The Additional Hetero Ring Is Five-membered And Contains Nitrogen Patents (Class 514/217.08)
  • Patent number: 10131658
    Abstract: Provided herein, inter alia, are methods and compositions for inhibiting ?v?1 integrin and for treating fibrosis.
    Type: Grant
    Filed: March 29, 2016
    Date of Patent: November 20, 2018
    Assignee: The Regents of the University of California
    Inventors: William F. DeGrado, Dean Sheppard, Hyunil Jo, Nilgun Isik Reed, Youzhi Tang
  • Patent number: 9464072
    Abstract: A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme activity.
    Type: Grant
    Filed: December 12, 2014
    Date of Patent: October 11, 2016
    Assignee: AbbVie Inc.
    Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Yixian Long, Jurgen Dinges, Karla Drescher, Peer Jacobson, Hwan-soo Jae, Ravi Kurukulasuriya, James T. Link, David J. Madar, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Lynne E. Rueter, Qi Shuai, Bryan K. Sorensen, Jiahong Wang, Karsten M. Wicke, Martin Winn, Dariusz Wodka, Vince Yeh, Hong Yong
  • Patent number: 9212172
    Abstract: Aspects of the present disclosure include crystalline bazedoxifene free base, crystalline bazedoxifene acetate Form D, and processes for their preparation. The drug compound having the adopted name “bazedoxifene acetate” has a chemical name 1-[4-(2-azepan-1-yl-ethoxy)benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol acetic acid, and has the chemical structure shown below as Formula I.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: December 15, 2015
    Assignees: DR. REDDY'S LABORATORIES LIMITED, DR. REDDY'S LABORATORIES, INC.
    Inventors: Sundra Lakshmi Kanniah, Rajesham Boge, Peddireddy Subbareddy, Lalita Kanwar, Srividya Ramakrishnan, Ramya Kumar, Rakeshwar Bandichhor, Amarnath Reddy Lekkala, Ravi Kumar Mylavarapu, Vagwala Raghunath
  • Patent number: 9145397
    Abstract: The present invention relates to a new process for the preparation of a crystalline polymorph of a vasopressin V2 agonist.
    Type: Grant
    Filed: March 30, 2012
    Date of Patent: September 29, 2015
    Assignee: Vantia Limited
    Inventor: Valerie Elizabeth Peal
  • Patent number: 9062031
    Abstract: The present invention provides a reliable process for the preparation of polymorphic pure form A of Bazedoxifene x acetate. In addition, the present invention relates to a process of wet granulation of polymorphic pure form A of Bazedoxifene x acetate. The present invention also relates to pharmaceutical compositions comprising polymorphic pure form A of Bazedoxifene x acetate as well as to the use of cyclic ethers for the preparation of such pharmaceutical composition.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: June 23, 2015
    Assignee: SANDOZ AG
    Inventors: Arthur Pichler, Andreas Hotter, Christoph Langes
  • Publication number: 20150080381
    Abstract: Method of treating alopecia and acne with are disclosed.
    Type: Application
    Filed: April 12, 2013
    Publication date: March 19, 2015
    Inventors: Mark G. Currie, Yueh-tyng Chien
  • Publication number: 20150031680
    Abstract: The present invention relates to the long-term administration of a selective estrogen receptor modulator (SERM) with a short half-life for the treatment of a variety of estrogen receptor-mediated conditions. The SERM may be administered at a concentration at or below that of a SERM with a long half-life in order to achieve an equivalent therapeutic effect.
    Type: Application
    Filed: February 14, 2013
    Publication date: January 29, 2015
    Applicant: REPROS THERAPEUTICS INC.
    Inventors: Joseph S. Podolski, Ronald D. Wiehle
  • Publication number: 20140349987
    Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo carboxamide compounds of Formula (1) and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: December 3, 2012
    Publication date: November 27, 2014
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Patent number: 8871208
    Abstract: A method for treating a patient suffering from inflammation, chronic inflammation, pain, rheumatoid arthritis (RA), osteoarthritis and osteoporosis, comprising administering an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: October 28, 2014
    Assignee: AbbVie Inc.
