Additional Hetero Ring Attached Directly Or Indirectly To The Purine Ring System By Nonionic Bonding Patents (Class 514/263.2)
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Publication number: 20100239522Abstract: A method of treating cancer in a subject in need thereof comprises administering said subject reserpine, yohimbine, an analog thereof, or a pharmaceutically acceptable salt or prodrug thereof, in an amount effective to treat the cancer. Compounds and compositions useful for carrying out the method are also described.Type: ApplicationFiled: February 24, 2010Publication date: September 23, 2010Inventors: Freddie R. Salsbury, JR., Karin D. Scarpinato, S. Bruce King
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Patent number: 7795269Abstract: Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.Type: GrantFiled: December 3, 2007Date of Patent: September 14, 2010Assignee: Gilead Palo Alto, Inc.Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
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Patent number: 7795268Abstract: The invention is related to methods of treating hepatic fibrosis using A2B adenosine receptor antagonists and utility in the treatment of liver damage caused by alcohol abuse, surgical intervention, viral hepatitis, the ingestion of hepatotoxic drugs, or other hepatic diseases.Type: GrantFiled: March 16, 2007Date of Patent: September 14, 2010Assignee: Gilead Palo Alto, Inc.Inventors: Dewan Zeng, Hongyan Zhong, Luiz Belardinelli
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Patent number: 7790730Abstract: The present invention relates to pharmaceutical compositions for the treatment or prevention of viral infections comprising as an active principle at least one compound having the general formula (A): wherein U is N or C; X is selected from C1-C10 alkylene, C2-10 alkenylene or C2-10 alkynylene, where each may include one or more intrachain heteroatoms selected from O, S, or NR11, provided any such heteroatom is not adjacent to the N in the ring; R3 is selected from aryl, aryloxy, arylthio, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl-N(R10)—, or heterocycle, where each said substituent is optionally substituted with at least one R17, provided that for cycloalkenyl the double bond is not adjacent to a nitrogen; and the other substituents are described in the specification.Type: GrantFiled: July 26, 2005Date of Patent: September 7, 2010Assignees: Gilead Sciences, Inc., K.U. Leuven Research & DevelopmentInventors: Choung U. Kim, Johan Neyts, David A. Oare, Gerhard Puerstinger
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Publication number: 20100222300Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.Type: ApplicationFiled: May 10, 2010Publication date: September 2, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
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Publication number: 20100216821Abstract: The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salts, solvates, stereoisomers thereof, R1 may be C1-C4 alkyl, aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; R2 may be halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano, nitro; or aryl, heteroaryl or heterocycle, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or R2 may correspond to —O—R3; R3 is a 6-membered aromatic carbocyclic ring which may contain 1 or 2 nitrogen X is carbon or oxygen; Z is carbon or nitrogen; G is a fused 6-membered aromatic carbocyclic ring which may contain 1 or 2 nitrogen; m may be 0 or an integer ranging from 1 to 4; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY-Y5 receptor antagonists.Type: ApplicationFiled: April 18, 2008Publication date: August 26, 2010Inventors: Nicholas Paul Barton, Benjamin Richard Bellenie, Jonathan Bentley, Matteo Biagetti, Thorsten Genski, Colin Philip Leslie, Angelica Mazzali, Domenica Antonia Pizzi, Fabio Maria Sabbatini, Catia Seri
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Patent number: 7781432Abstract: Analogs or derivatives of nitrobenzylthioinosine corresponding to formula I: in which R represents an unsubstituted or mono- or polysubstituted phenyl, benzyl or heteroaryl group or a phenyl group condensed with heteroaryl, and R? represents an unsubstituted or mono- or polysubstituted NH—C1-6-alkyl, NH-aryl, NH-heteroaryl, NH—C3-8-cycloalkyl, NH—C1-3-alkyl-aryl, NH—C1-3-alkyl-heteroaryl, N(C1-6-alkyl)2, N(C1-3-alkyl-aryl)2, N(C1-3-alkyl-heteroaryl)2, piperidine, piperazine, morpholine or pyrrolidine group; pharmaceutical compositions comprising such analogs or derivatives, and the use of such analogs or derivatives for treating pain and/or various other diseases.Type: GrantFiled: December 29, 2006Date of Patent: August 24, 2010Assignees: Gruenenthal GmbH, Leiden UniversityInventors: Adriaan Pieter Ijzermann, Reynier Tromp
