Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/434)
  • Patent number: 9650330
    Abstract: The present patent discloses a novel, efficient and transition-metal-free room temperature single step process for synthesis of aryl sulfones and substituted aryl sulfones starting from aryl substrates.
    Type: Grant
    Filed: December 12, 2014
    Date of Patent: May 16, 2017
    Assignee: Council of Scientific and Industrial Research
    Inventors: Santosh Baburao Mhaske, Virat Pandya
  • Patent number: 9024045
    Abstract: A process is provided which allows the synthesis of a large number of styrene derivatives with formation of C—C bonds, with use being possible of economically advantageous substrates, readily available carbon nucleophiles, and both inexpensive and environmentally unproblematic catalyst systems, permitting reaction under mild conditions and a high compatibility with functional groups on the reactants involved.
    Type: Grant
    Filed: May 31, 2013
    Date of Patent: May 5, 2015
    Assignee: Saltigo GmbH
    Inventors: Matthias Gotta, Bernd Wilhelm Lehnemann, Axel Von Wangelin Jacobi, Samet Guelak
  • Publication number: 20150038465
    Abstract: The invention relates to the use of a derivative compound of 1,3-benzodioxole of formula (I) wherein R is a linear or branched (C4-C10) alkyl substituent as a synergistic compound of insecticidal active ingredients insecticidal compositions comprising at least one compound of Formula (I) and at least one insecticidal active ingredient are also described.
    Type: Application
    Filed: March 14, 2013
    Publication date: February 5, 2015
    Applicant: ENDURA S.P.A.
    Inventors: Carlotta Gobbi, Valerio Borzatta, Elisa Capparella
  • Patent number: 8912188
    Abstract: Disclosed herein are substituted quinoxaline carboxylic acids of Formula (I): and compositions thereof, which may be useful as inhibitors of PAS Kinase (PASK) activity in a human or animal for the treatment of diseases such as diabetes mellitus.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: December 16, 2014
    Assignee: BioEnergenix, LLC
    Inventors: John M. McCall, Donna L. Romero, Robert C. Kelly
  • Publication number: 20140323508
    Abstract: The invention provides compounds of formula (I): Said compounds being modulators of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
    Type: Application
    Filed: December 6, 2012
    Publication date: October 30, 2014
    Inventors: Giuseppe Alvaro, Agostino Marasco
  • Patent number: 8835634
    Abstract: The present invention relates to methods for the treatment of a pathology associated with hyperglycaemia, particularly diabetes, by administering quinoxalinone compounds of formula (I), wherein R1, R2, R3, R4, R5 and R6 are as defined in the claims. The compounds have activity as insulin secretion stimulators. The invention also relates to the preparation and use of these quinoxalinone compounds for modulating insulin secretion in insulin-1 cells by contacting the cells with the compounds.
    Type: Grant
    Filed: January 4, 2013
    Date of Patent: September 16, 2014
    Assignee: Merck Patent GmbH
    Inventors: Gerard Botton, Eric Valeur, Micheline Kergoat, Christine Charon, Samer Elbawab
  • Patent number: 8815859
    Abstract: Arylpyrazinone derivatives of formula (I), as insulin secretion stimulators, the preparation and use of these pyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: August 26, 2014
    Assignee: Merck Patent GmbH
    Inventors: Gérard Botton, Eric Valeur, Christine Charon, Micheline Kergoat, Samer Elbawab
  • Patent number: 8691867
    Abstract: The present invention is a method for the treatment of alcohol abuse and/or addiction comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and/or formula (II) as herein defined.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: April 8, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Virginia L. Smith-Swintosky, Allen B. Reitz
  • Patent number: 8653286
    Abstract: Methods for forming maleimide functionalized polymers are provided. In one such embodiment, a maleimide functionalized polymer is prepared in a method that includes a step of carrying out a reverse Diels-Alder reaction. Intermediates useful in the methods, as well as methods for preparing the intermediates, are also provided. Also provided are polymeric reagents, methods of using polymeric reagents, compounds and conjugates.
