Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Piperidine Ring Patents (Class 546/245)
  • Publication number: 20110262872
    Abstract: There are provided a method of forming a resist pattern in which a resist pattern is formed on top of a substrate by using a chemically amplified resist composition and conducting patterning two or more times, the method being capable of reducing the extent of damage, caused by the second patterning, imposed upon the first resist pattern that is formed by the first patterning; as well as a resist composition that is useful for forming the first resist pattern in this method of forming a resist pattern. The method includes forming of a first resist pattern using a resist composition containing a thermal base generator as a chemically amplified resist composition during first patterning, and then conducting a hard bake for baking the first resist pattern under a bake condition such that a base is generated from the thermal base generator, prior to the second patterning.
    Type: Application
    Filed: March 28, 2011
    Publication date: October 27, 2011
    Applicant: TOKYO OHKA KOGYO CO., LTD.
    Inventors: Jiro YOKOYA, Tsuyoshi NAKAMURA, Masaru TAKESHITA, Yasuhiro YOSHII, Hirokuni SAITO
  • Publication number: 20110257130
    Abstract: Compounds are provided which can be useful in reducing the activity of an angiotensin-converting enzyme and thus be used to treat or prevent a renin-angiotensin aldosterone system-related disorder. These compounds include lipoic acid derivatives such as prolyl lipoic acid and pipecolinyl lipoic acid, and other compounds, and these compounds are useful in treating hypertension, stroke, or other renin-angiotensin aldosterone system-related disorders in human or animal patients. Pharmaceutical compositions prepared using these compounds and methods of treatment using these compounds are also provided.
    Type: Application
    Filed: October 16, 2009
    Publication date: October 20, 2011
    Inventor: Desikan Rajagopal
  • Publication number: 20110257398
    Abstract: Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3. In embodiments, compositions are capable of activation of procaspase-3.
    Type: Application
    Filed: April 15, 2011
    Publication date: October 20, 2011
    Applicant: The Board of Trustees of The University of Illinois
    Inventors: Paul J. HERGENROTHER, Karson S. PUTT, Quinn P. PETERSON, Valerie FAKO
  • Publication number: 20110257226
    Abstract: There is provided a halogen-containing organosulfur compound having a controlling effect on arthropod pests represented by the formula (I): wherein m represents 0, 1 or 2; n represents 0, 1 or 2; A represents an optionally substituted 3- to 8-membered saturated heterocyclic group; Q represents a fluorine atom or a C1-C5 haloalkyl group having at least one fluorine atom; R1, R1a and R3 independently represent an optionally halogenated C1-C4 chain hydrocarbon group, etc.; R2, R2a and R4 independently represent an optionally halogenated C1-C4 chain hydrocarbon group, etc.
    Type: Application
    Filed: December 24, 2009
    Publication date: October 20, 2011
    Inventor: Hiromasa Mitsudera
  • Patent number: 8017771
    Abstract: Disclosed are highly convergent processes for preparing compounds of formula (I), which compounds are potent active agents for the treatment of hepatitis C virus (HCV) infection: The disclosed processes use SNAr-type coupling reactions between peptidic compounds having a hydroxyproline moiety of the following formula: and halogenated or sulfonated bromoquinoline compounds.
    Type: Grant
    Filed: January 16, 2009
    Date of Patent: September 13, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Carl Alan Busacca, Rogelio Perez Frutos, Nizar Haddad, Suresh R. Kapadia, Jon Charles Lorenz, Anjan Saha, Chris Hugh Senanayake, Xudong Wei
  • Publication number: 20110212080
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.
    Type: Application
    Filed: July 28, 2009
    Publication date: September 1, 2011
    Inventors: Umar Faruk Mansoor, Panduranga Adulla Reddy, M. Arshad Siddiqui
  • Publication number: 20110207775
    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 vesicle-fusing ATPase; a method for assaying pesticidal activity of a test substance, which comprises measuring the activity of a vesicle-fusing ATPase in a reaction system in which the vesicle-fusing ATPase contacts with a test substance, and the like.
