Attached Directly To The Five-membered Hetero Ring Patents (Class 548/529)
  • Patent number: 8946682
    Abstract: The present invention relates to novel donor-acceptor fluorene compounds, which can be used as for the fabrication of electroluminescent devices, and a process of preparing said novel compounds. More particularly, the present invention relates to amine donor and nitrile/ester acceptor fluorenes, fluorenones their ?-conjugated systems and related compounds, processes for preparing the said compounds including oxidation of fluorenes to corresponding fluorenones and their use in preparing organic electronic devices such as organic light emitting diodes (OLEDs), photovoltaic/solar cell, Field effect transistors and other useful electroluminescent devices. The compounds are prepared by reacting 2H-pyran-2-ones in isolated or rigid conformations with cyclic ketones containing methylene carbonyl moiety in the presence of a base in an organic solvent.
    Type: Grant
    Filed: September 30, 2010
    Date of Patent: February 3, 2015
    Assignee: Council of Scientific & Industrial Research
    Inventors: Atul Goel, Sumit Chaurasia, Vijay Kumar, Sundar Manoharan, R. S. Anand
  • Publication number: 20140155357
    Abstract: The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression.
    Type: Application
    Filed: June 14, 2013
    Publication date: June 5, 2014
    Inventors: Paul Abato, Haregewein Assefa, Joel Berniac, Beena Bhatia, Todd Bowser, Jackson Chen, Mark Grier, Laura Honeyman, Mohamed Y. Ismail, Mark L. Nelson, Kwasi Ohemeng, Jingwen Pan
  • Publication number: 20130310558
    Abstract: Methods for the synthesis and use of functionalized, substituted naphthalenes are described. The functionalized, substituted naphthalenes display useful properties including liquid crystals and fluorescence properties, such as solvatochromatic fluorescence, with high quantum yields, Stoke's shift, and show emission maxima that are significantly red-shifted.
    Type: Application
    Filed: March 15, 2013
    Publication date: November 21, 2013
    Inventor: Key M. Brummond
  • Patent number: 8513437
    Abstract: The invention provides pyrrolidino-substituted 1,4-naphthoquinone derivatives that modulate the activity of protein kinases, and it relates to the use of the derivatives in pharmaceutical compositions for treating cardiovascular disorders and malignancies. The invention particularly provides medicaments for treating disorders associated with MAPKs signaling, ERKs signaling, p38 signaling, and JNKs signaling.
    Type: Grant
    Filed: July 21, 2005
    Date of Patent: August 20, 2013
    Assignee: Ben Gurion University of the Negev Research and Development Authority
    Inventors: Yossi Granot, Shmuel Bittner
  • Patent number: 8329377
    Abstract: An imide compound represented by the formula (I): wherein R1 represents a C1-C20 aliphatic hydrocarbon group etc., W1 represents —CO—O— etc., Q1 and Q2 each independently represent a fluorine atom etc., and A represents a group represented by the formula (I-1): wherein A1 represents —CH2—CH2— etc., and a chemically amplified resist composition containing the same.
    Type: Grant
    Filed: July 21, 2009
    Date of Patent: December 11, 2012
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Ichiki Takemoto, Tatsuro Masuyama, Takashi Hiraoka
  • Publication number: 20110210315
    Abstract: The present invention relates to novel donor-acceptor fluorene compounds, which can be used as for the fabrication of electroluminescent devices, and a process of preparing said novel compounds. More particularly, the present invention relates to amine donor and nitrile/ester acceptor fluorenes, fluorenones their ?-conjugated systems and related compounds, processes for preparing the said compounds including oxidation of fluorenes to corresponding fluorenones and their use in preparing organic electronic devices such as organic light emitting diodes (OLEDs), photovoltaic/solar cell, Field effect transistors and other useful electroluminescent devices. The compounds are prepared by reacting 2H-pyran-2-ones in isolated or rigid conformations with cyclic ketones containing methylene carbonyl moiety in the presence of a base in an organic solvent.
