Chalcogen Bonded Directly To Ring Carbon Of The Piperidine Ring Patents (Class 514/327)
  • Patent number: 8569341
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Grant
    Filed: June 3, 2011
    Date of Patent: October 29, 2013
    Assignee: Amgen Inc.
    Inventors: Michael Gribble, Jr., Zhihong Li
  • Publication number: 20130274249
    Abstract: Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them are useful as sodium and/or calcium channel modulators for preventing, alleviating and curing pathologies wherein the above mechanisms play a pathological role. The compounds may be particularly useful for the prevention, alleviation, and curing of, for example, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases.
    Type: Application
    Filed: March 11, 2013
    Publication date: October 17, 2013
    Inventors: Piero MELLONI, Alessandra Restivo, Emanuela Izzo, Simona Francisconi, Elena Colombo, Cibele Sabido-David
  • Publication number: 20130251673
    Abstract: 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: Application
    Filed: December 21, 2012
    Publication date: September 26, 2013
    Applicant: Novira Therapeutics, INC.
    Inventors: George D. HARTMAN, Osvaldo A. FLORES
  • Publication number: 20130252947
    Abstract: The present disclosure relates to a method to stimulate endogenous BMP-2 up-regulation in a subject which method comprises administering to a subject an effective amount of an H1 receptor antagonist, whereby endogenous BMP-2 up-regulation is stimulated in said subject. Also provided is a pharmaceutical formulation including an H1 receptor antagonist present in an effective amount to stimulate BMP-2 up-regulation in a subject and a kit.
    Type: Application
    Filed: May 17, 2013
    Publication date: September 26, 2013
    Applicant: Southwest Research Institute
    Inventor: Jorge Gianny ROSSINI
  • Publication number: 20130243688
    Abstract: Anionic non-phospholipids, as well as lipid nanostructures formed therefrom, are disclosed herein. Also disclosed are methods of producing and using same.
    Type: Application
    Filed: April 15, 2013
    Publication date: September 19, 2013
    Inventors: Vibhudutta Awasthi, Pallavi Lagisetty
  • Publication number: 20130245068
    Abstract: The present invention relates to a novel pharmaceutical composition of benproperine derivatives for preventing and treating angiogenesis-related diseases. The benproperine derivatives and pharmaceutically acceptable salts thereof according to the present invention inhibit cancer cell migration and the angiogenesis of vascular endothelial cells, and therefore can be effectively used not only as an anticancer agent, but also as an agent for preventing and treating diseases caused by abnormal angiogenesis, such as diabetic retinopathy and corneal transplant rejection.
    Type: Application
    Filed: May 10, 2013
    Publication date: September 19, 2013
    Applicant: Korea Research Institute of Bioscience and Biotechnology
    Inventors: Byoung Mog KWON, Dong Cho HAN, Dae Seop SHIN, Young Min HAN
  • Publication number: 20130245004
    Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.
    Type: Application
    Filed: May 9, 2013
    Publication date: September 19, 2013
    Applicant: Synchroneuron Inc.
    Inventors: Barry S. Fogel, William D. Kerns, Kei-Lai Fong
  • Publication number: 20130231311
    Abstract: Systems and methods are described for treating un-met medical needs in migraine and related conditions such as cluster headache. Included are treatments that are both rapid onset and long acting, which include sustained release formulations, and combination products. Also included are treatments for multiple symptoms of migraine, especially headache and nausea and vomiting. Systems that are self contained, portable, prefilled, and simple to self administer at the onset of a migraine attack are disclosed, and preferably include a needle-free injector and a high viscosity formulation, to eliminate such issues as fear of self administration with needles, and needle stick and cross contamination.
    Type: Application
    Filed: April 16, 2013
    Publication date: September 5, 2013
    Inventors: Stephen J. FARR, John TURANIN, Roger HAWLEY, Jeffrey A. SCHUSTER
  • Publication number: 20130224151
    Abstract: The present disclosure relates to methods of using fatty acid amide hydrolase (FAAH) inhibitors alone or in combination for the treatment or prevention of abdominal, visceral or pelvic pain. Also described herein are pharmaceutical compositions comprising a FAAH inhibitor, alone or in combination with an additional therapeutic agent for the treatment of abdominal, visceral or pelvic pain.
