The Aryl Ring Or Ring System Is Polycyclo Patents (Class 564/387)
  • Patent number: 10274874
    Abstract: An intermediate transfer member includes a resin substrate layer and a surface layer disposed on the substrate layer. The surface layer is a cured product of a resin composition containing a polyfunctional (meth)acrylate, a photopolymerization initiator, and a tertiary amine compound having a melting point of 30° C. or more. In the tertiary amine compound, at least one hydrogen atom is bonded to one carbon atom out of three carbon atoms bonded to a nitrogen atom.
    Type: Grant
    Filed: November 14, 2017
    Date of Patent: April 30, 2019
    Assignee: KONICA MINOLTA, INC.
    Inventors: Teruo Sasaki, Akihiro Honya, Shinichi Hamaguchi, Shinichi Yabuki, Junji Kanda
  • Publication number: 20150119825
    Abstract: A method is described for optimizing ungual treatment. The method can include (a) providing a nail having at least two spaced apart holes formed from a surface thereof and extending into the nail, and (b) topically applying a radiolabeled pharmaceutical composition to the nail. At least a portion of the composition is received in the at least two holes. The method also includes (c) sectioning a portion of the nail proximate the at least two holes into a plurality of sections, (d) determining, for each of the plurality of sections, a concentration of radioactivity in the section as a function of position with respect to the at least two holes, and (e) optimizing a spacing between the at least two holes based at least partially on the determinations in step (d). A method of ungual treatment using the optimized spacing is also described.
    Type: Application
    Filed: March 15, 2013
    Publication date: April 30, 2015
    Inventors: Hanan Osman-Ponchet, Martine Bouclier
  • Publication number: 20150105559
    Abstract: Disclosed is a method for producing a compound having an amino group and/or a hydroxyl group from a substrate compound having an atomic group containing CO or CS by eliminating such atomic group. The substrate compound, having an atomic group containing CO or CS (for example, an amide, a carbamate, or the like), is allowed to react with a compound expressed by formula (I) below, at a temperature of 120° C. or lower, preferably in the presence of an ammonium salt, to eliminate such atomic group containing CO or CS. In formula (I) A may not be present, and in a case where A is present, A represents an alkyl group having 1 to 6 carbon atoms. H2N-A—NH2 (I) - - -.
    Type: Application
    Filed: March 4, 2013
    Publication date: April 16, 2015
    Applicant: Kyushu University, National University Corporation
    Inventors: Takashi Ohshima, Hiroyuki Morimoto, Yuhei Shimizu
  • Publication number: 20150080608
    Abstract: Method for preparing cinacalcet hydrochloride having the steps of heating (R)-1-naphthyl ethylamine (Formula I) and 3-(trifluoromethyl)benzene (Formula II) wherein L is a halogen atom, methanesulfonate group (OMs), p-Toluenesulfonate (OTs), or triflate (OTf), in an organic solvent in presence of an inorganic base, refluxing until 3-(trifluoromethyl)benzene is completely consumed, obtaining a reaction mixture containing cinacalcet, and after treatment, obtaining cinacalcet hydrochloride having a formula of The post treatment separates (R)-1-naphthyl ethylamine hydrochloride and cinacalcet hydrochloride by adjusting pH value, extraction, and other simple operations, and the (R)-1-naphthyl ethylamine obtained is recycled for preparing the next batch of cinacalcet hydrochloride.
    Type: Application
    Filed: November 28, 2014
    Publication date: March 19, 2015
    Inventors: Miaohuan XU, Yue Huang, Min Zhang
  • Patent number: 8921606
    Abstract: 3-[3-(Trifluoromethyl)phenyl]propionaldehyde is a key intermediate for the preparation of cinacalcet hydrochloride. The present invention provides a novel process for the preparation of 3-[3-(trifluoromethyl)phenyl]propionaldehyde. The present invention also provides an improved process for preparation of cinacalcet hydrochloride in high yields. The present invention further provides a process for purification of cinacalcet hydrochloride.
