Morpholines (i.e., Fully Hydrogenated 1,4-oxazines Patents (Class 544/106)
  • Patent number: 10450261
    Abstract: The present invention relates to a method for the reductive amination of a carbonyl compound, comprising one or more carbonyl groups amenable to reductive amination, forming the corresponding primary amine, characterized in that the reaction is carried out in the presence of a homogeneously dissolved catalyst complex K, comprising at least one metal atom from Group 8, 9 or 10 of the periodic table, bearing a bidentate phosphane ligand, a carbonyl ligand, a neutral ligand and a hydride ligand, and also an acid as co-catalyst.
    Type: Grant
    Filed: May 27, 2016
    Date of Patent: October 22, 2019
    Assignee: BASF SE
    Inventors: Thomas Schaub, Joan Gallardo Donaire, Martin Ernst
  • Patent number: 10435380
    Abstract: Reaction products of primary and secondary diamines and bisanhydrides are included as additives in metal electroplating baths. The metal electroplating baths have good throwing power and deposit metal layers having substantially planar surfaces. The metal plating baths may be used to deposit metal on substrates with surface features such as through-holes and vias.
    Type: Grant
    Filed: October 11, 2018
    Date of Patent: October 8, 2019
    Assignees: Rohm and Haas Electronic Materials LLC, Dow Global Technologies LLC
    Inventors: Lingli Duan, Chen Chen, Shaoguang Feng, Zukhra I. Niazimbetova, Maria Anna Rzeznik
  • Patent number: 10370254
    Abstract: A process for obtaining borazane (NH3—BH3) includes introducing anhydrous liquid ammonia (NH3(l)) into a reactor thermostatically regulated to between a temperature ?1 and 40° C.; introducing, with stirring, into the reactor an amine borane complex (Am.BH3), the corresponding amine (Am) of which is soluble in anhydrous liquid ammonia only to a proportion of less than 10 g in 100 g of ammonia at 20° C., being introduced in an amount such that the mole ratio R=(NH3(l))/(Am.BH3) is greater than or equal to 5; stirring the mixture; stopping the stirring to obtain two demixed phases: a light phase constituted essentially of a solution of anhydrous liquid ammonia (NH3(l)) containing borazane; and a heavy phase constituted essentially of the amine corresponding to the amine borane complex introduced; isolating the borazane and drying under vacuum thereof; the temperature ?1 being greater than or equal to the melting point of the amine borane complex.
    Type: Grant
    Filed: May 22, 2015
    Date of Patent: August 6, 2019
    Assignees: AIRBUS SAFRAN LAUNCHERS SAS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE CLAUDE BERNARD LYON I
    Inventors: Guy M. Jacob, Henri R. Delalu, Ahmad A. El Hajj
  • Patent number: 10280149
    Abstract: The present invention relates to compounds useful as inhibitors of one or more histone demethylses, such as KDM2b. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
    Type: Grant
    Filed: July 7, 2017
    Date of Patent: May 7, 2019
    Assignees: GENENTECH, INC., CONSTELLATION PHARMACEUTICALS, INC.
    Inventors: Brian K. Albrecht, Alexandre Cote, Victor Gehling, Vickie Hsiao-Wei Tsui, James Richard Jr. Kiefer, Jun Liang, Steven Magnuson, Christopher G. Nasveschuk, Richard Pastor, F. Anthony Romero, Alexander M. Taylor, Birong Zhang
  • Patent number: 10166216
    Abstract: Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Grant
    Filed: May 5, 2016
    Date of Patent: January 1, 2019
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Jing Zhang, Catherine Sylvain, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding
  • Patent number: 10106512
    Abstract: Reaction products of primary and secondary diamines and bisanhydrides are included as additives in metal electroplating baths. The metal electroplating baths have good throwing power and deposit metal layers having substantially planar surfaces. The metal plating baths may be used to deposit metal on substrates with surface features such as through-holes and vias.
