The Additional Hetero Ring Is Five-membered And Contains Nitrogen Patents (Class 514/217.08)
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Patent number: 10416163Abstract: USP14 is a biomarker for recurrent disease and inhibition of USP14 is of therapeutic benefit for women with endometrial or ovarian cancer.Type: GrantFiled: February 27, 2017Date of Patent: September 17, 2019Assignee: Regents of the University of MinnesotaInventors: Martina Bazzaro, Tanya Pulver, Rahel Ghebre, Rachel Isaksson Vogel
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Patent number: 10131658Abstract: Provided herein, inter alia, are methods and compositions for inhibiting ?v?1 integrin and for treating fibrosis.Type: GrantFiled: March 29, 2016Date of Patent: November 20, 2018Assignee: The Regents of the University of CaliforniaInventors: William F. DeGrado, Dean Sheppard, Hyunil Jo, Nilgun Isik Reed, Youzhi Tang
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Patent number: 9464072Abstract: 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: GrantFiled: December 12, 2014Date of Patent: October 11, 2016Assignee: 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
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Patent number: 9212172Abstract: 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: GrantFiled: September 14, 2011Date of Patent: December 15, 2015Assignees: 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
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Patent number: 9145397Abstract: The present invention relates to a new process for the preparation of a crystalline polymorph of a vasopressin V2 agonist.Type: GrantFiled: March 30, 2012Date of Patent: September 29, 2015Assignee: Vantia LimitedInventor: Valerie Elizabeth Peal
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Patent number: 9062031Abstract: 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: GrantFiled: December 21, 2011Date of Patent: June 23, 2015Assignee: SANDOZ AGInventors: Arthur Pichler, Andreas Hotter, Christoph Langes
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Publication number: 20150080381Abstract: Method of treating alopecia and acne with are disclosed.Type: ApplicationFiled: April 12, 2013Publication date: March 19, 2015Inventors: Mark G. Currie, Yueh-tyng Chien
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Publication number: 20150031680Abstract: 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: ApplicationFiled: February 14, 2013Publication date: January 29, 2015Applicant: REPROS THERAPEUTICS INC.Inventors: Joseph S. Podolski, Ronald D. Wiehle
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Publication number: 20140349987Abstract: 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: ApplicationFiled: December 3, 2012Publication date: November 27, 2014Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
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Patent number: 8871208Abstract: 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: GrantFiled: December 2, 2010Date of Patent: October 28, 2014Assignee: AbbVie Inc.Inventors: Peer B. Jacobson, Lisa M. Olson, Sreeinvasarao Vepachedu
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Publication number: 20140296213Abstract: 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: ApplicationFiled: March 31, 2011Publication date: October 2, 2014Applicant: VANTIA LIMITEDInventors: Kjellstrom Henrik Johan, Johansson Erik Björn, Vilhelmsen Thomas
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Publication number: 20140294962Abstract: 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: ApplicationFiled: December 21, 2011Publication date: October 2, 2014Applicant: SANDOZ AGInventors: Arthur Pichler, Andreas Hotter, Christoph Langes
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Publication number: 20140228354Abstract: 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: ApplicationFiled: April 18, 2014Publication date: August 14, 2014Applicant: Vivolux ABInventors: Stig Linder, Rolf Larsson
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Patent number: 8802665Abstract: 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: GrantFiled: February 14, 2013Date of Patent: August 12, 2014Assignee: Genentech, Inc.Inventors: David Banner, Wolfgang Haap, Thomas Luebbers, Jens-Uwe Peters
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Patent number: 8765738Abstract: 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: GrantFiled: October 5, 2009Date of Patent: July 1, 2014Assignee: Incuron, LLCInventors: John Tucker, Sergey Sviridov, Leonid Brodsky, Catherine Burkhart, Andrei Purmal, Katerina Gurova, Andrei Gudkov
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Patent number: 8754107Abstract: 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: GrantFiled: November 16, 2007Date of Patent: June 17, 2014Assignee: AbbVie Inc.Inventors: Dawn M. George, Richard W. Dixon, Michael Friedman, Adrian D. Hobson, Biqin Li, Lu Wang, Xiaoyun Wu, Neil Wishart
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Patent number: 8735388Abstract: 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: GrantFiled: October 16, 2013Date of Patent: May 27, 2014Assignee: AbbVie B.V.Inventors: Axel Stoit, Hein K. A. C. Coolen, Cornelis G. Kruse, Jan H. Reinders
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Publication number: 20140051687Abstract: 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: ApplicationFiled: October 21, 2013Publication date: February 20, 2014Applicant: NeurAxon, Inc.Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
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Publication number: 20140005174Abstract: 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: ApplicationFiled: March 14, 2012Publication date: January 2, 2014Inventors: Anilkumar G. Nair, Joseph A. Kozlowski, Jose S. Duca, Stuart B. Rosenblum
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Publication number: 20130217665Abstract: 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: ApplicationFiled: February 14, 2013Publication date: August 22, 2013Applicant: HOFFMANN-LA ROCHE INC.Inventor: HOFFMANN-LA ROCHE INC.
