Hetero Ring Is Six-membered And Includes At Least Nitrogen And Sulfur As Ring Members Patents (Class 514/222.2)
  • Patent number: 11285215
    Abstract: Disclosed herein are compositions comprising an NSAID such as meloxicam and/or rizatriptan in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tmax of meloxicam of 3 hours or less.
    Type: Grant
    Filed: May 20, 2021
    Date of Patent: March 29, 2022
    Assignee: AXSOME THERAPEUTICS, INC.
    Inventor: Herriot Tabuteau
  • Patent number: 10537523
    Abstract: A drinkable pharmaceutical solution includes telmisartan or a pharmaceutically acceptable salt, hydrate or polymorph thereof, where the telmisartan has a concentration of 1 to 10 mg/ml within the drinkable pharmaceutical solution, and the drinkable pharmaceutical solution has a pH of 10.
    Type: Grant
    Filed: April 25, 2019
    Date of Patent: January 21, 2020
    Inventors: Detlef Mohr, Stefan Lehner
  • Patent number: 10221156
    Abstract: Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.
    Type: Grant
    Filed: July 6, 2016
    Date of Patent: March 5, 2019
    Assignee: VIIV HEALTHCARE UK (NO.5) LIMITED
    Inventors: John F. Kadow, B. Narasimhulu Naidu, Manoj Patel, Prasanna Sivaprakasam
  • Patent number: 10189819
    Abstract: The present invention provides a compound of Formula I, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.
    Type: Grant
    Filed: December 7, 2015
    Date of Patent: January 29, 2019
    Assignees: Merck Sharp & Dohme, Corp., Mochida Paraceuticals Co., Ltd.
    Inventors: Ting Zhang, Yi-Heng Chen, Liangqin Guo, Alan Hruza, Tianying Jian, Bing Li, Dongfang Meng, Dann L. Parker, Edward C. Sherer, Harold B. Wood, Isao Sakurada
  • Patent number: 10174015
    Abstract: The present invention relates to a class of substituted heterocyclic derivative and preparation method thereof.
    Type: Grant
    Filed: October 29, 2015
    Date of Patent: January 8, 2019
    Assignee: Xiamen University
    Inventors: Zuguo Liu, Yan Qiu, Jie Ren, Yuhang Li, Longhe Yang, Chenggang Zhu
  • Patent number: 10098970
    Abstract: The invention provides methods and composition developed to be used with imaging techniques and useful for diagnosis and monitoring the pain generator(s) of axial pain with or without radiculopathy and methods for screening therapeutic compounds potentially useful for treating axial pain with or without radiculopathy. Alternatively, degenerated discs can be monitored and treated before occurrence of a pathological pain condition. Pain markers and markers of degeneration include markers of neuronal, vascular, immune and matrix elements.
    Type: Grant
    Filed: April 11, 2017
    Date of Patent: October 16, 2018
    Assignee: Warsaw Orthopedic, Inc.
    Inventors: William F. McKay, Jeffrey M. Gross, Hai Trieu, Josee Roy, Susan J. Drapeau, Michael J. Schendel, Andrew J. Lowenthal Walsh
  • Patent number: 10039282
    Abstract: Illustrated are compounds of the formula (I), which are suitable for controlling animal pests including arthropods and in particular insects and acarids in which the structural elements have the meanings given in the description.
    Type: Grant
    Filed: December 12, 2014
    Date of Patent: August 7, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Adeline Köhler, Silvia Cerezo-Galvez, Bernd Alig, Reiner Fischer, Johanna Julia Hahn, Kerstin Ilg, Daniela Portz, Olga Malsam, Peter Lösel, David Wilcke
  • Patent number: 9856270
    Abstract: Dolutegravir potassium salt and solid state forms thereof are provided, as well as methods of making and interconverting these forms. The Dolutegravir potassium forms, and pharmaceutical compositions containing them, may be used to treat subjects in need of medical treatment, such as for HIV infection.
    Type: Grant
    Filed: July 17, 2014
    Date of Patent: January 2, 2018
    Assignee: Ratiopharm GMBH
    Inventors: Wolfgang Albrecht, Ludovic Coutable, Gertraud Koellner
  • Patent number: 9814707
    Abstract: The present invention is directed to provide cancer stem cell proliferation inhibitors and inducers of intracellular accumulation of reactive oxygen species. To this end, provided are cancer stem cell proliferation inhibitors and inducers of intracellular accumulation of reactive oxygen species in a cancer stem cell each containing pimozide or sertindole as an active ingredient.
