The Nitrogen Is Attached Directly To Carbon By A Double Or Triple Bond Patents (Class 549/442)
  • Patent number: 9096498
    Abstract: The present invention discloses a cheaper and practical protocol for the construction of a wide variety of o-cyanocinnamonitrile and their structural analogs that proceeds with good yields in a single step using CuCN as the only reagent.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: August 4, 2015
    Assignee: Council of Scientific & Industrial Research
    Inventors: Brij Bhushan Ahuja, Reddy S. Rekula, Arumugam Sudalai
  • Publication number: 20150133495
    Abstract: Disclosed herein is a compound of Formula I or a pharmaceutically acceptable salt thereof, in which A, G, R1 and R2 are as defined herein. The compounds and pharmaceutical compositions of the compounds are suitable for the treatment of HCV infection in mammals and are also useful to modulate or inhibit NS3/4 dimerization.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 14, 2015
    Inventor: Daniel Lamarre
  • Publication number: 20150031899
    Abstract: The present invention discloses a cheaper and practical protocol for the construction of a wide variety of o-cyanocin-namonitrile and their structural analogues that proceeds with good yields in a single step using CuCN as the only reagent.
    Type: Application
    Filed: March 7, 2013
    Publication date: January 29, 2015
    Inventors: Brij Bhushan Ahuja, Reddy Santosh Rekula, Arumugam Sudalai
  • Publication number: 20140341986
    Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
    Type: Application
    Filed: August 4, 2014
    Publication date: November 20, 2014
    Inventors: Alain D. Baron, Mark S. Fineman, Nigel R.A. Beeley
  • Publication number: 20140192305
    Abstract: The present invention relates to photoreactive compounds that are particularly useful in materials for the alignment of liquid crystals.
    Type: Application
    Filed: August 7, 2012
    Publication date: July 10, 2014
    Applicant: ROLIC AG
    Inventors: Frederic Lincker, Izabela Bury S. Pires, Sabrina Chappellet, Patricia Scandiucci De Freitas, Mohammed Ibn-Elhaj, Qian Tang, Satish Palika, Masato Hoshino, Jean-Francois Eckert
  • Publication number: 20140107247
    Abstract: The invention provides a polymerizable compound represented by formula (I), a polymerizable composition, and a polymer that have a practical low melting point, can be produced at low cost, and can produce an optical film that achieves uniform conversion of polarized light over a wide wavelength band, and an optically anisotropic article.
    Type: Application
    Filed: April 12, 2012
    Publication date: April 17, 2014
    Applicant: ZEON CORPORATION
    Inventors: Kei Sakamoto, Kumi Okuyama
  • Patent number: 8648071
    Abstract: The present invention relates to substituted hydrazonamide compounds. The invention further relates to methods of inhibiting the activity of Hs?90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted hydrazonamide compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Grant
    Filed: June 26, 2009
    Date of Patent: February 11, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Joseph Burlison, Dinesh U. Chimmanamada, Weiwen Ying, Shijie Zhang, David James
  • Patent number: 8642647
    Abstract: The present invention provides an N1-benzo[1,3]dioxol-5-ylmethyl-N2-substituted biguanide derivative of formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing same, and a pharmaceutical composition comprising same as an active ingredient. The inventive N1-benzo[1,3]dioxol-5-ylmethyl-N2-substituted biguanide derivative exhibits improved blood glucose level- and lipid level-lowering effects even with a reduced dosage as compared to conventional drugs, and thus, it is useful for preventing or treating diabetes, metabolic syndromes such as insulin-independent diabetes, obesity and atherosclerosis, or a P53 gene defect-related cancer.
    Type: Grant
    Filed: October 13, 2009
    Date of Patent: February 4, 2014
    Assignees: Hanall Biopharma Co., Ltd., Korea Research Institute of Chemical Technology
    Inventors: Sung Wuk Kim, Sung Soo Jun, Hyae Gyeong Cheon, Kwang Rok Kim, Sang Dal Rhee, Won Hoon Jung, Jong Cheol Lee
  • Patent number: 8536157
    Abstract: The present invention relates to non-steroidal compounds useful in the treatment of inflammatory conditions and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: April 14, 2008
    Date of Patent: September 17, 2013
    Assignee: The University of Melbourne
    Inventors: Alastair Stewart, Martin Banwell, Brenda Leung, Anu Augustine, Jacki Kitching, Thomasz Bilski
  • Publication number: 20130095140
    Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
    Type: Application
    Filed: July 11, 2012
    Publication date: April 18, 2013
    Applicant: Elcelyx Therapeutics, Inc.