    Type: Grant
    Filed: April 28, 2015
    Date of Patent: October 23, 2018
    Assignees: Dow Global Technologies LLC, Rohm and Haas Electronic Materials LLC
    Inventors: Lingli Duan, Chen Chen, Shaoguang Feng, Zukhra I. Niazimbetova, Maria Anna Rzeznik
  • Patent number: 10016438
    Abstract: The present disclosure relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR4 enzyme and are useful in the treatment of FGFR4-associated diseases such as cancer.
    Type: Grant
    Filed: September 22, 2017
    Date of Patent: July 10, 2018
    Assignee: Incyte Corporation
    Inventors: Liang Lu, Liangxing Wu, Bo Shen, Wenqing Yao
  • Patent number: 9908894
    Abstract: The present invention relates to novel methods for the preparation of 1,3-benzodioxole heterocyclic compounds and intermediates for the same. The compounds are useful as PDE4 inhibitors.
    Type: Grant
    Filed: June 22, 2015
    Date of Patent: March 6, 2018
    Assignee: LEO Pharma A/S
    Inventors: Bjorn Metzler, Andre Faldt
  • Patent number: 9873710
    Abstract: The invention relates to compounds of use as targeted cytotoxic agents and methods of use thereof. In particular, the invention relates to prodrugs that are substantially resistant to human AKR1C3 enzyme metabolism, methods of cell ablation using said compounds and methods of treatment of cancer and other hyperproliferative disorders using said compounds.
    Type: Grant
    Filed: October 31, 2016
    Date of Patent: January 23, 2018
    Assignee: Health Innovation Ventures B.V.
    Inventors: Jeffrey Bruce Smaill, Adam Vorn Patterson, Amir Ashoorzadeh, Christopher Paul Guise, Alexandra Marie Mowday, David Francis Ackerley, Elsie May Williams, Janine Naomi Copp
  • Patent number: 9845300
    Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: February 17, 2017
    Date of Patent: December 19, 2017
    Assignee: ADVERIO PHARMA GMBH
    Inventor: Peter Fey
  • Patent number: 9801889
    Abstract: The present disclosure relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR4 enzyme and are useful in the treatment of FGFR4-associated diseases such as cancer.
    Type: Grant
    Filed: January 17, 2017
    Date of Patent: October 31, 2017
    Assignee: Incyte Corporation
    Inventors: Liang Lu, Liangxing Wu, Bo Shen, Wenqing Yao
  • Patent number: 9745332
    Abstract: There is provided a process for the reduction of one or more amide moieties in a compound comprising contacting the compound with hydrogen gas and a transition metal catalyst in the presence or absence of a base under conditions for the reduction an amide bond. The presently described processes can be performed at low catalyst loading using relatively mild temperature and pressures, and optionally, in the presence or absence of a base or high catalyst loadings using low temperatures and pressures and high loadings of base to effect dynamic kinetic resolution of achiral amides.
    Type: Grant
    Filed: July 18, 2012
    Date of Patent: August 29, 2017
    Assignee: The Governors of the Univerity of Alberta
    Inventors: Steven Bergens, Jeremy M. John
  • Patent number: 9663446
    Abstract: Disclosed is a process for preparing a primary, a secondary or a tertiary amine via the direct amination of an alcohol in the presence of a catalyst. The catalyst is composed of palladium or a palladium compound and a cerium oxide supporter.
