Having -c(=x)-, Wherein X Is Chalcogen Attached Directly Or Indirectly To The Purine Ring System By Nonionic Bonding Or Halogen Bonded Directly At 8-position (e.g., Theophylline Acetate, 8-chlorotheophylline, Etc.) Patents (Class 544/271)
-
Patent number: 9163024Abstract: The present invention relates to a tris salt of 8-chloro-3-pentyl-3,7-dihydro-1H-purine-2,6-dione of Formula (A) or a pharmaceutically acceptable salt thereof: corresponding pharmaceutical formulations, manufacture processes and uses of the aforementioned compound in therapy, particularly in treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.Type: GrantFiled: December 7, 2009Date of Patent: October 20, 2015Assignee: GlaxoSmithKline LLCInventors: Holly Esken, Beth Adams Norton
-
Patent number: 9133196Abstract: The present invention relates to an improved process for preparing Acebrophylline comprising preparing a reaction mixture of theophylline-7-acetate and ambroxol base in a non-polar solvent; heating said reaction mixture at a suitable temperature; and isolating Acebrophylline by filtration. The yield of Acebrophylline is between 95-98% with a purity of 99%.Type: GrantFiled: February 7, 2013Date of Patent: September 15, 2015Assignee: AMI LIFESCIENCES PVT. LTD.Inventors: Kalpesh Ravajibhai Patel, Virendra Haridasbhai Thakrar, Dipti Kishorbhai Dodiya, Sharad Kanabhai Solanki, Kinchit Jitendrakumar Shah
-
Patent number: 9035050Abstract: This invention relates to novel deuterated compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. In particular, this invention relates to novel substituted xanthine derivatives that are deuterated derivatives of a pentoxifylline metabolite. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed deuterated compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial. The compounds of the invention are represented by the following structural formula: wherein the values of R1, R2, R3, R4, R5, Y1 and Y2 are described herein.Type: GrantFiled: July 24, 2013Date of Patent: May 19, 2015Assignee: Concert Pharmaceuticals, Inc.Inventors: Roger D. Tung, Julie F. Liu, Scott L. Harbeson
-
Publication number: 20150133407Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of respiratory disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of viscid or excessive mucus, cough, inflammation, redness in sore throat, infection in the throat, sore throat, abnormal mucus secretion, impaired mucus transport, allergic rhinitis, asthma, COPD, respiratory muscular disorders and pain in acute sore throat.Type: ApplicationFiled: May 14, 2013Publication date: May 14, 2015Inventor: Mahesh Kandula
-
Publication number: 20150087660Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of chronic diseases and inflammatory disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection.Type: ApplicationFiled: February 27, 2013Publication date: March 26, 2015Inventor: Mahesh KANDULA
-
Publication number: 20140194448Abstract: The present invention relates to a new application of phosphodiesterase inhibitors for couple infertility treatment which forms an effective alternative to the invasive assisted reproductive techniques such as conjugal artificial insemination and which consists of the transvaginal administration of a phosphodiesterase inhibitor immediately before and/or after coitus. It also relates to dosage forms suitable for the intravaginal administration of phosphodiesterase inhibitors.Type: ApplicationFiled: June 20, 2012Publication date: July 10, 2014Inventors: Maria Carmen Pardina Palleja, Miguel Angel Vaz-Romero Uña
-
Publication number: 20140121226Abstract: This invention relates to novel deuterated compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. In particular, this invention relates to novel substituted xanthine derivatives that are deuterated derivatives of a pentoxifylline metabolite. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed deuterated compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial. The compounds of the invention are represented by the following structural formula: wherein the values of R1, R2, R3, R4, R5, Y1 and Y2 are described herein.Type: ApplicationFiled: July 24, 2013Publication date: May 1, 2014Applicant: CONCERT PHARMACEUTICALS, INC.Inventors: Roger D. Tung, Julie F. Liu, Scott L. Harbeson
-
Publication number: 20140105898Abstract: This invention relates generally to methods and agents for modulating adiposity-related conditions. More particularly, the present invention relates to the use of TRAIL death receptor agonists, including nucleic acids such as TRAIL polynucleotides, peptides and polypeptides including TRAIL polypeptides, TRAIL DR agonist antigen-binding molecules, TRAIL DR peptide agonists as well as small molecule TRAIL DR agonists in compositions and methods for treating or preventing adiposity-related conditions such as obesity, diabetes mellitus and metabolic syndrome.Type: ApplicationFiled: February 27, 2012Publication date: April 17, 2014Applicant: Istituto Di Ricovero E Cura A Carattere Scientific Materno-Infantile Burlo GaroInventors: Merlin C. Thomas, Giorgio Zauli, Paola Secchiero, Bruno Fabris, Stella Bernardi
