Three Or More Ring Hetero Atoms In The Six-membered Hetero Ring Patents (Class 514/222.5)
  • Patent number: 11078170
    Abstract: The present disclosure provides, in part, cyclic sulfamide compounds, and pharmaceutical compositions thereof, useful as modulators of Hepatitis B (HBV) core protein, and methods of treating Hepatitis B (HBV) infection.
    Type: Grant
    Filed: March 1, 2018
    Date of Patent: August 3, 2021
    Assignee: Assembly Biosciences, Inc.
    Inventors: William W. Turner, Jr., Leping Li, Simon Nicolas Haydar, Mark G. Bures, Roopa Rai, Samson Francis, Lee D. Arnold
  • Patent number: 11021493
    Abstract: The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A, X, R2, R2?, R3, R4, R5, R6, and R7 of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A? plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, and other central nervous system conditions.
    Type: Grant
    Filed: December 13, 2017
    Date of Patent: June 1, 2021
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Matthew P. Bourbeau, James A. Brown, Ning Chen, Michael J. Frohn, Zice Fu, Longbin Liu, Qingyian Liu, Liping H. Pettus, Wenyuan Qian, Corey Reeves, Aaron C. Siegmund
  • Patent number: 10988468
    Abstract: A novel compound represented by the following general formula (1), or a salt thereof, which has a superior EP4 receptor agonist activity, and a medicament containing the compound or a salt thereof as an active ingredient, which can be used for promotion of osteogenesis, therapeutic treatment and/or promotion of healing of fracture and the like.
    Type: Grant
    Filed: December 25, 2018
    Date of Patent: April 27, 2021
    Assignee: ASAHI KASEI PHARMA CORPORATION
    Inventors: Daisuke Shikanai, Noriko Ishiguro
  • Patent number: 10968190
    Abstract: Methods for producing compounds useful in reactions to produce oxathiazin-like compounds are disclosed including a process of adding sodium 2-bromoethanesulfonate to a solution of benzyl alcohol and sodium benzyloxide to for mixture, boiling the mixture to reflux four times, concentrating under vacuum until dry, boiling with ethyl alcohol, filtering the ethyl alcohol, and concentrating to dryness to obtain solid sodium 2-benzyletherethanesulfonate.
    Type: Grant
    Filed: August 12, 2019
    Date of Patent: April 6, 2021
    Assignee: GEISTLICH PHARMA AG
    Inventor: Rolf W. Pfirrmann
  • Patent number: 10940240
    Abstract: Various embodiments relate to catheter locking solutions and catheter locking therapies with use of trisodium citrate and ethyl alcohol, and in particular 4.0 to 15.0 weight/volume % trisodium citrate as an anticoagulant component and/or an antibacterial component and 15.0 to 25.0 volume/volume % ethyl alcohol as an antibacterial component. Use of the catheter locking solution and catheter locking therapy can reduce treatment failure during medical procedures that may employ catheters to supply treatment by at least significantly reducing the risks associated with bloodstream infections, catheter system malfunction, emboli formation, patient discomfort, and patient illness. These benefits can be partially due to the synergistic antibacterial effects of the trisodium citrate and ethyl alcohol in solution, generating an effective catheter locking solution with minimal concentrations of ethyl alcohol.
    Type: Grant
    Filed: February 6, 2017
    Date of Patent: March 9, 2021
    Assignee: Medical Components, Inc.
    Inventors: Premkumar Babu, Benjamin R. Brozanski, Lisa Pagano, Jeffrey S. Bennett
  • Patent number: 10736902
    Abstract: A method of treating a patient suffering from TNBC by a multidisciplinary method involving treating the patient with a plurality of the following treatments: i) one or more checkpoint inhibitors; ii) hyperthermia treatment; iii) low dose chemotherapy; iv) Interleukin-2 (IL-2); and v) a compound selected from the group consisting of taurolidine, taurultam, oxathiazin-like compounds, and combinations thereof.
    Type: Grant
    Filed: March 17, 2017
    Date of Patent: August 11, 2020
    Assignee: GEISTLICH PHARMA AG
    Inventors: H. Paul Redmond, Rolf W. Pfirrmann
  • Patent number: 10618892
    Abstract: This invention provides an improved processes for the preparation of verubecestat (Compound of Formula (I)), a potent inhibitor of BACE-1 and BACE-2.