    Type: Grant
    Filed: October 15, 2013
    Date of Patent: May 30, 2017
    Assignees: RHODIA OPERATIONS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Zhen Yan, Mohamad Ousmane, Marc Pera-Titus, Floryan DeCampo
  • Patent number: 9617229
    Abstract: Provided herein are compounds and prodrugs and methods of preparation of compounds and prodrugs that are capable of functioning as releasers and/or uptake inhibitors of one or more monoamine neurotransmitters, including dopamine, serotonin, and norepinephrine. Also provided are pharmaceutical compositions comprising one or more of these compounds or prodrugs, which may further comprise one or more additional therapeutic agents. Also provided are methods of treatment of various conditions that may be responsive to modification of monoamine neurotransmitter levels, such as pre-obesity, obesity, addiction, and depression.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: April 11, 2017
    Assignees: Research Triangle Institute, The United States of America, As Represented by the Secretary Department of Health and Human Services
    Inventors: Bruce E. Blough, Richard Rothman, Antonio Landavazo, Kevin M. Page, Ann Marie Decker
  • Patent number: 9580438
    Abstract: The invention relates to a compound of the general formula (I) or a physiologically functional derivative, solvate or salt thereof, wherein A, X, L, Y, R, and RN are as defined herein. The invention further relates to the use of the compounds of formula (I) as a medicament, a pharmaceutical composition comprising them, a method of treatment or prevention of a medical condition entailing the administration thereof, and the use thereof in the manufacture of a medicament for the treatment or prevention of a medical condition, particularly autoimmune inflammatory disorders, CNS disorders, sleeping disorders, or proliferative diseases including cancer. The invention further relates to a specific process for the preparation of said compounds.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: February 28, 2017
    Assignee: 4SC DISCOVERY GMBH
    Inventors: Johann Leban, Mirko Zaja
  • Patent number: 9540384
    Abstract: The invention relates to compounds of formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
    Type: Grant
    Filed: November 26, 2014
    Date of Patent: January 10, 2017
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Christian Lerner
  • Patent number: 9522873
    Abstract: The present invention relates to a novel biphenyl derivative or a pharmaceutically acceptable salt thereof, a pharmaceutical composition for preventing or treating inflammatory diseases or autoimmune diseases comprising the same as an active ingredient, and methods for treating inflammatory disease or autoimmune diseases with the pharmaceutical composition. Novel biphenyl derivatives according to the present invention promote the phagocytosis of macrophages and inhibit the chemotaxis to exhibit excellent inflammation terminating and anti-inflammatory effects and thus can be effectively used as therapeutic agents for inflammatory diseases or autoimmune diseases.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: December 20, 2016
    Assignee: Dongguk University Industry-Academic Cooperation Foundation
    Inventors: Chang Hoon Lee, Kyeong Lee
  • Patent number: 9505791
    Abstract: The invention relates to compounds of use as targeted cytotoxic agents and methods of use thereof. In particular, the invention relates to prodrugs that are substantially resistant to human AKR1C3 enzyme metabolism, methods of cell ablation using said compounds and methods of treatment of cancer and other hyperproliferative disorders using said compounds.
    Type: Grant
    Filed: August 22, 2013
    Date of Patent: November 29, 2016
    Assignee: Health Innovation Ventures B.V.
    Inventors: Jeffrey Bruce Smaill, Adam Vorn Patterson, Amir Ashoorzadeh, Christopher Paul Guise, Alexandra Marie Mowday, David Francis Ackerley, Elsie May Williams, Janine Naomi Copp
  • Patent number: 9493411
    Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, and R10 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: November 15, 2016
    Assignee: AbbVie Inc.
    Inventors: Lisa A. Hasvold, John Pratt, Keith F. McDaniel, George S. Sheppard, Dachun Liu, Steven W. Elmore, Robert D. Hubbard
  • Patent number: 9309187
    Abstract: The compounds of formula (1) in which R1, R4, A and X have the meanings as given in the description, are novel effective EP2 agonists.
    Type: Grant
    Filed: April 30, 2013
    Date of Patent: April 12, 2016
    Assignee: Takeda GmbH
    Inventors: Angelika Hoffmeyer, Rainer Boer, Manuela Hessmann, Andreas Pahl, Torsten Dunkern, Simone Hartung, Christof Zitt, Jurgen Volz, Christiane Praechter, Mahindra Makhija, Hiteshkumar Jain, Sandip Gavade, Arati Prabhu, Manojkumar Tiwari, Ashish Keche, Sarvesh Patel
  • Patent number: 9290536
    Abstract: Disclosed herein are novel C4-monomethyl triterpenoid compounds and derivatives thereof, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example as antioxidant inflammation modulators, and compositions thereof are also provided.
    Type: Grant
    Filed: March 12, 2012
    Date of Patent: March 22, 2016
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Christopher F. Bender, Xiaofeng Liu, Xin Jiang, Melean Visnick
  • Patent number: 9040690
    Abstract: The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: July 21, 2011
    Date of Patent: May 26, 2015
    Assignee: Novartis AG
    Inventors: David Barnes, Scott Louis Cohen, Jiping Fu, Lei Shu, Rui Zheng
  • Patent number: 9040528
    Abstract: The present invention relates to compounds of Formula (I): to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.