-
Publication number: 20140100224Abstract: The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.Type: ApplicationFiled: June 26, 2013Publication date: April 10, 2014Applicants: The University of North Carolina at Chapel Hill, U.S. Government represented by the Department of Veterans Affairs, The Regents of the University of CaliforniaInventors: Frank M. Longo, Stephen M. Massa
-
Publication number: 20140046060Abstract: The present invention provides a method for utilizing recycled deuterium oxide synthesis of deuterated compounds.Type: ApplicationFiled: September 1, 2011Publication date: February 13, 2014Applicant: Concert Pharmaceuticals, Inc.Inventors: Andrew D. Jones, Bernhard J. Paul
-
Publication number: 20140030200Abstract: The present invention relates to the activation of peptidyl arginine deiminase (PADs) 1 and/or 3 in the epidermis by at least one active agent used alone or in combination, namely caffeine, acefylline and/or theobromine in a cosmetic and/or pharmaceutical composition. The present invention also relates to the use of the aforementioned active agents in cosmetics and/or therapeutics, alone or in combination, in order to improve the barrier functions of the epidermis, to prevent and/or treat symptoms related to dry skin or to improve and/or promote hydration of the keratinous layer. Finally, the invention relates to increasing the activity of PAD1 and/or PAD3 in the epidermis.Type: ApplicationFiled: April 11, 2012Publication date: January 30, 2014Applicant: PIERRE FABRE DERMO-COSMETIQUEInventors: Hélène Duplan, Sylvie Daunes-Marion, Stéphane Poigny, Marie-Claire Mechin, Guy Serre, Michel Simon
-
Publication number: 20130310404Abstract: Novel p75 receptor antagonist compounds and compositions and uses thereof for the prevention and treatment of p75-associated disorders, such as neurodegenerative diseases, are described.Type: ApplicationFiled: October 13, 2011Publication date: November 21, 2013Inventors: Horacio Uri Saragovi, Hinyu Nedev
-
Publication number: 20130303521Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.Type: ApplicationFiled: October 26, 2012Publication date: November 14, 2013Applicant: HYDRA BIOSCIENCES, INCInventor: HYDRA BIOSCIENCES, INC
-
Publication number: 20130245047Abstract: An animal model has been developed based the understanding that a central mechanism in patients with CTRF is that chemotherapy and/or radiation initiates canonical pathways leading to the development of disrupted sleep architecture, resulting in disruption of REM sleep and fatigue and cognitive dysfunction. Drugs that restore the activity patterns and levels towards normal and/or decrease the pro-inflammatory cytokines associated with the disrupted sleep, should be effective in alleviating one or more symptoms of CTRF. Pentoxifylline was demonstrated to improve activity levels in animals treated with etoposide.Type: ApplicationFiled: May 2, 2013Publication date: September 19, 2013Applicant: Tenera Therapeutics, LLCInventors: Stephen T. SONIS, Edward G. FEY, Edward B. RUBENSTEIN
-
Publication number: 20130123283Abstract: The present application relates to compounds and methods for treating pain, incontinence and other conditions.Type: ApplicationFiled: April 11, 2012Publication date: May 16, 2013Inventors: Magdalene M. Moran, Christopher Fanger, Jayhong A. Chong, Colleen McNamara, Xiaoguang Zhen, Josh Mendel-Brehm
-
Publication number: 20120322799Abstract: The present application is related to deuterated compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders involving degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such deuterated compounds.Type: ApplicationFiled: November 30, 2010Publication date: December 20, 2012Applicant: PHARMATROPHIX, INC.Inventor: Gopal Damodara
-
Patent number: 8324224Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.Type: GrantFiled: June 27, 2011Date of Patent: December 4, 2012Assignee: Gilead Sciences, Inc.Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
-
Publication number: 20120252782Abstract: 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: June 15, 2012Publication date: October 4, 2012Applicant: BOEHRINGER INGELHEIM PHARMA GMBH AND CO. KGInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
-
Publication number: 20120252783Abstract: 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: June 15, 2012Publication date: October 4, 2012Applicant: BOEHRINGER INGELHEIM PHARMA & CO. KGInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
-
