Additional -c(=x) Bonded Directly To The Five-membered Hetero Ring (e.g., N N-butyryl-l-proline, Etc.) Patents (Class 548/533)
  • Patent number: 9902693
    Abstract: The present invention relates to the field of medical synthesis, in particular to a preparation method for pyrrolidine-2-carboxylic acid derivatives. The present invention adopts the following technical solution: providing a compound having a structure of formula (E), wherein R is R1 or R2, R1 is C1-C6 an alkyl, benzyl, p-methoxybenzyl, or p-nitrobenzyl group, and R2 is hydrogen; R3 is a protecting group of the carboxyl group; and P1 is a protecting group on nitrogen.
    Type: Grant
    Filed: June 23, 2014
    Date of Patent: February 27, 2018
    Assignee: Zhejiang Jiuzhou Pharmaceutical Co., Ltd.
    Inventors: Bin Zhang, Yuanqiang Li, Daqing Che, Lingfeng Qian, Guoliang Zhu, Wenfa Ye
  • Publication number: 20150111859
    Abstract: Provided is a moisturizer having hygroscopicity and water retention ability, and also provided is a composition superior in antiseptic property and feeling on application, in addition to moisturizing property, and free of coloration and odorization. A moisturizer containing acylproline represented by the formula (1) wherein an acyl group represented by R1—CO— is an acyl group derived from a saturated or unsaturated fatty acid having 3-23 carbon atoms, or a salt thereof, and a composition containing (A) acylproline represented by the above formula (1) or a salt thereof and (B) bisphosphonate.
    Type: Application
    Filed: December 29, 2014
    Publication date: April 23, 2015
    Applicant: AJINOMOTO CO., INC.
    Inventors: Takanori SUGIMOTO, Nana HARAYA, Masatoshi SAITO
  • Patent number: 9006249
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: April 14, 2015
    Assignee: Novartis AG
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Publication number: 20150087823
    Abstract: The present invention relates to a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical agent containing the compound as an active ingredient. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt, which is the compound of the present invention, is specifically represented by the general formula (I): wherein X is a substituent such as a 1-pyrrolidyl, a 3-thiazolizyl, or a piperidino, and the compound is highly useful as a pharmaceutical agent, such as a prophylactic or therapeutic agent for a peripheral nerve disorder induced by administration of an anticancer agent, a prophylactic or therapeutic agent for neurodegenerative diseases or mental diseases such as dementia, Alzheimer's disease, Parkinson's disease, diabetic neuropathy, depression, glaucoma, or autistic disorder spectrum, a therapeutic or repairing agent for spinal cord injury, analgesics against various pain diseases, or the like.
    Type: Application
    Filed: April 26, 2013
    Publication date: March 26, 2015
    Inventors: Munekazu Iinuma, Shoei Furukawa, Mitsuru Naiki, Tomonori Matsumoto, Kunihiko Higashiura
  • Publication number: 20150087578
    Abstract: The present invention relates to the use of compounds selected from the group consisting of Lys-(D)Pro-Thr, N-acyl Lys-(D)Pro-Thr, C-amide Lys-(D)Pro-Thr, and C-esters of Lys-(D)Pro-Thr; or a pharmaceutically acceptable salt of said compound for the treatment of inflammatory disorders. The invention also relates to the use of ?MSH for inducing tolerance.
    Type: Application
    Filed: August 25, 2014
    Publication date: March 26, 2015
    Inventor: Thomas LUGER
  • Publication number: 20150064327
    Abstract: A flavour composition comprising a compound of formula (I) corresponding to the formula and edible salts thereof, wherein R1 is an alkyl residue containing 6 to 20 carbon atoms, or an alkene residue containing from 9 to 25 carbon atoms with 1 to 6 double bonds, R1 together with the carbonyl group to which it is attached is a residue of a carboxylic acid.
