Two Of The Cyclos Share At Least Three Ring Member (i.e., Bridged) Patents (Class 546/63)
  • Patent number: 11352365
    Abstract: The present invention is directed to a compound having Formula (I) and its enantiomer: wherein the definitions of n, R, X, Y and Y3, and Z are provided in the disclosure. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use as opioid-like agonists in the treatment of pain.
    Type: Grant
    Filed: March 18, 2019
    Date of Patent: June 7, 2022
    Assignee: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
    Inventors: Kenner Cralle Rice, Arthur E. Jacobson, Fuying Li, Eugene S. Gutman, Eric W. Bow
  • Patent number: 10233183
    Abstract: A compound having the following formula I: In formula I, R1 and R2 are independently H, alkyl, alkoxy, and halogen. A method of preparing the compound of formula I is also disclosed.
    Type: Grant
    Filed: July 23, 2018
    Date of Patent: March 19, 2019
    Assignee: SHAANXI UNIVERSITY OF SCIENCE AND TECHNOLOGY
    Inventors: Chengyuan Liang, Lei Tian, Yonghong Tang, Minghui Chang, Kaiqi Shi, Xingke Ju, Yuzhi Liu, Lili Wen, Han Li, Xuechuan Wang
  • Patent number: 9388182
    Abstract: The present invention relates to processes for preparing enantiopure Lupanine and Sparteine.
    Type: Grant
    Filed: May 20, 2014
    Date of Patent: July 12, 2016
    Assignee: STUDIENGESELLSCHAFT KOHLE MBH
    Inventors: Nuno Maulide, Bo Peng, Carlos Alberto Mateus Afonso, Raquel Frutuoso Machado Frade
  • Patent number: 9063126
    Abstract: The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) wherein a, R1, R2, R3, R4, R5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
    Type: Grant
    Filed: September 28, 2009
    Date of Patent: June 23, 2015
    Assignee: AbbVie Inc.
    Inventors: Michael R. Schrimpf, Chih-Hung Lee, Tao Li, Gregory A. Gfesser, Kathleen H. Mortell, Ramin Faghih, Diana L. Nersesian, Kevin B. Sippy, William H. Bunnelle, Marc Scanio, Lei Shi, Murali Gopalakrishnan, Diana L. Donnelly-Roberts, Min Hu
  • Patent number: 9006234
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic[4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: July 2, 2012
    Date of Patent: April 14, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty
  • Publication number: 20150098935
    Abstract: In this application Is described a composition and method for Inducing In a subject anti-hapten antibodies without Inducing antibodies to the carrier protein. Kits for designing and making compositions with desired haptens are also described. In this application Is disclosed a synthetic liposome composition comprising liposomes (L) containing monophosphoryl lipid A (MPLA) [L(MPLA)] and an immunoconjugate comprising a carrier and a hapten. In one embodiment, the carrier is a 23 amino acid hydrophobic membrane proximal external region peptide (MPER) derived from the gp41 transmembrane protein of HIV-1 that spontaneously associates with the outer surface of bilayers of liposomes containing MPLA during liposome formation.
    Type: Application
    Filed: February 8, 2013
    Publication date: April 9, 2015
    Applicant: Walter Reed Army Institute of Research
    Inventors: Carl R. Alving, Gary R. Matyas, Arthur E. Jacobson, Fuying Li, Malliga R. Iyer, Kenner C. Rice, Kejun Cheng, Alexander Mayorov
  • Publication number: 20150051393
    Abstract: A pseudorotaxane, a rotaxane and a catenane are provided. The pseudorotaxane includes at least a macrocyclic host molecule, a guest molecule, and a metal ion. The host molecule contains at least a binding unit and an aromatic linking spacer. The guest molecule has at least a recognition unit. The metal ion is used to template the threading of the guest molecule through the macrocycle host molecule by coordinating to a binding pocket formed from the binding unit of the macrocycle and the recognition moiety of the guest molecule. Rotaxanes or catenanes can be synthesized from the pseudorotaxane complexes, with or without the metal template ion in their molecular structures.