    Type: Application
    Filed: March 31, 2011
    Publication date: August 29, 2013
    Applicants: UNITED STATES OF AMERICA, IRONWOOD PHARMACEUTICALS, INC
    Inventors: James Philip Pearson, Mark G. Currie, Yvette Tache, Muriel Larauche
  • Publication number: 20130210766
    Abstract: Compositions containing a small molecule therapeutic and an alkyl N,N-disubstituted amino acetate are disclosed. Inclusion of the alkyl N,N-disubstituted amino acetate enhances the pharmacokinetic properties of the small molecule therapeutic.
    Type: Application
    Filed: May 4, 2011
    Publication date: August 15, 2013
    Applicant: NEXMED HOLDINGS, INC.
    Inventors: Bassam B. Damaj, Richard Martin
  • Patent number: 8507529
    Abstract: The present invention provides a dermatological and/or cosmetic composition which includes a methoxycinnamate, and a cyclic nitroxide. The present invention further provides a method of synthesizing photo absorbing-antioxidant compounds and their use in dermatological and/or cosmetic compositions. In addition, the present invention relates to the use of methoxycinnamate, and nitroxide compounds for the preparation of a composition for the dermatological and/or cosmetic treatment of skin.
    Type: Grant
    Filed: October 11, 2010
    Date of Patent: August 13, 2013
    Assignee: Jarrow Formulas, Inc.
    Inventors: Elisabetta Damiani, Paola Astolfi, Lucedio Greci
  • Publication number: 20130203734
    Abstract: Disclosed herein are methods of preventing or treating inflammatory diseases using sulfonamide analogs of 3-aminolactam compounds, each with aromatic “tail groups”. Compounds as defined by formulae (I) and (I?), and the medical uses of the compounds, are described herein.
    Type: Application
    Filed: June 8, 2011
    Publication date: August 8, 2013
    Inventors: David John Grainger, David John Fox
  • Publication number: 20130203815
    Abstract: The present invention provides compounds represented by general formula (I): wherein, R1, R2, R3, L and T are as defined in the specification, in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, and prodrugs thereof. The invention also relates to processes for the manufacture of compounds of formula (I) and pharmaceutical compositions containing them. The compounds and the pharmaceutical compositions of the present invention are useful in the treatment of a condition or disorder mediated by one or more cytokines selected from Tumor Necrosis Factor-alpha (TNF-?) and interleukins such as IL-1, IL-6, and IL-8. The present invention further provides a method of treatment of inflammatory disorders by administering a therapeutically effective amount of the said compound of formula (I) or its pharmaceutical composition, to a mammal in need thereof.
    Type: Application
    Filed: March 25, 2011
    Publication date: August 8, 2013
    Applicant: PIRAMAL ENTERPRISES LIMITED
    Inventors: Babasaheb Pandurang Bandgar, Jalindar Vasant Totre
  • Patent number: 8501778
    Abstract: The present invention relates to aralkyl piperidine derivatives, compositions containing the same, and their uses in the preparation of antalgic or ataractic medicament. The said derivatives are a free base of the compound represented by the following formula or a salt thereof. The pharmacological experiments show that they display favorable antalgic, ataractic activity and low side effects.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: August 6, 2013
    Assignees: NHWA Pharma. Corporation, Shanhai Institute of Pharmaceutical Industry
    Inventors: Jianqi Li, Guan Wang, Guisen Zhang, Yanqin Ma, Wenhua Ji, Yuan Zhang, Lin Guo
  • Patent number: 8501782
    Abstract: The present application describes modulators of MIP-1? of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators of formula (I) are disclosed.
    Type: Grant
    Filed: July 23, 2008
    Date of Patent: August 6, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Daniel S. Gardner, John V. Duncia, John Hynes, T.G. Murali Dhar, Percy H. Carter, Joseph B. Santella
  • Publication number: 20130196978
    Abstract: Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.
    Type: Application
    Filed: March 14, 2013
    Publication date: August 1, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • Publication number: 20130190288
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, A, X1, X2, X3, X4, R1, R2, R3a, R3b, R4a and R4b are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 25, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genentech, Inc.
  • Patent number: 8486381
    Abstract: The present invention relates to methods for treating intestinal fluid balance disorders and modulating intestinal fluid secretion and absorption using calcimimetics and calcilytics.