    Type: Grant
    Filed: February 10, 2017
    Date of Patent: April 14, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: William J. Morris, David Thaisrivongs, Thomas W. Lyons
  • Patent number: 10464932
    Abstract: A series of 3-imino-5-methyl-1,2,4-thiadiazinane 1,1-dioxide derivatives of formula (I), substituted in the 5-position by a phenyl moiety NH which in turn is meta-substituted by an optionally substituted fused bicyclic heteroaromatic ring system containing at least one nitrogen atom, being selective inhibitors of plasmepsin V activity, are beneficial as pharmaceutical agents, especially in the treatment of malaria.
    Type: Grant
    Filed: February 22, 2017
    Date of Patent: November 5, 2019
    Assignee: UCB Biopharma SPRL
    Inventors: Teresa De Haro Garcia, Martin Alexander Lowe, Malcolm Maccoss, Richard David Taylor, Zhaoning Zhu
  • Patent number: 10392355
    Abstract: Oxathiazin-like compounds, processes for making new oxathiazin-like compounds, compounds useful for making oxathiazin-like compounds, and their uses are disclosed. Processes of treating patients suffering from cancers, bacterial infections, fungal infections and/or viral infections by administering oxathiazin-like compounds are also disclosed. These compounds were found to have significantly longer half-life compared to taurolidine and taurultam.
    Type: Grant
    Filed: December 17, 2015
    Date of Patent: August 27, 2019
    Assignee: GEISTLICH PHARMA AG
    Inventor: Rolf W. Pfirrmann
  • Patent number: 10351578
    Abstract: The present invention relates to a heterocyclic-substituted pyridinopyrimidinone derivative and the use thereof as a therapeutically effective cyclin-dependent kinase (CDK) inhibitor. In particular, the present invention relates to the use of a new heterocyclic-substitute pyridinopyrimidinone derivative as shown in formula (I) and a pharmaceutical composition thereof as a selective CDK4/6 inhibitor in preventing or treating diseases related to CDK4/6.
    Type: Grant
    Filed: October 9, 2018
    Date of Patent: July 16, 2019
    Assignee: Shanghai Xunhe Pharmaceutical Technology Co. Ltd.
    Inventors: Yongyong Zheng, Hua Jin, Feng Zhou, Meihua Huang, Xin Meng
  • Patent number: 10231962
    Abstract: The present application relates to compositions, kits, uses, systems and methods of using naltrexone and bupropion, or pharmaceutically acceptable salts thereof, for reducing the risk of adverse cardiovascular outcomes or events, including Major Adverse Cardiovascular Events (MACE) in subjects, preferably those at increased risk of adverse cardiovascular outcomes or MACE, that may be overweight or obese. The present application also relates to compositions, kits, uses, systems and methods of using naltrexone and bupropion or pharmaceutically acceptable salts thereof for treatment of overweight or obesity in subjects, preferably at increased risk of adverse cardiovascular outcomes or MACE, wherein the treatment reduces the risk of MACE.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: March 19, 2019
    Assignee: Nalpropion Pharmaceuticals, Inc.
    Inventors: Preston Klassen, Kristin Taylor
  • Patent number: 9795591
    Abstract: The present invention provides methods of improving cognitive and motor deficits associated with central nervous system (CNS) disorder or condition in an animal. The methods comprise a general administration of phosphodiesterase 4 inhibitors and optionally training the animal under conditions sufficient to produce an improvement in performance.
    Type: Grant
    Filed: April 4, 2012
    Date of Patent: October 24, 2017
    Assignee: Dart Neuroscience (Cayman) Ltd.
    Inventors: Thomas M. Hallam, Tim Tully, Rusiko Bourtchouladze
  • Patent number: 9687494
    Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): (I) and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, L2-, and L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to ?-amyloid (A?) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers disease, are also disclosed.
    Type: Grant
    Filed: August 29, 2016
    Date of Patent: June 27, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh
  • Patent number: 9452996
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Grant
    Filed: October 30, 2015
    Date of Patent: September 27, 2016
    Assignee: Janssen Pharmaceutica NV
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
  • Patent number: 9447085
    Abstract: In its many embodiments, the present invention provides certain C2-ring-substituted iminothiadiazine compounds, or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers. The novel compounds of the invention are as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: December 9, 2013
    Date of Patent: September 20, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Jack D. Scott, Tesfaye Biftu
  • Patent number: 9428475
    Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): (I) and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, L2-, and L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to ?-amyloid (A?) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination nation with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers disease, are also disclosed.
    Type: Grant
    Filed: March 21, 2014
    Date of Patent: August 30, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming
  • Patent number: 9296726
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Grant
    Filed: October 29, 2014
    Date of Patent: March 29, 2016
    Assignee: Janssen Pharmaceutica NV
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth J. Wilson
  • Patent number: 9220814
    Abstract: Novel antimicrobial compositions and coatings are disclosed. The antimicrobial compositions consist of mixtures of taurolidine and protamine, including protamine salts. The antimicrobial compositions are particularly useful in coatings for implantable medical devices. The antimicrobial compositions are effective against a broad spectrum of microbes.
