Attached Directly To The Five-membered Hetero Ring Patents (Class 548/529)
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Patent number: 8946682Abstract: 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: GrantFiled: September 30, 2010Date of Patent: February 3, 2015Assignee: Council of Scientific & Industrial ResearchInventors: Atul Goel, Sumit Chaurasia, Vijay Kumar, Sundar Manoharan, R. S. Anand
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Publication number: 20140155357Abstract: 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: ApplicationFiled: June 14, 2013Publication date: June 5, 2014Inventors: 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
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Publication number: 20130310558Abstract: 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: ApplicationFiled: March 15, 2013Publication date: November 21, 2013Inventor: Key M. Brummond
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Patent number: 8513437Abstract: 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: GrantFiled: July 21, 2005Date of Patent: August 20, 2013Assignee: Ben Gurion University of the Negev Research and Development AuthorityInventors: Yossi Granot, Shmuel Bittner
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Patent number: 8329377Abstract: 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: GrantFiled: July 21, 2009Date of Patent: December 11, 2012Assignee: Sumitomo Chemical Company, LimitedInventors: Ichiki Takemoto, Tatsuro Masuyama, Takashi Hiraoka
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Publication number: 20110210315Abstract: 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: ApplicationFiled: September 30, 2010Publication date: September 1, 2011Inventors: Atul GOEL, Sumit CHAURASIA, Vijay KUMAR, Sundar MANOHARAN, R.S. ANAND
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Patent number: 7906228Abstract: 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: GrantFiled: April 17, 2009Date of Patent: March 15, 2011Assignee: Gracel Display Inc.Inventors: Mi Ae Lee, Young Jun Cho, Hyuck Joo Kwon, Bong Ok Kim, Sung Min Kim, Seung Soo Yoon
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Patent number: 7897784Abstract: 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: GrantFiled: November 24, 2009Date of Patent: March 1, 2011Assignee: Paratek Pharmaceuticals, Inc.Inventors: Sophie Huss, Jose M. Bueno, Jose M. Fiandor, Roger Frechette
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Patent number: 7767667Abstract: 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: GrantFiled: August 22, 2008Date of Patent: August 3, 2010Assignee: FMC CorporationInventors: 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
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Patent number: 7754744Abstract: 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: GrantFiled: August 6, 2007Date of Patent: July 13, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Alfred Binggeli, Andreas D. Christ, Hans P. Maerki, Rainer E. Martin
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Patent number: 7732622Abstract: 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 pharmacType: GrantFiled: April 30, 2008Date of Patent: June 8, 2010Assignee: Glaxo Group LimitedInventors: Miles Stuart Congreve, Gerard Martin Paul Giblin, Andrew McMurtrie Mason, Neil Derek Miller, Susan Roomans, Ann Louise Walker
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Patent number: 7696358Abstract: The present invention describes methods of treating bacterial infections with 7-pyrrolyl tetracycline compounds of formula (I):Type: GrantFiled: December 2, 2005Date of Patent: April 13, 2010Assignee: Paratek Pharmaceuticals, Inc.Inventors: Sophie Huss, Jose M. Bueno, Jose M. Fiandor, Roger Frechette
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Publication number: 20100081826Abstract: A compound of Formula (I):Type: ApplicationFiled: November 24, 2009Publication date: April 1, 2010Applicant: Paratek Pharmaceuticals, Inc.Inventors: Sophie Huss, Jose M. Bueno, Jose M. Fiandor, Roger Frechette
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Publication number: 20100028807Abstract: 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: ApplicationFiled: July 21, 2009Publication date: February 4, 2010Applicant: SUMITOMO CHEMICAL COMPANY, LTD.Inventors: Ichiki TAKEMOTO, Tatsuro MASUYAMA, Takashi HIRAOKA
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Publication number: 20090288707Abstract: 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: ApplicationFiled: April 17, 2009Publication date: November 26, 2009Applicant: Gracel Display Inc.Inventors: Mi Ae Lee, Young Jun Cho, Hyuck Joo Kwon, Bong Ok Kim, Sung Min Kim, Seung Soo Yoon
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Publication number: 20090209584Abstract: 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: ApplicationFiled: April 7, 2009Publication date: August 20, 2009Applicant: Nabriva Therapeutics Forschungs AGInventors: Gerd Ascher, Heinz Berner, Johannes Hildebrandt
