The Chain Consists Of Two Or More Carbons Which Are Unsubstituted Or Have Acyclic Hydrocarbyl Substituents Only Patents (Class 564/374)
  • Patent number: 10407352
    Abstract: A stable composition is provided as plant growth promoters. The composition comprises of at least one source of weak acid, at least one free base and at least one penetration agent. Fertilizers and stabilizers can also be present as additional materials 5 in the plant growth promoting composition.
    Type: Grant
    Filed: February 25, 2016
    Date of Patent: September 10, 2019
    Assignee: NICHEM SOLUTIONS
    Inventors: Vinod Chintamani Malshe, Rajan Balkrishna Raje, Rishikesh Ramakant Choudhari, Rupali Prakash Hande
  • Patent number: 9598350
    Abstract: The present patent application relates to a process for preparing cinacalcet or a pharmaceutically acceptable salt thereof, which comprises reacting 3-trifluoromethylbenzaldehyde having the following formula (II) with the phosphorus-comprising derivative having the following formula (III) in which R1 and R2, which may be identical or different, are each a (C1-C6)alkyl group. The present invention also relates to the phosphorus-comprising derivative having the formula (III), to the use thereof and to the process for preparing same. The present invention also relates to the phosphate salt of cinacalcet and to uses thereof.
    Type: Grant
    Filed: March 21, 2016
    Date of Patent: March 21, 2017
    Assignee: Produits Chimiques Auxiliaries et de Synthese
    Inventors: Jean-Marie Schneider, Jonathan Madec, Sergio Kreimerman, Gerard Guillamot
  • Patent number: 9133098
    Abstract: A method for producing an organolithium compound includes the step of reacting an aromatic compound or a halogenated unsaturated aliphatic compound and a lithiating agent in the presence of a coordinating compound containing three or more elements having a coordinating ability in a molecule, at least one thereof being a nitrogen element, or a coordinating compound containing three or more oxygen elements having a coordinating ability in a molecule, at least one of the groups containing the oxygen elements having a coordinating ability being a tertiary alkoxy group, at a temperature of ?40° C. to 40° C.
    Type: Grant
    Filed: October 3, 2014
    Date of Patent: September 15, 2015
    Assignee: Nippon Soda Co., Ltd.
    Inventor: Hiroki Inoue
  • Patent number: 9115056
    Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Grant
    Filed: October 24, 2014
    Date of Patent: August 25, 2015
    Assignee: ACUCELA INC.
    Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
  • Publication number: 20150148735
    Abstract: A pharmaceutical device for electric-field assisted administration of Tapentadol and/or of a physiologically acceptable salt thereof, the device comprising at least one pair of electrodes consisting of an active electrode and a counter electrode (1a and 2a and/or 1b and 2b), optionally at least one additional electrode as an auxiliary electrode, at least one drug reservoir (3) containing at least a portion of the Tapentadol and/or a physiologically acceptable salt thereof, and means (4) for applying the device to skin (5).
    Type: Application
    Filed: January 16, 2015
    Publication date: May 28, 2015
    Inventors: Ingo FRIEDRICH, Martin MIKYNA, Sandra GEDAT, Richard GUY
  • Patent number: 9012689
    Abstract: The present invention relates to a compound of formula A, wherein R is alkyl. Compound A may be used as an intermediate in the preparation of O-desmethyl venlafaxine or a salt thereof, and the present invention provides such a preparation, as well as a process for preparing the compound of formula A.
