The Additional Hetero Ring Consists Of One Nitrogen And Four Carbons (e.g., Nicotine, Etc.) Patents (Class 514/343)
  • Patent number: 11427566
    Abstract: A compound of formula (I): wherein A and A? independently represent a phenylene group or a pyridylene group; R2 is a hydrogen atom or a (C1-C4)alkyl group; R3 is a 2-pyridyl group, 3-pyridyl group, a 4-pyridyl group, a 2-pyrimidinyl group, a 4-pyrimidinyl group or a 5-pyrimidinyl group; R4 is a carbonyl group or a sulfonyl group; and R5 is a —NH—(CH2)a—NR6R7 group or a 4-methylpiperazinyl group, with a being an integer from 1 to 4, R6 and R7 representing independently a (C1-C4)alkyl group, or R6 and R7 together with the nitrogen atom to which they are linked forming a heterocycle group which is chosen among a 4-methylpiperazinyl group, a morpholino group, a pyrrolidinyl group and a piperidino group; or any one of its pharmaceutically acceptable salt.
    Type: Grant
    Filed: April 15, 2020
    Date of Patent: August 30, 2022
    Assignees: ABIVAX, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT CURIE, UNIVERSITE DE MONTPELLIER
    Inventors: Pierre Roux, Florence Mahuteau, Romain Najman, Gilles Gadea, Jamal Tazi, Didier Scherrer, Carsten Brock, Nathalie Cahuzac
  • Patent number: 11390600
    Abstract: The present invention provides crystalline forms of a compound of formula (I): Also provided are pharmaceutical compositions that include the provided crystalline forms and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer.
    Type: Grant
    Filed: July 7, 2020
    Date of Patent: July 19, 2022
    Assignees: Biomed Valley Discoveries, Inc., Vertex Pharmaceuticals Incorporated
    Inventors: Gary DeCrescenzo, Dean Welsch, Petinka I. Vlahova, Stephan X. M. Boerrigter, Alexander Aronov, Ali Keshavarz-Shokri, Alexander N. Scangas, Kathy Stavropoulos, Benjamin Littler, Irina Nikolaevna Kadiyala, Rossitza Gueorguieva Alargova
  • Patent number: 11246859
    Abstract: The present invention provides, inter alia, methods, pharmaceutical compositions, and kits for treating or ameliorating the effects of a cancer in a subject, which cancer is refractory or resistant to non-ERK MAPK pathway inhibitor therapy. Also provided are methods for identifying a subject having cancer who would benefit from therapy with an ERK inhibitor and methods for inhibiting phosphorylation of RSK in a cancer cell that is refractory or resistant to a non-ERK MAPK pathway inhibitor.
    Type: Grant
    Filed: May 22, 2017
    Date of Patent: February 15, 2022
    Assignee: BIOMED VALLEY DISCOVERIES, INC.
    Inventors: Saurabh Saha, Dean Welsch, Gary Decrescenzo, Jeffrey Roix
  • Patent number: 11219627
    Abstract: Analogs of (4aS,6R,8aS)-5,6,9,10,11,12-hexahydro-3-methoxy-11-methyl-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-6-ol of the formula: wherein R1 carbamate, carbonate or carboxlate group; R2 is alkoxy group of from one to six carbon atoms, a hydroxy group, hydrogen, an alkanoyloxy group or 2 to 10 carbon atoms, a benzoyloxy or substituted benzoyloxy group, a carbonate group of 1 to 10 carbon atoms or a carbamate group such as a mono alkyl or dialkyl or an aryl carbamate wherein the alkyl groups or aryl groups contain from 1 to 10 carbons; and R3 is hydrogen, alkyl of 1 to 10 carbon atoms, benzyl, cyclopropylmethyl group or a substituted or unsubstituted benzoyloxy group are of use in treating persons meeting criteria for having a risk of developing Alzheimer's type dementia, before symptoms of dementia are observed by reducing the decline of A? amyloid CSF.
