Nitrogen Bonded Directly To The Pteridine Ring System Patents (Class 544/258)
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Patent number: 8633202Abstract: The present invention relates to stable crystalline (6S)—N(5)-formyl-5,6,7,8-tetrahydrofolic acid, commonly referred to as levofolinic acid, in essentially pure 6S diastereomeric form, and to a process for its preparation.Type: GrantFiled: March 21, 2012Date of Patent: January 21, 2014Assignee: GMT Fine Chemicals SAInventor: Pascal Jequier
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Patent number: 8629142Abstract: Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: GrantFiled: November 16, 2012Date of Patent: January 14, 2014Assignee: Gilead Sciences, Inc.Inventors: Manoj C. Desai, Randall L. Halcomb, Paul Hrvatin, Hon Chung Hui, Ryan McFadden, Paul A. Roethle, Hong Yang
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Patent number: 8618106Abstract: In one aspect, the invention provides compounds of Formula I or pharmaceutically acceptable salts thereof. In another aspect, the invention provides methods for treatment of diseases or disorders mediated by a protein kinase, comprising administering a therapeutically effective amount of a compound of this invention.Type: GrantFiled: August 24, 2012Date of Patent: December 31, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steve Durrant
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Publication number: 20130331376Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, E1, E2, R1, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: August 14, 2013Publication date: December 12, 2013Applicant: Elan Corporation, Inc.Inventors: Robert A. Galemmo, Dean R. Artis, Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Patent number: 8598172Abstract: Dihydropteridin-6-one derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: GrantFiled: November 26, 2008Date of Patent: December 3, 2013Assignee: Nerviano Medical Sciences S.r.l.Inventors: Michele Caruso, Italo Beria, Maria Gabriella Brasca, Helena Posteri, Gabriele Fachin
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Patent number: 8592577Abstract: A method of preparing a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and claims. Additionally, the present invention relates to compounds of Structural Formula (I), which are useful as inhibitors of protein kinase.Type: GrantFiled: March 20, 2012Date of Patent: November 26, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven Durrant, Michael O'Donnell
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Publication number: 20130310390Abstract: The present invention relates to substituted pterin compounds, their synthesis and use. In particular, the present invention relates to a new precursor compound and its analogs for synthesizing a new substituted pterin compound and its analogs. These new compounds are particularly suitable for treating molybdenum cofactor deficiency.Type: ApplicationFiled: January 7, 2013Publication date: November 21, 2013Applicant: DUQUESNE UNIVERSITY OF THE HOLY GHOSTInventors: Partha Basu, Igor Pimkov
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Patent number: 8586595Abstract: Described herein are compositions and methods for diagnosing and/or monitoring pathogenic disease states using positron emission tomography, wherein the pathogenic cells uniquely express, preferentially express, or overexpress vitamin receptors. Also described herein are 18F conjugates of vitamins and vitamin receptor-binding analogs of the formula.Type: GrantFiled: February 7, 2008Date of Patent: November 19, 2013Assignee: Purdue Research FoundationInventors: Philip Stewart Low, Sumith K. Kularatne
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Patent number: 8546566Abstract: The present invention relates to an improved process for manufacturing dihydropteridinones of general formula (12) as well as intermediates thereof, wherein the groups R1, R2, R3, R4, and R5 have the meanings given in the claims and specification.Type: GrantFiled: September 15, 2011Date of Patent: October 1, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Juergen Schnaubelt, Rolf Herter
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Publication number: 20130251809Abstract: Disclosed are compounds, compositions and methods for systemic and local delivery of biologically active molecules.Type: ApplicationFiled: March 8, 2013Publication date: September 26, 2013Applicant: Egen, Inc.Inventors: Gregory Slobodkin, Richard Congo, Majed Matar, Jason Fewell, Khursheed Anwer, Brian Jeffery Sparks