    Inventors: Peer B. Jacobson, Lisa M. Olson, Sreeinvasarao Vepachedu
  • Publication number: 20140294962
    Abstract: The present invention provides a reliable process for the preparation of polymorphic pure form A of Bazedoxifene x acetate. In addition, the present invention relates to a process of wet granulation of polymorphic pure form A of Bazedoxifene x acetate. The present invention also relates to pharmaceutical compositions comprising polymorphic pure form A of Bazedoxifene x acetate as well as to the use of cyclic ethers for the preparation of such pharmaceutical composition.
    Type: Application
    Filed: December 21, 2011
    Publication date: October 2, 2014
    Applicant: SANDOZ AG
    Inventors: Arthur Pichler, Andreas Hotter, Christoph Langes
  • Publication number: 20140296213
    Abstract: The invention provides a new polymorph of 1-(2-methyl-4-(2,3,4,5-tetrahydro-1-benzazepin-1-ylcarbonyl)benzyl-carbamoyl)-L-proline-N,N-dimethylamide, pharmaceutical compositions containing it and its use in therapy.
    Type: Application
    Filed: March 31, 2011
    Publication date: October 2, 2014
    Applicant: VANTIA LIMITED
    Inventors: Kjellstrom Henrik Johan, Johansson Erik Björn, Vilhelmsen Thomas
  • Publication number: 20140228354
    Abstract: Compounds of the general structure S-1, wherein X and R1-R5 are defined in the specification, are capable of abrogating the deubiquitinating (DUB) activity of the 19S RP DUBs and are useful in methods and compositions for treating cancer, in particular, cancer tumors refractory to treatment by state-of-the-art chemotherapy.
    Type: Application
    Filed: April 18, 2014
    Publication date: August 14, 2014
    Applicant: Vivolux AB
    Inventors: Stig Linder, Rolf Larsson
  • Patent number: 8802665
    Abstract: The invention relates to a compound of formula (I) wherein A1 to A3 and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: February 14, 2013
    Date of Patent: August 12, 2014
    Assignee: Genentech, Inc.
    Inventors: David Banner, Wolfgang Haap, Thomas Luebbers, Jens-Uwe Peters
  • Patent number: 8765738
    Abstract: Compounds of the general structural formula (I) and (II) and use of the compounds and salts and hydrates thereof, as therapeutic agents are disclosed. Treatable diseases and conditions include cancers, inflammatory diseases and conditions, and immunodeficiency diseases.
    Type: Grant
    Filed: October 5, 2009
    Date of Patent: July 1, 2014
    Assignee: Incuron, LLC
    Inventors: John Tucker, Sergey Sviridov, Leonid Brodsky, Catherine Burkhart, Andrei Purmal, Katerina Gurova, Andrei Gudkov
  • Patent number: 8754107
    Abstract: The present invention is directed to novel aminopyrrolidines of formula I pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, stereoisomers thereof or pro-drugs thereof, wherein the variables are as defined herein. The compounds of formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: June 17, 2014
    Assignee: AbbVie Inc.
    Inventors: Dawn M. George, Richard W. Dixon, Michael Friedman, Adrian D. Hobson, Biqin Li, Lu Wang, Xiaoyun Wu, Neil Wishart
  • Patent number: 8735388
    Abstract: The present invention relates to heterocyclic compounds of formula (I) having affinity to muscarinic receptors, a pharmaceutical composition containing the compounds, as well as the use of the compounds for the preparation of a medicament for treating, alleviating or preventing muscarinic receptor medicated diseases and conditions.
    Type: Grant
    Filed: October 16, 2013
    Date of Patent: May 27, 2014
    Assignee: AbbVie B.V.
    Inventors: Axel Stoit, Hein K. A. C. Coolen, Cornelis G. Kruse, Jan H. Reinders
  • Publication number: 20140051687
    Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.
    Type: Application
    Filed: October 21, 2013
    Publication date: February 20, 2014
    Applicant: NeurAxon, Inc.
    Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
  • Publication number: 20140005174
    Abstract: Disclosed are the CCR2 antagonists of Formula I: I or pharmaceutically acceptable salt thereof wherein R7, A, X, B, and n are defined herein. Also disclosed are pharmaceutical compositions containing the compounds, methods of treatment using the compounds, and compositions to treat diseases or disorders associated with CCR2 activity.
    Type: Application
    Filed: March 14, 2012
    Publication date: January 2, 2014
    Inventors: Anilkumar G. Nair, Joseph A. Kozlowski, Jose S. Duca, Stuart B. Rosenblum
  • Publication number: 20130217665
    Abstract: The invention relates to a compound of formula (I) wherein A1 to A3 and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: February 14, 2013
    Publication date: August 22, 2013
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventor: HOFFMANN-LA ROCHE INC.
  • Publication number: 20130217679
    Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.
    Type: Application
    Filed: March 23, 2011
    Publication date: August 22, 2013
    Applicants: THE SCRIPPS RESEARCH INSTITUTE, THE JOHNS HOPKINS UNIVERSITY
    Inventors: Donald J. Zack, Thomas Bannister, Tomas Vojkovsky, Zhiyong Yang, Cynthia Berlinicke
  • Patent number: 8394788
    Abstract: Provided herein are small molecule compounds that alter the transport activity of solute transporters, particularly urea transporters. The compounds described herein belong to the phenylsulfoxyoxazole, phenylsulfoxyimidazole, phenylsulfoxythiazole class of compounds. The compounds described herein are useful for increasing solute clearance in states of fluid overload and for treating cardiovascular, renal, and metabolic diseases, disorders, and conditions. Methods for identifying and using these agents that inhibit urea transporters are described herein.
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: March 12, 2013
    Assignee: The Regents of the University of California
    Inventors: Alan S. Verkman, Marc Harris Levin
  • Patent number: 8318769
    Abstract: Substituted sulfonamide compounds corresponding to formula I: processes for the preparation thereof, pharmaceutical compositions containing these compounds, and the use of such substituted sulfonamide compounds in pharmaceutical compositions for the treatment and/or inhibition of pain and other conditions at least partly mediated by the bradykinin 1 receptor.
    Type: Grant
    Filed: April 8, 2009
    Date of Patent: November 27, 2012
    Assignee: Gruenethal GmbH
    Inventors: Stefan Oberboersch, Melanie Reich, Stefan Schunk, Michael Franz-Martin Engels, Ruth Jostock, Tieno Germann, Jean De Vry, Klaus Schiene, Sabine Hees
  • Publication number: 20120270847
    Abstract: Carbamate linked prodrugs of meptazinol and other opioid analgesics are provided. The prodrug moiety may comprise a single amino acid or short peptide. Additionally, the present invention relates to methods for reducing gastrointestinal side effects in a subject, the gastrointestinal side effects being associated with the administration of an opioid analgesic. The methods comprise orally administering an opioid prodrug or pharmaceutically acceptable salt thereof to a subject, wherein the opioid pro-drug is comprised of an opioid analgesic covalently bonded through a carbamate linkage to a prodrug moiety, and wherein upon oral administration, the prodrug or pharmaceutically acceptable salt minimizes at least one gastrointestinal side effect associated with oral administration of the opioid analgesic alone. Compositions for use with the method are also provided.
    Type: Application
    Filed: July 16, 2010
    Publication date: October 25, 2012
    Applicant: SHIRE LLC
    Inventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
  • Publication number: 20120245147
    Abstract: Methods for screening for inhibitors of endoplasmic reticulum (ER) stress are provided. These methods involve the addition of thapsigargin, which induces ER stress, and a test agent to mammalian cells in multi-well plates. Cell survival can be readily monitored by measuring intracellular ATP content using a bioluminescent reagent. Screening a commercially available library of 50,000 compounds led to the identification of 93 hit compounds that were subjected to secondary assays to confirm their ability to rescue cells from thapsigargin-induced cell death.
    Type: Application
    Filed: April 19, 2012
    Publication date: September 27, 2012
    Inventors: John C. REED, In-Ki Kim
  • Publication number: 20120232063
    Abstract: The present invention relates to methods of treating a subject with malaria comprising administering a 2-aminoindole compound represented by Formula: (I)—The values and preferred values of the variables in Structural Formula I are defined herein.
