Tetrazoles (including Hydrogenated) Patents (Class 514/381)
-
Patent number: 11466003Abstract: Provided are a nitrogenous heterocyclic aromatic compound, a preparation method therefor, a pharmaceutical composition thereof, and an application thereof. The nitrogenous heterocyclic aromatic compound can be used for treating and/or preventing various diseases mediated by ALK5.Type: GrantFiled: July 6, 2017Date of Patent: October 11, 2022Assignee: SHANGHAI YINGLI PHARMACEUTICAL CO., LTDInventors: Zusheng Xu, Yangtong Lou, Li Chen
-
Patent number: 11202907Abstract: Systems and methods for implementation of a disposable miniaturized implant for treatment of Post-Operative Ileums (POI),a miniaturized implant for treating chronic GI dysmotility (e.g., dysphagia, gastroesophageal reflux disease (GERD), nausea, functional dyspepsia, blockage of transit, and gastroparesis, inflammatory bowel disease) and obesity, by providing electrical stimulation to the part of bowel going through surgery to expedite the healing process while recording the smooth muscle activities simultaneously, or providing stimulation on a treatment location of the GI tract or the branch of the vagus nerve. Systems and methods are also provided for non-invasive, transcutaneous stimulation of anatomy within the abdomen of the patient.Type: GrantFiled: June 11, 2019Date of Patent: December 21, 2021Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Yi-Kai Lo, Wentai Liu
-
Patent number: 11179354Abstract: In certain embodiments, this disclosure relates to methods of treating or preventing nephrogenic diabetes insipidus comprising administering an effective amount of a compound of Formula (I) or derivatives thereof, as described herein, to a subject in need thereof. In certain embodiments, the subject has been diagnosed with nephrogenic diabetes insipidus.Type: GrantFiled: January 31, 2018Date of Patent: November 23, 2021Assignee: NephroDI Therapeutics, Inc.Inventors: Jeff Sands, Janet Klein, Ish Khanna, Sivaram Pillarisetti
-
Patent number: 11135187Abstract: Compositions and methods for treating diabetic retinopathy or symptoms thereof are provided. The disclosed compositions and methods for treating diabetic retinopathy contravene the existing paradigm that Renin-Angiotensin System (RAS) blockade alone can treat, prevent, or reduce diabetic retinopathy. The disclosed compositions and methods include a combination or alternation of EET antagonists and ATI antagonists.Type: GrantFiled: August 21, 2018Date of Patent: October 5, 2021Assignees: National Institutes of Health (NIH), U.S. Dept. of Health Human Services, (DHHS), U.S. Government NIH Division of Extramural Inventions and Technology Resources (DEITR)Inventors: Mong Heng Wang, Mohamed Al-Shabrawey
-
Patent number: 11129819Abstract: Aspects of the present disclosure include compounds that find use for the treatment of a variety of autoimmune and inflammatory diseases and disorders. Embodiments of the present disclosure also relate to pharmaceutical compositions that include 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: GrantFiled: October 14, 2019Date of Patent: September 28, 2021Assignee: Rigel Pharmaceuticals, Inc.Inventors: Matthew Duncton, Somasekhar Bhamidipati, Jiaxin Yu, Ihab Darwish, Rajinder Singh
-
Patent number: 11046673Abstract: The present invention provides a compound having excellent control efficacies against plant diseases. The compound is represented by formula (I): wherein, R1 represents a C1-C3 alkyl group optionally having one or more halogens; n is 1 or 2; R2 and R3 represent independently of each other a hydrogen atom, etc.; R4 represents a hydrogen atom, etc.; and R5 represents a C1-C3 alkyl group optionally having one or more halogen atoms, etc.Type: GrantFiled: August 24, 2017Date of Patent: June 29, 2021Assignee: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yuki Akioka, Nao Maehata
-
