Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Nitrogen Patents (Class 548/338.1)
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Patent number: 8653070Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: December 14, 2010Date of Patent: February 18, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Hui Cao, Lu Ying, Yat Sun Or
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Publication number: 20140045779Abstract: This invention relates with anti-tumor activities of new compounds containing an adamantyl group or analogs thereof.Type: ApplicationFiled: August 29, 2011Publication date: February 13, 2014Inventor: Lifeng Xu
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Publication number: 20140024835Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: September 24, 2013Publication date: January 23, 2014Applicant: THERAVANCE, INC.Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Publication number: 20140011851Abstract: The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.Type: ApplicationFiled: June 24, 2013Publication date: January 9, 2014Inventors: Luigi Anzalone, Frank J. Villani, Christopher A. Teleha, Penina Feibush, Barry Fegely
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Publication number: 20140005244Abstract: The invention relates to a family of stable polyamine arylethylamide compounds, and to the use of these compounds as agents inhibiting DNA damages induced by by-products of the non-enzymatic glycosylation of skin tissues. The invention also relates to cosmetic or dermocosmetic compositions intended to fight skin disorders associated with said glycosylation by-products.Type: ApplicationFiled: July 1, 2013Publication date: January 2, 2014Applicant: EXSYMOLInventor: Marie-Christine SEGUIN
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Patent number: 8609865Abstract: The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.Type: GrantFiled: July 1, 2011Date of Patent: December 17, 2013Assignee: Furiex Pharmaceuticals, Inc.Inventors: Luigi Anzalone, Frank J. Villani, Christopher A. Teleha, Penina Feibush, Barry Fegely
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Patent number: 8604056Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: GrantFiled: July 3, 2012Date of Patent: December 10, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Donald J. P. Pinto, Joanne M. Smallheer, James R. Corte, Zilun Hu, Cullen L. Cavallaro, Paul J. Gilligan, Mimi L. Quan, Leon M. Smith, II
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Publication number: 20130289034Abstract: Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.Type: ApplicationFiled: June 21, 2013Publication date: October 31, 2013Inventors: Orion D. JANKOWSKI, Kieron E. WESSON, Paul MOLLARD, William D. SHRADER
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Publication number: 20130267609Abstract: There is provided a gelator that is capable of forming a gel by an extremely small amount of addition in a wide pH range from acidic to alkaline regions, and a gel having high environmental compatibility, biocompatibility, and biodegradability. A gelator comprising: a lipid peptide of Formula (1) wherein R1 is a C9-23 aliphatic group, R2 is a hydrogen atom or a C1-4 alkyl group optionally having a C1-2 branched chain, R3 is a —(CH2)n—X group, n is a number from 1 to 4, and X is an amino group, a guanidino group, a —CONH2 group, or a 5-membered ring optionally having 1 to 3 nitrogen atoms, a 6-membered ring optionally having 1 to 3 nitrogen atoms, or a fused heterocycle including a 5-membered ring and a 6-membered ring that optionally has 1 to 3 nitrogen atoms); or a pharmaceutically usable salt of the lipid peptide.Type: ApplicationFiled: June 6, 2013Publication date: October 10, 2013Applicant: Nissan Chemical Industries, Ltd.Inventors: Misao MIYAMOTO, Nobuhide MIYACHI, Takehisa IWAMA
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Publication number: 20130267610Abstract: There is provided a gelator that is capable of forming a gel by an extremely small amount of addition in a wide pH range from acidic to alkaline regions, and a gel having high environmental compatibility, biocompatibility, and biodegradability. A gelator comprising: a lipid peptide of Formula (1) wherein R1 is a C9-23 aliphatic group, R2 is a hydrogen atom or a C1-4 alkyl group optionally having a C1-2 branched chain, R3 is a —(CH2)n—X group, n is a number from 1 to 4, and X is an amino group, a guanidino group, a —CONH2 group, or a 5-membered ring optionally having 1 to 3 nitrogen atoms, a 6-membered ring optionally having 1 to 3 nitrogen atoms, or a fused heterocycle including a 5-membered ring and a 6-membered ring that optionally has 1 to 3 nitrogen atoms); or a pharmaceutically usable salt of the lipid peptide.Type: ApplicationFiled: June 6, 2013Publication date: October 10, 2013Applicant: Nissan Chemical Industries, Ltd.Inventors: Misao MIYAMOTO, Nobuhide MIYACHI, Takehisa IWAMA