    Type: Grant
    Filed: January 13, 2014
    Date of Patent: May 26, 2015
    Assignee: AstraZeneca AB
    Inventors: Kevin Barvian, Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Irene Hauck, Fei Zhou
  • Patent number: 9034219
    Abstract: Described herein are compounds generally comprising an indeno[2?,3?:3,4]naptho[1,2-b]pyran structure. Such compounds may be useful for their photochromic properties, and be used in certain photochromic compositions. Such compositions may further comprise other photochromic compositions and/or materials. Additionally, such compounds and/or compositions may be suitable for preparing certain photochromic articles. Also described herein are methods for preparing certain photochromic compounds, compositions, and articles.
    Type: Grant
    Filed: December 7, 2011
    Date of Patent: May 19, 2015
    Assignee: Transitions Optical, Inc.
    Inventors: Meng He, Darrin R. Dabideen, Xiao-Man Dai, Wenjing Xiao, Ruisong Xu, Sujit Mondal, Anil Kumar, Anu Chopra
  • Patent number: 9029532
    Abstract: The present invention relates to naphthopyran compounds that include at least one compound represented by the following Formulas (I), (II), and (III): With reference to Formulas (I), (II), and (III), there is the proviso that: (i) at least one R1 is a group L; and/or (ii) B and/or B? is substituted with at least one group L. The group L can be described as a lengthening group. The present invention also relates to photochromic-dichroic naphthopyran compounds and photochromic-dichroic articles containing such compounds.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: May 12, 2015
    Assignee: Transitions Optical, Inc.
    Inventors: Darrin R. Dabideen, Meng He, Anil Kumar
  • Publication number: 20150126511
    Abstract: The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
    Type: Application
    Filed: September 30, 2014
    Publication date: May 7, 2015
    Inventors: Liming SHAO, Fengjiang WANG, Scott Christopher MALCOLM, Michael Charles HEWITT, Larry R. BUSH, Jianguo MA, Mark A. VARNEY, Una CAMPBELL, Sharon Rae ENGEL, Larry Wendell HARDY, Patrick KOCH, John E. CAMPBELL
  • Patent number: 9018374
    Abstract: Provision of crystal of 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride which has a superior rennin inhibitory activity and is useful as a prophylactic or therapeutic agent for hypertension and various organ disorders caused by hypertension, and the like. Crystal of 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride having an X-ray powder diffraction pattern showing characteristic peaks at interplanar spacings (d) of around 26.43±0.2, 7.62±0.2 and 4.32±0.2 angstroms.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: April 28, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventor: Masato Kitayama
  • Patent number: 9006426
    Abstract: The present application discloses novel squaric acid derivatives of the formula A: from —C(?O)—, —S(?O)2—, —C(?S)— and —P(?O)(R5)—; B: -, —O—, —NR6— and —C(?O)—NR6—; D: -, —O—, —CR7R8— and —NR9; m=0-12; n=0-12; m+n=1-20; p=0-2; R1: heteroaryl, aryl; R2: H, C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; R3: C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; or R2 and R3: N-containing heterocyclic/heteroaromatic ring; R4 and R4*: H, C1-12-alkyl, C1-12-alkenyl; and pharmaceutically acceptable salts and prodrugs thereof, and their use in the treatment of diseases/conditions caused by an elevated level of NAMPRT (inflammatory and tissue repair disorders, particularly rheumatoid arthritis, inflammatory bowel disease, asthma and CPOD, osteoarthritis, osteoporosis and fibrotic diseases; dermatosis; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankyl
    Type: Grant
    Filed: June 24, 2009
    Date of Patent: April 14, 2015
    Assignee: Topotarget A/S
    Inventors: Mette Knak Christensen, Fredrik Bjorkling
  • Patent number: 9000154
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: October 17, 2011
    Date of Patent: April 7, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Thomas Martin Kirrane, Daniel Richard Marshall, Robert Sibley, Roger John Snow, Fariba Soleymanzadeh, Ronald John Sorcek
  • Patent number: 8993611
    Abstract: The invention relates to a family of stable polyamine arylethylamide compounds, and to the use of these compounds as agents inhibiting DNA damages induced by by-products of the non-enzymatic glycosylation of skin tissues. The invention also relates to cosmetic or dermocosmetic compositions intended to fight skin disorders associated with said glycosylation by-products.