Patent number: 11046683Abstract: Disclosed is a compound of formula (I): wherein all symbols are defined in the description. Also disclosed are pharmaceutical compositions comprising the compounds, methods of making the compounds, kits comprising the compounds, and methods of using the compounds, compositions and kits for treatment of disorders associated with TREK-1, TREK-2 or both TREK-1 and TREK-2 dysfunction in a mammal.Type: GrantFiled: December 14, 2017Date of Patent: June 29, 2021Assignees: ONO PHARMACEUTICAL CO., LTD., VANDERBILT UNIVERSITYInventors: Craig W Lindsley, Joshua M. Wieting, Kevin M. McGowan, Jerod S. Denton, Kentaro Yashiro, Haruto Kurata, Yoko Sekioka, Takahiro Mori, Yuzo Iwaki
-
Patent number: 10835516Abstract: Provided herein is a novel mitochondrial Angiotensin II type 1 and type 2 AT1R and AT2R receptor which plays a role in protection of mitochondria against oxidative damage. Evidence from animal studies indicates a role for this receptor in preservation of mitochondria and up-regulation of survival genes, anti-inflammatory action, and improvement of wound healing in the skin and soft tissues. Pharmaceutical compositions for treatment directed to preserving mitochondrial function, anti-inflammation, wound healing and decreasing the signs of aging, as well as medicaments and their use are also provided.Type: GrantFiled: January 15, 2015Date of Patent: November 17, 2020Assignee: THE JOHNS HOPKINS UNIVERSITYInventors: Peter M. Abadir, Jeremy D. Walston
-
Patent number: 10745363Abstract: Provided are crystal forms A, B, D, E, F, G and H of valsartan disodium salt and a preparation method therefor.Type: GrantFiled: September 2, 2016Date of Patent: August 18, 2020Assignee: NANJING NORATECH PHARMACEUTICALS CO., LTDInventors: Fei Liu, Gang Wu, Weiming Jiang, Cheng-Gang Lin, Xuan Cai, Ping Lin, Yuling Lu, Lixiang Liu
-
Patent number: 10100039Abstract: Disclosed are polymorph of allisartan isoproxil and a pharmaceutical composition thereof. The polymorph is non-electrostatic, highly flowable and highly stable, and can be used for treating hypertension and complications thereof.Type: GrantFiled: June 5, 2015Date of Patent: October 16, 2018Assignee: SHENZHEN SALUBRIS PHARMACEUTICALS CO., LTDInventors: Duanming Tan, Jun Ou
-
Patent number: 10053448Abstract: A tetrazolinone compound represented by formula (1): wherein R1 represents a hydrogen atom, a C1-C3 alkyl group optionally having one or more halogen atoms, a C1-C3 alkoxy group optionally having one or more halogen atoms, a halogen atom, a cyano group, or a C1-C3 alkylthio group optionally having one or more halogen atoms; and R2 represents a C1-C3 alkyl group optionally having one or more halogen atoms, a C1-C3 alkoxy group optionally having one or more halogen atoms, a hydrogen atom, a halogen atom, or a C3-C4 cycloalkyl group optionally having one or more halogen atoms, has excellent control activity against plant diseases.Type: GrantFiled: March 28, 2016Date of Patent: August 21, 2018Assignee: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Nao Maehata, Sadayuki Arimori
-
Patent number: 9955693Abstract: Phytopathogenic filamentous fungi other than oomycete microorganisms are controlled using at least one compound selected from among tetrazoyloxime derivatives represented by formula (I) and salts thereof. In formula (I), X represents a C1 to C6 alkyl group or the like, n represents an integer of 0 to 5, Y represents a C1 to C6 alkyl group, Z represents a hydrogen atom or an amino group or the like, Q represents a hydrogen atom or a C1 to C8 alkyl group or the like, R represents a halogeno group or a C1 to C6 alkoxy group, and m represents an integer of 0 to 3.Type: GrantFiled: February 24, 2014Date of Patent: May 1, 2018Assignee: Nippon Soda Co., Ltd.Inventors: Tomoyuki Saiga, Kazushige Kato, Shinya Watanabe, Akie Fukuyo
-
Patent number: 9918964Abstract: It has been discovered that inhibiting mitochondrial respiration in platelets reduces platelet activation or platelet aggregation. Certain heterocyclic compounds significantly reduced one or more platelet functions including clumping, sticking or platelet-stimulated clotting. Thus diseases or disorders mediated by inappropriately high levels of platelet activation or platelet aggregation can be treated by administering a therapeutically effective amount of a heterocyclic compound or nonheterocyclic mitochondrial inhibitor that significantly reduces one or more platelet functions including clumping, sticking or platelet-stimulated clotting, preferably in a reversible manner.Type: GrantFiled: April 25, 2011Date of Patent: March 20, 2018Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: James P. Collman, Paul Clifford Herrmann, David Alvin Tyvoll, Richard Decreau, Brian Stanley Bull, Christopher Jeffrey Barile