    Type: Grant
    Filed: August 7, 2012
    Date of Patent: February 18, 2014
    Assignee: Nektar Therapeutics
    Inventors: Samuel P. McManus, Antoni Kozlowski, Tracy L. Hutchison, Brian Bray, Xiaoming Shen
  • Publication number: 20130324745
    Abstract: A process is provided which allows the synthesis of a large number of styrene derivatives with formation of C—C bonds, with use being possible of economically advantageous substrates, readily available carbon nucleophiles, and both inexpensive and environmentally unproblematic catalyst systems, permitting reaction under mild conditions and a high compatibility with functional groups on the reactants involved.
    Type: Application
    Filed: May 31, 2013
    Publication date: December 5, 2013
    Inventors: Matthias GOTTA, Bernd Wilhelm LEHNEMANN, Axel VON WANGELIN JACOBI, Samet GUELAK
  • Publication number: 20130096209
    Abstract: The present invention provides edible compositions comprising a compound of the present invention, food products comprising such edible compositions and methods of preparing such food products. The present invention also provides methods of reducing the amount of NaCl in a food product, methods of reducing the sodium intake in a diet, and methods of reducing bitter taste in a food product.
    Type: Application
    Filed: April 15, 2011
    Publication date: April 18, 2013
    Applicants: Kraft Foods Global Brands LLC, Chromocell Corporation
    Inventors: David Hayashi, William P. Jones, Jane V. Leland, Peter H. Brown, Joseph Gunnet, Daniel Lavery, Louise Slade, Kambiz Shekdar, Jessica Langer
  • Patent number: 8415353
    Abstract: Compounds of the Formula (I), where W represents CH or N; and Q represents —CN, —C(?NOH)NH2, —CONHR1 or various herein described heterocyclic radicals; as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.
    Type: Grant
    Filed: March 3, 2009
    Date of Patent: April 9, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joel M. Harris, Bernard R. Neustadt, Hong Liu, Jinsong Hao, Andrew W. Stamford
  • Patent number: 8415352
    Abstract: The present invention relates to quinoxalinone derivatives of formula (I): wherein R1, R2, R3, R4, R5 and R6 are as defined herein, as insulin secretion stimulators. Specific such quinoxaline compounds are also an aspect of the invention. The invention also relates to the preparation and use of these quinoxalinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.
    Type: Grant
    Filed: January 15, 2009
    Date of Patent: April 9, 2013
    Assignee: Merck Patent Gesellschaft mit Beschränkter Haftung
    Inventors: Gérard Botton, Eric Valeur, Micheline Kergoat, Christine Charon, Samer Elbawab
  • Patent number: 8344163
    Abstract: There is provided a nitrile compound having an excellent controlling effect on arthropod pests represented by the formula (I): wherein m represents in integer of 0 to 4; n represents an integer of 1 to 4; q represents an integer of 0 to 4; Q represents a C1-C4 fluoroalkyl group; Z represents an optionally substituted C2-C6 alkynyl group or a ?N—OR3 group; R1 and R2 independently represent a monovalent C1-C4 chain hydrocarbon group optionally substituted with a halogen atom, etc.; and A represents an optionally substituted monovalent C1-C6 chain hydrocarbon group, etc.
    Type: Grant
    Filed: March 18, 2009
    Date of Patent: January 1, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Hiromasa Mitsudera
  • Patent number: 8338432
    Abstract: A series of derivatives of 6,7-dihydro-3H-oxazolo[3,4-a]pyrazine-5,8-dione, mixtures thereof, their pharmaceutically acceptable salts, which are inhibitors of PDE-5, possessing vasodilatator properties and relaxing effects. In particular, compounds of formula (I), where R1, R2, R3, and R4 are defined herein, processes for the preparation of said compounds, pharmaceutical compositions containing them, as well as uses as inhibitors of the enzyme phosphodiesterase type 5 (PDE-5) in the treatment of the erectile dysfunction and PDE-5 inhibitor treatable disorders.
    Type: Grant
    Filed: August 2, 2011
    Date of Patent: December 25, 2012
    Assignee: Biolab Sanus Farmaceutica Ltda.
