Ring Nitrogen In The Additional Hetero Ring (e.g., Oxazole, Etc.) Patents (Class 514/340)
  • Patent number: 10336739
    Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.
    Type: Grant
    Filed: May 29, 2018
    Date of Patent: July 2, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: James A. Johnson, Soong-Hoon Kim
  • Patent number: 10280152
    Abstract: Provided herein are radiolabelled compounds useful for imaging GSK-3 kinase. An exemplary radiolabelled compound provided herein is useful as a radiotracer for imaging GSK-3 kinase using PET imaging. Methods for preparing the radiolabelled compounds and diagnostic methods using the radiolabelled compounds are also provided.
    Type: Grant
    Filed: March 30, 2016
    Date of Patent: May 7, 2019
    Assignee: The General Hospital Corporation
    Inventors: Neil Vasdev, Huan Steven Liang
  • Patent number: 10227340
    Abstract: Compounds having the following formula: or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein X is N or C—R7, are useful as kinase modulators, including IRAK-4 modulation.
    Type: Grant
    Filed: November 21, 2017
    Date of Patent: March 12, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Venkatram Reddy Paidi, Sreekantha Ratna Kumar, Abhisek Banerjee, Ramesh Kumar Sistla, Satheesh Kesavan Nair, William J. Pitts, John Hynes
  • Patent number: 10206400
    Abstract: The present invention relates to compounds of formula (I): wherein A1, A2, A3, A4, G1, L, Y1, Y2, Y3, Y4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: February 10, 2017
    Date of Patent: February 19, 2019
    Assignee: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
  • Patent number: 10189816
    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: August 10, 2016
    Date of Patent: January 29, 2019
    Assignee: ViiV HEALTHCARE UK (NO. 5) LIMITED
    Inventors: Kyle J. Eastman, John F. Kadow, Kyle E. Parcella, B. Narasimhulu Naidu, Tao Wang, Zhiwei Yin, Zhongxing Zhang
  • Patent number: 10174003
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted imidazole-pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase enzymes. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as pancreatic cancer, prostate cancer, breast cancer, bladder cancer, lung cancer, gastric cancer, leukemia and/or melanoma and the like.
    Type: Grant
    Filed: December 29, 2017
    Date of Patent: January 8, 2019
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Young K. Chen, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 10071085
    Abstract: The present disclosure relates to compositions and pharmaceutical formulations comprising at least one active pharmaceutical ingredient chosen from nitrocatechol derivatives of formula I as defined herein and salts, esters, hydrates, solvates and derivatives thereof and methods of making said compositions and pharmaceutical formulations.
    Type: Grant
    Filed: August 13, 2015
    Date of Patent: September 11, 2018
    Assignee: BIAL—Portela & CA, S.A.
    Inventors: Teofilo Cardoso de Vasconcelos, Ricardo Jorge dos Santos Lima, Rui Cerdeira de Campos Costa
  • Patent number: 10065944
    Abstract: A compound of formula (I) where R1, R2, X, Y, n, m, R3, R4, R5, R6 and R7 are as defined herein, for use in the prophylaxis or treatment of a central and peripheral nervous system disorder, wherein the compound of formula (I) is administered prior to sleep, before bedtime or at bedtime.
    Type: Grant
    Filed: August 9, 2013
    Date of Patent: September 4, 2018
    Assignee: BIAL-PORTELA & CA, S.A.
    Inventors: Patricio Manuel Vieira Araujo Soares Da Silva, Teresa Lucia Silva Pereira Nunes, Lyndon Christopher Wright, Pedro Nuno Leal Palma, David Alexander Learmonth
  • Patent number: 9994548
    Abstract: Disclosed are compounds and methods of using them to treat a disorder selected from the group consisting of addiction, pain, obesity, schizophrenia, epilepsy, mania and manic depression, anxiety, Alzheimer's disease, learning deficit, cognition deficit, attention deficit, memory loss, Lewy Body Dementia, Attention Deficit Hyperactivity Disorder (ADHD), Parkinson's disease, Huntington's disease, Tourette's syndrome, amyotrophic lateral sclerosis, inflammation, stroke, spinal cord injury, dyskinesias, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, autism, mutism, trichotillomania, hypothermia, and disorders of sleep.
    Type: Grant
    Filed: May 23, 2016
    Date of Patent: June 12, 2018
    Assignees: Georgetown University, Duke University
    Inventors: Milton L. Brown, Mikell A. Paige, Yingxian Xiao, Kenneth J. Kellar, Venkata M. Yenugonda, Edward D. Levin, Amir H. Rezvani
  • Patent number: 9993465
    Abstract: Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism, trichotillomania, and hypothermia.
