Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Four-membered Hetero Ring Patents (Class 514/210.17)
  • Patent number: 11242319
    Abstract: Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.
    Type: Grant
    Filed: November 5, 2015
    Date of Patent: February 8, 2022
    Assignee: Flexus Biosciences, Inc.
    Inventors: Hilary Plake Beck, Juan Carlos Jaen, Maksim Osipov, Jay Patrick Powers, Maureen Kay Reilly, Hunter Paul Shunatona, James Ross Walker, Mikhail Zibinsky, James Aaron Balog, David K. Williams, Weiwei Guo
  • Patent number: 11141404
    Abstract: Described herein are uses of the CB1 inhibitors (e.g., antagonists, neutral antagonists, inverse agonists) and various methods of using and administering a CB1 inhibitor to a patient, especially patients showing symptoms of drug overdose or suspected of a drug overdose. Further described herein are uses wherein the CB1 inhibitor is ANEB-001. Further described herein are treatments with a CB1 inhibitor for THC or synthetic cannabinoid overdose.
    Type: Grant
    Filed: November 20, 2020
    Date of Patent: October 12, 2021
    Assignee: ANEBULO PHARMACEUTICALS, INC.
    Inventors: Joseph Fenton Lawler, Daniel Pawel Schneeberger
  • Patent number: 11130726
    Abstract: The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables RAA, n, ring A, X1, L, m, X2, R2, R3, R4, R5, X, and R6 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Grant
    Filed: November 15, 2019
    Date of Patent: September 28, 2021
    Assignees: GENENTECH, INC., XENON PHARMACEUTICALS INC.
    Inventors: Ivan William Hemeon, Brian Salvatore Safina, Daniel Sutherlin
  • Patent number: 11046646
    Abstract: Disclosed are compounds of Formula (I): (I) or a salt thereof, wherein: X is —CH2— or —C(O)—; R1 is —OH or —OP(O)(OH)2; L is a bond, —CH2—, or —C(O)—; R2 is n-C6-8 alkyl; each R3 is independently selected from Cl and —CH3; and n is zero, 1, or 2; provided that if X is —CH2—, then L is —CH2— or —C(O)—. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Grant
    Filed: August 8, 2018
    Date of Patent: June 29, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alaric J. Dyckman, Ling Li, John L. Gilmore
  • Patent number: 11034658
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R3, R4, R5, R6, and Q are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-?-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
    Type: Grant
    Filed: June 17, 2019
    Date of Patent: June 15, 2021
    Assignee: Janssen Pharmaceutica NV
    Inventors: Steven Goldberg, Connor L. Martin, Elizabeth G. Fennema, Ronald L. Wolin, Anne M. Fourie, Xiaohua Xue
  • Patent number: 10975023
    Abstract: The present invention provides compounds useful in treating or preventing inflammation acne, bacterial conditions and promoting the appearance of healthy skin and compositions including these compounds.
    Type: Grant
    Filed: January 12, 2018
    Date of Patent: April 13, 2021
    Assignee: Signum Biosciences, Inc.
    Inventors: Michael Voronkov, Edwardo Perez, Jason Healy, Jose Fernandez
  • Patent number: 10800784
    Abstract: The present invention provides a compound having a PDHK inhibitory activity and useful for the treatment or prophylaxis of diabetes (type 1 diabetes, type 2 diabetes etc.), insulin resistance syndrome, metabolic syndrome, hyperglycemia, hyperlactacidemia, diabetic complications (diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, cataract etc.), cardiac failure (acute cardiac failure, chronic cardiac failure), cardiomyopathy, myocardial ischemia, myocardial infarction, angina pectoris, dyslipidemia, atherosclerosis, peripheral arterial disease, intermittent claudication, chronic obstructive pulmonary disease, brain ischemia, cerebral apoplexy, mitochondrial disease, mitochondrial encephalomyopathy, cancer, pulmonary hypertension or Alzheimer disease. The present invention relates to a compound of the formula [I-a] or the formula [II], or a pharmaceutically acceptable salt thereof: wherein each symbol means the same as that described in the specification.
    Type: Grant
    Filed: January 30, 2019
    Date of Patent: October 13, 2020
    Assignee: JAPAN TOBACCO INC.