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Publication number: 20100210598Abstract: Provided herein are small molecule conjugates that are agonists or antagonists of one or more toll-like receptors.Type: ApplicationFiled: February 11, 2010Publication date: August 19, 2010Applicant: Regents of the University of California, San DiegoInventors: Dennis A. Carson, Howard B. Cottam, Tomoko Hayashi, Michael Chan
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Publication number: 20100204250Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: April 27, 2010Publication date: August 12, 2010Applicant: Boehringer Ingelheim Pharma & Co. KGInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
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Publication number: 20100203146Abstract: The present invention provides methods of treating rheumatoid arthritis. The methods generally involve an intermittent dosing strategy for administering Atiprimod alone or in combination with a second therapeutic agent wherein the second therapeutic agent is selected from the group consisting of Methotrexate, gold compounds, antimalarials, cyclosporine A, leflunomide, azathioprine, sulfasalazine d-penicillamine, aurothioglucose, auranofin, or a TNF inhibitor.Type: ApplicationFiled: February 9, 2010Publication date: August 12, 2010Applicant: Callisto Pharmaceuticals, Inc.Inventor: Gary S. Jacob
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Patent number: 7772226Abstract: The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.Type: GrantFiled: August 28, 2008Date of Patent: August 10, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Seiji Yoshikawa, Eita Emori, Fumiyoshi Matsuura, Richard Clark, Hironori Ikuta, Kazunobu Kira, Nobuyuki Yasuda, Tadashi Nagakura, Kazuto Yamazaki
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Patent number: 7767670Abstract: The invention provides methods and compositions for treating conditions mediated by various kinases wherein substituted 3-carboxamido isoxazoles compounds are employed. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.Type: GrantFiled: November 15, 2004Date of Patent: August 3, 2010Assignee: Ambit Biosciences CorporationInventors: Shamal A. Mehta, Robert M. Grotzfeld, Zdravko V. Milanov, Andiliy G. Lai, Hitesh K. Patel, David J. Lockhart
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Patent number: 7767685Abstract: The present invention provides compounds of the formula which are adenosine A2B receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2B receptor activity. Such conditions include, but are not limited to, chronic and acute inflammatory diseases involving degranulation of mast cells, e.g., asthma, allergic rhinitis and allergic dermatitis; impaired sensitivity to insulin, e.g., type 2 diabetes, pre-diabetic state, and impaired glucose tolerance; diseases in which angiogenesis is a key component of pathogenesis, e.g., solid tumors and angiogenic retinopathies; apnea of preterm infants; myocardial reperfusion injury; inflammatory bowel disease; autoimmune diseases, such as rheumatoid arthritis, multiple sclerosis, and lupus erythematosis; diseases involving microvascular abnormalities of the retina that are mediated by adenosine A2B receptors, e.g.Type: GrantFiled: June 25, 2007Date of Patent: August 3, 2010Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Allan Moorman, Mojgan Aghazadeh Tabrizi
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Publication number: 20100189683Abstract: This invention relates to pulsatile dose administration of gossypol or pharmaceutical compositions thereof for treating diseases, disorders and conditions responsive to gossypol, inhibiting the activity of anti-apoptotic Bcl-2 family proteins, inducing apoptosis in cells and increasing the sensitivity of cells to inducers of apoptosis.Type: ApplicationFiled: December 10, 2009Publication date: July 29, 2010Applicant: Ascenta Therapeutics, Inc.Inventors: Jon T. Holmlund, Mel Sorensen, Lance Leopold, Dajun Yang
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Patent number: 7763625Abstract: A method for treating migraine comprising administering, as an active ingredient, a xanthine derivative represented by the following formula or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 28, 2005Date of Patent: July 27, 2010Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Megumi Takeuchi, Makoto Takayama, Shiro Shirakura, Hiroshi Kase