    Type: Application
    Filed: September 30, 2010
    Publication date: September 1, 2011
    Inventors: Atul GOEL, Sumit CHAURASIA, Vijay KUMAR, Sundar MANOHARAN, R.S. ANAND
  • Patent number: 7906228
    Abstract: The present invention relates to novel compounds for electronic material, and organic electroluminescent devices or organic solar cells comprising the same. Specifically, the compounds for electronic material according to the invention are characterized in that they are represented by Chemical Formula (1): Since the compounds for electronic material, when being applied to an organic electroluminescent device, show good luminous efficiency and excellent life property of material, OLED's having very good operation life can be manufactured therefrom.
    Type: Grant
    Filed: April 17, 2009
    Date of Patent: March 15, 2011
    Assignee: Gracel Display Inc.
    Inventors: Mi Ae Lee, Young Jun Cho, Hyuck Joo Kwon, Bong Ok Kim, Sung Min Kim, Seung Soo Yoon
  • Patent number: 7897784
    Abstract: The present invention provides processes for preparing a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein A is a pyrrole, tetrazole or triazole ring.
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: March 1, 2011
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventors: Sophie Huss, Jose M. Bueno, Jose M. Fiandor, Roger Frechette
  • Patent number: 7767667
    Abstract: It has now been found that certain novel heterocyclic derivitives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ?NCH(R6)CH(R7)N(R8)—, ?NC(R6)?C(R7)N(R8)—, or ?CHN?C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)?C(R12)C(R13)?C(R14) 1 12, -, where R,R,R6, R7, R8, RI1, R R13, R14, and X are described. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of a second compound with at least one insecticidally compatable carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Grant
    Filed: August 22, 2008
    Date of Patent: August 3, 2010
    Assignee: FMC Corporation
    Inventors: John A. Dixson, Zeinab M. Elshenawy, Harvey R. Wendt, Saroj Sehgel, Robert H. Henrie, II, David M. Roush, Ping Ding, John W. Lyga, Stephen F. Donovan
  • Patent number: 7754744
    Abstract: This invention is concerned with compounds of the formula and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
    Type: Grant
    Filed: August 6, 2007
    Date of Patent: July 13, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alfred Binggeli, Andreas D. Christ, Hans P. Maerki, Rainer E. Martin
  • Patent number: 7732622
    Abstract: A compound of formula (I) wherein R1 and R3 are the same or different and represent ?O, hydrogen, C1-6alkyl, C1-6dialkyl, ?CHC1-C5alkyl, ?S, or a 5- or 6-membered aryl; R4 to R9 are the same or different and represent hydrogen, C1-6alkoxy, OCF3, OCH2CF3, O-cyclopropyl, OCH2-cyclopropyl, C1-C6alkyl, S-alkyl, NR210 where R10 is hydrogen or C1-6alkyl, halogen, NO2, OH, CH2OC1-C6alkyl, CH2OH, or CF3; Q1 is hydrogen, C1-6alkyl, C1-6dialkyl, C1-6alkoxy, NHAc, NR210 where R10 is hydrogen or C1-6alkyl, difluoro, fluoro, ?O, or OH; Q2, Q3, Q4 and Q5 are the same or different and represent hydrogen, C1-6alkoxy, OCF3, OCH2CF3, O-cyclopropyl, OCH2-cyclopropyl, C1-C6alkyl, S-alkyl, NR210 where R10 is hydrogen or C1-6alkyl, halogen, NO2, OH, CH2OC1-C6alkyl, CH2OH, or a 5- or 6-membered aryl; with the proviso that the compounds [4-(1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]-2-propionic acid, sodium salt and [4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetic acid are excluded; and pharmac
    Type: Grant
    Filed: April 30, 2008
    Date of Patent: June 8, 2010
    Assignee: Glaxo Group Limited
    Inventors: Miles Stuart Congreve, Gerard Martin Paul Giblin, Andrew McMurtrie Mason, Neil Derek Miller, Susan Roomans, Ann Louise Walker
  • Patent number: 7696358
    Abstract: The present invention describes methods of treating bacterial infections with 7-pyrrolyl tetracycline compounds of formula (I):
    Type: Grant
    Filed: December 2, 2005
    Date of Patent: April 13, 2010
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventors: Sophie Huss, Jose M. Bueno, Jose M. Fiandor, Roger Frechette
  • Publication number: 20100081826
    Abstract: A compound of Formula (I):
    Type: Application
    Filed: November 24, 2009
    Publication date: April 1, 2010
    Applicant: Paratek Pharmaceuticals, Inc.