    Inventors: Alain D. Baron, Mark S. Fineman, Nigel R. A. Beeley
  • Publication number: 20120302563
    Abstract: Described herein are substituted norindenoisoquinoline compounds, and pharmaceutical compositions and formulations comprising the norindenoisoquinoline compounds. Also described herein are methods for using the compounds for the treatment and/or prevention of topoisomerase mediated diseases, such as cancer.
    Type: Application
    Filed: January 27, 2011
    Publication date: November 29, 2012
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventors: Mark S. Cushman, Yunlong Song
  • Publication number: 20120046255
    Abstract: The present invention relates to non-steroidal compounds useful in the treatment of inflammatory conditions and pharmaceutical compositions comprising them.
    Type: Application
    Filed: April 14, 2008
    Publication date: February 23, 2012
    Applicant: THE UNIVERSITY OF MELBOURNE of ROYAL PARADE PARKVILLE
    Inventors: Alastair Stewart, Martin Banwell, Brenda Leung, Anu Augustine, Jacki Kitching, Tomasz Bilski
  • Publication number: 20120046288
    Abstract: The present invention relates to substituted hydrazonamide compounds. The invention further relates to methods of inhibiting the activity of Hs?90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted hydrazonamide compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: June 26, 2009
    Publication date: February 23, 2012
    Inventors: Joseph A. Burlison, Dinesh U. Chimmanamada, Weiwen Ying, Shijie Zhang, David James
  • Publication number: 20110263567
    Abstract: The present invention relates to compounds of general formula (i) having an oxime moiety or a pharmaceutically acceptable salt, hydrate or solvate thereof and its use for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1), a pharmaceutical composition comprising the compound or a salt, hydrate or solvate thereof as an active ingredient, a method for the prevention or the treatment of a SSAO/VAP-1 related disease, said diseases including acute or chronic inflammatory diseases, diseases related to carbohydrate metabolism, diabetes-associated complications, diabetic retinopathy and macular oedema, diseases related to adipocyte or smooth muscle dysfunctions, neurodegenerative diseases and vascular diseases.
    Type: Application
    Filed: September 11, 2009
    Publication date: October 27, 2011
    Applicant: Semmelweis Egyetem
    Inventors: Péter Mátyus, Kálmán Magyar, Marjo Pihlavisto, Klára Gyires, Norbert Haider, Yinghua Wang, Patrick Woda, Petra Dunkel, Éva Tóth-Sarudy, Gÿorgy Túrós
  • Patent number: 7855309
    Abstract: The present invention relates to benzyloxy- and phenethyl-substituted phenyl-amidine derivatives of formula (I) wherein the substituents are as in the description, their process of preparation, their use as fungicide or insecticide active agents, particularly in the form of fungicide or insecticide compositions, and methods for the control of phytopathogenic fungi or damaging insects, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: September 12, 2006
    Date of Patent: December 21, 2010
    Assignee: Bayer CropScience AG
    Inventors: Klaus Kunz, Jörg Greul, Oliver Guth, Benoît Hartmann, Kerstin Ilg, Wahed Ahmed Moradi, Thomas Seitz, Peter Dahmen, Arnd Voerste, Ulrike Wachendorff-Neumann, Mark Drewes, Ralf Dunkel, Ronald Ebbert, Olga Malsam, Eva-Maria Franken
  • Publication number: 20100184851
    Abstract: Compounds of formula (I) and (II) are provided as modulators of Rb:Raf-1 interactions which are potent, selective disruptors of Rb:Raf-1 binding. Therapeutic methods of using the compounds, for example for treating or ameliorating a cell proliferation disorder such as cancer, are provided.