-
Patent number: 9856214Abstract: The invention provides EBNA1 inhibitors, and pharmaceutical compositions comprising the same, that are useful for the treatment of diseases caused by EBNA1 activity such as, but not limited to, cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and/or rheumatoid arthritis. The compounds and compositions of the invention are further useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. The compounds and compositions of the invention are further useful for the treatment of diseases caused by lytic EBV infection.Type: GrantFiled: November 14, 2014Date of Patent: January 2, 2018Assignee: THE WISTAR INSTITUTE OF ANATOMY AND BIOLOGYInventors: Troy E. Messick, Garry R. Smith, Allen B. Reitz, Paul M. Lieberman, Mark E. McDonnell, Yan Zhang, Venkata Velvadapu
-
Patent number: 9801866Abstract: Aspects of the present disclosure include compounds that find use for the treatment of a variety of autoimmune and inflammatory diseases and disorders. Embodiments of the present disclosure also relate to pharmaceutical compositions that include 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: GrantFiled: September 19, 2016Date of Patent: October 31, 2017Assignee: Rigl Pharmaceutical, Inc.Inventors: Matthew Duncton, Somasekhar Bhamidipati, Jiaxin Yu, Ihab Darwish, Rajinder Singh
-
Patent number: 9763953Abstract: The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g., galantamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as “pro-drugs”, in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. The compounds of this invention may be used as medicaments.Type: GrantFiled: April 11, 2013Date of Patent: September 19, 2017Assignee: NEURODYN LIFE SCIENCES INC.Inventor: Alfred Maelicke
-
Patent number: 9725423Abstract: The compound represented by formula (1): wherein R4 and R5 each represents a hydrogen atom, a halogen atom, or a C1-C3 alkyl group; R6 represents a C1-C4 alkyl group, a C3-C6 cycloalkyl group, or the like; R7, R8, and R9 each represents a hydrogen atom, a halogen atom, or the like; R10 represents a C1-C3 alkyl group, or the like; R13 represents a C1-C3 alkyl group, or the like; and Q represents a phenyl group, or the like; has an excellent control effect on pests.Type: GrantFiled: November 20, 2013Date of Patent: August 8, 2017Assignee: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Nao Hasegawa, Sadayuki Arimori, Yuichi Matsuzaki
-
Patent number: 9701175Abstract: A hybrid vehicle includes an exhaust turbine disposed in an exhaust path coupled to an electric machine and a compressor for an air-conditioning system. The vehicle includes a controller that controls the electric machine based on a difference between the power demand of the compressor and the power generated by the exhaust turbine. The electric machine may operate as a motor or a generator based on the difference. The vehicle may include a first clutch coupled to the electric machine and the compressor. The vehicle may include a second clutch coupled between the exhaust turbine and the electric machine. The controller may control the clutches based on the power demand and the power generated.Type: GrantFiled: April 14, 2015Date of Patent: July 11, 2017Assignee: Ford Global Technologies, LLCInventors: Kenneth James Miller, Thomas G. Leone
-
Patent number: 9573904Abstract: An aromatic compound represented by formula (1): wherein R1 and R2 each independently represents a halogen atom, a C1-C4 alkyl group, or a C1-C4 haloalkyl group; m and n each independently represents an integer of 0 to 4; R3 and R4 each represents a hydrogen atom; Y represents formula: —OC(?X)ZR5 or —SC(?X)ZR5; R5 represents a C1-C3 alkyl group optionally having one or more halogen atoms; Z represents a sulfur atom, NR8, or a direct bond; R8 represents a C1-C3 alkyl group or a hydrogen atom; Q represents a pyrazolyl group optionally having a substituent; and W and X each independently represents an oxygen atom or a sulfur atom, has excellent control activity against pests.Type: GrantFiled: December 10, 2014Date of Patent: February 21, 2017Assignee: Sumitomo Chemical Company, LimitedInventor: Takayuki Shioda