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Patent number: 8541418Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, E1, E2, R1, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: GrantFiled: December 21, 2010Date of Patent: September 24, 2013Assignee: Elan Pharmaceutical, Inc.Inventors: Robert A. Galemmo, Dean R. Artis, Xiaocong Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Publication number: 20130237543Abstract: The present invention is directed to treatment methods of administering tetrahydrobiopterin, including in oral dosage forms, in intravenous formulations, and with food. Also disclosed herein are biopterin assays for measuring the amount of biopterin and metabolites of biopterin in a sample.Type: ApplicationFiled: February 6, 2013Publication date: September 12, 2013Applicant: BIOMARIN PHARMACEUTICAL INC.Inventors: Daniel I. Oppenheimer, Alejandro Dorenbaum, Augustus O. Okhamafe, Erik Foehr, Sianna Castillo, Paul John Kostel
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Publication number: 20130197000Abstract: [Problem] To provide means for improving symptoms of cerebral dysfunction. [Solution Means] The inventor has newly found that peripheral administration of sepiapterin increases the bioavailability of aromatic monoamines in the brain. Accordingly, provided are a drug for preventing or improving cerebral dysfunction, which contains at least one of sepiapterin and its salt and also provided is a food and or drink for preventing or improving cerebral dysfunction, which contains at least one of sepiapterin and its salt. Unlike tetrahydrobiopterin, etc., sepiapterin is able to repress the lowering level of aromatic monoamines (such as serotonin, dopamine and noradrenaline) in neurons in the brain and also increase the bioavailability.Type: ApplicationFiled: April 22, 2011Publication date: August 1, 2013Applicant: NIHON UNIVERSITYInventors: Hiroyuki Hasegawa, Shin Aizawa
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Publication number: 20130197222Abstract: A preparation process of (6R)-tetrahydrobiopterin hydrochloride is provided, which comprises hydrogenating L-biopterin in the presence of a catalyst of Pt group metal in the basic substrate containing solvent, potassium hydroxide and potassium dihydrogen phosphate to obtain (6R)-tetrahydrobiopterin hydrochloride, wherein the pH value of the basic substrate is controlled by potassium hydroxide and potassium dihydrogen phosphate in the range of about 10 to about 13.Type: ApplicationFiled: November 15, 2010Publication date: August 1, 2013Applicant: INNOPHARMAX, INC.Inventors: Zhen Wang, Dongbing Zhao, Weida Wang, Jingbo Lan, Jingsong You
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Publication number: 20130172285Abstract: The disclosure provides linked purine pterin compounds and analogues thereof that are novel HPPK inhibitors. The HPPK inhibitors described herein are compounds and the pharmaceutically acceptable salts thereof of general Formula I The variables, e.g. A1 to A3, R1 to R4, L1, L2, B1, and B2 are described herein. Compounds and salts of Formula I bind to HPPK with high affinity and specificity. Pharmaceutical compositions containing an HPPK inhibitor of Formula I and methods of treating a bacterial infection in a patient by providing one or more HPPK inhibitors of Formula I to the patient are also provided. Processes and intermediates useful for preparing compounds of Formula I are also provided. Methods of using the disclosed compounds to guide the development of additional novel anti-bacterial agents are also provided.Type: ApplicationFiled: June 1, 2011Publication date: July 4, 2013Inventors: Genbin Shi, Gary X. Shaw, Xinhua Ji
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Patent number: 8460696Abstract: Disclosed are compounds, compositions and methods for systemic and local delivery of biologically active molecules.Type: GrantFiled: March 19, 2010Date of Patent: June 11, 2013Assignee: Egen, Inc.Inventors: Gregory Slobodkin, Richard Congo, Majed Matar, Jason Fewell, Khursheed Anwer, Brian Jeffery Sparks
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Patent number: 8461149Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: August 15, 2008Date of Patent: June 11, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Francoise Pierard, Jean-Damien Charrier
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Patent number: 8450347Abstract: The invention relates to a method of controlling feelings of pain in infants or diseased or elderly persons using a complete nutrition or a nutritional supplement. The method comprises administering increased levels of folic acid, vitamin B6 and vitamin B12 or their functional equivalents.Type: GrantFiled: February 19, 2008Date of Patent: May 28, 2013Assignee: N.V. NutriciaInventors: Robert Johan Joseph Hageman, Jacob Geert Bindels