    Type: Grant
    Filed: August 28, 2006
    Date of Patent: July 16, 2013
    Assignee: Amgen Inc.
    Inventors: John Peter Geibel, Steven Charles Hebert, David Martin, Deborah A. Russell
  • Publication number: 20130178444
    Abstract: The present application describes prodrugs of the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis using the prodrug compounds of the invention are disclosed.
    Type: Application
    Filed: March 5, 2013
    Publication date: July 11, 2013
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130172318
    Abstract: Disclosed herein are methods of preventing or treating inflammatory diseases using 3-aminolactam compounds, each with aromatic “tail groups”. Compounds as defined by formulae (I) and (I?), and the medical uses of the compounds, are described herein.
    Type: Application
    Filed: June 8, 2011
    Publication date: July 4, 2013
    Inventors: David John Grainger, David John Fox
  • Publication number: 20130165422
    Abstract: The disclosure relates to hexafluoroisopropyl carbamate derivatives of general formula (I): in which: R, Z, A, m, and n are as defined in the disclosure; in the form of the base or of an addition salt with an acid, and to the preparation process and therapeutic application thereof.
    Type: Application
    Filed: November 29, 2012
    Publication date: June 27, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • Publication number: 20130157990
    Abstract: A method of detoxifying a patient addicted to at least one drug comprises the step of administering a first-medication component to the patient for mitigating drug withdrawal symptoms of the patient. The method further comprises the step of administering an anesthetic component to the patient for putting the patient in a sedated state. The method further comprises the step of administering a detoxification component to the patient for detoxifying the patient of the drug(s) while the patient is in the sedated state. The detoxification component can comprise naloxone. The method further comprises the step of administering a second-medication component to the patient for further mitigating drug withdrawal symptoms of the patient while the patient is in the sedated state. The second-medication component can comprise naltrexone. The method further comprises the step of terminating administration of the anesthetic component to the patient for reviving the patient from the sedated state.
    Type: Application
    Filed: February 20, 2013
    Publication date: June 20, 2013
    Applicant: EAGLE ADVANCEMENT INSTITUTE LLC
    Inventor: EAGLE ADVANCEMENT INSTITUTE LLC
  • Publication number: 20130156761
    Abstract: The present invention includes compositions that are useful in preventing or treating metastasis in a subject diagnosed with cancer. The present invention also includes methods of preventing or treating metastasis in a subject diagnosed with cancer, wherein the method comprises administering to the subject in need thereof an effective amount of a pharmaceutical formulation comprising at least one pharmaceutically acceptable carrier and at least one CX3CR1 or fractalkine antagonist.
    Type: Application
    Filed: February 25, 2013
    Publication date: June 20, 2013
    Applicants: Alliance Discovery, Inc., Philadelphia Health & Education Corporation d/b/a Drexel University College of Medicine
    Inventors: Philadelphia Health & Education Corporation d/b/a Drexel University College of Medicine, Alliance Discovery, Inc.
  • Publication number: 20130150367
    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: Application
    Filed: September 12, 2012
    Publication date: June 13, 2013
    Applicants: Abbott Laboratories, Abbott GmbH & Co. KG
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Publication number: 20130143861
    Abstract: The subject invention provides methods for reducing stroke rate, methods for preventing atrial remodeling, and methods for reversing atrial remodeling by administering budiodarone to reduce atrial fibrillation (AF) episode duration and an anticoagulant (AC). According to some methods of the invention, the average AF episode duration can be reduced to less than about 24, 5, 3 or 1 hour(s), and the maximum AF episode duration may be reduced to less than about 20, 10 or 5 hours. According to some methods of the invention, the reduced stroke rate upon administration of budiodarone and AC is less than the age-adjusted overall stroke rate. Further, some methods provide that patients who were refractory to one or more anti-arrhythmic drugs prior to administration of budiodarone may also be treated. Some methods provide for prevention of atrial remodeling and others provide for the reversal of atrial remodeling, including methods to quantify the reversal of atrial remodeling.
    Type: Application
    Filed: February 4, 2013
    Publication date: June 6, 2013
    Applicant: ARMETHEON, INC.
    Inventor: Armetheon, Inc.
  • Publication number: 20130143867
    Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.