-
Patent number: 9499499Abstract: The invention relates to new salts of valsartan or crystalline, also partly crystalline and amorphous salts of valsartan, the respective production and usage, and pharmaceutical preparations containing such a salt.Type: GrantFiled: November 15, 2013Date of Patent: November 22, 2016Assignee: Novartis AGInventors: Erwin Marti, Hans Rudolf Oswald, Peter Buehlmayer, Wolfgang Marterer
-
Patent number: 9475781Abstract: Aspects of the present disclosure include compounds that find use for the treatment of a variety of autoimmune and inflammatory diseases and disorders. Embodiments of the present disclosure also relate to pharmaceutical compositions that include 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: GrantFiled: July 31, 2015Date of Patent: October 25, 2016Assignee: Rigel Pharmaceuticals, Inc.Inventors: Matthew Duncton, Somasekhar Bhamidipati, Jiaxin Yu, Ihab Darwish, Rajinder Singh
-
Patent number: 9447069Abstract: The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR.Type: GrantFiled: April 30, 2013Date of Patent: September 20, 2016Assignee: INNOV17 LLCInventors: Anderson Gaweco, Jefferson W. Tilley, John Walker, Samantha Palmer, James Blinn
-
Patent number: 9440952Abstract: The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.Type: GrantFiled: February 27, 2014Date of Patent: September 13, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Michael Miller, Kallol Basu, Duane DeMong, Jack Scott, Hong Liu, Xing Dai, Joel M. Harris, Bernard Neustadt, Andrew Stamford, Marc Poirier, John A. McCauley, Thomas Greshock, Heather Stevenson, John Sanders, Jonathan Kern
-
Patent number: 9382588Abstract: The present invention includes methods for identifying patients who will be resistant to endocrine therapy during breast cancer treatment and determining patient outcome. The methods are based on identifying increased expression of PBX1, or the cistrome signature associated therewith, in breast tissue samples.Type: GrantFiled: February 15, 2012Date of Patent: July 5, 2016Assignee: Trustees of Dartmouth CollegeInventors: Mathieu Lupien, Luca Magnani
-
Patent number: 9381172Abstract: Small molecule choline kinase inhibitors, pharmaceutical compositions thereof, and screening methods for identifying and evaluating choline kinase inhibitors are provided. Safe and effective methods for treating subjects suffering from a disorder or disease characterized by neoplastic cell proliferation employing the choline kinase inhibitors are also provided.Type: GrantFiled: May 12, 2012Date of Patent: July 5, 2016Assignee: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.Inventors: Brian Clem, Sucheta Telang, John Trent, Jason Chesney, Pooran Chand, Gilles Tapolsky
-
Patent number: 9371528Abstract: The invention relates generally to methods and compositions for treating sinusitis, asthma, or polyps. The invention also relates to methods and compositions for treating nasal polyps.Type: GrantFiled: February 12, 2014Date of Patent: June 21, 2016Assignee: Massachusetts Eye and Ear InfirmaryInventors: Konstantina M. Stankovic, Ralph Metson
-
Patent number: 9333233Abstract: The present invention provides, among other things, method of treating stroke including a step of administering an angiotensin (1-7) peptide to a subject suffering from a stroke, approximately 24 hours after the stroke. In some embodiments, treatment begins more than 24 hours after the stroke. In some embodiments, administration of an angiotensin (1-7) peptide results in a reduction in the intensity, severity, duration, and/or frequency of at least one symptom or feature of the one or more complications of stroke.Type: GrantFiled: November 20, 2014Date of Patent: May 10, 2016Assignee: TARIX PHARMACEUTICALS LTD.Inventor: Richard Franklin
-