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Patent number: 8445675Abstract: Disclosed are storage stable aqueous infusible or injectable solutions containing an active substance of general formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and in the specification, and an amount of a physiologically acceptable acid or mixture of acids sufficient to dissolve the active substance and act as a stabilizer, optionally together with other formulating excipients suitable for parenteral administration, and a process for preparing the infusible or injectable solutions according to the invention.Type: GrantFiled: February 6, 2009Date of Patent: May 21, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Detlef Mohr, Claus Veit, Fridtjof Traulsen
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Patent number: 8436002Abstract: The present invention provides AKT inhibitors of the formula: Formula I The present invention also provides pharmaceutical compositions comprising compounds of Formula I, uses of compounds of Formula I and method of using compounds of Formula I.Type: GrantFiled: October 20, 2010Date of Patent: May 7, 2013Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Timothy Paul Burkholder, Joshua Ryan Clayton, MariJean Eggen, Kenneth James Henry, Jr., Deidre Michelle Johns, Saravanan Parthasarathy, Huaxing Pei, Mark Edward Rempala, Jason Scott Sawyer
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Publication number: 20130090474Abstract: The application discloses a process for the preparation of 5-deoxy-L-arabinose of formula (VI); comprising the conversion of a compound of formula (XII); wherein n is 0, 1 or 2; which can be used as intermediate for the synthesis of sapropterin.Type: ApplicationFiled: June 13, 2011Publication date: April 11, 2013Applicant: DIPHARMA FRANCIS S.R.L.Inventors: Emanuele Attolino, Mario Michieletti, Davide Rossi, Pietro Allegrini
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Publication number: 20130040956Abstract: A process for the preparation of the stable, amorphous calcium salt of (6S)-N(5)-methyl-5,6,7,8-tetrahydrofolic acid of the formula V, and a stable, amorphous calcium salt of (6S)-N(5)-methyl-5,6,7,8-tetrahydrocolic acid of the formula V are provided.Type: ApplicationFiled: August 14, 2012Publication date: February 14, 2013Applicant: CERBIOS-PHARMA S.A.Inventors: Raffella MANZOTTI, Moreno Morosoli
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Publication number: 20130034496Abstract: The present invention relates to positron emission tomography tracers and methods of using these tracers.Type: ApplicationFiled: August 2, 2012Publication date: February 7, 2013Applicant: UNIVERSITY OF IOWA RESEARCH FOUNDATIONInventor: Amnon Kohen
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Patent number: 8367670Abstract: Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: GrantFiled: December 7, 2009Date of Patent: February 5, 2013Assignee: Gilead Sciences, Inc.Inventors: Manoj C. Desai, Randall L. Halcomb, Paul Hrvatin, Hon Chung Hui, Ryan McFadden, Paul A. Roethle, Hong Yang
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Publication number: 20130011362Abstract: Provided herein are monomers incorporating folate or other targeting agent, polymers prepared therefrom, polymers prepared therefrom having a therapeutic agent covalently coupled thereto, as well as micelles and therapeutic compositions thereof.Type: ApplicationFiled: November 17, 2010Publication date: January 10, 2013Applicants: PhaseRx, Inc., University of Washington through its Center for CommercializationInventors: Sean D. Monahan, Paul H. Johnson, Michael S. DeClue, Priyadarsi De, Anna S. Gall, Patrick S. Stayton, Allan S. Hoffman, Charbel Diab
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Patent number: 8344139Abstract: Crystal forms of (6R)-L-erythro-tetrahydrobiopterin dihydrochloride, hydrates and solvates and processes for their preparation are provided. These crystal forms are either intermediates for the preparation of stable polymorphic form B or are suitable for solid formulations.Type: GrantFiled: May 10, 2010Date of Patent: January 1, 2013Assignee: Merck Eprova AGInventors: Rudolf Moser, Viola Groehn, Thomas Egger, Fritz Blatter
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Publication number: 20120329803Abstract: The present invention relates to new dihydropteridinones of general formula (12) wherein the groups R1 to R5 and L, n, and m have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.Type: ApplicationFiled: February 16, 2011Publication date: December 27, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Guenter Linz, Daniel Bischoff, Thomas Ebner