Publication number: 20120225812Abstract: The present invention provides substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The present invention also provides process of preparation of compounds of formula (I).Type: ApplicationFiled: November 9, 2010Publication date: September 6, 2012Applicant: Advinus Therapeutics LimitedInventors: Vidya Ramdas, Summon Koul, Sujay Basu, Yogesh Waman, Yogesh Shejul, Dinesh Barawkar, Ventaka Poornapragnacharyulu Palle
-
Patent number: 8207175Abstract: The present invention relates to compounds and uses of compounds which interact with chitinase enzymes, in particular the inhibition of those enzymes.Type: GrantFiled: June 21, 2006Date of Patent: June 26, 2012Assignee: University Court of the University of DundeeInventors: Daniel Marinus Ferdinand Van Aalten, Ian Michael Eggleston
-
Patent number: 8163479Abstract: The invention relates to substrates for O6-alkylguanine-DNA alkyltransferases (AGT) of formula R1-A-X—CH2—R3—R4-L1, wherein A is a group recognized by AGT as a substrate, X is oxygen or sulfur, R1 is a group —R2-L2 or a group R5, R2 and R4 are, independently of each other, a linker, R3 is an aromatic or a heteroaromatic group, or an optionally substituted unsaturated alkyl, cycloalkyl or heterocyclyl group with the double bond connected to CH2, R5 is arylmethyl or heteroarylmethyl or an optionally substituted cycloalkyl, cycloalkenyl or heterocyclyl group, L1 is a label, a plurality of same or different labels, a bond connecting R4 to A forming a cyclic substrate, or a further group —R3—CH2—X-A-R1, and L2 is a label or a plurality of same or different labels. The invention further relates to methods of transferring a label from these substrates to O6-alkylguanine-DNA alkyltransferases (AGT) and AGT fusion proteins.Type: GrantFiled: March 1, 2005Date of Patent: April 24, 2012Assignee: Ecole Polytechnique Federale de LausanneInventors: Hughes Jaccard, Kai Johnsson, Maik Kindermann, India Christina Sielaff
-
Patent number: 8044061Abstract: Disclosed are novel compounds of the general formula (Ia), and pharmaceutically acceptable salts, isomers, diastereomers or enantiomers thereof and their use as medicines, for example in the treatment of dopamine-related movement disorders.Type: GrantFiled: December 21, 2007Date of Patent: October 25, 2011Assignee: UCB Pharma GmbHInventors: Christa E. Müller, Jörg Hockemeyer, Nikolay T. Tzvetkov, Joachim C. Burbiel
-
Publication number: 20110230479Abstract: The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.Type: ApplicationFiled: October 22, 2010Publication date: September 22, 2011Inventors: Frank M. Longo, Stephen M. Massa
-
Publication number: 20110144095Abstract: 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: February 23, 2011Publication date: June 16, 2011Applicant: BOEHRINGER INGELHEIM PHARMA & CO. KGInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
-
Publication number: 20110059995Abstract: This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial.Type: ApplicationFiled: September 1, 2010Publication date: March 10, 2011Inventors: Roger D. Tung, Julie F. Liu, Scott L. Harbeson
-
Patent number: 7902360Abstract: wherein R3 is Alk14ArR16, and wherein Alk14 is C1-8 straight or branched alkylene or alkenylene. The present invention provides novel adenosine receptor antagonists, more particularly, A1 adenosine receptor antagonists of formula (I). Pharmaceutical compositions comprising an A1 adenosine receptor antagonist of formula (I) and a pharmaceutically acceptable carrier are further provided. Compositions also include diagnostic assay-type probes comprising a novel A1 adenosine receptor antagonist of formula (I) that is labeled or conjugated with radioactive or non-radioactive material. Methods for treating A1 adenosine receptor related disorders comprising administering an A1 adenosine receptor antagonist of formula I are also disclosed. The novel A1 adenosine receptor antagonist compositions of formula (I) find further use in diagnostic and imaging methods.Type: GrantFiled: May 25, 2007Date of Patent: March 8, 2011Inventors: Constance N. Wilson, John J. Partridge
-
Patent number: 7838529Abstract: Compounds of formula (I) wherein R1 is a phenylcarbonylmethyl group wherein the phenyl moiety is substituted by R10 and R11 and R2 to R4 and R10 and R1l are defined as in the claims, or the prodrugs or salts thereof, particularly the physiologically acceptable salts thereof, pharmaceutical compositions containing these compounds, and methods of treating type II diabetes mellitus and obesity using these compounds.Type: GrantFiled: January 16, 2009Date of Patent: November 23, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf Lotz
-
