Plural Chalcogens Bonded Directly To The Bicyclo Ring System Patents (Class 549/54)
  • Publication number: 20150018547
    Abstract: The present invention provides a compound having a GOAT inhibitory action, which is useful for the prophylaxis or treatment of obesity and the like, and has superior efficacy. The present invention is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: February 22, 2013
    Publication date: January 15, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Nobuyuki Takakura, Yoshihiro Banno, Yoshito Terao, Atsuko Ochida, Sachie Morimoto, Shuji Kitamura, Yoshihide Tomata, Tsuneo Yasuma, Minoru Ikoma, Kei Masuda
  • Patent number: 8877801
    Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.
    Type: Grant
    Filed: February 12, 2014
    Date of Patent: November 4, 2014
    Assignee: Novartis AG
    Inventors: Heather Elizabeth Burks, Michael A. Dechantsreiter, Guo He, Jill Nunez, Stefan Peukert, Clayton Springer, Yingchuan Sun, Noel Marie-France Thomsen, George Scott Tria, Bing Yu
  • Publication number: 20140235660
    Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.
    Type: Application
    Filed: February 12, 2014
    Publication date: August 21, 2014
    Applicant: NOVARTIS AG
    Inventors: Heather Elizabeth BURKS, Michael A. DECHANTSREITER, Guo HE, Jill NUNEZ, Stefan PEUKERT, Clayton SPRINGER, Yingchuan SUN, Noel Marie-France THOMSEN, George Scott TRIA, Bing YU
  • Patent number: 8574607
    Abstract: Compounds of the formula (I) useful as pesticides are disclosed, wherein the substituents are as defined in claim 1.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: November 5, 2013
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Jürgen Harry Schaetzer, Thomas Pitterna, Long Lu, Yaming Wu, Peter Renold, Francesca Perruccio, Jérome Yves Cassayre, Michel Mueglebach
  • Publication number: 20110275515
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Application
    Filed: January 18, 2010
    Publication date: November 10, 2011
    Applicant: SYNGENTA CROP PROTECTION, LLC
    Inventors: William Guy Whittingham, Christopher John Mathews, Jeffrey Steven Wailes, Stephane André Marie Jeansmart, Louisa Robinson
  • Patent number: 7973180
    Abstract: The present invention provides a method for the production of an aqueous dispersion containing an electroconductive polymer component which enables electroconductive thin films which are outstanding in their transparency and electroconductivity to be formed, together with the aqueous dispersion obtained by said method. This method includes a stage in which a 3,4-dialkoxythiophene is polymerized in an aqueous solvent using an oxidizing agent in the presence of a polyanion and, in this stage, said oxidizing agent is added by the dropwise addition of a solution or dispersion containing said oxidizing agent to the reaction solution or, alternatively, in the polymerization stage, the alkali metal ion concentration in the reaction liquid is maintained at no more than 400 ppm.
    Type: Grant
    Filed: October 6, 2006
    Date of Patent: July 5, 2011
    Assignee: H.C. Starck GmbH
    Inventors: Yoshiyuki Morita, Yasuo Chikusa, Kyoko Miyanishi, Stephan Kirchmeyer, Wilfried Loevenich
  • Patent number: 7655641
    Abstract: The present invention is directed to a compound of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates or stereoisomers thereof, which are useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.
    Type: Grant
    Filed: February 10, 2004
    Date of Patent: February 2, 2010
    Assignee: Eli Lilly and Company
    Inventors: Scott Eugene Conner, Lynn Stacy Gossett, Jonathan Edward Green, Winton Dennis Jones, Jr., Nathan Bryan Mantlo, Donald Paul Matthews, Daniel Ray Mayhugh, Daryl Lynn Smith, Jennifer Ann Vance, Xiaodong Wang, Alan M Warshawsky, Leonard Larry Winneroski, Jr., Yanping Xu, Guoxin Zhu
  • Publication number: 20080275066
    Abstract: The invention provides compounds of formula (I) for use as GLP-1 receptor agonists.