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Publication number: 20090012070Abstract: 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: ApplicationFiled: August 22, 2008Publication date: January 8, 2009Applicant: Bayer Cropscience AGInventors: 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
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Publication number: 20080167318Abstract: 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: ApplicationFiled: April 9, 2007Publication date: July 10, 2008Applicant: APPLIED RESEARCH SYSTEM ARS HOLDING N.V.Inventors: Serge Halazy, Anna Quattropani, Alexander Scheer, Matthias Schwarz, Russell J. Thomas, Anthony Baxter
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Patent number: 7265110Abstract: 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: GrantFiled: September 6, 2002Date of Patent: September 4, 2007Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Duncan Edward Shaw, Brian John Williams
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Patent number: 7160877Abstract: 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: GrantFiled: June 22, 2004Date of Patent: January 9, 2007Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
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Patent number: 7087599Abstract: 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: GrantFiled: February 14, 2001Date of Patent: August 8, 2006Assignee: Merck & Co., Inc.Inventors: Dann LeRoy Parker, Jr., Ronald W. Ratcliffe, Robert R. Wilkening, Kenneth J. Wildonger
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Patent number: 7001918Abstract: A compound of Formula (I): wherein variables R, R1, R2, R3 and A are as defined in theType: GrantFiled: June 1, 2004Date of Patent: February 21, 2006Assignee: Paratek Pharmaceuticals, Inc.Inventors: Sophie Huss, Jose M. Bueno, Jose M. Fiandor, Roger Frechette
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Patent number: 6960667Abstract: 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: GrantFiled: October 10, 2002Date of Patent: November 1, 2005Assignee: Ciba Specialty Chemicals CorporationInventors: Kazuhiko Kunimoto, Junji Otani, Kunihiko Kodama, Hiroshi Yamamoto, Patrick Verhoustraeten, Sonia Megert, Adalbert Braig
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Publication number: 20040266740Abstract: A compound of formula (I): 1Type: ApplicationFiled: January 5, 2004Publication date: December 30, 2004Inventors: Sophie Huss, Jose M. Fiandor, Roger Frechette
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Publication number: 20040248857Abstract: A compound of Formula (I): 1Type: ApplicationFiled: June 1, 2004Publication date: December 9, 2004Applicants: Paratek Pharmaceuticals, Inc., Glaxo Group LimitedInventors: Sophie Huss, Jose M. Bueno, Jose M. Flandor, Roger Frechette
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Patent number: 6355669Abstract: 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: GrantFiled: April 18, 2000Date of Patent: March 12, 2002Assignee: Eisai Co., Ltd.Inventors: Toshihiko Yamauchi, Akira Ishibashi, Naoki Tokuhara, Mitsuo Nagai
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Patent number: 6140321Abstract: 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: GrantFiled: December 30, 1996Date of Patent: October 31, 2000Assignee: Eisai Co., Ltd.Inventors: Akio Imai, Hideaki Watanabe, Takashi Kajima, Yasushi Ishihama, Akiyo Ohtsuka, Tomohide Tanaka
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Patent number: 6057441Abstract: 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: GrantFiled: October 6, 1998Date of Patent: May 2, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Pilar Gil-Lopetegui, Francisco Javier Fernandez-Gadea, Theo Frans Meert
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Patent number: 5985864Abstract: 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: GrantFiled: June 6, 1997Date of Patent: November 16, 1999Assignee: Eisai Co., Ltd.Inventors: Akio Imai, Hideaki Watanabe, Takashi Kajima, Yasushi Ishihama, Akiyo Ohtsuka, Tomohide Tanaka, Yukio Narabu
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Patent number: 5914324Abstract: 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: GrantFiled: July 10, 1997Date of Patent: June 22, 1999Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Sergio De Munari, Elena Folpini, Marco Frigerio, Piero Melloni, Fulvio Serra, Simona Sputore
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Patent number: 5780486Abstract: 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: GrantFiled: May 27, 1997Date of Patent: July 14, 1998Assignee: Novo Nordisk A/SInventors: Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Henrik Sune Andersen, Rolf Hohlweg, Peter Madsen, Uffe Bang Olsen
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Patent number: 5686482Abstract: 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: GrantFiled: October 2, 1996Date of Patent: November 11, 1997Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Junya Ohmori, Kyoichi Maeno, Kazuyuki Hidaka, Kazuhiro Nakato, Shuichi Sakamoto, Shin-ichi Tsukamoto
