Additional Polycyclo Ring System, Which Is Not Another Purine, Having A Hetero Ring As One Of The Cyclos Patents (Class 544/268)
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Patent number: 11400096Abstract: Certain embodiments are directed to methods of treating autoimmune disorders by administering P2 purnergic receptor antagonist and/or adenosine receptor antagonists. The P2 purnergic receptor antagonist being chemical analogs of adenosine receptor antagonist 8-Ethoxy-9-ethyl-9H-purin-6-amine. The adenosine receptor antagonists being chemical analogs of the non-hydrolysable ATP analog adenosine 5?[?-thio]triphosphate (ATP?S). Certain embodiments are directed to the use of the chemical analogs to modulate IL-17 activity.Type: GrantFiled: October 19, 2018Date of Patent: August 2, 2022Assignee: Board of Regents, The University of Texas SystemInventor: Jean X. Jiang
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Patent number: 11401269Abstract: Disclosed are new intermediates for the synthesis of Linagliptin and of its salts and a process for its preparation involving said intermediates.Type: GrantFiled: May 13, 2019Date of Patent: August 2, 2022Assignee: CAMBREX PROFARMACO MILANO S.R.L.Inventors: Cristina Ciancimino, Michele Tragni, Daniele Vigo, Oreste Piccolo
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Patent number: 11040974Abstract: The present invention provides novel crystalline forms B1 & B2 of linagliptin intermediate of structural formula V and methods for production of novel crystalline form of linagliptin intermediate represented by the following structural formula V.Type: GrantFiled: March 27, 2020Date of Patent: June 22, 2021Assignee: BIOCON LIMITEDInventors: Venkata Raghavendracharyulu Palle, Shanmughasamy Rajmahendra, Dharshan Jakkali Chandregowda, Thangarasu Ponnusamy
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Patent number: 9353114Abstract: 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: GrantFiled: August 6, 2013Date of Patent: May 31, 2016Assignee: Glenmark Pharmaceuticals LimitedInventors: Sunil Kumar Singh, Sachin Srivastava, Shekhar Bhaskar Bhirud
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Patent number: 9108964Abstract: 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: GrantFiled: January 14, 2014Date of Patent: August 18, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier
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Patent number: 9056112Abstract: 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: GrantFiled: December 27, 2012Date of Patent: June 16, 2015Assignee: DR. REDDY'S LABORATORIES LIMITEDInventors: Pranab Haldar, Venkateswarlu Muvva, Anil Kumar Prataprao, Vijaya Kumar Karri, Bhanu Pratap Taduri, Venkateshwara Natraj Birudaraju
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Patent number: 9034883Abstract: 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: GrantFiled: November 14, 2011Date of Patent: May 19, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Thomas Klein, Andreas Daiber, Odd-Eric Johansen, Michael Mark, Sanjaykumar Patel, Hans-Juergen Woerle
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Publication number: 20150126593Abstract: 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: ApplicationFiled: February 27, 2013Publication date: May 7, 2015Inventor: Mahesh Kandula
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SUBSTITUTED QUINAZOLINES, THE PREPARATION THEREOF AND THE USE THEREOF IN PHARMACEUTICAL COMPOSITIONS
Publication number: 20150112062Abstract: 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: ApplicationFiled: December 23, 2014Publication date: April 23, 2015Inventors: Waldemar PFRENGLE, Markus FRANK, Thomas KLEIN -
Substituted quinazolines, the preparation thereof and the use thereof in pharmaceutical compositions
Patent number: 8962636Abstract: 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: GrantFiled: July 13, 2012Date of Patent: February 24, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Waldemar Pfrengle, Markus Frank, Thomas Klein -
Publication number: 20150051228Abstract: 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: ApplicationFiled: March 12, 2013Publication date: February 19, 2015Applicant: CADILA HEALTHCARE LIMITEDInventors: Shriprakash Dhar Dwivedi, Ashok Prasad, Kuldeep Natwarlal Jain, Kumar Kamlesh Singh, Jitendra Maganbhai Gajera
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Publication number: 20140357646Abstract: The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.Type: ApplicationFiled: August 19, 2014Publication date: December 4, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Peter SIEGER, Dirk KEMMER, Peter KOHLBAUER, Thomas NICOLA, Martin RENZ
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Publication number: 20140357863Abstract: 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: ApplicationFiled: December 27, 2012Publication date: December 4, 2014Inventors: Pranab Haldar, Venkateswarlu Muvva, Anil Kumar Prataprao, Vijaya Kumar Karri, Bhanu Pratap Taduri, Venkateshwara Natraj Birudaraju
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Patent number: 8901136Abstract: 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: GrantFiled: June 6, 2013Date of Patent: December 2, 2014Assignee: 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
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Patent number: 8883805Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.Type: GrantFiled: March 1, 2013Date of Patent: November 11, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Waldemar Pfrengle, Thorsten Pachur, Thomas Nicola, Adil Duran