    Type: Application
    Filed: October 28, 2010
    Publication date: September 13, 2012
    Inventors: Ralph Mazitschek, Jon C. Clardy, Dyann Wirth, Roger Wiegand, Sameer Urgaonkar, Mary Lynn Baniecki, Joseph Cortese, Cassandra Celatka, Yibin Xiang, Renato Skerlj, Elyse M.J. Bourque
  • Publication number: 20120220558
    Abstract: The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.
    Type: Application
    Filed: May 8, 2012
    Publication date: August 30, 2012
    Applicant: Wyeth LLC
    Inventors: Andrew Fensome, Gary S. Grubb, Diane Deborah Harrison, Richard Craig Winneker
  • Publication number: 20120135971
    Abstract: The present invention relates to methods and compositions for treating a subject suffering from a sclerosing disorder, comprising administering, to the subject, an effective amount of an estrogen receptor antagonist (“ERANT”), wherein said ERANT has essentially no estrogen receptor agonist activity under physiologic conditions.
    Type: Application
    Filed: January 18, 2012
    Publication date: May 31, 2012
    Inventors: Carol A. Feghali-Bostwick, Pamela Anne Hershberger
  • Publication number: 20120129827
    Abstract: The present invention relates to novel derivatives of 1-alkyl-6-oxo-piperidine-3-carboxylic acids and 1-alkyl-5-oxo-pyrrolidine-3-carboxylic acids represented by Formula I: wherein n is an integer of 1 or 2; R1, R2, R3, and R4 are each independently selected from the group consisting of hydrogen and methyl; X is selected from the group consisting of oxygen and nitrogen; and R5 is hydrogen or a C1-C7 linear or branched acyclic hydrocarbon group, or R5 together with X form a 3- to 8-membered heterocyclic hydrocarbon group, and their uses as cooling compounds.
    Type: Application
    Filed: November 22, 2010
    Publication date: May 24, 2012
    Inventor: Arkadiusz Kazimierski
  • Patent number: 8153625
    Abstract: The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.).
    Type: Grant
    Filed: May 10, 2010
    Date of Patent: April 10, 2012
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hiromu Habashita, Masaya Kokubo, Shiro Shibayama, Hideaki Tada, Tatsuya Tanihiro
  • Publication number: 20120040958
    Abstract: The invention is directed to novel indole carboxamide compounds. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: October 24, 2011
    Publication date: February 16, 2012
    Inventors: Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp
  • Publication number: 20110312945
    Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed.
    Type: Application
    Filed: October 1, 2009
    Publication date: December 22, 2011
    Inventors: James Jia, Ara Mermerian, Charles Kim, Regina Graul, Joel Moore
  • Publication number: 20110305661
    Abstract: Compounds of the general structural formula (I) and (II) and use of the compounds and salts and hydrates thereof, as therapeutic agents are disclosed. Treatable diseases and conditions include cancers, inflammatory diseases and conditions, and immunodeficiency diseases.
    Type: Application
    Filed: October 5, 2009
    Publication date: December 15, 2011
    Inventors: John Tucker, Sergey Sviridov, Leonid Brodsky, Catherine Burkhart, Andrei Purmal, Katerina Gurova, Andrei Gudkov
  • Patent number: 8071584
    Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: December 6, 2011
    Assignee: GlaxoSmithKline LLC
    Inventors: Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp
  • Publication number: 20110294777
    Abstract: Substituted bicyclic beta-lactams of Formula I: (I), are ?-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with ?-lactam antibiotics. In particular, the compounds can be employed with a ?-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to ?-lactam antibiotics due to the presence of the ?-lactamases.
    Type: Application
    Filed: January 15, 2009
    Publication date: December 1, 2011
    Inventors: Timothy A. Blizzard, Helen Chen, Candido Gude, Jeffrey D. Hermes, Jason Imbriglio, Seongkon Kim, Jane Y. Wu, Sookhee Ha, Christopher J. Mortko, Ian Mangion, Nelo Rivera, Rebecca T. Ruck, Michael Shevlin
  • Patent number: 8063041
    Abstract: The present disclosure relates to polymorphic Form D of bazedoxifene acetate, pharmaceutical compositions and methods of treatment using the same, and methods of preparing the same.