    Type: Grant
    Filed: May 18, 2015
    Date of Patent: January 11, 2022
    Assignee: Synaptec Development LLC
    Inventor: Bonnie M. Davis
  • Patent number: 11154547
    Abstract: Methods of use, formulations, and devices for delivering therapeutic drugs locally to the region of the spleen are described herein. A method for treating sepsis and other inflammatory disease conditions can include inserting a drug delivery system inside the body, advancing the device to the spleen through the splenic artery, splenic vein or other blood vessel adjacent to the splenic nerves, or within a ligament associated with the spleen, such as the splenorenal or gastrosplenic ligaments.
    Type: Grant
    Filed: June 29, 2017
    Date of Patent: October 26, 2021
    Assignee: Tulavi Therapeutics, Inc.
    Inventors: Corinne Bright, Kondapavulur T. Venkateswara-Rao, Emily Stein
  • Patent number: 11013743
    Abstract: The present invention provides, inter alia, methods, kits, and pharmaceutical compositions for treating or ameliorating the effects of a cancer in a subject in need thereof. The method comprises administering to the subject an effective amount of (i) a first anti-cancer agent, which is BVD-523 or a pharmaceutically acceptable salt thereof and (ii) a second anti-cancer agent, which is a CDK inhibitor or a pharmaceutically acceptable salt thereof, to treat or ameliorate the effects of the cancer. Additional methods for effecting cancer cell death are also provided.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: May 25, 2021
    Assignee: BioMed Valley Discoveries, Inc.
    Inventors: Saurabh Saha, Dean Welsch, Gary DeCrescenzo, Jeffrey James Roix
  • Patent number: 11007183
    Abstract: The present invention provides, inter alia, methods, kits, and compositions for treating or ameliorating the effects of a cancer in a subject in need thereof. This method includes administering to the subject an effective amount of (i) a first anti-cancer agent, which is BVD-523 or a pharmaceutically acceptable salt thereof and (ii) a second anti-cancer agent, which is an inhibitor of the PI3K/Akt pathway or a pharmaceutically acceptable salt thereof. Also provided are methods of treating or ameliorating the effects of a subject with cancer in which the subject has a somatic KRAS and a somatic PIK3CA mutation or in which the cancer is refractory to a therapy selected from RAF inhibitor therapy, MEK inhibitor therapy, and RAF and MEK inhibitor therapy.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: May 18, 2021
    Assignee: BIOMED VALLEY DISCOVERIES, INC.
    Inventors: Saurabh Saha, Dean Welsch, Gary DeCrescenzo, Jeffrey James Roix
  • Patent number: 11007184
    Abstract: The present invention provides, inter alia, methods, kits, and pharmaceutical compositions for treating or ameliorating the effects of a cancer in a subject in need thereof. The method includes administering to the subject an effective amount of (i) a first anti-cancer agent, which is BVD 523 or a pharmaceutically acceptable salt thereof and (ii) a second anti-cancer agent, which is a type 2 MEK inhibitor, or other MEK inhibitors, or pharmaceutically acceptable salts thereof, to treat or ameliorate the effects of the cancer. Additional methods for effecting cancer cell death are also provided.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: May 18, 2021
    Assignee: BIOMED VALLEY DISCOVERIES, INC.
    Inventors: Saurabh Saha, Dean Welsch, Gary DeCrescenzo, Jeffrey James Roix
  • Patent number: 10912850
    Abstract: Radiofluorinated FNDP for PET imaging of soluble epoxide hydrolase (sEH) and method of using the same are disclosed.
    Type: Grant
    Filed: May 4, 2017
    Date of Patent: February 9, 2021
    Assignees: The Johns Hopkins University, Oregon Health & Science University
    Inventors: Andrew Horti, Martin G. Pomper, Nabil J. Alkayed
  • Patent number: 10772872
    Abstract: Novel, antimitotic heteroaryl amides and pharmaceutically acceptable salts of Formula I where Ar, R5, R6, R8, R9, R11, X1, and X2 are as defined herein, as compounds for treatment and prevention of cancer and proliferative diseases and disorders.