    Type: Grant
    Filed: July 14, 2010
    Date of Patent: April 21, 2015
    Assignee: Cipla Limited
    Inventors: Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao, Manohar Raghunath Surve
  • 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
  • Patent number: 8981154
    Abstract: Provided herein are novel solid state forms of tapentadol salts, process for their preparation, pharmaceutical compositions, and method of treating thereof. The tapentadol salts include an L-(?)-camphorsulfonate salt, a dibenzoyl-(L)-tartrate salt, a dibenzoyl-(D)-tartrate salt, a malate salt, a maleate salt, or a salicylate salt.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: March 17, 2015
    Assignee: Actavis Group PTC EHF
    Inventors: Mayur Devjibhai Khunt, Sandipan Prabhurao Bondge, Nitin Sharadchandra Pradhan, Depashri Vikas Ahirao
  • Patent number: 8969623
    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: Grant
    Filed: October 11, 2013
    Date of Patent: March 3, 2015
    Assignee: Amneal Pharmaceuticals, LLC
    Inventors: Vijayavitthal Thippannachar Mathad, Navnath Chintaman Niphade, Gorakshanath Balasaheb Shinde, Sharad Subhash Ippar, Shrikant Prataprao Deshmukh, Raghavendra Kumar Panchangam
  • Publication number: 20150045444
    Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: October 24, 2014
    Publication date: February 12, 2015
    Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
  • Patent number: 8946302
    Abstract: The invention provides compounds of the formulas described herein and compositions thereof. The invention further provides methods of using the compounds and compositions. The compounds of the invention can provide high affinity binding to sigma-1 receptors in a mammal. The compounds can exhibit selectivity for the sigma-1 receptor over the sigma-2 receptor. The compounds and compositions of the invention can also be used to treat conditions that involve the sigma-1 receptor, such as addiction, cardiovascular conditions, and cancer, for example, cancer of the breast, lung, prostate, ovarian, colorectal, or the CNS.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: February 3, 2015
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Arnold E. Ruoho, Abdol R. Hajipour, Uyen B. Chu, Dominique A. Fontanilla
  • Patent number: 8946481
    Abstract: The invention relates to a process for producing a compound according to formula (i) or salt thereof, wherein R1 and R1? are independently hydrogen or an amine protecting group and R2 is a carboxyl group or an ester group, comprising reacting a compound according to formula (ii) or salt thereof, wherein R1, R1? and R2 are defined as above, with hydrogen in the presence of a transition metal catalyst and a chiral ligand, wherein the transition metal is selected from group 7, 8 or 9 of the periodic table. Furthermore, the invention relates to products obtainable by said process and to their use in the production of NEP inhibitors. Moreover, the invention relates to the use of transition metal catalyst in the preparation of NEP inhibitors or prodrugs thereof.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: February 3, 2015
    Assignee: Novartis AG
    Inventors: David Hook, Bernhard Wietfeld, Matthias Lotz
  • Patent number: 8933123
    Abstract: The present invention discloses polymorphic forms of O-desmethyl-venlafaxine succinate and processes for the preparation thereof.
    Type: Grant
    Filed: October 4, 2011
    Date of Patent: January 13, 2015
    Assignee: Cadila Healthcare Limited
    Inventors: Shriprakash Dhar Dwivedi, Ashok Prasad, Rushikesh Udaykumar Roy
  • Publication number: 20140378473
    Abstract: This invention relates to novel diarylamino compounds that bind to the sigma-2 receptor, to pharmaceutical compositions comprising such compounds, and to methods for inhibiting or restoring synapse loss in neuronal cells, modulating a membrane trafficking change in neuronal cells, and treating cognitive decline and neurodegenerative diseases and disorders therewith.
    Type: Application
    Filed: August 27, 2012
    Publication date: December 25, 2014
    Applicant: COGNITION THERAPEUTICS, INC.
    Inventors: Susan M. Catalano, Gilbert Rishton, Nicholas J. Izzo
  • Publication number: 20140378699
    Abstract: The present invention relates to an improved process for the preparation of Fesoterodine and pharmaceutically acceptable salts thereof. The present invention particularly relates to a process for the preparation of Fesoterodine from O-benzyl tolterodine.
    Type: Application
    Filed: January 4, 2013
    Publication date: December 25, 2014
    Inventors: Venkat Raman Jayaraman, Samir Patel, Indrajit Thakor, Viral Maheshbhai Parekh, Mahesh Ladani, Chetan Patil, Ronak Patel, Prashant Raval
  • Patent number: 8912217
    Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.
    Type: Grant
    Filed: April 12, 2012
    Date of Patent: December 16, 2014
    Assignee: Pisgah Laboratories, Inc.
    Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
  • Publication number: 20140350283
    Abstract: Compounds and methods for preparing substituted 3-(1-amino-2-methylpentane-3-yl)phenyl compounds from an isomerically pure starting material are described. In particular, methods of preparing a 3-(1-(dimethylamino)-2-methylpentane-3-yl)phenol as a substantially optically pure (R,R) stereoisomer are described. Using a method of the present invention, only the (R,R) and (S,S) stereoisomers of the target compound are produced, increasing the yield and stereoselectivity of the desired (R,R) stereoisomer.
    Type: Application
    Filed: May 24, 2013
    Publication date: November 27, 2014
    Inventors: Brian MORGAN, Olivier DAPREMONT, Patrick BERGET, Ali SULEMAN, William DUBAY, Jeffrey D. BUTLER
  • Patent number: 8889163
    Abstract: Facially amphiphilic polyphenylene and heteroarylene polymers and articles made therform having biocidal surfaces are disclosed. The polymers can inhibit the growth of microorganisms in contact with the surface or in areas adjacent to said biocidal surface. There is also disclosed a methods to attach facially amphiphilic polmers to a solid support. Utility as a contact disinfectant is disclosed.
    Type: Grant
    Filed: March 7, 2002
    Date of Patent: November 18, 2014
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: William F. DeGrado, Gregory N. Tew, Michael L. Klein
  • Patent number: 8853456
    Abstract: Disclosed herein is an improved process for the preparation of 3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol of Formula-I and its pharmaceutically acceptable salt which comprises the reaction of (S)-1-(dimethylamino)-2-methylpentan-3-one of formula VIII with 3-bromo anisole of formula II under Grignard conditions to get the compound (2S,3R)-1-(dimethylamino)-3-(3-methoxyphenyl)-2-methyl pentan-3-ol of formula V followed by activation of the —OH group of the formula V to convert into sulfonate esters of formula IX, which are on reductive deoxygenation to yield (2R,3R)-3-(3-methoxyphenyl)-N,N,2-trimethylpentan-1-amine of formula VII and demethylation of formula VII to obtain the compound 3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol of Formula-1.
    Type: Grant
    Filed: August 16, 2011
    Date of Patent: October 7, 2014
    Assignee: Indoco Remedies Limited
    Inventors: Mangesh Narayan Rajadhyaksha, Ranjeet Nair, Sandip Kacharu Deshmukh, Somnath Ambadas Khabale, Aditi Milind Panandikar
  • Publication number: 20140296574
    Abstract: A process for preparing N-[(1R)-1-(1-naphthyl)ethyl]-3-[3-(trifluoromethyl)-phenyl]propan-1-amine hydrochloride salt of formula (I) i.e. Cinacalcet hydrochloride and its intermediates of formulae (VII) and (VIII) wherein Z is chloride or another pharmaceutically acceptable anionic counterion.
    Type: Application
    Filed: June 13, 2014
    Publication date: October 2, 2014
    Inventors: Nicola Catozzi, Livius Cotarca, Johnny Foletto, Massimiliano Forcato, Roberto Giovanetti, Giorgio Soriato, Massimo Verzini
  • Publication number: 20140296346
    Abstract: A hitherto unknown crystalline form of (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride, pharmaceutical compositions containing the new crystalline form, methods of producing the new crystalline form, and a related method of use including treatment of, e.g., pain and/or urinary incontinence.
    Type: Application
    Filed: June 13, 2014
    Publication date: October 2, 2014
    Inventors: Andreas FISCHER, Helmut BUSCHMANN, Michael GRUSS, Dagmar LISCHKE
  • 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
  • Patent number: 8835665
    Abstract: Methods for recovery of recyclable water and/or fermentation co-products from thin stillage process streams. Microbial metabolites plant derivatives and/or plant extractives are removed from thin stillage after which water is recovered and recycled. Thin stillage is commingled with polar organic solvents or with oil to react microbial metabolites, plant derivatives and/or plant extractives. The reacted organic solvents are then separated from the processed thin stillage. Thin stillage may be commingled with an oil to re act with certain organic compounds, after which, the reacted oil is separated from the processed thin stillage is further extracted with one or more polar organic solvents. Alternatively, thin stillage may be first processed with one or more polar organic solvents, and then processed with an oil. Useful organic compounds may be recovered from the reacted oil and reacted organic solvents.