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Patent number: 8546400Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.Type: GrantFiled: January 9, 2013Date of Patent: October 1, 2013Assignee: Neosome Life Sciences, LLCInventors: Laxman S. Desai, Srinivas Chittaboina
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Publication number: 20130245087Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: November 26, 2012Publication date: September 19, 2013Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Publication number: 20130237702Abstract: A composition containing a compound represented by General Formula (I) below (see the definition in the specification for the symbols in the formula) or a salt thereof has an excellent CaSR agonistic effect and provides a pharmaceutical agent, a CaSR agonistic agent, a prophylactic or therapeutic agent for a disease that can be ameliorated through CaSR activation as well as seasonings and an agent for imparting kokumi.Type: ApplicationFiled: August 31, 2012Publication date: September 12, 2013Applicant: AJINOMOTO CO., INC.Inventors: Masayuki SUGIKI, Toru OKAMATSU, Tetsuo YANO, Shinya TANIGUCHI
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Publication number: 20130230501Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.Type: ApplicationFiled: July 16, 2012Publication date: September 5, 2013Applicant: Daiichi Sankyo Company, LimitedInventors: Tsutomu Nagata, Masahiro Inoue, Yuka Ashida, Kengo Noguchi, Makoto Ono
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Publication number: 20130231323Abstract: Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R1, R2, R3, R101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections.Type: ApplicationFiled: September 6, 2011Publication date: September 5, 2013Applicant: DUKE UNIVERSITYInventors: Pei Zhou, Eric J. Toone
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Publication number: 20130217660Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.Type: ApplicationFiled: May 12, 2011Publication date: August 22, 2013Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
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Publication number: 20130203895Abstract: The present invention relates to curatives for epoxy resins, and compositions (e.g. adhesives) containing such resins cured using the same, methods of preparation and uses therefor. More specifically, the present invention relates to hybrid curatives for epoxy resins comprising both aromatic amine, phenol and/or phenyl ester moieties. A further aspect of the current invention relates to new imidazole catalysts that posses a combination of excellent cure latency as well as low cure temperature onset.Type: ApplicationFiled: March 15, 2013Publication date: August 8, 2013Applicant: DESIGNER MOLECULES, INC.Inventor: Designer Molecules, Inc.
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Patent number: 8501824Abstract: This disclosure provides a range of amino acid lipid compounds and compositions useful for drug delivery, therapeutics, and the diagnosis and treatment of diseases and conditions. The amino acid lipid compounds and compositions can be used for delivery of various agents such as nucleic acid therapeutics to cells, tissues, organs, and subjects.Type: GrantFiled: March 30, 2011Date of Patent: August 6, 2013Assignee: Marina Biotech, Inc.Inventors: Steven C. Quay, Michael E. Houston, Jr., Pierrot Harvie, Roger C. Adami, Renata Fam, Mary G. Prieve, Kathy L. Fosnaugh, Shaguna Seth
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Patent number: 8501798Abstract: The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: June 19, 2012Date of Patent: August 6, 2013Assignee: Theravance, Inc.Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
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Patent number: 8492422Abstract: The present invention relates to method for treating skin diseases and skin conditions in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, or enantiomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: September 15, 2011Date of Patent: July 23, 2013Assignee: Allergan, Inc.Inventors: Mohammad I. Dibas, Ken Chow, Liming Wang, Michael E. Garst, John E. Donello, Daniel W. Gil
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Publication number: 20130184222Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.Type: ApplicationFiled: July 15, 2011Publication date: July 18, 2013Applicant: AGIOS PHARMACEUTICALS, INCInventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