    Type: Grant
    Filed: June 29, 2018
    Date of Patent: September 15, 2020
    Assignee: Frost Biologic, Inc.
    Inventor: Adam Siddiqui-Jain
  • Patent number: 10738027
    Abstract: The present invention provides crystalline forms of a compound of formula (I): Also provided are pharmaceutical compositions that include the provided crystalline forms and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: August 11, 2020
    Assignees: Biomed Valley Discoveries, Inc., Vertex Pharmaceuticals Incorporated
    Inventors: Gary DeCrescenzo, Dean Welsch, Petinka I. Vlahova, Stephan X. M. Boerrigter, Alexander Aronov, Ali Keshavarz-Shokri, Alexander N. Scangas, Kathy Stavropoulos, Benjamin Littler, Irina Nikolaevna Kadiyala, Rossitza Gueorguieva Alargova
  • Patent number: 10722506
    Abstract: In one aspect, a method of treating a disorder associated with chronic inflammation includes administering to an individual in need thereof a therapeutically effective amount of isomyosmine or a pharmaceutically acceptable salt thereof. In some aspects, the disorder is a cancer, an autoimmune disorder, hypertension, or autism. In other aspects, isomyosmine is administered to treat viral infections or disorders associated with elevated levels of hydrogen peroxide and/or other Reactive Oxygen Species (ROS).
    Type: Grant
    Filed: December 3, 2019
    Date of Patent: July 28, 2020
    Assignee: MyMD Pharmaceuticals, Inc.
    Inventor: Jonnie R. Williams
  • Patent number: 10668055
    Abstract: The present invention provides, inter alia, methods of treating or ameliorating the effects of a cancer in a subject. The methods include administering to the subject an effective amount of (i) a first anti-cancer agent, which is BVD-523 or a pharmaceutically acceptable salt thereof and (ii) a second anti-cancer agent, which is a type 1 RAF inhibitor (such as dabrafenib) or another RAF inhibitor (such as regorafenib) or a pharmaceutically acceptable salt thereof, to treat or ameliorate the effects of the cancer. Also provided are pharmaceutical compositions and kits for treating or ameliorating the effects of a cancer in a subject.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: June 2, 2020
    Assignee: BIOMED VALLEY DISCOVERIES, INC.
    Inventors: Saurabh Saha, Dean Welsch, Gary DeCrescenzo, Jeffrey James Roix
  • Patent number: 10517856
    Abstract: In one aspect, a method of altering programmed cell death includes administering to an individual in need thereof a therapeutically effective amount of isomyosmine or a pharmaceutically acceptable salt thereof. In other aspects, isomyosmine is administered to treat a wound, hemochromatosis, traumatic brain injury, or disorders associated with chronic oxidative stress. In other aspects, isomyosmine is administered to increase blood oxygen saturation levels.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: December 31, 2019
    Assignee: MyMD Pharmaceuticals, Inc.
    Inventor: Jonnie R. Williams
  • Patent number: 10493026
    Abstract: In one aspect the present invention features a process for making a tablet comprising the step of applying radiofrequency energy to a powder blend comprising lossy coated particles and at least one pharmaceutically active agent to sinter said powder blend into a tablet, said lossy coated particles comprising a substrate having a Q value of greater than 100 that is at least partially coated with a lossy coating comprising Hydrogenated Starch Hydrolysate.
    Type: Grant
    Filed: March 20, 2017
    Date of Patent: December 3, 2019
    Assignee: Johnson & Johnson Consumer Inc.
