Carbocyclic Ring Bonded Directly To The Chalcogen Patents (Class 548/575)
  • Publication number: 20150099810
    Abstract: Fragrances that provide a scent of freshness tend to be volatile and are therefore not very economical when used in typical applications such as washing or cleaning processes, so they have to be used in relatively large quantities to be able to produce adequate effects. The disclosed photolabile pro-fragrances provide a much longer-lasting sense of fragrance, in particular with a scent of freshness, when used in typical applications, thus allowing said fragrances to be used economically.
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Thomas Gerke, Christian Kropf, Ursula Huchel, Axel Griesbeck, Agnieszka Landes
  • Publication number: 20150093365
    Abstract: Provided herein are compositions containing photoactivatable caged tamoxifen and tamoxifen derivative molecules. Also provided are kits containing one of these compositions and a light source. Also provided are methods of optically inducing nuclear translocation of a fusion protein containing a mammalian estrogen receptor ligand binding domain in a eukaryotic cell and methods of optically inducing recombination in a eukaryotic cell that include contacting a eukaryotic cell with at least one of these compositions. Also provided are methods of treating breast cancer in a subject that include administering a photoactivatable caged tamoxifen or tamoxifen derivative molecule to a subject having breast cancer.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 2, 2015
    Inventors: Xin Lu, Sarit S. Agasti, Ronald A. DePinho, Ralph Weissleder
  • Publication number: 20140081017
    Abstract: The present invention relates to compositions and methods to selectively treat fungal infection. More particularly, the invention relates to compounds, compositions thereof, and methods for selectively enhancing fungal sensitivity to antifungal compounds.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 20, 2014
    Applicant: METHYLGENE INC.
    Inventor: METHYLGENE INC.
  • Publication number: 20120190854
    Abstract: A method includes reacting an amino group, a composition including rhodium and an organic ligand, and a substrate having structural formula (I) in a reaction mixture. R1 is an organic group including a sp3 carbon atom bonded to CA. R2 is selected from the group consisting of hydrogen, methyl, and an organic group including a sp3 carbon atom bonded to CA. R3 and R4 independently are selected from the group consisting of hydrogen, methyl, and an organic group including a sp3 carbon atom bonded to CB. The method further includes forming a hydroaminated product in the reaction mixture.
    Type: Application
    Filed: April 5, 2012
    Publication date: July 26, 2012
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Akihiro Takemiya, Zhijian Liu, John F. Hartwig
  • Patent number: 8202513
    Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Grant
    Filed: October 3, 2008
    Date of Patent: June 19, 2012
    Assignee: Bionomics Limited
    Inventors: Bernard Luke Flynn, Jonathan Bayldon Baell, Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Andrew John Harvey, Jorgen Alvar Mould, Dharam Paul
  • Publication number: 20110077231
    Abstract: Novel compounds, with the following being exemplary:
    Type: Application
    Filed: August 12, 2008
    Publication date: March 31, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Walter Rainer
  • Publication number: 20100297077
    Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Application
    Filed: October 3, 2008
    Publication date: November 25, 2010
    Applicant: BIONOMICS LIMITED
    Inventors: Bernard Luke Flynn, Jonathan Bayldon Baell, Jason Hugh Chaplin, Girmit Singh Gill, Damian Wojciech Grobelny, Andrew John Harvey, Jorgen Alvar Mould, Dharam Paul
  • Publication number: 20100279997
    Abstract: A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula A, wherein A, B, X, R1, R2, R7 and R8, and the dashed lines are defined within.
    Type: Application
    Filed: October 28, 2009
    Publication date: November 4, 2010
    Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
  • Publication number: 20100035929
    Abstract: Disclosed are dispyrin analogue compounds useful as H3 receptor activity modulators, methods of making same, pharmaceutical compositions comprising same, and methods of treating neurological and psychiatric disorders associated with histamine H3 receptor activity using same. In one aspect, the disclosed analogues can have a structure represented by a formula: This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: June 8, 2009
    Publication date: February 11, 2010
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, J. Phillip Kennedy, John T. Brogan
  • Publication number: 20090111808
    Abstract: The present patent application concerns compounds of formula (I) with R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.
