Hydroxy, Bonded Directly To Carbon, Or Ether In Substituent Q (h Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/170)
  • Patent number: 10815211
    Abstract: The invention relates to novel compounds that are useful for modulating cellular ROS. The compounds are amide-derivatives of 2-hydroxy-2-methyl-4-(3,5,6-trimethyl-1,4-benzoquinon-2-yl)-butanoic acid. The compounds of the invention are formulated into pharmaceutical or cosmetic compositions. The invention further relates to methods wherein the compounds of the invention are used for treating or preventing diseases associated with increased ROS levels mitochondrial disorders and/or conditions associated with mitochondrial dysfunction, including adverse drug effects. The invention also relates to cosmetic methods for treating or delaying further aging of the skin and veterinary applications.
    Type: Grant
    Filed: October 7, 2016
    Date of Patent: October 27, 2020
    Assignee: Khondrion IP B.V.
    Inventors: Julien David Beyrath, Mina Pellegrini, Petrus Maria van Zandvoort, Johannes Albertus Maria Smeitink
  • Patent number: 9856213
    Abstract: The subject of the invention is process for the preparation of the prostaglandin amides of the general formula I, where in the formula the bonds marked with dotted lines may be single or double bonds, in the case of double bounds at positions 5,6 and 13,14 they may be in cis or in trans orientation, Q stands for a hydroxyl-group and Z stands for a hydroxyl- or oxo-group, R1 and R2 independently represent hydrogen atom or a straight or branched C1-10 alkyl- or aralkyl-group, optionally substituted with —ONO2 group, or an aralkyl- or aryl-group, which contains heteroatom, R3 represents a straight or branched, saturated or unsaturated C4-6 hydrocarbon group, or a C4-10 alkylcycloalkyl- or cycloalkyl-group, or an optionally with alkyl group or halogen atom substituted phenyl-, C7-10 alkylaryl- or hetaryl-group, Y represents (CH2)n group or O atom or S atom, and where n=0-3.
    Type: Grant
    Filed: December 10, 2015
    Date of Patent: January 2, 2018
    Assignee: CHINOIN ZRT
    Inventors: Gábor Havasi, Tibor Kiss, Irén Hortobágyi, Zsuzsanna Kardos, István Lászlófi, Zoltán Bischof, Ádám Bódis
  • Publication number: 20150011793
    Abstract: The present invention relates to an improved process for the preparation of pure compound of Formula-II, which is an intermediate in the preparation of Aliskiren and further conversion of compound of Formula-II into Aliskiren or its pharmaceutically acceptable salts.
    Type: Application
    Filed: February 15, 2013
    Publication date: January 8, 2015
    Applicant: MYLAN LABORATORIES LTD
    Inventors: Shankar Rama, Seshadri Rao Manukonda, Srinivasa Rao Dasari
  • Publication number: 20140357678
    Abstract: A pharmaceutically acceptable salt, prodrug or derivative compound of the formula I, wherein R1 is selected from H, a (C1-C5) alkyl group and a COR4 group; R2 is selected from H, a (C1-C5) alkyl group and a COR5 group; R3 is selected from H, a (C1-C5) alkyl group, a (C1-C5)-O-alkyl group, a cycloalkyl of (C5-C6) carbon atoms, an aryl group, and an aryl (C1-C5) alkyl group wherein the aryl group can be an unsubstituted aryl or substituted with one or more R6 groups and an NHCOR5 group, or the R2 and R3 groups together with N may form a piperidine, morpholine or piperazine group; R4 is selected from H and a (C1-C5)alkyl group; R5 is selected from an aryl group unsubstituted or substituted with one or more R6, linear or branched(C1-C5) alkyl or pyridyne groups and a pyridine group; R6 is selected from (C1-C5)alkyl groups, halogen and nitro.
    Type: Application
    Filed: January 10, 2013
    Publication date: December 4, 2014
    Inventors: Gerardo Burton, Javier Duran, David Martinez, Elvira Zini, Veronica Mora Munoz, Lucila Bertoncello
  • Publication number: 20140357628
    Abstract: Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof, with the proviso that the compound is no Tranilast.
    Type: Application
    Filed: June 27, 2014
    Publication date: December 4, 2014
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, David Stapleton, Steven Zammit, Darren James Kelly, Richard Ernest Gilbert, Henry Krum
  • Patent number: 8853393
    Abstract: The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: October 7, 2014
    Assignee: Anhui New Star Pharmaceutical Development Co., Ltd.