    Type: Application
    Filed: March 28, 2013
    Publication date: March 5, 2015
    Inventors: Feng Shi, Harry Renes, Esther Van Ommeren, Susanna Magdalena Vorster, Yili Wang, Adri De Klerk
  • Patent number: 8927557
    Abstract: The compounds of Formula (I), wherein R1, R2, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the stereoisomers of the compounds and the salts thereof are effective inhibitors of the type 5 phosphodiesterase.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: January 6, 2015
    Assignee: Takeda GmbH
    Inventors: Josef Stadlwieser, Beate Schmidt, Heiko Bernsmann, Torsten Dunkern, Ewald Benediktus, Andreas Pahl, Ragna Hussong, Olaf Nimz, Matthias Mueller, Martin Viertelhaus
  • Patent number: 8927590
    Abstract: Provided are methods for the preparation of certain substituted pyrrolidine compounds, forms of (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride, and methods for preparing and using these forms.
    Type: Grant
    Filed: August 23, 2012
    Date of Patent: January 6, 2015
    Assignee: Zealand Pharma A/S
    Inventors: Asaf R. Alimardanov, Lalitha Krishnan, Maotang Zhou, Ting-Zhong Wang, Jianxin Ren, John Leo Considine, Charles C. Wu, Jason Brazzillo, Panolil Raveendranath, Karen Sutherland, Mahmoud Mirmehrabi, Subodh S. Deshmukh, Girija Raveendranath, Vijay Raveendranath, Sanjay Raveendranath
  • Publication number: 20140378523
    Abstract: The present invention relates to two novel crystalline forms of zofenopril calcium, to processes for their preparation and their use in pharmaceutical compositions.
    Type: Application
    Filed: September 5, 2014
    Publication date: December 25, 2014
    Inventors: Vinayak Govind GORE, Priyesh VIJAYAKAR, Ashok PEHERE
  • Publication number: 20140378430
    Abstract: The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to pyrrolidine and azetidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
    Type: Application
    Filed: January 4, 2013
    Publication date: December 25, 2014
    Applicant: SPINIFEX PHARMACEUTICALS PTY LTD
    Inventors: Thomas David McCarthy, Alan Naylor
  • Publication number: 20140336376
    Abstract: Provided is a compound represented by the following general formula (I), or a pharmaceutically acceptable salt thereof. This novel compound has a glycogen-synthase activation ability, but activates a receptor PPAR to a low degree and is highly safe. In the formula, Ar is an aromatic carbocyclic ring or a heterocyclic ring; and Ar2 is represented by any one of the following rings and the like.
    Type: Application
    Filed: May 2, 2014
    Publication date: November 13, 2014
    Applicant: Ajinomoto Co., Inc.
    Inventors: Tadakiyo NAKAGAWA, Kayo Matsumoto, Sen Takeshita, Tomomi Yoshida, Munetaka Tokumasu, Hiroki Inoue, Kaori Kobayashi
  • Publication number: 20140309193
    Abstract: There are provided inter alia compounds of formula (I) wherein R1, R2, R3, R4a and R4b are as defined in the specification and their use in therapy, especially in the treatment of bacterial (e.g. pneumococcal) infections.
    Type: Application
    Filed: December 5, 2012
    Publication date: October 16, 2014
    Inventors: Peter William Andrew, Rana Lonnen, Mafalda Pires Damaso, Fritz-Frieder Frickel, Simon Christopher Hirst, Mark William Davies, Daniel Hamza
  • Publication number: 20140309174
    Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.
    Type: Application
    Filed: November 12, 2013
    Publication date: October 16, 2014
    Applicant: Eisai Co., Ltd
    Inventors: James J. Kowalczyk, Galina Kuznetsov, Shawn Schiller, Boris M. Seletsky, Mark Spyvee, Hu Yang
  • Patent number: 8859492
    Abstract: It is an object of the present invention to provide improved pharmacological properties to molecules which bind to a target with low affinity (hereinafter referred to as a “ligand moiety”) through linkage of such molecules to a metal binding moiety, thereby generating a combination molecule commonly referred to as a “metallodrug” or “metallotherapeutic.” The metal binding domain of metallodrugs typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, resulting in modification of proteins and nucleic acids that are in close proximity due to binding of the ligand moiety to its target.