    Inventors: Gregory Koll, Gerard McNally, Christopher E. Szymczak
  • Patent number: 10381440
    Abstract: Aspects described herein relate to food and beverage compositions infused with lipophilic active agents and methods of use for the treatment of a variety of disorders. More particularly, aspects described herein relate to food and beverage compositions infused with lipophilic active agents such as cannabinoids, nicotine, nonsteroidal anti-inflammatories (NSAIDs), and vitamins, that provide enhanced bioavailability of the lipophilic active agents in a subject, and that mask unpleasant tastes of lipophilic active agents.
    Type: Grant
    Filed: October 1, 2018
    Date of Patent: August 13, 2019
    Inventors: Michelle Reillo, Marian E. Washington
  • Patent number: 10374036
    Abstract: Aspects described herein relate to food and beverage compositions infused with lipophilic active agents and methods of use for the treatment of a variety of disorders. More particularly, aspects described herein relate to food and beverage compositions infused with lipophilic active agents such as cannabinoids, nicotine, nonsteroidal anti-inflammatories (NSAIDs), and vitamins, that provide enhanced bioavailability of the lipophilic active agents in a subject, and that mask unpleasant tastes of lipophilic active agents.
    Type: Grant
    Filed: October 1, 2018
    Date of Patent: August 6, 2019
    Inventors: Michelle Reillo, Marian E. Washington
  • Patent number: 10238641
    Abstract: The subject invention concerns materials and methods for treating and/or preventing diseases associated with accumulation of A? peptide in neural tissue. The subject invention also concerns materials and methods for treating and/or preventing stress disorders, such as post-traumatic stress disorder (PTSD). In one embodiment, a method of the invention comprises administering a therapeutically effective amount of cotinine, or a pharmaceutically acceptable salt thereof, to a person or animal in need of treatment. The methods of the invention can be used to prevent and/or treat Alzheimer's disease, Parkinson's disease, and/or Down's syndrome. The subject invention also concerns compositions that comprise cotinine, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent or adjuvant.
    Type: Grant
    Filed: October 4, 2017
    Date of Patent: March 26, 2019
    Assignees: University of South Florida, The United States of America as represented by the Department of Veteran's Affairs
    Inventor: Valentina Echeverria Moran
  • Patent number: 10183927
    Abstract: The present invention provides crystalline forms of a compound of formula (I): Also provided are pharmaceutical compositions that include the provided crystalline forms and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer.
    Type: Grant
    Filed: May 17, 2017
    Date of Patent: January 22, 2019
    Assignees: Biomed Valley Discoveries, Inc., Vertex Pharmaceuticals Incorporated
    Inventors: Gary DeCrescenzo, Dean Welsch, Petinka I. Vlahova, Stephan X. M. Boerrigter, Alexander Aronov, Ali Keshavarz-Shokri, Alexander N. Scangas, Kathy Stavropoulos, Benjamin Littler, Irina Nikolaevna Kadiyala, Rossitza Gueorguieva Alargova
  • Patent number: 10182994
    Abstract: Disclosed are particles comprising a complex of nicotine and cerium oxide and a biodegradable coating comprising agglutinin. Also disclosed is a method of treating or preventing neurodegenerative or neurological disorders in a mammal in need thereof, comprising administering to the mammal a therapeutically effective amount of the particles.
    Type: Grant
    Filed: June 10, 2015
    Date of Patent: January 22, 2019
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventor: Syed Imam
  • Patent number: 10080747
    Abstract: The present invention relates to methods of treating and/or ameliorating the severity of inflammation and autoimmunity in the central nervous system (CNS). In one embodiment, the present invention provides a method of treating multiple sclerosis by administering a therapeutically effective dosage of nicotine, or a pharmaceutical equivalent, analog, derivative, or salt thereof.
    Type: Grant
    Filed: January 5, 2017
    Date of Patent: September 25, 2018
    Assignee: Dignity Health
    Inventors: Fu-Dong Shi, Ronald J. Lukas, Timothy Vollmer
  • Patent number: 9951041
    Abstract: The present invention provides a malonate salt of a compound of formula (I): which is a crystalline salt. Also provided are pharmaceutical compositions that include the provided malonate salt and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer.