    Type: Application
    Filed: August 31, 2009
    Publication date: July 22, 2010
    Applicant: University of South Florida
    Inventors: Said M. Sebti, Srikumar Chellappan, Nicholas James Lawrence
  • Patent number: 7741323
    Abstract: An indene derivative for selectively modulating the activities of peroxisome proliferator activated receptors (PPARs) having the following formula (I): wherein, R1 is C1-6 alkyl, C1-6 alkenyl, or C3-6 cycloalkyl, each of which is unsubstituted or substituted with one or more phenyl groups; R2 is H, CN, CO2Ra, CH2CO2Ra, CONRbRc, or phenyl; R3 is C1-6 alkyl, C3-6 cycloalkyl, naphthyl, phenyl, being each unsubstituted or substituted with one or more substituents selected from the group consisting of halogen, CN, NH2, NO2, ORa, phenyloxy, C1-6 alkyl, and C3-6 cycloalkyl; and R4, R5, R6, and R7 are each independently H, OH, OSO2CH3, O(CH2)mRe, CH2Rf, OCOCH2ORg, OCH2CH2ORg, OCH2CH?CHRg, or pyridine-2-yloxy, or R5 and R6 together form OCH2O.
    Type: Grant
    Filed: April 13, 2005
    Date of Patent: June 22, 2010
    Assignees: Korea Research Institute of Chemical Technology, Jeil Pharm. Co., Ltd., Korea Research Institute of Bioscience and Biotechnology, CJ Corp.
    Inventors: Hyae Gyeong Cheon, Sung-Eun Yoo, Sung Soo Kim, Sung-Don Yang, Kwang-Rok Kim, Sang Dal Rhee, Jin Hee Ahn, Seung Kyu Kang, Won Hoon Jung, Sung Dae Park, Nam Gee Kim, Jang Hyuk Lee, Sun Chul Huh, Jae Mok Lee, Seog Beom Song, Soon Ji Kwon, Jong Hoon Kim, Jeong-Hyung Lee, Seung Jun Kim
  • Patent number: 7470723
    Abstract: The present invention relates to Diphenylethylene Compounds and compositions comprising a Diphenylethylene Compound. The present invention also relates to methods for preventing or treating various diseases and disorders by administering to a subject in need thereof one or more Diphenylethylene Compounds. In particular, the invention relates to methods for preventing or treating cancer or an inflammatory disorder by administering to a subject in need thereof one or more Diphenylethylene Compounds. The present invention further relates to articles of manufacture and kits comprising one or more Diphenylethylene Compounds.
    Type: Grant
    Filed: September 3, 2004
    Date of Patent: December 30, 2008
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Faribourz Payvandi, Ling H. Zhang, Michael J. Robarge, Roger Chen, Hon-Wah Man, Alexander L. Ruchelman
  • Patent number: 7019024
    Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: March 28, 2006
    Assignee: Allelix Neuroscience Inc.
    Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
  • Patent number: 6444850
    Abstract: A fungicidal compound of formula (I) having a fluorovinyloxyphenyl moiety and stereoisomers thereof are useful for protecting crops from fungal diseases: wherein: X is CH or N; Y is O or S; Z is O or NH; R1 is hydrogen or CF3; and R2 is hydrogen, a C1-10 alkyl, naphthyl, thiophenyl or a phenyl group optionally carrying one or more substituents selected from the group consisting of C1-6 alkyl, halogen-substituted C1-6 alkyl, C1-6 alkoxy, phenoxy, halogen, and methylenedioxy radicals.
    Type: Grant
    Filed: February 8, 2000
    Date of Patent: September 3, 2002
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Chwang-Siek Pak, Bum-Tae Kim, No-Kyun Park, Gyung-Ja Choi, Heung-Tae Kim
  • Patent number: 6407100
    Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.
    Type: Grant
    Filed: September 1, 1993
    Date of Patent: June 18, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans Peter Isenring, Bettina Weiss
  • Patent number: 6355634
    Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 12, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans Peter Isenring, Bettina Weiss
  • Patent number: 6288071
    Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.
    Type: Grant
    Filed: December 10, 1998
    Date of Patent: September 11, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Henry Szczepanski, Martin Zeller, Ottmar Franz Hüter
  • Patent number: 6048893
    Abstract: This invention is directed to compounds of formula I ##STR1## wherein R.sup.1 is CN, CH.sub.2 CN, CH.dbd.CHCN, CHO, or CH.dbd.CHCO.sub.2 H;R.sup.2 is aryl lower alkoxy, heteroaryl lower alkoxy, aryl lower alkylthio or heteroaryl lower alkylthio wherein each of the aryl and heteroaryl moieties is optionally substituted;R.sup.3 is halogen;R.sup.4 is optionally substituted aryl or optionally substituted heteroaryl;R.sup.5 is carboxy or an acid isostere;X is oxygen or sulphur; andn is zero or 1; or an N-oxide thereof, prodrug thereof solvate thereof, or pharmaceutically acceptable salt thereof, which compounds have endothelin antagonist activity. The invention is also directed to methods for preparing the compounds of formula I and their pharmaceutical use.