    Type: Application
    Filed: April 25, 2006
    Publication date: April 30, 2009
    Inventors: Isabelle Bertrand, Marc Capet, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Olivia Poupardin-Olivier, Philippe Robert, Jean-Charles Schwartz, Olivier Labeeuw
  • Publication number: 20090012314
    Abstract: Disclosed is a novel process for production of lasofoxifene, nafoxidine or an analogue thereof, which comprises reduced number of reaction steps, has a high efficiency, and is practically advantageous. For the production of lasofoxifene or an analogue thereof, a compound represented by the formula (4) is used as an intermediate. The compound represented by the formula (4) can be produced using compounds represented by the formulae (1) to (3) as starting compounds by performing the coupling of the three components in one step.
    Type: Application
    Filed: January 25, 2007
    Publication date: January 8, 2009
    Applicant: TOKYO UNIVERSITY OF SCIENCE EDUCATIONAL FOUNDATION ADMINISTRATIVE ORGANIZATION
    Inventors: Isamu Shiina, Yoshiyuki Sano, Kenya Nakata
  • Publication number: 20080255089
    Abstract: Triphenylethylene compounds of formula (I) are provided. The compounds are particularly useful for selective estrogen receptor modulation.
    Type: Application
    Filed: November 22, 2006
    Publication date: October 16, 2008
    Inventor: Subba Reddy Katamreddy
  • Patent number: 6900243
    Abstract: There are provided novel compounds of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: May 31, 2005
    Assignee: AstraZeneca AB
    Inventors: David Cheshire, Stephen Connolly, David Cox, Antonio Mete
  • Patent number: 6890920
    Abstract: Novel quaternary ammonium compounds of the formula and any stereoisomers thereof, wherein R1, R2 and R3 independently represent C1-C6 alkyl, optionally substituted with phenyl or hydroxyl, or both, and wherein any two of R1, R2 and R3 may form a ring together with the quaternary ammonium nitrogen; R4 represents —H, —CH3, or —CO—R4-1, wherein R4-1 represents —(C1-C4 alkyl), —(C1-C4 alkoxy), or —NR4-2R4-3, wherein R4-2 and R4-3 independently represent —H or —(C1-C4 alkyl); R5, R6 and R7 independently represent —H, —OCH3, —OH, —CONH2, —SO2NH2, —F, —Cl, —Br, —I, —CF3, or —(C1-C4 alkyl), optionally substituted with one or two —OH, —(C1-C4 alkoxy), —COOH, or —CO—O—(C1-C3 alkyl); and X? represents an anion of a pharmaceutically acceptable acid, the compounds for use as medicaments, use of the compounds for the manufacture of specific medicaments, and pharmaceutical compositions comprising the compounds. The present invention also concerns a method of treatment involving administration of the compounds.
    Type: Grant
    Filed: October 25, 2002
    Date of Patent: May 10, 2005
    Assignee: Pharmacia & Upjohn Company
    Inventors: Ivan Richards, Sue K. Cammarata, Craig D. Wegner, Michael Hawley, Mark Peter Warchol, Mark Kontny, Walter Morozowich, Karen Patrice Kolbasa, Malcolm Wilson Moon, Dominique Bonafoux, Sergey Gregory Wolfson, Patrick James Lennon
  • Patent number: 6821998
    Abstract: Methods for treating CMV and CMV-related diseases are provided that use compounds having the formula: wherein the subscripts m and n are each independently integers from 1 to 2; and the R groups are as defined in the specification.
    Type: Grant
    Filed: August 29, 2002
    Date of Patent: November 23, 2004
    Assignee: ChemoCentryx, Inc.
    Inventors: Brian E. McMaster, Thomas J. Schall, Mark Penfold, J. J. Wright, Daniel J. Dairaghi
  • Patent number: 6812244
    Abstract: The instant invention provides novel substituted naphthyl compounds, intermediates, compositions, pharmaceutical formulations, and methods of use.
    Type: Grant
    Filed: May 27, 2003
    Date of Patent: November 2, 2004
    Assignee: Eli Lilly and Company
    Inventors: Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones, Alan David Palkowitz
  • Patent number: 6774244
    Abstract: Primary intermediates for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein R is selected from C1 to C5 alkyl or hydroxyalkyl, a C3 to C6 cyclic ring containing hetero atoms selected from O, S and N atoms, and —CH2—Ar where Ar is an aromatic ring wherein the aromatic ring may be substituted with one or two hydroxy C1 to C3 alkoxy, or amino groups.