    Type: Application
    Filed: November 19, 2007
    Publication date: August 25, 2011
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Yasutaka Shimokawatoko, Marc Van De Craen, Irene Nooren, Bert Oosthuyse, Bert Demey, Wendy Maddelein, Geraldine Drevon
  • Publication number: 20110166354
    Abstract: The present application relates to a method for producing an optically active ?-amino acid derivative, comprising steps of reacting an ?-haloester derivative represented by the general formula (1): of which alcohol part of the ester group is an optically active alcohol derivative, with an amine compound; then deprotecting the obtained compound; further carrying out an ester exchange reaction. According to the present invention method, it is possible to easily produce an optically active ?-amino acid ester derivative which is useful as an intermediate for drugs with high selectivity.
    Type: Application
    Filed: June 2, 2009
    Publication date: July 7, 2011
    Inventors: Shohei Yamamoto, Akio Fujii, Masaru Mitsuda
  • Publication number: 20110160244
    Abstract: The present invention relates to new phenylpiperidine modulators of ?-opioid receptors, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: September 16, 2009
    Publication date: June 30, 2011
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Manoucherhr M. Shahbaz
  • Publication number: 20110152464
    Abstract: The present invention relates to a pipecolic linker and its use as a solid-phase linker in organic synthesis. Said pipecolic solid-phase linker may be used for coupling functional groups chosen between primary amines, secondary amines, aromatic amines, alcohols, phenols and thiols. In particular, said pipecolic solid-phase linker may be used for peptide or pseudopeptide synthesis, such as the reverse N to C peptide synthesis or the retro-inverso peptide synthesis, or for the synthesis of small organic molecules.
    Type: Application
    Filed: August 28, 2009
    Publication date: June 23, 2011
    Applicant: UNIVERSITE DE MONTPELLIER I
    Inventors: Jean Martinez, Pawel Zajdel, Maciej Pawlowski, Gilles Subra
  • Publication number: 20110137036
    Abstract: The present invention relates to the stereoselective synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine, as well as the conversion thereof, to give Moxifloxacin. Particularly, the present invention relates to a method for the synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) comprising: (a) the optical resolution by enzymatic hydrolysis of the intermediate dialkyl-1-alkylcarbonylpiperidine-2,3-dicarboxylate racemate of formula (II) to give, following isolation, the intermediate dialkyl-(2S,3R)-1-alkylcarbonyl-piperidine-2,3-dicarboxylate of formula (III) in which AIk is a straight or branched C1-C5 alkyl group; (b) the conversion of the intermediate (III) to (4aR,7aS)-1-alkylcarbonylhexahydrofuro[3,4-b]pyridine-5,7-dione of formula (IV) in which AIk has the meanings set forth above; (c) the conversion of the intermediate (IV) to (4aS,7as)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) with an optical purity above 99%.
    Type: Application
    Filed: March 4, 2010
    Publication date: June 9, 2011
    Inventors: Riccardo Motterle, Giancarlo Arvotti, Elisabetta Bergantino, Andrea Castellin, Stefano Fogal, Marco Galvagni
  • Patent number: 7947834
    Abstract: The present invention is related to a compound of formula (I): wherein i, j, n, o, p, q, r, R1a, R1b, R1c, R1d, R2a, R2b, R2c, R2d, R3a, R3b and R4 are as defined herein, or an addition salt with an acid thereof, or a hydrate or solvate thereof, its preparation, pharmaceutical composition, and uses for treating a disease in which the enzyme 11?-HSD1 is involved.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: May 24, 2011
    Assignee: Sanofi-Aventis
    Inventors: Alain Braun, Patrick Mougenot, Claudie Namane, Eric Nicolai, Francois Pacquet, Christophe Philippo, Olivier Venier, Olivier Crespin, Cecile Pascal, Michel Aletru, Stefan Gussregen
  • Patent number: 7943768
    Abstract: A compound of formula (I) P—W—C(?X)-L-Q??(I) wherein P is an optionally substituted aryl or heteroaryl group; W is an optionally substituted 6 or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 independently selected from Oxygen and Nitrogen, X is selected from Oxygen, Nitrogen and Sulphur; L is an optional C1-4 linker; and Q is an optionally substituted 4-7 membered aliphatic ring: for use in the treatment of chemokine mediated diseases or disorders.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: May 17, 2011