    Type: Grant
    Filed: April 5, 2016
    Date of Patent: June 12, 2018
    Assignees: Georgetown University, Duke University
    Inventors: Yingxian Xiao, Kenneth J. Kellar, Milton L. Brown, Mikell A. Paige, Yong Liu, Edward D. Levin, Amir H. Rezvani
  • Patent number: 9809588
    Abstract: Disclosed herein are compounds and compositions useful in the treatment of GLS1 mediated diseases, such as cancer, having the structure of Formula I: Methods of inhibition GLS1 activity in a human or animal subject are also provided.
    Type: Grant
    Filed: July 2, 2015
    Date of Patent: November 7, 2017
    Assignee: Board of Regents, The University of Texas System
    Inventors: Maria Emilia Di Francesco, Philip Jones, Timothy Heffernan, Matthew M. Hamilton, Zhijun Kang, Michael J. Soth, Jason P. Burke, Kang Le, Christopher Lawrence Carroll, Wylie S. Palmer, Richard Lewis, Timothy McAfoos, Barbara Czako, Gang Liu, Jay Theroff, Zachary Herrera, Anne Yau
  • Patent number: 9745290
    Abstract: The invention relates to the use of an oxodiazolyl compound (I) for the preparation of a medicament for the prevention or treatment of central and peripheral nervous system associated disorders, wherein said medicament is administered according to a dosing regimen having a dosing periodicity ranging from about twice a day to about once every other day.
    Type: Grant
    Filed: April 17, 2015
    Date of Patent: August 29, 2017
    Assignee: BIAL—PORTELA & CA, S.A.
    Inventors: David Alexander Learmonth, Laszlo Erno Kiss, Pedro Nuno Leal Palma, Humberto dos Santos Ferreira, Patricio Manuel V. A. Soares da Silva
  • Patent number: 9718793
    Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C?O)—, —(C?S)—, —SO.sub.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: August 1, 2017
    Assignees: Vernalis (R&D) Ltd., Cancer Research Technology Limited, The Institute of Cancer Research
    Inventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
  • Patent number: 9695118
    Abstract: The present invention relates to benzamide derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 24, 2013
    Date of Patent: July 4, 2017
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Takeshi Murata, Satoshi Niizuma, Sousuke Hara, Hatsuo Kawada, Kihito Hada, Hideaki Shimada, Hiroshi Tanaka, Yoshito Nakanishi
  • Patent number: 9598367
    Abstract: The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
    Type: Grant
    Filed: January 15, 2016
    Date of Patent: March 21, 2017
    Assignee: Zenith Epigenetics Ltd.
    Inventors: Shuang Liu, Bryan Cordell Duffy, John Frederick Quinn, May Xiaowu Jiang, Ruifang Wang, Gregory Scott Martin, He Zhao, Bruce Francis Molino, Peter Ronald Young
  • Patent number: 9573955
    Abstract: Heterocyclic compounds and salts according to formula (I), which are pyrimidinone derivatives, described herein exhibit human neutrophil elastase inhibitory properties, and useful for treating diseases or conditions in which HNE is implicated.
    Type: Grant
    Filed: December 16, 2014
    Date of Patent: February 21, 2017
    Assignee: Chiese Farmaceutici S.p.A.
    Inventors: Lilian Alcaraz, Jonathan Mark Sutton, Elisabetta Armani, Carmelida Capaldi
  • Patent number: 9527822
    Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water.
    Type: Grant
    Filed: May 19, 2016
    Date of Patent: December 27, 2016
    Assignee: E.I. du Pont de Nemours and Company
    Inventor: Gary David Annis
  • Patent number: 9511060
    Abstract: One aspect of the present invention relates to substituted pyridines and pharmaceutically acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels.
    Type: Grant
    Filed: November 4, 2015
    Date of Patent: December 6, 2016
    Assignee: Trustees of Tufts College
    Inventors: William W. Bachovchin, Hung-sen Lai
  • Patent number: 9499524
    Abstract: The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests.