    Type: Grant
    Filed: June 11, 1999
    Date of Patent: April 11, 2000
    Assignee: Rhone-Poulenc Rorer Limited
    Inventors: Christopher Smith, Barry Porter, Roger Walsh, Tahir Majid, Clive McCarthy, Neil Harris, Peter Astles, Iain McLay, Andrew Morley, Andrew Bridge, Andrew Van Sickle, Frank Halley, Alan Roach, Martyn Foster
  • Patent number: 5998667
    Abstract: The invention relates to new substituted biphenyloxazolines of the formula (I) ##STR1## in which R.sup.1 represents C.sub.1 -C.sub.6 -halogenoalkylthio andR.sup.2 represents hydrogen, orR.sup.1 and R.sup.2 together with the carbon atoms to which they are bonded form a halogen-substituted 5- or 6-membered heterocyclic ring,X represents hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.
    Type: Grant
    Filed: June 4, 1998
    Date of Patent: December 7, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhard Lantzsch, Albrecht Marhold, Christoph Erdelen
  • Patent number: 5919954
    Abstract: A process for stereoselectively forming N-substituted dihydro-2,3 benzodiazepines which are useful as AMPA receptor antagonists. The process includes an opening reduction step which sets the stereochemistry of the intermediates and the final compounds to the desired enantiomer. The reduction step may be carried out by an enzymatic reduction.
    Type: Grant
    Filed: April 14, 1997
    Date of Patent: July 6, 1999
    Assignee: Eli Lilly and Company
    Inventors: Benjamin A. Anderson, Marvin M. Hansen, David L. Varie, Jeffrey T. Vicenzi, Milton J. Zmijewski
  • Patent number: 5665878
    Abstract: A process for stereoselectively forming N-substituted dihydro-2,3 benzodiazepines which are useful as AMPA receptor antagonists. The process includes an opening reduction step which sets the stereochemistry of the intermediates and the final compounds to the desired enantiomer. The reduction step may be carried out by an enzymatic reduction.
    Type: Grant
    Filed: March 28, 1995
    Date of Patent: September 9, 1997
    Assignee: Eli Lilly and Company
    Inventors: Benjamin A. Anderson, Marvin M. Hansen, David L. Varie, Jeffrey T. Vicenzi, Milton J. Zmijewski
  • Patent number: 5616718
    Abstract: A compound having the formula: ##STR1## wherein W, X, Y, and Z are as defined in the specification is useful for making 2,4-diaminoquinazolines.
    Type: Grant
    Filed: April 20, 1995
    Date of Patent: April 1, 1997
    Assignee: FMC Corporation
    Inventors: Robert N. Henrie, II, Clinton J. Peake, Thomas G. Cullen, Walter H. Yeager, John W. Buser, James J. Fiordeliso, John A. Dixson
  • Patent number: 5493032
    Abstract: The reaction of 2,2-difluorobenzo-1,3-dioxole with (a) an alkali metal or an alkali metal compound and then (b) a compound R.sup.1 -Z.sup.1 in which Z.sup.
    Type: Grant
    Filed: March 6, 1995
    Date of Patent: February 20, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Ackermann, Hans-Ruedi Kanel, Bruno Schaub
  • Patent number: 5329023
    Abstract: The invention relates to a method of preparing optically active alcohols which consist substantially (at least 75% e.e.) or entirely of one enantiomer of formula 4 ##STR1## wherein R and A are as defined therein. The method comprises, which maintaining enantiomeric excess, converting an optically active cyanohydrin of formula 1 ##STR2## into optically active protected cyanohydrin of formula 2 ##STR3## converting the protected cyanohydrin of formula 2 into an optically active compound of formula 3 ##STR4## removing the protecting group B.
    Type: Grant
    Filed: June 15, 1992
    Date of Patent: July 12, 1994
    Assignee: Duphar International Research B.V.