    Type: Grant
    Filed: July 1, 2013
    Date of Patent: March 31, 2015
    Assignee: Exsymol
    Inventor: Marie-Christine Seguin
  • Publication number: 20150083223
    Abstract: A fullerene derivative represented by the following formula (1): wherein “FLN” represents a fullerene core, R1 represents an optionally substituted C1-C24 alkyl group or an optionally substituted C7-C24 aralkyl group, R2 and R3 independently represent a hydrogen atom or an optionally substituted C1-C24 hydrocarbon group but excluding a case where both of R2 and R3 are hydrogen atoms, and R2 and R3 may combine together to form a ring.
    Type: Application
    Filed: September 25, 2013
    Publication date: March 26, 2015
    Applicants: Tohoku University, Showa Denko K.K.
    Inventors: Tienan JIN, Weili Si, Yoshinori Yamamoto, Takeshi Igarashi
  • Patent number: 8981119
    Abstract: The present invention is directed to compounds of Formula I: wherein R1, R2, R3, R4, R5, X and n are described herein. These compounds and their pharmaceutically acceptable salts thereof are useful as IK1 channel activators.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: March 17, 2015
    Assignee: Astellas Pharma Inc.
    Inventors: Tsukasa Ishihara, Kazuhiro Ikegai, Ikumi Kuriwaki, Hiroyuki Hisamichi, Nobuaki Takeshita, Ryuichi Takezawa
  • Patent number: 8962624
    Abstract: A method of inhibiting formation of cancerous metabolites, of inhibiting cytochrome P450 2A13 from forming carcinogen metabolites, and/or inhibiting formation of cancerous lung cells in a subject can include: providing a morpholine compound that selectively interacts with cytochrome P450 2A13 over cytochrome P450 2A6; administering a therapeutically effective amount of the morpholine compound or derivative to the subject. The morpholine compound or derivative can be substantially more selective for interacting with the cytochrome P450 2A13 over the cytochrome P450 2A6. The morpholine compound or derivative can also be substantially non-interactive with other physiological components. The morpholine compound or derivative can include a structure that selectively interacts with cytochrome P450 2A13 over cytochrome P450 2A6, such as Compounds 1-34 of Formulas A-D.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: February 24, 2015
    Assignee: University of Kansas
    Inventors: Emily Scott, Anuradha Roy
  • Publication number: 20150011755
    Abstract: The present application relates to amine salts of prostaglandin analogs and their uses for the preparation of substantially pure prostaglandin analogs. Specific embodiments relate to amine salts of tafluprost and their uses for the preparation of substantially pure tafluprost.
    Type: Application
    Filed: February 6, 2013
    Publication date: January 8, 2015
    Applicant: DR. REDDYS LABORATORIES LIMITED
    Inventor: Mark P Jackson
  • Patent number: 8912361
    Abstract: Process for preparing primary amines which have at least one functional group of the formula (—CH2—NH2) and at least one further primary amino group by alcohol amination of starting materials having at least one functional group of the formula (—CH2—OH) and at least one further functional group (—X), where (—X) is selected from among hydroxyl groups and primary amino groups, by means of ammonia with elimination of water, wherein the reaction is carried out homogeneously catalyzed in the presence of at least one complex catalyst comprising at least one element selected from groups 8, 9 and 10 of the Periodic Table and also at least one donor ligand.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: December 16, 2014
    Assignee: BASF SE
    Inventors: Thomas Schaub, Boris Buschhaus, Marion Kristina Brinks, Mathias Schelwies, Rocco Paciello, Johann-Peter Melder, Martin Merger
  • Patent number: 8907084
    Abstract: The invention relates to a process for the production of 2AEE with selectivity towards 2AEE being significantly higher i.e. the ratio of 2AEE:morpholine >3. DEG and Ammonia are reacted in a continuous mode in hydrogen atmosphere in the presence of a catalyst at temperature of 150° C. to 250° C. and pressure of 10 Bar to 20 Bar, the products being separated by distillation. The catalyst used is metal and its oxide or metal oxide on silica or alumina support. The molar ratio of ammonia:DEG is >20 and the molar ratio of hydrogen:DEG is >1, preferably 1-30. The reactants are optionally fed in a downward flow mode. The catalyst charged into the reactor has metal and its oxide or metal oxide equivalent to a metal content of 10% to 70% on the support.