    Type: Grant
    Filed: June 22, 2010
    Date of Patent: November 22, 2011
    Assignee: Wyeth LLC
    Inventors: Paolo Andreella, Roberto Brescello, Ivan Michieletto, Mauro Maffini, Nicola Catozzi, Andrea Nicoli, Paolo Fornasari, Massimo Verzini, Livius Cotarca, Franco Brazzarola
  • Publication number: 20110275612
    Abstract: Disclosed is a compound of formula (I). Wherein R1, R2Ar and Cy are as defined herein, or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions of the compound of formula (I), methods of making the compounds of formula I, and methods of using the compounds of formula (I) to treat a disorder associated with activation of CCR10.
    Type: Application
    Filed: May 14, 2009
    Publication date: November 10, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Derek Cogan, Alexander Heim-Riether, Wang Mao, Craig Andrew Miller, Philip Dean Ramsden, Lana Louise Smith Keenan, Roger John Snow, Jiang-Ping Wu, Yu Yang
  • Publication number: 20110269737
    Abstract: The present invention provides compounds according to general formula (I) which are proposed for the treatment of respiratory complaints, particularly asthma and COPD.
    Type: Application
    Filed: August 26, 2009
    Publication date: November 3, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Holger Wagner, Birgit Jung, Frank Himmelsbach, Rolf Goeggel, Georg Dahmann
  • Publication number: 20110268820
    Abstract: Methods for facilitating joint immobilization or fusion using selective estrogen receptor modulator (SERM) such as raloxifene are disclosed. The SERM may be administered systemically or locally. In conjunction with SERM, other therapeutic agents such as calcium, vitamin D, bone morphogenetic protein may be administered simultaneously. The method can similarly be applied to facilitate bone repair, bone healing, and connective tissue healing processes in a patient.
    Type: Application
    Filed: April 30, 2010
    Publication date: November 3, 2011
    Inventor: John G. Stark
  • Patent number: 8034807
    Abstract: The invention deals with new crystalline salts of bazedoxifene, by means of which a high API quality can be achieved in a high yield.
    Type: Grant
    Filed: July 24, 2008
    Date of Patent: October 11, 2011
    Assignee: Zentiva k.s.
    Inventors: Josef Jirman, Jindrich Richter
  • Patent number: 8022063
    Abstract: Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis, wherein A represents a carboxyl group —COON, or a carboxyl bioisostere; A1, is hydrogen or methyl; ring Ar1 is an optionally substituted phenyl ring 5- or 6-membered monocyclic heteroaryl ring, in which AA1CHO— and L2 are linked to adjacent ring atoms; rings Are2, Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; t is 0 or 1; L2 and L3 are linker radicals as defined in the description.
    Type: Grant
    Filed: May 30, 2005
    Date of Patent: September 20, 2011
    Assignee: 7TM Pharma A/S
    Inventors: Trond Ulven, Thomas Frimurer, Øystein Rist, Evi Kostenis, Thomas Högberg, Jean-Marie Receveur, Marie Grimstrup
  • Publication number: 20110212947
    Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.
    Type: Application
    Filed: May 6, 2011
    Publication date: September 1, 2011
    Applicant: NeurAxon Inc.
    Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
  • Patent number: 7989447
    Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, or chronic pain.
    Type: Grant
    Filed: April 13, 2007
    Date of Patent: August 2, 2011
    Assignee: NeurAxon, Inc.
    Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
  • Publication number: 20110182888
    Abstract: Methods of treating patients with an HDAC inhibitor and a HER-2 inhibitor are provided herein. In some embodiments, a SERM is also administered.