    Inventors: Ziao Xu, Yuanhai Zhao, Degang Li, Xiaoxiang Li
  • Publication number: 20140296339
    Abstract: Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and/or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, and/or premature ejaculation are described.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 2, 2014
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Publication number: 20140288183
    Abstract: This invention relates to the use of bis- and tris-dihydroxyaryl compounds as well as sulfonamides, heteroaryls, tricycloalkyl and their analogs and pharmaceutically acceptable salts, for modulating tau aggregation and alleviating tauopathies, such as Alzheimer's disease (AD), Pick's disease (PiD), progressive supranuclear palsy (PSP), corticobasal degeneration (CBD) and familial frontotemporal dementia/Parkinsonism linked to chromosome 17 (FTDP-17), amyotrophic lateral sclerosis/Parkinsonism-dementia complex, argyrophilic grain dementia, dementia pugilistic, diffuse neurofibrillary tangles with calcification, progressive subcortical gliosis and tangle only dementia.
    Type: Application
    Filed: June 10, 2014
    Publication date: September 25, 2014
    Inventors: Alan D. Snow, Qubai Hu, Thomas Lake, Judy Cam
  • Publication number: 20140231729
    Abstract: A negative-type photosensitive resin composition capable of forming a pattern having favorable adhesiveness at a low light exposure; a pattern forming method using the resin composition; a cured film, an insulating film, a color filter formed using resin composition; and a display device provided with the cured film, insulating film, or color filter. The resin composition contains a compound represented by the following formula (1). In the formula, R1 and R2 each independently indicate a hydrogen atom or an organic group, but at least one indicates an organic group. R1 and R2 may be bonded to form a ring structure and may contain a hetero atom bond. R3 indicates a single bond or an organic group. R4 to R9 each independently indicate a hydrogen atom, an organic group, etc., but R6 and R7 are never hydroxyl groups. R10 indicates a hydrogen atom or an organic group.
    Type: Application
    Filed: June 15, 2012
    Publication date: August 21, 2014
    Applicant: TOKYO OHKA KOGYO CO., LTD.
    Inventors: Dai Shiota, Mayumi Kuroko, Kunihiro Noda, Yoshinori Tadokoro
  • Publication number: 20140221649
    Abstract: A novel compound suitable for obtaining a negative-type photosensitive resin composition capable of forming a pattern having favorable adhesiveness at a low light exposure. The compound is represented by the following formula (1). In the formula, R1 and R2 each independently indicate a hydrogen atom or an organic group, but at least one indicates an organic group. R1 and R2 may be bonded to form a ring structure and may contain a hetero atom bond. R3 indicates a single bond or an organic group. R4 to R9 each independently indicate a hydrogen atom, an organic group, etc., but R6 and R7 are never hydroxyl groups. R10 indicates a hydrogen atom or an organic group.
    Type: Application
    Filed: June 15, 2012
    Publication date: August 7, 2014
    Applicants: DAICEL CORPORATION, TOKYO OHKA KOGYO CO., LTD.
    Inventors: Dai Shiota, Mayumi Kuroko, Kunihiro Noda, Yoshinori Tadokoro, Yasuyuki Akai, Hideyuki Takai
  • Publication number: 20140199254
    Abstract: This invention relates to the synthesis of a multifunctional hair color protector, p-methoxy cinnamidoproyl dimethyl behenyl ammonium chloride of Formula I and the compositions containing the same for hair care.
    Type: Application
    Filed: March 25, 2013
    Publication date: July 17, 2014
    Applicant: GALAXY SURFACTANTS LTD.
    Inventors: Nirmal KOSHTI, Pooja Vaidya KSHIRSAGAR, Bhagyesh SAWANT
  • Patent number: 8779015
    Abstract: Provided are a recycling method for industrially, simply and effectively recycling a phenolic body from a phenolic antioxidant which is masked by an organoaluminum compound and contained in an olefin polymer obtained by supplying the masked phenolic antioxidant upon polymerization; and an olefin polymer obtained by this method. In a method for recycling a phenolic antioxidant wherein a phenolic antioxidant which is masked by an organoaluminum compound and contained in an olefin polymer obtained by supplying the masked phenolic antioxidant upon polymerization is recycled to a phenolic body, a nitrogen gas comprising water and/or a proton donor at a volume ratio of 1.0×10?6 to 2.5×10?2 with respect to 1 volume of nitrogen is brought into contact with the olefin polymer.