    Assignee: AstraZeneca AB
    Inventors: Justin Fairfield Bower, Peter Wedderburn Kenny, Jeffrey Philip Poyser
  • Patent number: 7939531
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: May 10, 2011
    Assignee: Roche Palo Alto
    Inventors: Joe Timothy Bamberg, Mark Bartlett, Daisy Joe DuBois, Todd Richard Elworthy, Robert Than Hendricks, Johannes Cornelius Hermann, Rama K. Kondru, Remy Lemoine, Yan Lou, Timothy D. Owens, Jaehyeon Park, David Bernard Smith, Michael Soth, Hanbiao Yang, Calvin Wesley Yee
  • Publication number: 20110105503
    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: Application
    Filed: June 20, 2008
    Publication date: May 5, 2011
    Applicants: NHWA PHARMA. CORPORATION, SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY
    Inventors: Jianqi Li, Guan Wang, Guisen Zhang, Yanqin Ma, Wenhua Ji, Yuan Zhang, Lin Guo
  • Publication number: 20110098319
    Abstract: The invention relates to novel derivatives of short-chain fatty acids, in particular derivatives of butyric acid, useful for all the known clinical applications of the latter, which show physicochemical characteristics suitable for an easy oral administration, being devoid of the unpleasant organoleptic properties that characterize butyrate. The new compounds are amide derivatives which can be synthesized by reaction of the corresponding fatty acid halide with a naturally occurring amino acid, phenylalanine or a suitable derivative thereof, and which are in a poorly hygroscopic, easily weighable form, stable to acids and alkalis and able to release the acid at the small and large bowel level in a constant manner over time. They do not have disagreeable odors and are practically tasteless, thus allowing the manufacture of preparations for oral administration also suitable for the therapy of chronic diseases and in the pediatric field.
    Type: Application
    Filed: April 21, 2009
    Publication date: April 28, 2011
    Inventors: Roberto Berni Canani, Antonio Calignano, Orietta Mazzoni, Anna Coruzzo
  • Patent number: 7932254
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q1 and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: April 26, 2011
    Assignee: Roche Palo Alto
    Inventors: Daisy Joe DuBois, Robert Than Hendricks, Johannes Cornelius Hermann, Rama K. Kondru, Yan Lou, Timothy D. Owens, Calvin Wesley Yee
  • Publication number: 20110053901
    Abstract: Among other things, the present invention provides novel compounds capable of effectively inhibiting inflammatory responses that are mediated by G-proteins or GPCRs in neutrophils, macrophages and platelets. In particular, compounds of the present invention act as inhibitors of edema, inhibitors of erythema and inhibitors of MPO (myeloperoxidase), pharmaceutical compositions containing the same compounds and the use thereof for the treatment of diseases that may benefit from edema, erythema and MPO inhibition, such as inflammation (acute or chronic), asthma, autoimmune diseases, and chronic obstructive pulmonary disease (COPD) (e.g., emphysema, chronic bronchitis and small airways disease, etc.), inflammatory responses of the immune system, skin diseases (e.g., reducing acute skin irritation for patients suffering from rosacea, atopic dermatitis, seborrheic dermatitis, psoriasis), irritable bowel syndrome (e.g., Chron's disease and ulcerative colitis, etc.), and central nervous system disorders (e.g.
    Type: Application
    Filed: February 13, 2009
    Publication date: March 3, 2011
    Applicants: SIGNUM BIOSCIENCES, INC., Signum Biosciences, Inc.
    Inventors: Seung-Yub Lee, Michael Voronkov, Peter Wolanin
  • Publication number: 20110046179
    Abstract: This invention relates to novel piperidine derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: August 29, 2007
    Publication date: February 24, 2011
    Inventors: Birgitte L. Eriksen, Dan Peters, Bjarne H. Dahl, Elsebet Østergaard Nielsen, John Paul Redrobe
  • Patent number: 7888351
    Abstract: The present invention relates to compounds of the formula; and their use in therapy.