    Type: Grant
    Filed: January 23, 2015
    Date of Patent: November 14, 2017
    Assignee: Keio University
    Inventors: Hideyuki Saya, Osamu Nagano, Shogo Okazaki
  • Patent number: 9757476
    Abstract: The invention provides methods and composition developed to be used with imaging techniques and useful for diagnosis and monitoring the pain generator(s) of axial pain with or without radiculopathy and methods for screening therapeutic compounds potentially useful for treating axial pain with or without radiculopathy. Alternatively, degenerated discs can be monitored and treated before occurrence of a pathological pain condition. Pain markers and markers of degeneration include markers of neuronal, vascular, immune and matrix elements.
    Type: Grant
    Filed: June 8, 2006
    Date of Patent: September 12, 2017
    Assignee: Warsaw Orthopedic, Inc.
    Inventors: William F. McKay, Jeffrey M. Gross, Hai Trieu, Josee Roy, Susan J. Drapeau, Michael J. Schendel, Andrew J. Lowenthal Walsh
  • Patent number: 9493485
    Abstract: Compounds are provided having a structure according to Formula (I): wherein A1, A2, A3, Y, R1, R2, R3, R4, R5, R6, m, n and p are defined herein. Further provided are pharmaceutical compositions including the compounds provided and methods of making and using the compounds and compositions as provided, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
    Type: Grant
    Filed: March 20, 2013
    Date of Patent: November 15, 2016
    Assignee: Imago Pharmaceuticals, Inc.
    Inventors: Ying-Zi Xu, Dean R. Artis, Simeon Bowers, Roy K. Hom, Hing L. Sham, Shendong Yuan
  • Patent number: 9415054
    Abstract: A transdermal composition and method to be used as a treatment for plantar fasciitis is provided. Transdermal composition may include a combination of about 2% w/w to about 5% w/w of piroxicam and about 95% w/w to about 98% w/w of a natural permeation enhancement (NPE) composition. The NPE composition may increase the skin permeability, enhancing the transdermal delivery flux of piroxicam via a single transdermal application, thus, reducing the time of treatment. Transdermal composition may be applied upon an area of treatment, which may include myofascial trigger points linked to pain caused by plantar fasciitis, thus treating this condition more effectively. Moreover, employing a long acting NSAID such as piroxicam, in combination with the NPE composition, may act as a faster and effective treatment for an inflammatory process compared to typical treatments.
    Type: Grant
    Filed: June 13, 2013
    Date of Patent: August 16, 2016
    Assignee: Professional Compounding Centers of America (PCCA)
    Inventor: Andrew B. Glasnapp
  • Patent number: 9115101
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, W, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 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: Grant
    Filed: July 11, 2013
    Date of Patent: August 25, 2015
    Assignee: Genentech, Inc.
    Inventors: Monique Bodil van Niel, Benjamin Fauber, Simon Gaines, Alberto Gobbi, Olivier Rene, David Vesey, Stuart Ward
  • Patent number: 9040525
    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 other diseases. [Means of Solving the Problem] A compound of Formula (1): (where n is 0 to 2; p is 0 to 4; h is 0 to 3; j is 0 to 3; k is 0 to 2; a ring B is an aryl group or a heteroaryl group; X is O, S, or —NR7—; J1 is —CR11aR11b— or —NR11c—; J2 is —CR12aR12b— or —NR12c—; and R1 to R12c are specific groups), a salt of the compound, or a solvate of the salt or the compound.
    Type: Grant
    Filed: October 11, 2011
    Date of Patent: May 26, 2015
    Assignee: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Akihiro Okano, Munetaka Ohkouchi, Muneyoshi Makabe
  • Publication number: 20150011525
    Abstract: A stable ternary solid dispersion composition with enhanced physical stability and/or bioavailability comprising: (a) about 1% wt. to about 50% wt. of one or more poorly soluble active pharmaceutical ingredient (API) which belongs to Biopharmaceutics Classification System (BCS) class II and/or IV; (b) about 11% wt. to about 50% wt. of at least one water-soluble polymer; and (c) about 20% wt. to about 99% wt. of crosslinked polyvinylpyrrolidone (crospovidone, a water-insoluble polymer). The solid dispersion is capable of inhibiting crystallization of API in solid state and/or aqueous gastrointestinal tract (GIT) medium. Also disclosed is a method of preparation of such solid dispersion composition by fusion or solvent or fusion-solvent method.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 8, 2015
    Applicant: ISP Investments Inc.
