Carboxyl, Or Salt Thereof, In Side Chain Having Sulfur Bonded Directly To A Ring Patents (Class 562/431)
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Patent number: 11649220Abstract: The present invention relates to the field of compounds, and in particular to a probucol derivative, a preparation method therefor and use thereof, the probucol derivative having a structure represented by general formula I. The probucol derivative provided in the present invention can be used for the prevention and treatment of vascular diseases including diabetes, cardio-cerebrovascular diseases or complications thereof, and can be effectively used for reducing blood glucose, reducing blood lipid, reducing cholesterol, reducing body weight, reducing triglyceride, anti-inflammatory, and anti-oxidation, etc., having broad prospective applications.Type: GrantFiled: January 18, 2019Date of Patent: May 16, 2023Assignee: DEMOTECH.INC.Inventors: Song Lu, Wenwei Xie, Shuangjiang He
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Publication number: 20150045274Abstract: The present invention relates to the field of perfumery. More particularly, it concerns compounds comprising at least one ?-thio carbonyl or nitrile moiety capable of liberating an active molecule selected from an ?,?-unsaturated ketone, aldehyde or nitrile. The present invention concerns also the use of said compounds in perfumery as well as the perfuming compositions or perfumed articles comprising the invention's compounds. (I) wherein: a) m represents an integer from 1 to 6; b) Pro represents a hydrogen atom or a group susceptible of generating an odoriferous ?,?-unsaturated ketone, aldehyde or nitrile and is represented by the formulae (II) or (II?) in which the wavy line indicates the location of the bond between said Pro and the sulfur atom S; and at least one of the Pro groups is of the formula (II) or (II?).Type: ApplicationFiled: March 19, 2013Publication date: February 12, 2015Inventors: Peter Fankhauser, Andreas Herrmann, Umberto Maddalena, Alain Trachsel, Youqing Shen
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Patent number: 8933267Abstract: The present invention relates to a compound according to formula I in particular as anti-ulcer agent and/or anti-Helicobacter pylori agent, wherein R1 is selected from linear or branched C1-C6 alkyl, H, thioether and benzyl, and R2 is selected from linear or branched C1-C10 alkanediyl and pharmaceutical compositions thereof.Type: GrantFiled: March 13, 2014Date of Patent: January 13, 2015Assignee: King Saud UniversityInventors: Amani S. Awaad, Reham Moustafa El-Meligy, Ahmed M. Alafeefy
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Publication number: 20140163042Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(?O), —S(?O)2—, —C(?O)O—, —C(O)NR3—, —C(?S)—NR3, —C(?NH)NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n and p are independently 0 or 1, Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula —X2-Q1- or -Q1-X2— wherein X2 is —O—, S— or NRA— wherein RA is hydrogen or optionally substituted C1-C3 alkyl, and Q1 is an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic rType: ApplicationFiled: February 13, 2014Publication date: June 12, 2014Applicant: Chroma Therapeutics Ltd.Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Charles Moffat, Kenneth William John Baker, Alastair David Graham Donald
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Publication number: 20140046075Abstract: The invention is directed to compounds of formula I: wherein Ar, r, R3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.Type: ApplicationFiled: January 31, 2013Publication date: February 13, 2014Applicant: THERAVANCE, INC.Inventors: Seok-ki Choi, Paul R. Fatheree, Ryan Hudson, Keith Jendza, Robert Murray McKinnell, Vivek Sasikumar
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Publication number: 20130217652Abstract: The present invention relates to novel thiobenzyl and sulfinylbenzyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: February 20, 2013Publication date: August 22, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Publication number: 20130150479Abstract: The present invention provides a photocurable composition prepared using mercapto benzophenone compounds as key raw materials. The present invention aims to solve the problems existing in the prior photo-curing technology that low-molecular photoinitiators are easy to remain and migrate, while macromolecular photoinitiators has low initiation efficiency due to a low content of effective components and also has the problem of certain migration. The photocurable composition in the present invention can be easily prepared and has high addition efficiency with ethylenically unsaturated compounds, and the photocurable composition obtained by addition has no residual mercapto and has features of high initiation activity and zero migration rates when it is used in photocurable coatings, binder and ink formula.Type: ApplicationFiled: February 7, 2013Publication date: June 13, 2013Applicant: Insight High Technology (Beijing) Co. Ltd.Inventor: Insight High Technology (Beijing) Co. Ltd.