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Publication number: 20140303194Abstract: 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: ApplicationFiled: May 9, 2014Publication date: October 9, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Peter SIEGER, Waldemar PFRENGLE
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SUBSTITUTED QUINAZOLINES, THE PREPARATION THEREOF AND THE USE THEREOF IN PHARMACEUTICAL COMPOSITIONS
Publication number: 20140228283Abstract: 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: ApplicationFiled: July 13, 2012Publication date: August 14, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Waldemar Pfrengle, Markus Frank, Thomas Klein -
Patent number: 8785455Abstract: 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: GrantFiled: May 9, 2012Date of Patent: July 22, 2014Assignee: Sandoz AGInventors: Andreas Hotter, Arthur Pichler
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Publication number: 20140128604Abstract: 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: ApplicationFiled: January 14, 2014Publication date: May 8, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Michael MARK, Roland MAIER, Ralf LOTZ, Mohammad TADAYYON
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Publication number: 20140121225Abstract: 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: ApplicationFiled: May 9, 2012Publication date: May 1, 2014Applicant: SANDOZ AGInventors: Andreas Hotter, Arthur Pichler
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Patent number: 8664232Abstract: 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: GrantFiled: April 17, 2012Date of Patent: March 4, 2014Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf R. H. Lotz, Mohammad Tadayyon
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Publication number: 20140057901Abstract: 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 21, 2013Publication date: February 27, 2014Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
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Substituted quinazolines, the preparation thereof and the use thereof in pharmaceutical compositions
Publication number: 20130184204Abstract: 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: ApplicationFiled: July 13, 2012Publication date: July 18, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Waldemar PFRENGLE, Markus FRANK, Thomas KLEIN -
Publication number: 20130178485Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.Type: ApplicationFiled: March 1, 2013Publication date: July 11, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Waldemar PFRENGLE, Thorsten PACHUR, Thomas NICOLA, Adil DURAN
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Publication number: 20130165428Abstract: 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: February 21, 2013Publication date: June 27, 2013Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
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Publication number: 20130150578Abstract: The present invention relates to novel hypoglycemic compounds of formula (1) and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 1, 2011Publication date: June 13, 2013Applicant: CADILA PHARMACEUTICALS LIMITEDInventors: Bakulesh Mafatlal Khamar, Chandan Singh, Rajiv Indravadan Modi
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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
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Publication number: 20120296091Abstract: The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.Type: ApplicationFiled: August 1, 2012Publication date: November 22, 2012Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KGInventors: Peter SIEGER, Dirk KEMMER, Peter KOHLBAUER, Thomas NICOLA, Martin RENZ
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Publication number: 20120258170Abstract: 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: ApplicationFiled: March 19, 2012Publication date: October 11, 2012Applicant: Nutracryst Therapeutics Private LimitedInventors: Anil Kumar KRUTHIVENTI, Iqbal Javed, Satyanarayana Reddy Jaggavarapu, RaviKumar Nagalapalli, Ganesh Saraswatula Viswanadha, Solomon Kamalakaran Anand
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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
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Patent number: 8252797Abstract: 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: GrantFiled: March 26, 2009Date of Patent: August 28, 2012Assignee: Advinus Therapeutics Pvt. Ltd.Inventors: Venkata Palle, Sujay Basu, Yogesh Waman, Vidya Ramdas, Dinesh Barawkar, Meena Patel, Anil Panmand
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Publication number: 20120165525Abstract: 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: ApplicationFiled: December 14, 2011Publication date: June 28, 2012Applicant: DIPHARMA FRANCIS S.R.L.Inventors: Pietro ALLEGRINI, Emanuele ATTOLINO, Marco ARTICO
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Publication number: 20120129874Abstract: 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: ApplicationFiled: December 22, 2009Publication date: May 24, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Peter Sieger, Waldemar Pfrengle