    Type: Grant
    Filed: July 16, 2010
    Date of Patent: December 30, 2014
    Assignee: Hetero Research Foundation
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Rapolu Raji Reddy, Jambula Mukunda Reddy, Bandi Vamsi Krishna
  • Publication number: 20140322304
    Abstract: Anti-cancer compositions and methods are described herein. In particular, compositions including one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described. Methods for treatment of pathological conditions particularly cancer, in a subject using one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described herein.
    Type: Application
    Filed: July 10, 2014
    Publication date: October 30, 2014
    Inventors: Gavin P. Robertson, Raghavendra Gowda Chandagalu D., Subbarao V. Madhunapantula, Gajanan S. Inamdar, Omer F. Kuzu
  • Publication number: 20140081048
    Abstract: A method for the preparation of Cinacalcet is disclosed comprising treating (R)-1-naphthyl ethylamine with an aromatic aldehyde to form (1R)-1-(2-naphthyl)-N-(aryl methylene)ethanamine derivative of Formula (IV), which is further treated with 1-(3-halopropyl)-3-(trifluoromethyl)benzene of Formula (V) to obtain an iminium salt of Formula (VI), followed by hydrolysis to obtain Cinacalcet free base.
    Type: Application
    Filed: October 11, 2013
    Publication date: March 20, 2014
    Applicants: Megafine Pharma (P) Ltd., Amneal Pharmaceuticals, LLC
    Inventors: Vijayavitthal Thippannachar Mathad, Navnath Chintaman Niphade, Gorakshanath Balasaheb Shinde, Sharad Subhash Ippar, Shrikant Prataprao Deshmukh, Raghavendra Kumar Panchangam
  • Publication number: 20140039184
    Abstract: The present disclosure relates to a compound of formula (1): where R1 through R8, which can be identical or different from each other, each are selected from of the group comprising hydrogen and the radical —(CH2)k—X, where k is a whole number from 1 to 20 and where X is an organic radical comprising a) at least one neutral, protonizable nitrogen atom and/or b) at least one positively charged nitrogen atom, under the provision that at least 1 radical R1 through R8 is not hydrogen. The invention further relates to the production and use of said compound.
    Type: Application
    Filed: February 23, 2012
    Publication date: February 6, 2014
    Inventors: Wolfgang Bäumler, Ariane Felgenträger, Karin Lehner, Tim Maisch, Johannes Regensburger, Francesco Santarelli, Andreas Spath
  • Patent number: 8629135
    Abstract: A class of compounds useful in pharmaceutical compositions and methods for treating or preventing cancer is described. The compounds' ability to inhibit RET kinase is quantified, i.e., their respective RET IC50 and EC50 values are described. One such compound, known as cyclobenzaprine and herein as SW-01, has been identified as RET-specific with an IC50 of 300 nM. SW-01 inhibits RET autophosphorylation and blocks the growth and transformation of thyroid cancer cell lines. It has been further tested in pancreatic cancer, breast cancer, and SCLC cell lines. The compounds show utility for inhibition of survival and proliferation of tumor cells.
    Type: Grant
    Filed: July 14, 2009
    Date of Patent: January 14, 2014
    Assignee: Queen's University at Kingston
    Inventors: Taranjit S. Gujral, Lois M. Mulligan, Vinay K. Singh
  • Patent number: 8614353
    Abstract: A process for preparing N-[(1R)-1-(1-naphthyl)ethyl]-3-[3-(trifluoromethyl)-phenyl]propan-1-amine of formula (I) i.e. Cinacalcet and its intermediates of formulae (V), (Va) and (Vb).
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: December 24, 2013
    Assignee: Zach System S.p.A.