    Inventors: Johannes Brussee, Arne Van Der Gen
  • Patent number: 5326785
    Abstract: Described are caffeic acid derivatives represented by the following formula: ##STR1## wherein either one of R.sup.1 and R.sup.2 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, a group --CO.sub.2 R.sup.4, or a group --CONR.sup.5 R.sup.6, R.sup.4, R.sup.5 and R.sup.6 being either a hydrogen atom or a particular group, and the other is the group --CO.sub.2 R.sup.4 or the group --CONR.sup.5 R.sup.6, or R.sup.1 and R.sup.2 are coupled together to represent a 5-membered ring so formed, Y represents a particular group or atom, X represents a substituted or unsubstituted C.sub.6 -C.sub.10 aryl, C.sub.7 -C.sub.12 aralkyl, heterocyclic or heterocyclic ring-alkyl group, m and n stand for particular integers, and R.sup.3 represents a hydrogen atom, a hydroxyl group, a group --OCO.sub.2 R.sup.7, R.sup.7 being a hydrogen atom or a particular group, or a group --OCONR.sup.8 R.sup.9, R.sup.8 representing a C.sub.1 -C.sub.6 alkyl group and R.sup.9 representing a hydrogen atom or a C.sub.1 -C.sub.
    Type: Grant
    Filed: March 31, 1993
    Date of Patent: July 5, 1994
    Assignee: Suntory Limited
    Inventors: Hidetsura Cho, Mie Tamaoka, Seiitsu Murota, Ikuo Morita
  • Patent number: 5321144
    Abstract: Described are p-methylenedioxyphenyl propionitrile and propiohydroxylamine derivatives defined according to the generic structure: ##STR1## wherein Z.sub.1 represents the moiety: ##STR2## and the moiety: ##STR3## and R.sub.1 is hydrogen or methyl and also having the generic structure: ##STR4## wherein X is HSO.sub.4.sup.-- ; SO.sub.4 ; .sup.= Cl.sup.-- ; Br.sup.-- ; PO.sub.4.sup..dbd. ; H.sub.2 PO.sub.4.sup.-- ; and HPO.sub.4.sup.= ; and the process of preparing these compounds.
    Type: Grant
    Filed: July 16, 1993
    Date of Patent: June 14, 1994
    Assignee: International Flavors & Fragrances Inc.
    Inventors: Anubhav P. S. Narula, John J. De Virgilio, Charles E. J. Beck, Marie R. Hanna, Jan T. Van Elst
  • Patent number: 5274133
    Abstract: Described are p-methylenedioxyphenyl propionitrile and prophiohydroxylamine derivatives defined according to the generic structure: ##STR1## wherein Z.sub.1 represents the moiety: ##STR2## and the moiety: ##STR3## and R.sub.1 is hydrogen or methyl and also having the generic structure; ##STR4## wherein X is HSO.sub.4.sup.- ; SO.sub.4 ; .sup.= Cl.sup.- ; BR.sup.- ; PO.sub.4 ; H.sub.2 PO.sub.4.sup.- ; and HPO.sub.4.
    Type: Grant
    Filed: January 21, 1993
    Date of Patent: December 28, 1993
    Assignee: International Flavors & Fragrances Inc.
    Inventors: Anubhav P. S. Narula, John J. De Virgilio, Charles E. J. Beck, Marie R. Hanna, Jan T. Van Elst
  • Patent number: 5246808
    Abstract: The present invention provides a hydrazone compound of the following general formula (I). This compound presents a higher hole mobility as compared with a conventional electric charge transferring material such as a conventional hydrazone compound or the like. Accordingly, when a photosensitive layer contains, as the electric charge transferring material, the hydrazone compound of the present invention, there can be obtained an electrophotosensitive material which is excellent in sensitivity and charging ability and has high repeating characteristics. ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 may be same as or different from one another, and each is a hydrogen atom, an alkyl group, an alkoxy group, an aralkyl group or an aryl group, each of said alkyl, alkoxy, aralkyl and aryl groups may have a substituent group; A.sup.1, A.sup.2, A.sup.3, A.sup.4, A.sup.5 and A.sup.
    Type: Grant
    Filed: March 12, 1992
    Date of Patent: September 21, 1993
    Assignee: Mita Industrial Co., Ltd.
    Inventors: Yasuyuki Hanatani, Hiroaki Iwasaki
  • Patent number: 5241087
    Abstract: A method of enantiomerically enriching chiral cyanohydrins is disclosed that involves selective cleavage of the unwanted enantiomer into its cleavage products HCN and the corresponding aldehyde or ketone by use of an enantioselective dehydrocyanation catalyst, coupled with simultaneous removal of at least one of the dehydrocyanation products.