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Publication number: 20130123485Abstract: The present invention provides cationic lipids, methods for preparing the same, and delivery systems comprising the same. The present invention can provide cationic lipids which enhance the efficiency of intracellular or in vivo delivery of multiple-anionic target compounds such as drugs, anticancer agents, nucleic acids, etc., have no intracellular toxicity, but show increased stability, methods for preparing the same, and delivery systems comprising the same.Type: ApplicationFiled: July 12, 2011Publication date: May 16, 2013Inventors: Myung-Ok Park, Eun Young Yoon
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Publication number: 20130109866Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: ApplicationFiled: October 23, 2012Publication date: May 2, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Publication number: 20130096315Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.Type: ApplicationFiled: September 12, 2012Publication date: April 18, 2013Inventors: Xiangping Qian, Andrew I. McDonald, Han-Jie Zhou, Luke W. Ashcraft, Bing Yao, Hong Jiang, Jennifer Kuo Chen Huang, Jianchao Wang, David J. Morgans, JR., Bradley P. Morgan, Gustave Bergnes, Dashyant Dhanak, Steven D. Knight, Nicholas D. Adams, Cynthia A. Parrish, Kevin Duffy, Duke Fitch, Rosanna Tedesco
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Publication number: 20130090478Abstract: The present invention is directed to novel opioid receptor modulators of Formula (I). The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of disorders that may be ameliorated or treated by the modulation of opioid receptors.Type: ApplicationFiled: November 30, 2012Publication date: April 11, 2013Inventor: Jannsen Pharmaceutica, N.V.
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Publication number: 20130029991Abstract: The present invention relates to new sulfonamide derivatives of formula (I) wherein R1-R8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.Type: ApplicationFiled: August 1, 2012Publication date: January 31, 2013Inventors: Gyula Beke, Eva Bozo, Sandor Farkas, Katalin Hornok, Gyorgy Keseru, Eva Schmidt, Eva Szentirmay, Istvan Vago, Monika Vastag
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Publication number: 20130022587Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.Type: ApplicationFiled: July 16, 2012Publication date: January 24, 2013Applicant: Daiichi Sankyo Company, LimitedInventors: Tsutomu Nagata, Masahiro Inoue, Yuka Ashida, Kengo Noguchi, Makoto Ono
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Publication number: 20130017196Abstract: The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Inventors: Weibo Wang, Paul A. Barsanti, Yia Xia, Rustum Boyce, Sabina Pecchi, Nathan Brammeier, Megan C. Phillips, Kris Mendenhall, Kelly Wayman, Liana Marie Lagnition, Ryan Constantine, Hong Yang, Elizabeth Mieuli, Savithri Ramurthy, Elisa Jazan, Anu Sharma, Rama Jain, Sharadha Subramanian, Paul A. Renhowe, Kenneth W. Bair, David Duhl, Annette Walter, Tinya Abrams, Kay Huh, Eric Martin, Mark Knapp, Vincent P. Le
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Publication number: 20130012620Abstract: The present invention relates to curatives for epoxy resins, and compositions (e.g. adhesives) containing such resins cured using the same methods of preparation and uses therefor. More specifically, the present invention relates to hybrid curatives for epoxy resins comprising both aromatic amine, phenol and/or phenyl ester moieties. A further aspect of the current invention relates to new imidazole catalysts that possess a combination of excellent cure latency as well as low cure temperature onset.Type: ApplicationFiled: March 16, 2011Publication date: January 10, 2013Applicant: DESIGNER MOLECULES, INC.Inventor: Stephen M Dershem
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Publication number: 20120329711Abstract: The invention relates to GLP-1 receptor agonist compounds with a modified N-terminus. The compounds are of the formula Chem. 1: Y—Z—P, wherein P represents a fragment of a GLP-1 receptor agonist peptide lacking the two N-terminal amino acid residues; and Y—Z represents novel His-Ala mimetics. Examples of GLP-1 receptor agonist compounds are derived from human GLP-1 (7-37), exendin-4(1-39), or GLP-1 A (1-37). The invention also relates to derivatives of these compounds, in particular compounds with one or more albumin binding side chains capable of protracting the duration of action in vivo of these compounds. The peptides and derivatives of the invention have a good potency, a protracted pharmacokinetic profile, are stable against degradation by gastro intestinal enzymes, and/or have a high oral bioavailability. These properties are of importance in the development of GLP-1 receptor agonist compounds for subcutaneous, intravenous, and/or in particular oral administration.Type: ApplicationFiled: December 16, 2010Publication date: December 27, 2012Applicant: Nordisk A/SInventors: Janos Tibor Kodra, Johnny Madsen, Patrick William Garibay
