Additional Polycyclo Ring System, Which Is Not Another Purine, Having A Hetero Ring As One Of The Cyclos Patents (Class 544/268)
  • Patent number: 9353114
    Abstract: Provided is a process for the preparation of linagliptin of Formula I, comprising deprotecting a compound of Formula II wherein R1 and R2 together with the nitrogen to which they are attached form a phthalimido group, wherein the aromatic ring of the phthalimido group is substituted with one or more R3 substituents selected from the group consisting of halogen, alkyi, nitro and amino; or R1 is H and R2 is selected from the group consisting of trialkylsilyl, 2-trialkylsilylethoxycarbamates, acetyl, trihaloacetyl, 9-fluorenylmethoxycarbonyl, trityl, alkylsulfonyl, arylsulfonyl, diphenylphosphine and sulfonylethoxycarbonyl.
    Type: Grant
    Filed: August 6, 2013
    Date of Patent: May 31, 2016
    Assignee: Glenmark Pharmaceuticals Limited
    Inventors: Sunil Kumar Singh, Sachin Srivastava, Shekhar Bhaskar Bhirud
  • Patent number: 9108964
    Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, 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: Grant
    Filed: January 14, 2014
    Date of Patent: August 18, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier
  • Patent number: 9056112
    Abstract: The present application provides a process for preparation of Linagliptin reacting (R)-piperidine-3-amine of Formula II or an acid addition salt thereof with 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-bromoxanthine of Formula III in the presence of a suitable base in an inert organic solvent.
    Type: Grant
    Filed: December 27, 2012
    Date of Patent: June 16, 2015
    Assignee: DR. REDDY'S LABORATORIES LIMITED
    Inventors: Pranab Haldar, Venkateswarlu Muvva, Anil Kumar Prataprao, Vijaya Kumar Karri, Bhanu Pratap Taduri, Venkateshwara Natraj Birudaraju
  • Patent number: 9034883
    Abstract: The present invention relates to certain DPP-4 inhibitors for treating and/or preventing oxidative stress, vascular stress and/or endothelial dysfunction as well as to the use of such DPP-4 inhibitors in treatment and/or prevention of diabetic or non-diabetic patients, including patient groups at risk of cardiovascular and/or renal disease.
    Type: Grant
    Filed: November 14, 2011
    Date of Patent: May 19, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Thomas Klein, Andreas Daiber, Odd-Eric Johansen, Michael Mark, Sanjaykumar Patel, Hans-Juergen Woerle
  • Publication number: 20150126593
    Abstract: 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 asthma and allergy may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of respiratory diseases, respiratory disorders, COPD, bronchitis, brain injury, inflammation, inflammatory skin diseases, asthma, allergic reactions, infections due to acute allergy, bronchospasm, respiratory distress, acute asthma, leukotrienes over activity, 5-LO enzyme activity and cancer.
    Type: Application
    Filed: February 27, 2013
    Publication date: May 7, 2015
    Inventor: Mahesh Kandula
  • Publication number: 20150112062
    Abstract: The present invention relates to substituted quinazolines of formula (I) wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: December 23, 2014
    Publication date: April 23, 2015
    Inventors: Waldemar PFRENGLE, Markus FRANK, Thomas KLEIN
  • Patent number: 8962636
    Abstract: The present invention relates to substituted quinazolines of formula (I) wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV(DPP-IV).
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: February 24, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Markus Frank, Thomas Klein
  • Publication number: 20150051228
    Abstract: The present invention relates to an amorphous form of linagliptin and processes for the preparation thereof. The invention also relates to a pharmaceutical composition comprising therapeutically effective amount of an amorphous form of linagliptin and use of said composition for treatment of diabetes especially type-I or type-II, prediabetes or reduction of glucose tolerance.
    Type: Application
    Filed: March 12, 2013
    Publication date: February 19, 2015
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Shriprakash Dhar Dwivedi, Ashok Prasad, Kuldeep Natwarlal Jain, Kumar Kamlesh Singh, Jitendra Maganbhai Gajera
  • Publication number: 20140357646
    Abstract: The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.