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Publication number: 20120309747Abstract: In one aspect, the invention provides compounds of Formula I or pharmaceutically acceptable salts thereof. In another aspect, the invention provides methods for treatment of diseases or disorders mediated by a protein kinase, comprising administering a therapeutically effective amount of a compound of this invention.Type: ApplicationFiled: July 23, 2012Publication date: December 6, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven Durrant
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Patent number: 8324210Abstract: Disclosed herein are analogs of tetrahydrobiopterin, compositions containing the same, and methods of treating an individual suffering from a condition responsive to tetrahydrobiopterin by administration of the analog. These analogs are contemplated for use wherever tetrahydrobiopterin is currently used to treat conditions responsive to tetrahydrobiopterin therapies.Type: GrantFiled: October 12, 2009Date of Patent: December 4, 2012Assignee: BioMarin Pharmaceutical, Inc.Inventor: Emil D. Kakkis
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Publication number: 20120302575Abstract: The present disclosure is generally related to methods of preventing oxidative stress injury induced by renal is-chemia-reperfusion by a Folate-TEMPOL conjugate.Type: ApplicationFiled: September 21, 2010Publication date: November 29, 2012Applicants: GEORGIA TECH RESEARCH CORPORATION, EMORY UNIVERSITYInventors: W. Robert Taylor, Sarah F. Knight, Niren Murthy, Kousik Kundu
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Patent number: 8318745Abstract: Crystal forms of (6R)-L-erythro-tetrahydrobiopterin dihydrochloride, hydrates and solvates and processes for their preparation are provided. These crystal forms are either intermediates for the preparation of stable polymorphic form B or are suitable for solid formulations.Type: GrantFiled: December 3, 2009Date of Patent: November 27, 2012Assignee: Merck & CIEInventors: Rudolf Moser, Viola Groehn, Thomas Egger, Fritz Blatter
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Patent number: 8314102Abstract: There is provided a stable, crystalline (6S)-N(5)-methyl-5,6,7,8-tetrahydrofolic acid of the formula IV, This compound belongs to the family of reduced folates which are useful in vitaminic and oncological field.Type: GrantFiled: May 29, 2008Date of Patent: November 20, 2012Assignee: Cerbios-Pharma S.A.Inventors: Raffella Manzotti, Moreno Morosoli
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Publication number: 20120271045Abstract: A method of preparing a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and claims. Additionally, the present invention relates to compounds of Structural Formula (I), which are useful as inhibitors of protein kinase.Type: ApplicationFiled: March 20, 2012Publication date: October 25, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jean-Damien Charrier, Steven Durrant, Michael O'Donnell
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Patent number: 8278297Abstract: In one aspect, the invention provides compounds of Formula I or pharmaceutically acceptable salts thereof. In another aspect, the invention provides methods for treatment of diseases or disorders mediated by a protein kinase, comprising administering a therapeutically effective amount of a compound of this invention.Type: GrantFiled: December 23, 2010Date of Patent: October 2, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven Durrant
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Publication number: 20120238754Abstract: The present invention relates to an improved process for manufacturing dihydropteridinones of general formula (12) as well as intermediates thereof, wherein the groups R1, R2, R3, R4, and R5 have the meanings given in the claims and specification.Type: ApplicationFiled: September 15, 2011Publication date: September 20, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Juergen Schnaubelt, Rolf Herter
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Patent number: 8252787Abstract: In one aspect, the invention provides compounds of Formula I or pharmaceutically acceptable salts thereof. In another aspect, the invention provides methods for treatment of diseases or disorders mediated by a protein kinase, comprising administering a therapeutically effective amount of a compound of this invention.Type: GrantFiled: December 23, 2010Date of Patent: August 28, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven Durrant