    Inventors: Sophie Huss, Jose M. Bueno, Jose M. Fiandor, Roger Frechette
  • Publication number: 20100028807
    Abstract: An imide compound represented by the formula (I): wherein R1 represents a C1-C20 aliphatic hydrocarbon group etc., W1 represents —CO—O— etc., Q1 and Q2 each independently represent a fluorine atom etc., and A represents a group represented by the formula (I-1): wherein A1 represents —CH2—CH2— etc., and a chemically amplified resist composition containing the same.
    Type: Application
    Filed: July 21, 2009
    Publication date: February 4, 2010
    Applicant: SUMITOMO CHEMICAL COMPANY, LTD.
    Inventors: Ichiki TAKEMOTO, Tatsuro MASUYAMA, Takashi HIRAOKA
  • Publication number: 20090288707
    Abstract: The present invention relates to novel compounds for electronic material, and organic electroluminescent devices or organic solar cells comprising the same. Specifically, the compounds for electronic material according to the invention are characterized in that they are represented by Chemical Formula (1): Since the compounds for electronic material, when being applied to an organic electroluminescent device, show good luminous efficiency and excellent life property of material, OLED's having very good operation life can be manufactured therefrom.
    Type: Application
    Filed: April 17, 2009
    Publication date: November 26, 2009
    Applicant: Gracel Display Inc.
    Inventors: Mi Ae Lee, Young Jun Cho, Hyuck Joo Kwon, Bong Ok Kim, Sung Min Kim, Seung Soo Yoon
  • Publication number: 20090209584
    Abstract: A compound of formula (I) wherein R and R2 and the attached nitrogen atom form pyrrolidinyl or piperidinyl. R1 is a group of formula (II). R3 and R?3 are hydrogen, deuterium or halogen. R4, R5 and R10 are independently of each other hydrogen or alkyl. R6, R7 and R8 are hydrogen or deuterium. R9 is amino, alkyl, aryl, heterocyclyl or mercapto. If X is oxygen, R9 is additionally hydrogen; R?10 is alkyl, X is sulphur, oxygen, NR10, or N+(R?10)2; Y is sulphur or oxygen, and m is 0, 1 or 2, with the proviso that, when R and R2 and the attached nitrogen atom form piperidinyl, m is O, Y is S and Y is attached in position 3 of the piperidine ring, that group of formula (I) which is attached to the piperidine ring via the residue Y is either in the (S)-configuration or in the (R)-configuration, preferably in the (S)-configuration which is useful as antimicrobial, antibacterial.
    Type: Application
    Filed: April 7, 2009
    Publication date: August 20, 2009
    Applicant: Nabriva Therapeutics Forschungs AG
    Inventors: Gerd Ascher, Heinz Berner, Johannes Hildebrandt
  • Publication number: 20090012070
    Abstract: It has now been found that certain novel heterocyclic derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ?NCH(R6)CH(R7)N(R8)—, ?NC(R6)=C(R7)N(R8)-, or ?CHN?C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)=C(R12)C(R13)=C(R14) 112, -, where R, R, R6, R7, R8, R11, R R13, R14, and X are described. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Application
    Filed: August 22, 2008
    Publication date: January 8, 2009
    Applicant: Bayer Cropscience AG
    Inventors: John A. Dixson, Zeinab M. Elshenawy, Harvey R. Wendt, Saroj Sehgel, Robert H. Henrie, II, David M. Roush, Ping Ding, John W. Lyga, Stephen F. Donovan
  • Publication number: 20080167318
    Abstract: The present invention is related to pyrrolidine derivatives of formula I. Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula I are useful in the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including premature labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation.
    Type: Application
    Filed: April 9, 2007
    Publication date: July 10, 2008
    Applicant: APPLIED RESEARCH SYSTEM ARS HOLDING N.V.
    Inventors: Serge Halazy, Anna Quattropani, Alexander Scheer, Matthias Schwarz, Russell J. Thomas, Anthony Baxter
  • Patent number: 7265110
    Abstract: The present invention relates compounds of the formula (I); wherein R1, R2, R3, R4, R5, R6, R7, R8, and R10 represent a variety of substituents; A represents NR9 or O; B represents a bond, CH2, NR9 or O, wherein one or both hydrogen atoms in said CH2 moiety may be replaced with one or both of R7 and R8, or alternatively, one of the hydrogen atoms in said CH2 moiety together with a hydrogen atom from an adjacent carbon are replaced by a double bond; with the proviso that when A is O, then B is NR9; n is zero, 1 or 2; and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 6, 2002
    Date of Patent: September 4, 2007
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Jose Luis Castro Pineiro, Duncan Edward Shaw, Brian John Williams
  • Patent number: 7160877
    Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower-alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.