    Type: Grant
    Filed: May 12, 2012
    Date of Patent: October 14, 2014
    Assignee: MetalloPharm, LLC
    Inventors: James A. Cowan, Ada S. Cowan, Donna T. Palmer
  • Patent number: 8853421
    Abstract: The present invention relates to two novel crystalline forms of zofenopril calcium, to processes for their preparation and their use in pharmaceutical compositions.
    Type: Grant
    Filed: December 12, 2012
    Date of Patent: October 7, 2014
    Assignee: Generics [UK] Limited
    Inventors: Vinayak Govind Gore, Priyesh Vijayakar, Ashok Pehere
  • Publication number: 20140288142
    Abstract: The invention relates to nitric oxide donor compounds and their use for treating cardiovascular diseases, inflammation, pain, fever, gastrointestinal disorders, ophthalmic diseases, hepatic disorders, renal diseases, respiratory disorders, immunological diseases, bone metobolisms dysfunctions, central and peripheral nervous system diseases, sexual dysfunctions, infectious diseases, for the inhibition of platelet aggregation and platelet adhesion, for treating pathological conditions resulting from abnormal cell proliferation, vascular diseases. The invention also relates to compositions comprising at least one nitric oxide releasing compounds of the invention and composition comprising at least one nitric oxide releasing compounds according to the invention and at least one 15 therapeutic agent.
    Type: Application
    Filed: June 9, 2014
    Publication date: September 25, 2014
    Inventors: Nicoletta ALMIRANTE, Stefano BIONDI, Ennio ONGINI, Laura STORONI, Alessia NICOTRA
  • Publication number: 20140288144
    Abstract: A compound of formula (I): R?—O-A-O—R??, in which R? and R? are a hydrogen atom or a monovalent radical of formula (IIa), or a monovalent radical of formula (IIb), it being understood that at least one of the radicals R? or R? is not a hydrogen atom and that, when none of the radicals R? and R? is a hydrogen atom, R? and R? are identical, and in which A is a divalent radical of formula (III): —CH(X1)-[C(X2)(X3)]p-CH(X4) in which X1, X2, X3 and X4 are identical or different and are either a hydrogen atom or a methyl radical or an ethyl radical, and p is an integer greater than or equal to 1 and less than or equal to 6. Also the method for preparing the compound of formula (I) and to the use thereof in cosmetics and as a drug.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 25, 2014
    Applicant: Societe D'Exploitation de Produits Pour Les Industries Chimiques Seppic
    Inventors: Sandy Dumont, Jerome Guilbot, Stephanie Garcel, Laetitia Cattuzzato
  • Publication number: 20140275480
    Abstract: The disclosure includes novel processes for producing Sovaprevir comprising adding compound E to F-1 to provide Sovaprevir. The disclosure further includes intermediates useful for producing Sovaprevir. The disclosure also include a novel crystalline form of Sovaprevir, Form F, and a method for preparing spray-dried amorphous Sovaprevir from crystalline Form F.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Achillion Pharmaceuticals, Inc.
    Inventors: Avinash Phadke, Akihiro Hashimoto, Venkat Gadhachanda
  • Publication number: 20140163241
    Abstract: The present invention relates to two novel crystalline forms of zofenopril calcium, to processes for their preparation and their use in pharmaceutical compositions.
    Type: Application
    Filed: December 12, 2012
    Publication date: June 12, 2014
    Applicant: Generics [UK] Limited
    Inventors: Vinayak Gore, Priyesh Vijayakar
  • Publication number: 20140154183
    Abstract: What is described are the compounds and the synthesis of [F-18]-labelled L-glutamic acid, [F-18]-labelled L-glutamate, their derivatives of the formula (I) and their use.