    Type: Application
    Filed: January 18, 2013
    Publication date: June 6, 2013
    Applicant: SYCHRONEURON INC.
    Inventor: SYCHRONEURON INC.
  • Publication number: 20130143924
    Abstract: The present invention is directed to a non-therapeutical process for deterring vermin, which is based on the usage of the largely known beta amino-alcohol derivatives of formula (I) as described herein. Further, the present invention is directed to corresponding vermin-deterring compositions which contain these substances as the active ingredient, compounds of the formula (I) for the preparation of vermin-deterring compositions, and the use of compounds of formula (I) in the defense against vermin.
    Type: Application
    Filed: November 16, 2012
    Publication date: June 6, 2013
    Inventors: Pierre DUCRAY, Tania Cavaliero, Maike Lohrmann, Jacques Bouvier
  • Publication number: 20130143858
    Abstract: The invention relates to compounds according to Formula I: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, x and y are as defined herein. Compounds according to Formula I are pharmacologically effective as potassium channel inhibitors, in particular inhibitors of the acetylcholine operated inward rectifying potassium channel current (i.e. IKACh blockers), and are believed to be useful in the treatment of cardiac arrhythmias, in particular supraventricular tacharrhythmias, such as atrial fibrillation and atrial flutter.
    Type: Application
    Filed: January 28, 2013
    Publication date: June 6, 2013
    Applicant: ASTRAZENECA AB
    Inventor: AstraZeneca AB
  • Publication number: 20130142845
    Abstract: The present invention is concerned with the use of combinations of opioid agonists and antagonists for treating Crohn's disease.
    Type: Application
    Filed: January 30, 2013
    Publication date: June 6, 2013
    Applicant: Euro-Celtique S.A.
    Inventor: Euro-Celtique S.A.
  • Patent number: 8450345
    Abstract: Provided are methods of treating or preventing viral infections caused by or associated with a Dengue virus using iminosugars.
    Type: Grant
    Filed: February 22, 2010
    Date of Patent: May 28, 2013
    Assignees: The Chancellor, Masters and Scholars of the University of Oxford, United Therapeutics Corporation
    Inventors: Urban Ramstedt, Brennan Klose, Nicole Zitzmann, Raymond A. Dwek, Terry D. Butters
  • Publication number: 20130131052
    Abstract: Ophthalmically acceptable compositions used in arresting the development of cataracts or macular degeneration comprising a pharmaceutically acceptable carrier or diluent and a compound having the formula: where R1 and R2 are, independently, H or C1 to C3 alkyl; R3 and R4 are, independently C1 to C3 alkyl; and where R1 and R2, taken together, or R3 and R4, taken together, or both may be cycloalkyl; R5 is H, OH, or C1 to C6 alkyl; R6 is or C1 to C6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl; R7 is C1 to C6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl or where R6 and R7, or R5, R6 and R7, taken together, form a carbocycle or heterocycle having from 3 to 7 atoms in the ring.
    Type: Application
    Filed: December 21, 2012
    Publication date: May 23, 2013
    Inventors: William L. Matier, Ghanshyam Patil
  • Publication number: 20130109718
    Abstract: This invention relates to novel 1-cycloalkyl- or 1-heterocyclyl-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.
    Type: Application
    Filed: October 24, 2012
    Publication date: May 2, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Patent number: 8431563
    Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 23, 2011
    Date of Patent: April 30, 2013
    Assignee: Amgen Inc.
    Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, Jr., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
  • Patent number: 8426431
    Abstract: The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, anxiety, or manic depression, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
    Type: Grant
    Filed: January 7, 2011
    Date of Patent: April 23, 2013
    Assignee: Purdue Neuroscience Company
    Inventors: Nancy C. Lan, Yan Wang, Sui Xiong Cai
  • Publication number: 20130095156
    Abstract: The invention provides disintegratable films containing a mixture of high molecular weight and low molecular weight water soluble components; and a pharmaceutically or cosmetically active ingredient. Optionally, the films contain a starch component, a glucose component, a filler, a plasticizer and/or humectant. The films are preferably in the form of a mucoadhesive monolayer having a thickness sufficient to rapidly disintegrate in the oral environment and release the active ingredient without undue discomfort to the oral mucosa. The monolayer can be cut to any desired size or shape to provide conveniently useable unit dosage forms for administration to oral or other mucosal surfaces for human pharmaceutical, cosmetic, or veterinary applications. The invention further provides methods of administering the film compositions by placing the composition into, for example, the oral cavity for a sufficient period of time to permit the film to disintegrate and release the active ingredient.