    Inventors: Nicola Catozzi, Johnny Foletto, Massimiliano Forcato, Roberto Giovanetti, Giorgio Soriato, Massimo Verzini
  • Patent number: 8614354
    Abstract: There is described a process for the preparation of cinacalcet hydrochloride (I) which includes the steps of: a) reacting (R)-(+)-1-(1-naphthyl)ethylamine (II) with 3-[3-(trifluoromethyl)phenyl]propenaldehyde (III) to afford the non isolated intermediate (R)—N-[3-[3-(trifluoromethyl)phenyl]-2-propenylimino-N-[1-(1-naphthyl)ethylamine (IV); b) reducing the non isolated intermediate (R)—N-[3-[3-(trifluoromethyl)phenyl]-2-propenylimino-N-[-1-(1-naphthyl)ethylamine (IV) with a sequential addition of:—a solution of sodium borohydride, methanol and a base,—oxalic acid and—a base to obtain (R)—N-[3-[3-(tifluoromethyl)phenyl]-2-propenyl]-1-(1-naphthyl)ethylamine (V) by passing through the precipitation of the oxalate salt of compound (V) after the addition of oxalic acid; c) hydrogenating (R)—N-[3-[3-(trifluoromethyl)phenyl]-2-propenyl]-1-(1-naphthyl)ethylamine (V) thus obtaining (R)—N-(3-(3-(trifluoromethyl)phenyl]propyl]-1-(1-naphthyl)ethylamine cinacalcet base (VI), which is retaken in ethyl acetate; and d) treati
    Type: Grant
    Filed: June 18, 2008
    Date of Patent: December 24, 2013
    Assignee: Erregierre S.p.A.
    Inventors: Massimo Ferrari, Marcello Ghezzi, Matteo Bonaldi
  • Publication number: 20130261298
    Abstract: Process for the synthesis of ivabradine of formula (I): and addition salts thereof with a pharmaceutically acceptable acid.
    Type: Application
    Filed: March 25, 2013
    Publication date: October 3, 2013
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Alexandre LE FLOHIC, Mathieu GRANDJEAN
  • Publication number: 20130217910
    Abstract: The present invention relates to a process for the preparation of substituted N-(benzyl)cyclopropanamines of the general formula (II) starting from N-[(aryl)methylene]cyclopropanamine derivatives. The present invention further provides the N-[(arypmethylene]cyclopropanamine derivatives used as starting compounds in this process according to the invention, and their use for the preparation of substituted N (benzyl)cyclopropanamines.
    Type: Application
    Filed: November 4, 2011
    Publication date: August 22, 2013
    Inventors: Norbert Lui, Wahed Ahmed Moradi, Thomas Norbert Muller
  • Publication number: 20130190407
    Abstract: The present invention relates to the different roles inorganic ion receptors have in cellular and body processes. The present invention features: (1) molecules which can modulate one or more inorganic ion receptor activities, preferably the molecule can mimic or block an effect of an extracellular ion on a cell having an inorganic ion receptor, more preferably the extracellular ion is Ca2+ and the effect is on a cell having a calcium receptor; (2) inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (3) nucleic acids encoding inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (4) antibodies and fragments thereof, targeted to inorganic ion receptor proteins, preferably calcium receptor protein; and (5) uses of such molecules, proteins, nucleic acids and antibodies.
    Type: Application
    Filed: December 28, 2012
    Publication date: July 25, 2013
    Applicant: NPS Pharmaceuticals, Inc.
    Inventor: NPS Pharmaceuticals, Inc.
  • Publication number: 20130178654
    Abstract: 3-[3-(Trifluoromethyl)phenyl]propionaldehyde is a key intermediate for the preparation of cinacalcet hydrochloride. The present invention provides a novel process for the preparation of 3-[3-(trifluoromethyl)phenyl]propionaldehyde. The present invention also provides an improved process for preparation of cinacalcet hydrochloride in high yields. The present invention further provides a process for purification of cinacalcet hydrochloride.
    Type: Application
    Filed: July 16, 2010
    Publication date: July 11, 2013
    Applicant: HETERO RESEARCH FOUNDATION
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Rapolu Raji Reddy, Jambula Mukunda Reddy, Bandi Vamsi Krishna
  • Publication number: 20120309842
    Abstract: The present invention provides processes and intermediates for preparing cinacalcet base and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: September 16, 2010
    Publication date: December 6, 2012
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Sayeed Mukhtar, Dinesh Shashidharan Nair, Roshan Ramesh Medhane, Nitin Maheshwari, Hashim Nizar Poovanathil Nagoor Meeran, Neera Tewari, Mohan Prasad
  • Publication number: 20120172392
    Abstract: Compositions and methods are disclosed for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1). The compounds disclosed are amine-containing and amide-containing compounds. The compounds and compositions are useful for treatment of diseases, including inflammation, inflammatory diseases and autoimmune disorders.