    Type: Grant
    Filed: March 11, 2011
    Date of Patent: November 22, 2016
    Assignee: Syngenta Participations AG
    Inventors: Pierre Joseph Marcel Jung, Peter Danko, Christopher Richard Ayles Godfrey, Peter Renold, Ottmar Franz Hueter
  • Patent number: 9475785
    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: February 27, 2015
    Date of Patent: October 25, 2016
    Assignee: 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: 9453006
    Abstract: Means for improving the solubility of luliconazole is provided. A crystal of luliconazole represented by the following formula is provided, wherein the crystal has such a crystal habit that (011) plane is a specific crystal growth plane. The crystal is characterized in that I(011) with respect to a sum total of I(001), I(100), I(10-1), I(011), I(110), I(11-1), I(10-2), I(11-2), I(020), I(021), I(20-2), I(121), I(013), I(11-3), and I(221) is not less than 25%, provided that integrated intensities of diffraction peaks, which correspond to the (001), (100), (10-1), (011), (110), (11-1), (10-2), (11-2), (020), (021), (20-2), (121), (013), (11-3), and (221) planes, are designated as I(001), I(100), I(10-1), I(011), I(110), I(11-1), I(10-2), I(11-2), I(020), I(021), I(20-2), I(121), I(013), I(11-3), and I(221) respectively in relation to the diffraction peaks detected in a range of 2?=5 to 35° in a powder X-ray diffractometry using CuK? radiation.
    Type: Grant
    Filed: June 24, 2013
    Date of Patent: September 27, 2016
    Assignees: POLA PHARMA INC., NIHON NOHYAKU CO., LTD.
    Inventors: Takaaki Masuda, Yoshiyuki Miyata, Hideo Kaneda
  • Patent number: 9440953
    Abstract: Disclosed are amino triazole compounds substituted by a carboxylate functional group or an bioisosteric polar functional group. Compounds having the carboxylate moiety or carboxylate bioisostere inhibit acidic mammalian chitinase. Also provided are methods of using the compounds to treat asthma reactions caused by allergens.
    Type: Grant
    Filed: December 4, 2015
    Date of Patent: September 13, 2016
    Assignee: OncoArendi Therapeutics Sp. z o.o.
    Inventors: Adam Golebiowski, Robert Koralewski, Wojciech J. Czestkowski, Krzysztof Matyszewski, Sylwia Olejniczak, Jacek Olczak, Paul Beckett
  • Patent number: 9426995
    Abstract: Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.
    Type: Grant
    Filed: February 8, 2013
    Date of Patent: August 30, 2016
    Assignee: Monsanto Technology LLC
    Inventors: Urszula Slomczynska, Matt W. Dimmic, Al Wideman, William P. Haakenson, Jr.
  • Patent number: 9403807
    Abstract: The present invention is directed to compounds of the Formula I as well as pharmaceutically acceptable salts thereof, that are useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula I.
    Type: Grant
    Filed: December 2, 2014
    Date of Patent: August 2, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alejandro Crespo, Ping Lan, Rudrajit Mal, Anthony Ogawa, Hong Shen, Peter J. Sinclair, Zhongxiang Sun, Ellen K. Vande Bunte, Zhicai Wu, Kun Liu, Robert J. DeVita, Dong-Ming Shen, Min Shu, John Qiang Tan, Changhe Qi, Yuguang Wang, Richard Beresis
  • Patent number: 9365540
    Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.
    Type: Grant
    Filed: January 11, 2013
    Date of Patent: June 14, 2016
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Shizuo Kasai, Hideyuki Igawa, Masashi Takahashi, Tsuyoshi Maekawa, Keiko Kakegawa, Asato Kina, Jumpei Aida, Uttam Khamrai, Mrinalkanti Kundu
  • Patent number: 9296711
    Abstract: The invention is concerned with a compound of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compound of formula (I) as well as pharmaceutical compositions containing such compounds. The compound of formula (I) are SCD1 inhibitors and may be useful in treating cancer.
    Type: Grant
    Filed: December 2, 2013
    Date of Patent: March 29, 2016
    Assignee: HOFFMAN-LA ROCHE INC.
    Inventors: Shawn David Erickson, Paul Gillespie, Eric Mertz
  • Patent number: 9282742
    Abstract: A compound of formula (I): where A1, A2, A3, A4, A5, A6, G1, L, R1, R2, R3, R4, Y1, Y2 and Y3 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising compounds of formula (I) and to methods of using compounds of formula (I) to combat and control insect, acarine, mollusc and nematode pests.
    Type: Grant
    Filed: February 24, 2014
    Date of Patent: March 15, 2016
    Assignee: Syngenta Participations AG
    Inventors: Peter Renold, Jerome Yves Cassayre, Myriem El Qacemi, Thomas Pitterna
  • Patent number: 9278935
    Abstract: A method for preparing a fluorinated organic compound (II) from an organic compound (I) comprising at least one nucleofugal group Nu, and also a preparation of different specific organic compounds, in particular a fluoro-methylpyrazole compound. The method comprises: a reaction, in the presence of water, of the organic compound (I) and at least one salt providing at least one fluoride anion; and a replacement of at least one nucleofugal group Nu of the compound (I) with a fluorine atom, in order to obtain the fluorinated organic compound (II).