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Publication number: 20130150381Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of dis orders related to aberrant levels of uric acid.Type: ApplicationFiled: June 15, 2011Publication date: June 13, 2013Applicant: ARDEA BIOSCIENCE, INC.Inventors: Samedy Ouk, Jean-Michel Vernier, Esmir Gunic
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Publication number: 20130018026Abstract: The present invention provides compositions and methods for the targeted delivery, release and/or formation of a drug compound at a target site(s) within the body of an individual, such as a diseased and/or inflamed tissue in the body of the individual. These compositions may comprise a halogenated phenol ring cleavably linked to a core structure of a drug compound. Due to the variety of substituents that may be utilized in forming the different types of linkages, numerous examples of drug compounds linked to a halogenated phenol ring are proposed. The present invention further provides compositions comprising halogenated phenol starting compounds that do not undergo cleavage during a dehalogenation reaction to form a drug compound in a targeted tissue when administered to an individual. Methods of administering these non-cleaving compounds are further provided.Type: ApplicationFiled: July 13, 2012Publication date: January 17, 2013Inventor: Keith R. Latham
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Publication number: 20130005767Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.Type: ApplicationFiled: September 14, 2012Publication date: January 3, 2013Applicant: Allergan, Inc.Inventors: David W. Old, Vinh X. Ngo
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Patent number: 8283453Abstract: The present invention provides a method for selectively placing carbon nanotubes on a substrate surface by using functionalized carbon nanotubes having an organic compound that is covalently bonded to such carbon nanotubes. The organic compound comprises at least two functional groups, the first of which is capable of forming covalent bonds with carbon nanotubes, and the second of which is capable of selectively bonding metal oxides. Such functionalized carbon nanotubes are contacted with a substrate surface that has at least one portion containing a metal oxide. The second functional group of the organic compound selectively bonds to the metal oxide, so as to selectively place the functionalized carbon nanotubes on the at least one portion of the substrate surface that comprises the metal oxide.Type: GrantFiled: August 14, 2009Date of Patent: October 9, 2012Assignee: International Business Machines CorporationInventors: Ali Afzali-Ardakani, Phaedon Avouris, James B. Hannon, Christian Klinke
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Patent number: 8188148Abstract: The present invention concerns substituted 1,3-diphenylpropane derivatives, pharmaceutical compositions comprising them and the therapeutic uses thereof, particularly in the field of human and animal health.Type: GrantFiled: June 21, 2007Date of Patent: May 29, 2012Assignee: GenfitInventors: Jean-François Delhomel, Rémy Hanf, Karine Caumont-Bertrand
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Patent number: 8143447Abstract: The present invention provides compositions of matter, kits and methods for their use in the treatment of cancer. In particular, the invention provides compositions and methods for treating cancer in a subject by inhibiting a poly-ADP-ribose polymerase, as well as providing formulations and modes of administering such compositions.Type: GrantFiled: September 5, 2007Date of Patent: March 27, 2012Assignee: BiPar Sciences, Inc.Inventors: Jerome Moore, Bruce Keyt, John Burnier, Barry M. Sherman, Max Totrov, Valeria S. Ossovskaya
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Patent number: 8093386Abstract: There are described compounds having the general formula (I) below and their pharmaceutically acceptable salts thereof, wherein E, X, m, q, R1, R2, n and ZBG have the meanings reported in the description useful, in therapy, as inhibitors of zinc metalloproteinases.Type: GrantFiled: July 25, 2007Date of Patent: January 10, 2012Assignee: Bracco Imaging S.p.AInventors: Armando Rossello, Elisabetta Orlandini, Aldo Balsamo, Laura Panelli, Elisa Nuti