    Type: Application
    Filed: February 5, 2014
    Publication date: June 5, 2014
    Inventors: Matthias FRIEBE, Heribert SCHMITT-WILLICH, Matthias BERNDT, Ludger DINKELBORG, Norman KOGLIN, Keith GRAHAM
  • Publication number: 20140127155
    Abstract: The invention provides small molecule mimics of the Smac peptide that are dimer-like or trimer-like compounds having two or three amide-containing domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.
    Type: Application
    Filed: January 16, 2014
    Publication date: May 8, 2014
    Applicant: JOYANT PHARMACEUTICALS, INC
    Inventors: Gunnar Hanson, Haizho Sun
  • Publication number: 20140121260
    Abstract: The present application discloses conjugates comprising an aminic moiety covalently linked to a hydrophobic moiety, through an amidic bond, which are selective inhibitors of COX-2 enzyme and can be beneficially used in the treatment of various inflammatory disease or disorder and cancer.
    Type: Application
    Filed: January 6, 2014
    Publication date: May 1, 2014
    Applicant: MedWell Laboratories Ltd.
    Inventors: Taher NASSAR, Raiyn Nureldin, Rayan Anwar
  • Patent number: 8710229
    Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
    Type: Grant
    Filed: May 24, 2013
    Date of Patent: April 29, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alan Xiangdong Wang, Li-Qiang Sun, Sing-Yuen Sit, Ny Sin, Paul Michael Scola, Yan Chen
  • Publication number: 20140094615
    Abstract: Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.
    Type: Application
    Filed: April 26, 2012
    Publication date: April 3, 2014
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Martin D. Burke, Junqi Li, Eric P. Gillis
  • Publication number: 20140038903
    Abstract: The present invention relates to compounds of Formula I, II, IA-VA, IVA1-IVA5, IIIA1-IIIA5 and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more cysteine proteases. Also described are methods where the compounds of Formula I, II, IA-VA, IVA1-IVA5, IIIA1-IIIA5 are used in the prevention and/or treatment of various diseases and conditions in subjects, including cysteine protease-mediated diseases and/or caspase-mediated diseases such as sepsis, myocardial infarction, cancer, tissue atrophy, ischemia, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative diseases such as multiple sclerosis (MS), ALS, Alzheimer's disease, Parkinson's disease, and Huntington's disease).
    Type: Application
    Filed: April 15, 2012
    Publication date: February 6, 2014
    Applicant: NEW WORLD LABORATORIES, INC.
    Inventors: Jan-Eric Ahlfors, Khalid Mekouar
  • Publication number: 20130296245
    Abstract: Provided are a compound of formula (I), pharmaceutically acceptable salts thereof, preparation methods and applications thereof for inhibiting thrombin, and applications in the treatment and prevention of thrombin-mediated and thrombin-related diseases.
    Type: Application
    Filed: November 14, 2011
    Publication date: November 7, 2013
    Inventors: Min Li, Hanbin Shan, Yu Huang, Zhedong Yuan, Xiong Yu
  • Publication number: 20130267713
    Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
    Type: Application
    Filed: May 24, 2013
    Publication date: October 10, 2013
    Inventors: ALAN XIANGDONG WANG, LI-QIANG SUN, SING-YUEN SIT, NY SIN, PAUL MICHAEL SCOLA, YAN CHEN
  • Publication number: 20130225644
    Abstract: Lysine mimetic compounds having useful pharmacological activity such as antiarrhythmic activity and desirable bioavailability properties are disclosed.
    Type: Application
    Filed: April 1, 2013
    Publication date: August 29, 2013
    Applicant: Zealand Pharma A/S
    Inventor: Zealand Pharma A/S
  • Publication number: 20130158070
    Abstract: Novel chemical conjugates derived from unsaturated fatty acids and therapeutically active agents, are disclosed. The chemical conjugates are designed and characterized as COX-2 and/or 5-LOX inhibitors and are useful in the treatment of inflammatory diseases and disorders such as Alzheimer's disease, Parkinson's disease, asthma, osteoarthritis, rheumatoid arthritis, pain, primary dysmenorrhea, Crohn's disease and ulcerative colitis.