    Inventors: Sérgio Luiz Sacurai, Márcio Henrique Zaim, Carlos Eduardo da Costa Touzarim, Artur Franz Keppler, Gilberto De Nucci
  • Patent number: 8258324
    Abstract: Methods for forming maleimide functionalized polymers are provided. In one such embodiment, a maleimide functionalized polymer is prepared in a method that includes a step of carrying out a reverse Diels-Alder reaction. Intermediates useful in the methods, as well as methods for preparing the intermediates, are also provided. Also provided are polymeric reagents, methods of using polymeric reagents, compounds and conjugates.
    Type: Grant
    Filed: September 15, 2011
    Date of Patent: September 4, 2012
    Assignee: Nektar Therapeutics
    Inventors: Samuel P. McManus, Antoni Kozlowski, Tracy L. Hutchison, Brian Bray, Xiaoming Shen
  • Publication number: 20120190738
    Abstract: The present invention relates to compounds of general formula I for the treatment of malignancy by inhibition of PI3-Akt pathway and or induction of NO. The present invention also relates to the use of compound of general formula I for the treatment of malignancy by inhibition of PI3-Akt pathway and or induction of NO. The present invention further relates to a method of treating malignancy by inhibition of PI3-Akt pathway and or induction of NO by administration of compound or said composition to a mammal in need thereof.
    Type: Application
    Filed: January 12, 2010
    Publication date: July 26, 2012
    Inventors: Santu Bandyopadhyay, Bikas Chandra Pal, Jaisankar Parasuraman, Siddhartha Roy, Jayashree Bagchi Chakrabotry, Indrani Choudhury Mukherjee, Sanjit Kumar Mahato, Aditya Konar, Srabanti Rakshit, Labanya Mandal, Dipyaman Ganguly, Kausik Paul, Anirban Manna, Jayaraman Vinayagam, Churala Pal
  • Patent number: 8168808
    Abstract: A production method of fluorinated compounds, for producing a compound represented by formula (3) in a fluorine-based solution in a flow of fluorine gas after reaction of at least one type of compounds represented by formula (1) and at least one type of compounds represented by formula (2). Similarly, fluorinated compounds represented by formula (4) prepared by the fluorination of compounds obtained by the reaction of formula (1) and formula (2)?. The fluorinated polymers obtained by the polymerizations of formula (3) and (4) compounds are useful as an optical or electrical materials. wherein R1, R2, R3, R4, Rff1, Rff2, Rff3, Rff4, X, Y, Z, and n are defined in the specification respectively.
    Type: Grant
    Filed: November 9, 2009
    Date of Patent: May 1, 2012
    Assignee: Japan Science and Technology Agency
    Inventors: Yoshiyuki Okamoto, Yasuhiro Koike
  • Publication number: 20120029069
    Abstract: This invention relates to a novel compound extracted from antrodia Cinnamomea and related compounds of formula (1), and pharmaceutical compositions comprising the compound of formula (1) and a pharmaceutically acceptable carrier or excipient. The invention further comprises the method of inhibit cancer cells by administering an effective amount of the compound of formula (1).
    Type: Application
    Filed: May 6, 2011
    Publication date: February 2, 2012
    Inventors: Ching-Kuo Lee, Pi-Yu Chen, Jir-Mehng Lo, Wen-Bin Zhong, Tien-Wang Chiu, Chieh-Chou YU
  • Patent number: 8076324
    Abstract: The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: December 3, 2009
    Date of Patent: December 13, 2011
    Assignee: Sanofi-Aventis
    Inventors: Thomas Bohme, Uwe Gerlach, Dirk Gretzke, Heinz-Werner Kleemann, Stefania Pfeiffer-Marek, Henning Vollert, Jean-Michel Altenburger, Sergio Mallart
  • Patent number: 7985872
    Abstract: A method for producing an olefin compound represented by the formula (2): wherein R1 and R2 are the same or different, and independently represent an alkyl group or the like, with the proviso that R1 and R2 are not hydrogen atoms at the same time, R3 represents an alkyl group or the like, which comprises contacting a palladium catalyst with an ?,?-unsaturated aldehyde compound represented by the formula (1): wherein R1, R2 and R3 are the same as defined above, in the presence of an inorganic base.