    Type: Grant
    Filed: January 18, 2002
    Date of Patent: August 10, 2004
    Assignee: The Procter & Gamble Company
    Inventors: Mu-Ill Lim, Yuh-Guo Pan
  • Patent number: 6680336
    Abstract: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
    Type: Grant
    Filed: February 15, 2002
    Date of Patent: January 20, 2004
    Assignee: ICOS Corporation
    Inventors: Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Laurence E. Burgess, Stephen T. Schlachter
  • Patent number: 6608212
    Abstract: The present invention provides a process for preparing a vinylaromatic compound comprising reacting an arylmetal reagent selected from arylmagnesium reagents and aryllithium reagents with a vinylphosphate in the presence of a palladium catalyst. The present invention also provides a process for preparing a vinylphosphate comprising reacting an enolizable ketone with a sterically hindered Grignard reagent and a halophosphate diester.
    Type: Grant
    Filed: June 4, 2002
    Date of Patent: August 19, 2003
    Assignees: Pfizer, Inc., DSM NV
    Inventor: Joseph Miller
  • Patent number: 6541471
    Abstract: A compound of formula (I): wherein: G represents a group such as: wherein R1 and R2 independently represent a hydrogen atom or an alkyl, cycloalkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl or heteroarylalkyl group, or, R1 and R2 together with the nitrogen atom form a heterocycloalkyl group, R3 represents a hydrogen atom or an alkyl or optionally substituted phenyl group, Ra represents a hydroxy group, a linear or branched (C1-C6)alkoxy group or an amino group, Rb and Rc, which may be identical or different, each represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a hydroxy group or a trihaloalkyl group, m is an integer of from 0 to 1 inclusive, n and q are integers of from 0 to 6 inclusive, p and r are integers of from 1 to 6 inclusive, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base; and medicinal products containing the same which are useful as a TXA2 recept
    Type: Grant
    Filed: July 12, 2002
    Date of Patent: April 1, 2003
    Assignee: Les Laboratoires Servier
    Inventors: Gilbert Lavielle, Thierry Dubuffet, Bernard Cimetiere, Tony Verbeuren, Serge Simonet, Christine Vayssettes-Courchay
  • Patent number: 6509356
    Abstract: A class of substituted benzylnaphthylene compounds of the structure where R1 and R2 are independently hydrogen, alkyl of one to six carbon atoms, acyl of two to six carbon atoms, or phenacyl; X is —(CH2)1-6; Y is absent or is selected from 1,4-piperazinylene; ureido; N-(lower alkyl)ureido; N′-(lower alkyl)ureido; or N, N′-(di-lower alkyl ureido; and Z is 1-, 2- or 3-pyrrolidinyl; 1-, 2-, or 3-[1-(lower alkyl) pyrrolidinyl]; 1- 2-, 3- or 4-piperidinyl; 1-, 2-, 3- or 4-[1-lower alkyl)piperidinyl]; N,N-dialkyl; 1-azepinyl; 1- or 2-naphthylamino, 4-morpholinyl, dimethyl-4-morpholinyl, 3-azaspiro[5.
    Type: Grant
    Filed: August 4, 1998
    Date of Patent: January 21, 2003
    Assignee: Eli Lilly and Company
    Inventors: Jeffrey Alan Dodge, Andrew Lawrence Glasebrook, Charles Willis Lugar, III
  • Patent number: 6444688
    Abstract: The instant invention provides compounds of formula I wherein R1 is OH, O—C(O)—(C1-C6 alkyl), O—C(O)—O(C1-C6 alkyl), O—C(O)—Ar, or O—C(O)—O—Ar; R2 is H, OH, O(C1-C6 alkyl), O—C(O)—(C1-C6 alkyl), O—C(O)—O(C1-C6 alkyl), O—C(O)—Ar, O—C(O)—O—Ar, O—SO2—(C4-C6 alkyl), chloro, fluoro, or bromo; V is S, O, or CH2CH2; W is CHOH, C(O), or CH2; X is (CH2)n; R3 and R4 each, independently, are H, C1-C6 alkyl, C(O)—(C1-C6 alkyl), C(O)—NH—(C1-C6 alkyl), C(O)—Ar, or together with the nitrogen to which they are attached form a 5- or 6-membered imide or cyclic amide; n is 1, 2, or 3; and Ar is optionally substituted phenyl; povided that at least one of R3 and R4 contains a carbonyl functional group, and their use in the treatment of estrogen deficiency pathologies.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 3, 2002
    Assignee: Eli Lilly and Company
    Inventors: Jeffrey A. Dodge, Charles D. Jones, Kristin Marron, James P. Sluka, Mark G. Stocksdale
  • Patent number: 6362373
    Abstract: The disclosed invention comprises a compound having the formula: in which R1 and R2 independently represent a hydrogen or an alkyl group of 4 carbon atoms or greater. Further disclosed is a process for the preparation of the disclosed chiral amino alcohols from a starting amine compound and a limonene oxide.