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Publication number: 20110269985Abstract: Compounds having stable isotopes 13C and/or 2H were synthesized from precursor compositions having solid phase supports or affinity tags.Type: ApplicationFiled: June 2, 2011Publication date: November 3, 2011Applicant: Los Alamos National Security, LLCInventors: Jurgen G. Schmidt, David B. Kimball, Marc A. Alvarez, Robert F. Williams, Rudolfo A. Martinez
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Publication number: 20110244045Abstract: The present invention provides a controlled-release composition which provides a therapeutically effective plasma concentration of N-acetylcysteine over prolonged period of time. The present invention also includes the use of the controlled-release composition, either alone or in combination with at least one additional active agent, for reduction of vascular inflammation marker and treatment of diseases, conditions, and/or symptoms associated with systemic and/or vascular inflammation in a patient. Furthermore, the present invention provides a process of making granules comprising N-acetylcysteine, or a salt, solvate, prodrug, and/or analog thereof.Type: ApplicationFiled: May 11, 2009Publication date: October 6, 2011Applicant: TIARA PHARMACEUTICALS ,INC.Inventors: Yadon Arad, Liang C. Dong
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Publication number: 20110230452Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.Type: ApplicationFiled: September 23, 2010Publication date: September 22, 2011Inventor: Irving Sucholeiki
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Patent number: 8008513Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.Type: GrantFiled: August 28, 2009Date of Patent: August 30, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Gee-Hong Kuo, Rui Zhang, Aihua Wang, Alan R. DeAngelis
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Publication number: 20110190515Abstract: The invention concerns novel substituted 1,3-diphenylprop-2-en-1-one derivatives, pharmaceutical compositions comprising same, their therapeutic uses, in particular for treating cerebral ischemia. The invention also concerns a method for preparing said derivatives.Type: ApplicationFiled: April 11, 2011Publication date: August 4, 2011Applicant: GENFITInventors: Jamila NAJIB, Karine Caumont-Bertrand
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Publication number: 20110144170Abstract: The present invention provides compounds capable of binding to an Fc receptor and modulating Fc receptor activity comprising a core lipophilic group in the form of an Aryl zing substituted with a group rich in p-electrons. The invention further provides for a method of treating an autoimmune disease involving Fc receptor activity using such compounds. A method for obtaining a compound which modulates Fc receptor activity is also provided, the method comprising: (a) providing or designing compounds having structural characteristics to fit in the groove of the Fc?RIIa structure; and (b) screening the compounds for modulating activity on the Fc receptor.Type: ApplicationFiled: February 18, 2011Publication date: June 16, 2011Inventors: Mark Phillip Hogarth, Geoffrey Allan Pietersz, Gerard Peter Moloney
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Publication number: 20110136888Abstract: The present invention involves substituted 1,3-diphenylpropane derivatives, pharmaceutical compositions comprising them and the therapeutic uses thereof, in particular in the fields of human and animal health.Type: ApplicationFiled: June 21, 2007Publication date: June 9, 2011Inventors: Jean-Francois Delhomel, Rémy Hanf, Karine Caumont-Bertrand
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Patent number: 7943796Abstract: An overbased salt of an oligomerized alkylhydroxyaromatic compound is disclosed, wherein the alkyl group of the alkylhydroxyaromatic compound is derived from an olefin mixture comprising propylene oligomers having an initial boiling point of at least about 195° C. and a final boiling point of no more than about 325° C. as measured by ASTM D86. Also disclosed is a lubricating oil composition containing at least (a) a major amount of an oil of lubricating viscosity and (b) the overbased salt of the oligomerized alkylhydroxyaromatic compound.Type: GrantFiled: July 31, 2008Date of Patent: May 17, 2011Assignee: Chevron Oronise Company LLCInventors: Curtis B. Campbell, Charles Michael Cisson