    Type: Grant
    Filed: June 22, 2004
    Date of Patent: January 9, 2007
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
  • Patent number: 7087599
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
    Type: Grant
    Filed: February 14, 2001
    Date of Patent: August 8, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Dann LeRoy Parker, Jr., Ronald W. Ratcliffe, Robert R. Wilkening, Kenneth J. Wildonger
  • Patent number: 7001918
    Abstract: A compound of Formula (I): wherein variables R, R1, R2, R3 and A are as defined in the
    Type: Grant
    Filed: June 1, 2004
    Date of Patent: February 21, 2006
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventors: Sophie Huss, Jose M. Bueno, Jose M. Fiandor, Roger Frechette
  • Patent number: 6960667
    Abstract: The present invention is directed to maleimides and preparation of compounds of the formula I wherein R1 and R2 independently from each other stand for variously substituted, and R3 stands for allyl, variously substituted, with the proviso, that R1 and R2 not simultaneously stand for phenyl.
    Type: Grant
    Filed: October 10, 2002
    Date of Patent: November 1, 2005
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Kazuhiko Kunimoto, Junji Otani, Kunihiko Kodama, Hiroshi Yamamoto, Patrick Verhoustraeten, Sonia Megert, Adalbert Braig
  • Publication number: 20040266740
    Abstract: A compound of formula (I): 1
    Type: Application
    Filed: January 5, 2004
    Publication date: December 30, 2004
    Inventors: Sophie Huss, Jose M. Fiandor, Roger Frechette
  • Publication number: 20040248857
    Abstract: A compound of Formula (I): 1
    Type: Application
    Filed: June 1, 2004
    Publication date: December 9, 2004
    Applicants: Paratek Pharmaceuticals, Inc., Glaxo Group Limited
    Inventors: Sophie Huss, Jose M. Bueno, Jose M. Flandor, Roger Frechette
  • Patent number: 6355669
    Abstract: The present invention provides a therapeutic or prophylactic agent as a substitute for conventional steroids or immunosuppressive agents to treat or prevent systemic erythematosus, glomerulonephritis, lupus nephritis, idiopathic thrombocytopenic purpura or autoimmune anemia.
    Type: Grant
    Filed: April 18, 2000
    Date of Patent: March 12, 2002
    Assignee: Eisai Co., Ltd.
    Inventors: Toshihiko Yamauchi, Akira Ishibashi, Naoki Tokuhara, Mitsuo Nagai
  • Patent number: 6140321
    Abstract: Donepezil hydrochloride, 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride, is provided here in the form of four polymorphs which are stable against heat and humidity in the pharmaceutical use. They can be industrially produced. They are specified by peaks in X-ray powder diffraction pattern and absorption peaks in infrared absorption spectra in potassium bromide.
    Type: Grant
    Filed: December 30, 1996
    Date of Patent: October 31, 2000
    Assignee: Eisai Co., Ltd.
    Inventors: Akio Imai, Hideaki Watanabe, Takashi Kajima, Yasushi Ishihama, Akiyo Ohtsuka, Tomohide Tanaka
  • Patent number: 6057441
    Abstract: This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; halomethylcarbonyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R.sup.3 and R.sup.4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or halomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.
    Type: Grant
    Filed: October 6, 1998
    Date of Patent: May 2, 2000
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Pilar Gil-Lopetegui, Francisco Javier Fernandez-Gadea, Theo Frans Meert
  • Patent number: 5985864
    Abstract: Donepezil hydrochloride, 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride, is provided here in the form of four polymorphs which are stable against heat and humidity in the pharmaceutical use. They can be industrially produced. They are specified by peaks in X-ray powder diffraction pattern and absorption peaks in infrared absorption spectra in potassium bromide.
    Type: Grant
    Filed: June 6, 1997
    Date of Patent: November 16, 1999
    Assignee: Eisai Co., Ltd.