    Type: Application
    Filed: October 28, 2014
    Publication date: February 19, 2015
    Inventors: Sheng-Hsien CHIU, You-Han LIN
  • Patent number: 8937084
    Abstract: The application is directed to compounds of Formula I-A and pharmaceutically acceptable salts and solvates thereof, wherein R1a-R3a, R4, Y, and Z are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I-A to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: January 20, 2015
    Assignee: Purdue Pharma L.P.
    Inventors: Jae Hyun Park, Laykea Tafesse
  • Publication number: 20140303144
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?2B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: October 9, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvajit Chakravarty
  • Publication number: 20140296209
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?1B—The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: October 2, 2014
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventors: Andrew Asher Protter, Sarvajit Chakravarty
  • Publication number: 20140228353
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 14, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvvajit Chakravarty
  • Patent number: 8778959
    Abstract: The present application relates to indole and indoline derivatives of formula (I) wherein a, R1, R2, R3, h, i, j, m, n, L, Q, and X are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: July 15, 2014
    Assignee: AbbVie Inc.
    Inventors: Lei Shi, William H. Bunnelle, Tao Li, Marc J. Scanio, Michael R. Schrimpf, Chih-Hung Lee
  • Publication number: 20140179669
    Abstract: The present invention relates to compounds defined by formula I wherein the groups A, B, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.
    Type: Application
    Filed: February 27, 2014
    Publication date: June 26, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Stefan PETERS, Matthias ECKHARDT, Bradford S. HAMILTON, Frank HIMMELSBACH, Joerg KLEY
  • Publication number: 20140171461
    Abstract: The application is directed to compounds of Formula I-A and pharmaceutically acceptable salts and solvates thereof, wherein R1a-R3a, R4, Y, and Z are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I-A to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: December 13, 2013
    Publication date: June 19, 2014
    Applicant: Purdue Pharma L.P.
    Inventors: Jae Hyun PARK, Laykea Tafesse
  • Publication number: 20140163012
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described.
    Type: Application
    Filed: October 31, 2013
    Publication date: June 12, 2014
    Applicant: Albany Molecular Research, Inc.
    Inventors: Matthew D. SURMAN, Emily E. FREEMAN, Peter R. GUZZO, Alan J. HENDERSON, Mark HADDEN
  • Patent number: 8703103
    Abstract: Sterically hindered imidazole ligands are described, along with their synthesis, which are capable of coordinating to Group 2 metals, such as: calcium, magnesium, strontium, in an eta-5 coordination mode which permits the formation of monomeric or dimeric volatile complexes. A compound comprising one or more polysubstituted imidazolate anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-imidazolate anion. Synthesis of the novel compounds and their use to form BST films is also contemplated.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: April 22, 2014
    Assignee: Air Products and Chemicals, Inc.
    Inventors: John Anthony Thomas Norman, Melanie K. Perez, Moo-Sung Kim
  • Patent number: 8680111
    Abstract: The invention relates to compounds of formula (?) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: March 25, 2014
    Assignee: Pfizer Inc.
    Inventors: Simon Bailey, Benjamin Joseph Burke, Michael Raymond Collins, Jingrong Jean Cui, Judith Gail Deal, Robert Louis Hoffman, Qinhua Huang, Ted William Johnson, Robert Steven Kania, John Charles Kath, Phuong Thi Quy Le, Michele Ann McTigue, Cynthia Louise Palmer, Paul Francis Richardson, Neal William Sach
  • Patent number: 8630703
    Abstract: Hydrophobic weak base compounds such as hydrophobic weak base chemotherapeutic agents (which are not an anthracycline) for use in the treatment of medical conditions such as proliferative disease or disorder in a subject, in combination with illumination of a region in a body of the subject which is characterized by the presence of proliferating cells, are disclosed. The hydrophobic weak base compound and a wavelength of illumination are selected such that the hydrophobic weak base compound acts as a therapeutically effective photosensitizer when exposed to the illumination.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: January 14, 2014
    Assignee: Technion Research & Development Foundation Limited
    Inventors: Yehuda G. Assaraf, Yamit Adar Turgeman, Andrzej M. Skladanowski, Arjan W. Griffioen, Henk Verheul, Kristy Gotink, Hubert Van Den Bergh, Patrycja Nowak-Sliwinska
  • Patent number: 8629158
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
    Type: Grant
    Filed: July 1, 2010
    Date of Patent: January 14, 2014
    Assignee: Albany Molecular Research, Inc.