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Publication number: 20130217679Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.Type: ApplicationFiled: March 23, 2011Publication date: August 22, 2013Applicants: THE SCRIPPS RESEARCH INSTITUTE, THE JOHNS HOPKINS UNIVERSITYInventors: Donald J. Zack, Thomas Bannister, Tomas Vojkovsky, Zhiyong Yang, Cynthia Berlinicke
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Patent number: 8394788Abstract: 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: GrantFiled: November 16, 2007Date of Patent: March 12, 2013Assignee: The Regents of the University of CaliforniaInventors: Alan S. Verkman, Marc Harris Levin
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Patent number: 8318769Abstract: 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: GrantFiled: April 8, 2009Date of Patent: November 27, 2012Assignee: Gruenethal GmbHInventors: Stefan Oberboersch, Melanie Reich, Stefan Schunk, Michael Franz-Martin Engels, Ruth Jostock, Tieno Germann, Jean De Vry, Klaus Schiene, Sabine Hees
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Publication number: 20120270847Abstract: 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: ApplicationFiled: July 16, 2010Publication date: October 25, 2012Applicant: SHIRE LLCInventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
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Publication number: 20120245147Abstract: 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: ApplicationFiled: April 19, 2012Publication date: September 27, 2012Inventors: John C. REED, In-Ki Kim
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Publication number: 20120232063Abstract: 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: ApplicationFiled: October 28, 2010Publication date: September 13, 2012Inventors: 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
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Publication number: 20120220558Abstract: 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: ApplicationFiled: May 8, 2012Publication date: August 30, 2012Applicant: Wyeth LLCInventors: Andrew Fensome, Gary S. Grubb, Diane Deborah Harrison, Richard Craig Winneker
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Publication number: 20120135971Abstract: 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: ApplicationFiled: January 18, 2012Publication date: May 31, 2012Inventors: Carol A. Feghali-Bostwick, Pamela Anne Hershberger
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Publication number: 20120129827Abstract: 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: ApplicationFiled: November 22, 2010Publication date: May 24, 2012Inventor: Arkadiusz Kazimierski
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Patent number: 8153625Abstract: 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: GrantFiled: May 10, 2010Date of Patent: April 10, 2012Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hiromu Habashita, Masaya Kokubo, Shiro Shibayama, Hideaki Tada, Tatsuya Tanihiro
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Publication number: 20120040958Abstract: 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: ApplicationFiled: October 24, 2011Publication date: February 16, 2012Inventors: Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp
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Publication number: 20110312945Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed.Type: ApplicationFiled: October 1, 2009Publication date: December 22, 2011Inventors: James Jia, Ara Mermerian, Charles Kim, Regina Graul, Joel Moore
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Publication number: 20110305661Abstract: 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: ApplicationFiled: October 5, 2009Publication date: December 15, 2011Inventors: John Tucker, Sergey Sviridov, Leonid Brodsky, Catherine Burkhart, Andrei Purmal, Katerina Gurova, Andrei Gudkov
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Patent number: 8071584Abstract: 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: GrantFiled: March 20, 2008Date of Patent: December 6, 2011Assignee: GlaxoSmithKline LLCInventors: Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp
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Publication number: 20110294777Abstract: 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: ApplicationFiled: January 15, 2009Publication date: December 1, 2011Inventors: 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