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Publication number: 20100183564Abstract: The present invention relates to compounds and compositions for expanding the number of CD34+ cells for transplantation. The invention further relates to a cell population comprising expanded hematopoietic stem cells (HSCs) and its use in autologous or allogeneic transplantation for the treatment of patients with inherited immunodeficient and autoimmune diseases and diverse hematopoietic disorders to reconstitute the hematopoietic cell lineages and immune system defense.Type: ApplicationFiled: October 29, 2009Publication date: July 22, 2010Applicant: IRM LLCInventors: Anthony E. Boitano, Michael Cooke, Shifeng Pan, Peter G. Schultz, John Tellew, Yongqin Wan, Xing Wang
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Patent number: 7759355Abstract: The present invention provides methods of treating restless legs syndrome or related disorders, comprising administering an effective amount of at least one adenosine A2A receptor antagonist to a patient in need thereof. More preferably the adenosine A2A receptor antagonist is a xanthine derivative or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 27, 2003Date of Patent: July 20, 2010Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Hiroshi Kase, Naoki Seno, Akihisa Mori, Dayao Zhao
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Publication number: 20100179128Abstract: The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for the manufacture of said derivatives, pharmaceutical formulations containing these active compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficialType: ApplicationFiled: August 8, 2006Publication date: July 15, 2010Inventors: Richard Jonathan Daniel Hatley, Jag Paul Heer, John Liddle, Andrew McMurtrie Mason, Ivan Leo Pinto, Shahzad Sharooq Rahman, Ian Edward David Smith
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Patent number: 7754728Abstract: A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.Type: GrantFiled: September 26, 2003Date of Patent: July 13, 2010Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Yoshiaki Isobe, Haruo Takaku, Haruhisa Ogita, Masanori Tobe, Ayumu Kurimoto, Tetsuhiro Ogino, Hitoshi Fujita
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Publication number: 20100173916Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are defined as in claim 1, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: March 16, 2010Publication date: July 8, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
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Publication number: 20100168122Abstract: The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for manufacture of said derivatives, pharmaceutical formulations containing these compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficialType: ApplicationFiled: August 8, 2006Publication date: July 1, 2010Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Richard Jonathan Daniel Hatley, Andrew McMurtrie Mason, Ivan Leo Pinto
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Publication number: 20100160352Abstract: Novel adenine derivatives of the formula (I), in which R1, R2, R3, X and Y have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: July 20, 2006Publication date: June 24, 2010Applicant: MERCK PATENT GMBHInventors: Hans-Peter Buchstaller, Hans-Michael Eggenweiler, Bertram Cezanne, Michael Wolf
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Patent number: 7741331Abstract: Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.Type: GrantFiled: December 5, 2007Date of Patent: June 22, 2010Assignee: Gilead Palo Alto, Inc.Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
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Publication number: 20100152210Abstract: This invention relates to novel purinyl derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.Type: ApplicationFiled: March 27, 2008Publication date: June 17, 2010Applicant: NEURO SEARCH A/S/Inventors: Birgitte L. Eriksen, Ulrik Svane Sørensen, Charlotte Hougaard, Dan Peters, Tina Holm Johansen, Palle Christophersen
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Publication number: 20100143499Abstract: Compounds, compositions, and methods of using such compounds to modulate apoptosis including IAP antagonists are provided herein. Compositions including mimetics of the invention and, optionally, secondary agents, may be used to treat proliferative disorders such as, cancer and autoimmune diseases.Type: ApplicationFiled: July 24, 2007Publication date: June 10, 2010Applicant: TETRALOGIC PHARMACEUTICALS CORPORATIONInventor: Stephen M. Condon