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Publication number: 20110082120Abstract: The invention relates to substituted thioacetic acid salicylate derivatives; compositions comprising an effective amount of a substituted thioacetic acid salicylate derivative; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a substituted thioacetic acid salicylate derivative.Type: ApplicationFiled: October 5, 2010Publication date: April 7, 2011Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Patent number: 7910770Abstract: The present invention provides compounds capable of binding to an Fc receptor and modulating Fc receptor activity comprising a core lipophilic group in the form of an Aryl ring substituted with a group rich in p-electrons. The invention further provides for a method of treating an autoimmune disease involving Fc receptor activity using such compounds. A method for obtaining a compound which modulates Fc receptor activity is also provided, the method comprising: (a) providing or designing compounds having structural characteristics to fit in the groove of the Fc?RIIa structure; and (b) screening the compounds for modulating activity on the Fc receptor.Type: GrantFiled: February 1, 2008Date of Patent: March 22, 2011Assignee: Trillium Therapeutics Inc.Inventors: Mark Phillip Hogarth, Geoffrey Allan Pietersz, Gerard Peter Moloney
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Patent number: 7902381Abstract: The invention relates to preparing derivatives of formula (1), wherein, in particular R1 and R2, identical or different, represent a hydrogen, flourine or chlorine atom, a hydroxy group, an alkyl radical and an alkoxy radical, R3 is an alkyl radical, a hydroxy group, or a methoxy radical, R4 is a hydrogen atom or a methyl radical and R5 and R6, identical or different, represent a hydrogen atom, an alkyl radical, an alkoxy radical, an alkylthio radical, and an alkylamino radical. The inventive method consists in reducing an amid of formula (9).Type: GrantFiled: April 8, 2005Date of Patent: March 8, 2011Assignee: Pierre Fabre MedicamentInventors: Bernard Vacher, Yves Brunel, Florence Castan-Cuisiat
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Publication number: 20110053779Abstract: 2-(3-Alkylthiobenzoyl)cyclohexanediones of the formula (I) are described as herbicides. In this formula (I), X, Y, R1 to R8 represent radicals such as hydrogen, organic radicals such as alkyl and alkoxy.Type: ApplicationFiled: July 27, 2010Publication date: March 3, 2011Applicant: BAYER CROPSCIENCE AGInventors: Hartmut AHRENS, Andreas VAN ALMSICK, Jan DITTGEN, Christopher Hugh ROSINGER, Isolde HÄEUSER-HAHN, Stefan LEHR, Dieter FEUCHT
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Publication number: 20110039851Abstract: The invention relates to a compound of formula (I): or a tautomer thereof or a pharmaceutically acceptable salt thereof, wherein R1 to R11, W, X, Y, Z, and n are as defined herein. The invention also relates to methods of using the compounds of formula (I) and compositions thereof to treat various diseases and disorders in a patient. The invention also relates to processes for preparing the compounds of formula (I) and intermediates useful in these processes.Type: ApplicationFiled: October 14, 2008Publication date: February 17, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Kaka Dey, Donghong Amy Gao, Daniel R. Goldberg, Alexander Heim-Riether, John Edward Mangette, Ingo Andreas Mugge, Roger John Snow, Alan David Swinamer, Jiang-Ping Wu, Zhaoming Xiong, Yu Yang
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Publication number: 20100286276Abstract: The present invention concerns substituted 1,3-diphenylpropane derivatives, pharmaceutical compositions comprising them and the therapeutic uses thereof, particularly in the field of human and animal health.Type: ApplicationFiled: June 21, 2007Publication date: November 11, 2010Applicant: GENFITInventors: Jean-Fancois Delhomel, Rémy Hanf, Karine Caumont-Bertrand