    Inventors: Peter R. Guzzo, Matthew David Surman, Alan John Henderson, Mark Hadden, Emily Elizabeth Freeman
  • Patent number: 8575186
    Abstract: The present invention relates to epiminocycloalkyl[b]indole derivatives as serotonin sub-type 6 (5-HT6) modulators, pharmaceutical compositions including these compounds, and methods of preparation and use thereof. These compounds are useful in the treatment of central nervous system disorders including obesity, metabolic syndrome, cognition, and schizophrenia. The subject compounds have the structure of formula (I) with the substituents being described herein.
    Type: Grant
    Filed: October 5, 2010
    Date of Patent: November 5, 2013
    Assignee: Albany Molecular Research, Inc.
    Inventors: Peter R. Guzzo, Alan J. Henderson, Kassoum Nacro, Matthew L. Isherwood, Animesh Ghosh, Kai Xiang
  • Patent number: 8546381
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: March 24, 2009
    Date of Patent: October 1, 2013
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Publication number: 20130252961
    Abstract: The invention relates to compounds of formula (?) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.
    Type: Application
    Filed: March 5, 2013
    Publication date: September 26, 2013
    Applicant: PFIZER INC.
    Inventors: Simon BAILEY, Benjamin Joseph Burke, Michael Raymond Collins, Jingrong Jean Cui, Judith Gail Deal, Robert Louis Hoffman, Qinhua Huang, Ted William Johnson, Robert Steven Kania, John Charles Kath, Phuong Thi Quy Le, Michele Ann McTigue, Cynthia Louise Palmer, Paul Francis Richardson, Neal William Sach
  • Publication number: 20130217675
    Abstract: This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: February 18, 2011
    Publication date: August 22, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20130190293
    Abstract: This disclosure is directed to tetracyclic pyrido[4,3-b]indole and pyrido[3,4-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: February 18, 2011
    Publication date: July 25, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20130190308
    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 25, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: Medivation Technologies, Inc.
  • Publication number: 20130190344
    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 25, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: MEDIVATION TECHNOLOGIES, INC.
  • Publication number: 20130190303
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 25, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: MEDIVATION TECHNOLOGIES, INC.
  • Publication number: 20130184269
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic[4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: March 7, 2013
    Publication date: July 18, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: Medivation Technologies, Inc.
  • Publication number: 20130172320
    Abstract: This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: February 18, 2011
    Publication date: July 4, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20130172366
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: July 2, 2012
    Publication date: July 4, 2013
    Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty
  • Patent number: 8283358
    Abstract: The current invention provides compounds having a structure according to Formulae 1, 2, 3, and 4: wherein the A-ring, B-ring, C-ring, m, n, R25, R50, and R51 are as described in the specification. The invention also provides pharmaceutical compositions comprising compounds of Formulae 1, 2, 3, and 4, as well as methods of treating cognitive disorders, such as Alzheimer's disease. The invention further provides intermediates useful in preparing the compounds of Formulae 1, 2, 3, and 4.
    Type: Grant
    Filed: September 4, 2009
    Date of Patent: October 9, 2012
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Andrei W. Konradi, Xiaocong Michael Ye, Simeon Bowers, Albert W. Garofalo, Danielle L. Aubele, Darren Dressen, Raymond Ng, Gary Probst, Christopher M. Semko, Minghua Sun, Anh P. Truong, Michael S. Dappen
  • Publication number: 20120184531
    Abstract: The present invention relates to benzofuro[3,2-c]pyridine and azepine analogs as serotonin sub-type 6 (5-HT6) modulators, pharmaceutical compositions including these compounds, methods of preparation, and use thereof. These compounds are useful in the treatment of central nervous system disorders including obesity, metabolic syndrome, cognition, schizophrenia, attention deficit hyperactivity disorder, bipolar disorder, rare and orphan diseases, and sleep disorders. The subject compounds have the structure of formula (I) with the substituents being described herein.
    Type: Application
    Filed: January 18, 2012
    Publication date: July 19, 2012
    Applicant: ALBANY MOLECULAR RESEARCH, INC.