    Type: Grant
    Filed: May 17, 2017
    Date of Patent: April 24, 2018
    Assignee: BIOMED VALLEY DISCOVERIES, INC.
    Inventors: Gary DeCrescenzo, Dean Welsch, Jon G. Selbo, Ekaterina V. Albert, Emily M. Rigsbee
  • Patent number: 9937168
    Abstract: A composition intended to be employed for therapeutic purposes incorporates nicotine and at least one other nicotinic compound. Representative forms of nicotine can be as a free base (e.g., as a mixture of nicotine and microcrystalline cellulose), as a form of nicotine salt (e.g., as nicotine bitartrate) or as nicotine polacrilex. The other nicotinic compound is a compound that can be considered to bind selectively to certain nicotinic receptor subtypes, and particularly those of the central nervous system. For example, the other nicotinic compound can be a compound that binds selectively to the nicotinic receptor subtypes ?7 or ?4?2. The composition is useful for treatment of central nervous system conditions, diseases and disorders, and as a nicotine replacement therapy.
    Type: Grant
    Filed: June 8, 2017
    Date of Patent: April 10, 2018
    Assignee: Niconovum USA, Inc.
    Inventor: August J. Borschke
  • Patent number: 9844513
    Abstract: The present application provides a method for treating or preventing Celiac disease. In one embodiment the method comprises administering to a patient in need thereof a composition comprising minicapsules, wherein the minicapsules comprise a steroid in a liquid, semi-solid or solid core, the minicapsules having release profiles to release the steroid in an active form at one or more sites along the gastrointestinal tract, the one or more sites comprising the proximal small intestine beginning at the duodenum and ending at the ileum. In a related embodiment the method comprises administering budesonide to a patient in need thereof in a pre-solubilized drug delivery format.
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: December 19, 2017
    Assignee: Sigmoid Pharma Limited
    Inventor: Ivan Coulter
  • Patent number: 9801865
    Abstract: The subject invention concerns materials and methods for treating and/or preventing diseases associated with accumulation of A? peptide in neural tissue. The subject invention also concerns materials and methods for treating and/or preventing stress disorders, such as post-traumatic stress disorder (PTSD). In one embodiment, a method of the invention comprises administering a therapeutically effective amount of cotinine, or a pharmaceutically acceptable salt thereof, to a person or animal in need of treatment. The methods of the invention can be used to prevent and/or treat Alzheimer's disease and Parkinson's disease. The subject invention also concerns compositions that comprise cotinine, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent or adjuvant.
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: October 31, 2017
    Assignees: The United States of America as represented by the Department of Veteran Affairs, University of South Florida
    Inventor: Valentina Echeverria Moran
  • Patent number: 9695148
    Abstract: This 2-pyridone compound represented by formula [1] or a tautomer of said compound, or a pharmaceutically acceptable salt of said compound or said tautomer, or a solvate of said compound or the like has a superior GK-activating effect and is useful as a pharmaceutical.
    Type: Grant
    Filed: November 12, 2013
    Date of Patent: July 4, 2017
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Shoichi Kuroda, Yudai Imai, Takanori Kawaguchi, Keiko Fusegi, Masahiro Bohno, Hajime Asanuma, Tomomichi Chonan, Nagaaki Sato, Souichi Monma, Shigetada Sasako, Marie Mizutani, Shin Itoh, Takumi Okada, Hirofumi Ota, Seishi Ishiyama
  • Patent number: 9682085
    Abstract: Disclosed are compounds that modulate the physiological action of the proprotein convertase subtilisin kexin type 9 (PCSK9), as well as therapeutic methods for use of such compounds to reduce LDL-cholesterol levels and/or for the treatment and/or prevention of cardiovascular disease (CVD), including treatment of hypercholesterolemia. Examples of compounds include thiadiazole, isoxazole, 1,2,4-triazole, thiazole, indole, pyrazole, and pyrrolinone derivatives.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: June 20, 2017
    Assignee: Shifa Biomedical Corporation
    Inventors: Sherin Salaheldin Abdel-Meguid, Nabil Elshourbagy, Harold Meyers, Shaker A. Mousa
  • Patent number: 9676746
    Abstract: The present invention provides crystalline forms of a compound of formula (I): Also provided are pharmaceutical compositions that include the provided crystalline forms and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer.