    Type: Grant
    Filed: March 9, 1992
    Date of Patent: August 31, 1993
    Assignee: Bend Research, Inc.
    Inventor: Paul van Eikeren
  • Patent number: 5233057
    Abstract: Novel biphenyl derivatives of the formula: ##STR1## wherein R.sup.1 is a substituted or unsubstituted aminocarbonyl group, aminothiocarbonyl group, a substituted or unsubstituted lower alkoxycarbonyl group, cyano group, or a group of the formula: ##STR2## one or two of R.sup.2 to R.sup.7 are hydrogen atom, and the remaining groups are the same or different and are each a lower alkoxy group, a phenyl(lower)alkoxy group or hydroxy group, or the adjacent two groups thereof combine to form a lower alkylenedioxy group, and Alk.sup.1 is a lower alkylene group, or a pharmaceutically acceptable salt thereof, which are useful for the prophylaxis and treatment of hepatic diseases, and processes for preparing the same, and intermediates therefor.
    Type: Grant
    Filed: October 1, 1992
    Date of Patent: August 3, 1993
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Tameo Iwasaki, Kazuhiko Kondo, Yuzo Matsuoka, Mamoru Matsumoto, Masaki Sugiura
  • Patent number: 5118813
    Abstract: For the preparation of compounds such as ranitidine, niperotidine and cimetidine a urea of the formula:R.sub.1 --NH--C--NH--(CH.sub.2).sub.n --SD--S--(CH.sub.2).sub.n --NH--C--NH--R.sub.1 (I)which is synthesized by reaction with a compound of formula ##STR1##[H.sub.2 N--(CH.sub.2).sub.n --S--] (IX)is converted in a first stage into the corresponding bis-carbodiimideR.sub.1 --N.dbd.C.dbd.N--(CH.sub.2).sub.n --S--S--(CH.sub.2).sub.n --N.dbd.C.dbd.N--R.sub.1 (II)by reaction with triphenylphospine and bromine in the presence of a strong base and in a second stage the diimide thus obtained is reacted with nitromethane or a saline derivative of the cyanamide.The product thus obtained is reduced at the disulfide bridge obtaining a compound of formula: ##STR2## which is reacted with: ##STR3## to obtain ranitidine and niperotidine or cimetidine respectively depending on whether the first or the second of the described reactants is used.
    Type: Grant
    Filed: October 16, 1990
    Date of Patent: June 2, 1992
    Assignee: Biote kfarma Srl
    Inventor: Alberto Reiner
  • Patent number: 5075489
    Abstract: Unsaturated nitriles of the general formula I ##STR1## where R is a branched or straight-chain alkyl radical of 4 to 10 carbon atoms or a phenyl ring which is substituted by alkyl of 1 to 4 carbon atoms, one or more alkoxy groups of 1 to 3 carbon atoms, preferably 1 or 2 methoxy groups, or alkylenedioxy, preferably methylenedioxy, and their preparation and their use as scents.
    Type: Grant
    Filed: April 25, 1990
    Date of Patent: December 24, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerald Lauterbach, Rainer Becker, Klaas Jansen
  • Patent number: 5066673
    Abstract: Substituted benzyl 2-phenylalk(en)-1-ylcyclopropanecarboxylates of the general formula I ##STR1## where R.sup.1 is halogen or in each case low molecular weight, alkyl, alkoxy, haloalkyl or haloalkoxy (n=1 to 5),R.sup.2 is halogen or, in each case low molecular weight, alkyl or haloalkyl,R.sup.3, R.sup.4 are halogen or each is an electron in a double bond formed by them together,R.sup.5 is hydrogen or, in each case low molecular weight, alkyl, alkenyl, alkynyl or cyano,R.sup.6 is halogen or alkyl (n=1 to 4),R.sup.7 is halogen (p=0 to 25),and their use for combating pests.
    Type: Grant
    Filed: February 22, 1990
    Date of Patent: November 19, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Winfried Zombik, Hans Theobald, Bernd Wolf, Ludwig Schuster, Peter Hofmeister, Christoph Kuenast
  • Patent number: 4954160
    Abstract: The invention provides compounds of the general formula ##STR1## wherein R represents a hydrogen atom, or an optionally substituted alkyl or acyl group, or an alkenyl or alkynyl group or an inorganic or organic cation;R.sup.1 represents an alkyl, haloalkyl, alkenyl, alkynyl or optionally substituted aralkyl or phenyl group;R.sup.2 represents an optionally substituted alkyl or phenalkyl group or a cycloalkyl, alkenyl, haloalkenyl or alkynyl group;each R.sup.3 represents an optionally substituted alkyl group;one of R.sup.4 or R.sup.5 represents a hydrogen atom or an alkyl group while the other of R.sup.4 and R.sup.5 represents an optionally substituted phenyl group; together with their use as herbicides and their preparation using novel intermediates.