    Inventors: Peter R. GUZZO, Alan J. HENDERSON, Matthew ISHERWOOD, Chong Yew LEE, Animesh GHOSH, He ZHAO
  • Publication number: 20120058939
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
    Type: Application
    Filed: July 1, 2010
    Publication date: March 8, 2012
    Applicant: ALBANY MOLECULAR RESEARCH, INC.
    Inventors: Peter R. GUZZO, Matthew David SURMAN, Alan John HENDERSON, Mark HADDEN, Emily Elizabeth FREEMAN
  • Publication number: 20120035351
    Abstract: Sterically hindered imidazole ligands are described, along with their synthesis, which are capable of coordinating to Group 2 metals, such as: calcium, magnesium, strontium, in an eta-5 coordination mode which permits the formation of monomeric or dimeric volatile complexes. A compound comprising one or more polysubstituted imidazolate anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-imidazolate anion.
    Type: Application
    Filed: January 28, 2011
    Publication date: February 9, 2012
    Applicant: AIR PRODUCTS AND CHEMICALS, INC.
    Inventors: John Anthony Thomas Norman, Melanie K. Perez, Moo-Sung Kim
  • Publication number: 20110269791
    Abstract: The present invention relates to compounds defined by Formula (I), wherein the groups A, B, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.
    Type: Application
    Filed: May 12, 2009
    Publication date: November 3, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Stefan Peters, Matthias Eckhardt, Bradford S. Hamilton, Frank Himmelsbach, Joerg Kley, Thorsten Lehmann-Lintz
  • Publication number: 20110245272
    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: September 23, 2010
    Publication date: October 6, 2011
    Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty
  • Publication number: 20110237582
    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: September 23, 2010
    Publication date: September 29, 2011
    Inventors: Rajendra Parasmal JAIN, Sarvajit Chakravarty
  • Publication number: 20110190262
    Abstract: The present invention relates to compounds defined by formula I wherein the groups R1 to R3, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.
    Type: Application
    Filed: November 14, 2008
    Publication date: August 4, 2011
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Matthias Eckhardt, Bradford S. Hamilton, Armin Heckel, Joerg Kley, Thorsten Lehmann-Lintz, Herbert Nar, Stefan Peters, Annette Schuler-Metz, Matthias Zentgraf
  • Publication number: 20110152248
    Abstract: The present application relates to indole and indoline derivatives of formula (I), formula (II), formula (III), or formula (IV) wherein a, R2, R3, h, k, m, n, L, Q, X, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions.
    Type: Application
    Filed: December 14, 2010
    Publication date: June 23, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Lei Shi, William H. Bunnelle, Tao Li, Marc J. Scanio, Michael R. Schrimpf, Chih-Hing Lee
  • Publication number: 20110152306
    Abstract: The present application relates to indole and indoline derivatives of formula (I) wherein a, R1, R2, R3, h, i, j, m, n, L, Q, and X are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions.
    Type: Application
    Filed: December 14, 2010
    Publication date: June 23, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Lei Shi, William H. Bunnelle, Tao Li, Marc J. Scanio, Michael R. Schrimpf, Chih-Hing Lee
  • Publication number: 20110112122
    Abstract: The present invention relates to epiminocycloalkyl[b]indole derivatives as serotonin sub-type 6 (5-HT6) modulators, pharmaceutical compositions including these compounds, and methods of preparation and use thereof. These compounds are useful in the treatment of central nervous system disorders including obesity, metabolic syndrome, cognition, and schizophrenia. The subject compounds have the structure of formula (I) with the substituents being described herein.
    Type: Application
    Filed: October 5, 2010
    Publication date: May 12, 2011
    Applicant: ALBANY MOLECULAR RESEARCH, INC.
    Inventors: Peter R. GUZZO, Alan J. HENDERSON, Kassoum NACRO, Matthew L. ISHERWOOD, Animesh GHOSH, Kai XIANG
  • Patent number: 7919620
    Abstract: The antihypertensive agent of the present invention contains a soluble silicon compound. The soluble silicon compound is preferably metasilicic acid or a salt thereof. In one embodiment, the antihypertensive agent of the present invention contains deep sea water containing the soluble silicon compound, or a dried product of such deep sea water. It is preferred that in such embodiment, the antihypertensive agent further contains metasilicic acid or a salt thereof. The amount of silicon present in the deep sea water in the form of silicic acid (SiO2—Si) is 25 ?M or more. The deep sea water is typically collected at a depth of 300 m or deeper, and preferably at a depth of 600 m or deeper.