    Type: Grant
    Filed: April 10, 2007
    Date of Patent: February 15, 2011
    Assignee: Novartis AG
    Inventors: Daniel Kaspar Baeschlin, Garry Fenton, Kenji Namoto, Nils Ostermann, Richard Sedrani, Finton Sirockin
  • Publication number: 20110034510
    Abstract: The invention relates to an insect- and mite-repelling agent, characterized by a content of at least one substituted, enantiomer-enriched ?-,?-amino alcohol derivative of formula (1) wherein X represents hydrogen, COR11 or R13, R13 represents C1-C6 alkyl, R1 represents C1-C7 alkyl, C3-C7alkenyl or C2-C7 alkinyl, R2 R11, R13 are identical or different and represent C1-C6 alkyl or C2-C7 alkenyl, R3-R8 are identical or different and represent hydrogen or C1-C6 alkyl, wherein R2 and R3 or R3 and R7 or R3 and R5 or R5 and R7 can also form, together with the atoms to which they are bonded, a 5- or 6-membered monocycle ring. Also disclosed is a method for producing said agent.
    Type: Application
    Filed: October 18, 2007
    Publication date: February 10, 2011
    Applicant: SALTIGO GMBH
    Inventors: Thomas Gernot, Nikolaus Mueller, Andreas Job, Bernd-Wieland Kruger, Gunther Nentwig
  • Publication number: 20110027718
    Abstract: A radiation-sensitive resin composition includes a compound shown by a formula (1) in which R1 represents a divalent hydrocarbon group having 1 to 20 carbon atoms and R2 represents a hydrogen atom or a monovalent hydrocarbon group having 1 to 20 carbon atoms, or R1 and R2 form a heterocyclic structure having 4 to 20 carbon atoms, R3 represents a monovalent acid-dissociable group, n is an integer from 1 to 6, each of R4A, R4B, and R4C represents one of an alkyl group having 1 to 4 carbon atoms and a monovalent alicyclic hydrocarbon group having 4 to 20 carbon atoms, or R4A represents one of an alkyl group having 1 to 4 carbon atoms and a monovalent alicyclic hydrocarbon group having 4 to 20 carbon atoms and R4B and R4C form a divalent alicyclic hydrocarbon group having 4 to 20 carbon atoms.
    Type: Application
    Filed: July 30, 2010
    Publication date: February 3, 2011
    Applicant: JSR Corporation
    Inventors: Mitsuo SATO, Kazuo NAKAHARA, Hiromitsu NAKASHIMA, Takanori NAKANO, Makoto SUGIURA
  • Publication number: 20110021358
    Abstract: Methods and compositions for controlling plant pests, particularly weeds and/or plant phytopathogens using sarmentine and/or analogs thereof are disclosed.
    Type: Application
    Filed: July 20, 2010
    Publication date: January 27, 2011
    Applicant: Marrone Bio Innovations, Inc.
    Inventors: Huazhang Huang, Ratnakar Asolkar
  • Publication number: 20110003852
    Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
    Type: Application
    Filed: February 18, 2008
    Publication date: January 6, 2011
    Inventor: Soren Ebdrup
  • Publication number: 20100292439
    Abstract: A subject of the invention is the use of a salt with a dedicated task of formula (I): A+-L-R—OY, X? as soluble support for peptide synthesis, in which: X? represents a functional or non-functional anion, Y represents either a hydrogen atom, or a —COOR1 group, R1 representing in particular an alkyl group comprising 1 to 20 carbon atoms, A+ represents a cationic entity, L represents an arm, in particular an alkyl group of 3 to 20 carbon atoms, R represents in particular a group of formula —C(Ra)(Rb)—, Ra and Rb representing independently of one another in particular a hydrogen or an alkyl group, comprising 1 to 20 carbon atoms.
    Type: Application
    Filed: July 5, 2006
    Publication date: November 18, 2010
    Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE`, UNIVERSITE DE RENNES
    Inventors: Michel Vaultier, Céline Roche, Saïd Gmouh, Alain Commercon
  • Publication number: 20100280034
    Abstract: The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;
    Type: Application
    Filed: December 28, 2007
    Publication date: November 4, 2010
    Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
  • Publication number: 20100280005
    Abstract: Disclosed are compounds of Formula I, wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
    Type: Application
    Filed: April 4, 2008
    Publication date: November 4, 2010
    Inventors: Jonh J. Baldwin, Salvacion Cacatian, David Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Bahman Ghavimi-Alagha, John Gleason, Alexey V. Ishchenko, Brian Lawhorn, Gerard McGeehan, Jaclyn R. Patterson, Simon F. Semus, Robert D. Simpson, Suresh B. Singh, Colin Tice, Tritin Tran, Zhenrong Xu, Jing Yuan, Wei Zhao
  • Publication number: 20100266717
    Abstract: Compositions and methods for controlling molluscs, members of the Gastropoda and Bivalvia classes which includes but is not limited to lactones, lactams, carbamates, amides, and/or carboxylic acid containing compounds as active ingredients and/or compounds derived from Pseudomonas and/or Erwinia. Also provided are methods and compositions for increasing the efficacy of chemical and biological control for invasive molluscs in open waters, power plants, and drinking water treatment facilities under coldwater conditions.