    Type: Grant
    Filed: September 14, 2010
    Date of Patent: December 9, 2014
    Assignee: Alkyl Amines Chemicals Ltd.
    Inventors: Sameer Sharad Katdare, Prasanna Krishna Somalwar, Vishwanathan Ramaswamy, Saimani Srinivasan
  • Patent number: 8877971
    Abstract: The present invention relates to a method for preparing formamide compounds using carbon dioxide, and to the use of said method for manufacturing vitamins, pharmaceutical products, adhesives, acrylic fibers, synthetic leathers, pesticides and fertilizers. The invention also relates to a method for manufacturing vitamins, pharmaceutical products, adhesives, acrylic fibers, synthetic leathers, pesticides and fertilizers which includes a step of preparing formamide compounds by the method according to the invention.
    Type: Grant
    Filed: April 4, 2012
    Date of Patent: November 4, 2014
    Assignee: Commissariat a l'Energie Atomique et aux Energies Alternatives
    Inventors: Thibault Cantat, Christophe Gomes, Olivier Jacquet
  • Patent number: 8877753
    Abstract: The invention relates to the use of a group of sigma receptor ligands of formula (I) for the potentiation of the analgesic effect of opioids and opiates and at the same time for decreasing the dependency induced by them.
    Type: Grant
    Filed: April 24, 2009
    Date of Patent: November 4, 2014
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Helmut Heinrich Buschmann, Jose Miguel Vela Hernandez, Daniel Zamanillo-Castanedo
  • Publication number: 20140315926
    Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: July 1, 2014
    Publication date: October 23, 2014
    Inventor: Peter FEY
  • Patent number: 8865893
    Abstract: A method for preparing 2-morpholinoisobornane-10-thiol is disclosed, which has simplified steps and avoids the use of Na metal. Accordingly, it is advantageous to apply the method in a mass production.
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: October 21, 2014
    Assignee: National Tsing Hua University
    Inventors: Biing-Jiun Uang, Yu-Han Tsao, Ping-Yu Wu
  • Patent number: 8859765
    Abstract: The present invention provides efficient and economical methods for synthesis of (?)-2-exo-morpholinoisoborne-10-thiol, its enantiomer, and related chiral catalysts. Novel compounds and methods of asymmetric synthesis are also disclosed.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: October 14, 2014
    Assignee: ScinoPharm Taiwan, Ltd.
    Inventors: Ping-Yu Wu, Julian Paul Henschke
  • Patent number: 8853390
    Abstract: The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceutical compositions comprising the compounds and salts; and method of using such compositions. The chiral cyclopropyl amine derivatives are useful for binding to histamine H3 receptor sites and for providing therapeutic agents for histamine H3 mediated disease.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: October 7, 2014
    Assignee: AbbVie Inc.
    Inventors: Yi-Yin Ku, Timothy A. Grieme, Jeffrey M. Kallemeyn, Mathew M. Mulhern
  • Publication number: 20140227161
    Abstract: An organosolv process for producing bio-products by decomposing lignocellulosic materials comprises providing an initial lignin solvent with water, an acid, and a lignin dissolving chemical comprising at least one of an organic ester, butyl acetate, an organic furan, and furfural. The process also includes placing the lignin solvent in contact with a biomass to form a circulation solvent, and recycling at least a portion of the circulation solvent by circulating the circulation solvent back into contact with the biomass. The circulating of the circulation solvent occurs for a period of time, after which, the process then includes separating material such as chemicals and lignin from the circulation solvent. The chemicals can be recycled as new solvent or sold while lignin can be used as natural and renewable colorant for polymers such as poly lactic acid.