    Type: Grant
    Filed: December 12, 2006
    Date of Patent: July 26, 2011
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Kouji Yoshikawa
  • Patent number: 7981460
    Abstract: The present invention relates to a pharmaceutical composition, a food composition or a cosmetic composition, containing one or more kinds of a compound represented by the following formula (I?) wherein R1 is a hydrogen atom, a hydroxyl group, a methoxy group or an ethoxy group, R2 is a hydroxyl group, a methoxy group or an acetoxy group, or R1 and R2 in combination optionally form a methylenedioxy group, R is represented by the following formula wherein Y is an ethylene group or a vinylene group, m and n are each an integer of 0 to 7, which satisfy m+n=2 to 8, and R3 and R4 are each independently a hydrogen atom, a methyl group or an ethyl group, provided that, (1) when R1 is a methoxy group, then R2 is not a hydroxyl group; and (2) when R1 is a hydroxyl group, then R2 is not a hydroxyl group and an acetoxy group.
    Type: Grant
    Filed: December 29, 2008
    Date of Patent: July 19, 2011
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yusuke Amino, Yoshinobu Takino
  • Publication number: 20110160276
    Abstract: A compound has Formula VIII where, X is —C(O)R, —C(O)OR, —CN, —NO2, —S(O)2R?, —P(O)(OR)2; each R is individually H, alkyl, or alkenyl; R? is alkyl or akenyl; R1 is aryl, alkenyl, arylalkenyl, heterocyclyl, or heteroaryl; and R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11 are individually H, alkoxy, or hydroxy. In some cases, X is NO2. Pharmaceutical compositions of the compound of Formula VIII with a pharmaceutically acceptable carrier may be prepared. The compounds may be used for inhibition of cyclooxygenase-2.
    Type: Application
    Filed: March 4, 2010
    Publication date: June 30, 2011
    Inventors: Irishi N.N. Namboothiri, Narasimham Ayyagari, Deena Jose
  • Patent number: 7928137
    Abstract: Compounds of formula I in which R1, R2, R3, each X, L, Y, Cy, Lp, D and n have the meanings as set out in the specification, and corresponding compounds in which the unsubstituted or substituted amidine group is replaced with an unsubstituted or substituted aminomethyl group, are useful as serine protease inhibitors.
    Type: Grant
    Filed: March 2, 2007
    Date of Patent: April 19, 2011
    Assignee: Tularik Limited
    Inventors: John Walter Liebeschuetz, William Alexander Wylie, Bohdan Waszkowycz, Christopher William Murray, Andrew David Rimmer, Pauline Mary Welsh, Stuart Donald Jones, Jonathan Michael Ernest Roscoe, Stephen Clinton Young, Phillip John Morgan
  • Patent number: 7902255
    Abstract: A ?-butyrolactone compound as shown in Formula (I) and pharmaceutical composition thereof: wherein X?N, O, S, Se; and A and B are selected from substituents having the following formula: wherein R1, R2, R3, R4, and R5 are selected from a hydrogen atom, a halogen atom, a hydroxyl group, a mercapto group, an amino group, an alkoxy group, and a nitro group. The ?-butyrolactone compound and pharmaceutical composition thereof butyrolactone have inhibitory effects on hepatoma, ovarian cancer, breast cancer, lung cancer, malignant glioblastoma or colorectal carcinoma, and are cytotoxic with high specificity to inhibit Paclitaxel-resistant tumor cells at later stage of chemotherapy without any damage on normal cells.
    Type: Grant
    Filed: February 17, 2009
    Date of Patent: March 8, 2011
    Assignee: Tzu Chi Buddhist General Hospital
    Inventors: Shinn-Zong Lin, Horng-Jyh Harn
  • Patent number: 7868004
    Abstract: A compound of the formula I in which X and Y are selected as follows: (i) X is H and Y is selected from the group consisting of (ii) X and Y together form a bivalent radical selected from the group consisting of —O—CH2—O—, —N?CH—O— and —N?CH—S— thus forming together with the carbon atoms to which the radical is attached a 5-membered ring. The compounds have cooling properties and are useful in, for example, foodstuffs, dentifrices and cosmetics.
    Type: Grant
    Filed: February 23, 2006
    Date of Patent: January 11, 2011
    Assignee: Givaudan S.A.
