CENTER FOR BIOTECHNOLOGYInventors: Jiann-Jyh Huang, Chu-Bin Liao, Pao-Nien Chen
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Patent number: 8470838Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.Type: GrantFiled: August 25, 2009Date of Patent: June 25, 2013Assignee: Cytokinetics, IncorporatedInventors: Jeffrey T. Finer, Gustave Bergnes, Whitney W. Smith, John C. Chabala, Bainian Feng