    Type: Grant
    Filed: January 29, 2016
    Date of Patent: June 13, 2017
    Assignees: BioMed Valley Discoveries, Inc., Vertex Pharmaceuticals Incorporated
    Inventors: Gary DeCrescenzo, Dean Welsch, Petinka I. Vlahova, Stephan X. M. Boerrigter, Alexander Aronov, Ali Keshavarz-Shokri, Alexander N. Scangas, Kathy Stavropoulos, Benjamin Littler, Irina Nikolaevna Kadiyala, Rossitza Gueorguieva Alargova
  • Patent number: 9670177
    Abstract: The present invention provides a malonate salt of a compound of formula (I): which is a crystalline salt. Also provided are pharmaceutical compositions that include the provided malonate salt and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer.
    Type: Grant
    Filed: January 29, 2016
    Date of Patent: June 6, 2017
    Assignees: BioMed Valley Discoveries, Inc., Albany Molecular Research, Inc.
    Inventors: Gary DeCrescenzo, Dean Welsch, Jon G. Selbo, Ekaterina V. Albert, Emily M. Rigsbee
  • Patent number: 9662315
    Abstract: Patients which are treated with stimulants (e.g., CNS stimulants, sympathomimetic amine, or anorectic/anorexigenic), such as patients being treated for attention deficit/hyperactivity disorder or obesity, often are at risk in developing high blood pressure. Similarly, patients which are treated with analgesics such as non-steroidal anti-inflammatory drugs (NSAIDs) over an extended period of time risk developing high blood pressure. These and other iatrogenic therapies (therapies which inadvertently cause an increase in, e.g., blood pressure) are addressed by providing the patient with one or more antihypertensive drugs, most preferably calcium channel blockers, during the treatment period. The CNS or NSAIDs can be provided separately or together with the antihypertensive drugs or as part of a combined composition. The adjunctive therapy can prevent or reduces cardiovascular disease and other complications of high blood pressure attendant with these iatrogenic therapies.
    Type: Grant
    Filed: November 10, 2015
    Date of Patent: May 30, 2017
    Assignee: Kitov Pharmaceuticals Ltd.
    Inventors: Peter C. Hoyle, Paul Waymack
  • Patent number: 9504680
    Abstract: Disclosed are compounds of the formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and m are as described herein, as modulators of the nicotinic acetylcholine receptors, particularly the ?7 subtype, their tautomeric forms, stereoisomers, and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, and combinations thereof with suitable other medicaments. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and/or treatment of disorders such as Alzheimer's disease, mild cognitive impairment, and senile dementia.
    Type: Grant
    Filed: June 16, 2014
    Date of Patent: November 29, 2016
    Assignee: Lupin Limited
    Inventors: Neelima Sinha, Navnath Popat Karche, Shridhar Keshav Adurkar, Dnyaneshwar Changdeo Bhanage, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 9492541
    Abstract: A pharmaceutical dosage form which comprises phenylepherine or a pharmaceutically acceptable salt thereof and a second drug. The dosage form provides a plasma concentration within the therapeutic range of the second drug over a period which is coextensive with at least about 70% of the period over which the dosage form provides a plasma concentration within the therapeutic range of phenylepherine. This abstract is neither intended to define the invention disclosed in this specification nor intended to limit the scope of the invention in any way.