    Type: Grant
    Filed: September 13, 2000
    Date of Patent: March 26, 2002
    Assignees: The Dow Chemical Company
    Inventors: Christian T. Goralski, Bakthan Singaram, William Chrisman
  • Patent number: 6323345
    Abstract: This invention provides an improved process for cis-1-{2-[4-(6-methoxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenoxy]ethyl}pyrrolidine which is an intermediate for the preparation of (−)cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol which is useful for the treatment of osteoporosis.
    Type: Grant
    Filed: February 27, 2001
    Date of Patent: November 27, 2001
    Assignee: Pfizer Inc.
    Inventor: Charles K. F. Chiu
  • Patent number: 6307087
    Abstract: One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.
    Type: Grant
    Filed: January 13, 1999
    Date of Patent: October 23, 2001
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, David W. Old, John P. Wolfe, Michael Palucki, Ken Kamikawa
  • Patent number: 6201130
    Abstract: Compounds of the formula I: stereoisomeric forms, and physiologically tolerable salts thereof are suitable for the production of pharmaceuticals for the therapy and prophylaxis of disorders involving matrix-degrading metalloproteinases.
    Type: Grant
    Filed: November 5, 1999
    Date of Patent: March 13, 2001
    Assignee: Aventis Pharma Duetschland GmbH
    Inventors: Wilfried Schwab, Werner Thorwart, Manfred Schudok, Burkhard Haase
  • Patent number: 6197770
    Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where X, W, Z, A, G, R1, R2, R3, R4, R5, R5′ and k have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof Also described are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: March 6, 2001
    Assignee: The Procter & Gamble Co.
    Inventors: Michael George Natchus, Roger Gunnard Bookland, Neil Gregory Almstead, Stanislaw Pikul, Biswanath De, Menyan Cheng
  • Patent number: 6100428
    Abstract: An improved method for guanylating amines is provided. Broadly, the amines are reacted with a guanylating agent in the presence of a nickel catalyst. Preferably, the nickel catalyst comprises nickel in the zero oxidation state. Suitable nickel(0) catalysts are derived from nickel-boride alloys, nickel-phosphide alloys, aluminum-nickel alloys, nickel on kieselguhr, and nickel on silica/alumina catalysts. Preferred guanylating agents are thioureas and isothioureas. In one embodiment, protecting groups are selectively attached to the guanylating agents to yield particular substituted guanidines. The preferred protecting groups are Boc groups, Cbz groups, and arylsulfonyl groups. The reactions are particularly well suited for guanylating primary and secondary amines. The methods of the invention can be carried out under ambient conditions to provide high yields of the corresponding guanidines, with the nickel catalyst being essentially completely recoverable for reuse.
    Type: Grant
    Filed: October 6, 1999
    Date of Patent: August 8, 2000
    Assignee: The University of Kansas
    Inventors: Laxminarayan Bhat, Gunda I. Georg
  • Patent number: 5998443
    Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel phosphorous-containing benzothiophene compounds which are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.
    Type: Grant
    Filed: October 8, 1997
    Date of Patent: December 7, 1999
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, Jeffrey A. Dodge, Jeffrey S. Nissen
  • Patent number: 5948809
    Abstract: (-)Cis-6(S)-phenyl-5(R)-?4-(2-pyrrolidin-1-yl ethoxy)phenyl!-5,6,7,8-tetrahydro-naphthalen-2-ol D-tartrate, pharmaceutical compositions comprising this compound, and an advantageous process for preparing the compound.
    Type: Grant
    Filed: April 28, 1998
    Date of Patent: September 7, 1999
    Assignee: Pfizer Inc
    Inventors: Charles K. Chiu, Morgan Meltz
  • Patent number: 5686464
    Abstract: A 3,3-diphenylpropylamine of the formula I, or its physiologically acceptable acid salt thereof: ##STR1## wherein R.sup.1 represents hydrogen or methyl, R.sup.2 and R.sup.3 independently represent hydrogen, methyl, methoxy, hydroxy, carbamoyl, sulphamoyl or halogen, and X represents a tertiary amino group of formula II ##STR2## wherein R.sup.4 and R.sup.5 independently represent a hydroxy substituted or unsubstituted non-aromatic hydrocarbyl group which can join together to form a ring and which together contain at least three carbon atoms, wherein at least one of R.sup.4 and R.sup.5 is hydroxy substituted, is useful in treating acetylcholine-mediated disorders such as urinary incontinence.