    Type: Grant
    Filed: May 29, 2012
    Date of Patent: March 8, 2016
    Assignee: RHODIA OPERATIONS
    Inventors: Olivier Buisine, Michael Dejoux
  • Patent number: 9271978
    Abstract: The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
    Type: Grant
    Filed: December 19, 2013
    Date of Patent: March 1, 2016
    Assignee: Zenith Epigenetics Corp.
    Inventors: Shuang Liu, Bryan Cordell Duffy, John Frederick Quinn, May Xiaowu Jiang, Ruifang Wang, Gregory Scott Martin, He Zhao, Bruce Francis Molino, Peter Ronald Young
  • Patent number: 9259470
    Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Grant
    Filed: February 14, 2014
    Date of Patent: February 16, 2016
    Assignees: Array BioPharma Inc., Genentech, Inc.
    Inventors: James F. Blake, Mark Joseph Chicarelli, Rustam Ferdinand Garrey, John Gaudino, Jonas Grina, David A. Moreno, Peter J. Mohr, Li Ren, Jacob Schwarz, Huifen Chen, Kirk Robarge, Aihe Zhou
  • Patent number: 9250552
    Abstract: To provide a polymeric compound having superior charge-providing properties, the polymeric compound contains at least one unit represented by the following general formula (5). In the general formula (5), R1 represents a hydrogen atom or an alkyl group; R2 to R4 each represent a hydrogen atom, an alkyl group, an alkoxy group, a hydroxyl group or a halogen atom, or R3 and R4 may combine each other to form a ring; and A represents a divalent linking group.
    Type: Grant
    Filed: March 27, 2012
    Date of Patent: February 2, 2016
    Assignee: CANON KABUSHIKI KAISHA
    Inventors: Kei Inoue, Yasuaki Murai, Ryuji Murayama, Kazuyuki Sato, Soichiro Kawakami, Masashi Hirose
  • Patent number: 9216169
    Abstract: Provided is a pharmaceutical composition comprising candesartan or ester thereof and chlorthalidone, and use thereof, wherein the weight ratio of candesartan or ester thereof to chlorthalidone is 5.3:1 to 1:6.25. The pharmaceutical composition has a synergistic antihypertensive effect, and can enhance the antihypertensive effect and extend duration of antihypertension.
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: December 22, 2015
    Assignee: TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCH
    Inventors: Lida Tang, Zhuanyou Zhao, Weiting Wang, Wengong Xi, Chunhua Hao, Xiangwei Xu, Bing Yu
  • Patent number: 9206158
    Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Grant
    Filed: June 10, 2015
    Date of Patent: December 8, 2015
    Assignee: Karyopharm Therapeutics Inc.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
  • Patent number: 9205077
    Abstract: The present application relates to novel 2-alkoxy-substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: June 13, 2014
    Date of Patent: December 8, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Walter Hübsch, Daniel Meibom, Alexandros Vakalopoulos, Barbara Albrecht-Küpper, Peter Nell, Katja Zimmermann, Frank Süβmeier, Joerg Keldenich
  • Patent number: 9186349
    Abstract: The invention relates generally to optical agents, including phototherapeutic agents, for biomedical applications, including phototherapy. The invention includes optical agents, and related therapeutic methods, comprising alicyclic diaza compounds, including 1,2 diaza heterocyclic compounds, having a photolabile N—N bond directly or indirectly linked to at least one carbocyclic aromatic and/or heterocyclic aromatic group. In some embodiments, for example, the invention provides alicyclic diaza compounds for phototherapeutic methods having a photolabile N—N bond that undergoes photoactivated cleavage to produce reactive species, such as radicals, ions, etc., that achieve a desired therapeutic effect, such as selective and/or localized tissue damage and/or cell death.
    Type: Grant
    Filed: May 12, 2010
    Date of Patent: November 17, 2015
    Assignee: Mallinckrodt LLC
    Inventor: Raghavan Rajagopalan
  • Patent number: 9133179
    Abstract: The invention relates to pyridine derivatives of Formula (I) wherein A, R1, R2, R3, and R4 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
    Type: Grant
    Filed: January 18, 2012
    Date of Patent: September 15, 2015
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Martin Bolli, Cyrille Lescop, Boris Mathys, Keith Morrison, Claus Mueller, Oliver Nayler, Beat Steiner
  • Patent number: 9045467
    Abstract: The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: June 2, 2015
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Harry Chobanian, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo
  • Publication number: 20150148373
    Abstract: The invention provides heterocyclic guanidine compounds that inhibit F1F0-ATPase, and methods of using heterocyclic guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 28, 2015
    Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood
  • Publication number: 20150148346
    Abstract: Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.