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Publication number: 20100144705Abstract: Provided herein are electrophilically enhanced kinase inhibitors. Also provided herein are methods of making and utilizing the same.Type: ApplicationFiled: December 5, 2008Publication date: June 10, 2010Applicant: Principia Biopharma Inc.Inventor: Richard MILLER
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Publication number: 20100143347Abstract: The present invention concerns protection of an organ or tissue following an ischemic episode In particular aspects, the invention concerns organ preservation for transplantation, angina pectoris, kidney reperfusion injury, and so forth In specific embodiments, the organ is subjected to an inhibitor of an NCCa-ATP channel that is regulated by SUR1 Exemplary inhibitors include sulfonylurea compounds, such as glibenclamide, for exampleType: ApplicationFiled: January 11, 2008Publication date: June 10, 2010Inventor: J. Marc Simard
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Patent number: 7732455Abstract: Selective antagonists of A2B adenosine receptors like those of formula I are provided. These compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: December 14, 2007Date of Patent: June 8, 2010Assignee: PGx Health, LLCInventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
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Publication number: 20100130498Abstract: The present invention relates to agonists of the human bitter-taste receptors hTAS2R14, hTAS2R10 and hTAS2R4 and their role in bitter taste transduction. The invention also relates to methods for identifying molecules that modulate, e.g. suppress, or enhance hTAS2R14, hTAS2R10 and hTAS2R4 bitter taste transduction or bitter taste response.Type: ApplicationFiled: March 31, 2008Publication date: May 27, 2010Applicant: Deutshes Institut Fur Ernahrungsforschung Potsdam- RehbruckeInventors: Maik Behrens, Anne Brockhoff, Christina Kuhn, Wolfgang Meyerhof, Giovanni Appendino
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Publication number: 20100130516Abstract: This invention relates to novel purinyl derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.Type: ApplicationFiled: March 27, 2008Publication date: May 27, 2010Applicant: NeuroSearch A/SInventors: Birgitte L. Eriksen, Ulrik Svane Sørensen, Charlotte Hougaard, Dan Peters, Palle Christophersen
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Publication number: 20100130491Abstract: The present invention provides compounds of formula (I) wherein R1, Y1, X1, L and R2 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: March 19, 2008Publication date: May 27, 2010Inventors: Roger Victor Bonnert, Thomas Mcinally, Stephen Thom
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Patent number: 7723340Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.Type: GrantFiled: January 12, 2006Date of Patent: May 25, 2010Assignees: Signal Pharmaceuticals, LLC, Pharmacopeia Drug Discovery, Inc.Inventors: Ronald J. Albers, Leticia Ayala, Steven S. Clareen, Maria Mercedes Delgado Mederos, Robert Hilgraf, Sayee G. Hegde, Kevin Hughes, Adam Kois, Veronique Plantevin-Krenitsky, Meg McCarrick, Lisa Nadolny, Moorthy S. S. Palanki, Kiran Sahasrabudhe, John Sapienza, Yoshitaka Satoh, Marianne K. Sloss, Elise Sudbeck, Jonathan Wright, Ian Henderson, Andrew G. Cole
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Publication number: 20100105705Abstract: This invention relates to novel purinyl derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.Type: ApplicationFiled: March 27, 2008Publication date: April 29, 2010Applicant: NeuroSearch A/SInventors: Birgitte L. Eriksen, Ulrik Svane, Charlotte Hougaard, Dan Peters, Tina Holm Johansen, Palle Christophersen
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Publication number: 20100093768Abstract: The present invention provides methods for discovering agents that are effective in reversing epigenetic silencing by inhibiting the interaction of methyl-binding (MBD) proteins with methylated genomic DNA. Also provided are methods for reactivating silenced genes having CpG island hypermethylation along with methods for treatment and prevention of diseases, such as cancer and sickle cell anemia, by administering an agent that modulates methyl-binding domain (MBD) protein-mediated transcriptional repression, thereby increasing gene transcription to prevent or treat disease. Additionally, compounds identified by the present invention useful for treatment and prevention of diseases, such as cancer and sickle cell anemia, are provided.Type: ApplicationFiled: December 21, 2007Publication date: April 15, 2010Inventors: William G. Nelson, Srinivasan Yegnasubramanian, Xiaohui Lin, Traci J. Speed, Zachery Reichert