    Type: Application
    Filed: September 6, 2011
    Publication date: June 20, 2013
    Inventor: Taher Nassar
  • Publication number: 20130072438
    Abstract: Disclosed herein are opioid peptide conjugates (for example, opioid peptide esters). In some embodiments, the disclosed conjugates include an opioid peptide consisting of two to six amino acids and a moiety conjugated to the opioid peptide by an ester bond. In some examples, the moiety is an alcohol, a sugar, a lipid, or dehydroascorbic acid. Also disclosed are methods of altering nociception including administering an effective amount of one or more disclosed opioid peptide conjugates to a subject (such as a human subject).
    Type: Application
    Filed: September 13, 2012
    Publication date: March 21, 2013
    Inventor: Joel S. Goldberg
  • Publication number: 20130053344
    Abstract: Provided are methods for the preparation of certain substituted pyrrolidine compounds, forms of (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride, and methods for preparing and using these forms.
    Type: Application
    Filed: August 23, 2012
    Publication date: February 28, 2013
    Applicant: Zealand Pharma A/S
    Inventors: Asaf R. Alimardanov, Lalitha Krishnan, Maotang Zhou, Ting-Zhong Wang, Jianxin Ren, John Leo Considine, Charles C. Wu, Jason Brazzillo, Girija Raveendranath, Vijay Raveendranath, Sanjay Raveendranath, Karen Sutherland, Mahmoud Mirmehrabi, Subodh S. Deshmukh
  • Publication number: 20130023539
    Abstract: The present invention is directed to novel compounds of formula (I) and their use in treating and/or preventing metabolic diseases.
    Type: Application
    Filed: June 18, 2012
    Publication date: January 24, 2013
    Applicant: Euroscreen S.A.
    Inventors: Hamid R. Hoveyda, Didier Schils, Ludivine Zoute, Julien Parcq
  • Publication number: 20120330019
    Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
    Type: Application
    Filed: August 29, 2012
    Publication date: December 27, 2012
    Inventors: Xiangdong Alan Wang, Li-Qiang Sun, Sing-Yuen Sit, Ny Sin, Paul Michael Scola, Piyasena Hewawasam, Andrew Charles Good, Yan Chen, Jeffrey Allen Campbell
  • Publication number: 20120289454
    Abstract: It is an object of the present invention to provide improved pharmacological properties to molecules which bind to a target with low affinity (hereinafter referred to as a “ligand moiety”) through linkage of such molecules to a metal binding moiety, thereby generating a combination molecule commonly referred to as a “metallodrug” or “metallotherapeutic.” The metal binding domain of metallodrugs typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, resulting in modification of proteins and nucleic acids that are in close proximity due to binding of the ligand moiety to its target.
    Type: Application
    Filed: May 12, 2012
    Publication date: November 15, 2012
    Applicant: METALLOPHARM LLC
    Inventors: James A. Cowan, Ada S. Cowan, Donna T. Palmer
  • Patent number: 8293943
    Abstract: Preventing skin aging by targeting multiple causes by a single bullet is of primal scientific and consumer interest.
    Type: Grant
    Filed: February 18, 2012
    Date of Patent: October 23, 2012
    Assignee: Island Kinetics, Inc.
    Inventors: Shyam K Gupta, Linda Walker
  • Publication number: 20120258929
    Abstract: The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect peptidyl-dipeptidase A; a method for assaying pesticidal activity of a test substance, which comprises a step of measuring the activity of a peptidyl-dipeptidase A in a reaction system in which the peptidyl-dipeptidase A contacts with a test substance, and the like.
    Type: Application
    Filed: June 23, 2006
    Publication date: October 11, 2012
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Yasutaka Shimokawatoko, Marc Van De Craen, Irene Nooren, Sandra Turconi, Yann Naudet, Guy Nys, Jurgen Debaveye
  • Publication number: 20120252830
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: June 7, 2012
    Publication date: October 4, 2012
    Applicant: NOVARTIS AG
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Patent number: 8258343
    Abstract: Preventing skin aging by targeting multiple causes by a single bullet is of primal scientific and consumer interest.