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Publication number: 20120316212Abstract: The present invention relates to amino alcohol derivatives of general formula I: These derivatives possess an interesting activity in that they block the secondary products of lipid oxidative stress, and are consequently suitable for therapeutic use in all disorders related with the presence of reactive carbonyl compounds.Type: ApplicationFiled: December 20, 2010Publication date: December 13, 2012Applicants: UNIVERSITA DEGLI STUDI DI MILANO, FLAMMA S.P.A.Inventors: Gianpaolo Negrisoli, Renato Canevotti, Massimo Previtali, Giancarlo Aldini, Marina Carini, Marica Orioli, Giulio Vistoli
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Patent number: 8324401Abstract: Novel non-steroidal compounds are provided that are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases having the structure of formula (I): or enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, where X is A1QA2-; Q is a bond, —C(?O)—, —OC(O)—, —C(?O)NR5—, —SOp—, —SOpNR5—, —C(O)O—, —NR5C(O)—, —OC(O)NR5—, —NR5C(O)O—, —S(O)pNR5C(O)—, —C(O)NR5S(O)p— —NR5S(O)p—, or —NR5C(?O)NR6—. Y is selected from hydrogen, C1-6alkyl, OR16, substituted C1-6alkyl, cycloalkyl, aryl, heterocyclo and heteroaryl. A1 and A2 are independently selected from a bond, C1-3alkylene, or C1-3alkenylene, and R1-R11 are defined herein. Also provided are pharmaceutical compositions, combinations, and methods of treating obesity, diabetes and inflammatory- or immune-associated diseases comprising said compounds.Type: GrantFiled: August 18, 2009Date of Patent: December 4, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Jingwu Duan, Bin Jiang
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Patent number: 8324261Abstract: The present invention is to provide a novel compound which is useful as a pharmaceutical agent such as an analgesic. The present invention is to provide the novel histidine derivative having an excellent analgesic action and the like. The compound of the present invention has a very high intermigration into the blood upon oral administration and is very useful as a pharmaceutical agent, especially an analgesic for the treatment of acute or chronic pain diseases and of neuropathic pain diseases.Type: GrantFiled: July 18, 2008Date of Patent: December 4, 2012Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Yoshitaka Nakazawa, Kenji Mitsuda, Tomohiro Ookubo, Teppei Seguchi, Hiroyoshi Nanba
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Patent number: 8318950Abstract: The present invention relates to N-acyl derivatives of amino acids and pharmaceutically acceptable salts thereof wherein n is 2 or 3; and R1 represents or pharmaceutically acceptable salts thereof, to novel processes for preparing the same, to use thereof as anti-allergic, anti-anaphylactic, anti-inflammatory and hypolipidemic agents as well as to a pharmaceutical composition comprising the indicated compounds in an efficient amount and to a method for treating allergic and inflammatory diseases and lipid metabolism disorders: bronchial asthma, allergic rhinitis, pollinoses, seasonal and year-round rhinitis, allergic pneumonitis, atopic dermatitis, psoriasis, urticaria, allergic (including anaphylactic) reactions to insect stings and medicaments, cold allergy, allergic conjunctivitis, atherosclerosis, obesity, ischemic heart and cerebral disease, myocardial infarction and stroke.Type: GrantFiled: April 21, 2010Date of Patent: November 27, 2012Assignee: Otkrytoe Aktsionernoe Obschestvo-Otechestvennye LekarstvaInventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova, Galina Alexandrovna Alexandrovna Zheltukhina, Violetta Leonidovna Kovaleva