    Type: Application
    Filed: March 7, 2012
    Publication date: July 5, 2012
    Inventors: LUISA M. SALTER-CID, ERIC Y. WANG, MARY T. MACDONALD, JINGJING ZHAO
  • Patent number: 8183415
    Abstract: Methods of preparing cinacalcet, cinacalcet derivatives, and salts thereof is disclosed herein. Also disclosed herein are polymorphs of cinacalcet, compositions of cinacalcet, and methods of treating a subject by administering cinacalcet, wherein cinacalcet is prepared by the disclosed methods.
    Type: Grant
    Filed: May 17, 2011
    Date of Patent: May 22, 2012
    Assignee: Amgen, Inc.
    Inventors: Oliver Thiel, Charles Bernard, Robert Larsen, Michael John Martinelli, Masooma Tamim Raza
  • Publication number: 20120116112
    Abstract: Process for the preparation of compounds of formula (IV): wherein R1-R6 are as defined in the specification. Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
    Type: Application
    Filed: December 30, 2011
    Publication date: May 10, 2012
    Applicants: LES LABORATOIRES SERVIER, UNIVERSITÉ CLAUDE BERNARD LYON 1, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Jean-Louis PEGLION, Olivier Baudoin, Nicolas Audic, Manon Chaumontet, Riccardo Piccardi
  • Publication number: 20110318417
    Abstract: Provided herein are impurities of cinacalcet, (R)-?-methyl-N-[3-[3-(trifluoromethyl)phenyl]propyl]-1-(5,6,7,8-tetrahydronaphthalene)methaneamine (tetrahydro cinacalcet impurity), (R)-?-Methyl-N-[3-[3-(trifluoromethyl)phenyl]propyl]-1-naphthalenemethaneamine-N-oxide (cinacalcet N-oxide impurity) and (R)-?-methyl-N-[3-[3-(trifluoromethyl)phenyl]methyl]-1-naphthalenemethaneamine (benzylamine impurity); and processes for preparation and isolation thereof. Provided further herein is a highly pure cinacalcet or a pharmaceutically acceptable salt thereof substantially free of impurities, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure cinacalcet or a pharmaceutically acceptable salt thereof substantially free of impurities.
    Type: Application
    Filed: December 8, 2009
    Publication date: December 29, 2011
    Applicant: ACTAVIS GROUP PTC EHF
    Inventors: Sonny Sebastian, Seetha Rama Sarma Peri, Katikireddy Ramamurthy, Nitin Sharadchandra Pradhan
  • Patent number: 8084646
    Abstract: Disclosed is a process for producing 1-hydroxy-4-aminoadamantane.
    Type: Grant
    Filed: September 28, 2007
    Date of Patent: December 27, 2011
    Assignee: Shionogi & Co., Ltd.
    Inventor: Hideaki Watanabe
  • Publication number: 20110295037
    Abstract: The invention relates to cinacalcet hydrochloride, new polymorphic crystalline forms of cinacalcet hydrochloride, amorphous cinacalcet hydrochloride and synthetic processes for their preparation.
    Type: Application
    Filed: June 8, 2007
    Publication date: December 1, 2011
    Applicant: MEDICHEM, S.A.
    Inventors: Tibor Szekeres, Jozsef Repasi, Andras Szabo, Monica Benito Velez, Bernardino Mangion
  • Publication number: 20110263041
    Abstract: In one embodiment of the present invention, a composition is disclosed for measuring a binding affinity between a nucleic acid and a test substance, which contains an organic fluorescent substance capable of binding to an RNA and which emits fluorescence having an intensity greater while the organic fluorescent substance is liberated from an RNA than while the organic fluorescent substance is bound to an RNA. This enables a highly accurate and easy measurement of a binding affinity between a test substance and a nucleic acid, and allows various substances to be examined as a test substance.