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Publication number: 20100210842Abstract: The present invention relates to a method of preparing compounds of general formula I wherein m, n, R1 and R2 are defined as mentioned hereinafter, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases.Type: ApplicationFiled: February 8, 2010Publication date: August 19, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Adil DURAN, Markus FRANK, Waldemar PFRENGLE, Juergen SCHNAUBELT
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Publication number: 20100189781Abstract: Disclosed are alkoxyalkyl S-prenylthiosalicylates and pharmaceutical compositions containing the same and a pharmaceutically acceptable carrier. Methods for treating a human afflicted with cancer, including solid tumors, or a hematological malignancy by administering to the human in need thereof an effective amount of an alkoxyalkyl S-prenylthiosalicylate are also disclosed.Type: ApplicationFiled: January 20, 2010Publication date: July 29, 2010Applicants: RAMOT AT TEL-AVIV UNIVERSITY LTD., CONCORDIA PHARMACEUTICALS, INC.Inventors: Yoel Kloog, Liat Goldberg, Victor J. Bauer
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Publication number: 20100145034Abstract: The present invention provides a method for selectively placing carbon nanotubes on a substrate surface by using functionalized carbon nanotubes having an organic compound that is covalently bonded to such carbon nanotubes. The organic compound comprises at least two functional groups, the first of which is capable of forming covalent bonds with carbon nanotubes, and the second of which is capable of selectively bonding metal oxides. Such functionalized carbon nanotubes are contacted with a substrate surface that has at least one portion containing a metal oxide. The second functional group of the organic compound selectively bonds to the metal oxide, so as to selectively place the functionalized carbon nanotubes on the at least one portion of the substrate surface that comprises the metal oxide.Type: ApplicationFiled: August 14, 2009Publication date: June 10, 2010Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATIONInventors: Alina Afzali-Ardakani, Phaedon Avouris, James B. Hannon, Christian Klinke
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Publication number: 20100137347Abstract: Disclosed herein is a compound of the formula (I). Therapeutic methods, compositions, and medicaments, related thereto are also disclosed.Type: ApplicationFiled: January 21, 2008Publication date: June 3, 2010Applicant: ALLERGAN, INC.Inventors: Yariv Donde, Jeremiah H. Nguyen
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Publication number: 20100137635Abstract: It is an object to provide a radical scavenger, an active oxygen-scavenging agent and the like, which are highly efficacious clinically and novel, and so as to attain the object, 3,4-dihydroxyphenylalanine derivatives such as N-?-alanyl-5-S-glutathionyl-1-3,4-dihydroxyphenylalanine (5-S-GAD) or pharmaceutically acceptable salts thereof are contained as an active ingredient.Type: ApplicationFiled: June 6, 2006Publication date: June 3, 2010Applicant: INBIOTEX INC.Inventors: Shunji Natori, Kunimiki Ootsu, Hajime Okuyama
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Patent number: 7728169Abstract: A pharmaceutical composition comprising a compound of formula (1) in polymorphic crystalline Form A: together with a pharmaceutically acceptable carrier or excipient, wherein the compound of formula (1) is present in polymorphic Form A (see, e.g., FIG. 6) substantially free of other polymorphic forms.Type: GrantFiled: April 21, 2008Date of Patent: June 1, 2010Assignee: Medicinova, Inc.Inventors: Kenneth Walter Locke, David Gregory Roe
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Publication number: 20100048669Abstract: Disclosed herein are compounds of the formula therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: September 8, 2009Publication date: February 25, 2010Applicant: ALLERGAN, INC.Inventors: David W. OLD, Vinh X. NGO
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Publication number: 20100004470Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.Type: ApplicationFiled: August 28, 2009Publication date: January 7, 2010Inventors: Gee-Hong Kuo, Rui Zhang, Aihua Wang, Alan R. DeAngelis