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Patent number: 5574175Abstract: 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: GrantFiled: May 16, 1995Date of Patent: November 12, 1996Assignee: American Cyanamid Co.Inventor: Venkataraman Kameswaran
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Patent number: 5488119Abstract: 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: GrantFiled: October 12, 1993Date of Patent: January 30, 1996Assignee: Ciba-Geigy CorporationInventors: Evelyn Fischer-Reimann, Walter Fischer
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Patent number: 5276053Abstract: 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: GrantFiled: October 6, 1992Date of Patent: January 4, 1994Assignee: Warner-Lambert CompanyInventor: Graham Johnson
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Patent number: 5274135Abstract: 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: GrantFiled: September 20, 1991Date of Patent: December 28, 1993Assignee: The Dow Chemical CompanyInventors: Kenneth J. Bruza, Arnold E. Young, Kurt A. Bell
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Patent number: 5252317Abstract: 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: GrantFiled: May 22, 1992Date of Patent: October 12, 1993Assignee: The State of Oregon Acting by and through the State Board of Higher Education on Behalf of the University of OregonInventor: John F. W. Keana
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Patent number: 5202486Abstract: 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: GrantFiled: July 31, 1990Date of Patent: April 13, 1993Assignee: E. R. Squibb & Sons, Inc.Inventors: Joel C. Barrish, Steven H. Spergel
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Patent number: 5189065Abstract: 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: GrantFiled: October 17, 1991Date of Patent: February 23, 1993Assignee: Roussel UclafInventors: Jorg Czech, Hans H. Sedlacek, Lucien Nedelec, Jacques Guillaume, Christian Marchandeau
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Patent number: 5180736Abstract: 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: GrantFiled: May 17, 1991Date of Patent: January 19, 1993Assignee: Warner-Lambert CompanyInventor: Graham Johnson
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Patent number: 5132313Abstract: 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: GrantFiled: October 26, 1989Date of Patent: July 21, 1992Assignee: University of PittsburghInventors: Alan P. Kozikowski, Yuan-Ping Pang
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Patent number: 5093031Abstract: 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: GrantFiled: October 14, 1988Date of Patent: March 3, 1992Assignee: ISP Investments Inc.Inventors: Robert B. Login, Ratan K. Chaudhuri, Rama K. Haldar, Mohamed M. Hashem, Michael W. Helioff, David J. Tracy
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Patent number: 5071853Abstract: 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: GrantFiled: February 27, 1990Date of Patent: December 10, 1991Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
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Patent number: 4904688Abstract: 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: GrantFiled: March 8, 1989Date of Patent: February 27, 1990Assignee: Akzo N.V.Inventors: Duncan R. Rae, James Cairns
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Patent number: 4876269Abstract: 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: GrantFiled: July 16, 1987Date of Patent: October 24, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventors: Penio Pennev, Parthasarathi Rajagopalan, Richard M. Scribner
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Patent number: 4826996Abstract: 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: GrantFiled: December 9, 1985Date of Patent: May 2, 1989Assignee: Groupement d'Interet Economique dit Centre International De Recherches Dermatologioues C.I.R.D.Inventors: Braham Shroot, Jean Maignan, Gerard Lang
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Patent number: 4798894Abstract: 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: GrantFiled: May 11, 1987Date of Patent: January 17, 1989Assignee: Ethyl CorporationInventor: Duane C. Hargis
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Patent number: 4461899Abstract: 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: GrantFiled: May 24, 1982Date of Patent: July 24, 1984Assignee: Diamond Shamrock Chemicals CompanyInventors: William J. Pyne, Han S. Ku, Robert E. Holm
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Patent number: 4447368Abstract: 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: GrantFiled: March 31, 1982Date of Patent: May 8, 1984Assignee: Siemens-Allis, Inc.Inventors: Herbert Emde, Heinz U. Blank, Peter Schnegg
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Patent number: 4435336Abstract: 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: GrantFiled: March 31, 1982Date of Patent: March 6, 1984Assignee: Bayer AktiengesellschaftInventors: Herbert Emde, Heinz U. Blank, Peter Schnegg