    Type: Grant
    Filed: June 2, 2009
    Date of Patent: September 16, 2014
    Assignee: University of Saskatchewan
    Inventors: Martin J. Reaney, Yunhua Jia, Jianheng Shen, Komsulee Ratanapariyanuch
  • Publication number: 20140249180
    Abstract: A tau aggregation inhibitor reduces tau aggregation in cells. The tau aggregation inhibitor can include a catechol structure-containing compound or a salt thereof, and the catechol structure-containing compound can be one of isoprenaline, dopamine, dobutamine, levodopa, levodopa/carbidopa, trimetoquinol, hexoprenaline, methyldopa, and droxidopa. One example of the catechol structure-containing compound is isoprenaline, which can be d-enantiomer of isoprenaline or d/l-racemic mixture of isoprenaline. Tauopathies to be prevented or treated by the inhibitor include AD, Down's syndrome, Pick's disease, corticobasal degeneration, and progressive supranuclear palsy.
    Type: Application
    Filed: October 3, 2012
    Publication date: September 4, 2014
    Applicants: National Center for Geriatrics and Gerontology, THE DOSHISHA
    Inventors: Akihiko Takashima, Yoshiyuki Soeda, Hiroyuki Nagata, Yasuo Ihara, Tomohiro Miyasaka, Hachiro Sugimoto
  • Publication number: 20140228380
    Abstract: The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.
    Type: Application
    Filed: August 2, 2013
    Publication date: August 14, 2014
    Applicants: University of Medicine and Dentistry New Jersey Medical School, Philadelphia Health & Education Corporation d/b/a Drexel University College of Medicine
    Inventors: Sandhya Kortagere, Eldo V. Kuzhikandahil
  • Publication number: 20140221498
    Abstract: The present invention relates to amino diol derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 4, 2014
    Publication date: August 7, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Wenkui K. Fang, Ken Chow
  • Publication number: 20140200345
    Abstract: Provided is a method for producing a 2-alkenylamine compound efficiently and at low cost, using a primary or secondary amine compound and a 2-alkenyl compound as the starting materials therefor. The 2-alkenyleamine compound is produced by 2-alkenylating a primary or secondary amine compound, using a specified 2-alkenylating agent and in the presence of a catalyst comprising a complexing agent and a transition metal precursor stabilized by a monovalent anionic five-membered conjugated diene.
    Type: Application
    Filed: August 29, 2012
    Publication date: July 17, 2014
    Applicants: NATIONAL UNIV. CORP. NAGOYA UNIVERSITY, SHOWA DENKO K.K.
    Inventors: Yoshitaka Ishibashi, Naoya Fukumoto, Masato Kitamura
  • Patent number: 8754285
    Abstract: The invention relates generally to thin-film adhesive materials suitable for various applications. In particular, the present invention provides pliable viscoelastic thin-films configured to form strong water-resistant adhesive bonds to various surface types.
    Type: Grant
    Filed: July 14, 2010
    Date of Patent: June 17, 2014
    Assignee: Kensey Nash Corporation
    Inventors: Bruce P. Lee, Jediah White, Fangmin Xu, John L. Murphy, Laura Vollenweider
  • Patent number: 8722732
    Abstract: The invention relates to (among other things) oligomer-calcimimetic conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.
    Type: Grant
    Filed: March 28, 2012
    Date of Patent: May 13, 2014
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Lin Cheng, David Martin
  • Publication number: 20140127130
    Abstract: The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.
    Type: Application
    Filed: January 9, 2014
    Publication date: May 8, 2014
    Applicant: HAMMERSMITH IMANET LIMITED
    Inventors: ERIK ARSTAD, MATTHIAS EBERHARD GLASER
  • Patent number: 8716530
    Abstract: The present invention discloses methods of use of facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, including, but not limited to, pharmaceutical uses of the polymers and oligomers as antimicrobial agents and as antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, compositions of the novel polymers and oligomers, including pharmaceutical compositions, and methods of designing and synthesizing the facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers.