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Publication number: 20120277289Abstract: Activity-generating delivery molecules comprising the structure R3—(C?O)-Xaa-NH—R4 wherein Xaa is any D- or L-amino acid residue with a non-hydrogen, substituted or unsubstituted side chain, R3—(C?O)— and —NH—R4 are independently a long chain group, each long chain group containing one or more carbon-carbon double bonds, and salts, compositions and methods of use thereof. The activity-generating delivery compounds and compositions are useful for generating activity of an active agent in a cell, tissue, or subject.Type: ApplicationFiled: November 4, 2010Publication date: November 1, 2012Applicant: MARINA BIOTECH, INC.Inventors: Renata Fam, Roger C. Adami, Kathy L. Fosnaugh, Pierrot Harvie, Rachel E. Johns, Shaguna Seth, Michael E. Houston, JR., Michael V. Templin
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Publication number: 20120277256Abstract: Embodiments of the present disclosure include a coordination complex, comprising a first biologically active moiety, a second biologically active moiety, and a metal, wherein the first biologically active moiety and second biologically active moiety are bound to the metal by covalent coordination bonds, and wherein the first biologically active moiety and second biologically active moiety are different. These complexes may enhance the pharmacodynamic properties of biologically active moieties.Type: ApplicationFiled: July 5, 2012Publication date: November 1, 2012Applicant: Synthonics, Inc.Inventors: Thomas Piccariello, Scott B. Palmer, John D. Price, Robert Oberlender, Mary C. Spencer, Michaela E. Mulhare
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Patent number: 8293943Abstract: Preventing skin aging by targeting multiple causes by a single bullet is of primal scientific and consumer interest.Type: GrantFiled: February 18, 2012Date of Patent: October 23, 2012Assignee: Island Kinetics, Inc.Inventors: Shyam K Gupta, Linda Walker
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Publication number: 20120258059Abstract: It is an object of the present invention to provide a cosmetic or external skin preparation that has an improved feel in use, e.g., excellent stretching on the skin surface, excellent permeation into the skin, and no stickiness, or crinkles. A cosmetic or an external skin preparation, and a medical instrument, comprising at least one lipid peptide-based gelator that contains a low-molecular lipid peptide of Formula (1): (where R1 to R3 are independently an organic group) or a pharmaceutically usable salt thereof.Type: ApplicationFiled: October 26, 2010Publication date: October 11, 2012Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Takehisa Iwama, Keigo Matsumoto, Takayuki Imoto, Nobuhide Miyachi, Masahiro Goto
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Publication number: 20120232120Abstract: A compound of the formula: where X is phenyl substituted at the 3, 4 and 5 positions with R1, R2 or R3 which are selected from hydrogen, chloro, lower alkyl of 1 to 5 carbons, phenoxy, phenyl, naphthyl, or phenyl (lower) alkyl where the lower alkyl group has 1-5 carbon atoms and m is 0 or 1; Y is —CONH— or —NHCONH— where the nitrogen atoms are unsubstituted or substituted with other phenoxyisobutyric acid derivatives, or the residue of a phenoxyisobutyric acid and n is 0 or 1; Z is unsubstituted phenyl when m is 1 and n is 1; when Y is 0, X is 0; Z is also substituted.Type: ApplicationFiled: March 8, 2012Publication date: September 13, 2012Inventors: IRAJ LALEZARI, JILL FABRICANT
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Publication number: 20120230986Abstract: A method for treating an autism spectrum condition includes administering an effective dose of a TNF-? inhibiting agent to a person having an autism spectrum condition or pervasive development disorder and at least one of elevated TNF-? in the cerebrospinal fluid or elevated TNF-? in the serum, as compared to normal conditions; and lowering at least one of the elevated TNF-? in the cerebrospinal fluid or elevated TNF-? in the serum. A TNF-? inhibiting agent includes at least one of Lenalinomide; Thalidomide; L-Carnosine; Infliximab; Etanercept; a stem cell preparation; derivatives thereof, isomers thereof, or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: May 4, 2012Publication date: September 13, 2012Inventor: Michael Chez
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Patent number: 8258343Abstract: Preventing skin aging by targeting multiple causes by a single bullet is of primal scientific and consumer interest.Type: GrantFiled: February 15, 2012Date of Patent: September 4, 2012Assignee: Island Kinetics, Inc.Inventors: Shyam K Gupta, Linda Walker