    Type: Application
    Filed: June 21, 2005
    Publication date: November 6, 2008
    Applicant: Novo Nordisk A/S
    Inventors: Sanne Moller Knudsen, Ingrid Pettersson, Jesper Lau, Carsten Behrens, Anders Klarskov Petersen, Jesper Lau, Patrick William Garibay
  • Publication number: 20080207922
    Abstract: A condensation compound of a fluorinated cyclopentane ring and an aromatic ring, which is useful, for example, for electronic materials, and a process for producing the same are provided. For instance, according to Scheme 1 below, a compound (68) containing a condensed structure formed of a hexafluorocyclopentane ring and an aromatic ring is synthesized. The aromatic ring is not limited to a thiophene ring but can be any ring and any substituent can be used. Thus a compound containing a condensed ring structure formed of a hexafluorocyclopentane ring and an aromatic ring, particularly, for instance, a thiophene ring, which was impossible to produce conventionally, can be produced easily with high yield. The compound of the present invention is particularly suitable to be applied to, for example, electronic materials or semiconductors.
    Type: Application
    Filed: March 2, 2006
    Publication date: August 28, 2008
    Applicant: SUMITOMO CHEMICAL CO., LTD
    Inventors: Yutaka Ie, Yoshio Aso
  • Publication number: 20080146632
    Abstract: The present invention provides compounds capable of binding to an Fc receptor and modulating Fc receptor activity comprising a core lipophilic group in the form of an Aryl zing substituted with a group rich in p-electrons. The invention further provides for a method of treating an autoimmune disease involving Fc receptor activity using such compounds. A method for obtaining a compound which modulates Fc receptor activity is also provided, the method comprising: (a) providing or designing compounds having structural characteristics to fit in the groove of the Fc?RIIa structure; and (b) screening the compounds for modulating activity on the Fc receptor.
    Type: Application
    Filed: February 1, 2008
    Publication date: June 19, 2008
    Applicant: TRILLIUM THERAPEUTICS, INC.
    Inventors: Mark Phillip Hogarth, Geoffrey Allan Pietersz, Gerard Peter Moloney
  • Patent number: 7332616
    Abstract: The present invention provides a polymer which has at least one or more of a repeating unit represented by a following general formula (1a), a repeating unit represented by a following general formula (2a) and a repeating unit represented by a following general formula (3b), and a repeating unit represented by a following general formula (1c), and a positive resist composition which contains as a base resin the polymer. Thereby, there can be provided a positive-resist composition having high sensitivity and high resolution in exposure with a high energy beam, wherein line edge roughness is small since swelling at the time of development is suppressed, and the residue after development is few.
    Type: Grant
    Filed: February 8, 2007
    Date of Patent: February 19, 2008
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Jun Hatakeyama, Yuji Harada, Yoshio Kawai
  • Patent number: 7019024
    Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: March 28, 2006
    Assignee: Allelix Neuroscience Inc.
    Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
  • Patent number: 6864254
    Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.
    Type: Grant
    Filed: November 1, 2000
    Date of Patent: March 8, 2005
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
  • Publication number: 20040043326
    Abstract: An optical information recording medium has a recording layer composed essentially of an oxonol compound of the following formula: 1
    Type: Application
    Filed: June 6, 2003
    Publication date: March 4, 2004
    Applicant: FUJI PHOTO FILM CO. , LTD.
    Inventors: Naoki Saito, Koji Wariishi, Michihiro Shibata
  • Patent number: 6514967
    Abstract: The invention relates to compounds of the following general formula (I): in which: R1 and R2 represent a hydrogen atom, or form a ring, especially a benzene ring, R3 represents a hydrogen atom or an alkyl group, especially a methyl group, X and Y, independently of one another, represent a carbon atom, or a heteroatom such as a sulphur atom S, or a group with the formula (a) in which R4 and R5 represent a hydrogen atom or a methyl group, or R4 and R5 form a heterocycle, and their use for the preparation of a drug intended for the treatment of pathologies associated with abnormally high concentrations of extracellular glutamate.