    Type: Grant
    Filed: February 15, 2012
    Date of Patent: September 4, 2012
    Assignee: Island Kinetics, Inc.
    Inventors: Shyam K Gupta, Linda Walker
  • Publication number: 20120213702
    Abstract: The present invention relates to aminopeptidase N (APN) inhibitor conjugates of formula I wherein W is a —CO— or an —SO2— group and at least one of R1 or R2 represents (OCH2—CH2)n-X, where n is an integer of 1 to 100 and X represents H or a detectable label or a therapeutic, and the other represents an alkoxy group or OH, and wherein R3, R3? and R3? is independently selected from an alkoxy group or (OCH2—CH2)n-X, where n is an integer of 1 to 100 and X represents H or a detectable label or a therapeutic, and R4 is selected from the group comprising: wherein R is an alkyl group. Furthermore, the present invention relates to a diagnostic and/or pharmaceutical composition comprising the conjugate of the invention.
    Type: Application
    Filed: August 31, 2010
    Publication date: August 23, 2012
    Inventors: Christoph Bremer, Carsten Höltke
  • Patent number: 8212076
    Abstract: Preventing skin aging by targeting multiple causes by a single bullet is of primal scientific and consumer interest.
    Type: Grant
    Filed: April 12, 2011
    Date of Patent: July 3, 2012
    Assignee: Covalence, Inc.
    Inventors: Shyam K Gupta, Linda Walker
  • Publication number: 20120148952
    Abstract: A radiation-sensitive resin composition includes a compound, a resin and a radiation-sensitive acid generator. The compound has a structure in which a group represented by a following formula (1) is bound to a nitrogen atom. The resin has an acid-dissociative dissolution-controlling group and has a property such that alkali solubility of the resin increases by an action of an acid. In the formula (1), Y is a monovalent group having 5 to 20 carbon atoms, and “*” represents a bonding hand with the nitrogen atom. In the formula (i), R1, R2 and R3 each independently represent a linear or branched alkyl group having 1 to 4 carbon atoms or a monovalent alicyclic hydrocarbon group having 4 to 12 carbon atoms, or R1 and R2 are linked with each other to form a bivalent alicyclic hydrocarbon group, and “*” represents a bonding hand with the oxygen atom.
    Type: Application
    Filed: January 17, 2012
    Publication date: June 14, 2012
    Applicant: JSR Corporation
    Inventors: Kazuo NAKAHARA, Mitsuo SATO
  • Publication number: 20120129818
    Abstract: Ortho methoxy phenolic compounds are provided that include methylenedioxyphenyl ferulate and ferulylproline and derivatives thereof. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating cardiovascular diseases, including hypertension, atherosclerosis, coronary heart disease, angina, stroke, and myocardial infarction, are further provided. The compounds are also useful in reducing low-density lipoprotein oxidation, improving or increasing vasodilation, and reducing plaque destabilization in a subject.
    Type: Application
    Filed: April 23, 2010
    Publication date: May 24, 2012
    Inventor: Desikan Rajagopal
  • Publication number: 20120122764
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, B, X, m and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of compounds of the invention, and a combination of pharmacologically active agents and a compound of the invention.
    Type: Application
    Filed: November 10, 2011
    Publication date: May 17, 2012
    Applicant: NOVARTIS AG
    Inventors: Rajeshri Ganesh KARKI, Toshio KAWANAMI, Gary Michael KSANDER, Qian LIU, Muneto MOGI, Nikolaus SCHIERING, Robert SUN
  • Publication number: 20120088919
    Abstract: The invention relates to compounds having the formula: wherein: Ar, r, R3, Z, X, 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. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 19, 2011
    Publication date: April 12, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Seok-Ki CHOI, Paul R. FATHEREE, Roland GENDRON, Ryan HUDSON, Robert Murray MCKINNELL, Vivek SASIKUMAR
  • Publication number: 20120077752
    Abstract: The present invention provides a composition which may be ingested orally in a small dose for the purpose of improving brain function, and a method for improving brain function. The present invention is a composition for improving brain function, comprising, as an active ingredient, Phe-Pro.