    Type: Application
    Filed: April 20, 2010
    Publication date: October 21, 2010
    Applicant: Marrone Bio Innovations, Inc.
    Inventors: Ratnakar Asolkar, Sarahann Dow, Huazhang Huang, Marja Koivunen, Pamela Marrone, Stephanie Shu
  • Publication number: 20100249101
    Abstract: The present invention relates to compounds of formula I, The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
    Type: Application
    Filed: January 7, 2010
    Publication date: September 30, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Henning STEINHAGEN, Hauke SZILLAT, Markus FOLLMANN, Reinhard KIRSCH, Volkmar WEHNER, Hans MATTER, Martin LORENZ, Kent W. Neuenschwander, Anthony C. SCOTESE
  • Publication number: 20100234392
    Abstract: [Problems] To provide compounds useful as preventives or remedies for circulatory diseases, nervous diseases, metabolic diseases, reproductive system diseases, and digestive diseases. [Means for Solving Problems] Compounds represented by the general formula (I) or pharmaceutically acceptable salts thereof: wherein R1 is C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 is phenyl, heteroaryl, or the like; Q is N or CH; and M1, M2, M3 and M4 are each independently hydrogen or C1-6 alkyl, or alternatively M1 together with M2 or M3 forms —CH2-CH2- or the like, or M4 together with M2 or M3 forms —CH2-CH2- or the like, with the proviso that M1, M2, M3, and M4 are such that one —CH2- or —CH2-CH2- group is formed thereamong.
    Type: Application
    Filed: September 12, 2008
    Publication date: September 16, 2010
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • Publication number: 20100234427
    Abstract: This invention relates to novel 1-phenethylpiperidine derivatives useful as opioid receptor ligands. More specifically, the invention provides compounds useful as ? opioid receptor ligands. In other aspects the invention relates to the use of these compounds in a method for therapy, such as for the treatment of pain, and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: February 13, 2007
    Publication date: September 16, 2010
    Inventors: Dan Peters, Birgitte L. Eriksen, Gordon Munro, Elsebet Østergaard Nielsen, John Paul Redrobe
  • Patent number: 7781437
    Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.
    Type: Grant
    Filed: October 10, 2006
    Date of Patent: August 24, 2010
    Assignee: Schering Corporation
    Inventors: Seong Heon Kim, Bandarpalle B. Shankar, Joseph A. Kozlowski, Stuart B. Rosenblum, Neng-Yang Shih
  • Publication number: 20100210620
    Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
    Type: Application
    Filed: September 30, 2008
    Publication date: August 19, 2010
    Inventors: Prasun K. Chakravarty, Yanbing Ding, Joseph L. Duffy, Hassan Pajouhesh, Pengeheng Patrick Shao, Sriram Tyagarajan, Feng Ye
  • Publication number: 20100210618
    Abstract: The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —O—C(?O)—; —C(?O)—C(?O)—; —NRX—C(?O)—; —Z—C(?O)—; —Z—NRX—C(?O)—; —C(?O)—Z—; —NRX—C(?O)—Z—; —C(?S)—; —NRX—C(?S)—; —Z—C(?S)—; —Z—NRX—C(?S)—; —C(?S)—Z—; —NRX—C(?S)—Z—; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents —C(?O)—NRX— or —NRX—C(?O)—; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein sai
    Type: Application
    Filed: June 6, 2008
    Publication date: August 19, 2010
    Inventors: Jean-Pierre Andre Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Mieerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J.M. De Waepenaret, Peter Walter Maria Roevens, Petr Vladimirivich Davidenko
  • Patent number: 7776884
    Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis, asthma, restinosis, organ transplantation, and cancer.