    Type: Application
    Filed: July 30, 2008
    Publication date: October 27, 2011
    Inventors: Kazuhiko Nakatani, Jinhua Zhang, Shiori Umemoto, Shinichi Sasaoka, Takahiro Wazaki
  • Publication number: 20110201598
    Abstract: A class of compounds useful in pharmaceutical compositions and methods for treating or preventing cancer is described. The compounds' ability to inhibit RET kinase is quantified, i.e., their respective RET IC50 and EC50 values are described. One such compound, known as cyclobenzaprine and herein as SW-01, has been identified as RET-specific with an IC50 of 300 nM. SW-01 inhibits RET autophosphorylation and blocks the growth and transformation of thyroid cancer cell lines. It has been further tested in pancreatic cancer, breast cancer, and SCLC cell lines. The compounds show utility for inhibition of survival and proliferation of tumour cells.
    Type: Application
    Filed: July 14, 2009
    Publication date: August 18, 2011
    Inventors: Taranjit S. Gujral, Lois M. Mulligan, Vinay K. Singh
  • Publication number: 20110189241
    Abstract: The invention relates to a process for tightly controlling the particle size of cinacalcet hydrochloride, i.e. a process for preparing large or small crystals of cinacalcet hydrochloride, which yields cinacalcet hydrochloride in a narrow, reproducible and consistent distribution of particles, which hence does not require to reprocess, rework or destroy material of undesired size, which is efficient and cost-effective, and which is suitable for industrial implementation.
    Type: Application
    Filed: May 4, 2009
    Publication date: August 4, 2011
    Applicant: Medichem, S.A.
    Inventor: Bernardino Mangion
  • Publication number: 20110178316
    Abstract: Fullerene compounds represented by the formulae Cm[C(R)CON3]n, Cm[C(R)NCO]n, Cm[C(R)NHCORd]n, and Cm[C(R)NH2]n, wherein Cm represents a fullerene moiety having m carbon atoms, m represents an even integer from about 60 to about 200, n represents an integer of about 1 or more, R represents an electron-withdrawing group, and Rd represents an alkoxy or alkylamino group. In addition, processes for preparing these fullerene compounds involving reacting an acyl azide with a fullerene in the presence of a base.
    Type: Application
    Filed: July 28, 2009
    Publication date: July 21, 2011
    Applicant: Luna Innovations Incorporated
    Inventor: Jing Zhang
  • Publication number: 20110145970
    Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.
    Type: Application
    Filed: August 26, 2009
    Publication date: June 23, 2011
    Applicant: BASF SE
    Inventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
  • Publication number: 20110105799
    Abstract: There is described a process for the preparation of cinacalcet hydrochloride (I) which includes the steps of: a) reacting (R)-(+)-1-(1-naphthyl)ethylamine (II) with 3-[3-(trifluoromethyl)phenyl]propenaldehyde (III) to afford the non isolated intermediate (R)—N-[3-[3-(trifluoromethyl)phenyl]-2-propenylimino-N-[1-(1-naphthyl)ethylamine (IV); b) reducing the non isolated intermediate (R)—N-[3-[3-(trifluoromethyl)phenyl]-2-propenylimino-N-[-1-(1-naphthyl)ethylamine (IV) with a sequential addition of:—a solution of sodium borohydride, methanol and a base,—oxalic acid and ? a base to obtain (R)—N-[3[3-(tifluoromethyl)phenyl]-2-propenyl]-1-(1-naphthyl)ethylamine (V) by passing through the precipitation of the oxalate salt of compound (V) after the addition of oxalic acid; c) hydrogenating (R)—N-[3-[3-(trifluoromethyl)phenyl]-2-propenyl]-1-(1-naphthyl)ethylamine (V) thus obtaining (R)—N-(3-(3-(trifluoromethyl)phenyl]propyl]-1-(1-naphthyl)ethylamine cinacalcet base (VI), which is retaken in ethyl acetate; and d) treat
    Type: Application
    Filed: June 18, 2008
    Publication date: May 5, 2011
    Inventors: Massimo Ferrari, Marcello Ghezzi, Matteo Bonaldi
  • Publication number: 20110105704
    Abstract: The present invention discloses post-metallocene complexes based on sterically encumbered bi- and tri-dentate naphthoxy-imine ligands. It also relates to the use of such post-metallocene complexes in the oligomerisation of ethylene to selectively prepare vinyl-end capped linear alpha-olefins.