    Inventors: Yunxia Bi, Mohammed Abdul Rahman, James David Lester
  • Publication number: 20150005293
    Abstract: 5-Membered heterocyclic amides and related compounds are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Application
    Filed: September 9, 2014
    Publication date: January 1, 2015
    Inventors: Hongbin Li, Jun Yuan, Rajagopal Bakthavatchalam, Kevin J. Hodgetts, Qin Guo, Scott M. Capitosti, Jianmin Mao, David J. Wustrow
  • Publication number: 20140371211
    Abstract: A transdermal composition and method to be used as a treatment for plantar fasciitis is provided. Transdermal composition may include a combination of about 2% w/w to about 5% w/w of piroxicam and about 95% w/w to about 98% w/w of a natural permeation enhancement (NPE) composition. The NPE composition may increase the skin permeability, enhancing the transdermal delivery flux of piroxicam via a single transdermal application, thus, reducing the time of treatment. Transdermal composition may be applied upon an area of treatment, which may include myofascial trigger points linked to pain caused by plantar fasciitis, thus treating this condition more effectively. Moreover, employing a long acting NSAID such as piroxicam, in combination with the NPE composition, may act as a faster and effective treatment for an inflammatory process compared to typical treatments.
    Type: Application
    Filed: June 13, 2013
    Publication date: December 18, 2014
    Applicant: PROFESSIONAL COMPOUNDING CENTERS OF AMERICA
    Inventor: Andrew B. Glasnapp
  • Patent number: 8906962
    Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.
    Type: Grant
    Filed: September 23, 2013
    Date of Patent: December 9, 2014
    Assignee: Duke University
    Inventors: Mitchell A. deLong, John M. McIver, Robert S. Youngquist
  • 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: 8889595
    Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: November 18, 2014
    Assignees: Syngenta Participations AG, Syngenta Limited
    Inventors: John Benjamin Taylor, Jeffrey Steven Wailes, Stephane André Marie Jeanmart, Mangala Govenkar
  • Publication number: 20140323468
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2. R3, R4, R5, R6, R7, W, Y, m and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: April 28, 2014
    Publication date: October 30, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Michael BALESTRA, Jennifer BURKE, Zhidong CHEN, Derek COGAN, Lee FADER, Xin GUO, Bryan MCKIBBEN, Daniel Richard MARSHALL, Peter Allen NEMOTO, Hui YU
  • 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: 20140315895
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Application
    Filed: June 26, 2014
    Publication date: October 23, 2014
    Inventors: Michael D. Bartberger, Ana Gonzalez Buenrostro, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason A. Duquette, John Eksterowicz, Benjamin Fisher, Brian M. Fox, Jiasheng Fu, Zice Fu, Felix Gonzalez Lopez de Turiso, Michael W. Gribble, Darin J. Gustin, Julie A. Heath, Xin Huang, XianYun Jiao, Michael G. Johnson, Frank Kayser, David John Kopecky, SuJen Lai, Yihong Li, Zhihong Li, Jiwen Liu, Jonathan D. Low, Brian S. Lucas, Zhihua MA, Lawrence R. McGee, Joel Mcintosh, Dustin L. McMinn, Julio C. Medina, Jeffrey Thomas Mihalic, Steven H. Olson, Yosup Rew, Philip M. Roveto, Daqing Sun, Xiaodong Wang, Yingcai Wang, Xuelei Yan, Ming Yu, Jiang Zhu
  • Patent number: 8865705
    Abstract: Benzimidazoles having inhibitory activity on RSV replication and having the formula the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof, compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: October 21, 2014
    Assignee: Janssen R&D Ireland
    Inventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
  • Publication number: 20140303140
    Abstract: The present invention discloses compounds according to Formula I: Wherein R1a, R1b, R2, R4, R5, R6a, R6b, R7, R8, W, X, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.
    Type: Application
    Filed: March 12, 2014
    Publication date: October 9, 2014
    Applicant: GALAPAGOS NV
    Inventors: Nicolas DESROY, Bertrand HECKMANN, Reginald Christophe Xavier BRYS, Agnès Marie JONCOUR, Christophe PEIXOTO, Xavier Marie BOCK
  • Publication number: 20140275043
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted 3-phenylpropylamine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Applicant: Acucela Inc.
    Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
  • Publication number: 20140271921
    Abstract: A topical composition comprises at least 5 wt % metronidazole or a pharmacologically acceptable derivative thereof in a non-aqueous vehicle. The composition may be used in the treatment of conditions of the colon, rectum, anorectum and perianal region, in particular inflammatory bowel disease and perianal Crohn's disease. The composition also relieves pain and inflammation and promotes healing of the colon, rectum, anorectum and perianal region following surgical operations. One advantage of the composition is that topical administration of metronidazole results in a primarily local effect and thus side effects observed from systemic administration are avoided.
    Type: Application
    Filed: May 28, 2014
    Publication date: September 18, 2014
    Applicant: SLA PHARMA AG
    Inventor: DAVID NIGEL ARMSTRONG
  • Publication number: 20140256700
    Abstract: The present invention is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
    Type: Application
    Filed: February 26, 2014
    Publication date: September 11, 2014
    Inventors: Michael A. Poss, David R. Tortolani, Dharmpal S. Dodd, Christopher P. Mussari, John S. Tokarski, Ashvinikumar V. Gavai, Yufen Zhao, George V. Delucca, Daniel O'Malley, Derek J. Norris, Patrice Gill, Claude A. Quesnelle, Wen-Ching Han
  • 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: 20140249142
    Abstract: Diagnostic assays for facilitating the diagnosis of lymphoplasmacytic lymphoma (LPL) are provided. The method comprises assessing a biological sample of the subject for the presence of a mutation at position 38182641 in chromosome 3p22.2, wherein presence of the mutation is indicative that the subject has LPL. Also, provided are targeted therapies, methods for monitoring the progression or recurrence of LPL, and a sensitive and inexpensive real-time allele specific polymerase chain reaction assay for reliable and quantitative assessments of the mutation.
    Type: Application
    Filed: June 29, 2012
    Publication date: September 4, 2014
    Applicant: Dana-Farber Cancer Institute, Inc.
    Inventor: Steven P. Treon
  • 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: 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: 20140135319
    Abstract: The present invention relates to substituted imidazopyrazine compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined in the claims, to methods of and intermediates for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: December 13, 2011
    Publication date: May 15, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Marcus Koppitz, Ulrich Klar, Rolf Jautelat, Dirk Kosemund, Rolf Bohlmann, Benjamin Bader, Philip Lienau, Gerhard Siemeister
  • 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
  • Patent number: 8648118
    Abstract: This invention relates to bicyclic ring system substituted amide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: February 11, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Riccardo Giovannini, Dieter Hamprecht, Barbara Kistler, Iain Lingard
  • Publication number: 20140031330
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, W, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 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: July 11, 2013
    Publication date: January 30, 2014
    Inventors: Monique Bodil van Niel, Benjamin Fauber, Simon Gaines, Alberto Gobbi, Olivier Rene, David Vesey, Stuart Ward
  • Publication number: 20140011796
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Application
    Filed: September 12, 2013
    Publication date: January 9, 2014
    Applicant: AMGEN INC.
    Inventors: Michael David BARTBERGER, Ana Gonzalez Buenrostro, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason Duquette, John Eksterwicz, Benjamin Fisher, Brian Matthew Fox, Jiasheng Fu, Zice Fu, Felix Gonzalez Lopez De Turiso, Michael William Gribble, Dann James Gustin, Julie Anne Heath, Xin Huang, Xianyun Jiao, Michael Johnson, Frank Kayser, David John Kopecky, Sujen Lai, Yihong Li, Zhihong Li, Jiwen Liu, Jonathan Dante Low, Brian Stuart Lucas, Zhihua Ma, Lawrence R. McGee, Joel McIntosh, Dustin McMinn, Julio Cesar Medina, Jeffrey Thomas Mihalic, Steven Howard Olson, Yosup Rew, Philip Marley Roveto, Daqing Sun, Xiaodong Wang, Yingcai Wang, Xuelei Yan, Ming Yu, Jiang Zhu
  • Patent number: 8618086
    Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.