    Inventors: Takaki Maeba, Koichi Suzawa, Masayuki Kotoku, Ritsuki Masuo, Dai Motoda, Nobutaka Yamaoka
  • Patent number: 10570146
    Abstract: Disclosed are compounds that may be used to inhibit the action of fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL) or dual FAAH/MAGL. More particularly, compounds of formula II have utility in a variety of therapeutic uses such as treatment of pain, inflammation, neuropathy, or appetite disorder.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: February 25, 2020
    Assignee: Northeastern University
    Inventors: Alexandros Makriyannis, Vidyanand G Shukla, Shakiru O Alapafuja
  • Patent number: 10179767
    Abstract: The invention provides compounds having activity as sodium channel (e.g., NaV1.7) inhibitors that are useful for treating sodium channel-mediated diseases or conditions, such as pain, as well as other diseases and conditions associated with the mediation of sodium channels, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Grant
    Filed: May 20, 2016
    Date of Patent: January 15, 2019
    Assignees: GENENTECH, INC., XENON PHARMACEUTICALS INC.
    Inventors: Sultan Chowdhury, Christoph Martin Dehnhardt, Abid Hasan, Ivan William Hemeon, Qi Jia, Jun Li, Zhiguo Liu, Daniel F. Ortwine, Brian Safina, Daniel Sutherlin, Shaoyi Sun, Andrew D. White, Wei Gong, Alla Yurevna Zenova, Jiuxiang Zhu
  • Patent number: 9890172
    Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
    Type: Grant
    Filed: May 5, 2016
    Date of Patent: February 13, 2018
    Assignees: The Broad Institute, Inc., The General Hospital Corporation
    Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Stephen J. Haggarty, Yan-Ling Zhang
  • Patent number: 9676719
    Abstract: An object of the present invention is to provide a compound having strong human S1P2 antagonistic activity in order to develop a useful medicament for therapy of a S1P2-mediated disease such as a disease resulting from vascular constriction, fibrosis and respiratory disease. The compound represented by the general formula (I), wherein all the symbols have the same meanings as described in the specification, has a halogen atom or a haloalkyl group and a phenoxy group at certain substitution sites, and thus has strong human S1P2 antagonistic activity. Therefore, the compound can be a therapeutic agent for a S1P2-mediated disease, such as a disease resulting from vascular constriction, fibrosis and respiratory disease.
    Type: Grant
    Filed: March 25, 2014
    Date of Patent: June 13, 2017
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Kensuke Kusumi, Atsushi Naganawa, Kazuhiro Otsuki, Tetsuya Sekiguchi, Koji Shinozaki, Hiroshi Yamamoto, Yasuko Yamamoto
  • Patent number: 9622989
    Abstract: According to the invention there is provided a compound of formula (I): wherein R1, R2, R3 and n have meanings given in the description, or a pharmaceutically acceptable solvate, salt or prodrug thereof for use in the treatment of osteoporosis and/or osteopenia.
    Type: Grant
    Filed: October 21, 2014
    Date of Patent: April 18, 2017
    Assignee: HAOMA MEDICA LIMITED
    Inventors: Stephen Hodges, Robin Soper
  • Patent number: 9339542
    Abstract: A composition effective to relax smooth muscles in an individual in an altered state is described. The composition includes a dosage of GABA or GABA-a analog, and a dosage of at least one of an ACE inhibitor and an ARB combined with the dosage of GABA or GABA-a analog into a deliverable form.
    Type: Grant
    Filed: April 14, 2014
    Date of Patent: May 17, 2016
    Inventor: John L Couvaras
  • Patent number: 9221792
    Abstract: Compounds of general Formula (I), and compositions comprising compounds of general formula I that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: December 29, 2015
    Assignee: AGIOS PHARMACEUTICALS, INC
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders, Shunqi Yan
  • Patent number: 9193700
    Abstract: The invention described herein pertains to compounds and compositions for treating Ape1 mediated diseases. In particular, the invention described herein pertains to quinone compounds and pharmaceutical compositions containing them for treating Ape1 mediated diseases.