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Patent number: 8063041Abstract: 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: GrantFiled: June 22, 2010Date of Patent: November 22, 2011Assignee: Wyeth LLCInventors: Paolo Andreella, Roberto Brescello, Ivan Michieletto, Mauro Maffini, Nicola Catozzi, Andrea Nicoli, Paolo Fornasari, Massimo Verzini, Livius Cotarca, Franco Brazzarola
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Publication number: 20110275612Abstract: 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: ApplicationFiled: May 14, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: 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
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Publication number: 20110269737Abstract: The present invention provides compounds according to general formula (I) which are proposed for the treatment of respiratory complaints, particularly asthma and COPD.Type: ApplicationFiled: August 26, 2009Publication date: November 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Holger Wagner, Birgit Jung, Frank Himmelsbach, Rolf Goeggel, Georg Dahmann
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Publication number: 20110268820Abstract: 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: ApplicationFiled: April 30, 2010Publication date: November 3, 2011Inventor: John G. Stark
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Patent number: 8034807Abstract: 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: GrantFiled: July 24, 2008Date of Patent: October 11, 2011Assignee: Zentiva k.s.Inventors: Josef Jirman, Jindrich Richter
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Patent number: 8022063Abstract: 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: GrantFiled: May 30, 2005Date of Patent: September 20, 2011Assignee: 7TM Pharma A/SInventors: Trond Ulven, Thomas Frimurer, Øystein Rist, Evi Kostenis, Thomas Högberg, Jean-Marie Receveur, Marie Grimstrup
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Publication number: 20110212947Abstract: 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: ApplicationFiled: May 6, 2011Publication date: September 1, 2011Applicant: NeurAxon Inc.Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
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Patent number: 7989447Abstract: 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: GrantFiled: April 13, 2007Date of Patent: August 2, 2011Assignee: NeurAxon, Inc.Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
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Publication number: 20110182888Abstract: 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: ApplicationFiled: April 7, 2009Publication date: July 28, 2011Inventors: Peter Ordentlich, Bob Goodenow, Bolin Liu, Xiaoping Huang
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Publication number: 20110165241Abstract: 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: ApplicationFiled: October 27, 2010Publication date: July 7, 2011Applicant: Wyeth LLCInventors: Anjali Agrawal, Ramarao S. Chatlapalli, Arwinder S. Nagi, Lawrence Van Pelt, Srinivas Chirra
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Patent number: 7968591Abstract: 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: GrantFiled: December 9, 2008Date of Patent: June 28, 2011Assignee: Gruenenthal GmbHInventors: Stefan Oberboersch, Bernd Sundermann, Corinna Sundermann, Edward Bijsterveld, Hagen-Heinrich Hennies
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Publication number: 20110129542Abstract: 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: ApplicationFiled: August 12, 2008Publication date: June 2, 2011Inventors: Santhosh Neelamkavil, Craig D. Boyle, Samuel Chackalamannil
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Patent number: 7943605Abstract: 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: GrantFiled: October 25, 2006Date of Patent: May 17, 2011Assignee: UCB Pharma S.A.Inventors: Sylvain Celanire, Luc Quere, Frédéric Denonne, Laurent Provins
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Publication number: 20110104121Abstract: 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: ApplicationFiled: May 21, 2009Publication date: May 5, 2011Inventors: Charles R. Wira, John V. Fahey, Charles L. Sentman, Paul M. Guyre
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Publication number: 20110086113Abstract: 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: ApplicationFiled: June 4, 2009Publication date: April 14, 2011Inventors: Guillermo Velasco Diez, Manuel Guzman Pastor, Mar Lorente, Sofia Torres