Patent number: 7799524Abstract: The invention relates to compounds of formula 1 wherein R1-R2 is a guanine derivative; X is oxygen or sulfur; R3 is a heteroaromatic, unsaturated heterocyclyl or an alkynyl group with the double or triple bond connected to CH2; R4 is a linker; and L is a label, a plurality of same or different labels, a bond connecting R4 to R1 forming a cyclic substrate, or a further group —R3—CH2—X—R1-R2. The invention relates also to methods of manufacture of such novel AGT substrates, to intermediates useful in the synthesis of such AGT substrates, and to a method of transferring a label from such AGT substrates to O6-alkylguanine-DNA alkyltransferase (AGT) fusion proteins comprising proteins of interest.Type: GrantFiled: October 1, 2003Date of Patent: September 21, 2010Assignee: Ecole Polytechnique Ferdeale de LausanneInventors: Maik Kindermann, Kai Johnsson, Christoph Bieri
-
Publication number: 20100228015Abstract: This invention relates to novel homotopic prodrugs and medicaments and methods for their preparation, testing and use. In one embodiment, the homotopic prodrug has the general formula wherein is a biologically-active moiety comprising a carboxylic acid functional group, and Rb is a homotopically-symmetrical alcohol bonded to the biologically-active moiety through the carboxylic acid functional group to form an ester linkage, as well as optical isomers, enantiomers, pharmaceutically acceptable salts, biohydrolyzable amides, esters, and imides thereof and combinations thereof.Type: ApplicationFiled: April 23, 2010Publication date: September 9, 2010Inventors: Mitchell A. deLong, Jill M. McFadden, Susan M. Royalty, Eric J. Toone, Jeffrey D. Yingling
-
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
-
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
-
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
-
Publication number: 20100190746Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides quinazolinone, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.Type: ApplicationFiled: November 20, 2009Publication date: July 29, 2010Applicant: ICAGEN, INC.Inventors: Grant A. McNaughton-Smith, James B. Thomas, JR., George S. Amato
-
Patent number: 7713982Abstract: The present invention relates to a therapeutically active xanthine derivative compound of formula (I): corresponding pharmaceutical formulations containing, manufacture processes for, methods or uses of such compounds in therapy, in particular for treatment of diseases where under-activation of the HM74A receptor contributes to such diseases or where activation of the HM74A receptor will be beneficial.Type: GrantFiled: February 10, 2005Date of Patent: May 11, 2010Assignee: Smithkline Beecham CorporationInventor: Ivan Leo Pinto
-
Publication number: 20090239886Abstract: This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial.Type: ApplicationFiled: February 27, 2009Publication date: September 24, 2009Applicant: CoNCERT Pharmaceuticals, Inc.Inventors: Roger D. Tung, Julie F. Liu, Scott L. Harbeson
-
Publication number: 20090221821Abstract: The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1 receptor. Adenosine A1 antagonists can be useful in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable.Type: ApplicationFiled: February 10, 2009Publication date: September 3, 2009Applicant: BIOGEN IDEC MA INC.Inventors: Carol L. Ensinger, James E. Dowling, Russell C. Petter, Gnanasambandam Kumaravel
-
Patent number: 7569574Abstract: The invention relates to new purine derivatives of general formula wherein R1 to R4 are defined as in the claims, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV), the preparation thereof, the use thereof for the prevention or treatment of diseases or conditions associated with an increased DPP-IV activity or capable of being prevented or alleviated by reducing the DPP-IV activity, particularly type I or type II diabetes mellitus, the pharmaceutical compositions containing a compound of general formula (I) or a physiologically acceptable salt thereof as well as processes for the preparation thereof.Type: GrantFiled: August 4, 2003Date of Patent: August 4, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Roland Maier, Frank Himmelsbach, Matthias Eckhardt, Elke Langkopf, Michael Mark, Ralf R. H. Lotz
-
Patent number: 7560450Abstract: The present invention relates to substituted xanthines of general formula the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: November 18, 2003Date of Patent: July 14, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co., KGInventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Roland Maier, Michael Mark, Mohammad Tadayyon
-
Patent number: 7550468Abstract: A variety of N-substituted derivatives are based upon the base chemicals of that provide for the induction of cavernosal relaxation in animals. R2 is a derivative based on a hetroaromatic group, an aromatic group or a cyclohexane.Type: GrantFiled: May 4, 2005Date of Patent: June 23, 2009Inventor: Ing-Jun Chen
-
Patent number: 7495005Abstract: Compounds of formula (I) wherein R1 is a phenylcarbonylmethyl group wherein the phenyl moiety is substituted, and R2 to R4 are defined as in the claims, or the prodrugs or salts thereof, particularly the physiologically acceptable salts thereof, pharmaceutical compositions containing these compounds, and methods of treating type I and type II diabetes mellitus, arthritis, obesity, allograft transplantation and calcitonin-induced osteoporosis using these compounds.Type: GrantFiled: August 7, 2003Date of Patent: February 24, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf R. H. Lotz