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Publication number: 20100093717Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of treating or inhibiting angiogenesis in a subject in need thereof and methods for blocking, occluding, or otherwise disrupting blood flow in neo vasculature, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: August 14, 2007Publication date: April 15, 2010Inventors: Weiwen Ying, Kevin Foley
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Publication number: 20100069360Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the groups R1, R2, R3, R7 and X are as defined in the specification.Type: ApplicationFiled: August 28, 2007Publication date: March 18, 2010Inventors: Laszlo Revesz, Achim Schlapbach, Rudolf Walchli
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Publication number: 20100061984Abstract: Methods of treating autoimmune disorders, coronary artery disease, allergy symptoms, allograft rejection sepsis/toxic shock are disclosed. Some methods comprise administering one or more regulatory compositions to activate the T suppressor cells by increasing the acetylation level and/or protein level of FOXP3 in combination with a T suppressor stimulus and/or an antigen. Some methods comprise administering one or more regulatory compositions to activate the T suppressor cells by increasing the acetylation level and/or protein level of FOXP3. Some methods comprise administering soluble GITR or antibodies that bind to GITR ligand. Methods of treating cancer, infectious diseases, and immune deficiency are also disclosed as are vaccination methods. The methods comprise administering one or more regulatory compositions to inactivate the T suppressor cells by reducing the acetylation level and/or protein level of FOXP3. Improved vaccines and vaccination methods are disclosed.Type: ApplicationFiled: January 22, 2007Publication date: March 11, 2010Applicants: The Trustees of the University of Pennsylvania, The Children's Hospital of PhiladelphiaInventors: Mark L. Greene, Sandra W. Saouaf, Bin Li, Hongtao Zhang, Wayne Hancock
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Publication number: 20100056494Abstract: The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with kinase activity, particularly malaria.Type: ApplicationFiled: January 10, 2008Publication date: March 4, 2010Applicants: IRM LLC, THE SCRIPPS RESEARCH INSTITUTEInventors: Elizabeth Winzeler, Nathanael S. Gray, Dong Han, Dai Cheng
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Publication number: 20100055094Abstract: The invention provides combinations of an ancillary compound and a compound which is a salt of 1-cyclopropyl-3-[3-(5-morpholin-4-ylmethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea selected from the lactate and citrate salts and mixtures thereof. Also provided are crystalline forms of the salts, methods for making the salts and their uses in treating cancers. The invention further provides combinations of an ancillary compound and a compound of the formula (I) as defined in PCT/GB2004/002824 (WO 2005/002552) or a compound of the formula (I?) or a salt, solvate, tautomer or N-oxide thereof, wherein R1, E, A and M are as defined in the claims.Type: ApplicationFiled: June 29, 2007Publication date: March 4, 2010Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Jayne Elizabeth Curry, Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson
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Patent number: 7662827Abstract: Compounds of the formula (I), in which R, X, R1, R2, R3 and R4 have the meanings indicated in Claim (1), are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: July 24, 2006Date of Patent: February 16, 2010Assignee: Merck Patent GmbHInventors: Guenter Hoelzemann, Helene Crassier, Wilfried Rautenberg
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Patent number: 7659278Abstract: The present invention provides novel compounds, corresponding to formulae I and II, respectively, which are able to reactivate the apoptosis-inducing function of mutant p53 proteins. This reactivation is provided by restoration of sequence-specific DNA-binding activity and transcriptional transactivation function to mutant p53 proteins, and modulation of the conformation-dependent epitopes of the p53 protein. Accordingly, the substances according to the invention will be used in pharmaceutical compositions and methods for treatment of patients suffering from various types of tumours.Type: GrantFiled: February 7, 2003Date of Patent: February 9, 2010Assignee: Aprea ABInventors: Vladimir Bykov, Galina Selivanova, Klas Wiman