    Type: Grant
    Filed: February 3, 2012
    Date of Patent: May 6, 2014
    Assignee: The Trustess of the University of Pennsylvania
    Inventors: William F. DeGrado, Dahui Liu, Gregory N. Tew, Michael L. Klein
  • Patent number: 8704002
    Abstract: Process for the preparation of substituted dimethyl-(3-aryl-butyl)-amine compounds. The process comprises dehydration by heterogeneous catalysis of substituted 4-dimethylamino-2-aryl-butan-2-ol compounds, to form substituted dimethyl-(3-aryl-but-3-enyl)-amine intermediates, which are then converted by hydrogenation with hydrogen to substituted dimethyl-(3-aryl-butyl)-amine compounds.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: April 22, 2014
    Assignee: Grünenthal GmbH
    Inventors: Utz-Peter Jagusch, Wolfgang Hoelderich, Monika Voerckel
  • Publication number: 20140081019
    Abstract: The present invention relates to a process for deuteration of amines in the alpha and/or beta position of the N-atom by using a deuterium source and a Ruthenium(II) based catalyst.
    Type: Application
    Filed: May 21, 2012
    Publication date: March 20, 2014
    Applicant: SANOFI
    Inventors: Jens Atzrodt, Volker Derdau, Wolfgang Holla, Matthias Beller, Lorenz Neubert, Dirk Michalik
  • Patent number: 8653106
    Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: February 18, 2014
    Assignee: Pisgah Laboratories, Inc.
    Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
  • Publication number: 20140039181
    Abstract: The invention relates to a method for producing a N-substituted amine compound by catalyzed alkylation. The method uses amine and alcohol or two kinds of amines as the reaction materials, employs composite metal oxides catalyst at a reaction temperature of 80-180° C. to catalyze the reaction for 6-36 hours, so as to produce the N-substituted amine compound. The reaction condition of the method of the invention is relatively moderate, using a catalyst made of cheap non-noble metals, which is non-caustic and easy to be separated and reused. The reaction does not need any medium and has relatively high conversion rate and selectivity.
    Type: Application
    Filed: December 28, 2012
    Publication date: February 6, 2014
    Applicant: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
    Inventor: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
  • Publication number: 20140011886
    Abstract: A hitherto unknown crystalline form of (?)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride, pharmaceutical compositions containing the new crystalline form, methods of producing the new crystalline form, and a related method of use including treatment of, e.g., pain and/or urinary incontinence.
    Type: Application
    Filed: June 21, 2013
    Publication date: January 9, 2014
    Applicant: GRUENENTHAL GmbH
    Inventors: Andreas Fischer, Helmut Buschmann, Michael Gruss, Dagmar Lischke
  • Publication number: 20130338399
    Abstract: A process for the preparation of substituted 3-(1-amino-2-methylpentane-3-yl)phenyl compounds which has advantages over conventional processes with respect to higher conversions and yields, flexibility, a shorter overall route, environmentally acceptable conditions, influence of stereoselectivity such as diastereoselectivity in a targeted manner and at least partial suppression of the formation of undesired side-products and/or undesired stereoisomers, in particular undesired diastereomers.
    Type: Application
    Filed: August 21, 2013
    Publication date: December 19, 2013
    Applicant: Gruenenthal GmbH
    Inventors: Helmut Heinrich BUSCHMANN, Joerg Holenz
  • Patent number: 8575395
    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: Grant
    Filed: September 6, 2011
    Date of Patent: November 5, 2013
    Assignees: Amneal Pharmaceuticals, LLC, Megafine Pharma (P) Ltd.
    Inventors: Vijayavitthal Thippannachar Mathad, Navnath Chintaman Niphade, Gorakshanath Balasaheb Shinde, Sharad Subhash Ippar, Shrikant Prataprao Deshmukh, Raghavendra Kumar Panchangam
  • Publication number: 20130259802
    Abstract: The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.