    Type: Application
    Filed: April 24, 2009
    Publication date: May 5, 2011
    Applicants: TOTAL PETROCHEMICALS RESEARCH FELUY, Centre National De Le Recherche Scientifique (CNRS)
    Inventors: Jean-Francois Carpentier, Evgueni Kirillov, Abbas Razavi
  • Publication number: 20110086071
    Abstract: This invention provides a terbinafine pharmaceutical composition which is emulsifable or self-emulsifying or in form of an emulsion wherein the composition is adapted for oral administration.
    Type: Application
    Filed: December 14, 2010
    Publication date: April 14, 2011
    Inventors: Jean-Daniel Bonny, Andreas Carl Eugster, Patrice Guitard, Stefan Hirsch
  • Patent number: 7901594
    Abstract: The present invention relates to polyacene derivatives represented by general formula (I) below: (wherein R1 to R10, etc. each represents hydrogen atom, hydrocarbon group, or an alkoxy group; A1 and A2 are hydrogen atom, a halogen atom, a hydrocarbon group, an alkoxy group, cyano group, etc.; n is an integer of not less than 1; R6 and R7 may be linked to each other to form a ring); and a process for preparing the polyacene derivatives from polyhydro compounds as well as electrically conductive materials comprising the polyacene derivatives. According to the process for preparing the polyacene derivatives of the present invention, optional substituents can be introduced into any carbon atoms of the polyacene, and the number of aromatic rings can be increased.
    Type: Grant
    Filed: February 28, 2001
    Date of Patent: March 8, 2011
    Assignee: Japan Science and Technology Corporation
    Inventor: Tamotsu Takahasi
  • Publication number: 20100267988
    Abstract: The invention relates, in general, to an improved process for preparing compounds (e.g., 3-(3-trifluoromethylphenyl)propanal (Compound III, below)), which are key intermediates for the synthesis of cinacalcet, its salts and/or solvates thereof, as well as the use of such compounds prepared by such process for the preparation of cinacalcet and/or its salts or solvates.
    Type: Application
    Filed: June 8, 2007
    Publication date: October 21, 2010
    Applicant: Medichem, S.A.
    Inventors: Tibor Szekeres, Jozsef Repasi, Andras Szabo, Bernardino Mangion
  • Publication number: 20100197804
    Abstract: Pharmaceutical compositions for oral administration comprising terbinafine, a buffering component and a disintegrant. The compositions show rapid disintegration and having taste-masking properties.
    Type: Application
    Filed: April 12, 2010
    Publication date: August 5, 2010
    Inventors: Stefan Hirsch, Dieter Becker, Patrice Guitard, Andreas Carl Eugster
  • Publication number: 20100172993
    Abstract: The present invention discloses compositions having particles comprising, inorganic element; one or more active ingredient and optionally a release rate modulating agent, suitable for the delivery of active ingredients to human and animal tissues. The particles are nanoparticles or microparticles or mixtures thereof, made preferably by sol-gel method. The compositions are useful for application to the topical or mucosal surfaces preferably in the form of creams, gels, lotions, dry powders, spray, foam and other suitable forms.
    Type: Application
    Filed: August 10, 2007
    Publication date: July 8, 2010
    Inventors: Amarjit Singh, Sarabjit Singh, Paramjit Singh, Rajesh Jain
  • Publication number: 20100105864
    Abstract: A compound which is able to activate a calcium receptor can be used as an active ingredient of a prophylactic or therapeutic agent for treating diarrhea. The compound can be a peptide such as ?-Glu-X-Gly (X represents an amino acid or an amino acid derivative), ?-Glu-Val-Y (Y represents an amino acid or an amino acid derivative), ?-Glu-Ala, ?-Glu-Gly, ?-Glu-Cys, ?-Glu-Met, ?-Glu-Thr, ?-Glu-Val, ?-Glu-Orn, Asp-Gly, Cys-Gly, Cys-Met, Glu-Cys, Gly-Cys, Leu-Asp, ?-Glu-Met(O), ?-Glu-?-Glu-Val, ?-Glu-Val-NH2, ?-Glu-Val-ol, ?-Glu-Ser, ?-Glu-Tau, ?-Glu-Cys(S-Me)(O), ?-Glu-Leu, ?-Glu-Ile, ?-Glu-t-Leu, and ?-Glu-Cys(S-Me).