    Type: Application
    Filed: December 10, 2012
    Publication date: April 18, 2013
    Applicant: Adhesives Research, Inc.
    Inventor: Adhesives Research, Inc.
  • Publication number: 20130096181
    Abstract: Provided herein are therapies for the treatment of pathological conditions, such as cancer, and method of using SCD1 antagonists.
    Type: Application
    Filed: October 12, 2012
    Publication date: April 18, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genentech, Inc.
  • Patent number: 8420674
    Abstract: The invention relates to methods for decreasing adverse events associated with pirfenidone (5-methyl-1-phenyl-2-(1H)-pyridone) therapy. The invention discloses an optimized dose escalation scheme that results in the patient having increased tolerance to adverse events associated with the administration of pirfenidone. The invention also discloses a starter pack that may be used in conjunction with the dose escalation scheme.
    Type: Grant
    Filed: July 7, 2010
    Date of Patent: April 16, 2013
    Assignee: Intermune, Inc.
    Inventor: Williamson Z. Bradford
  • Patent number: 8420823
    Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].
    Type: Grant
    Filed: April 17, 2009
    Date of Patent: April 16, 2013
    Assignee: MSD K.K.
    Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
  • Publication number: 20130085127
    Abstract: A heterocyclic compound useful as an antiallergic agent is provided. A compound represented by the following formula (1) or a salt thereof: wherein the ring A is a homocyclic or heterocyclic ring; the ring B is a heterocyclic ring which contains G and nitrogen atom N as constituent atoms thereof, wherein G is CH or N; R1 is a carbonyl group or an alkylene group; R2a and R2b are an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; X is an oxygen atom or a sulfur atom; Z is a hydroxyl group, an alkoxy group, a cycloalkyloxy group, an aryloxy group, an aralkyloxy group, an amino group, or an N-substituted amino group; and n is 0 or 1; with the proviso that when the ring A is a benzene ring or when the ring B is a piperazine ring, R1 is an alkylene group which may have a substituent.
    Type: Application
    Filed: May 23, 2011
    Publication date: April 4, 2013
    Applicant: ASKA Pharmaceutical Co., Ltd
    Inventors: Makoto Okada, Koichi Hasumi, Takahiro Nishimoto, Miwa Yoshida, Kouki Ishitani, Tomoji Aotsuka, Hashime Kanazawa
  • Patent number: 8410139
    Abstract: The present application describes prodrugs of the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis using the prodrug compounds of the invention are disclosed.
    Type: Grant
    Filed: October 4, 2010
    Date of Patent: April 2, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: John Hynes, Percy H. Carter, Lyndon A. M. Cornelius, T.G. Murali Dhar, John V. Duncia, Satheesh Nair, Joseph B. Santella, Jayakumar S. Warrier, Hong Wu
  • Publication number: 20130079370
    Abstract: A method of treating in a person a cancer tumor refractory to treatment with bortezomib or an agent sharing the apoptosis generating activity of bortezomib or any other anti-cancer drug, comprises administering to the person, in a pharmaceutically acceptable carrier, a pharmacologically effective dose of an agent selected from the group consisting of b-AP15 and other proteasome inhibitor abrogating the deubiquitinating (DUB) activity of the 19S RP DUBs.
    Type: Application
    Filed: September 20, 2012
    Publication date: March 28, 2013
    Applicant: VIVOLUX AB
    Inventor: Vivolux AB
  • Patent number: 8404717
    Abstract: Methods of treating, preventing and/or managing myelodysplastic syndromes are disclosed. Specific methods encompass the administrations of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidin-2,6-dione in combination with 5-azacytidine.