    Type: Grant
    Filed: September 21, 1988
    Date of Patent: September 4, 1990
    Assignee: Shell Internationale Research Maatschappij, B.V.
    Inventors: Terence Gilkerson, Robert W. Shaw
  • Patent number: 4939142
    Abstract: The new compounds of the general Formula I ##STR1## (wherein A stands for a C.sub.2-4 straight or branched chain alkylene group;R.sup.1 and R.sup.2 may be same or different and each stands for hydrogen, halogen, lower alkyl or lower alkoxy; orR.sup.1 and R.sup.2 together form a methylenedioxy group;R.sup.3 and R.sup.4 may be the same or different and each stands for C.sub.1.ident. alkyl or C.sub.3.notident. cycloalkyl orR.sup.3 and R.sup.4 together with the nitrogen atom, they are attached to, form a 4-7 membered ring which may contain as additional ring member an oxygen or sulfur atom or a further nitrogen atom and the latter nitrogen atom may optionally bear a C.sub.
    Type: Grant
    Filed: January 26, 1989
    Date of Patent: July 3, 1990
    Assignee: EGIS Gyogyszergyar
    Inventors: Zoltan Budai, Lujza Petocz, Tibor Mezei, Eniko Szirt nee Kiszelly, Maria Szecsey nee Hegedus, Gabor Gigler, Klara Reiter nee Esses, Aranka Lay nee Konya, Eva Furdyga, Istvan Gertyan, Istvan Gacsalyi
  • Patent number: 4929738
    Abstract: Microbicidal substituted pyrazolin-5-ones of the formula ##STR1## in which R.sup.1 and R.sup.2 independently of one another each represent hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxycarbonyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl or dialkylaminocarbonylalkyl, or represent in each case optionally substituted oxiranylalkyl, aralkyl, heterocyclyl or aryl andHet represents an optionally substituted heterocyclic radial.Intermediates therefor of the formula ##STR2## in which R is alkyl, are also new.
    Type: Grant
    Filed: May 10, 1989
    Date of Patent: May 29, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Jelich, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
  • Patent number: 4921524
    Abstract: The invention provides compounds of the general formula ##STR1## wherein R represents a hydrogen atom, or an optionally substituted alkyl or acyl group, or an alkenyl or alkynyl group or an inorganic or organic cation;R.sup.1 represents an alkyl, haloalkyl, alkenyl, alkynyl or phenyl group;R.sup.2 represents an optionally substituted alkyl or phenalkyl group or a cycloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl group;R.sup.3 represents a hydrogen atom or an alkyl group; andone of R.sub.4 and R.sup.5 represents a hydrogen atom or an alkyl group, while the other of R.sup.4 and R.sup.5 represents an optionally substituted phenyl group; together with their use as herbicides and their preparation using novel intermediates.
    Type: Grant
    Filed: April 14, 1988
    Date of Patent: May 1, 1990
    Assignee: Shell Internationale Research Maatschappij B.V.
    Inventors: Terence Gilkerson, Robert W. Shaw, David C. Jennens
  • Patent number: 4874781
    Abstract: A compound of formula II: ArCHR.sub.1 CO.sub.2 CHDR.sub.2in which formula:Ar represents a phenyl or naphthyl group optionally substituted by one or more halogen, alkoxy, haloalkoxy, methylenedioxy, C.sub.1 -C.sub.6 alkyl or haloalkyl groups;R.sub.1 represents the group --CH(CF.sub.3)CH.sub.3 or --C(CF.sub.3).dbd.CH.sub.2R.sub.2 represents the residue of an alcohol R.sub.2 CHDOH in which D is hydrogen or cyano and of which the [1R, cis]2,2-dimethyl-3-(2,2-dibromovinyl)cyclopropane carboxylic ester is significantly insecticidal.