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Patent number: 7642267Abstract: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I. The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.Type: GrantFiled: November 19, 2007Date of Patent: January 5, 2010Assignee: Neurogen CorporationInventors: Guiying Li, Pamela Albaugh, Kevin S. Currie, Guolin Cai, Linda M. Gustavson, Kyungae Lee, Alan Hutchison, George D. Maynard, Jun Yuan, Ling Hong Xie, Manuka Ghosh, Nian Liu, George P. Luke, Scott Mitchell, Martin Patrick Allen, Spiros Liras
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Publication number: 20090318445Abstract: The invention relates to novel compounds that are inhibitors of peptidyl deformylase (PDF). The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and uses of the compounds are also disclosed.Type: ApplicationFiled: December 28, 2006Publication date: December 24, 2009Applicants: NORVARTIS AG, NOVARTIS PHARMA GMBHInventors: Arkadius Pichota, Jeyaraj Duraiswamy, Zheng Yin, Thomas Hugo Keller, Mark Schreiber
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Publication number: 20090312320Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.Type: ApplicationFiled: August 12, 2009Publication date: December 17, 2009Inventors: Ronald J. Albers, Leticia Ayala, Steven S. Clareen, Maria Mercedes Delgado Mederos, Robert Hilgraf, Sayee G. Hegde, Kevin Hughes, Adam Kois, Veronique Plantevin-Krenitsky, Meg McCarrick, Lisa Nadolny, Moorthy S.S. Palanki, Kiran Sahasrabudhe, John Sapienza, Yoshitaka Satoh, Marianne K. Sloss, Elise Sudbeck, Jonathan Wright, Ian Henderson, Andrew G. Cole
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Publication number: 20090297619Abstract: Described are controlled release nanoparticulate formulations comprising a nanoparticulate agent to be administered and a rate-controlling polymer which functions to prolong the release of the agent following administration. The novel compositions release the agent following administration for a time period ranging from about 2 to about 24 hours or longer.Type: ApplicationFiled: June 11, 2009Publication date: December 3, 2009Inventors: Jon Swanson, Rajeev A. Jain, Robert Hontz, John G. Devane, Kenneth Iain Cumming, Maurice Joseph Anthony Clancy, Janet Elizabeth Codd, Gary G. Liversidge
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Publication number: 20090298744Abstract: Compounds of the present disclosure are fused pyrimidine compounds of formula (I), its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts thereof, as Adenosine receptor antagonists. Processes of their preparation are also described in the disclosure.Type: ApplicationFiled: March 26, 2009Publication date: December 3, 2009Applicant: ADVINUS THERAPEUTICS PVT. LTD.Inventors: Venkata Palle, Sujay Basu, Yogesh Waman, Vidya Ramdas, Dinesh Barawkar
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Patent number: 7625881Abstract: Disclosed are prodrugs of A2B adenosine receptor antagonists, having the following structure and their use in treating mammals for various disease states.Type: GrantFiled: June 14, 2006Date of Patent: December 1, 2009Assignee: Gilead Palo Alto, Inc.Inventors: Rao Kalla, Dmitry Koltun, Jeff Zablocki, Elfatih Elzein
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Publication number: 20090286813Abstract: There are disclosed novel compounds of Formula (I) wherein R1, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders, cardio- and cerebrovascular atherosclerotic disorders and peripheral artery disease and respiratory disorders.Type: ApplicationFiled: April 12, 2007Publication date: November 19, 2009Applicant: ASTRAZENECA ABInventors: Donald Pivonka, Anna-Karin Tiden, Jenny Viklund
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Patent number: 7618962Abstract: The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xanthines of formula I which are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: February 27, 2006Date of Patent: November 17, 2009Assignee: PGX Health, LLCInventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
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Publication number: 20090281075Abstract: A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKC? inhibitors, and their methods of use are disclosed.Type: ApplicationFiled: November 7, 2008Publication date: November 12, 2009Applicant: PHARMACOPEIA, INC.Inventors: Andrew L. Roughton, Yajing Rong, Koc-Kan Ho, Michael J. Ohlmeyer, David Diller, Ray Jui-Hsiang Chan, Gaifa Lai