    Type: Grant
    Filed: December 16, 1999
    Date of Patent: February 4, 2003
    Assignee: Centre National de la Recherche Scientifique
    Inventors: Jean-Marc Kamenka, Isoline Caubere, Gerard Barbanel
  • Patent number: 6479514
    Abstract: Compounds of formula (I) in which the substituents and symbols have the meanings indicated in the description, are suitable for the control of Helicobacter bacteria.
    Type: Grant
    Filed: November 17, 2000
    Date of Patent: November 12, 2002
    Assignee: Altana Pharma AG
    Inventors: Peter Zimmerman, Gerhard Grundler
  • Patent number: 6391912
    Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups and G, V, W, X, Y and Z are each as defined in the description, to processes and intermediates for their preparation and to their use as pesticides and herbicides.
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: May 21, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hermann Hagemann, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Peter Dahmen, Markus Dollinger, Alan Graff, Wolfram Andersch
  • Patent number: 6302837
    Abstract: A compound selected from those of formula (I): wherein: X represents oxygen, sulphur, or NR3 wherein R3 is as defined in the description, Y represents oxygen, sulphur, NR3, or may represent single bond in certain cases, T represents nitrogen, carbon, or CH, A represents single bond, alkylene, arylene, cycloalkylene, heterocycloalkylene, heteroarylene, or —SO2—R4— wherein R4 is as defined in the description, W represents hydroxy, alkoxy, aryloxy, arylalkoxy, cycloalkyloxy, heterocycloalkyloxy or heteroaryloxy, or hydroxyamino, U1 represents hetero, or alkylene wherein one or more of carbon may optionally be replaced by one or more hetero atoms, V1 represents arylene, heteroarylene,or heterocycloalkylene, U2 represents single bond, hetero or alkylene wherein one or more carbon may optionally be replaced by one or more hetero atoms, V2 represents aryl, heteroaryl, or heterocycloalkyl, Ra, Rb, Rc, which may be identical or different, each independently of the others r
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: October 16, 2001
    Assignee: Adir et Compagnie
    Inventors: Guillaume De Nanteuil, Christine Lila, Tony Verbeuren, Alain Rupin
  • Patent number: 6288107
    Abstract: Novel sulfatase inhibitor/estrogen receptor blocker compounds useful in the treatment of estrogen dependent illnesses are disclosed. The compounds generally comprise a sulfamate moiety and an aromatic, estrogen receptor blocker moiety. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of an estrogen-dependent disease are also disclosed.
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: September 11, 2001
    Assignee: Duquesne University of the Holy Ghost
    Inventors: Pui-Kai Li, Kyle W. Selcer
  • Patent number: 6281240
    Abstract: This invention provides methods of treating secretory diarrhea or cystic fibrosis in a mammal which comprises administering to a mammal in need thereof an effective amount of diarylsulfonylurea. This invention also describes specific diarylsulfonylureas for use in treating secretory diarrhea or cystic fibrosis.
    Type: Grant
    Filed: January 31, 2000
    Date of Patent: August 28, 2001
    Assignee: Eli Lilly and Company
    Inventor: Bruce D Schultz
  • Patent number: 6169087
    Abstract: The present invention provides novel compounds of Formula 1 or Formula 2 and compositions thereof, methods of their use, and methods of their manufacture, wherein X, Y, Z, W, R1, R2 and R3 are defined more fully in the description. These compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, and a number of other diseases.
    Type: Grant
    Filed: September 21, 1998
    Date of Patent: January 2, 2001
    Assignees: Novo Nordisk A/S, Ontogen
    Inventors: Henrik Sune Andersen, Sven Branner, Claus Bekker Jeppesen, Niels Peter Hundahl Moeller, Adnan M. M. Mjalli, Sepehr Sarshar
  • Patent number: 6100292
    Abstract: This invention relates to ketones represented by the following formula ##STR1## and to drugs in which such a ketone or pharmacologically acceptable salt thereof is an effective component.The ketones of the present invention encourage the production of platelets, red blood cells, white blood cells and the like, and can be used to prevent or treat cytopaenia brought about by cancer chemotherapy, radiotherapy, bone marrow transplantation and drug therapy, or by immunological abnormality or anaemia, and the like.