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Publication number: 20090325893Abstract: Methods are provided for using doxorubicin active agents in which reduced host toxicity is observed. Aspects of the methods including administering to a subject an effective amount of a doxorubicin active agent in conjunction with a doxorubicin toxicity-reducing adjuvant, e.g., a nitrone compound, or a nitrone compound in combination with a bisdioxopiperazine compound. Also provided are compositions for use in practicing the subject methods. The methods and compositions find use in a variety of different applications, including in the treatment of a variety of different disease conditions.Type: ApplicationFiled: February 11, 2009Publication date: December 31, 2009Inventors: William A. Garland, Brian D. Frenzel
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Publication number: 20090264660Abstract: An alkyl aryl sulfide of Chemical Formula (III) is prepared by substituting an aryl halogen compound of Chemical Formula (I) with an alkyl lithium organometallic reagent. The sulfide is subsequently reacted with a compound of Chemical Formula (II). Alternatively an aryl halogen compound of Chemical Formula (I) is reacted with Grignard reagent to protect the hydrogen-donating substituent, and then reacted with an alkyl lithium organometallic reagent, and subsequently with sulfur and a compound of Chemical Formula (II). An alkyl aryl sulfide of Chemical Formula (III) is prepared via a one-step reaction without separation or purification of an intermediate compound from various aryl halogen compounds.Type: ApplicationFiled: October 21, 2005Publication date: October 22, 2009Inventors: Heonjoong Kang, Jungyeob Ham, Jaeyoung Ko
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Publication number: 20090258817Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are also provided.Type: ApplicationFiled: July 27, 2007Publication date: October 15, 2009Inventors: Stephen Pusztay, Sushma Saraf, Nai Fang Wang
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Publication number: 20090209588Abstract: Novel compounds of the general formula (I), in which the variables are as defined in claim 1, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype, namely, type 1 diabetes, type 2 diabetes, dyslipidaemia, syndrome X (including the metabolic syndrome, i.e. impaired glucose tolerance, insulin resistance, hyper-triglyceridaemia and/or obesity), cardiovascular diseases (including atherosclerosis) and hypercholesterolaemia.Type: ApplicationFiled: May 3, 2005Publication date: August 20, 2009Applicant: Novo Nordisk A/SInventors: Miroslav Havranek, Per Sauerberg, Ingrid Pettersson, Pavel Pihera, Søren Ebdrup
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Publication number: 20090197201Abstract: The present invention relates to the use of end groups Y, where Y stands for (formula I), where Rf stands for CF3—(CH2)r—, CF3—(CH2)r—O—, CF3—(CH2)r—S—, CF3CF2—S—, SF5—(CH2)r—, [CF3—(CH2)r]2N—, [CF3—(CH2)r]NH— or (CF3)2N—(CH2)r—, B stands for a single bond, O, NH, NR, CH2, C(O)—O, C(O), S, CH2—O, O—C(O), N—C(O), C(O)—N, O—C(O)—N, N—C(O)—N, O—SO2 or SO2—O, R stands for alkyl having 1 to 4 C atoms, b stands for 0 or 1 and c stands for 0 or 1, q stands for 0 or 1, where at least one radical from b and q stands for 1, and r stands for 0, 1, 2, 3, 4 or 5, as end group in surface-active compounds, to corresponding novel compounds, and to processes for the preparation of these compounds.Type: ApplicationFiled: July 2, 2007Publication date: August 6, 2009Inventors: Wolfgang Hierse, Nikolai (Mykola) Ignatyev, Martin Seidel, Elvira Montenegro, Peer Kirsch, Andreas Bathe
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Patent number: 7557244Abstract: The present invention relates to compounds having the general Formula (I) with the definitions of X, Y, R1, R2, R3, R4, R9, and R10 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of ?-secretase activity.Type: GrantFiled: April 20, 2007Date of Patent: July 7, 2009Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Francis Wilson, Alison Reid, Valerie Reader, Richard John Harrison, Mihiro Sunose, Remedios Hernadez-Perni, Jeremy Major, Cyrille Boussard, Kathryn Smelt, Jess Taylor, Adeline LeFormal, Andrew Cansfield, Svenja Burckhardt, Chih Yung Ho, Yan Zhang