    Inventors: Lucienne Cole, Stefan Michael Furrer, Christophe C. Galopin, Pablo Victor Krawec, Adam Mazur, Jay Patrick Slack
  • Patent number: 7868204
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Grant
    Filed: March 25, 2005
    Date of Patent: January 11, 2011
    Assignee: MethylGene Inc.
    Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain
  • Patent number: 7847110
    Abstract: The invention relates to a method for producing optionally substituted methylenedioxybenzene. The invention particularly relates to the production of methylenedioxybenzene. The inventive production method is characterized by the fact that it involves the reaction of an optionally substituted catechol with an aldehyde in the presence of a solid acid catalyst selected among: a titanium silicalite and a zeolite that is doped with tin and/or titanium.
    Type: Grant
    Filed: April 19, 2005
    Date of Patent: December 7, 2010
    Assignee: Rhodia Chimie
    Inventors: Roland Jacquot, Jean-Roger Desmurs
  • Patent number: 7825145
    Abstract: The present invention relates to a method of treatment and/or prophylaxis of a microbial infection, comprising the step of administering an effective amount of a compound of formula (I), in which X and Y are either the same or different and selected from a heteroatom; is a double or single bond depending on the heteroatoms X and Y; R1 to R5 are either the same or different and selected from hydrogen or a non-deleterious substituent; and R6 and R7 are either the same or different and selected from hydrogen and a non-deleterious substituent or one of R6 and R7 are absent when there is a double bond present, pharmaceutically acceptable salts or derivatives, pro-drugs, tautomers and/or isomers thereof. The present invention also relates to a method for protecting a subject from radiation damage, a method of cancer radiotherapy and use as an antimicrobial or radioprotective agent of the compound of formula (I) defined above.
    Type: Grant
    Filed: October 24, 2007
    Date of Patent: November 2, 2010
    Assignee: Biodiem Ltd
    Inventors: Peter Prokofievich Denisenko, Nickolay Sergeevich Sapronov, Alexander Alexandrovich Tarasenko
  • Patent number: 7825260
    Abstract: Compounds of formula I, wherein X, a, b, R1, R2, R3, R4 and R5 are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
    Type: Grant
    Filed: April 29, 2004
    Date of Patent: November 2, 2010
    Assignee: Novartis AG
    Inventors: Rainer Albert, Claus Ehrhardt, Peter Ettmayer, Klaus Hinterding, Klemens Högenauer, Peter Nussbaumer
  • Publication number: 20100273106
    Abstract: A positive resist composition including a base component (A) which exhibits increased solubility in an alkali developing solution under the action of acid and an acid generator component (B) which generates acid upon exposure, wherein the base component (A) includes a polymeric compound (A1) having a structural unit (a0) containing an acid-dissociable, dissolution-inhibiting group, and the acid-dissociable, dissolution-inhibiting group has a 1,3-dioxole skeleton.
    Type: Application
    Filed: April 19, 2010
    Publication date: October 28, 2010
    Applicant: TOKYO OHKA KOGYO CO., LTD.
    Inventors: Yoshiyuki Utsumi, Jun Iwashita
  • Patent number: 7807712
    Abstract: The present invention provides appropriately substituted chalcones, such as, for example, represented by the structural formula as shown herein below Wherein R1, R2 and R3 are selected from the group consisting of H, OH, O-alkyl, O-phenyl and O-substituted phenyl; B represents Ar—Z—O or RO; where Z is an alkane having up to 5 carbon atoms; R is substituted propanol amino, wherein substituted amino groups are selected from the group consisting of t-butyl, n-butyl, i-butyl, i-propyl, 4-phenyl piperazine-1-yl, 4-(2-methoxyphenyl)-piperazin-1-yl and 3,4-dimethoxy phenethyl; and Ar is thiazolidine-dione methylene phenoxy. The compounds prepared have been demonstrated to exhibit significant antidiabetic effect in various animal models indicating potential for further exploitation.