    Type: Grant
    Filed: February 10, 2006
    Date of Patent: August 17, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventor: Robert J. Cherney
  • Publication number: 20100204275
    Abstract: This invention relates to novel N-piperidin-4-ylmethyl amide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy, and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: July 31, 2008
    Publication date: August 12, 2010
    Applicant: NeuroSearch A/S
    Inventors: Dan Peters, Birgitte L. Eriksen, John Paul Redrobe, Gordon Munro, Elsebet Østergaard Nielsen
  • Publication number: 20100190789
    Abstract: The invention relates to a DGAT inhibitor of formula (I): including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —C(?O)—; —O—C(?O)—; C(?O)—C(?O)—; —NRx—C(?O)—; —Z1—C(O)—; —Z1—NRx—C(?O)—; —C(?O)—Z1—; —NRx—C(?O)—Z1—; —S(?O)p-; —C(?S)—; —NRx—C(?S)—; —Z1—C(?S)—; —Z1—NRx—C(?S)—; —C(?S)—Z1-; NRx—C(?S)—Z—; Y represents NRx—C(=0)-Z2—; —NRx—C(=0)-Z2—NRy—; —NRx—C(=0)-Z 2—NRy—C(=0)—; —NRx—C(=0)-Z2—NRy—C(=0)-; O—; —NRx—C(=0)-Z2-0-; —NRx—C(=0)-Z2-0-C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-0-; —NRx—C(?O)—O—Z2—O—C(?O)—; —NRx—C(?O)—Z2—C(?O)—NRy—; —NRx—C(?O)—Z2—NRy—C(=0)-NRy—; —C(?O)—Z2—; —C(?O)—Z2—O—; —C(=0)-NRx—Z2—; —C(=0)-NRx—Z2-0-; —C(=0)-NRx—Z2—C(=0)-0-; —C(=0)-NRx—Z2-0-C(=0)-; —C(=0)-NRx—Z2—NRy—; —C(=0)—NRx—Z2—NRy—C(=0)-; —C(=0)-NRx—Z2—NRy—C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkyl
    Type: Application
    Filed: June 6, 2008
    Publication date: July 29, 2010
    Inventors: Jean-Pierre Andre Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Meerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J.M De Waepenaert, Peter Walter Maria Roevens, Gustaaf Maria Boeckx, Peter Vladimirivich Davidenko
  • Publication number: 20100168421
    Abstract: The present invention relates to the novel antibacterial compounds having potent antibacterial activity as inhibitors of peptide deformylase. This invention further relates to pharmaceutically acceptable salts thereof, to processes for their preparation, and to pharmaceutical compositions containing them as an active ingredient.
    Type: Application
    Filed: June 4, 2008
    Publication date: July 1, 2010
    Applicant: ILDONG PHARMACEUTICAL CO., LTD.
    Inventors: Jae Hoon KANG, Seung Woo YU, Hee Yeol LEE, Kyung Mi AN, Bong Hwan CHO
  • Publication number: 20100168083
    Abstract: Novel substituted adamantane based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
    Type: Application
    Filed: March 20, 2007
    Publication date: July 1, 2010
    Inventor: Soren Ebdrup
  • Patent number: 7745464
    Abstract: The present invention relates to heterocyclic compounds that bind to Bcl proteins and inhibit Bcl function, compositions comprising such compounds, and methods for treating and modulating disorders associated with hyperproliferation, such as cancer.
    Type: Grant
    Filed: December 15, 2006
    Date of Patent: June 29, 2010
    Inventors: Alfredo C. Castro, Michael J. Grogan, Edward B. Holson, Brian T. Hopkins, Nii O. Koney, Stephane Peluso, Daniel A. Snyder
  • Publication number: 20100158996
    Abstract: A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1?) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R9 and R9 are each independently hydrogen atom, C1-C6 alkyl, —CON(R18) (R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.