    Type: Grant
    Filed: May 25, 1999
    Date of Patent: August 8, 2000
    Assignee: Toray Industries, Inc.
    Inventors: Tsuyoshi Matsumoto, Hideki Kawai, Kiyoshi Okano, Katsuyuki Mori, Yasumoto Adachi
  • Patent number: 6048875
    Abstract: A compound of formula (I): ##STR1## wherein: X represents oxygen, sulphur, or NR.sub.3 wherein R.sub.3 is as defined in the description,Y represents oxygen, sulphur, NR.sub.3, or may a single bond when X represents NR.sub.3,Z represents nitrogen, carbon, or CH,A represents a single bond, alkylene (optionally substituted), arylene, cycloalkylene, heterocycle, or --SO.sub.2 --R.sub.4 -- wherein R.sub.4 is as defined in the description,W represents hydroxy, alkoxy, aryloxy, arylalkoxy, cycloalkyloxy, heterocycle bonded to oxygen, amino, or hydroxyamino,Ra, Rb, Rc, Rd, which may be the same or different, each independently of the others are as defined in the description,R.sub.1 represents aryl substituted by one to five identical or different substituents, each independently of the others,R.sub.
    Type: Grant
    Filed: April 26, 1999
    Date of Patent: April 11, 2000
    Assignee: Adir et Compagnie
    Inventors: Guillaume De Manteuil, Christine Lila, Tony Verbeuren, Alain Rupin
  • Patent number: 6040309
    Abstract: Compounds of formula I, ##STR1## wherein X represents O or S(O).sub.m ;R.sup.1 and R.sup.2 independently represent phenyl, naphthyl or heteroaryl; each of which is optionally fused and optionally substituted;Y represents a bond, O, (CH.sub.2).sub.n, O(CH.sub.2).sub.n, (CH.sub.2).sub.n O, or CH(C.sub.1-6 alkyl)O;R.sup.3 represents H or C.sub.1-6 alkyl;m represents 0, 1, or 2; andn represents 1, or 2;and pharmaceutically acceptable salts thereof, are useful in therapy, in particular in the treatment of restenosis, renal failure and pulmonary hypertension.
    Type: Grant
    Filed: December 3, 1998
    Date of Patent: March 21, 2000
    Assignee: Pfizer, Inc.
    Inventors: Kevin Neil Dack, Roger Peter Dickinson
  • Patent number: 5989451
    Abstract: This invention provides chiral thioindigo compounds for doping smectic liquid crystal hosts, wherein the compounds modulate a chiral bulk property of an induced chiral smectic liquid crystal phase upon irradiation at a wavelength in the visible range. Modulation of the chiral bulk property is effected by reversible trans-cis photoisomerization of the compound upon irradiation. The compounds maintain their rod-like shape in both isomeric forms, and hence do not destabilize the chiral smectic liquid crystal phase. Compounds according to the invention are useful in optical devices such as optical switches, displays, and memory.
    Type: Grant
    Filed: February 6, 1998
    Date of Patent: November 23, 1999
    Assignee: Queen's University at Kingston
    Inventors: Robert P. Lemieux, Liviu Dinescu
  • Patent number: 5986109
    Abstract: A compound of fomula XIV: ##STR1## wherein: R.sup.1a is --H or --OR.sup.7a in which R.sup.7a is a hydoxy protecting group;R.sup.2a is --H, halo, or OR.sup.8a in which R.sup.8a is a hydroxy protecting group; andR.sup.