-
Publication number: 20080249089Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are defined as in claims 1 to 16, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof 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: June 20, 2008Publication date: October 9, 2008Applicant: Boehringer Ingelheim Pharma KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf R.H. Lotz, Mohammad Tadayyon
-
Patent number: 7407955Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are defined as in claims 1 to 16, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: August 12, 2003Date of Patent: August 5, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co., KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf R. H. Lotz, Mohammad Tadayyon
-
Patent number: 7317017Abstract: 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: July 25, 2005Date of Patent: January 8, 2008Assignee: CV Therapeutics, Inc.Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
-
Patent number: 7312223Abstract: The present invention is directed to a metabolite of a xanthine Phosphodiesterase type 5 inhibitor having the following structure derivatives, and formulations thereof, and processes for preparing the same.Type: GrantFiled: July 29, 2004Date of Patent: December 25, 2007Assignee: Schering CorporationInventors: Anima Ghosal, Wei Tong, Swapan K. Chowdhury, Shmuel Zbaida, Mark A. Wirth, Kevin B. Alton, James E. Patrick, Craig D. Boyle, Andrew Stamford
-
Patent number: 7307166Abstract: The invention relates to certain oxypurine nucleosides, congeners of such oxypurine nucleosides, and acyl derivatives thereof, and compositions which contain at least one of these compounds. The invention also relates to methods of treating or preventing hematopoietic disorders and modifying hematopoiesis, and treating or preventing inflammatory diseases and bacterial infections by administering a compound or composition of the present invention to an animal.Type: GrantFiled: June 5, 1995Date of Patent: December 11, 2007Assignee: Wellstat Therapeutics CorporationInventors: Reid W. von Borstel, Michael K. Bamat, Bradley M. Hiltbrand, James C. Butler, Shyam Shirali
-
Patent number: 7304070Abstract: 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: September 16, 2004Date of Patent: December 4, 2007Assignee: CV Therapeutics, Inc.Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
-
Patent number: 7247639Abstract: The present invention provides novel adenosine receptor antagonists, more particularly, A1 adenosine receptor antagonists of formula (I). Pharmaceutical compositions comprising an A1 adenosine receptor antagonist of formula (I) and a pharmaceutically acceptable carrier are further provided. Compositions also include diagnostic assay-type probes comprising a novel A1 adenosine receptor antagonist of formula (I) that is labeled or conjugated with radioactive or non-radioactive material. Methods for treating A1 adenosine receptor related disorders comprising administering an A1 adenosine receptor antagonist of formula (I) are also disclosed. The novel A1 adenosine receptor antagonist compositions of formula (I) find further use in diagnostic and imaging methods. wherein R3 is Alk14ArR16, and wherein Alk14 is C1-8 straight or branched alkylene or alkenylene.Type: GrantFiled: June 4, 2004Date of Patent: July 24, 2007Assignee: Endacea, Inc.Inventors: Constance N. Wilson, John J. Partridge
-
Patent number: 7235538Abstract: The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, which are of formula I wherein each n is one or two independently and R1, R2, R3, R6, R7, R9, and R10 are defined herein. The present invention also relates to pharmaceutical compositions comprising the compounds of formula I and the use of the compounds for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type-2 diabetes and obesity.Type: GrantFiled: July 17, 2003Date of Patent: June 26, 2007Assignee: Novo Nordisk A/SInventors: Anders Bendtz Kanstrup, Lise Brown Christiansen, Jane Marie Lundbeck, Christian K. Sams, Marit Kristiansen
-
Patent number: 7148229Abstract: The present invention is a sulfonamide substituted xanthine derivative of formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is lower alkyl, lower alkyl substituted by phenyl, or lower alkyl substituted by halogen substituted phenyl; R2 is lower alkyl or lower alkyl substituted by lower cycloalkyl; and R3 is: Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.Type: GrantFiled: February 11, 2004Date of Patent: December 12, 2006Assignee: Hoffman-La Roche Inc.Inventors: Peter W. Dunten, Louise H. Foley, Nicholas J. S. Huby, Sherrie L. Pietranico-Cole, Weiya Yun