    Type: Grant
    Filed: September 1, 2010
    Date of Patent: July 15, 2014
    Assignee: Adeka Corporation
    Inventors: Naoshi Kawamoto, Tsuyoshi Urushihara, Kohei Okamoto, Tetsuya Seguchi
  • Patent number: 8772544
    Abstract: The present invention relates to a process for the purification of crude bimatoprost to obtain pure bimatoprost comprising a chromatography, preferably a chromatography using an achiral stationary phase and an eluent comprising an alcohol and an apolar solvent; and crystallization of the product obtained the chromatography to obtain pure bimatoprost.
    Type: Grant
    Filed: June 10, 2009
    Date of Patent: July 8, 2014
    Assignee: Sandoz AG
    Inventors: Dominic De Souza, Martin Albert, Hubert Sturm
  • Patent number: 8765812
    Abstract: Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof; with the proviso that the compound is not Tranilast.
    Type: Grant
    Filed: July 5, 2007
    Date of Patent: July 1, 2014
    Assignee: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Willams, David Stapleton, Steven Zammit, Darren James Kelly, Richard Ernest Gilbert, Henry Krum
  • Patent number: 8697332
    Abstract: An object of the present invention is to provide a base generator which has sensitivity and is applicable to a wide range of applications, and a photosensitive resin composition which is applicable to a wide range of applications due to the structure of a polymer precursor in which reaction into a final product is promoted by a basic substance or by heating in the presence of a basic substance. The base generator generates a base by exposure to electromagnetic radiation and heating. The photosensitive resin composition comprises a polymer precursor in which reaction into a final product is promoted by the base generator and a basic substance or by heating in the presence of a basic substance.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: April 15, 2014
    Assignee: Dai Nippon Printing Co., Ltd.
    Inventors: Mami Katayama, Shunji Fukuda, Katsuya Sakayori, Kouji Kawaguchi
  • Publication number: 20140066466
    Abstract: Described herein are compositions that inhibit the production of TNF? downstream of CD40 activation. As such, also described are various methods of using compositions exhibiting this activity for the treatment or prevention of inflammatory diseases associated with TNF? production or CD40 activation.
    Type: Application
    Filed: March 12, 2012
    Publication date: March 6, 2014
    Applicant: President and Fellows of Harvard College
    Inventor: Junying Yuan
  • Publication number: 20140046074
    Abstract: The present invention relates to a (2R, 3R)-3-(3-substituted phenyl)-2-methyl n-pentanamide compounds as shown in the formula I and the preparation method thereof, wherein, the substituents are as defined in the specification, the present invention further relates to a use of the above compounds for the preparation of tapentadol II or its pharmaceutically acceptable salt, and the intermediates involved in the preparation process.
    Type: Application
    Filed: January 31, 2012
    Publication date: February 13, 2014
    Inventors: Qiang Zhang, Rongxia Zhang, Guanghui Tian, Jianfeng Li, Fuqiang Zhu, Xiangrui Jiang, Jingshan Shen
  • Publication number: 20140039060
    Abstract: The invention relates to compounds and their use in treating cell proliferative disorders, more specifically Syk tyrosine kinase-mediated disorders.
    Type: Application
    Filed: October 9, 2013
    Publication date: February 6, 2014
    Inventor: Eliahu Kaplan
  • Patent number: 8624062
    Abstract: A method for producing a phenylacetamide compound represented by formula (1): wherein Q represents a hydrogen atom or a halogen atom, R2 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, R4 represents an alkyl group having 1 to 4 carbon atoms, Ar represents an unsubstituted or substituted phenyl group, R5 represents R4 when R2 is a hydrogen atom, and R5 represents a hydrogen atom when R2 is an alkyl group having 1 to 4 carbon atoms; including reacting a phenylacetamide compound represented by formula (2): wherein Q, R2 and Ar have the same meanings as defined above; with a dialkyl sulfate represented by formula (3): wherein R4 has the same meaning as defined above; in the presence of a base.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: January 7, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hajime Ishida, Masaji Hirota, Yoko Miyanaga, Yuya Mizushima
  • Patent number: 8580752
    Abstract: The present invention relates to an aromatic substituted pentadienoic acid amides and there use in combination of specific amounts of aromatic amides i.e. 4-alkyl-5-(substituted phenyl)-2(E),4(E)-pentadienoic acid amides, its geometrical isomers or their dihydro or tetrahydro derivatives and an anti-infective drug useful in potentiating the bioefficacy of antiinfective drug. The combination of the present invention is useful in the treatment of certain infections and disease at lower concentration of anti-infectives necessary to inhibit the growth of microbial strains and may also find applications in reducing the resistance in microorganisms.