    Inventors: Akio Imai, Hideaki Watanabe, Takashi Kajima, Yasushi Ishihama, Akiyo Ohtsuka, Tomohide Tanaka, Yukio Narabu
  • Patent number: 5914324
    Abstract: 6-hydroxy and 6-oxo-androstane derivatives of formula (I), active on the cardiovascular system. ##STR1## wherein: the symbol A represents CH--OR, C.dbd.N--OR, CH--CH.dbd.N--OR and C.dbd.CH--N--OR; and R.sup.1, R.sup.2 and R.sup.3 are as defined herein.
    Type: Grant
    Filed: July 10, 1997
    Date of Patent: June 22, 1999
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Sergio De Munari, Elena Folpini, Marco Frigerio, Piero Melloni, Fulvio Serra, Simona Sputore
  • Patent number: 5780486
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: May 27, 1997
    Date of Patent: July 14, 1998
    Assignee: Novo Nordisk A/S
    Inventors: Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Henrik Sune Andersen, Rolf Hohlweg, Peter Madsen, Uffe Bang Olsen
  • Patent number: 5686482
    Abstract: N-(3-Pyrrodinyl)benzamide derivatives represented by the following general formula (I) which have potent and selective antagonism against dopamine D.sub.3 and/or D.sub.4 receptor and are useful as a psychotropic, a schizophrenia-treating agent and the like, or a pharmaceutically acceptable salt thereof or a pharmaceutical preparation thereof.
    Type: Grant
    Filed: October 2, 1996
    Date of Patent: November 11, 1997
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Junya Ohmori, Kyoichi Maeno, Kazuyuki Hidaka, Kazuhiro Nakato, Shuichi Sakamoto, Shin-ichi Tsukamoto
  • Patent number: 5574175
    Abstract: The present invention provides a process for the manufacture of 2-aryl-5-(perfluoroalkyl)pyrrole-3-carbonitrile comprising the cycloaddition of 5-amino-4-aryl-2-perfluoroalkyl-1,3-oxazole and the appropriate 1,3-dipolarifile. The arylpyrrole-3-carbonitrile product and its derivatives are highly effective insecticidal, acaricidal and nematocidal agents.
    Type: Grant
    Filed: May 16, 1995
    Date of Patent: November 12, 1996
    Assignee: American Cyanamid Co.
    Inventor: Venkataraman Kameswaran
  • Patent number: 5488119
    Abstract: Compounds of formulae I and II ##STR1## wherein D is H or --OR wherein R is phenyl and R.sub.1 to R.sub.4 are H or a substituent such as phenylthio, and one of the substituents R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is a group of formula III--E-CR.sub.5 =C(R.sub.6).sub.2 (III)or R is substituted by a group of formula III, wherein E is a direct bond or --X-C(O)-- wherein X is a linking group, and R.sub.5 and R.sub.6 are each independently of the other H, halogen, C.sub.1 -C.sub.12 alkyl or C.sub.6 -C.sub.10 aryl, can be polymerised to homopolymers or copolymers. The monomers and polymers are reversible photochromic systems which can be used as color indicators, as photochemically modifiable color filters, or for the optical storage of information.
    Type: Grant
    Filed: October 12, 1993
    Date of Patent: January 30, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Evelyn Fischer-Reimann, Walter Fischer
  • Patent number: 5276053
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: January 4, 1994
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5274135
    Abstract: A process for preparing a 3- or 4-aminobenzocyclobutene comprises aminating a 3- or 4-halo- or sulfonyloxybenzocyclobutene reactant with an aminating agent by heating at a temperature from about 80.degree. C. to a temperature at which dimerization or oligomerization of a benzocyclobutene reactant or product is a significant side reaction, in the presence of a metal-containing catalyst, for a time sufficient to aminate the halo- or sulfonyloxybenzocyclobutene reactant. In another aspect, this invention relates to a process for making a 3- or 4-phthalimido- or maleimidobenzocyclobutene, comprising reacting a 3- or 4-halobenzocyclobutene reactant with a phthalimide or maleimide compound in the presence of a metal-containing catalyst. The resulting phthalimido- or maleimidobenzocyclobutene can be hydrolyzed to a 3- or 4-aminobenzocyclobutene.