    Type: Grant
    Filed: December 22, 2004
    Date of Patent: October 5, 2010
    Inventors: Ram Pratap, Mavurapu Satyanarayana, Chandeshwar Nath, Ram Raghubir, Anju Puri, Ramesh Chander, Priti Tiwari, Brajendra Kumar Tripathi, Arvind Kumar Srivastava
  • Publication number: 20100239726
    Abstract: Methods for removing safrole from a sample, molecular imprinted copolymers that bind safrole, and methods of making the same are provided.
    Type: Application
    Filed: April 10, 2006
    Publication date: September 23, 2010
    Applicant: R.J. REYNOLDS TOBACCO COMPANY
    Inventor: Svetlana Pertsovich
  • Patent number: 7799954
    Abstract: Derivatives of dicarbonyl compounds having antitumor and antibiotic activity which can be used as anticancer agents.
    Type: Grant
    Filed: November 14, 2007
    Date of Patent: September 21, 2010
    Assignee: Abraxis BioScience, LLC
    Inventors: Chunlin Tao, Qinwei Wang, Vuong Trieu, Neil Desai, Patrick Soon-Shiong
  • Publication number: 20100204206
    Abstract: Di(hetero)arylcyclohexane derivatives, their preparation, their use and pharmaceutical compositions comprising them The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: December 3, 2009
    Publication date: August 12, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Thomas BOHME, Uwe GERLACH, Dirk GRETZKE, Heinz-Werner KLEEMANN, Stefania PFEIFFER-MAREK, Henning VOLLERT, Jean-Michel ALTENBURGER, Sergio MALLART
  • Patent number: 7745445
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPAR?.
    Type: Grant
    Filed: May 13, 2005
    Date of Patent: June 29, 2010
    Assignee: IRM LLC
    Inventors: Robert Epple, Mihai Azimioara
  • Patent number: 7728020
    Abstract: The present invention relates to new amino acid derivatives, process for the production, their use, in particular in transplantation, and pharmaceutical compositions containing them.
    Type: Grant
    Filed: March 8, 2005
    Date of Patent: June 1, 2010
    Assignee: Novartis AG
    Inventors: Klaus Hinterding, Klemens Högenauer
  • Publication number: 20100105739
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: January 7, 2010
    Publication date: April 29, 2010
    Inventors: Sara S. Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D.J. Grootenhuis
  • Patent number: 7700620
    Abstract: The present invention provides novel C-linked cyclic compounds and analogues of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.
    Type: Grant
    Filed: June 26, 2006
    Date of Patent: April 20, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: James C. Sutton, Jennifer X. Qiao, Carl Thibeault, Rejean Ruel
  • Patent number: 7671221
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: June 29, 2007
    Date of Patent: March 2, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D. J. Grootenhuis
  • Publication number: 20090291958
    Abstract: Provided herein are substituted PDE5 inhibitors of Formula 1, and processes of preparation and pharmaceutical compositions thereof. Also provided are methods of their use for the treatment and/or management of hypertension, erectile dysfunction, and/or the inability to maintain improved erectile function.
    Type: Application
    Filed: June 7, 2007
    Publication date: November 26, 2009
    Applicant: Auspex Pharmaceuticals, Inc.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Patent number: 7612053
    Abstract: 7-substituted fused ring tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7-substituted fused ring tetracycline compounds are described.
    Type: Grant
    Filed: December 16, 2005
    Date of Patent: November 3, 2009
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventors: Mark L. Nelson, Laura McIntyre
  • Patent number: 7595343
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Grant
    Filed: September 12, 2002
    Date of Patent: September 29, 2009
    Assignee: MethylGene, Inc.
    Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain
  • Patent number: 7576129
    Abstract: The present invention relates to a carboxylic acid compound of formula (I): wherein R1 is H, alkyl; m is 2, 3; n is 0-2; R2 is phenyl, naphthyl, benzofuran, benzothiophene; Q is —CH2—O-Cyc1, —CH2-Cyc2, -L-Cyc3; R3a and R3b each independently is hydrogen, alkyl or taken together form tetrahydro-2H-pyran; a pharmaceutically acceptable salt thereof, a method for producing a process of the preparation thereof and a pharmaceutical agent comprising the same as an active ingredient. The compound of formula (I) have an antagonizing activity against PGE2 receptor, specifically EP3 receptor which is subtype thereof, and are useful for the prevention and/or treatment of itching, pain, urinary disturbance or stress disease.