    Type: Grant
    Filed: January 11, 1988
    Date of Patent: October 17, 1989
    Assignee: National Research Development Corporation
    Inventors: Michael Elliott, Norman F. Janes, Bhupinder P. S. Khambay
  • Patent number: 4873344
    Abstract: The present invention relates to novel indene derivatives with the general formula I: ##STR1## wherein R.sup.1 is (a) a phenyl group optionally substituted with one or two groups selected from halogen, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulfonyl, dilower alkylamino, acylamino such as acetylamino, cyano, trifluoromethyl, trifluoromethoxy, pyrrole and dilower alkylpyrrole,(b) a polycyclic aromatic or heteroaromatic group, such as naphthalene or quinoline,(c) a heteroaromatic group such as thiophene, pyridine, and pyrrole, optionally substituted with one or more groups selected from halogen, lower alkyl, lower alkoxy, lower alkylthio, trifluoromethyl or trifluoromethoxy,R.sub.2 is selected from H, halogen, lower alkyl, benzyl, lower alkylthio, methoxy, lower alkylsulfonyl, dilower alkylsulfamoyl, acylamino such as acetylamino, benzylamino, dilower alkylamino, cyano, pyrrole, dilower alkylpyrrole, trifluoromethyl and trifluoromethoxy,R.sup.3 is CN, COOR.sup.4, --CON(R.sup.4).sub.2 or COR.sup.
    Type: Grant
    Filed: November 24, 1987
    Date of Patent: October 10, 1989
    Assignee: H. Lundbeck A/S
    Inventors: Klaus P. Bogeso, Michael B. Sommer
  • Patent number: 4859784
    Abstract: Optically active cyanohydrins are produced by the reaction of an aldehyde with hydrocyanic acid in the presence of D-oxynitrilase (E.C.4.1.2.10). The reaction takes place in an organic solvent which is not miscible with water, but which is saturated with water or an aqueous buffer solution.
    Type: Grant
    Filed: January 19, 1988
    Date of Patent: August 22, 1989
    Assignee: Degussa Aktiengesellschaft
    Inventors: Franz Effenberger, Thomas Ziegler, Siegfried Foerster
  • Patent number: 4857663
    Abstract: N-(3-Dialkylamino-2-propenylidene)-N-alkylalkanaminium salts substituted in the 2-position with an ether or thioether and having the formula ##STR1## are active as hypoglycemic agents.
    Type: Grant
    Filed: November 16, 1988
    Date of Patent: August 15, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Eugene R. Wagner, Donald P. Matthews, Charlotte L. Barney
  • Patent number: 4857651
    Abstract: This invention provides novel .alpha.-[2,2-di(C.sub.1 -C.sub.4 alkoxy)ethylamino]-.beta.-cyanostyrene and .alpha.-[2,2-di(C.sub.1 -C.sub.4 alkoxy)ethylamino]-.beta.-nitrostyrene compounds that are useful for the preparation of pesticidal arylpyrroles. The invention also provides a method for the preparation of the above-said .beta.-cyanostyrene and .beta.-nitrostyrene compounds.
    Type: Grant
    Filed: July 29, 1987
    Date of Patent: August 15, 1989
    Assignee: American Cyanamid Company
    Inventors: Dale G. Brown, Jack K. Siddens, Robert E. Diehl, Donald P. Wright, Jr.
  • Patent number: 4804684
    Abstract: Drugs with high anticonvulsant and analgesic activities constituted by symmetrical .beta.-dialkoxyiminocycloalklene derivatives in which the imine double bonds are conjugated with the cyclic double bond or bonds belonging to one or more fused benzene rings.
    Type: Grant
    Filed: January 20, 1987
    Date of Patent: February 14, 1989
    Assignee: Panmedica S.A.
    Inventors: Claude Laruelle, Marcel Lepant, Bernard Raynier
  • Patent number: 4789743
    Abstract: The invention relates to a process for the preparaton of compounds of the formula I by reacting an alkali metal alcoholate with a compound of the formula II in the presence of an aliphatic ester such as methyl formate, and then condensing guanidine with the resulting compound of the formula III.The compound of the formula II can be prepared by reacting the corresponding benzaldehyde with acrylonitrile in the presence of diazabicyclo-2,2,2,-octane.
    Type: Grant
    Filed: July 31, 1987
    Date of Patent: December 6, 1988
    Assignee: Societe Anonyme: Sanofi Pharma S.A. - Succursale de Carouge
    Inventor: Abram Becker