    Type: Application
    Filed: May 20, 2013
    Publication date: October 3, 2013
    Applicant: HAMMERSMITH IMANET LIMITED
    Inventors: ERIK ARSTAD, MATTHIAS EBERHARD GLASER
  • Publication number: 20130210924
    Abstract: A compound of formula (I) wherein X is O, S, SO or SO2; R1 is halogen, trihalomethyl, —OH, C1-7alkyl, C1-4alkoxy, trifluoromethoxy, phenoxy, cyclohexylmethyloxy, pyridylmethoxy, cinnamyloxy, naphthylmethoxy, phenoxymethyl, —CH2—OH, —CH2—CH2—OH, C1-4alkylthio, C1-4alkylsulfinyl, C1-4alkylsulfonyl, benzylthio, acetyl, nitro or cyano, or phenyl, phenylC1-4alkyl or phenyl-C1-4alkoxy each phenyl group thereof being optionally substituted by halogen, CF3, C1-4alkyl or C1-4alkoxy; R2 is H, halogen, trihalomethyl, C1-4alkoxy, C1-7alkyl, phenethyl or benzyloxy; R3H, halogen, CF3, OH, C1-7alkyl, C1-4alkoxy, benzyloxy, phenyl or C1-44alkoxymethyl; each of R4 and R5, independently is H or a residue of formula (a) wherein each of R8 and R9, independently, is H or C1-4alkyl optionally substituted by halogen; and n is an integer from 1 to 4; or a pharmaceutically acceptable salt, hydrate, solvate, isomer or prodrug thereof; or a compound of formula (II) wherein R1a is halogen, trihalomethyl, C1-4alkyl, C1-4alkoxy, C1-4alkyl
    Type: Application
    Filed: May 5, 2011
    Publication date: August 15, 2013
    Applicant: NOVARTIS AG
    Inventors: Peter Gergely, Erik Wallstroem, Eric Legangneux
  • Publication number: 20130211045
    Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
    Type: Application
    Filed: December 17, 2012
    Publication date: August 15, 2013
    Applicant: TRANZYME PHARMA INC.
    Inventor: TRANZYME PHARMA INC.
  • Publication number: 20130190529
    Abstract: The invention relates to a process for producing a process for producing an 18F-labelled compound, the process comprising treating a compound of formula (I) wherein EDG is an electron-donating group selected from —OH, —OR4, —NHR5 and —NR55R5; R1, R2, X1 and X2 are as defined herein; and R3 is selected from H, X3 and X4, wherein X3 is a monodentate cleavable surrogate group, and X4 is a bidentate cleavable surrogate group which is bonded (a) to said X1 or X2 and (b) to the ring carbon atom para to EDG; with [18F]fluoride in the presence of an oxidant, thereby producing, when R3 in the compound of formula (I) is H, an 18F-labelled compound of formula (II), wherein EDG is as defined above and R1, R2, X1 and X2 are as defined herein; or thereby producing, when R3 in the compound of formula (I) is said monodentate cleavable surrogate group X3, a compound of formula (IIa), wherein EDG? is O, NR5, —NR55R5 or [OR4]+, and wherein R4, R5, R55, R1, R2, X1, X2 and X3 are as defined herein; or thereby producing, whe
    Type: Application
    Filed: July 6, 2011
    Publication date: July 25, 2013
    Inventors: Veronique Gouveneur, Lei Li, Yee-Hwee Lim, Mickael Huiban
  • Publication number: 20130190522
    Abstract: Provided is a process for the preparing 1-phenyl-3-dimethylaminopropane derivatives of formula I, (The formula should be inserted here) and its pharmaceutically acceptable salts thereof via novel intermediates.
    Type: Application
    Filed: September 20, 2011
    Publication date: July 25, 2013
    Applicant: IND-SWIFT LABORATORIES LIMITED
    Inventors: Shekhar Bhaskar Bhirud, Perminder Singh Johar, Sushanta Mishra, Danish Jamshad
  • Publication number: 20130178620
    Abstract: The present invention provides processes and intermediates for the preparation of 3-benzazepines and salts thereof which can be useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.