    Type: Grant
    Filed: March 24, 2011
    Date of Patent: March 26, 2013
    Assignee: Celgene Corporation
    Inventor: Jerome B. Zeldis
  • Publication number: 20130065885
    Abstract: The present invention relates generally to therapeutic formulations. More particularly, this present invention provides an oral delivery system for a therapeutic compound that is a base, a salt of a base or an amphoteric compound or a salt of a amphoteric compound with pharmacological, physiological or biochemical activity or a proactive form thereof. The present invention even more particularly provides a swallow formulation comprising a therapeutic compound that is a base, a salt of a base, an amphoteric compound or a salt of an amphoteric compound which facilitates the rapid delivery of the therapeutic compound to the circulatory system.
    Type: Application
    Filed: September 14, 2012
    Publication date: March 14, 2013
    Applicant: IMAGINOT PTY LTD.
    Inventors: Michael Stephen Roberts, Ruoying Jiang, Keivan Bezanehtak, Greg Andrew Davey, George Alexander Davidson, Geraldine Ann Elliott, Stephen Douglas Chandler, Mantu Sarkar
  • Patent number: 8394960
    Abstract: The present invention relates to novel Heterocyclic Ether or Thioether Derivatives, compositions comprising the Heterocyclic Ether or Thioether Derivatives, and methods for using the Heterocyclic Ether or Thioether Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: March 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gerald W. Shipps, Jr., Matthew Richards, Cliff C. Cheng, Xiaohua Huang
  • Patent number: 8383648
    Abstract: Ophthalmically acceptable compositions used in arresting the development of cataracts or macular degeneration comprising a pharmaceutically acceptable carrier or diluent and a compound having the formula: where R1 and R2 are, independently, H or C1 to C3 alkyl; R3 and R4 are, independently C1 to C3 alkyl; and where R1 and R2, taken together, or R3 and R4, taken together, or both may be cycloalkyl; R5 is H, OH, or C1 to C6 alkyl; R6 is or C1 to C6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl; R7 is C1 to C6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl or where R6 and R7, or R5, R6 and R7, taken together, form a carbocycle or heterocycle having from 3 to 7 atoms in the ring.
    Type: Grant
    Filed: June 18, 2008
    Date of Patent: February 26, 2013
    Assignee: Colby Pharmaceutical Company
    Inventors: William L. Matier, Ghanshyam Patil
  • Patent number: 8383651
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: September 15, 2010
    Date of Patent: February 26, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Doris Riether, Renee M. Zindell, Patricia Amouzegh, Nigel James Blumire, Monika Ermann, Innocent Mushi, Robert John Scott
  • Publication number: 20130045951
    Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.
    Type: Application
    Filed: October 18, 2012
    Publication date: February 21, 2013
    Applicant: CARDIOXYL PHARMACEUTICALS, INC.
    Inventor: CARDIOXYL PHARMACEUTICALS, INC.
  • Patent number: 8376140
    Abstract: A vehicle to carry a powered medication that addresses the limitations of the prior art. It includes a system and method. A powder delivery system includes a first panel and a second panel coupled together around a periphery of the panels to form a sealed void therebetween, each the panel having a width and length about equal to a standard credit card width and length, respectively; and a powder, disposed in the void, having a quantity at least about equal to an active dose of the powder; wherein a thickness of the panels with the powder disposed therebetween is not greater than about 0.1 inches and more preferably not greater than about 0.03 inches.
    Type: Grant
    Filed: April 20, 2009
    Date of Patent: February 19, 2013
    Assignee: Breakthrough Products, Inc.
    Inventor: Jordan Eisenberg
  • Patent number: 8362040
    Abstract: Compounds of the present invention having the formula exhibit inhibitory activity on the natural enzyme renin. Thus, compounds of formula (I) may be employed for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: January 29, 2013
    Assignee: Novartis AG
    Inventors: Richard Sedrani, Juergen Klaus Maibaum, Werner Breitenstein, Holger Sellner, Claus Ehrhardt, Nils Ostermann
  • Publication number: 20130023563
    Abstract: Provided are a novel amidine derivative having an activated blood coagulation factor X inhibitory activity, a production method thereof, a production intermediate therefor, and a pharmaceutical composition containing the amidine derivative. An amidinoaniline derivative represented by the following formula (1-1) or a pharmaceutically acceptable salt thereof: <in the formula (1-1), each symbol is as defined in the Description>, and a pharmaceutical composition containing the amidinoaniline derivative or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 26, 2012
    Publication date: January 24, 2013
    Applicant: AJINOMOTO CO., INC.
    Inventor: AJINOMOTO CO., INC.