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Publication number: 20120214995Abstract: The present invention relates to a specific salt of a dihydropteridione derivative, namely the trihydrochloride salt of the compound N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide, to its crystallisation in the form of an hydrate with water, to a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.Type: ApplicationFiled: April 27, 2012Publication date: August 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Guenter Linz, Peter Sieger, Matthias Grauert, Rolf Schmid
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Patent number: 8232278Abstract: Specifically substituted pyrido(3,2-d)pyrimidine derivatives having the structural formula (I) are useful for the treatment of hepatitis C.Type: GrantFiled: June 26, 2006Date of Patent: July 31, 2012Assignee: Gilead Sciences, Inc.Inventors: Steven Cesar Alfons De Jonghe, Piet André Maurits Maria Herdewijn, William A. Lee, William John Watkins
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Publication number: 20120184543Abstract: Dihydroperidinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specially, new dihydroperidinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is defined as in the description, their preparation process, pharmaceutical compositions comprising said derivatives and their use as therapeutical agents, especially as Plk kinase inhibitors are disclosed.Type: ApplicationFiled: September 14, 2010Publication date: July 19, 2012Applicants: SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD., JIANGSU HENGRUI MEDICINE CO., LTD.Inventors: Peng Cho Tang, Nong Zhang, Baolei Zhang, Weimin Wang, Hao Zheng, Lin Wu
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Patent number: 8178670Abstract: The present disclosure provides a method that efficiently produces (6R)-tetrahydrobiopterin of Formula I in high yield and purity. The method includes the step of hydrolyzing diacetylbiopterin to biopterin under basic conditions in a biphasic mixture comprising an organic phase and an aqueous phase. After substantially complete hydrolysis of diacetylbiopterin, the aqueous phase containing biopterin can be separated from the organic phase containing most of the organic impurities, which avoids the time-consuming step of isolating biopterin as a solid. The aqueous solution containing biopterin is stereoselectively hydrogenated to (6R)-tetrahydrobiopterin under basic conditions and high hydrogen pressure in the presence of a metal catalyst (e.g., a platinum catalyst). To improve the purification of an acid addition salt of (6R)-tetrahydrobiopterin (e.g., (6R)-tetrahydrobiopterin dihydrochloride), any residual salts (e.g.Type: GrantFiled: January 6, 2009Date of Patent: May 15, 2012Assignee: BioMarin Pharmaceutical Inc.Inventors: Mark Henderson, Steven Jungles, Gabriele Roidl, Robert Baffi, Adriano Indolese, Christian Müller, Philipp Schmidt, Stefan Kaiser
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Publication number: 20120115244Abstract: Methods of assaying for (i) a pterin by immunoassay employing a pterin as capture agent, (ii) neopterin by chemiluminescent microparticle immunoassay (CMIA) employing an anti-neopterin antibody (Ab) as capture agent, (iii) neopterin by an immunoassay (IA) employing an acridinium (Acr)-labeled anti-neopterin Ab as conjugate, and (iv) neopterin by an IA employing Acr-labeled neopterin as tracer; an Acr-labeled anti-neopterin Ab; a conjugate/complex comprising anti-neopterin Ab and a carrier scaffold; a conjugated pterin; a conjugate comprising an Acr-labeled pterin and a carrier scaffold; an immunogen comprising neopterin and a carrier protein; a conjugate comprising such an immunogen and an Acr compound; an immunogen comprising a carrier protein and a neopterin hapten; a conjugate comprising such an immunogen and an Acr compound; a kit for assaying a pterin comprising a pterin as a capture agent and instructions for IA; and a kit for assaying neopterin comprising an anti-neopterin Ab as a capture agent and insType: ApplicationFiled: November 9, 2010Publication date: May 10, 2012Applicant: ABBOTT LABORATORIESInventors: Maciej Adamczyk, R. Jeffrey Brashear, Stephen C. Hsu, Phillip G. Mattingly