    Type: Grant
    Filed: September 29, 2011
    Date of Patent: December 29, 2015
    Assignee: Ethicon, Inc.
    Inventors: Joerg Priewe, Xintian Ming
  • Publication number: 20150148287
    Abstract: A liquid excipient is added to a lock solution formulation containing a lower alcohol and an anti-coagulant, antibiotic, and/or anti-microbial, such as the ethanol and tri-sodium citrate lock solution formulation, to prevent citrate from crystallizing in catheters made from silicone. The locking solution could include a liquid excipient, such as glycerol, polysorbate-20, or polyethylene glycol (PEG)-400, along with a lower alcohol, such as ethanol, and an anti-coagulant, such as tri-sodium citrate, antibiotic, and/or anti-microbial.
    Type: Application
    Filed: November 25, 2014
    Publication date: May 28, 2015
    Applicant: EXCELSIOR MEDICAL CORPORATION
    Inventors: Lecon Woo, William Anderson
  • Patent number: 9029362
    Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, -L2-, and -L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to ?-amyloid (“A?”) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: March 21, 2014
    Date of Patent: May 12, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming
  • Publication number: 20150051196
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Application
    Filed: October 29, 2014
    Publication date: February 19, 2015
    Inventors: CARL R. ILLIG, SHELLEY K. BALLENTINE, JINSHENG CHEN, RENEE LOUISE DESJARLAIS, SANATH K. MEEGALLA, MARK WALL, KENNETH J. WILSON
  • Patent number: 8952148
    Abstract: The present invention relates to a process for the preparation of substantially pure Taurolidine.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: February 10, 2015
    Assignee: Biophore India Pharmaceuticals Pvt Ltd
    Inventors: Manik Reddy Pullagurla, Jagadeesh Babu Rangisetty, Neelam Naidu Dokula
  • Patent number: 8927504
    Abstract: The present invention provides a novel therapeutic or preventive method, a pharmaceutical composition and use thereof, that exhibit superior anti-obesity effects (body weight-reducing (losing) effects and/or body fat mass-reducing effects). Specifically, the present invention provides a pharmaceutical composition comprising the combination of a dipeptidyl peptidase 4 inhibitor and a sweetener having a GLP-1 secretion-stimulating action, as well as use thereof for the manufacture of a medicament. The present invention also provides a method for treating or preventing obesity, comprising administering an effective amount of (a) a dipeptidyl peptidase 4 inhibitor and (b) a sweetener having a GLP-1 secretion-stimulating action to a patient suffering from symptoms of obesity.
    Type: Grant
    Filed: April 3, 2008
    Date of Patent: January 6, 2015
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Masaharu Shiotani, Tomomi Ishihara, Chiaki Matsushita
  • Patent number: 8901114
    Abstract: The invention relates to the compounds of formula (I) and physiologically acceptable salts thereof. The compounds are suitable, e.g., for treating hyperglycemia.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: December 2, 2014
    Assignee: Sanofi
    Inventors: Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Gerhard Kretzschmar, Kurt Ritter, Georg Tschank
  • Patent number: 8895547
    Abstract: The invention relates to the compounds of formula (I) and to the physiologically acceptable salts thereof. Said compounds are suitable e.g. for the treatment of hyperglycemia.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: November 25, 2014
    Assignee: Sanofi
    Inventors: Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Kurt Ritter, Georg Tschank
  • Patent number: 8883750
    Abstract: Methods are provided for treating diabetes, lowering plasma level of HbA1c, glucose plasma levels, total cholesterol plasma level, and/or triglyceride plasma level while increasing HDL cholesterol levels and delaying onset of diabetic retinopathy in a diabetic, pre-diabetic, or non-diabetic mammal while minimizing undesirable side effects.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: November 11, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Andrew A. Wolff, Markus Jerling
  • Patent number: 8871758
    Abstract: The invention relates to the compounds of formula (I) and to the physiologically acceptable salts thereof. Said compounds are suitable e.g. for the treatment of hyperglycemia.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: October 28, 2014
    Assignee: Sanofi
    Inventors: Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Kurt Ritter, Georg Tschank
  • Publication number: 20140309185
    Abstract: This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 16, 2014
    Inventors: Alexander Keith Stewart, Artem Plekhov, Robert Greenhouse
  • Publication number: 20140296221
    Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, -L2-, and -L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to ?-amyloid (“A?”) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimer's disease, are also disclosed.