    Type: Grant
    Filed: March 29, 2006
    Date of Patent: November 12, 2013
    Assignee: Council of Scientitic and Industrial Research
    Inventors: Surrinder Koul, Jawahir Lal Koul, Subhash Chandra Taneja, Pankaj Gupta, Inshad Ali Khan, Zahid Mehmood Mirza, Ashwani Kumar, Rakesh Kamal Johri, Monika Pandita, Anita Khosa, Ashok Kumar Tikoo, Subhash Chander Sharma, Vijeshwar Verma, Ghulam Nabi Qazi
  • Publication number: 20130274323
    Abstract: Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2, Pgp, or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering effective amounts of certain compounds to the mammal, for example, a compound of the formula (I): wherein R1, R2, R3, X1, X2, X3, a, and b are as described herein. Uses of these compounds in the preparation of a medicament are also disclosed. Also disclosed are compounds of formula (II), pharmaceutical compositions comprising such compounds and uses thereof.
    Type: Application
    Filed: June 5, 2013
    Publication date: October 17, 2013
    Inventors: Curtis J. Henrich, Heidi R. Bokesch, Laura K. Cartner, Richard W. Fuller, Kirk R. Gustafson, Kentaro Takada, James B. McMahon, Susan E. Bates, Robert W. Robey, Suneet Shukla, Suresh V. Ambudkar, Michael C. Dean
  • Patent number: 8557812
    Abstract: The invention relates to small molecules which function as inhibitors of anti-apoptotic Bcl-2 family member proteins (e.g., Bcl-2 and Bcl-xL). The invention also relates to the use of these compounds for inducing apoptotic cell death and sensitizing cells to the induction of apoptotic cell death.
    Type: Grant
    Filed: August 22, 2005
    Date of Patent: October 15, 2013
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Guoping Wang, Guozhi Tang, Renxiao Wang, Zaneta Nikolovska-Coleska, Dajun Yang, Liang Xu
  • Publication number: 20130261178
    Abstract: A compound of formula I-0, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein Z1 is C1-C4 linear or branched alkyl or alkenyl; R4 is selected from unsubstituted and substituted C3-C3 cycloalkyl, C1-C8 linear or branched alkyl, C2-5 alkenyl, C6-C10 heteroaryl or aryl, or C3-C8 heterocyclyl which may be part unsaturated, and combinations thereof; Z is linear C2-3 alkylene; X1 is selected from NH and O; X2 is selected from unsaturated C and unsaturated S; and X3 is selected from NH and CH2; or one of X1 and X3 is a single bond; or X1 is O and X2 and X3 together are a single bond; and R7 is selected from oxo, F, Cl, Br, CN, NH2, NR92, NO2, CF3, OR9, COR9, OCOR9, COOR9, NR9COR9, CONR92SO2NR92, NR9SO2R9; and R8 is selected from C1-5 alkyl, C1-5 alkoxyl, C2-5 alkenyl or alkynyl, C6-10 aryl and C3-8 cycloalkyl and combinations thereof, which may be unsubstituted or further substituted by one or more F, Cl, Br, CN, NH2, NR32, NO2, CF3;
    Type: Application
    Filed: July 5, 2010
    Publication date: October 3, 2013
    Inventors: Shailesh Mistry, Etienne Daras, Christophe Fromont, Gopal Jadhav, Peter Martin Fischer, Barrie Kellam, Stephen John Hill, Jillian Glenda Baker
  • Publication number: 20130253038
    Abstract: It is intended to provide a polynucleotide that is resistant to RNase and has an RNA interference effect, etc. The present invention provides a single-stranded polynucleotide that is derived from a double-stranded polynucleotide comprising a sense strand polynucleotide corresponding to a target gene, and an antisense strand polynucleotide having a nucleotide sequence complementary to the sense strand polynucleotide, and has a structure in which the 5?-end of the antisense strand and the 3?-end of the sense strand are linked via a phenyl group-containing linker to form a phosphodiester structure at each of these ends.