    Type: Application
    Filed: August 19, 2014
    Publication date: December 4, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Peter SIEGER, Dirk KEMMER, Peter KOHLBAUER, Thomas NICOLA, Martin RENZ
  • Publication number: 20140357863
    Abstract: The present application provides a process for preparation of Linagliptin reacting (R)-piperidine-3-amine of Formula II or an acid addition salt thereof with 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-bromoxanthine of Formula III in the presence of a suitable base in an inert organic solvent.
    Type: Application
    Filed: December 27, 2012
    Publication date: December 4, 2014
    Inventors: Pranab Haldar, Venkateswarlu Muvva, Anil Kumar Prataprao, Vijaya Kumar Karri, Bhanu Pratap Taduri, Venkateshwara Natraj Birudaraju
  • Patent number: 8901136
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: December 2, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Stephen Critchley, Courtney A. Cullis, Steven P. Langston, Hirotake Mitzutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil, Gabriel S. Weatherhead
  • Patent number: 8883805
    Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: November 11, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Thorsten Pachur, Thomas Nicola, Adil Duran
  • Publication number: 20140303194
    Abstract: The present invention relates to novel salt forms of a certain DPP-4 inhibitor and their use in pharmaceutical compositions useful in the treatment of type 2 diabetes, as well as their production.
    Type: Application
    Filed: May 9, 2014
    Publication date: October 9, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Peter SIEGER, Waldemar PFRENGLE
  • Publication number: 20140228283
    Abstract: The present invention relates to substituted quinazolines of formula (I) wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-W (DPP-IV).
    Type: Application
    Filed: July 13, 2012
    Publication date: August 14, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Waldemar Pfrengle, Markus Frank, Thomas Klein
  • Patent number: 8785455
    Abstract: The present invention relates to a novel polymorph of Linagliptin benzoate and to methods for its preparation. Furthermore the present invention relates to the use of the novel polymorph for the preparation of a medicament. In addition the present invention relates to pharmaceutical compositions comprising an effective amount of the novel polymorph of Linagliptin benzoate.
    Type: Grant
    Filed: May 9, 2012
    Date of Patent: July 22, 2014
    Assignee: Sandoz AG
    Inventors: Andreas Hotter, Arthur Pichler
  • Publication number: 20140128604
    Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, 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: Application
    Filed: January 14, 2014
    Publication date: May 8, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Michael MARK, Roland MAIER, Ralf LOTZ, Mohammad TADAYYON
  • Publication number: 20140121225
    Abstract: The present invention relates to a novel polymorph of Linagliptin benzoate and to methods for its preparation. Furthermore the present invention relates to the use of the novel polymorph for the preparation of a medicament. In addition the present invention relates to pharmaceutical compositions comprising an effective amount of the novel polymorph of Linagliptin benzoate.
    Type: Application
    Filed: May 9, 2012
    Publication date: May 1, 2014
    Applicant: SANDOZ AG
    Inventors: Andreas Hotter, Arthur Pichler
  • Patent number: 8664232
    Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, 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: Grant
    Filed: April 17, 2012
    Date of Patent: March 4, 2014
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf R. H. Lotz, Mohammad Tadayyon
  • Publication number: 20140057901
    Abstract: 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: Application
    Filed: February 21, 2013
    Publication date: February 27, 2014
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
  • Publication number: 20130184204
    Abstract: The present invention relates to substituted quinazolines of formula (I): wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: July 13, 2012
    Publication date: July 18, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Waldemar PFRENGLE, Markus FRANK, Thomas KLEIN
  • Publication number: 20130178485
    Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.
    Type: Application
    Filed: March 1, 2013
    Publication date: July 11, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Waldemar PFRENGLE, Thorsten PACHUR, Thomas NICOLA, Adil DURAN
  • Publication number: 20130165428
    Abstract: 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: Application
    Filed: February 21, 2013
    Publication date: June 27, 2013
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
  • Publication number: 20130150578
    Abstract: The present invention relates to novel hypoglycemic compounds of formula (1) and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 1, 2011
    Publication date: June 13, 2013
    Applicant: CADILA PHARMACEUTICALS LIMITED
    Inventors: Bakulesh Mafatlal Khamar, Chandan Singh, Rajiv Indravadan Modi
  • Publication number: 20130123283
    Abstract: The present application relates to compounds and methods for treating pain, incontinence and other conditions.