    Type: Application
    Filed: March 21, 2014
    Publication date: October 2, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming
  • Publication number: 20140296223
    Abstract: This invention relates to a method for regulating skin pigmentation of a subject, comprising the step of administering the agent for inhibiting the expression or activation of Microphthalmia Transcription Factor (MITF) to the subject who is in need of regulation of skin pigmentation.
    Type: Application
    Filed: August 31, 2012
    Publication date: October 2, 2014
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: David E. Fisher, Rizwan Haq, Hans Ragnar Valdemar Widlund
  • Publication number: 20140296222
    Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, -L2-, and -L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to ?-amyloid (“A?”) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimer's disease, are also disclosed.
    Type: Application
    Filed: March 21, 2014
    Publication date: October 2, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh
  • Patent number: 8846666
    Abstract: The invention relates to the compounds of formula (I) and to the physiologically acceptable salts thereof. Said compounds are suitable for the treatment of hyperglycemia.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: September 30, 2014
    Assignee: Sanofi
    Inventors: Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Kurt Ritter, Georg Tschank
  • Publication number: 20140286931
    Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: June 5, 2014
    Publication date: September 25, 2014
    Inventor: Chengzhi Zhang
  • Publication number: 20140275032
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, X5, X6, Y, Z, G, R1a, R2a, R1b, R2b, R3, R4, R5 and R6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Genentech, Inc.
    Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Stuart Ward
  • Patent number: 8828995
    Abstract: The invention relates to compounds of formula (I) and to the physiologically compatible salts thereof. Said compounds are suitable, for example, for treating hyperglycemia.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: September 9, 2014
    Assignee: Sanofi
    Inventors: Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Kurt Ritter, Georg Tschank
  • Patent number: 8828994
    Abstract: The invention relates to compounds of formula (I) and to the physiologically compatible salts thereof. Said compounds are suitable, for example, for treating hyperglycemia.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: September 9, 2014
    Assignee: SANOFI
    Inventors: Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Kurt Ritter, Georg Tschank
  • Publication number: 20140243323
    Abstract: The present invention relates to inhibiting or preventing infection and protecting against patency complications after a blood catheter has been inserted in a patient comprising administering to the device a pharmaceutically effective amount of a composition comprising: (A) at least one taurinamide derivative, (B) at least one compound selected from the group consisting of biologically acceptable acids and biologically acceptable salts thereof; and (C) heparin at a low concentration.
    Type: Application
    Filed: September 24, 2013
    Publication date: August 28, 2014
    Applicant: ND Partners, LLC
    Inventor: Frank R. Prosl
  • Patent number: 8809324
    Abstract: The invention relates to the compounds of formula (I) and to the physiologically acceptable salts thereof. Said compounds are suitable e.g. for the treatment of hyperglycemia.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: August 19, 2014
    Assignee: Sanofi
    Inventors: Thomas Boehme, Kurt Ritter, Christian Engel, Torsten Haack, Stefan Guessregen, Georg Tschank
  • Patent number: 8809325
    Abstract: Disclosed is a benzyl-oxathiazine derivative, as shown in Formula I, the derivative being substituted with adamantane or noradamantane: the variables of which are as described herein; also disclosed is a method of preparation and use of same.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: August 19, 2014
    Assignee: SANOFI
    Inventors: Thomas Boehme, Kurt Ritter, Christian Engel, Torsten Haack, Stefan Guessregen, Georg Tschank
  • Publication number: 20140206675
    Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): (I) and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, L2-, and L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to ?-amyloid (A?) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination nation with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers disease, are also disclosed.
    Type: Application
    Filed: March 21, 2014
    Publication date: July 24, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh, Jeffrey A. Misiaszek, Guoqing Li
  • Patent number: 8785432
    Abstract: A single layer pharmaceutical composition comprising active agent(s) amlodipine or a pharmaceutically acceptable salt thereof and valsartan or a pharmaceutically acceptable salt thereof wherein the composition exhibits bioequivalence to the commercially available bilayer tablet dosage form comprising amlodipine besylate and valsartan; when administered to human subject, under the bioequivalence parameters of a 90% Confidence Interval for AUC which is between 80% and 125%, and a 90% Confidence Interval for Cmax, which is between 80% and 125%.