Patent number: 9314450Abstract: The invention relates to pharmaceutical compositions comprising: (a) at least one angiotensin receptor blocker or a pharmaceutically acceptable salt thereof, and (b) at least one chemokine receptor pathway inhibitor or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising: (a) at least one angiotensin receptor blocker or a pharmaceutically acceptable salt thereof; and (b) at least one chemokine receptor pathway inhibitor or a pharmaceutically acceptable salt thereof which inhibits a component of the chemokine receptor pathway other than the chemokine receptor. Oral sustained release pharmaceutical compositions comprising the pharmaceutical composition, as well as injectable sustained release pharmaceutical compositions comprising the pharmaceutical composition are described. The invention further relates to tablets, capsules, injectable suspensions, and compositions for pulmonary or nasal delivery comprising the pharmaceutical composition.Type: GrantFiled: January 11, 2012Date of Patent: April 19, 2016Assignee: DIMERIX BIOSCIENCE PTY LTD.Inventors: Kevin D. G. Pfleger, Elizabeth McCall, James Williams
-
Patent number: 9295255Abstract: The present invention relates to the use of new and known dithiine derivatives for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to new dithiine derivatives, to processes for preparing them, to their use, and to crop protection compositions comprising these new dithiine derivatives.Type: GrantFiled: March 11, 2013Date of Patent: March 29, 2016Assignee: Bayer Intellectual Property GmbHInventors: Thomas Seitz, Jurgen Benting, Ulrike Wachendorff-Neumann
-
Patent number: 9243001Abstract: The present invention relates to azole compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: GrantFiled: March 14, 2014Date of Patent: January 26, 2016Assignee: Epizyme, Inc.Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
-
Patent number: 9179678Abstract: The present invention relates to compounds of Formula (I), or an agronomically acceptable salt of said compounds wherein A1, A2, A3, A4, A5, X, R1, R2 and R6 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), and to their use for controlling weeds, in particular in crops of useful plants.Type: GrantFiled: March 27, 2013Date of Patent: November 10, 2015Assignee: Syngenta LimitedInventors: Glynn Mitchell, Olivia Anabelle Sageot
-
Patent number: 9173849Abstract: The present invention provides a solid preparation containing compound (I) or a salt thereof, a pH control agent and a calcium antagonist, which is superior in the dissolution property, stability and the like.Type: GrantFiled: September 25, 2009Date of Patent: November 3, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Kazuhiro Hirata, Junya Nomura, Yutaka Tanoue
-
Patent number: 9102622Abstract: Disclosed are compounds of formula R—X—Y that may be used to inhibit the action of fatty acid amide hydrolase (FAAH). Inhibition of fatty acid amide hydrolase (FAAH) will slow the normal degradation and inactivation of endogenous cannabinoid ligands by FAAH hydrolysis and allow higher levels of those endogenous cannabinergic ligands to remain present. These higher levels of endocannabinoid ligands provide increased stimulation of the cannabinoid CB1 and CB2 receptors and produce physiological effects related to the activation of the cannabinoid receptors. They will also enhance the effects of other exogenous cannabinergic ligands and allow them to produce their effects at lower concentrations as compared to systems in which fatty acid amide hydrolase (FAAH) action is hot inhibited. Thus, a compound that inhibits the inactivation of endogenous cannabinoid ligands by fatty acid amide hydrolase (FAAH) may increase the levels of endocannabinoids and, thus, enhance the activation of cannabinoid receptors.Type: GrantFiled: July 27, 2007Date of Patent: August 11, 2015Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Spyridon P. Nikas, Shakiru O. Alapafuja, Vidyanand G. Shukla
-