    Type: Application
    Filed: February 11, 2013
    Publication date: August 14, 2014
    Applicant: AMERICAN SCIENCE AND TECHNOLOGY CORPORATION
    Inventors: Ali Manesh, Reza Hemyeri, Susanta Mohapatra, John Guenther, Edwin Zoborowski, Mohammad Ali Manesh
  • Patent number: 8796267
    Abstract: This invention relates to novel N-[[3-[3-Fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]-acetamide derivatives, their acceptable acid addition salts, solvates and hydrates. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by antimicrobial agents.
    Type: Grant
    Filed: June 17, 2008
    Date of Patent: August 5, 2014
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Roger Tung, Scott Harbeson
  • Patent number: 8785693
    Abstract: Process for the preparation of primary amines which have at least one functional group of the formula (—CH2—NH2) by alcohol amination of starting materials which have at least one functional group of the formula (—CH2—OH), with ammonia, with the elimination of water, where the alcohol amination is carried out under homogeneous catalysis in the presence of at least one complex catalyst which comprises at least one element selected from groups 8 and 9 of the Periodic Table of the Elements, and also at least one phosphorus donor ligand of the general formula (I).
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: July 22, 2014
    Assignee: BASF SE
    Inventors: Thomas Schaub, Boris Buschhaus, Marion Kristina Brinks, Mathias Schelwies, Rocco Paciello, Johann-Peter Melder, Martin Merger
  • Publication number: 20140163225
    Abstract: There is provided a process for the reduction of one or more amide moieties in a compound comprising contacting the compound with hydrogen gas and a transition metal catalyst in the presence or absence of a base under conditions for the reduction an amide bond. The presently described processes can be performed at low catalyst loading using relatively mild temperature and pressures, and optionally, in the presence or absence of a base or high catalyst loadings using low temperatures and pressures and high loadings of base to effect dynamic kinetic resolution of achiral amides.
    Type: Application
    Filed: July 18, 2012
    Publication date: June 12, 2014
    Applicant: THE GOVERNORS OF THE UNIVERSITY OF ALBERTA
    Inventors: Steven Bergens, Jeremy M. John
  • Patent number: 8729073
    Abstract: The invention relates to pyrazole derivatives of formula I having pharmacological activity and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and/or prophylaxis of pain.
    Type: Grant
    Filed: December 2, 2011
    Date of Patent: May 20, 2014
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Antoni Torrens Jover, María Rosa Cuberes-Altisent
  • Patent number: 8658641
    Abstract: The present invention relates to compounds of Formula (I); to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.
    Type: Grant
    Filed: October 13, 2009
    Date of Patent: February 25, 2014
    Assignee: AstraZeneca AB
    Inventors: Kevin Barvian, Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Irene Hauck, Fei Zhou
  • Publication number: 20140045851
    Abstract: A method of inhibiting formation of cancerous metabolites, of inhibiting cytochrome P450 2A13 from forming carcinogen metabolites, and/or inhibiting formation of cancerous lung cells in a subject can include: providing a morpholine compound that selectively interacts with cytochrome P450 2A13 over cytochrome P450 2A6; administering a therapeutically effective amount of the morpholine compound or derivative to the subject. The morpholine compound or derivative can be substantially more selective for interacting with the cytochrome P450 2A13 over the cytochrome P450 2A6. The morpholine compound or derivative can also be substantially non-interactive with other physiological components. The morpholine compound or derivative can include a structure that selectively interacts with cytochrome P450 2A13 over cytochrome P450 2A6, such as Compounds 1-34 of Formulas A-D.
    Type: Application
    Filed: October 21, 2013
    Publication date: February 13, 2014
    Applicant: University of Kansas
    Inventors: Emily Scott, Anuradha Roy
  • Patent number: 8648201
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R7 and Y have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumors and for the treatment of inflammatory diseases.
    Type: Grant
    Filed: June 17, 2010
    Date of Patent: February 11, 2014
    Assignee: MERCK PATENT GmbH
    Inventors: Michel Calderini, Margarita Wucherer-Plietker, Ulrich Graedler, Christina Esdar