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Publication number: 20090105474Abstract: The anthranilic acid derivative or the salt thereof represented by the general formula wherein R1 and R2 are hydrogen atom, or the like; R3 is a phenyl, cycloalkyl or bicyclic heterocyclic group which may be substituted, or the like; R4 is a phenyl, cycloalkyl or pyridyl group which may be substituted, or the like; X1 is an alkylene or alkenylene group which may be substituted or a bond; X2 is the general formula -X3-X4- or -X4-X3-, wherein X3 is a sulfur atom, an imino group or a bond, or the like; X4 means an alkylene or alkenylene group which may be substituted or a bond; is useful for a remedy such as rheumatoid arthritis, osteoarthritis and carcinoma, because it shows MMP-13 production inhibitory effect.Type: ApplicationFiled: March 14, 2006Publication date: April 23, 2009Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Yoichi Taniguchi, Eiji Hara, Hitoshi Akitsu, Hidehiko Tanaka, Shuzo Anzai
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Publication number: 20090093484Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.Type: ApplicationFiled: December 21, 2006Publication date: April 9, 2009Inventors: Per Sauerberg, Pavel Pihera, Zdenek Polivka, Miroslav Havranek, Ingrid Pettersson, John Patrick Mogensen
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Patent number: 7470810Abstract: Novel C3-C19 alkyl- and aryl-thiotrifluoroacetates are provided which have the structure wherein Q is C9-C19 alkyl or aryl, and are useful protecting agents for the amino or hydroxy functional groups of amines, amino acids or primary or secondary alcohols or amino alcohols to enable formation of amide bonds in peptides or proteins which are useful as screening agents, pharmaceuticals and cosmetics. A process for preparing C3-C19 alkyl- and aryl-thiotrifluoroacetates is also provided wherein a C3-C19 alkylthiol or arylthiol is treated with trifluoroacetic anhydride (TFAA) in the presence of organic base such as pyridine, a solvent such as dichloromethane (DCM) and dimethylaminopyridine (DMAP) as a catalyst to form the desired C3-C19 alkyl- or aryl-thiotrifluoroacetate.Type: GrantFiled: January 11, 2005Date of Patent: December 30, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Padam N. Sharma, Edward J. Gublo, Susan D. Boettger, Saibaba Racha, John Usher
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Publication number: 20080300269Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.Type: ApplicationFiled: August 6, 2008Publication date: December 4, 2008Applicant: ALLERGAN, INC.Inventors: David W. Old, Vinh X. Ngo
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Publication number: 20080286219Abstract: Skin brightening compositions based on hydroquinone derivatives and methods of making and using the composition. The hydroquinone derivatives are 2-thio-hydroquinone derivatives.Type: ApplicationFiled: May 17, 2007Publication date: November 20, 2008Inventors: Michael Fitzpatrick Wempe, Jeffrey M. Clauson
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Patent number: 7385082Abstract: The invention relates to a method for the preparation of de 1,3-diphenylprop-2-en-1-one substituted on one of the two phenyl groups by a carboxyalkyloxy group or a carboxyalkylthio group.Type: GrantFiled: July 8, 2004Date of Patent: June 10, 2008Assignee: GENFITInventors: Jean-François Delhomel, Karine Caumont-Bertrand
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Patent number: 7365224Abstract: A pharmaceutical composition comprising a compound of formula (1) in polymorphic crystalline Form A: together with a pharmaceutically acceptable carrier or excipient, wherein the compound of formula (1) is present in polymorphic Form A (see, e.g., FIG. 6) substantially free of other polymorphic forms.Type: GrantFiled: December 29, 2005Date of Patent: April 29, 2008Assignee: Medicinova, Inc.Inventors: Kenneth Walter Locke, David Gregory Roe
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Patent number: 7365085Abstract: Disclosed is a compound having the formula: pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein. The compounds, salts and solvates of this invention are useful as LXR agonists.Type: GrantFiled: March 26, 2003Date of Patent: April 29, 2008Assignee: SmithKline Beecham CorporationInventors: Ajita Bhat, John Jeffrey McAtee, Scott K. Thompson, James S. Frazee, Lara S. Kallander, Chun Ma, Joseph Marino, Michael J. Neeb, Robert A. Stavenger