    Type: Application
    Filed: April 11, 2012
    Publication date: May 16, 2013
    Inventors: Magdalene M. Moran, Christopher Fanger, Jayhong A. Chong, Colleen McNamara, Xiaoguang Zhen, Josh Mendel-Brehm
  • Publication number: 20120296091
    Abstract: The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.
    Type: Application
    Filed: August 1, 2012
    Publication date: November 22, 2012
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG
    Inventors: Peter SIEGER, Dirk KEMMER, Peter KOHLBAUER, Thomas NICOLA, Martin RENZ
  • Publication number: 20120258170
    Abstract: A co-crystal composition comprised of Quercetin and at least one antidiabetic agent acts as a combination drug having unique physical properties and biological activity, which differ from both Quercetin in pure form and the at least one antidiabetic agent in pure form. The co-crystal composition may comprise quercetin and metformin. The co-crystals of quercetin and metformin may be prepared by grinding the compounds, and used in pharmaceutical compositions comprising these co-crystals. Co-crystal compositions of quercetin and Metformin may be used in combination with other anti-diabetic agents, including DPP-IV inhibitors.
    Type: Application
    Filed: March 19, 2012
    Publication date: October 11, 2012
    Applicant: Nutracryst Therapeutics Private Limited
    Inventors: Anil Kumar KRUTHIVENTI, Iqbal Javed, Satyanarayana Reddy Jaggavarapu, RaviKumar Nagalapalli, Ganesh Saraswatula Viswanadha, Solomon Kamalakaran Anand
  • Publication number: 20120225812
    Abstract: 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: Application
    Filed: November 9, 2010
    Publication date: September 6, 2012
    Applicant: Advinus Therapeutics Limited
    Inventors: Vidya Ramdas, Summon Koul, Sujay Basu, Yogesh Waman, Yogesh Shejul, Dinesh Barawkar, Ventaka Poornapragnacharyulu Palle
  • Patent number: 8252797
    Abstract: 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: Grant
    Filed: March 26, 2009
    Date of Patent: August 28, 2012
    Assignee: Advinus Therapeutics Pvt. Ltd.
    Inventors: Venkata Palle, Sujay Basu, Yogesh Waman, Vidya Ramdas, Dinesh Barawkar, Meena Patel, Anil Panmand
  • Publication number: 20120165525
    Abstract: The present invention relates to processes for the preparation of 8-(3R)-3-aminopiperidinyl)-7-butyn-2-yl-3 -methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione and novel intermediates useful in its synthesis.
    Type: Application
    Filed: December 14, 2011
    Publication date: June 28, 2012
    Applicant: DIPHARMA FRANCIS S.R.L.
    Inventors: Pietro ALLEGRINI, Emanuele ATTOLINO, Marco ARTICO
  • Publication number: 20120129874
    Abstract: The present invention relates to novel salt forms of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, a DPP-4 inhibitor and their use in pharmaceutical compositions useful in the treatment of type 2, diabetes, as well as their production.
    Type: Application
    Filed: December 22, 2009
    Publication date: May 24, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Peter Sieger, Waldemar Pfrengle
  • Patent number: 8143264
    Abstract: The present invention relates to a xanthine compound derivative which is 3-butyl-8-chloro-1-(3-{5-[(4-fluorophenyl)methyl]-2H-tetrazol-2-yl}propyl)-3,7-dihydro-1H-purine-2,6-dione: a pharmaceutically acceptable salt thereof, corresponding pharmaceutical formulations, combinations, preparation methods and methods or uses 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: Grant
    Filed: August 8, 2006
    Date of Patent: March 27, 2012
    Assignee: GlaxoSmithKline LLC
    Inventors: Richard Jonathan Daniel Hatley, Andrew McMurtrie Mason, Ivan Leo Pinto
  • Publication number: 20120035158
    Abstract: 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: Application
    Filed: October 25, 2011
    Publication date: February 9, 2012
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH AND CO. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
  • Publication number: 20110282031
    Abstract: This invention relates to a diagnostic probe comprising a compound of formula (I): such as 3-[2-[4-(5-aminopentyl-3-amidocarboxypropanoyl)]aminophenyl]ethyl]-8-benzyl-7-[2-ethyl(2-hydroxyethyl)amino]ethyl-1-propylxanthine, with one or more label moieties attached thereto. The compounds of the present invention are useful as diagnostic probes, including probes for diagnostic assays and imaging. Accordingly, the invention provides A1 adenosine receptor antagonist compounds with radioactive or non-radioactive labels suitable for executing such assays and imaging measurements. Labeled compounds are useful to obtain quantitative measurements of the A1 adenosine receptor antagonist compounds. They may be employed as an imaging agent in diagnostic procedures such as MRI and PET as well as cell or receptor based assays.