    Type: Application
    Filed: January 28, 2015
    Publication date: May 28, 2015
    Applicant: PTC Therapeutics Inc.
    Inventors: Gary Mitchell Karp, Seongwoo Hwang, Guangming Chen, Neil Gregory Almstead, Young-Choon Moon
  • Patent number: 9040530
    Abstract: Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: May 26, 2015
    Assignee: PORTOLA PHARMACEUTICALS, INC.
    Inventors: Zhaozhong J. Jia, Brian Kane, Jack Rose, Shawn M. Bauer, Yonghong Song, Qing Xu, Anjali Pandey
  • Patent number: 9040566
    Abstract: The present invention relates to the use of selective adenosine A1 agonists, in particular the dicyanopyridines of formula (I), for the treatment and/or prophylaxis of glaucoma and ocular hypertension as well as the their use for the production of a medicament for the treatment and/or prophylaxis of glaucoma and ocular hypertension.
    Type: Grant
    Filed: August 29, 2011
    Date of Patent: May 26, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Jürgen Klar, Georges Von Degenfeld, Hans-Georg Lerchen, Barbara Albrecht-Küpper, Andreas Knorr, Peter Sandner, Daniel Meibom
  • Patent number: 9040558
    Abstract: The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: May 26, 2015
    Assignee: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dager, Shanavas Alikunju
  • Publication number: 20150141433
    Abstract: Compounds that selectively negatively modulate NMDA receptors containing an NR2A subunit, pharmaceutical compositions comprising the compounds, and methods of treating a disease using the compounds are disclosed.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 21, 2015
    Inventors: David R. Anderson, Robert A. Volkmann
  • Patent number: 9035064
    Abstract: A description is given of N-(1,2,5-oxadiazol-3-yl)pyridinecarboxamides of the general formula (I) as herbicides. R in this formula (I) stands for radicals such as hydrogen, organic radicals, and other radicals such as halogen. W stands for a substituted pyridyl radical.
    Type: Grant
    Filed: March 12, 2012
    Date of Patent: May 19, 2015
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Arnim Köhn, Andreas Van Almsick, Ralf Braun, Monika H. Schmitt, Jörg Tiebes, Ines Heinemann, Isolde Häeuser-Hanh, Elmar Gatzweiler, Christopher Hugh Rosinger
  • Publication number: 20150133495
    Abstract: Disclosed herein is a compound of Formula I or a pharmaceutically acceptable salt thereof, in which A, G, R1 and R2 are as defined herein. The compounds and pharmaceutical compositions of the compounds are suitable for the treatment of HCV infection in mammals and are also useful to modulate or inhibit NS3/4 dimerization.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 14, 2015
    Inventor: Daniel Lamarre
  • Patent number: 9029377
    Abstract: Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: May 12, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anthony Ogawa, Feroze Ujjainwalla, Lin Chu, Bing Li, Lan Wei, Jinyou Xu, Hyun Ok, Aaron Lackner, Ihor Kopka
  • Patent number: 9029400
    Abstract: The present invention relates to 5-oxoisoxazole derivatives of the formula I, the pharmaceutically usable salts thereof and the use thereof as medicinal substances.
    Type: Grant
    Filed: October 5, 2009
    Date of Patent: May 12, 2015
    Assignee: Sanofi
    Inventors: Stefan Petry, Manfred Seidel, Gerhard Zoller, Gunter Müller, Karl-Heinz Baringhaus, Hubert Heuer
  • Publication number: 20150126499
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: January 7, 2015
    Publication date: May 7, 2015
    Inventors: Joseph Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
  • Patent number: 9023872
    Abstract: The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: May 5, 2015
    Assignee: Ixchelsis Limited
    Inventors: Alan Daniel Brown, Andrew Antony Calabrese, David Ellis
  • Patent number: 9023836
    Abstract: The present invention relates to the use of compounds of formula wherein the variables are as defined in the description, in the free form or in salt form, for controlling sea lice on fish.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: May 5, 2015
    Assignee: Novartis Tiergesundheit AG
    Inventors: Jean-Luc Perret, David Blaser, Steve Nanchen