    Type: Application
    Filed: December 1, 2011
    Publication date: September 26, 2013
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Makoto Koizumi, Yasuhide Hirota, Makiko Nakayama, Mika Ikeda
  • Patent number: 8541603
    Abstract: Therapeutic compounds, methods, and compositions are disclosed herein for treating glaucoma and baldness in mammals. The specific compounds are described herein and are modified prostaglandin derivates.
    Type: Grant
    Filed: May 13, 2009
    Date of Patent: September 24, 2013
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Todd S. Gac, Vinh X. Ngo
  • Patent number: 8529688
    Abstract: Provided is a recording material with a superior storage property for the background and image, particularly with a remarkable superiority in any of light resistance of the background, and light, moisture and heat resistance of the image. The recording material contains a phenolic compound represented by formula (I) [wherein R1-R3 each independently represent a hydrogen atom or C1-C4 alkyl group; R5 represents a hydrogen atom, C1-C4 alkyl group or C1-C4 alkoxy group, with the proviso that when R5 is a hydrogen atom, R4 is a C1-C4 alkyl group, when R5 is a C1-C4 alkyl group, R4 is a hydrogen atom, and when R5 is a C1-C4 alkoxy group, R4 is a C1-C4 alkoxy group].
    Type: Grant
    Filed: February 1, 2010
    Date of Patent: September 10, 2013
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Satoshi Kodama, Shinichi Satoh, Toshio Aihara, Tadashi Kawakami, Kazumi Jyujyo
  • Publication number: 20130231478
    Abstract: The invention discloses a novel intermediate for preparing tapentadol and analogues thereof, wherein the structural formula is shown as formula I or II, and the groups are defined as the specification. The invention further discloses a method for preparing the novel intermediate and use of the intermediate for preparing tapentadol and analogues thereof. The invention can remarkably improve the product yield and quality of tapentadol, reduce the production cost, and simplify the production procedure. The preparation process is environment friendly, thus more suitable for the requirements of industrial production.
    Type: Application
    Filed: July 29, 2011
    Publication date: September 5, 2013
    Inventors: Ziao Xu, Yuanhai Zhao, Degang Li, Xiaoxiang Li
  • Patent number: 8481593
    Abstract: The invention relates to the use of para-coumaric acid or para-hydroxycinnamic acid derivatives in cosmetic or dermatological compositions, specifically to the use of at least one compound derived from para-coumaric acid having a general formula (I) below: in which, especially, Z represents an oxygen or an —NH— group; X and Y are identical and each represent a CH or CH2 group, as an active principle with depigmenting, free-radical-scavenging and/or antiinflammatory activity. The invention also relates to the use of the above compounds for cosmetic care or for the preparation of a pharmaceutical composition, especially for depigmenting an area of skin, having antiradical and/or antiinflammatory activity.
    Type: Grant
    Filed: June 3, 2011
    Date of Patent: July 9, 2013
    Assignees: BASF Beauty Care Solutions S.A.S., Universite Joseph Fourier-Grenoble 1
    Inventors: Sabrina Okombi, Delphine Rival, Ahcene Boumendjel, Anne-Marie Mariotte, Eric Perrier
  • Patent number: 8461289
    Abstract: New bioresorbable polymers are synthesized from monomer analogs of natural metabolites In particular, polymers are polymerized from analogs of amino acids that contribute advantageous synthesis, processing and material properties to the polymers prepared therefrom, including particularly advantageous degradation profiles.
    Type: Grant
    Filed: May 29, 2012
    Date of Patent: June 11, 2013
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Joachim B. Kohn, Durgadas Bolikal
  • Publication number: 20130109880
    Abstract: The present invention relates to novel phenyl-N-acyl derivatives of biogenic amines and amino acids of general formula (I) as cyclooxynease inhibitors, possessing analgetic and anti-inflammatory properties and devoid of side effects in particular ulcerogeneity and pro-spasmodic actions, as well as capability to potentiate effect of other analgetics, and possessing in addition antihypoxic, antidepressant and anti-Parkinsonistic action; as well as to the processes for the preparation novel and known phenyl-N-acyl derivatives of biogenic amines, to a pharmaceutical composition and to an agent comprising compounds of general formula (I) as well as to use thereof and a method of treating.