    Type: Application
    Filed: January 20, 2011
    Publication date: November 17, 2011
    Inventors: Constance N. Wilson, John J. Partridge
  • Patent number: 8044061
    Abstract: 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: Grant
    Filed: December 21, 2007
    Date of Patent: October 25, 2011
    Assignee: UCB Pharma GmbH
    Inventors: Christa E. Müller, Jörg Hockemeyer, Nikolay T. Tzvetkov, Joachim C. Burbiel
  • Patent number: 8026244
    Abstract: There are disclosed novel compounds of Formula (I) wherein L, 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: Grant
    Filed: April 12, 2007
    Date of Patent: September 27, 2011
    Assignee: AstraZeneca AB
    Inventors: Anna-Karin Tiden, Jenny Viklund
  • Publication number: 20110165118
    Abstract: The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: November 13, 2008
    Publication date: July 7, 2011
    Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
  • Publication number: 20110118257
    Abstract: The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Application
    Filed: November 3, 2010
    Publication date: May 19, 2011
    Applicants: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant VISWANADHA, Govindarajulu BABU, Swaroop Kumar V.S. VAKKALANKA
  • Publication number: 20110086868
    Abstract: The present application describes isoindoles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful inhibitors of VEGFR.
    Type: Application
    Filed: December 16, 2010
    Publication date: April 14, 2011
    Applicant: NOVA Southeastern University
    Inventors: Appu Rathinavelu, Sivanesan Dakshanamurthy, Nagarajan Pattabiraman
  • Publication number: 20110046368
    Abstract: The invention relates to novel ligands of 5-HT6 receptor, to a pharmaceutical composition containing said novel ligands of 5-HT6 receptor as active component and to novel medicaments used for humans and warm-blooded animals for treating diseases and conditions of central nervous system, in pathogenesis of which neuromediator systems induced by 5-HT6 receptors are playing an essential role. Azaheterocyclic compounds of the general formula 1 or racemates, or optical or geometrical isomers, or pharmaceutically acceptable salts and/or hydrates thereof are used as 5-HT6 ligands.
    Type: Application
    Filed: November 15, 2007
    Publication date: February 24, 2011
    Inventors: Andrey Alexandrovich Ivashchenko, Alexander Vasilievich Ivashchenko, Sergey Yevgenievich Tkachenko, Ilya Matusovich Okun, Nikolay Filippovich Savchuk
  • Patent number: 7888343
    Abstract: The present invention involves substituted bicyclic 8-pyrrolidinoxanthines and their derivatives of formula I: wherein the various R groups are defined herein. The present invention also comprises pharmaceutical compositions comprising them as well as processes for the preparation of these compounds and methods for the treatment of metabolic disorders such as type-2 diabetes, insulin resistance, hyperglycemia, arteriosclerosis diseases and the like through the administration of said compositions.
    Type: Grant
    Filed: January 18, 2007
    Date of Patent: February 15, 2011
    Assignee: Sanofi-A Ventis Deutschland GmbH
    Inventors: Karl Schoenafinger, Gerhard Jaehne, Elisabeth Defossa, Lothar Schwink, Holger Wagner, Christian Buning, Georg Tschank, Ulrich Werner
  • Patent number: 7838528
    Abstract: Compounds for the treatment of elevated blood glucose levels and the physiological and metabolic disorders arising therefrom are disclosed and comprise novel substituted bicyclic 8-pyrrolidinoxanthines and their derivatives of formula I: wherein the various R groups are hereinafter defined. The present invention also comprises pharmaceutical compositions comprising them as well as processes for the preparation of these compounds. Particular blood glucose disorders treatable thereby include type-2 diabetes, insulin resistance, hyperglycemia, arteriosclerotic diseases and the like.