    Type: Grant
    Filed: September 14, 2004
    Date of Patent: November 15, 2016
    Assignee: SOVEREIGN PHARMACEUTICALS, LLC
    Inventors: Viswanathan Srinivasan, Ralph Brown, David Brown, Juan Carlos Menendez, Venkatesh Balasubramanian, Somphet Peter Suphasawud
  • Patent number: 9487462
    Abstract: Compounds of general formula (I), salts or solvates thereof and pharmaceutical compositions containing same: wherein Z is N or CH or the Z(R1) part is replaced with a covalent bond, m and n is 0, 1, 2 or 3; HET is heteroaryl; X is CF3, halogen, CO-heterocyclyl, COOR3 or CONHR3; R1 is H, (CH2)o-aryl, (CH2)p-heteroaryl, (CH2)q-biphenyl; C(O)—R5; S(O)2—R6; R2 is H, aryl, heteroaryl, Y—(CH2)r-aryl, Y—(CH2)s-heteroaryl, where some of the above substituents may be substituted; Y is O or S; with the exclusion of the compound where HET is 1,3-thiazol, X is COOH, R1 is 4-fluorophenyl and R2 is benzyloxy. The invention also relates to the use of a compound of general formula (I), salts or solvates thereof for the use in the prevention or treatment of diseases where the activation of MMPs is involved in the pathomechanism. In this aspect the use of the above excluded compound is also inventive.
    Type: Grant
    Filed: December 19, 2011
    Date of Patent: November 8, 2016
    Assignees: PharmaHungary 2000 Kft., TargetEx Kft.
    Inventors: Péter Ferdinandy, Tamás Bálint Csont, Csaba Csonka, Krisztina Kedvesné Kupai, László Kovács, Attila Kis-Tamás, Ferenc Tamás Takács, Dénes Kónya, Gábor Medgyes, Sándor Cseh, István Hajdú, Zsolt Lörincz, György Dormán, Anikó Görbe
  • Patent number: 9475801
    Abstract: The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.
    Type: Grant
    Filed: July 8, 2015
    Date of Patent: October 25, 2016
    Assignee: ALLERGAN, INC.
    Inventors: Xialing Guo, Zhen Zhu
  • Patent number: 9464053
    Abstract: Novel small molecule compounds for reduction of A? 42 production and for treatment of Alzheimer's disease and other neurodegenerative disorders, methods of making them and pharmaceutical compositions containing them are described.
    Type: Grant
    Filed: August 26, 2014
    Date of Patent: October 11, 2016
    Assignee: KAREUS THERAPEUTICS, SA
    Inventors: Venkateswarlu Akella, Uday Saxena, Anji Reddy Kallam
  • Patent number: 9440948
    Abstract: Embodiments of the present disclosure provide for compounds such as those shown in FIG. 1.1 (compounds A, B, C, and D), 2?substituted nicotine compounds, azetidine compounds, ether linked nicotine compounds (FIG. 1.2, compounds E, F, G, and H), methods of synthesis of the compounds, methods of treatment of a condition using compounds A, B, C, D, 2?substituted nicotine compounds, azetidine compounds, or ether linked nicotine compounds, methods of selectively stimulating alpha7 nAChR and/or alpha4beta2 receptors, and the like.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: September 13, 2016
    Assignees: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC., THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
    Inventors: William Reade Kem, Ferenc Soti, Anne Rouchaud, Hong Xing, Jon Lindstrom, Kristin Marie Andrud
  • Patent number: 9328103
    Abstract: The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.
    Type: Grant
    Filed: October 15, 2013
    Date of Patent: May 3, 2016
    Assignee: Allergan, Inc.
    Inventors: Xialing Guo, Zhen Zhu
  • Patent number: 9268311
    Abstract: A method for allowing a human subject having a mouth to time a predetermined duration, the method comprising: initiating a first oral sensation in the mouth of the human subject to indicate a beginning of the predetermined duration; and initiating a second oral sensation in the mouth of the human subject to indicate an end of the predetermined duration, the second oral sensation differing from the first oral sensation. Initiations of the first and second oral sensations are separated in time by substantially the predetermined duration. Also, an oral timer for performing the method and a kit including a plurality of the oral timers.