    Type: Application
    Filed: November 12, 2012
    Publication date: May 2, 2013
    Applicant: Obschestvo S Ogranichennoi Otvetstvennostiyu Pharmenterprises
    Inventor: Obschestvo S Ogranichennoi Otvetstvennostiyu
  • Patent number: 8426644
    Abstract: The present invention is directed to methods of modulating the activity of an isoform of manganese superoxide dismutase which is useful for the treatment of diseases such as neurodegenerative diseases and heart failure.
    Type: Grant
    Filed: June 28, 2011
    Date of Patent: April 23, 2013
    Assignee: MitoTek, LLC
    Inventor: Paul Q. Anziano
  • Publication number: 20130011417
    Abstract: The present invention relates to colchicine derivatives expressed in chemical formula 1, or to pharmaceutically acceptable salts thereof, to a method for preparing said derivatives, and to a pharmaceutical composition comprising said derivatives. The colchicine derivatives according to the present invention exhibit superior immunomodulatory effects as compared with conventional immunomodulators or colchicines, and therefore can be valuably used as an immunomodulator for modulating an acute or chronic immune response in organ transplantation.
    Type: Application
    Filed: February 18, 2011
    Publication date: January 10, 2013
    Inventors: Duck Jong Han, Sung-eun Yoo, Jeehee Suh
  • Patent number: 8338637
    Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.
    Type: Grant
    Filed: August 6, 2008
    Date of Patent: December 25, 2012
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Publication number: 20120301423
    Abstract: The present invention relates to derivatives of ?,?-disubstituted amide compounds which comprise a substituted aryl at the ? carbon such that the substituent provides a means for attachment or incorporation of the compound to or in a polymer. The provision of such a substituent on the aryl has surprisingly been found not only to permit attachment to or incorporation in a polymer but also retention of useful antifouling activity. In embodiments, the substituent is selected from hydroxyl, ethers, es ters, carboxyls, alkylsilyls and alkenyls. Experiments demonstrate that antifouling activity can be as good or better as the corresponding unsubstituted compound and that polymers functionalised so as to include or be formed from the substituted compound can be used to reduce settlement.
    Type: Application
    Filed: February 2, 2011
    Publication date: November 29, 2012
    Applicants: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH, MARITIME AND PORT AUTHORITY OF SINGAPORE, NATIONAL UNIVERSITY OF SINGAPORE
    Inventors: Christina Li Lin Chai, Brendan Adrian Burkett, Serena Lay Ming Teo, Daniel Rittschof, Serina Siew Chen Lee, Gary Howard Dickinson, Han Hong
  • Patent number: 8309766
    Abstract: The present invention relates to novel phenyl-N-acyl derivatives of biogenic amines and amino acids of general formula (I) as cyclooxynease inhibitors, possessing analgetic and anti-inflammatory properties and devoid of side effects in particular ulcerogeneity and pro-spasmodic actions, as well as capability to potentiate effect of other analgetics, and possessing in addition antihypoxic, antidepressant and anti-Parkinsonistic action; as well as to the processes for the preparation novel and known phenyl-N-acyl derivatives of biogenic amines, to a pharmaceutical composition and to an agent comprising compounds of general formula (I) as well as to use thereof and a method of treating.
    Type: Grant
    Filed: March 24, 2006
    Date of Patent: November 13, 2012
    Assignee: Obschestvo S. Organichennoi Otvetstvennostiyu Pharmenterprises
    Inventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova, Galina Alexandrovna Zheltukhina, Violetta Leonidovna Kovaleva
  • Publication number: 20120283200
    Abstract: The present invention provides a pharmaceutical composition for preventing or treating a chronic heart disease, comprising a compound of a formula (I): wherein: R1 is one independently selected from a group consisting of a hydrogen, a methyl and an ethyl; R2 is one of a hydrogen and a methyl; and R3 is one selected from a group consisting of a hydrogen, (CH2)nAr and (CH2)nArR?R?, wherein n is one of 1 and 2, R? and R? is located at C-3 and C-4 positions, respectively, R? is a hydrogen and R? is one of a hydroxy, a fluorine, a bromine and a OMe, or R?+R?=—OCH2O—; or R2+R3 is one of wherein n is one of 4 and 5.
    Type: Application
    Filed: March 27, 2012
    Publication date: November 8, 2012
    Applicants: CHINA MEDICAL UNIVERSITY, National Taiwan University
    Inventors: MING-JAI SU, YUEH-HSIUNG KUO
  • Publication number: 20120283463
    Abstract: The present invention discloses processes for the preparation of 3-[(1R,2R)-3-(dimethyl-amino)-1-ethyl-2-methyl-propyl]phenol (Tapentadol), salts thereof and related compounds of formula (A), including stereoisomers and pharmaceutically acceptable salts thereof, and to certain intermediates used in such process.