    Type: Grant
    Filed: January 17, 2007
    Date of Patent: November 23, 2010
    Assignee: sanofi-aventis Deutschland GmbH
    Inventors: Karl Schoenafinger, Gerhard Jaehne, Elisabeth Defossa, Lothar Schwink, Holger Wagner, Christian Buning, Georg Tschank, Ulrich Werner
  • Patent number: 7820815
    Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines. The process involves reacting a compound of the formula (III) with 3-(phthalimido)piperidine or an enantiomer thereof where X is a leaving group selected from halogens and sulphonic ester acid residues, and R1 to R3 are as defined herein, to obtain a compound of the formula (II) and deprotecting the obtained compound of the formula (II) to obtain the product xanthines.
    Type: Grant
    Filed: November 4, 2005
    Date of Patent: October 26, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Thorsten Pachur, Thomas Nicola, Adil Duran
  • Patent number: 7772226
    Abstract: 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: Grant
    Filed: August 28, 2008
    Date of Patent: August 10, 2010
    Assignee: 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: 20100179128
    Abstract: 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 beneficial
    Type: Application
    Filed: August 8, 2006
    Publication date: July 15, 2010
    Inventors: Richard Jonathan Daniel Hatley, Jag Paul Heer, John Liddle, Andrew McMurtrie Mason, Ivan Leo Pinto, Shahzad Sharooq Rahman, Ian Edward David Smith
  • Patent number: 7696212
    Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, 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: Grant
    Filed: December 10, 2008
    Date of Patent: April 13, 2010
    Assignee: Boehringer Ingelheim Pharma GmbH and Co. KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Ralf Lotz, Michael Mark, Mohammad Tadayyon
  • Patent number: 7687503
    Abstract: The invention relates to a compound having general formula (I): Wherein m, R1 and R2 are as defined herein. The invention also relates to the use of the compound in therapeutics. More specifically, the compounds of the invention are inhibitors of the FAAH enzyme, and therefore, can be used for the treatment of various disorders associated with FAAH enzyme, which include in a non-limiting manner, pain, eating disorders, neurological and psychiatric pathologies, among other disorders.
    Type: Grant
    Filed: June 22, 2006
    Date of Patent: March 30, 2010
    Assignee: Sanofi-Aventis
    Inventors: Ahmed Abouabdellah, Antonio Almario Garcia, Christian Hoornaert, Adrien Tak Li
  • Publication number: 20100056506
    Abstract: The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein: R1, R2, Z1, t, and ring A are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of JNK, such as diabetes, the method comprising administering to a mammal an effective amount of a compound of formula (I).
    Type: Application
    Filed: April 19, 2007
    Publication date: March 4, 2010
    Applicant: PFIZER PRODUCTS INC.
    Inventors: Liming Huang, Song Liu, Elizabeth A. Lunney, Simon P. Planken
  • Patent number: 7645763
    Abstract: The present invention relates to substituted xanthines of general formula wherein R1 and R2 are defined as in the claims, the tautomers, the stereoisomers, the mixtures 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: Grant
    Filed: February 22, 2005
    Date of Patent: January 12, 2010
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Mohammad Tadayyon, Leo Thomas
  • Patent number: 7598379
    Abstract: The present invention provides processes for making pyridyl-linked-xanthines of formula VII, from 5,6-diamino-1H-pyrimidine-2,4-diones of formula II and acylating agents of formula VI. The xanthines are expected to be are selective antagonists of A2B adenosine receptors (ARs).
    Type: Grant
    Filed: February 27, 2006
    Date of Patent: October 6, 2009
    Assignee: PGx Health, LLC
    Inventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
  • Publication number: 20090192146
    Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.
    Type: Application
    Filed: February 9, 2009
    Publication date: July 30, 2009
    Applicant: ACEA BIOSCIENCES, INC.
    Inventors: Xiao XU, Haoyun An, Xiaobo Wang