    Type: Grant
    Filed: July 22, 1996
    Date of Patent: November 11, 1997
    Assignee: Pharmacia AB
    Inventors: Rolf Arne Johansson, Pinchas Moses, Lisbeth Nilvebrant, Bengt .ANG.ke Sparf
  • Patent number: 5565611
    Abstract: The present invention provides a process for preparing an acid addition salt of the Z-isomer of a compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 represent a lower alkyl group, or taken together with the nitrogen atom to which they are attached, form a nitrogen-containing heterocyclic group optionally containing other hetero atom or atoms; R.sup.3 and R.sup.4 represent H, a lower alkyl group, OH, a lower alkoxy group, a lower alkylcarbonyloxy group, an arylcarbonyloxy group optionally substituted with 1-2 substituents selected from lower alkyl, lower alkoxy, halo and CN on the benzene ring, a benzylcarbonyloxy group, a mono- or di(lower alkyl)aminocarbonyloxy group or a mono- or di(aryl)aminocarbonyloxy group; R.sup.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 15, 1996
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Shinozaki Fumihiko, Nagasawa Hiroshi, Maruhashi Kazuo
  • Patent number: 5552412
    Abstract: Compounds of this formula ##STR1## are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.
    Type: Grant
    Filed: January 9, 1995
    Date of Patent: September 3, 1996
    Assignee: Pfizer Inc
    Inventors: Kimberly O. Cameron, Paul A. Dasilva Jardine, Robert L. Rosati
  • Patent number: 5525633
    Abstract: The present invention relates to novel triaryl-ethylene derivatives that are useful as anti-neoplastic agents, antiatherosclerotic agents, and hypocholesterolemic agents.
    Type: Grant
    Filed: June 15, 1994
    Date of Patent: June 11, 1996
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Donald P. Matthews, Alan J. Bitonti, William A. Van Sickle, Donald A. Kaplan
  • Patent number: 5500443
    Abstract: A compound of formula (I): ##STR1## in which: X represents oxygen or methylene,n represents 1, 2 or 3,R.sub.1 represents hydrogen, aminocarbonyl or hydroxymethyl,R.sub.2 represents: ##STR2## in which R.sub.3 and R.sub.4 are as defined in the description, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same are useful in the treatment of schizophrenia.
    Type: Grant
    Filed: February 22, 1995
    Date of Patent: March 19, 1996
    Assignee: Adir et Compagnie
    Inventors: Gilbert Lavielle, Patrick Hautefaye, Olivier Muller, Mark Millan, Mauricette Brocco
  • Patent number: 5492922
    Abstract: The present invention provides pharmaceutically active compounds of formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl), or halo, providing when Z is --S--, R.sup.2 is not halo;R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andz is --O-- or --S--;or a pharmaceutically acceptable salt thereof, for inhibiting aortal smooth muscle proliferation.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: February 20, 1996
    Assignee: Eli Lilly and Company
    Inventor: Alan D. Palkowitz
  • Patent number: 5416210
    Abstract: In one aspect, compounds, methods of using them, compositions comprising such compounds, and uses of such compositions.These objects, and others which will become apparent from the following disclosure, are achieved by the present invention which comprises in one aspect compounds of the formula ##STR1## wherein R is alkyl, cycloalkyl, aryl, substituted aryl, alkaryl optionally substituted on the aryl portion or aralkyl optionally substituted on the aryl portion, R having up to 20 carbon atoms and is optionally branched, andA is (CH.sub.2).sub.p, (CH.sub.2).sub.q --O--(CH.sub.2).sub.r, or (CH.sub.2).sub.q --S--(CH.sub.2).sub.r,wherein p=2 to 8, q=1 to 8, and r=1 to 8.R.sub.1 =--(CH.sub.2).sub.m --, --(CH.sub.2 CH.sub.2 --O).sub.n --CH.sub.2 CH.sub.2 --, or --(CH.sub.2 CH.sub.2 CH.sub.2 --O).sub.n --CH.sub.2 CH.sub.2 CH.sub.2 --.