    Type: Application
    Filed: December 26, 2010
    Publication date: November 8, 2012
    Applicant: MAPI PHARMA LIMITED
    Inventors: Ehud Marom, Michael Mizhiritskii
  • Publication number: 20120263659
    Abstract: The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.
    Type: Application
    Filed: November 22, 2010
    Publication date: October 18, 2012
    Applicants: BASF SE, SYMRISE AG
    Inventors: Thomas Subkowski, Michael Backes, Heiko Oertling, Arnold Machinek, Hubert Loges, Ulrike Simchen, Horst Surburg, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel
  • Patent number: 8288590
    Abstract: Biocompatible, bioresorbable polymers comprising a plurality of monomeric repeating units containing an amide group, wherein said amide groups are N-substituted and the N-substituent and degree of N-substitution are effective to lower the melt viscosity, the solution viscosity, or both, compared to the same polymer without N-substitution.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: October 16, 2012
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Joachim B. Kohn, Durgadas Bolikal, Jaap Schut, Ernest G. Baluca
  • Publication number: 20120252891
    Abstract: Three unique subtypes of N-hydroxyamides and N-hydroxycarbamates containing both the vanilloid moiety (4-hydroxy-3-methoxybenzyl) and a lipophilic aliphatic moiety. Also disclosed are direct syntheses of these vanilloid fatty hydroxamates. The compounds possess inhibitory activity against the enzymes fatty acid amide hydrolase (FAAH) and matrix metallo-proteinase 9 (MMP-9). In addition, these substances bind to the calcium channel protein TRPV1 and inhibit vesicant-induced inflammation in skin and cornea. The compounds have utility in treating topical or systemic inflammatory processes in the skin and/or eye.
    Type: Application
    Filed: March 16, 2012
    Publication date: October 4, 2012
    Applicants: University of Medicine and Dentistry of New Jersey, Lehigh University, Rutgers, The State University of New Jersey
    Inventors: Jeffrey D. Laskin, Ned D. Heindel, Carl Jeffrey Lacey, Abhilash N. Pillai, Marion Gordon, Diane E. Heck
  • Patent number: 8252843
    Abstract: The present invention provides methods for treating Acquired Immunodeficiency Syndrome (AIDS) and other viral diseases and Human Immunodeficiency Virus (HIV) related infections by administering one or more compounds of formula I: wherein: the dotted line represents a single or a double bond; and R1 and R2 are the same or different and independently of each other represent —CH2OH, —CH2OR4, —CH(OH)CH3, —CH(OR4)CH3 or a group represented by the formula: or salts or hydrates thereof in a carrier which minimizes micellar formation or van der Waals attraction of molecules of said compound. The invention also provides S enantiomeric forms of such compounds which possess the ability to inhibit cell growth while being of low toxicity to such cells and methods of making such compounds.
    Type: Grant
    Filed: July 12, 2010
    Date of Patent: August 28, 2012
    Assignee: Novaremed Limited
    Inventor: Eliahu Kaplan
  • Patent number: 8227643
    Abstract: This invention relates to bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable salts and their use in the modulation of Sirtuin 1 (Sirt1) and there use in neuroprotection for subject suffering from neurodegenerative diseases such as Alzheimer's disease, Huntington's disease, Amyotrophic lateral sclerosis, frontotemporal dementia, Parkinson's disease, including Parkinson's plus diseases such as multiple system atrophy, progressive supranuclear palsy, corticobasal degeneration and dementia with Lewy bodies, and in the manufacture of medicaments for such Sirt1 modulation and neuroprotection.
    Type: Grant
    Filed: January 12, 2010
    Date of Patent: July 24, 2012
    Assignee: ProteoTech, Inc.
    Inventors: Alan D. Snow, Qubai Hu, Judy A. Cam
  • Publication number: 20120183751
    Abstract: The present invention is to provide a photosensitive resin composition which has excellent resolution, is low in cost and is applicable to a wide range of applications due to the structure of a polymer precursor in which reaction into a final product is promoted by a basic substance or by heating in the presence of a basic substance. The present invention is also to provide a base generator which is applicable to such a photosensitive resin composition. Disclosed is a base generator which has a specific structure and generates a base by exposure to electromagnetic radiation and heating. Also disclosed is a photosensitive resin composition which comprises the base generator and a polymer precursor in which reaction into a final product is promoted by a basic substance or by heating in the presence of a basic substance.