    Type: Application
    Filed: February 12, 2010
    Publication date: June 24, 2010
    Inventors: Atsushi Hagiwara, Yasuhiro Ohe, Naoya Odani, Shizue Watanabe, Taku Ikenogami, Takashi Kawai, Kenya Madono, Toshio Taniguchi
  • Publication number: 20100160285
    Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Application
    Filed: December 18, 2009
    Publication date: June 24, 2010
    Inventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
  • Publication number: 20100151388
    Abstract: A (meth)acrylate compound having a nitrogen-containing cyclic group, a photosensitive polymer, and a resist composition including the same, the (meth)acrylate compound being represented by the following Chemical Formula 1:
    Type: Application
    Filed: December 11, 2009
    Publication date: June 17, 2010
    Inventors: Young-Soo Yang, Seung-Jib Choi, Jun-Sunk Kim, Sang-Jun Choi
  • Patent number: 7723307
    Abstract: Novel Amino Acid Derivatives and Pharmaceutical Uses Thereof Provided are novel compounds of Formula I: wherein ‘X’ represents an amino acid group, ‘n’ is an integer between 1 and 4, ‘R1’ represents benzyl, t-butyl or 9-fluorenylmethyl and ‘R2’ represents a tetramethylmercaptoimidazole derivative or —S+R3R4, wherein R3 and R4 each independently represent lower alkyl, or a pharmaceutically and/or veterinarily acceptable derivative thereof. Further provided are pharmaceutical formulations of the compounds and the use thereof in the preparation of a medicament for inhibiting diseases in which transglutaminase has been implicated. Advantageously, the medicament is for treating fibrosis, scarring and/or cancer. Additionally provided are methods, of inhibiting autoimmune diseases such as coeliac disease, neurodegeneration and chronic inflammatory diseases (e.g.
    Type: Grant
    Filed: June 16, 2004
    Date of Patent: May 25, 2010
    Assignee: Aston University
    Inventors: Martin Griffin, Ian G. Coutts, Robert E. Saint
  • Publication number: 20100125075
    Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1-C6 alkoxy, C1-C6 alkenyloxy, amino, C1-C6 alkylamino, or di-(C1-C6 alkylamino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl(C1-C6 alkyl)- or aryl(C1-C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.
    Type: Application
    Filed: December 14, 2006
    Publication date: May 20, 2010
    Applicant: British Biotech Pharmaceuticals Ltd.
    Inventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
  • Patent number: 7718673
    Abstract: The invention is directed to novel isonipecotamide derivatives of Formula (I): which are useful in treating integrin-mediated disorders.
    Type: Grant
    Filed: January 16, 2003
    Date of Patent: May 18, 2010
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Michael J. Costanzo, William J. Hoekstra, Bruce E. Maryanoff
  • Publication number: 20100105917
    Abstract: The present invention relates to a method for producing an optically active 3-aminopiperidine or salt thereof. In the method, a racemic nipecotamide is stereoselectively hydrolyzed to obtain an optically active nipecotamide and an optically active nipecotic acid in the presence of an enzyme source derived from an organism, and then the optically active nipecotamide is derived into an optically active aminopiperidine or salt thereof by aroylation, Hofmann rearrangement, deprotection of the amino group and further deprotection; or the optically active nipecotamide is derived into an optically active aminopiperidine or salt thereof by selective protection with BOC, Hofmann rearrangement and further deprotection. It is possible by the present invention to produce an optically active 3-aminopiperidine or salt thereof useful as a pharmaceutical intermediate from an inexpensive and easily available starting material by easy method applicable to industrial manufacturing.
    Type: Application
    Filed: February 18, 2008
    Publication date: April 29, 2010
    Applicant: KANEKA CORPORATION
    Inventors: Kohei Mori, Masutoshi Nojiri, Akira Nishiyama, Naoaki Taoka
  • Publication number: 20100099677
    Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-V) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
    Type: Application
    Filed: April 20, 2009
    Publication date: April 22, 2010
    Inventor: Kevin James Doyle
  • Publication number: 20100099880
    Abstract: An alternate process for synthesizing opiate or opioid analgesics and anesthetics, and intermediates thereof is provided. In particular, a process of synthesizing synthetic opiate or opioid compounds such as, for example, remifentanil, carfentanil, sufentanil, fentanyl, and alfentanil are disclosed.
    Type: Application
    Filed: September 20, 2007
    Publication date: April 22, 2010
    Inventor: Brian Cheng
  • Patent number: 7700622
    Abstract: Compounds and compositions for modulating the activity of p38 kinases are provided, including p38? and p38? kinase. Methods for treating, preventing or ameliorating one or more symptoms of a p38 kinase mediated disease or disorder are also provided.
    Type: Grant
    Filed: July 23, 2004
    Date of Patent: April 20, 2010
    Assignee: Novartis AG
    Inventors: Hengyuan Lang, Jiong Lan, Yunfeng Fang