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Patent number: 8252832Abstract: The invention provides novel compounds having a substituted imidazole ring, and methods of using such compounds for the treatment of certain disorders such as hematological cancers and solid tumors. The compounds of the invention are tri-substituted imidazole derivatives that inhibit KSP. These compounds are also useful for the treatment of drug resistant tumors, such as solid tumors that express elevated levels of P-glycoprotein.Type: GrantFiled: November 25, 2008Date of Patent: August 28, 2012Assignee: Novartis AGInventors: Tinya Abrams, Paul Barsanti, David Duhl, Michel Faure, Paul A. Renhowe, Annette Olga Walter
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Publication number: 20120214849Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 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: November 17, 2011Publication date: August 23, 2012Applicant: THERAVANCE, INC.Inventors: Seok-ki Choi, Paul R. Fatheree, Roland Gendron, Robert Murray McKinnell, Brooke Blair
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Patent number: 8236844Abstract: A novel histidine derivative represented by the following formula (I), and a pharmaceutically acceptable salt and hydrate thereof, useful as a pharmaceutical agent such as analgesics for the treatment of various kinds of acute or chronic pain diseases and of neuropathic pain diseases: wherein, R1 is hydrogen, alkyl having 1 to 6 carbon(s) or benzyl which may be substituted with alkyl having 1 to 4 carbon(s) or halogen; R2 is hydrogen or alkyl having 1 to 4 carbon(s); R3 and R4 are same or different and each is hydrogen, alkyl having 1 to 4 carbon(s) or phenyl which may be substituted with any one or two of alkyl having 1 to 6 carbon(s), alkoxy having 1 to 6 carbon(s), halogen, trifluoromethyl, nitro and cyano; and R5 is hydrogen or an alkyl group having 1 to 4 carbon(s).Type: GrantFiled: January 23, 2007Date of Patent: August 7, 2012Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Ko Nakamura, Yoshitaka Nakazawa, Minoru Kawamura, Kunihiko Higashiura, Tomoshi Miura
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Patent number: 8227497Abstract: The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: June 22, 2011Date of Patent: July 24, 2012Assignee: Theravance, Inc.Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
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Patent number: 8212076Abstract: Preventing skin aging by targeting multiple causes by a single bullet is of primal scientific and consumer interest.Type: GrantFiled: April 12, 2011Date of Patent: July 3, 2012Assignee: Covalence, Inc.Inventors: Shyam K Gupta, Linda Walker
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Publication number: 20120142746Abstract: The present invention relates to method of lowering intraocular pressure in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising a ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, of enantiomers thereof, of tautomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: September 15, 2011Publication date: June 7, 2012Applicant: ALLERGAN, INC.Inventors: Mohammed I. Dibas, Daniel W. Gil, John E. Donello, Ken Chow, Liming Wang, Michael E. Garst
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Publication number: 20120136036Abstract: The present invention relates to method for treating skin diseases and skin conditions in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, or enantiomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: September 15, 2011Publication date: May 31, 2012Applicant: ALLERGAN, INC.Inventors: Mohammed I. Dibas, Ken Chow, Liming Wang, Michael E. Garst, John E. Donello, Daniel W. Gil
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Publication number: 20120129908Abstract: The invention relates to an agent for the treatment and/or prophylaxis of highly pathogenic infectious diseases, such as highly pathogenic influenza A (in particular, subtypes H5 and H7) and severe acute respirator syndrome caused by the genotype IV coronavirus. The agent is in the form of glutaryl histamine or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition based on glutaryl histamine or a pharmaceutically acceptable salt thereof and to a method for the treatment and/or prophylaxis of highly pathogenic infectious diseases.Type: ApplicationFiled: May 10, 2010Publication date: May 24, 2012Inventors: Vladimir Evgenievich Nebolsin, Galina Alexandrovna Zheltukhina, Sergey Vladimirovich Borisevich, Svetlana Yakovlevna Loginova, Alexander Grigorievich Chuchalin
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Publication number: 20120122792Abstract: S-t-butyl protected cysteine di-peptide analogs and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).Type: ApplicationFiled: November 11, 2011Publication date: May 17, 2012Applicant: PROMENTIS PHARMACEUTICALS, INC.Inventors: Edward M. Johnson, II, Daniel G. Lawton