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Patent number: 8143264Abstract: 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: GrantFiled: August 8, 2006Date of Patent: March 27, 2012Assignee: GlaxoSmithKline LLCInventors: Richard Jonathan Daniel Hatley, Andrew McMurtrie Mason, Ivan Leo Pinto
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Publication number: 20120035158Abstract: 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: October 25, 2011Publication date: February 9, 2012Applicant: BOEHRINGER INGELHEIM PHARMA GMBH AND CO. KGInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
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Publication number: 20110282031Abstract: 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: ApplicationFiled: January 20, 2011Publication date: November 17, 2011Inventors: Constance N. Wilson, John J. Partridge
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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
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Patent number: 8026244Abstract: 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: GrantFiled: April 12, 2007Date of Patent: September 27, 2011Assignee: AstraZeneca ABInventors: Anna-Karin Tiden, Jenny Viklund
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Publication number: 20110165118Abstract: 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: ApplicationFiled: November 13, 2008Publication date: July 7, 2011Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
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Publication number: 20110118257Abstract: 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: ApplicationFiled: November 3, 2010Publication date: May 19, 2011Applicants: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant VISWANADHA, Govindarajulu BABU, Swaroop Kumar V.S. VAKKALANKA
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Publication number: 20110086868Abstract: The present application describes isoindoles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful inhibitors of VEGFR.Type: ApplicationFiled: December 16, 2010Publication date: April 14, 2011Applicant: NOVA Southeastern UniversityInventors: Appu Rathinavelu, Sivanesan Dakshanamurthy, Nagarajan Pattabiraman
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Publication number: 20110046368Abstract: 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: ApplicationFiled: November 15, 2007Publication date: February 24, 2011Inventors: Andrey Alexandrovich Ivashchenko, Alexander Vasilievich Ivashchenko, Sergey Yevgenievich Tkachenko, Ilya Matusovich Okun, Nikolay Filippovich Savchuk
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Patent number: 7888343Abstract: 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: GrantFiled: January 18, 2007Date of Patent: February 15, 2011Assignee: Sanofi-A Ventis Deutschland GmbHInventors: Karl Schoenafinger, Gerhard Jaehne, Elisabeth Defossa, Lothar Schwink, Holger Wagner, Christian Buning, Georg Tschank, Ulrich Werner
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Patent number: 7838528Abstract: 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: GrantFiled: January 17, 2007Date of Patent: November 23, 2010Assignee: sanofi-aventis Deutschland GmbHInventors: Karl Schoenafinger, Gerhard Jaehne, Elisabeth Defossa, Lothar Schwink, Holger Wagner, Christian Buning, Georg Tschank, Ulrich Werner
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Patent number: 7820815Abstract: 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: GrantFiled: November 4, 2005Date of Patent: October 26, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Waldemar Pfrengle, Thorsten Pachur, Thomas Nicola, Adil Duran
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Patent number: 7772226Abstract: The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.Type: GrantFiled: August 28, 2008Date of Patent: August 10, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Seiji Yoshikawa, Eita Emori, Fumiyoshi Matsuura, Richard Clark, Hironori Ikuta, Kazunobu Kira, Nobuyuki Yasuda, Tadashi Nagakura, Kazuto Yamazaki
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Publication number: 20100179128Abstract: The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for the manufacture of said derivatives, pharmaceutical formulations containing these active compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficialType: ApplicationFiled: August 8, 2006Publication date: July 15, 2010Inventors: Richard Jonathan Daniel Hatley, Jag Paul Heer, John Liddle, Andrew McMurtrie Mason, Ivan Leo Pinto, Shahzad Sharooq Rahman, Ian Edward David Smith
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Patent number: 7696212Abstract: 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: GrantFiled: December 10, 2008Date of Patent: April 13, 2010Assignee: Boehringer Ingelheim Pharma GmbH and Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Ralf Lotz, Michael Mark, Mohammad Tadayyon
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Patent number: 7687503Abstract: 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: GrantFiled: June 22, 2006Date of Patent: March 30, 2010Assignee: Sanofi-AventisInventors: Ahmed Abouabdellah, Antonio Almario Garcia, Christian Hoornaert, Adrien Tak Li
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Publication number: 20100056506Abstract: 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: ApplicationFiled: April 19, 2007Publication date: March 4, 2010Applicant: PFIZER PRODUCTS INC.Inventors: Liming Huang, Song Liu, Elizabeth A. Lunney, Simon P. Planken