    Type: Grant
    Filed: September 20, 1991
    Date of Patent: December 28, 1993
    Assignee: The Dow Chemical Company
    Inventors: Kenneth J. Bruza, Arnold E. Young, Kurt A. Bell
  • Patent number: 5252317
    Abstract: Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines.
    Type: Grant
    Filed: May 22, 1992
    Date of Patent: October 12, 1993
    Assignee: The State of Oregon Acting by and through the State Board of Higher Education on Behalf of the University of Oregon
    Inventor: John F. W. Keana
  • Patent number: 5202486
    Abstract: Tetrahydronaphthaleneamine derivatives having the formula ##STR1## wherein R, R', R.sub.1 and R.sub.2 are as defined herein, are novel calcium channel blockers.
    Type: Grant
    Filed: July 31, 1990
    Date of Patent: April 13, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Joel C. Barrish, Steven H. Spergel
  • Patent number: 5189065
    Abstract: The use of products of formula (I) is described, wherein X and Y represent hydrogen, hydroxy or alkoxy; and R.sub.1 and R.sub.2 represent H, alkyl, alkenyl or alkynyl, arylalkyl, acyl or R.sub.1 and R.sub.2 together with nitrogen form a heterocycle for preparing an antitumoral drug.
    Type: Grant
    Filed: October 17, 1991
    Date of Patent: February 23, 1993
    Assignee: Roussel Uclaf
    Inventors: Jorg Czech, Hans H. Sedlacek, Lucien Nedelec, Jacques Guillaume, Christian Marchandeau
  • Patent number: 5180736
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: January 19, 1993
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5132313
    Abstract: The present invention relates to novel NMDA receptor antagonists and methods for their use. The present invention also provided pharmaceutical compositions comprising such NMDA receptor antagonists.
    Type: Grant
    Filed: October 26, 1989
    Date of Patent: July 21, 1992
    Assignee: University of Pittsburgh
    Inventors: Alan P. Kozikowski, Yuan-Ping Pang
  • Patent number: 5093031
    Abstract: The invention relates to properties and uses of N-hydrocarbon substituted lactams, particularly N-alkyl substituted lactams having the formula ##STR1## wherein R' is a hydrophobic radical such as linear or branched chain alkyl group containing from 8 to 27 carbon atoms, most preferably micelle forming pyrrolidones having 12 to 16 carbon atoms in the R' group. The invention particularly relates to the uses of the N-hydrocarbon substituted lactams which involve surfactant properties, such as solubility, wetting, viscosity building, emulsifying and/or complexing properties.
    Type: Grant
    Filed: October 14, 1988
    Date of Patent: March 3, 1992
    Assignee: ISP Investments Inc.
    Inventors: Robert B. Login, Ratan K. Chaudhuri, Rama K. Haldar, Mohamed M. Hashem, Michael W. Helioff, David J. Tracy
  • Patent number: 5071853
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: February 27, 1990
    Date of Patent: December 10, 1991
    Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
  • Patent number: 4904688
    Abstract: The present invention deals with dibenzo-oxocin-, dibenzo-thiocin-, dibenzo-azocin- and dibenzocyclo-octenamine derivatives suitable for use as antipsychotic compounds without extra-pyrimidal side-effects.
    Type: Grant
    Filed: March 8, 1989
    Date of Patent: February 27, 1990
    Assignee: Akzo N.V.
    Inventors: Duncan R. Rae, James Cairns
  • Patent number: 4876269
    Abstract: Benzo-fused cycloalkane and oxa- and thia-cycloalkane trans-1,2-diamine compounds of the formula: ##STR1## wherein A, B, C, D, n, X, Y, R, R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, e.g., trans-3,4-dichloro-N-methyl-N-[2-(pyrrolidin-1-yl)-5-methoxy-1,2,3,4-tetra hydronaphth-1-yl]benzeneacetamide, and the pharmaceutically acceptable salts of N-oxides thereof, are useful as analgesics and/or diuretics.