    Type: Application
    Filed: November 6, 2009
    Publication date: April 29, 2010
    Inventors: Junya Yoneda, Tetsuo Yano, Yukie Seki, Yuzuru Eto, Yusuke Amino
  • Publication number: 20100087545
    Abstract: Process for the preparation of pure allylamine pharmaceutical terbinafine of formula I in free base form or acid addition salt form, by distilling crude terbinafine base, preferably by short path distillation, e.g. at a temperature above 100° C. and reduced pressure, e.g. 0.2 mbar, and recovering the purified product in free base or acid addition salt form. The process is indicated for use in removal of metal or non-metal contaminants, optionally together with salt formation under simultaneous precipitation of pure trans isomer. Detection of non-metal contaminants such as substance A of formula preferably is effected by RP HPLC analysis with UV detection.
    Type: Application
    Filed: January 16, 2009
    Publication date: April 8, 2010
    Inventors: Ulrich Beutler, Peter Funfschilling, Gerhard Penn, Alfons Roth
  • Publication number: 20090216047
    Abstract: Purification process for the preparation of the allylamine pharmaceutical terbinafine of formula I in free base form or acid addition salt form, by distilling crude terbinafine base, preferably by short path distillation, e.g. at a temperature above 100° C. and reduced pressure, e.g. 0.2 mbar, and recovering the purified product in free base or acid addition salt form.
    Type: Application
    Filed: November 14, 2008
    Publication date: August 27, 2009
    Inventors: Ulrich Beutler, Gerhard Penn
  • Publication number: 20090197970
    Abstract: The present invention relates to the polymorph form II of Cinacalcet hydrochloride, methods for the preparation of pure form II of Cinacalcet hydrochloride, and pharmaceutical compositions comprising the new polymorphic form in an pharmaceutically effective amount The present invention also provides novel solvates of Cinacalcet hydrochloride, methods for the preparation of these solvates, the use of these novel solvates for the preparation of pure Cinacalcet hydrochloride, the use of these novel solvates for the preparation of polymorphic form II of Cinacalcet hydrochloride and pharmaceutical compositions comprising the acetic acid solvate of Cinacalcet hydrochloride.
    Type: Application
    Filed: June 25, 2007
    Publication date: August 6, 2009
    Inventors: Johannes Ludescher, Ulrich Griesser, Doris Braun, Josef Wieser
  • Publication number: 20090163719
    Abstract: There is provided a process for the de-enrichment of enantiomerically enriched compositions which comprises reacting an enantiomerically enriched composition comprising at least a first enantiomer or diastereomer of a substrate comprising a carbon-heteroatom bond, wherein the carbon is a chiral centre and the heteroatom is a group V heteroatom, in the presence of a catalyst system and optionally a reaction promoter to give a product composition comprising first and second enantiomers or diastereomers of the substrate having a carbon-heteroatom bond, the ratio of second to first enantiomer or diastereomer in the product composition being greater than the ratio of second to first enantiomer or diastereomer in the enantiomerically enriched composition.
    Type: Application
    Filed: October 27, 2005
    Publication date: June 25, 2009
    Inventors: Andrew John Blacker, Matthew John Stirling
  • Patent number: 7538250
    Abstract: An object of the present invention is to provide a novel pyrene compound. Provided is a pyrene compound represented by the following general formula (I): wherein: R1 and R2 each represent a substituted or unsubstituted alkyl group; and Ar1, Ar2, Ar3, and Ar4 each represent a substituted or unsubstituted aryl group and the like.
    Type: Grant
    Filed: November 8, 2007
    Date of Patent: May 26, 2009
    Assignee: Canon Kabushiki Kaisha
    Inventors: Koichi Suzuki, Naoki Yamada, Kazunori Ueno
  • Publication number: 20090069441
    Abstract: Disclosed herein are motuporamine mimic agents and methods of making and using same. Particularly exemplified are motuporamine mimic agents comprising cytotoxic activity and/or anti-metaplastic activity.