    Type: Grant
    Filed: May 25, 2012
    Date of Patent: November 24, 2015
    Assignees: Indiana University Research and Technology Corporation, Apex Therapeutics, Inc.
    Inventors: Mark R. Kelley, James H. Wikel
  • Patent number: 9061067
    Abstract: The invention relates to methods for increasing the plasma half-life of a molecule, such as human growth hormone, comprising covalently linking the molecule to a heterocyclic carboxylic acid bioisostere.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: June 23, 2015
    Assignee: Novo Nordisk A/S
    Inventors: Florencio Zaragoza Dörwald, Christine Bruun Schiødt, Thomas Kruse Hansen, Kjeld Madsen
  • Publication number: 20150141399
    Abstract: Disclosed are compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
    Type: Application
    Filed: February 5, 2015
    Publication date: May 21, 2015
    Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
  • Publication number: 20150126486
    Abstract: The compound represented by the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis and respiratory diseases.
    Type: Application
    Filed: January 8, 2015
    Publication date: May 7, 2015
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Atsushi NAGANAWA, Kensuke KUSUMI, Kazuhiro OTSUKI, Tetsuya SEKIGUCHI, Akito KAKUUCHI, Koji SHINOZAKI, Hiroshi YAMAMOTO, Shigeyuki NONAKA
  • Publication number: 20150099734
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, Y and W are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Daniel HUNZIKER, Patrizio MATTEI, Harald MAUSER, Marco PRUNOTTO, Christoph ULLMER
  • Patent number: 8993553
    Abstract: The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: June 24, 2013
    Date of Patent: March 31, 2015
    Assignee: Allergan, Inc.
    Inventors: Santosh C. Sinha, Smita S. Bhat, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im, Wenkui K. Fang
  • Publication number: 20150087626
    Abstract: There is described a novel group of cyclic amine derivative compounds, having an EP4 receptor antagonistic activity and specifically pharmaceutical compounds which are useful for the treatment or alleviation of Prostaglandin E mediated diseases. The present invention therefore relates to novel compounds which are selective antagonists of the EP4 subtype of PGE2 receptors with analgesic and antinflammatory activity, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, migraine and endometriosis.
    Type: Application
    Filed: July 4, 2011
    Publication date: March 26, 2015
    Inventors: Manuela Borriello, Sabrina Pucci, Luigi Piero Stasi, Lucio Rovati
  • Patent number: 8987247
    Abstract: Disclosed are compounds, compositions and methods for treating metabolic diseases, including obesity and diabetes, and for reducing weight gain. Such compounds are represented by formula (I) as follows: wherein Y and Z are defined herein.
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: March 24, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Margery Connelly, Christopher M. Flores, Mark J. Macielag
  • Publication number: 20150080347
    Abstract: Disclosed is a concentrate for dilution comprising a S1P receptor agonist or a pharmaceutically acceptable salt thereof, propylene glycol and optionally glycerin. This formulation is adapted for patients in a difficult condition to swallow.
    Type: Application
    Filed: December 6, 2013
    Publication date: March 19, 2015
    Applicant: NOVARTIS AG
    Inventors: Vivian Georgousis, Wei-Qin Tong
  • Publication number: 20150057261
    Abstract: The present invention relates to azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: August 20, 2014
    Publication date: February 26, 2015
    Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
  • Publication number: 20150051186
    Abstract: The present invention relates to aryl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: August 14, 2014
    Publication date: February 19, 2015
    Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
  • Patent number: 8957061
    Abstract: The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: February 12, 2014
    Date of Patent: February 17, 2015
    Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
  • Publication number: 20150045341
    Abstract: The present invention relates to disubstituted aryl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: August 6, 2014
    Publication date: February 12, 2015
    Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
  • Patent number: 8927527
    Abstract: The present invention provides cyclic nitro compound, pharmaceutical compositions of cyclic nitro compounds and methods of using cyclic nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.
    Type: Grant
    Filed: October 19, 2012
    Date of Patent: January 6, 2015
    Assignees: EpicentRx, Inc., Alliant Techsystems Inc.