    Type: Application
    Filed: September 15, 2011
    Publication date: March 29, 2012
    Inventors: Kazuhito OHSAWA, Naoto Uchida, Kohji Ohki
  • Patent number: 8119817
    Abstract: A process for separating the diastereomers of RSS— and SSS—N-?[1-carboxy-3-phenylpropyl]lysylproline is described. Previous chromatographic processes for separating the diastereomers of this peptide active substance, such as for example adsorption chromatography, exhibited disadvantages with regard to the solvents used and throughput. These disadvantages do not occur if basic ion exchangers are used in the chromatographic separation of the diastereomers. In particular, purely aqueous solutions may be used as the eluent.
    Type: Grant
    Filed: August 3, 1999
    Date of Patent: February 21, 2012
    Assignee: Degussa-Huels AG
    Inventors: Frédéric Boisivon, Jean Debas, Gérard Richet
  • Publication number: 20120041025
    Abstract: Compounds are provided that comprise dinitroso-derivatives of dihydrolipoic acid. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating various diseases and disorders, including angina, hypertension, diabetes, dyslipidemia, renal insufficiency, myocardial infarction, stroke, atherosclerosis, and the target organ damage that accompanies these various diseases and disorders, are further provided. The compounds are useful in improving vasodilation, reducing low-density lipoprotein oxidation, and reducing inflammation in a subject.
    Type: Application
    Filed: February 19, 2010
    Publication date: February 16, 2012
    Inventor: Sampath Parthasarathy
  • Patent number: 8106191
    Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula M-L-Q where M is a synthetic ligand for an FKBP protein.
    Type: Grant
    Filed: June 13, 2003
    Date of Patent: January 31, 2012
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Dennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
  • Patent number: 8084622
    Abstract: An industrially advantageous process for the production of (3R,4S)-3-cyclopropylaminomethyl-4-fluoropyrrolidine or an enantiomer thereof that is useful as an intermediate for the production of novel antimicrobial agents 10-(3-cyclopropylaminomethyl-4-fluoropyrrolidinyl)pyridobenzoxazine carboxylic acid derivatives. Highly stereoselective asymmetric hydrogenation of 1-protected-4-alkoxycarbonyl-3-oxopyrrolidine, followed by ester hydrolysis, followed by amidation with cyclopropylamine gives crude crystals. The crude crystals are purified by recrystallization to give a novel compound (3R,4S)-1-protected-3-cyclopropylcarbamoyl-4-hydroxypyrrolidine or an enantiomer thereof at high optical purity. The use of these intermediates enables industrial production of high-quality products of (3R,4S)-3-cyclopropylaminomethyl-4-fluoropyrrolidine or an enantiomer thereof. The process is highly simple and can produce the desired products at high purity and stable yields.
    Type: Grant
    Filed: November 6, 2009
    Date of Patent: December 27, 2011
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Takayuki Gotoh, Ichirou Araya
  • Publication number: 20110306761
    Abstract: The present invention relates to a process for preparing a porphyrin of formula (I), optionally in the form of a salt with an alkali metal and/or in the form of a metal complex: in which: R and R? are as defined in claim 1, comprising: a step of condensation, in an acidic medium, between a dipyrromethane of formula (II): in which R?b is as defined above for (I), and a dipyrromethane of formula (III): in which R? is as defined in claim 1, and also the compounds of formula (III).
    Type: Application
    Filed: August 25, 2011
    Publication date: December 15, 2011
    Applicant: SANOFI PASTEUR SA
    Inventors: Pierre Martin, Markus Mueller, Dirk Spielvogel, Dietmar Flubacher, Andreas Boudier