    Type: Grant
    Filed: July 16, 1987
    Date of Patent: October 24, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Penio Pennev, Parthasarathi Rajagopalan, Richard M. Scribner
  • Patent number: 4826996
    Abstract: The invention concerns 1,8-dihydroxy-9-anthrones substituted in the 10-position of the formula: ##STR1## in which R.sub.1 represents a group taken from the set constituted by: ##STR2## wherein R.sub.2 represents H, C.sub.1-8 alkyl, C.sub.1-3 mono- or poly-hydroxyalkyl, carbamoyl or phenyl,R.sub.3, R.sub.4, and R.sub.5 represent H, C.sub.1-8 alkyl, C.sub.3-8 mono- or poly-hydroxyalkyl, possibly interrupted by an oxygen, C.sub.3-6 cycloalkyl, or R.sub.3 and R.sub.4 form a divalent group: --(CH.sub.2).sub.(4 or 5) --, --(CH.sub.2).sub.2 --O--(CH.sub.2).sub.2 --, or --(CH.sub.2).sub.2 --N(R.sub.8)--(CH.sub.2).sub.2 --, R.sub.8 being H, --CH.sub.3, or --CH.sub.2 CH.sub.2 OH,R.sub.6 represents --CO.sub.2 R.sub.5, --CN, CHO, --CONH.sub.2, or --CONH--CH.sub.2 OH,and R.sub.7 and R'.sub.7 are H or --CH.sub.3, and their optical isomers.Utilization of the compounds (I) in human or veterinary medicine, in particular in the treatment of psoriasis and of warts, in cosmetics.
    Type: Grant
    Filed: December 9, 1985
    Date of Patent: May 2, 1989
    Assignee: Groupement d'Interet Economique dit Centre International De Recherches Dermatologioues C.I.R.D.
    Inventors: Braham Shroot, Jean Maignan, Gerard Lang
  • Patent number: 4798894
    Abstract: Compounds containing at least one N,N-dialkylatable amino or amido group (e.g., aniline, dodecylamine, acetamide) are converted in a highly efficient manner into gem cyclodialkylated compounds by reaction with an unstrained cyclic ether (e.g., tetrahydrofuran) or a polyol (e.g., 1,4-butane diol) cyclizable to an unstrained ether using titanium dioxide catalysts that have prior to use:(1) a surface area of at least 70 square meters per gram (as determined by the BET method), and(2) the capability of chemically adsorbing at 100.degree. C. at least 35.times.10.sup.4 millimoles of gaseous ammonia per square meter of surface area.
    Type: Grant
    Filed: May 11, 1987
    Date of Patent: January 17, 1989
    Assignee: Ethyl Corporation
    Inventor: Duane C. Hargis
  • Patent number: 4461899
    Abstract: A series of ester and salt derivatives of fluorene-9-carboxylic acid and fluorene-1-carboxylic acid exhibit significant plant growth regulating properties, useful in controlling the size, shape, dormancy time, flowering time and/or fruit setting of plants, depending upon the concentrations used. They may also be used to control the growth rate, texture and color of turf grass. Presently preferred compounds include the cis-2,5-dimethylpyrrolidine salt of 1-fluorenecarboxylic acid, 9-cis-2,5-dimethyl-1-pyrrolidinyl-2-chlorofluorene-9-carboxylic acid, methyl ester, the 2,6-dimethylpiperidine salt of 1-fluorenecarboxylic acid, and the cis-2,5-dimethylpyrrolidine salt of 9-hydroxyfluorene-9-carboxylic acid.
    Type: Grant
    Filed: May 24, 1982
    Date of Patent: July 24, 1984
    Assignee: Diamond Shamrock Chemicals Company
    Inventors: William J. Pyne, Han S. Ku, Robert E. Holm
  • Patent number: 4447368
    Abstract: Aromatic aminosulphonic acids which have a reduced content of discoloring by-products are obtained when aromatic amines are reacted with a sulphonating agent in a reaction medium at least some of which consists of tetramethylene sulphone.
    Type: Grant
    Filed: March 31, 1982
    Date of Patent: May 8, 1984
    Assignee: Siemens-Allis, Inc.
    Inventors: Herbert Emde, Heinz U. Blank, Peter Schnegg
  • Patent number: 4435336
    Abstract: Aminoarylsulphonic acids which have a relatively high purity and a relatively low content of aminoaryldisulphonic acids can be obtained, if they are prepared, from the corresponding arylammonium hydrogen sulphates, by an improved version of the so-called baking process, wherein the reaction is carried out under pressure at a temperature of at least 140.degree. C. and, at least partially, in the presence of water.
    Type: Grant
    Filed: March 31, 1982
    Date of Patent: March 6, 1984
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Emde, Heinz U. Blank, Peter Schnegg