    Type: Grant
    Filed: June 10, 1992
    Date of Patent: May 16, 1995
    Assignee: Rohm and Haas Company
    Inventors: Samuel E. Sherba, Raj J. Mehta, Margaret M. Bowers-Daines, Adam C. Hsu
  • Patent number: 5321138
    Abstract: The present invention provides compounds having glutathione peroxidase activity and, therefore, are effective glutathione peroxidase replacements. These compounds are useful as drugs for the prevention of cataracts and as anti-oxidants for H.sub.2 O.sub.2 and other peroxides. The present invention also provides methods and pharmaceutical compositions of the compound.
    Type: Grant
    Filed: April 29, 1991
    Date of Patent: June 14, 1994
    Assignees: The Trustees of Columbia University in the City of New York, New York University
    Inventors: Abraham Spector, Stephen R. Wilson, Paul A. Zucker
  • Patent number: 5272144
    Abstract: Aryloxy- and heteroaryloxy-alkylene derivatives of amines of formula ##STR1## wherein each of A and B is a group of formula (i) to (iii): ##STR2## wherein Y is --O--, --S-- or --NR-- in which R is hydrogen or C.sub.1 -C.sub.6 alkyl; each of R.sub.3, R.sub.4, R.sub.5 and R.sub.6 is independently:a) hydrogen, halogen, hydroxy, cyano or nitro;b) C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by halogen,c) C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio;d) C.sub.1 -C.sub.6 alkyl-sulfonyl;e) a substituted amine group --NR.sub.7 R.sub.8 ;f) a --COR.sub.12 group; org) two adjacent groups of R.sub.3, R.sub.4, R.sub.5 and R.sub.6, taken together, form a C.sub.1 -C.sub.4 alkylenedioxy group;each of R.sub.1 and R.sub.2 independently is hydrogen, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 alkenyl or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl; or R.sub.1 and R.sub.
    Type: Grant
    Filed: June 13, 1991
    Date of Patent: December 21, 1993
    Assignee: Farmitalia Carlo Erba s.r.l.
    Inventors: Piero Melloni, Philippe Dostert, Arturo D. Torre, Alberto Bonsignori
  • Patent number: 5250562
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are lower-alkyl; or together are alkylene with 3-5 C-atoms in a straight chain; one of the residues R.sup.3 and R.sup.4 is hydrogen and the other is hydrogen or lower-alkyl; R.sup.6 and R.sup.7 are hydrogen or lower-alkyl; R.sup.5 and R.sup.8 are hydrogen, lower-alkyl, lower-alkoxy or halogen; X signifies --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.9 ; R.sup.9 is hydrogen, lower-alkyl or acyl; Y is --S(O).sub.m R.sup.10 or --NHet and, where X is --NR.sup.9 --, --S--, --SO-- or --SO.sub.2 --, also --N(R.sup.11).sub.2 or --OR.sup.12 ; R.sup.10 is lower-alkyl; R.sup.11 and R.sup.12 are hydrogen, lower-alkyl or acyl; --NHet is a 5-8 membered, saturated or unsaturated, monocyclic heterocycle attached via a N-atom; n is 2, 3 or 4 and m is 0, 1 or 2, are described. The compounds of formula I are useful as agents for the treatment of disorders such as neoplasms, dermatoses or ageing of the skin.
    Type: Grant
    Filed: February 3, 1992
    Date of Patent: October 5, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
  • Patent number: 5192799
    Abstract: Amine represented by the following formula (1), or their acid addition salts or their quaternary ammonium salts. ##STR1## The amines of formula (1) or their pharmaceutically acceptable acid addition salts or quaternary ammonium salts are useful for the treatment and prevention of heart diseases of animals, particularly arrhythima, myocardial infarction, angina pectoris and heart failure and psychoneurological diseases.
    Type: Grant
    Filed: June 5, 1992
    Date of Patent: March 9, 1993
    Assignee: Mitsui Petrochemical Industries, Ltd.