    Type: Grant
    Filed: June 18, 1998
    Date of Patent: November 16, 1999
    Assignee: Eli Lilly and Company
    Inventors: Alan David Palkowitz, Kenneth Jeff Thrasher
  • Patent number: 5981765
    Abstract: The present invention provides a compound of formula ##STR1## wherein R.sup.1a is --H or --OR.sup.7a in which R.sup.7a is a hydroxy protecting group;R.sup.2a is --H, halo, or --OR.sup.8a in which R.sup.8a is a hydroxy protecting group;R.sup.6 is --H or a hydroxy protecting group which can be selectively removed;R.sup.11 is non-existent or .dbd.O; andZ is --O-- or --S--;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 18, 1998
    Date of Patent: November 9, 1999
    Assignee: Eli Lilly and Company
    Inventors: Alan David Palkowitz, Kenneth Jeff Thrasher
  • Patent number: 5977098
    Abstract: The invention provides a compound of formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations containing a compound of formula I, and methods of using a compound of formula I for the inhibition of bone loss or bone resorption and for treatment of cardiovascular-related pathological conditions.
    Type: Grant
    Filed: June 30, 1998
    Date of Patent: November 2, 1999
    Assignee: Eli Lilly and Company
    Inventor: Alan David Palkowitz
  • Patent number: 5977382
    Abstract: The instant invention provides novel benzo[b]thiophene compounds, intermediates, compositions, pharmaceutical formulations, and methods of use.
    Type: Grant
    Filed: June 30, 1998
    Date of Patent: November 2, 1999
    Assignee: Eli Lilly and Company
    Inventor: Alan David Palkowitz
  • Patent number: 5863936
    Abstract: Methods and compositions for treating cancer and other diseases in which inhibition of telomerase activity can ameliorate disease symptoms or prevent or treat the disease relate to compounds characterized by the following structure: ##STR1## and their pharmaceutically acceptable salts. Y is selected from the group consisting of oxygen, sulfur, sulfonyl, sulfinyl, and --NR.sub.7 --. R.sub.1 is --TR.sub.8, where T is --C(X.sub.1)-- or --SO.sub.2 --, and R.sub.8 is selected from the group consisting of --OR.sub.9, --NHNHSO.sub.2 R.sub.9, --NHNHC(X.sub.2)OR.sub.9, --NR.sub.9 R.sub.10, --NHNHC(X.sub.2)NR.sub.9 R.sub.10, --NHCR.sub.9 R.sub.10 C(X.sub.2)NR.sub.11 R.sub.12, --NHC(X.sub.2)NR.sub.9 R.sub.10, and the piperazinyl moiety shown below: ##STR2## where n is 0 or 1, and Q.sub.n, for n=1, is --SO.sub.2 --, --C(X.sub.2)-- or --C(X.sub.2)NR.sub.10 --. R.sub.2 -R.sub.
    Type: Grant
    Filed: October 27, 1995
    Date of Patent: January 26, 1999
    Assignee: Geron Corporation
    Inventors: Federico C.A. Gaeta, Adam A. Galan, Elaine C. Stracker
  • Patent number: 5843965
    Abstract: The instant invention provides novel benzo?b!thiophene compounds, intermediates, compositions, pharmaceutical formulations, and methods of use for the inhibition of bone loss or bone resorption and for treatment of cardiovascular-related pathological conditions.
    Type: Grant
    Filed: August 27, 1997
    Date of Patent: December 1, 1998
    Assignee: Eli Lilly and Company
    Inventor: Alan David Palkowitz
  • Patent number: 5789436
    Abstract: A compound represented by formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom, a lower alkyl group or an acyl group; R.sub.2 and R.sub.3, which may be the same or different, each represents a hydrogen atom, an optionally substituted alkyl group, or an optionally substituted alkenyl group; R.sub.4 represents a hydrogen atom, an optionally substituted alkyl group, or an optionally substituted alkenyl group, or R.sub.4 forms a double bond between the carbon atom to which R.sub.3 is bonded and the adjacent carbon atom to form a benzothiophene skeleton, or R.sub.3 and R.sub.4 are taken together to form a 5- to 8-membered spiro ring which may contain a hetero atom, e.g., oxygen, sulfur or nitrogen; and n represents an integer of 0 to 2, or a pharmaceutically acceptable salt thereof. The compound of formula (I) exhibits an inhibitory action on the oxidative modification of LDL and is useful as therapeutics of arteriosclerosis.
    Type: Grant
    Filed: October 9, 1996
    Date of Patent: August 4, 1998
    Assignee: Chugai Seiyak Kabushiki Kaisha
    Inventors: Yoshiaki Kato, Akira Ishikawa, Kunio Tamura
  • Patent number: 5780648
    Abstract: Benzothiophenes, and uses and formulations thereof, are provided by the present invention.
    Type: Grant
    Filed: June 25, 1997
    Date of Patent: July 14, 1998
    Assignee: Eli Lilly and Company
    Inventors: David Thompson Berg, George Joseph Cullinan, Brian William Grinnell, Mark Alan Richardson
  • Patent number: 5739296
    Abstract: Polarizing coatings are formed from dyestuffs which provide a stable liquid crystalline phase in a wide range of concentrations, temperatures and pH-values. Particles formed by aggregates of the liquid crystal molecules are oriented in a predetermined direction to polarize light. The stability of the liquid crystalline state allows orienting the particles by mechanical forces such as a shearing force applied when the liquid crystal (10) is spread on a support surface (20) by a knife-like doctor (90) or a tension deformation force acting on the meniscus of the liquid crystal deposited between two surfaces (20, 30) as the surfaces are peeled off one another. As a result, the polarizing coatings are formed in some embodiments by simple methods. In some embodiments, the polarizing coatings have a high lightfastness, a high thermal stability, and a high dichroic ratio.
    Type: Grant
    Filed: November 20, 1995
    Date of Patent: April 14, 1998
    Assignee: Russian Technology Group
    Inventors: Khan Ir Gvon, Yuri A. Bobrov, Victor A. Bykov, Leonid Y. Ignatov, Tatiana D. Ivanova, Sergei I. Popov, Elena Y. Shishkina, Georgiy N. Vorozhtsov
  • Patent number: 5719287
    Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of their use.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: February 17, 1998
    Assignee: Eli Lilly and Company
    Inventors: Stephen W. Kaldor, Marlys Hammond
  • Patent number: 5684033
    Abstract: This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: November 4, 1997
    Assignee: Eli Lilly and Company
    Inventors: Sung Y. Cho, Thomas A. Crowell, Bruce D. Gitter, Philip A. Hipskind, J. Jeffry Howbert, Joseph H. Krushinski, Jr., Karen L. Lobb, Brian S. Muehl, James A. Nixon
  • Patent number: 5663375
    Abstract: Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 7, 8, 9 or 10, and each R.sup.1 is halo, carboxy, trifluoromethyl, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, nitrogen-containing heterocyclyl, nitro, trifluoromethoxy, --COOR.sup.5 where R.sup.5 is an ester group, --COR.sup.6, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl;R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl;R.sup.3 is nitrile, carboxy, --COOR.sup.8 where R.sup.8 is an ester group, or --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl; andR.sup.4 is --NR.sup.11 R.sup.12, --NR.sup.11 COR.sup.
    Type: Grant
    Filed: August 22, 1994
    Date of Patent: September 2, 1997
    Assignees: Eli Lilly and Company, Lilly Industries Limited
    Inventors: Michael Brunavs, Colin Peter Dell, Peter Thaddeus Gallagher, William Martin Owton, Colin William Smith
  • Patent number: 5635527
    Abstract: A novel carboxylic acid compound having a condensed ring, which is represented by the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and pharmaceutical use thereof. The novel carboxylic acid compound having a condensed ring and pharmacologically acceptable salt thereof of the present invention have superior GPIIb/IIIa antagonism in mammals inclusive of human; can be administered orally; have long life in blood and low toxicity; and show less side-effects. Accordingly, they are extremely useful for the prophylaxis and treatment of thrombotic diseases and other diseases.
    Type: Grant
    Filed: February 6, 1996
    Date of Patent: June 3, 1997
    Assignee: The Green Cross Corporation
    Inventors: Shinichiro Ono, Tomohiro Yoshida, Atsuyuki Ashimori, Keigo Kosaka, Takehiro Okada, Kazuhiro Maeda, Masahiro Eda, Fumio Mori, Yoshihisa Inoue, Hajime Ebisu, Teruaki Imada, Ruriko Ikegawa, Feng Wang, Norifumi Nakamura
  • Patent number: 5608074
    Abstract: An improved process for the preparation of 3-chlorobenzo[b]thiophene-2-carbonyl chlorides is described where a cinnamic acid is converted in the presence of thionyl chloride and a 4-N,N'-disubstituted aminopyridine in one step to the desired product.
    Type: Grant
    Filed: December 19, 1994
    Date of Patent: March 4, 1997
    Assignee: Warner-Lambert Company
    Inventor: Jonathan Walker
  • Patent number: 5569772
    Abstract: The present invention is directed to a new process for the synthesis of 2-aryl benzo[b]thiophenes, and to novel intermediates therefor.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 29, 1996
    Assignee: Eli Lilly and Company
    Inventors: David W. Hoard, Wayne D. Luke
  • Patent number: 5532254
    Abstract: A method for modulating calcium channels, increasing the density of calcium channels in vascular and cardiac tissue with no changes in inotropic or pressor response, comprising administering to a warm-blooded animal in need thereof a pharmaceutically-effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.4 alkyl, --CO--(C.sub.1 -C.sub.6 alkyl), or --CH.sub.2 Ar, --CO--Ar, wherein Ar is phenyl or substituted phenyl;R.sup.2 is selected from the group consisting of pyrrolidine, hexamethylenemino, and piperidino; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 2, 1996
    Assignee: Eli Lilly and Company
    Inventor: Nancy L. Bowling
  • Patent number: 5498630
    Abstract: A method of controlling Take-All disease of plants by applying a fungicide of the formula ##STR1## wherein Z1 and Z2 are C and are part of an aromatic ring which is benzothiophene; andA is selected from --C(X)-amine wherein the amine is an unsubstituted, monosubstituted or disubstituted amino radical, --C(O)--SR.sub.3, --NH--C(X)R.sub.4, and --C(.dbd.NR.sub.3)--XR.sub.7 ;B is --W.sub.m --Q(R.sub.2).sub.3 or selected from O-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ;Q is C, Si, Ge, or Sn;W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W is selected from --C(R.sub.3).sub.p H(.sub.2-p), --N(R.sub.3).sub.m H(.sub.1-m)--, --S(O)p--, and --O--;X is 0 or S;n is 0, 1, 2, or 3;m is 0 or 1;p is 0, 1, or 2;each R and R.sub.2 is independently defined herein;R.sub.3 is C.sub.1 -C.sub.4 alkyl;R.sub.4 is C.sub.1 -C.sub.4 alkyl, haloalkyl, alkoxy, alkylthio, alkylamino, or dialkylamino; andR.sub.7 is C.sub.1 -C.sub.
    Type: Grant
    Filed: November 16, 1994
    Date of Patent: March 12, 1996
    Assignee: Monsanto Company
    Inventors: Dennis P. Phillion, Diane S. Braccolino, Matthew J. Graneto, Wendell G. Phillips, Karey A. Van Sant, Daniel M. Walker, Sai C. Wong
  • Patent number: 5407901
    Abstract: This patent application relates to Certain tricyclic ether herbicidal compounds and their use to control a broad spectrum of undesirable plant growth.
    Type: Grant
    Filed: November 16, 1993
    Date of Patent: April 18, 1995
    Assignee: E. I. Du Pont de Nemours
    Inventor: Eric de G. Taylor
  • Patent number: 5378699
    Abstract: Methods of treating an immune disease, cell proliferation, restenosis and vascular smooth muscle cells using the pharmaceutical compounds of the formula ##STR1## in which R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl; and salts thereof.
    Type: Grant
    Filed: February 5, 1993
    Date of Patent: January 3, 1995
    Assignees: Lilly Industries Limited, Eli Lilly and Company
    Inventors: Michael Brunavs, Colin P. Dell, Peter T. Gallagher, William M. Owton, Jai P. Singh, Colin W. Smith
  • Patent number: 5356926
    Abstract: 3-Alkyloxy-, aryloxy-, or arylalkyloxybenzo[b]-thiophene-2-carboxamides are described as agents which block leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases. Certain of these compounds are novel and methods of preparation are also described.
    Type: Grant
    Filed: February 9, 1993
    Date of Patent: October 18, 1994
    Assignee: Warner-Lambert Company
    Inventors: Diane H. Boschelli, David T. Connor, Clifford D. Wright
  • Patent number: 5338735
    Abstract: Compounds of the formula: ##STR1## in which each R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl, R.sup.3 and R.sup.4 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or C.sub.6-9 cycloalkyl optionally substituted by 1 to 4 C.sub.1-4 alkyl groups, R.sup.5 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C.sub.6-10 cycloalkyl optionally substituted with 1 to 4 C.sub.1-4 alkyl groups or a phenyl group, or C.sub.4-9 heterosubstituted cycloalkyl optionally substituted with 1 to 4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.The compounds are indicated for use in the treatment of disorders of the central nervous system.
    Type: Grant
    Filed: August 12, 1993
    Date of Patent: August 16, 1994
    Assignee: Lilly Industries Limited
    Inventors: John Fairhurst, David E. Tupper
  • Patent number: 5304657
    Abstract: A hydrazine compound of the formula (I) or its salt: ##STR1## wherein A is a benzofuranyl group which may be substituted, a quinolinyl group which may be substituted, a benzothienyl group which may be substituted, a benzothiazolyl group which may be substituted, a thienothienyl group which may be substituted, a dihydrothienothienyl group which may be substituted, a dihydrocyclopentathienyl group which may substituted, a tetrahydrobenzothienyl group which may be substituted, an indanyl group which may be substituted, or a hexahydroindanyl group which may be substituted, W is a hydrogen atom, a cyano group, --COCOOR', --S--N(R")COOR' or --CH.sub.
    Type: Grant
    Filed: October 10, 1991
    Date of Patent: April 19, 1994
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Tadaaki Toki, Toru Koyanagi, Kiyomitsu Yoshida, Kazuhiro Yamamoto, Masayuki Morita
  • Patent number: 5288749
    Abstract: The present invention provides tertiary and secondary amine compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof which are antagonists for alpha-2 adrenoreceptors and which inhibit serotonin (5-hydroxytryptamine, 5-HT) uptake.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: February 22, 1994
    Assignee: Abbott Laboratories
    Inventors: Michael D. Meyer, John F. DeBernardis, Rajnandan Prasad, Kevin B. Sippy, Karin R. Tietje
  • Patent number: 5280032
    Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.
    Type: Grant
    Filed: September 8, 1992
    Date of Patent: January 18, 1994
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
  • Patent number: RE36562
    Abstract: A method of controlling Take-All disease of plants by applying a fungicide of the formula ##STR1## wherein Z.sub.1 and Z.sub.2 are C and are part of an aromatic ring which is .[.benzothiophene.]..Iadd.thiophene.Iaddend.; andA is .[.selected from.]. --C(X)-amine .[.wherein the amine is an unsubstituted, monosubstituted or disubstituted amino radical.]..Iadd.wherein the amine is a monosubstituted or a disubstituted amine, wherein one of the substituents has a cyclic moiety, said cyclic moiety which is chosen from the group consisting of thienyl, furanyl, and a non-heterocyclic substituent, wherein when the amine is disubstituted, the second substituent is a non-cyclic substituent.Iaddend., --C(O)--SR.sub.3, --NH--C(X)R.sub.4, .[.and.]. .Iadd.or .Iaddend.--C(.dbd.NR.sub.3)--XR.sub.7 ;B is --W.sub.m --Q(R.sub.2).sub.3 or selected from .[.O-tolyl.]..Iadd.o-tolyl.Iaddend., 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ;Q is C, Si, Ge, or Sn;W is --C(R.sub.3).sub.p H.
    Type: Grant
    Filed: March 11, 1998
    Date of Patent: February 8, 2000
    Assignee: Monsanto Company
    Inventors: Dennis P. Phillion, Diane S. Braccolino, Matthew J. Graneto, Wendell G. Phillips, Karey A. Van Sant, Daniel M. Walker, Sai C. Wong