    Type: Grant
    Filed: June 13, 2008
    Date of Patent: December 31, 2013
    Assignee: Duke University
    Inventors: Mitchell Anthony deLong, John McMillan McIver, Robert Scott Youngquist
  • Patent number: 8618091
    Abstract: The present invention provides a photosensitizing composition for treatment of MRSA comprising a photosensitizer and chlorhexidine and a pharmaceutically acceptable carrier. The present invention also provides a method for reducing disease causing microbes comprising: applying the composition comprising a photosensitizer, chlorhexidine at a concentration of more than about 0.01% and less than about 2% v/v, and a pharmaceutically acceptable carrier to a treatment site; and applying light to the treatment site at a wavelength absorbed by the photosensitizer so as to reduce the microbes at the treatment site.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: December 31, 2013
    Assignee: Ondine International Ltd.
    Inventors: Cale Street, Nicolas Loebel, Lisa Pedigo
  • Patent number: 8609690
    Abstract: The present invention relates to compounds defined by formula (I) wherein the groups R1 and R2 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 ?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
    Type: Grant
    Filed: August 21, 2009
    Date of Patent: December 17, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Bradford S. Hamilton, Frank Himmelsbach, Stefan Peters
  • Publication number: 20130303524
    Abstract: The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C, D, E, F, G, H, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.
    Type: Application
    Filed: May 10, 2013
    Publication date: November 14, 2013
    Inventors: Ross Bersot, Paul Humphries
  • Publication number: 20130267508
    Abstract: Benzimidazoles having inhibitory activity on RSV replication and having the formula the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof, compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
    Type: Application
    Filed: December 16, 2011
    Publication date: October 10, 2013
    Applicant: Janssen R&D Ireland
    Inventors: Ludwig Paul Cooymans, Lili Wu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
  • Publication number: 20130252937
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: March 14, 2013
    Publication date: September 26, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Matthias ECKHARDT, Sara FRATTINI, Dieter HAMPRECHT, Frank HIMMELSBACH, Elke LANGKOPF, Iain LINGARD, Stefan PETERS, Holger WAGNER
  • Patent number: 8541466
    Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.
    Type: Grant
    Filed: August 4, 2009
    Date of Patent: September 24, 2013
    Assignee: Duke University
    Inventors: Mitchell Anthony DeLong, John McMillan McIver, Robert Scott Youngquist
  • Publication number: 20130237522
    Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Application
    Filed: April 19, 2013
    Publication date: September 12, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning PRIEPKE, Kai GERLACH, Roland PFAU, Norbert HAUEL, Iris KAUFFMANN-HEFNER, Georg DAHMANN, Herbert NAR, Sandra HANDSCHUH, Wolfgang WIENEN, Annette SCHULER-METZ
  • Publication number: 20130203739
    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 other diseases. [Means of solving the problem] A compound of Formula (1): (where n is 0 to 2; p is 0 to 4; h is 0 to 3; j is 0 to 3; k is 0 to 2; a ring B is an aryl group or a heteroaryl group; X is O, S, or —NR7—; J1 is —CR11aR11b— or —NR11c—; J2 is —CR12aR12b— or —NR12c—; and R1 to R12c are specific groups), a salt of the compound, or a solvate of the salt or the compound.
    Type: Application
    Filed: October 11, 2011
    Publication date: August 8, 2013
    Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Akihiro Okano, Munetaka Ohkouchi, Muneyoshi Makabe
  • Patent number: 8466145
    Abstract: Described are novel compounds of the Formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are effective in lowering blood glucose, serum insulin, free fatty acids, cholesterol, triglyceride levels; treatment of obesity, inflammation, autoimmune diseases such as multiple sclerosis, rheumatoid arthritis; treatment and/or prophylaxis of type II diabetes. These compounds are more particularly dipeptidyl peptidase (DPP IV) inhibitors.
    Type: Grant
    Filed: January 7, 2010
    Date of Patent: June 18, 2013
    Assignee: Orchid Chemicals & Pharmaceuticals Limited
    Inventors: Gopalan Balasubramanian, Sukumar Sakamuri, Gajendra Singh, Sivanesan Dharmalingam, Franklin Pooppady Xavier, Shridhar Narayanan, Jeyamurugan Mookkan, Jeganatha Sivakumar Balasubramanian, Agneeswari Rajalingam, Jayanarayan Kulathingal
  • Patent number: 8440613
    Abstract: The present invention relates to the use of nifurtimox for the treatment of diseases caused by trichomonads, such as, for example, histomoniasis, in particular in turkeys.
    Type: Grant
    Filed: June 20, 2009
    Date of Patent: May 14, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Achim Harder, Gisela Greif, Robrecht Froyman