    Type: Grant
    Filed: February 26, 2014
    Date of Patent: February 23, 2016
    Inventor: Pierre-Pascal Gauthier
  • Patent number: 9260388
    Abstract: Disclosed are compounds of formulae (I) and (II) and salts, hydrates, or solvates thereof, where R1, R2, R3, R5, and R6 are defined herein, compositions containing these compounds, methods of preparing these compounds, and methods of using these compounds in a variety of applications, such as a surfactant or additive in personal care products.
    Type: Grant
    Filed: December 13, 2012
    Date of Patent: February 16, 2016
    Assignee: Dow Global Technologies LLC
    Inventors: Daniel R. Henton, Cynthia L. Rand, Sze-Sze Ng
  • Publication number: 20150132408
    Abstract: The present invention provides sorafenib analogs for use in a method of treating a disease mediated by p21, said method comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I. The present invention also provides methods of inhibiting p21 in a cell comprising contacting the cell with an effective amount of a compound of formula I.
    Type: Application
    Filed: June 20, 2013
    Publication date: May 14, 2015
    Inventors: Robert H. Weiss, Bruce D. Hammock, Hiromi Inoue, Sung Hee Hwang
  • Publication number: 20150133430
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 14, 2015
    Inventors: Qing XU, Zhe LI
  • Patent number: 9029402
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: January 2, 2014
    Date of Patent: May 12, 2015
    Assignee: Nivalis Therapeutics, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Patent number: 9029401
    Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: May 12, 2015
    Assignee: The Regents of the University of California
    Inventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
  • Publication number: 20150126485
    Abstract: The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Publication number: 20150126561
    Abstract: A smokeless tobacco product or medicinal nicotine product includes nicotine and camphor dissolved in a non-flavored oily carrier. Preferably, the camphor is present in a concentration ranging from about 600 ppm to about 1300 ppm. Also disclosed are methods of making such products.
    Type: Application
    Filed: January 7, 2015
    Publication date: May 7, 2015
    Inventors: Gerd Kobal, Prasad Polur, Maria Gogova, Diana McKinney
  • Publication number: 20150126522
    Abstract: This invention relates to novel substituted benzamides according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
    Type: Application
    Filed: May 15, 2013
    Publication date: May 7, 2015
    Applicant: GlaxoSmithKline LLC
    Inventors: Joelle Lorraine Burgess, Celine Duquenne, Steven David Knight, William Henry Miller, Kenneth Allen Newlander, Sharad Kumar Verma
  • Publication number: 20150126490
    Abstract: The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.
    Type: Application
    Filed: October 29, 2014
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Jeffrey T. BAGDANOFF, Yu DING, Wooseok HAN, Zilin HUANG, Qun JIANG, Jeff Xianming JIN, Xiang KOU, Patrick LEE, Mika LINDVALL, Zhongcheng MIN, Yue PAN, Sabina PECCHI, Keith Bruce PFISTER, Daniel POON, Vivek RAUNIYAR, Xiaojing Michael WANG, Qiong ZHANG, Jianguang ZHOU, Shejin ZHU
  • Publication number: 20150119384
    Abstract: The present invention relates to ethynyl derivatives of formula I X, O, R1, R2, R3, R3?, R4, R4?, R5, R6, R6?, m, and n are as defined hereinor to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They can be used for the treatment of schizophrenia or cognitive disorders.
    Type: Application
    Filed: January 6, 2015
    Publication date: April 30, 2015
    Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • Publication number: 20150119378
    Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
    Type: Application
    Filed: October 24, 2014
    Publication date: April 30, 2015
    Inventors: Srinivasa Rao Akireddy, Scott R. Breining
  • Patent number: 9018206
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: April 28, 2015
    Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins