C=x Bonded Directly To The Piperidine Ring (x Is Chalcogen) Patents (Class 514/330)
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Patent number: 8846072Abstract: The present invention relates to novel anesthetic compositions containing a non-polymeric carrier material and an anesthetic, where the compositions are suitable for providing a sustained local anesthesia without an initial burst and having a duration for about 24 hours or longer. Certain compositions are also provided that include a first anesthetic and a second anesthetic. In such compositions, the second anesthetic is a solvent for the first anesthetic and provides an initial anesthetic effect upon administration to a subject. The non-polymeric carrier may optionally be a high viscosity liquid carrier material such as a suitable sugar ester. The compositions can further include one or more additional ingredients including active and inactive materials. Methods of using the compositions of the invention to produce a sustained anesthetic effect at a site in a subject are also provided.Type: GrantFiled: March 7, 2013Date of Patent: September 30, 2014Assignee: Durect CorporationInventor: A. Neil Verity
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Patent number: 8846068Abstract: The present invention is directed to an implantable drug depot useful for reducing, preventing or treating post-operative pain in a patient in need of such treatment, the implantable drug depot comprising a polymer and a therapeutically effective amount of a local anesthetic or pharmaceutically acceptable salt thereof, wherein the drug depot is implantable at a site beneath the skin to reduce, prevent or treat post-operative pain, and the drug depot is capable of releasing (i) a bolus dose of the local anesthetic or pharmaceutically acceptable salt thereof at a site beneath the skin and (ii) a sustained release dose of an effective amount of the local anesthetic or pharmaceutically acceptable salt thereof over a period of at least 4 days.Type: GrantFiled: April 8, 2009Date of Patent: September 30, 2014Assignee: Warsaw Orthopedic, Inc.Inventors: Amira Wohabrebbi, William F. McKay, Vanja Margareta King, Danielle L. Biggs, Katara Shaw, Christopher M. Hobot, Phillip Edward McDonald
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Publication number: 20140288045Abstract: Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.Type: ApplicationFiled: March 14, 2014Publication date: September 25, 2014Inventors: Pingda Ren, Yi Liu, Liansheng Li, Jun Feng, Tao Wu
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Publication number: 20140288077Abstract: In one aspect, the invention relates to substituted 4-phenoxyphenol analogs, derivatives thereof, and related compounds, which are useful as inhibitors of proliferating cell nuclear antigen (PCNA); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating hyperproliferative disorders associated with PCNA using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: July 5, 2012Publication date: September 25, 2014Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITALInventors: Naoaki Fujii, Marcelo Actis, Chandanamali Punchihewa, Michele Connelly, Sean Wu
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Patent number: 8841328Abstract: The present invention relates to the use of selective insecticidal compositions, characterized by an effective amount of an active compound combination comprising (a) (1) at least one haloalkylnicotinic acid derivative of the formula (I) in which AA and R1A are as defined in the description, or (2) at least one phthalic acid diamide of the formula (II) in which XB, R1B, R2B, R3B, L1B, L2B and L3B are as defined in the description, or (3) at least one anthranilamide of the formula (III) in which A1C, A2C, XC, R1C, R2C, R3C, R4C, R5C, R7C, R8C and R9C are as defined in the description, and (b) at least one crop plant compatibility-improving compound from the group of compounds given in the description, in particular cloquintocet-mexyl, isoxadifen-ethyl and mefenpyr-diethyl for controlling insects and/or arachnids, and a method for controlling insects and/or arachnids using the compositions.Type: GrantFiled: December 3, 2013Date of Patent: September 23, 2014Assignee: Bayer CropScience AGInventors: Reiner Fischer, Rüdiger Fischer, Christian Funke, Achim Hense, Wolfram Andersch, Heike Hungenberg, Wolfgang Thielert, Udo Reckmann, Lothar Willms, Christian Arnold
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Patent number: 8841345Abstract: Compositions and methods for the treatment of premature ejaculation are provided wherein a composition comprising a topical anesthetic, a shear-thinning polymeric thickener, a lipophilic component that is selected from the group consisting of an aliphatic C1 to C8 alcohol, an aliphatic C8 to C30 ester, a liquid polyol and a mixture thereof, water and a buffer system that provides a buffered pH value for the composition in the range of about 3 to about 7.4 is administered to the penile meatus.Type: GrantFiled: March 22, 2004Date of Patent: September 23, 2014Assignee: Nexmed Holdings, Inc.Inventors: Mingqi Lu, Qin Wang, James L. Yeager, Y. Joseph Mo
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Publication number: 20140275145Abstract: Delivery systems and compositions comprised of a biodegradable polyorthoester polymer, an aprotic solvent, and a drug are described. The solvent is selected to modulate release of drug from the composition, where, in some embodiments, the solvent is rapidly released after administration and provides a corresponding rapid rate of drug release. Alternatively, in other embodiments, the solvent is slowly released from the composition after its administration, and provides a correspondingly slow rate of drug release.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: Heron Therapeutics, Inc.Inventors: Thomas B. Ottoboni, Lee Ann Lynn Schillinger
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Publication number: 20140275170Abstract: The present invention improves the bad taste of injected anesthetics and analgesics by incorporating a flavoring or cooling agent such as menthol into the parenteral composition.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: JSN I, LLCInventors: Jeremy Nehleber, Neil Ross
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Publication number: 20140275152Abstract: 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: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventors: Brian W. Metcalf, Zhe Li
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Publication number: 20140275046Abstract: Delivery systems and compositions comprised of a biodegradable polyorthoester polymer, an aprotic solvent, and a drug are described. The solvent is selected to modulate release of drug from the composition, where, in some embodiments, the solvent is rapidly released after administration and provides a corresponding rapid rate of drug release. Alternatively, in other embodiments, the solvent is slowly released from the composition after its administration, and provides a correspondingly slow rate of drug release.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: Heron Therapeutics, Inc.Inventors: Thomas B. Ottoboni, Lee Ann Lynn Schillinger, Joseph Niemann
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Publication number: 20140275037Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).Type: ApplicationFiled: December 19, 2013Publication date: September 18, 2014Applicant: Siga Technologies, Inc.Inventors: Yijun Deng, Theodore J. Nitz, Thomas R. Bailey, Yanming Zhang, Sylvie Laquerre
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Publication number: 20140271863Abstract: The present disclosure is in the field of controlled release delivery of actives (e.g., drug-delivery, cosmeceutics, alternative medicine) though from an unusual and novel delivery vehicle: personal clothing. Means are disclosed for producing controlled-release systems well-suited not only for affixation to fabrics—e.g., clothing, bedding—but also for maintenance of active throughout washing cycles including hot-wash laundry cycles. Some embodiments comprise a material comprising a unique combination of the thermoresponsive polymer poly-N-isopropylacrylamide, crosslinked and water-swollen in the form of a hydrogel, with embedded thin platelet-shaped solid crystals, drug-solubilizing microparticles, and a drug or other active that is released at ambient or body temperature, but only slowly in warm or hot water.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: TEXTILE-BASED DELIVERY, INC.Inventors: David Anderson, Jordan Schindler
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Publication number: 20140275008Abstract: 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: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventors: Qing Xu, Zhe Li
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Publication number: 20140275043Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted 3-phenylpropylamine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.Type: ApplicationFiled: March 11, 2014Publication date: September 18, 2014Applicant: Acucela Inc.Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
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Patent number: 8822416Abstract: This invention concerns a synergistic combination of a topical anesthetic and wound barrier forming agent capable of providing extended analgesia of ‘significant open wounds’ (that being, for example, a laceration, surgical incision, abrasion, ulcer or burn, but not being a minor cut, scratch, sting, burn or abrasion) in which conventional management alternatives (such as suturing and/or administration of injected or systemic analgesia) are impractical, unaffordable or otherwise unavailable.Type: GrantFiled: September 17, 2007Date of Patent: September 2, 2014Assignee: Animal Ethics Pty Ltd.Inventors: Meredith Sheil, Allan Giffard, Charles Robert Olsson
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Publication number: 20140243373Abstract: There is described a group of novel cyclic amine derivative compounds having an EP4 receptor agonistic activity. Specifically, the compounds according to the invention are provided with analgesic, antinflammatory, antiglaucoma activity, and also with anti-osteoporosis and antiulcerative activity. The present invention therefore relates to novel cyclic amine derivative compounds, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as pain, glaucoma, ulcerative colitis and osteoporosis.Type: ApplicationFiled: July 4, 2011Publication date: August 28, 2014Applicant: Rottapharm S.P.A.Inventors: Manuela Borriello, Sabrina Pucci, Luigi Piero Stasi, Lucio Rovati
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Publication number: 20140235628Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: September 10, 2012Publication date: August 21, 2014Inventors: Shawn Walsh, Alexander Pasternak, Brian Cato, Paul E. Finke, Jessica Frie, Qinghong Fu, Dooseop Kim, Barbara Pio, Aurash Shahripour, Zhi-Cai Shi, Haifeng Tang
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Publication number: 20140200225Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.Type: ApplicationFiled: March 27, 2014Publication date: July 17, 2014Applicant: ORION CORPORATIONInventors: Rajeev GOSWAMI, Anil Kumar VUPPALA, Ramesh VELUDANDI, Ramesh SISTLA, Chakshusmathi GHADIYARAM, Muralidhara RAMACHANDRA
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Patent number: 8772291Abstract: This invention relates to multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use in, for example, the treatment of cognitive disorders.Type: GrantFiled: December 8, 2009Date of Patent: July 8, 2014Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Joseph Barbosa, Li Dong, Cynthia Anne Fink, Jiancheng Wang, G. Gregory Zipp
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Publication number: 20140187532Abstract: 4-(azacycloalkyl)benzene-1,3-diol compounds are described corresponding to general formula (I) below: Also described, are compositions including the same, processes for preparation thereof and uses thereof in pharmaceutical or cosmetic compositions to treat pigmentary disorders.Type: ApplicationFiled: March 7, 2014Publication date: July 3, 2014Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Jean-Guy BOITEAU, Karine BOUQUET, Sandrine TALANO, Corinne MILLOIS BARBUIS
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Publication number: 20140179665Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.Type: ApplicationFiled: December 9, 2013Publication date: June 26, 2014Inventors: George D. Hartman, Osvaldo A. Flores
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Publication number: 20140171404Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in the treatment of an ATX-dependent or ATX-mediated disease or condition.Type: ApplicationFiled: December 17, 2013Publication date: June 19, 2014Applicant: NOVARTIS AGInventors: Vikki FURMINGER, Owen Rhys HUGHES, Darren Mark LEGRAND, Emily STANLEY, Christopher THOMSON
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Patent number: 8753665Abstract: The present invention relates to novel anesthetic compositions containing a non-polymeric carrier material and an anesthetic, where the compositions are suitable for providing a sustained local anesthesia without an initial burst and having a duration for about 24 hours or longer. Certain compositions are also provided that include a first anesthetic and a second anesthetic. In such compositions, the second anesthetic is a solvent for the first anesthetic and provides an initial anesthetic effect upon administration to a subject. The non-polymeric carrier may optionally be a high viscosity liquid carrier material such as a suitable sugar ester. The compositions can further include one or more additional ingredients including active and inactive materials. Methods of using the compositions of the invention to produce a sustained anesthetic effect at a site in a subject are also provided. Preferably the composition contains bupivacaine and a sugar ester such as saib.Type: GrantFiled: September 15, 2005Date of Patent: June 17, 2014Assignee: Durect CorporationInventor: A. Neil Verity
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Publication number: 20140163072Abstract: Methods, compositions and kits for treating a headache in a human patient are provided. The methods comprise intranasally administering to the patient a composition comprising a short-acting local anesthetic, a long-acting local anesthetic and a non-steroidal anti-inflammatory drug. A composition useful for practicing the methods of the disclosure is described which comprises a short-acting local anesthetic, a long-acting local anesthetic and a non-steroidal anti-inflammatory drug, wherein the composition is formulated for intranasal delivery. A kit comprising the composition and an intranasal applicator and a method of systemically delivering the composition to a human patient is also included in the disclosure. The headache-treating effectiveness of a local anesthetic in a Sphenopalatine Ganglion Block (SFGB) is significantly enhanced by coadministering diclofenac.Type: ApplicationFiled: December 6, 2012Publication date: June 12, 2014Inventor: Jose Carlos Romon-de-Jesus
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Publication number: 20140163024Abstract: Compounds of the formula Ia or Ib: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: December 10, 2013Publication date: June 12, 2014Applicant: GENENTECH, INC.Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Simon Gaines, Jonathan Killen, Stuart Ward
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Publication number: 20140155434Abstract: The present invention relates to a thermogelling pharmaceutical composition comprising local anaesthetics in base form and which is suitable for topical administration. The compositions further comprise a polyoxyethylene castor oil and one or more surfactants to obtain thermogelling characteristics.Type: ApplicationFiled: February 4, 2014Publication date: June 5, 2014Applicant: Pharmanest ABInventors: Mark Sundberg, Arne Brodin, Nils Kallberg
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Publication number: 20140148432Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of certain neurologic disorders, including disorders related to NMDA receptor activation, including neuropsychiatric disorders, neurodegenerative diorders and other neurologic diseases, disorders and conditions including stroke, brain injury, epilepsy, neuropsychiatric disorders, mood disorders, chronic pain and related conditions.Type: ApplicationFiled: January 31, 2014Publication date: May 29, 2014Inventors: Ruppa Poornachary Kamalesh Babu, Scott James Myers
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Publication number: 20140148486Abstract: A scleral lens is provided with a sodium channel blocker or a sodium channel modulator disposed in the pre-corneal tear film between the scleral lens and the cornea. This system can be used to deliver sodium channel blockers or a sodium channel modulators not currently used because of poor bioavailability. Methods of using this sodium channel blocker delivery system or a sodium channel modulator delivery system are also disclosed.Type: ApplicationFiled: January 29, 2014Publication date: May 29, 2014Applicant: Boston Foundation for SightInventor: Perry ROSENTHAL
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Patent number: 8735428Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: GrantFiled: March 1, 2013Date of Patent: May 27, 2014Assignee: Celgene CorporationInventor: Jerome B. Zeldis
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Publication number: 20140141086Abstract: Injectable depot compositions are provided that include a bioerodible, biocompatible polymer, a solvent having a miscibility in water of less than or equal to 7 wt. % at 25° C., in an amount effective to plasticize the polymer and form a gel therewith, a thixotropic agent, and a beneficial agent. The solvent comprises an aromatic alcohol, an ester of an aromatic acid, an aromatic ketone, or mixtures thereof. The compositions have substantially improved the shear thinning behavior and reduced injection force, rendering the compositions readily implanted beneath a patients body surface by injection.Type: ApplicationFiled: November 18, 2013Publication date: May 22, 2014Applicant: Durect CorporationInventors: Guohua Chen, Paul R. Houston, Lothar W. Kleiner
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Patent number: 8729069Abstract: The invention relates to compounds of structural formula (Ia): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, X4, X6, X10, R1, Y, Z, L, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: GrantFiled: September 28, 2010Date of Patent: May 20, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Gary Bohnert, Shoujun Chen, Yu Xie
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Patent number: 8722647Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: GrantFiled: May 30, 2012Date of Patent: May 13, 2014Assignee: Celgene CorporationInventor: Jerome B. Zeldis
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Patent number: 8722930Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.Type: GrantFiled: May 18, 2010Date of Patent: May 13, 2014Assignee: Orion CorporationInventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
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Publication number: 20140128368Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: June 11, 2012Publication date: May 8, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Michael Miller, Andrew Stamford, Kallol Basu, Harold B. Wood, Duane DeMong, Wanying Sun, Joie Garfunkle, Christopher Moyes, Zhiyong Hu, Ping Liu, Scott D. Edmondson, Xing Dai, Byron Gabriel DuBois
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Publication number: 20140124514Abstract: Anesthetics and other medical solutions are stored in a cartridge including a hollow body having a needle-penetrable septum at one end and a plunger at another end. A protective plug is inserted into the open plunger end of the cartridge and protects the cartridge from contamination per use. A buffer or other material may be injected into the cartridge, causing displacement of the protective plug, allowing the cartridge to then be used in a syringe or other delivery system. The anesthetic may contain at least one solute and have an initial tonicity and an initial pH. A volume of buffer may be injected through the septum into the anesthetic, where the initial solute concentration and initial pH of the anesthetic may be selected to provide a target pH and target tonicity after the buffer is introduced.Type: ApplicationFiled: October 31, 2013Publication date: May 8, 2014Applicant: Onpharma, Inc.Inventors: Matthew Stepovich, Michael Falkel, Mark Foley
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Publication number: 20140121217Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein A, Y, L, R1, W1 and W2 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: January 2, 2014Publication date: May 1, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Lijun Sun, Jun Jiang, Yu Xie
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Publication number: 20140107159Abstract: The present disclosure relates to compositions and methods for fabricating films for the delivery of a therapeutic agent containing at least one polymer and at least one therapeutic agent in a composition including a decreased alcohol fraction for providing smoother films and desired release characteristics. Drug-eluting films are also disclosed.Type: ApplicationFiled: September 17, 2013Publication date: April 17, 2014Applicant: Covidien LPInventors: Garrett Ebersole, Ryan Witherell, Amin Elachchabi, Joshua B. Stopek
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Publication number: 20140105989Abstract: Drug formulations that provide sustained action and/or reduced dosage requirements are provided. In the formulations the drugs (particularly local anesthetics) are associated with reversed cubic phase and reversed hexagonal phase lyotropic liquid crystalline material.Type: ApplicationFiled: December 23, 2013Publication date: April 17, 2014Applicant: Lyotropic Therapeutics, Inc.Inventors: David Anderson, Benjamin G. Cameransi, JR.
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Patent number: 8685985Abstract: The present invention relates to the use of selective insecticidal compositions, characterized by an effective amount of an active compound combination comprising (a) (1) at least one haloalkylnicotinic acid derivative of the formula (I) in which AA and R1A are as defined in the description, or (2) at least one phthalic acid diamide of the formula (II) in which XB, R1B, R2B, R3B, L1B, L2B and L3B are as defined in the description, or (3) at least one anthranilamide of the formula (III) in which A1C, A2C, XC,R1C, R2C, R3C, R4C, R5C, R7C, R8Cand R9C are as defined in the description, and (b) at least one crop plant compatibility-improving compound from the group of compounds given in the description, in particular cloquintocet-mexyl, isoxadifen-ethyl and mefenpyr-diethyl for controlling insects and/or arachnids, and a method for controlling insects and/or arachnids using the compositions.Type: GrantFiled: November 11, 2010Date of Patent: April 1, 2014Assignee: Bayer CropScience AGInventors: Reiner Fischer, Rüdiger Fischer, Christian Funke, Achim Hense, Wolfram Andersch, Heike Hungenberg, Wolfgang Thielert, Udo Reckmann, Lothar Willms, Christian Arnold
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Publication number: 20140088074Abstract: Fluorinated arylalkylaminocarboxamide derivatives of formula (I) are described wherein W, J, n, R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification and pharmaceutically salts thereof, pharmaceutical compositions containing them as active ingredients and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urological, and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.Type: ApplicationFiled: May 29, 2012Publication date: March 27, 2014Applicant: NEWRON PHARMACEUTICALS S.P.A.Inventor: Paolo Pevarello
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Publication number: 20140086936Abstract: The present invention provides matriptase inhibitors and compositions for treating and preventing orthomyxovirus infections such as flu infections. The present invention also provides novel compounds, compositions, methods of use, uses and kits thereof for inhibiting matriptase. Such compounds are useful for treating and preventing orthomyxovirus infections, such as flu infections, and for inhibiting tumor growth, progression and/or metastasis.Type: ApplicationFiled: May 28, 2012Publication date: March 27, 2014Applicant: SOCPRA SCIENCES SANTE ET HUMAINES S.E.C.Inventors: Martin Richter, Richard Leduc, Eloic Colombo, Eric Marsault
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Patent number: 8680279Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of certain neurologic disorders, including disorders related to NMDA receptor activation, neuropsychiatric disorders, neurodegenerative disorders and other neurologic diseases, disorders and related conditions. The compounds are of the Formulas I and Ia-Ij as described herein.Type: GrantFiled: June 13, 2012Date of Patent: March 25, 2014Assignee: Neurop, Inc.Inventors: Ruppa Poornachary Kamalesh Babu, Scott James Myers
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Publication number: 20140080802Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.Type: ApplicationFiled: October 28, 2013Publication date: March 20, 2014Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen Haggarty, Yan-Ling Zhang
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Patent number: 8673939Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: GrantFiled: March 1, 2013Date of Patent: March 18, 2014Assignee: Celgene CorporationInventor: Jerome B. Zeldis
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Publication number: 20140066481Abstract: The present invention relates to a water-free pharmaceutical composition comprising one or more local anaesthetics in base form and which is suitable for topical administration. The composition further comprises a lipid vehicle comprising long-chain triglycerides (LCT) and at least 10% by weight of medium-chain monoglycerides (MCM) selected so the composition has an at least semi-solid appearance at the body temperature at the site of administration. The invention further relates to methods of producing and sterilizing the compositions.Type: ApplicationFiled: March 30, 2011Publication date: March 6, 2014Applicant: PHARMANEST ABInventors: Mark Sundberg, Arne Brodin, Anders Carlsson
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Publication number: 20140051680Abstract: This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).Type: ApplicationFiled: February 28, 2012Publication date: February 20, 2014Applicant: REPLIGEN CORPORATIONInventors: Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
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Publication number: 20140031392Abstract: A method for treating bisretinoid-mediated macular degeneration in a mammal afflicted therewith comprising administering to the mammal an effective amount of a compound having the structure: or an ester or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: November 22, 2011Publication date: January 30, 2014Inventors: Konstantin Petrukhin, Janet Sparrow, Rando Allikmets
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Patent number: 8637576Abstract: Benzamide derivatives of formulae I and II, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof, and pharmaceutical compositions comprising the same, are described and have therapeutic utility, particularly in the treatment of diabetes, obesity, and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are defined as provided herein.Type: GrantFiled: October 20, 2009Date of Patent: January 28, 2014Assignee: Amgen Inc.Inventors: Jay P. Powers, Michael R. Degraffenreid, Xiao He, Lisa D. Julian, Dustin L. McMinn, Daqing Sun, Yosup Rew, Xuelei Yan
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Publication number: 20140018371Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.Type: ApplicationFiled: March 30, 2012Publication date: January 16, 2014Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Robert M. Jones, Sangdon Han, Juerg Lehmann, Lars Thoresen
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Publication number: 20140005226Abstract: The present invention provides a compound of the Formula II: wherein X is: R1 is H, —CN, or F; R2 is H or methyl; R3 is H; and R4 is H, methyl, or ethyl; or R3 and R4 joined together form a cyclopropyl ring; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 20, 2013Publication date: January 2, 2014Inventors: Matthew Allen SCHIFFLER, Jeremy Schulenburg YORK