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Publication number: 20120065149Abstract: The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety includes vitamins, and vitamin receptor binding analogs and derivatives thereof, and the drug includes analogs and derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) includes components such as spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.Type: ApplicationFiled: September 7, 2011Publication date: March 15, 2012Inventors: Iontcho R. Vlahov, Christopher P. Leamon, Matthew A. Parker, Stephen J. Howard, Hari Krishna Santhapuram, Apparao Satyam, Joseph Anand Reddy
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Publication number: 20120028966Abstract: In one aspect, the invention provides compounds of Formula I or pharmaceutically acceptable salts thereof. In another aspect, the invention provides methods for treatment of diseases or disorders mediated by a protein kinase, comprising administering a therapeutically effective amount of a compound of this invention.Type: ApplicationFiled: December 23, 2010Publication date: February 2, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steve Durrant
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Publication number: 20120022072Abstract: Disclosed herein are analogs of tetrahydrobiopterin, compositions containing the same, and methods of treating an individual suffering from a condition responsive to tetrahydrobiopterin by administration of the analog. These analogs are contemplated for use wherever tetrahydrobiopterin is currently used to treat conditions responsive to tetrahydrobiopterin therapies.Type: ApplicationFiled: September 16, 2011Publication date: January 26, 2012Applicant: BIOMARIN PHARMACEUTICAL INC.Inventors: Emil D. Kakkis, Erik Foehr, Sianna Castillo, Steven W. Szczepanski, Paul John Kostel
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Publication number: 20120010197Abstract: In one aspect, the invention provides compounds of Formula I or pharmaceutically acceptable salts thereof. In another aspect, the invention provides methods for treatment of diseases or disorders mediated by a protein kinase, comprising administering a therapeutically effective amount of a compound of this invention.Type: ApplicationFiled: December 23, 2010Publication date: January 12, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven Durrant
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Publication number: 20110286958Abstract: Polymeric platinum amidomalonate complexes, where the platinum is in +2 or +4 oxidation state, and where the complexes optionally contain tumor seeking groups, are useful in the treatment of cancer.Type: ApplicationFiled: May 16, 2011Publication date: November 24, 2011Inventors: Paul Sood, N. Rao Ummaneni, Bruce Thurmond, Ryszard Zarzycki
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Publication number: 20110288090Abstract: The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: January 25, 2010Publication date: November 24, 2011Inventors: Donna J. Armstrong, Yasuhiro Goto, Takashi Hashihayata, Tetsuya Kato, Michael J. Kelly, III, Mark E. Layton, Craig W. Lindsley, Yoshio Ogino, Yu Onozaki, Kenvin J. Rodzinak, Michael A. Rossi, Philip E. Sanderson, Jiabing Wang, Melissa M. Yaroschak
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Publication number: 20110281880Abstract: The present invention is directed to treatment methods of administering tetrahydrobiopterin, including in oral dosage forms, in intravenous formulations, and with food. Also disclosed herein are biopterin assays for measuring the amount of biopterin and metabolites of biopterin in a sample.Type: ApplicationFiled: April 29, 2011Publication date: November 17, 2011Applicant: BIOMARIN PHARMACEUTICAL INC.Inventors: Daniel I. Oppenheimer, Alejandro Dorenbaum, Augustus Okhamafe, Erik Foehr, Sianna Castillo, Paul J. Kostel
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Patent number: 8044200Abstract: Methods for purifying pteroic acid, analogs of pteroic acid, and derivatives of pteroic acid are described. Methods for synthesizing and purifying conjugates of vitamins, including FITC conjugates of folic acid, folic acid analogs, and derivatives of folic acid and folic acid analogs are also described. Purified forms of pteroic acid, derivatives and analogs of pteroic acid, and conjugates thereof are also described.Type: GrantFiled: March 14, 2006Date of Patent: October 25, 2011Assignee: Endocyte, Inc.Inventors: Le-Cun Xu, Iontcho Radoslavov Vlahov, Christopher Paul Leamon, Hari Krishna Santhapuram, Chunhong Li
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Publication number: 20110251363Abstract: The invention relates to stereoregular ROMP polymers, the monomers used to make them, and the processes used to convert the monomers to the polymers.Type: ApplicationFiled: July 17, 2007Publication date: October 13, 2011Inventors: Nicole S. Sampson, Kathlyn A. Parker