    Inventors: Ikuo Tomino, Masaharu Ishiguro, Takumi Kitahara, Keiichi Yokoyama, Noriaki Kihara, Joji Kamiya, Kanji Yoshihara, Masaaki Ishii, Akira Mizuchi, Kazutoshi Horikomi, Akira Awaya, Takuo Nakano
  • Patent number: 5071844
    Abstract: The invention provides compounds of the formula: ##STR1## wherein k is 1, 2 or 3;m is 1, 2 or 3;n is 1, 2 or 3;p is 0, 1 or 2;X is O, S or a direct link, with the proviso that when X is O or S, n is 2 or 3;R.sup.1 is H or C.sub.1-C.sub.4 alkyl; andR.sup.2 is an optionally substituted phenyl or heteroaryl group; andpharmaceutically acceptable salts thereof.These compounds are useful for the treatment of motility disorders, particularly those of the gut such as irritable bowel syndrome.
    Type: Grant
    Filed: May 23, 1990
    Date of Patent: December 10, 1991
    Assignee: Pfizer Inc.
    Inventors: David Alker, Robert J. Bass, Peter E. Cross
  • Patent number: 5068245
    Abstract: N-Substituted 3-arylpyrrolidine derivatives of the formula ##STR1## where R.sup.1 is 2,2-dimethylpropyl, 3,3-dimethylbutyl, 4,4-dimethylpentyl, 2,4,4-trimethylpentyl, 6-methylhept-2-yl, 3,5,5-trimethylhexyl, 6,10-dimethylundec-2-yl, 3-methylcyclohexyl, 3,3-dimethylcyclohexyl, 3,3,5-trimethylcyclohexyl, 3,3,5,5-tetramethylcyclohexyl, 4-methylcyclohexyl, 4-ethylcyclohexyl, 4-propylcyclohexyl, 4-isopropylcyclohexyl, 4-tert.-butylcyclohexyl, trans-4-tert.-butylcyclohexyl, 4(2-methylbut-2-yl)cyclohexyl, 4(2,4,4-trimethylpent-2-yl)-cyclohexyl, cyclododecanyl, C.sub.3 -C.sub.9 -trialkylsilyl-substituted C.sub.4 -C.sub.12 -cycloalkyl, 4-hydroxycyclohexyl, 4-hydroxy-3-methylcyclohexyl, 4-hydroxy-3,5-dimethylcyclohexyl, 4-hydroxy-3,3-dimethylcyclohexyl, 4-hydroxy-3,3,5-trimethylcyclohexyl, unsubstituted or hydroxy-, C.sub.1 -C.sub.9 -alkyl-, C.sub.1 -C.sub.5 -alkoxy- or C.sub.3 -C.sub.9 -trialkylsilyl-substituted C.sub.5 -C.sub.12 -cycloalkenyl,R.sup.1 is further bicycloalkyl,R.sup.1 is further 4-tert.
    Type: Grant
    Filed: September 30, 1988
    Date of Patent: November 26, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Matthias Zipplies, Hubert Sauter, Franz Roehl, Walter Himmele, Eberhard Ammermann, Ernst-Heinrich Pommer
  • Patent number: 5068246
    Abstract: 3-Alkyl-4-arylpyrrolidine derivatives of the formula ##STR1## where R.sup.1 is alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkyl-cycloalkyl, cycloalkyl-alkyl, alkyl-cycloalkyl-alkyl, cycloalkenyl-alkyl, alkyl-cycloalkenyl, bicycloalkyl, bicycloalkylalkyl, alkyl-bicycloalkyl, heterocycloalkyl, heterocycloalkylmethyl, aryl, arylalkyl, alkylary, alkyl-aryl-alkyl,R.sup.2 is alkyl, alkoxy,R.sup.3 is alkylR.sup.4 is alkyl, alkenyl, alkynyl and phenylalkyl,X.sup.- is a plant-tolerated anion, andn is 0 or 1,their plant-tolerated salts, and fungicides containing these compounds.
    Type: Grant
    Filed: September 30, 1988
    Date of Patent: November 26, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Matthias Zipplies, Hubert Sauter, Walter Himmele, Eberhard Ammermann, Ernst-Heinrich Pommer
  • Patent number: 5017572
    Abstract: The present invention relates to compounds of formula: ##STR1## in which: R.sub.1 and R.sub.2 are such that:either R.sub.1 represents a methoxy group in which case R.sub.2 is a group chosen from the following: hydroxyl; C.sub.1 -C.sub.4 alkyl; C.sub.2 -C.sub.8 alkyloxy; C.sub.5 -C.sub.7 cycloalkyloxy; benzyloxy;or R.sub.2 represents a methoxy group in which case R.sub.1 is a group chosen from the following: hydroxyl; C.sub.2 -C.sub.8 alkyloxy; C.sub.2 -C.sub.8 alkyloxy substituted by a methoxy group; C.sub.1 -C.sub.4 trifluoroalkyloxy; C.sub.3 -C.sub.4 alkenyloxy; C.sub.5 -C.sub.7 cycloalkyloxy; benzyloxy; C.sub.1 -C.sub.4 alkyhlthio;n=2 or 3; andp=4, 5 or 6,as well as their addition salts with mineral or organic acids, said compounds and salts being useful as drugs.