    Type: Grant
    Filed: June 1, 2005
    Date of Patent: April 5, 2011
    Assignee: Coral Biotech Kabushiki Kaisha
    Inventor: Fusako Maehira
  • Publication number: 20110003737
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
    Type: Application
    Filed: July 1, 2010
    Publication date: January 6, 2011
    Applicant: ALBANY MOLECULAR RESEARCH, INC.
    Inventors: Peter R. GUZZO, Matthew David SURMAN, Alan John HENDERSON, Mark HADDEN, Emily Elizabeth FREEMAN
  • Publication number: 20100168427
    Abstract: Process for the preparation of N-methylnaltrexone bromide, wherein a compound of the general formula (I): wherein X? represents an anion other than the bromide anion, and R represents hydrogen or a leaving group, is dissolved or dispersed in a suitable polar solvent, the solution or dispersion is mixed with a compound containing bromide anions, and the resulting reaction mixture is stirred until N-methylnaltrexone bromide has formed and crystallised, wherein, in the case where R represents a leaving group, that group is removed during or after the reaction.
    Type: Application
    Filed: May 14, 2008
    Publication date: July 1, 2010
    Applicant: CILAG AG
    Inventors: Ulrich Weigl, Pascal Schär, Alfred Stutz
  • Publication number: 20100130512
    Abstract: Compounds of formula: are disclosed. In these compounds is a heterocyclic ring. The compounds are useful as analgesics, anti-pruritics, anti-diarrheal agents, anticonvulsants, antitussives, anorexics/antiobesity agents and as treatments for hyperalgesia, drug addiction, respiratory depression, dyskinesia, pain (including neuropathic pain), irritable bowel syndrome and gastrointestinal motility disorders.
    Type: Application
    Filed: May 15, 2008
    Publication date: May 27, 2010
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. Wentland
  • Publication number: 20100099667
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: March 24, 2009
    Publication date: April 22, 2010
    Inventors: David T. Hung, Andrew Asher Protter, Sarjavit Chakravarty, Rajendra Parasmal Jain
  • Publication number: 20090306085
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: December 19, 2008
    Publication date: December 10, 2009
    Applicant: Avila Therapeutics, Inc.
    Inventors: Russell C. Petter, Juswinder Singh, Arthur F. Kluge, Deqiang Niu, Lixin Qiao, Shomir Ghosh
  • Patent number: 7625921
    Abstract: A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) its stereoisomers thereof, or a solvate thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Z is CONR1R2 or CH2NR1R2 and where at least one of X1-X8 is N, and R, Ra, Rb, Rc and Rd are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
    Type: Grant
    Filed: January 13, 2005
    Date of Patent: December 1, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jingwu Duan, James Sheppeck, Bin Jiang, John L. Gilmore
  • Patent number: 7605264
    Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or stereoisomers or prodrugs or solvates or pharmaceutically acceptable salts thereof, wherein A, B, J, K, Z, R, Ra, Rb, Rc, and Rd, are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
    Type: Grant
    Filed: January 13, 2005
    Date of Patent: October 20, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: David S. Weinstein, James Sheppeck, John L. Gilmore
  • Publication number: 20090143417
    Abstract: The present invention is directed to methods and compositions for inducing, promoting or otherwise facilitating pain relief. More particularly the present invention discloses the combination of a nitric oxide donor and an opioid analgesic in the therapeutic management of vertebrate animals including humans, for the prevention or alleviation of pain, particularly moderate to severe pain. In particular, the nitric oxide donor is a slow-release nitric oxide donor or is formulated to provide a sustained release of a low dose of nitric oxide.
    Type: Application
    Filed: December 23, 2005
    Publication date: June 4, 2009
    Applicant: The University of Queensland
    Inventors: Maree Therese Smith, Craig McKenzie Williams