    Type: Grant
    Filed: February 21, 2008
    Date of Patent: July 22, 2014
    Assignee: Lupin Limited
    Inventors: Anirudha Bhagirath Kute, Nikhil Prabhakar Malewar, Makarand Krishnakumar Avachat
  • Publication number: 20140194412
    Abstract: The present invention provides an anticancer drug having a Ras function inhibitory action. The present invention provides a Ras function inhibitor comprising a compound represented by the formula (I?): wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Application
    Filed: May 9, 2012
    Publication date: July 10, 2014
    Applicants: KNC LABORATORIES CO., LTD., NATIONAL UNIVERSITY CORPORATION KOBE UNIVERSITY
    Inventors: Tohru Kataoka, Fumi Shima, Masahiro Neya, Daisuke Sasahara
  • Publication number: 20140155390
    Abstract: The present invention relates to a compound of Formula 1, 2 or 3: wherein A is N or —CR0—, where R0 is hydrogen, C1-C6 linear or branched chain alkyl, etc., Z is —CRe—, or, —N—, where Re is hydrogen, C1-C6 linear or branched chain alkyl,etc.; R1 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R2 are independently hydrogen or C1-C6 linear or branched chain alkyl; R3 and R4 are independently hydrogen, C1-C6 linear or branched chain alkyl, etc.;. R5 and R6 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; R8 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R9 and R10 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.
    Type: Application
    Filed: December 2, 2013
    Publication date: June 5, 2014
    Applicant: Pfizer Inc.
    Inventors: James Thomas Anderson, Eugene Lvovich Piatnitski Chekler, Edmund L. Ellsworth, Bruce Kipp Erickson, Adam Matthew Gilbert, Anthony P. Ricketts, David P. Thompson, Rayomand Jal Unwalla, Patrick Robert Verhoest
  • Patent number: 8729071
    Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): (I) and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, L2-, and L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to ?-amyloid (A?) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers disease, are also disclosed.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: May 20, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming
  • Patent number: 8710050
    Abstract: The invention relates to compounds of formula (I) and to the physiologically compatible salts thereof. Said compounds are suitable, for example, for treating hyperglycemia.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: April 29, 2014
    Assignee: Sanofi
    Inventors: Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Kurt Ritter, Georg Tschank
  • Publication number: 20140066437
    Abstract: The invention relates to the compounds of formula (I) and to the physiologically acceptable salts thereof. Said compounds are suitable e.g. for the treatment of hyperglycemia.
    Type: Application
    Filed: March 7, 2012
    Publication date: March 6, 2014
    Applicant: SANOFI
    Inventors: Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Kurt Ritter, Georg Tschank
  • Publication number: 20140057871
    Abstract: [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogues and a prophylactic and/or therapeutic agent against diabetes, obesity, or the like. [Means of solving the problem] A compound of Formula (III): (where f is 0 to 2; g is 1 to 4; j is 0 to 3; k is 0 to 2; n is 0 to 2; p is 0 to 4; h is 0 to 3; q1 id 0 to 3; q2 is 0 or 1; r1 is 0 to 2 (with the proviso that q1+q2+r1 is 0 to 5); J1a is —CR11a—, N; J2 is —CR12aR12b—, —CR12c—; T is —CH2—, O, —S(O)i— (i is an integer of 0 to 2) or —NR7—; X is O, S, or —NR7—; ring A?? is a benzene ring, a pyridine ring; ring B? is a benzene ring, a pyridine ring, a pyrimidine ring; and R1 to R14 are specific groups), a salt of the compound, or a solvate of the salt or the compound.
    Type: Application
    Filed: April 11, 2012
    Publication date: February 27, 2014
    Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Akihiro Okano, Munetaka Ohkouchi, Muneyoshi Makabe
  • Publication number: 20140038948
    Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Application
    Filed: June 25, 2013
    Publication date: February 6, 2014
    Applicant: Plexxikon Inc.
    Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
  • Publication number: 20140024636
    Abstract: Provided is a sulfamide derivative having an adamantyl group represented by the following Formula 1, or a pharmaceutically acceptable salt thereof. The sulfamide derivative suppresses the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1), and is useful in the treatment of various diseases that are mediated by 11?-HSD1.
    Type: Application
    Filed: March 30, 2012
    Publication date: January 23, 2014
    Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Ki Young Kim, Jin Hee Ahn, Seung Kyu Kang, Sang Dal Rhee, Myung Ae Bae, Sung Hoon Ahn, Hee Youn Kim, Won Hoon Jung, Nam Sook Kang
  • Publication number: 20140024584
    Abstract: The invention relates to the compounds of formula (I) and to the physiologically acceptable salts thereof. Said compounds are suitable e.g. for the treatment of hyperglycemia.
    Type: Application
    Filed: March 7, 2012
    Publication date: January 23, 2014
    Applicant: SANOFI
    Inventors: Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Kurt Ritter, Georg Tschank