    Type: Application
    Filed: February 26, 2008
    Publication date: March 12, 2009
    Inventor: Otto Phanstiel
  • Patent number: 7288678
    Abstract: A process for the preparation of terbinafine, comprising the reaction of a compound of formula (II), or a salt thereof, wherein X is a leaving group, with tert-butylacetylene, in the presence of a platinum catalyst
    Type: Grant
    Filed: November 21, 2003
    Date of Patent: October 30, 2007
    Assignee: Dipharma S.p.A.
    Inventors: Antonio Tarquini, Graziano Castaldi, Gianluca Galdi, Pietro Allegrini
  • Patent number: 7022883
    Abstract: Disclosed are methods of making aryl intermediate compounds of the formula (A) which are useful in the production of heteroaryl ureas, Y and P are defined herein below.
    Type: Grant
    Filed: November 17, 2003
    Date of Patent: April 4, 2006
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Jinhua J. Song, Zhulin Tan, Nathan K. Yee
  • Patent number: 6919317
    Abstract: Synergistic combinations of a squalene epoxidase inhibitor such as terbinafine and a macrolide T-cell immunomodulator or immunosuppressant such as 33-epichloro, 33-desoxyascomycin are provided, which are useful in particular in the treatment of diseases involving fungal or suspected fungal infection, for immunomodulation or immunosuppression in conditions in which fungal or suspected fungal colonisation of e.g. the skin plays a role, such as atopic dermatitis and seborrhoeic dermatitis, and in situations of fungal resistance.
    Type: Grant
    Filed: February 16, 2001
    Date of Patent: July 19, 2005
    Assignee: Novartis AG
    Inventors: Neil Stewart Ryder, Friedrich Karl Mayer
  • Patent number: 6787570
    Abstract: The invention relates to substituted N-Alkyl/Alkenyl/Cycloalkyl/Heterocycyl N-Aryl/Heteroaryl tertiary-Heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery disease. Preferred tertiary-heteroalkylamine compounds are substituted N-cycloalkyl N-benzyl aminoalcohols.
    Type: Grant
    Filed: December 16, 2002
    Date of Patent: September 7, 2004
    Assignee: Pfizer, Inc.
    Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Deborah A. Mischke, Emily J. Reinhard, Barry L. Parnas, Melvin L. Rueppel
  • Patent number: 6710089
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-fused-phenyl-N-benzyl aminoalcohols.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: March 23, 2004
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6689913
    Abstract: Provided is a process for preparing terbinafine or its HCl salt comprising: reacting a furan derivative with a base to form a second compound; performing a reductive alkylation of the second compound obtained in the step with N-methyl-1-naphthalenemethylamine or its HCl salt to form a third compound; and purifying the third compound.
    Type: Grant
    Filed: December 27, 2002
    Date of Patent: February 10, 2004
    Assignee: Yuhan Corporation
    Inventors: Tai-Au Lee, Kyu-Jung Wang, Hong-Bae Kim, Kyoung-Chan Kwon, Chang-Hoe Ku
  • Patent number: 6583183
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-fused-benzyl aminoalcohols.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: June 24, 2003
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6515181
    Abstract: A process for the preparation of terbinafine which comprises the reaction of tert-butylacetylene with a compound of formula (II) characterized in that the reaction is carried out in the presence of copper (I) salts and of a base, in the absence of palladium.
    Type: Grant
    Filed: February 28, 2002
    Date of Patent: February 4, 2003
    Assignee: Dipharma S.p.A.
    Inventors: Graziano Castaldi, Giuseppe Barreca, Renzo Rossi
  • Patent number: 6495496
    Abstract: Low molecular weight Mannich base condensates of hydroxy aromatic compounds, an aldehyde; and an amine, wherein the combined number of substituent carbon atoms does not exceed 80. Such compounds are useful as soot dispersants in lubricating oils when used alone, or in combination with high molecular weight dispersants.
    Type: Grant
    Filed: December 22, 2000
    Date of Patent: December 17, 2002
    Assignee: Infineum International Ltd.
    Inventors: Antonio Gutierrez, Mark G. Stevens, Ricardo A. Bloch, Robert A. Kleist