    Type: Application
    Filed: April 7, 2009
    Publication date: July 28, 2011
    Inventors: Peter Ordentlich, Bob Goodenow, Bolin Liu, Xiaoping Huang
  • Publication number: 20110165241
    Abstract: This disclosure relates to pharmaceutical compositions comprising bazedoxifene and an antioxidant such as vitamin E, vitamin E TPGS, propyl gallate, citric acid, or BHA/BHT, substantially free of ascorbic acid, as well as methods of making such compositions. Also provided are methods of enhancing dissolution stability and/or enhancing bioavailability of bazedoxifene in a formulation containing an antioxidant, and methods of reducing interactions of at least one of bazedoxifene and hydroxymethyl cellulose with at least one of ascorbic acid and one or more degradant products of ascorbic acid in such compositions.
    Type: Application
    Filed: October 27, 2010
    Publication date: July 7, 2011
    Applicant: Wyeth LLC
    Inventors: Anjali Agrawal, Ramarao S. Chatlapalli, Arwinder S. Nagi, Lawrence Van Pelt, Srinivas Chirra
  • Patent number: 7968591
    Abstract: 1,3-disubstituted 4-methyl-1H-pyrrole-2-carboxamides corresponding to formula I methods for their production, pharmaceutical compositions containing them, and the use thereof for noradrenalin receptor regulation, particularly for inhibiting noradrenalin reuptake, and/or for 5-HT receptor regulation, particularly for inhibiting 5-hydroxy tryptophan reuptake, and/or for opioid receptor regulation and/or for batrachotoxin (BTX) receptor regulation and/or for treating or inhibiting pain and other conditions.
    Type: Grant
    Filed: December 9, 2008
    Date of Patent: June 28, 2011
    Assignee: Gruenenthal GmbH
    Inventors: Stefan Oberboersch, Bernd Sundermann, Corinna Sundermann, Edward Bijsterveld, Hagen-Heinrich Hennies
  • Publication number: 20110129542
    Abstract: In its many embodiments, the present invention relates to a novel class of substituted azepine- and diazepine-sulfonamide compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: August 12, 2008
    Publication date: June 2, 2011
    Inventors: Santhosh Neelamkavil, Craig D. Boyle, Samuel Chackalamannil
  • Patent number: 7943605
    Abstract: The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.
    Type: Grant
    Filed: October 25, 2006
    Date of Patent: May 17, 2011
    Assignee: UCB Pharma S.A.
    Inventors: Sylvain Celanire, Luc Quere, Frédéric Denonne, Laurent Provins
  • Publication number: 20110104121
    Abstract: The present invention provides methods for boosting mucosal immunity in the female reproductive tract of pre- and post-menopausal women using a TGF-beta inhibitor, a Selective Estrogen Receptor Modulator, and/or a recombinant commensal bacterium that expresses endogenous microbicides into the intestinal tract or reproductive tract of a subject. It also provides methods for boosting innate and adaptive immunity by providing a glucocorticoid. Methods for preventing sexually transmitted infections including HIV infection are also provided.
    Type: Application
    Filed: May 21, 2009
    Publication date: May 5, 2011
    Inventors: Charles R. Wira, John V. Fahey, Charles L. Sentman, Paul M. Guyre
  • Publication number: 20110086113
    Abstract: The invention relates to the use of one or more cannabinoids, particularly THC and/or CBD in combination with a non-cannabinoid chemotherapeutic agent in the manufacture of a medicament for use in the treatment of cancer. In particular the cancer to be treated is a brain tumour, more particularly a glioma, more particularly still a glioblastoma multiforme (GBM). The non-cannabinoid chemotherapeutic agent may be a selective estrogen receptor modulator or an alkylating agent.
    Type: Application
    Filed: June 4, 2009
    Publication date: April 14, 2011
    Inventors: Guillermo Velasco Diez, Manuel Guzman Pastor, Mar Lorente, Sofia Torres
  • Patent number: 7910576
    Abstract: The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; R7; R8; R9; R10; R11; R12; R13; A; B, D and E have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
    Type: Grant
    Filed: December 16, 2009
    Date of Patent: March 22, 2011
    Assignee: Sanofi-Aventis
    Inventors: Otmar Klingler, Joerg Czech, Werngard Czechtizky, Tilo Weiss, Melitta Just