    Type: Application
    Filed: September 14, 2012
    Publication date: July 11, 2013
    Inventors: Beverly L. Wolgast, CHARLES A. GILSON, III, SHELLEY AYTES, SCOTT A. ESTRADA, DIPANJAN SENGUPTA, BRIAN SMITH, MAX REY, ULRICH WEIGL, HEIDEDORE JLSABETH REY-PAPINA
  • Publication number: 20130178644
    Abstract: The object of the present invention is a new process for the synthesis of tapentadol, both as free base and in hydrochloride form, which comprises the step of alkylation of the ketone (VII) to yield the compound (VIII), as reported in Diagram 1, with high stereoselectivity due to the presence of the benzyl group as substituent of the amino group. It was surprisingly found that this substitution shifts the keto-enol equilibrium towards the desired enantiomer and amplifies the capacity of the stereocenter present in the compound (VII) to orient the nucleophilic addition of the organometallic compound at the carbonyl towards the desired stereoisomer. This substitution thus allows obtaining a considerable increase of the yields in this step, and consequently allows significantly increasing the overall yield of the entire tapentadol synthesis process. A further object of the present invention is constituted by the tapentadol free base in solid form, obtainable by means of the process of the invention.
    Type: Application
    Filed: June 20, 2011
    Publication date: July 11, 2013
    Applicant: EUTICALS S.P.A.
    Inventors: Giuseppe Motta, Domenico Vergani, Giorgio Bertolini, Nicola Landoni
  • Publication number: 20130165672
    Abstract: The invention relates to a process for preparing primary amines which comprises the process steps A) provision of a solution of a secondary alcohol in a fluid, nongaseous phase, B) contacting of the phase with free ammonia and/or at least one ammonia-releasing compound and a homogeneous catalyst and optionally C) isolation of the primary amine formed in process step B), characterized in that the volume ratio of the volume of the liquid phase to the volume of the gas phase in process step B is greater than or equal to 0.25, and/or in that the ammonia is used in process step B) in a molar ratio based on the hydroxyl groups in the secondary alcohol of at least 5:1.
    Type: Application
    Filed: August 23, 2011
    Publication date: June 27, 2013
    Applicant: Evonik Degussa GmbH
    Inventors: Florian Klasovsky, Jan Christoph Pfeffer, Thomas Tacke, Thomas Haas, Andreas Martin, Jens Deutsch, Angela Koeckritz
  • Publication number: 20130165674
    Abstract: The disclosure relates to a process for preparing benzofuran derivatives of general formula I: in which R, R1, and R2 are as defined in the disclosure; by coupling the hydroxylamine with a diketone of general formula III: in order to form an oxime that is then cyclized by heating in order to form the desired compound.
    Type: Application
    Filed: January 16, 2013
    Publication date: June 27, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • Publication number: 20130150622
    Abstract: A process for the synthesis of a salt of tapentadol.
    Type: Application
    Filed: December 10, 2012
    Publication date: June 13, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Boehringer Ingelheim International GmbH
  • Publication number: 20130137890
    Abstract: Disclosed herein is an improved process for the preparation of 3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol of Formula-I and its pharmaceutically acceptable salt which comprises the reaction of (S)-1-(dimethylamino)-2-methylpentan-3-one of formula VIII with 3-bromo anisole of formula II under Grignard conditions to get the compound (2S, 3R)-1-(dimethylamino)-3-(3-methoxyphenyl)-2-methyl pentan-3-ol of formula V followed by activation of the —OH group of the formula V to convert into sulfonate esters of formula IX, which are on reductive deoxygenation to yield (2R,3R)-3-(3-methoxyphenyl)-N,N,2-trimethylpentan-1-amine of formula VII and demethylation of formula VII to obtain the compound 3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol of Formula-1.
    Type: Application
    Filed: August 16, 2011
    Publication date: May 30, 2013
    Applicant: Indoco Remedies Limited
    Inventors: Mangesh Narayan Rajadhyaksha, Ranjeet Nair, Sandip Kacharu Deshmukh, Somnath Ambadas Khabale, Aditi Milind Panandikar
  • Publication number: 20130137900
    Abstract: Disclosed is a novel method of preparing a secondary amine compound using a microflow reactor. According to the method, a primary amine compound and a halide compound are allowed to react with each other in the microflow reactor, such that the production of a tertiary amine compound or an ammonium salt is minimized, whereby the secondary amine compound is efficiently prepared.
    Type: Application
    Filed: February 1, 2011
    Publication date: May 30, 2013
    Applicant: UNIVERSITY-INDUSTRY COOPERATION GROUP OF KYUNGHEE UNIVERSITY
    Inventors: Jin-Hyun Jeong, Han-Seo Moon, Liu-Lan Shen, Yong-Sung Choi