    Type: Grant
    Filed: April 18, 1989
    Date of Patent: May 21, 1991
    Assignee: Delalande S.A.
    Inventors: Mona Ward, Pierre-Andre Ph.Settembre, Alain Renaud, Michel Langlois
  • Patent number: 4999361
    Abstract: The present invention provides compounds of the general formula ##STR1## wherein R.sub.1 is a hydrogen atom, a straight-chained or branched C.sub.1 -C.sub.12 -alkyl radical, a C.sub.3 -C.sub.7 -cycloalkyl radical, a straight-chained or branched C.sub.2 -C.sub.12 -alkenyl radical or an unsubstituted or substituted C.sub.3 -C.sub.7 -mono- or bicycloalkenyl radical, an unsubstituted or singly or multiple substituted monocyclic aromatic or heteroaromatic radical, R.sub.2 and R.sub.3, which can be the same or different, are straight-chained, branched, saturated or unsaturated C.sub.1 -C.sub.6 -aliphatic radicals or, together with the nitrogen atom to which they are attached, form a saturated or unsaturated ring which can contain further heteroatoms and can optionally be substituted by a lower alkyl radical, a lower alkoxy radical or an oxygen atom, R.sub.4 is an unsubstituted or singly or multiple substituted monocyclic aromatic radical, an unsubstituted or substituted five- or six-membered heteroaromatic ring, R.
    Type: Grant
    Filed: February 27, 1989
    Date of Patent: March 12, 1991
    Assignee: Boehringer Mannheim GmbH
    Inventors: Christos Tsaklakidis, Herbert Leinert, Peter Freund
  • Patent number: 4996225
    Type: Grant
    Filed: October 12, 1989
    Date of Patent: February 26, 1991
    Assignee: Farmos Group Ltd.
    Inventors: Reijo J. Toivola, Arto J. Karjalainen, Kauko O. A. Kurkela, Marja-Liisa Soderwall, Lauri V. M. Kangas, Guillermo L. Blanco, Hannu K. Sundquist
  • Patent number: 4996215
    Abstract: A new piperidine compound is pharmacologically effective for treatment of the arrythmia and is defined by the formula: ##STR1## in which R.sup.1 is a lower alkyl or a tolyl, R.sup.2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R.sup.3 is hydrogen, a lower alkyl, a lower alkenyl, a cycloalkyl or a cycloalkylalkyl, X is --CO--, --CH.sub.2 -- or --CHOH--, g is an integer of 1 to 3, h is an integer of 1 to 3, Y is hydrogen, a lower alkyl, a lower alkenyl, cyano, --CH.sub.2 COOR, R being hydrogen or a lower alkyl, a cycloalkyl, a cycloalkylalkyl, ##STR2## l being 1 or 2, --A--B, A being --(CH.sub.2).sub.
    Type: Grant
    Filed: September 15, 1989
    Date of Patent: February 26, 1991
    Assignee: Eisai Co., Ltd.
    Inventors: Hitoshi Oinuma, Motosuke Yamanaka, Kazutoshi Miyake, Tomonori Hoshiko, Norio Minami, Tadao Shoji, Yoshiharu Daiku, Kohei Sawada, Kenichi Nomoto
  • Patent number: 4933346
    Abstract: Compounds I are described ##STR1## with R.sup.1 equal to (cyclo)alk(en)yl or ##STR2## R.sup.2 /R.sup.3 equal to phenyl or phenylalkyl, A equal to ##STR3## m equal to 2-4, and n equal to 1-4.Compounds I and their salts are calcium antagonists.
    Type: Grant
    Filed: May 10, 1988
    Date of Patent: June 12, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Ruger, Hansjorg Urbach, Joachim Kaiser
  • Patent number: RE39558
    Abstract: Compounds of this formula are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.
    Type: Grant
    Filed: December 23, 2004
    Date of Patent: April 10, 2007
    Assignee: Pfizer Inc.
    Inventors: Kimberly O. Cameron, Paul A. DaSilva Jardine, Robert L. Rosati