Patent number: 9078446Abstract: Use of N-(tetrazol-4-yl)- or N-(triazol-3-yl)arylcarboxamides of formula (I) or salts thereof for controlling unwanted plants in areas of transgenic crop plants being tolerant to HPPD inhibitor herbicides by containing one or more chimeric gene(s) comprising (I) a DNA sequence encoding hydroxyphenylpyruvate dioxygenase (HPPD) derived from a member of a group of organisms consisting of (a) Avena, (b) Pseudomonas, (c) Synechococcoideae, (d) Blepharismidae, (e) Rhodococcus, (f) Picrophilaceae, (g) Kordia, or (II) comprising one or more mutated DNA sequences of HPPD encoding genes of the before defined organisms.Type: GrantFiled: March 21, 2012Date of Patent: July 14, 2015Assignee: BAYER INTELLECTUAL PROPERTY GMBHInventors: Fabien Poree, Andreas Almsick, Ralf Braun, Bernd Laber, Ruediger Hain
-
Patent number: 9073891Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.Type: GrantFiled: September 14, 2012Date of Patent: July 7, 2015Assignee: Imago Pharmaceuticals, Inc.Inventors: Hing L. Sham, Roy K. Hom, Andrei W. Konradi, Gary D. Probst, Simeon Bowers, Anh Truong, R. Jeffrey Neitz, Jennifer Sealy, Gergely Toth
-
Patent number: 9066936Abstract: The present invention provides a solid pharmaceutical composition containing compound (I) having an angiotensin II receptor antagonistic action and defined in the specification and a pH control agent, which composition is superior in the stability and dissolution property of compound (I).Type: GrantFiled: March 26, 2008Date of Patent: June 30, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Shuji Yoneyama, Yutaka Tanoue
-
Patent number: 9056844Abstract: A mGlu2/3 receptor antagonist of the formula: its uses, and methods for its preparation are described.Type: GrantFiled: November 15, 2011Date of Patent: June 16, 2015Assignee: Eli Lilly and CompanyInventors: Bruce Anthony Dressman, Mark Donald Chappell, Adam Michael Fivush, Charles Howard Mitch, Paul Leslie Ornstein, Eric George Tromiczak, Tatiana Natali Vetman
-
Patent number: 9040569Abstract: The present invention provides novel crystalline polymorphic forms of MDT-637, in particular, crystalline polymorphic forms with physicochemical properties specifically suited for drug production, amorphous formation, composite form, and methods of preparation thereof. The novel polymorphs described herein are useful for the treatment of respiratory disease, such as disease caused by respiratory syncytial virus.Type: GrantFiled: June 28, 2013Date of Patent: May 26, 2015Assignee: MICRODOSE THERAPEUTXInventors: Robert O. Cook, Eugene R. Reynolds, Boris Shekunov, Siead I. Zegar
-
Publication number: 20150141464Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit cdk5 -mediated phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: ApplicationFiled: November 20, 2012Publication date: May 21, 2015Inventors: Amy S. RIPKA, Jeffrey O. SAUNDERS
-
Publication number: 20150133414Abstract: It was determined whether SNPs in SLC4A5 are associated with salt sensitivity of blood pressure (BP). Subjects consumed an isocaloric constant diet with a randomized order of 7 days low Na+ (10 mmol/d) and 7 days high Na+ (300 mmol/d) intake. Salt sensitivity was defined as a ?7 mm Hg increase in mean arterial pressure (MAP). 35 polymorphisms in 17 candidate genes were assayed. Association analyses with salt sensitivity revealed three variants that associated with salt sensitivity, two in SLC4A5 (rs7571842, rs10177833; P<0.001), and one in GRK4 (rs1801058; P=0.020). Paradoxical changes in blood pressure in response to changes in salt intake were also found associated with a SNP for DRD2 (rs6276). In conclusion, SLC4A5 variants are strongly associated with salt sensitivity of BP in Caucasian and a DRD2 SNP is a marker for paradoxical response to salt intake.Type: ApplicationFiled: April 22, 2013Publication date: May 14, 2015Applicant: University of Virginia Patent FoundationInventors: Robin A. Felder, Robert M. Carey, John E. Jones, Pedro A. Jose, Scott M. Williams
-