    Type: Application
    Filed: September 29, 2010
    Publication date: July 19, 2012
    Applicant: DAI NIPPON PRINTING CO., LTD.
    Inventors: Mami Katayama, Shunji Fukuda, Katsuya Sakayori
  • Publication number: 20120149838
    Abstract: Provided are a recycling method for industrially, simply and effectively recycling a phenolic body from a phenolic antioxidant which is masked by an organoaluminum compound and contained in an olefin polymer obtained by supplying the masked phenolic antioxidant upon polymerization; and an olefin polymer obtained by this method. In a method for recycling a phenolic antioxidant wherein a phenolic antioxidant which is masked by an organoaluminum compound and contained in an olefin polymer obtained by supplying the masked phenolic antioxidant upon polymerization is recycled to a phenolic body, a nitrogen gas comprising water and/or a proton donor at a volume ratio of 1.0×10?6 to 2.5×10?2 with respect to 1 volume of nitrogen is brought into contact with the olefin polymer.
    Type: Application
    Filed: September 1, 2010
    Publication date: June 14, 2012
    Applicant: ADEKA CORPORATION
    Inventors: Naoshi Kawamoto, Takashi Ayabe, Tsuyoshi Urushihara, Kohei Okamoto, Tetsuya Seguchi
  • Publication number: 20120123145
    Abstract: Described are antioxidant macromolecules and methods of making and using same.
    Type: Application
    Filed: October 4, 2011
    Publication date: May 17, 2012
    Applicant: Polnox Corporation
    Inventors: Ashok L. Cholli, Rajesh Kumar
  • Publication number: 20120108666
    Abstract: The invention relates to compounds and their use in treating cell proliferative disorders, more specifically Syk tyrosine kinase-mediated disorders.
    Type: Application
    Filed: January 6, 2012
    Publication date: May 3, 2012
    Inventor: Eliahu Kaplan
  • Publication number: 20120093742
    Abstract: A method of modulating the flavour of an orally-receivable product, such as a foodstuff, beverage, dentifrice or medicine, comprising the addition thereto of a flavour-modulating proportion of at least one compound of the formula I in which X is selected from CHOH, C?O, CH2—CO and CH?C(OH), Y is selected from C1-C7 linear and branched alkyl and CH2CH2OH, Z is selected from CH3 and a moiety of the formula II in which the wavy bond represents bond linking Z to X and R1 and R2 are selected from the possibilities (i) both hydrogen; (ii) independently OH and OCH3; and (iii) R1 and R2 together with their bonds to the phenyl ring form a ring of the formula —O—CH2—O—; such that, when Z is CH3, X is C?O and Y is CH2CH2OH.
    Type: Application
    Filed: June 24, 2010
    Publication date: April 19, 2012
    Applicant: Givaudan S.A.
    Inventors: Abdelmajid Kaouas, Harry Renes, Alexander P. Tondeur, Cornelis Winkel
  • Patent number: 8158828
    Abstract: The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.
    Type: Grant
    Filed: April 16, 2007
    Date of Patent: April 17, 2012
    Assignee: GTx, Inc.
    Inventors: James T. Dalton, Christina Barrett, Yali He, Seoung-Soo Hong, Duane D. Miller, Michael L. Mohler, Ramesh Narayanan, Zhongzhi Wu
  • Publication number: 20120070395
    Abstract: Compound represented by formula (I): wherein the symbols are as defined in the description, and salts thereof, are useful as skin whitening agents.
    Type: Application
    Filed: September 22, 2011
    Publication date: March 22, 2012
    Applicant: AJINOMOTO CO. INC
    Inventors: Yusuke AMINO, Yoshinobu TAKINO, Satoru OHASHI, Fumie OKURA, Megumi KANEKO
  • Publication number: 20120059188
    Abstract: The present invention relates to halogenated compounds of formula (I) with the substituents as described within the specification. The compounds may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation.
    Type: Application
    Filed: December 19, 2008
    Publication date: March 8, 2012
    Applicants: The University of Melbourne, Fibrotech Therapeutics Pty Ltd
    Inventors: Darren James Kelly, Spencer John Williams, Steven Zammit