    Type: Grant
    Filed: February 6, 2004
    Date of Patent: August 18, 2009
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Masaki Asada, Kaoru Kobayashi, Masami Narita, Kazutoyo Sato, Atsushi Kinoshita, Toshihiko Nagase, Ken Yoshikawa
  • Publication number: 20090202662
    Abstract: A process for the production of a substance or composition for the therapeutic or prophylactic treatment of erectile dysfunction or the enhancement of libido in a male human or animal subject comprises the step of formulating the substance or composition from at least one of plant material and an extract of plant material of at least one plant species of the family Geraniaceae.
    Type: Application
    Filed: May 23, 2007
    Publication date: August 13, 2009
    Applicant: CSIR
    Inventors: Gerda Fouche, Eric Khorombi, Vinesh Jaichand Maharaj
  • Publication number: 20090198051
    Abstract: An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R2 of N12 site is trichloroethoxicarbonyl (Troc) to which various substituents can be introduced by mild condition, further having 10 members ring structure which can be converted to a ring of other numbered members.
    Type: Application
    Filed: April 25, 2007
    Publication date: August 6, 2009
    Inventors: Tohru FUKUYAMA, Toshiyuki KAN
  • Publication number: 20090143432
    Abstract: The present invention provides a convenient and efficient process for the synthesis of d2-benzo[d][1,3]dioxoles.
    Type: Application
    Filed: September 12, 2008
    Publication date: June 4, 2009
    Applicant: CoNCERT Pharmaceuticals, Inc.
    Inventors: Andrew D. Jones, Robert E. Zelle, I. Robert Silverman
  • Patent number: 7524976
    Abstract: The invention relates to a process for preparing difluorobenzo-1,3-dioxole-5-carboxylic acid and derivatives thereof, and to the use thereof for preparing medicaments and crop protection agents.
    Type: Grant
    Filed: May 12, 2005
    Date of Patent: April 28, 2009
    Assignee: LANXESS Deutschland GmbH
    Inventors: Axel Pleschke, Albrecht Marhold
  • Patent number: 7491748
    Abstract: A carboxylic acid derivative of formula (I): wherein R1 is —COOH, —COOR6, etc.; A is a single bond, alkylene, etc.; R2 is alkyl, alkoxy, etc.; B is a carbocyclic ring or a heterocyclic ring; Q is alkylnene-Cyc2, etc.; D is a linking chain; and R3 is alkyl, a carbocyclic ring or a heterocyclic ring, or a non-toxic salt thereof. The compound of formula (I) binds to PGE2 receptor, especially subtypes EP3 and/or EP4 and show the antagonizing activity, are useful for the prevention and/or treatment of diseases induced pain, itch, urticaria, allergy, urinary frequency, urinary disturbance, Alzheimer's disease, cancer, dysmenorrhea, endometriosis, etc.
    Type: Grant
    Filed: August 8, 2002
    Date of Patent: February 17, 2009
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Kousuke Tani, Masaki Asada, Kaoru Kobayashi, Masami Narita, Mikio Ogawa
  • Publication number: 20090012137
    Abstract: The present invention relates to a method of treatment and/or prophylaxis of a microbial infection, comprising the step of administering an effective amount of a compound of formula (I), in which X and Y are either the same or different and selected from a heteroatom; is a double or single bond depending on the heteroatoms X and Y; R1 to R5 are either the same or different and selected from hydrogen or a non-deleterious substituent; and R6 and R7 are either the same or different and selected from hydrogen and a non-deleterious substituent or one of R6 and R7 are absent when there is a double bond present, pharmaceutically acceptable salts or derivatives, pro-drugs, tautomers and/or isomers thereof. The present invention also relates to a method for protecting a subject from radiation damage, a method of cancer radiotherapy and use as an antimicrobial or radioprotective agent of the compound of formula (I) defined above.
    Type: Application
    Filed: October 24, 2007
    Publication date: January 8, 2009
    Applicant: BIODIEM LTD.
    Inventors: Peter Prokofievich Denisenko, Nikolay Sergeevich Sapronov, Alexander Alexandrovich Tarasenko