Publication number: 20150133378Abstract: A method for identifying a kidney transplant recipient at an increased risk of developing interstitial fibrosis or tubular atrophy which comprises obtaining a post-transplant urine sample from the kidney transplant recipient; measuring the level of clusterin in the urine sample; comparing the level of clusterin in the patient sample to the level of clusterin in a control sample from the urine of a non-fibrotic kidney transplant recipient; diagnosing a kidney transplant recipient with a clusterin level that is significantly higher than the clusterin level in the control as being at an increased risk of developing interstitial fibrosis or tubular atrophy.Type: ApplicationFiled: April 17, 2013Publication date: May 14, 2015Inventors: Barbara Murphy, Philip J. O'Connell
-
Publication number: 20150133500Abstract: The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: and pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein W1, W2, W3, W4, U, G, m, R1, and R2 are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II to V as set forth supra. The invention also provides the use of compounds of any of the above discussed formulae to treat a disorder responsive to blockade of sodium channels. In one embodiment, Compounds of the Invention are useful for treating pain.Type: ApplicationFiled: November 6, 2014Publication date: May 14, 2015Inventors: Laykea Tafesse, Jiangchao Yao, Xiaoming Zhou
-
COMPOSITIONS AND METHODS FOR THE TREATMENT OF HYPERTENSION AND MANAGEMENT OF DIABETIC KIDNEY DISEASE
Publication number: 20150126568Abstract: The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing hypertension and diabetic kidney disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of diabetes related renal complications, hypertension, albuminuria, Heart Diseases, ESRD, Kidney GFR complications, Vascular Disease, Ventricular Septal Defect, vascular dilation, high blood pressure, congestive heart failure (CHF), post-myocardial infarction (MI).Type: ApplicationFiled: August 18, 2013Publication date: May 7, 2015Inventor: Mahesh Kandula -
Patent number: 9023874Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.Type: GrantFiled: November 11, 2010Date of Patent: May 5, 2015Assignee: Merial, Inc.Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
-
Publication number: 20150119329Abstract: The present invention is directed to a composition for the treatment or prevention of cerebral malaria that comprises an angiotensin receptor type-2 agonist and an antimalaria drug. The present invention is further directed to methods for treating and preventing cerebral malaria that involve administering an angiotensin receptor type-2 agonist and/or an angiotensin receptor type-1 antagonist.Type: ApplicationFiled: April 16, 2013Publication date: April 30, 2015Applicant: NEW YORK UNIVERSITYInventors: Ana Maria Rodriguez Fernandez, Julio Gallego-Delgado
-
Publication number: 20150105392Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Applicant: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Paul R. Fatheree, Robert Murray McKinnell
-
Patent number: 9006454Abstract: The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.Type: GrantFiled: March 26, 2010Date of Patent: April 14, 2015Assignee: Merck Serono S.A.Inventors: Siva Sanjeeva Rao Thunuguntla, Hosahalli Subramanya, Satish Reddy Kunnam, Sekhar Reddy Sanivaru Vijay, Chakrapani Bingi, Raviraj Kusanur, Matthias Schwarz, Michael Arlt
-
Publication number: 20150099730Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein L1, a, b, m, n, R1, R2, R3, R4, and R5 are defined herein.Type: ApplicationFiled: September 6, 2013Publication date: April 9, 2015Applicant: Janssen Pharmaceutica, NVInventor: Peter J. Connolly
-
Patent number: 8993614Abstract: There are provided compounds of the formula wherein X, Y, Z, R1, R2, R3 and R4 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.Type: GrantFiled: March 5, 2013Date of Patent: March 31, 2015Assignee: F. Hoffmann-La Roche AGInventors: David Joseph Bartkovitz, Xin-Jie Chu, Binh Thanh Vu, Chunlin Zhao, Daniel Fishlock
-
Publication number: 20150087512Abstract: The subject invention is directed toward antimicrobial agents and methods of treating and preventing infection by pathogenic microorganisms and endophytic microorganisms in a plant through the use of SecA inhibitors.Type: ApplicationFiled: September 26, 2014Publication date: March 26, 2015Inventors: Nian WANG, Nagaraju AKULA