    Inventors: Mark D. Bednarski, Susan Knox, Louis Cannizzo, Kirstin Warner, Robert Wardle, Stephen Velarde, Shoucheng Ning
  • Publication number: 20140378430
    Abstract: The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to pyrrolidine and azetidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
    Type: Application
    Filed: January 4, 2013
    Publication date: December 25, 2014
    Applicant: SPINIFEX PHARMACEUTICALS PTY LTD
    Inventors: Thomas David McCarthy, Alan Naylor
  • Publication number: 20140371200
    Abstract: The present invention relates to alkene azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
  • Publication number: 20140371197
    Abstract: 4-(Azacycloalkyl)benzene-1,3-diol compounds are described corresponding to general formula (I) below: Also described, are compositions including the same, processes for preparation thereof and uses thereof in pharmaceutical or cosmetic compositions to treat pigmentary disorders.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Inventors: Jean-Guy BOITEAU, Karine BOUQUET, Sandrine Talano, Corinne MILLOIS BARBUIS
  • Publication number: 20140371198
    Abstract: Compounds are disclosed that have a formula represented by the following: These compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example inflammatory conditions, infectious diseases, autoimmune diseases, diseases involving impairment of immune cell functions, cardiometabolic diseases, and/or proliferative diseases.
    Type: Application
    Filed: June 23, 2014
    Publication date: December 18, 2014
    Inventors: Laurent Raymond Maurice Sanière, Mathieu Rafaël Pizzonero, Nicolas Triballeau, Nick Ernest René Vandeghinste, Steve Irma Joel De Vos, Reginald Christophe Xavier Brys, Christelle Dominique Bénédict Pourbaix-L'ebraly
  • Publication number: 20140349988
    Abstract: The invention provides organonitro thioether compounds, compositions containing such compounds, isolated organonitro thioether compounds and methods for using such compounds and compositions to treat cancer in a patient. Exemplary organonitro thioether compounds described herein include 2-(3,3-dinitroazetidin-1-yl)-2-oxoethyl thioethers and variants thereof. Another aspect of the invention provides a pharmaceutical composition, comprising a pharmaceutically acceptable carrier and an organonitro thioether compound described herein, such as a compound of Formula I or II. Another aspect of the invention provides a method of treating cancer in a patient. The method comprises administering to a patient in need thereof a therapeutically effective amount of an organonitro thioether compound described herein, such as a compound of Formula I or II, to treat the cancer.
    Type: Application
    Filed: May 18, 2012
    Publication date: November 27, 2014
    Applicant: RadioRx, Inc.
    Inventors: Jan Scicinski, Bryan T. Oronsky
  • Publication number: 20140343000
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: July 24, 2014
    Publication date: November 20, 2014
    Inventors: Alicia Regueiro-Ren, Zheng Liu, Jacob Swidorski, Ny Sin, Brian Lee Venables, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell
  • Patent number: 8871755
    Abstract: The present invention relates to alkene azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: February 6, 2014
    Date of Patent: October 28, 2014
    Assignee: Allergan, Inc.
    Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
  • Publication number: 20140309190
    Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphin-gosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 16, 2014
    Applicant: BIOGEN IDEC MA INC.
    Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Ma Bin, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
  • Publication number: 20140294804
    Abstract: The invention relates to methods for treating pain disorders including neuropathic and inflammatory pain and to methods to reduce or eliminate nociceptive tolerance induced by opiate analgesic use by administering an agent that suppresses or blocks S1P biological activity.
    Type: Application
    Filed: April 7, 2014
    Publication date: October 2, 2014
    Applicant: SAINT LOUIS UNIVERSITY
    Inventor: Daniela SALVEMINI
  • Publication number: 20140288034
    Abstract: A compound having an ability to bind to an S1P receptor and represented by formula (I), a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like: wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R1 is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R1 is a substituent, and wherein m is 2 or more, R1s are the same or different.
    Type: Application
    Filed: June 4, 2014
    Publication date: September 25, 2014
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Shinji NAKADE, Hirotaka Mizuno, Takeji ONO, Masashi Minami, Hiroshi Saga, Hiroshi Hagiya, Takaki Komiya, Hiromu Habashita, Haruto Kurata, Kazuhiro Ohtsuki, Kensuke Kusumi
  • Patent number: 8835418
    Abstract: The disclosure relates to hexafluoroisopropyl carbamate derivatives of general formula (I): in which: R, Z, A, m, and n are as defined in the disclosure; in the form of the base or of an addition salt with an acid, and to the preparation process and therapeutic application thereof.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: September 16, 2014
    Assignee: SANOFI
    Inventors: Regine Bartsch, Dorothee Cheuret, Luc Even, Christian Hoornaert, Jean Jeunesse, Frank Marguet
  • Patent number: 8828985
    Abstract: This invention relates to novel compounds of the Formula (I) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Grant
    Filed: February 15, 2013
    Date of Patent: September 9, 2014
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Suresh B. Singh, Colin M. Tice, Yuanjie Ye, Linghang Zhuang
  • Publication number: 20140235610
    Abstract: Use of an S1P receptor modulator in the treatment or prevention of a disease or condition dependent on brain-derived neurotrophic factor (BDNF) expression.
    Type: Application
    Filed: December 5, 2013
    Publication date: August 21, 2014
    Inventors: Yves-Alain BARDE, Graeme BILBE, Ruben DEOGRACIAS, Rainer R. KUHN, Tomoya MATSUMOTO, Anis Khusro MIR, Anna Svenja SCHUBART
  • Publication number: 20140235611
    Abstract: The compound represented by the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis and respiratory diseases.
    Type: Application
    Filed: September 27, 2012
    Publication date: August 21, 2014
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Atsushi Naganawa, Kensuke Kusumi, Kazuhiro Otsuki, Tetsuya Sekiguchi, Akito Kakuuchi, Koji Shinozaki, Hiroshi Yamamoto, Shigeyuki Nonaka
  • Patent number: 8809316
    Abstract: The present invention discloses various immunosuppressants, salts and polymorphs thereof useful in the treatment of various disorders, including peripheral neuropathy. The invention also discloses pharmaceutical formulations utilizing the immunosuppressants, alone or in combination with other compounds, useful in treating disorders such as peripheral neuropathy. The present invention also discloses a method of treating peripheral neuropathy with immunosuppressants disclosed herein.
    Type: Grant
    Filed: March 6, 2013
    Date of Patent: August 19, 2014
    Assignee: Novartis AG
    Inventors: David Leppert, Erik Wallstroem, Barbara Nuesslein-Hildesheim
  • Publication number: 20140228341
    Abstract: The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 12, 2014
    Publication date: August 14, 2014
    Applicant: Allergan, Inc.
    Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
  • Publication number: 20140228344
    Abstract: The present invention relates to alkene azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 6, 2014
    Publication date: August 14, 2014
    Applicant: Allergan, Inc.
    Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
  • Patent number: 8802659
    Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: August 12, 2014
    Assignee: Biogen Idec MA Inc.
    Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
  • Patent number: 8791100
    Abstract: The present invention relates to substituted aryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: July 29, 2014
    Assignee: Novartis AG
    Inventors: Daniela Angst, Birgit Bollbuck, Philipp Janser, Jean Quancard, Nikolaus Johannes Stiefl
  • Publication number: 20140187532
    Abstract: 4-(azacycloalkyl)benzene-1,3-diol compounds are described corresponding to general formula (I) below: Also described, are compositions including the same, processes for preparation thereof and uses thereof in pharmaceutical or cosmetic compositions to treat pigmentary disorders.
    Type: Application
    Filed: March 7, 2014
    Publication date: July 3, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Jean-Guy BOITEAU, Karine BOUQUET, Sandrine TALANO, Corinne MILLOIS BARBUIS
  • Publication number: 20140179636
    Abstract: Disclosed is a concentrate for dilution comprising a S1P receptor agonist or a pharmaceutically acceptable salt thereof, propylene glycol and optionally glycerin. This formulation is adapted for patients in a difficult condition to swallow.
    Type: Application
    Filed: December 6, 2013
    Publication date: June 26, 2014
    Applicant: NOVARTIS AG
    Inventors: Vivian Georgousis, Wei-Qin Tong
  • Publication number: 20140179665
    Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
    Type: Application
    Filed: December 9, 2013
    Publication date: June 26, 2014
    Inventors: George D. Hartman, Osvaldo A. Flores