The Additional Hetero Ring Is Six-membered Patents (Class 544/149)
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Publication number: 20140336378
    Abstract: Disclosed are a novel benzamide derivative and pharmaceutical use thereof, and more particularly, a novel benzamide derivative having a structure of Formula 1 or pharmaceutically acceptable salts thereof, and a composition for prevention or treatment of pain or itching including the above material. The novel benzamide derivative and pharmaceutically acceptable salt thereof according to the present invention exhibit excellent pain-suppressive effect and, in particular, pain-suppressive effect in not only a neuropathic animal model but also other models such as a formalin model, and therefore, may be used in suppression of different pains such as nociceptive pain, chronic pain, etc.
    Type: Application
    Filed: November 29, 2012
    Publication date: November 13, 2014
    Inventor: Doo Hyun Lee
  • Patent number: 8828678
    Abstract: A compound comprising the structure: (SIG)-(SI-MOD)m. is provided in which SIG is a signaling molecule, SI is a self-immolative structure bound to SIG such that SIG has a reduced signal relative to the signal of SIG without SI, MOD is a moiety bound to SI that is subject to modification by an activator, and m is an integer from 1 to about 10. When MOD is modified by an activator, SI is destabilized and self-cleaved from SIG such that SIG generates an increased signal. Also provided are methods of determining whether a sample comprises an activator such as a nitroreductase, and methods of determining whether a mammalian cell is hypoxic using a compound of the formula (SIG)-(SI-MOD)m.
    Type: Grant
    Filed: November 16, 2010
    Date of Patent: September 9, 2014
    Assignee: Enzo Life Sciences, Inc.
    Inventors: Maciej Szczepanik, Irina V. Lebedeva, Yuejun Xiang, Praveen Pande, Wayne Forrest Patton
  • Publication number: 20140005181
    Abstract: The present disclosure relates to compounds and methods for treating a disease mediated by apelin.
    Type: Application
    Filed: June 20, 2013
    Publication date: January 2, 2014
    Applicant: Sanford-Burnham Medical Research Institute
    Inventors: Layton Smith, Anthony B. Pinkerton
  • Publication number: 20130281366
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as Hyperlipidemia and also have a beneficial effect on cholesterol.
    Type: Application
    Filed: December 26, 2011
    Publication date: October 24, 2013
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pankaj, Sairam Kalapatapu, V.V.M., Mukul R. JAIN
  • Publication number: 20120329775
    Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: June 4, 2012
    Publication date: December 27, 2012
    Inventors: Rhonan Ford, Andrew Mather, Antonio Mete, Ian Millichip
  • Patent number: 8178593
    Abstract: The invention provides B-sides of urethane formulations, wherein the B-sides comprise both alcohol and epoxy moieties. Also provided are urethane formulations comprising the B-side of the invention, as well as A-sides comprising isocyanate molecules.
    Type: Grant
    Filed: February 26, 2010
    Date of Patent: May 15, 2012
    Assignee: The Curators of the University of Missouri
    Inventors: Galen Suppes, Fu-Hung Hsieh, Yuan-Chan Tu, Pimphan Kiatsimkul
  • Publication number: 20110201584
    Abstract: Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Application
    Filed: January 14, 2011
    Publication date: August 18, 2011
    Inventor: Xiangping Qian
  • Publication number: 20100286118
    Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: May 6, 2010
    Publication date: November 11, 2010
    Inventors: Rhonan Ford, Andrew Mather, Antonio Mete, Ian Millichip
  • Patent number: 7655808
    Abstract: Leptomycin-type compounds according to formula I wherein R0, R1, R2, R10, R11, R12, R13, R14, and m are as defined herein, exhibit anti-tumor activity.
    Type: Grant
    Filed: September 30, 2008
    Date of Patent: February 2, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Steven D. Dong, Daniel V. Santi, David C. Myles, Brian Hearn
  • Patent number: 7572793
    Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1: wherein R1 represents a C1-C12 alkyl group which may be substituted; R represents, for example, a group represented by the following formula (II): wherein R2 and R3 independently represent a hydrogen atom or a C1-C8 alkyl group; R4 represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.
    Type: Grant
    Filed: September 20, 2002
    Date of Patent: August 11, 2009
    Assignees: Mitsubishi Tanabe Pharma Corporation, Sanofi-Aventis
    Inventors: Fumiaki Uehara, Keiichi Aritomo, Aya Shoda, Shinsuke Hiki, Masahiro Okuyama, Yoshihiro Usui, Mitsuru Ooizumi, Kazutoshi Watanabe
  • Publication number: 20090186884
    Abstract: Described are diaminopropanols of which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of renin activity or in the treatment of aspartic protease mediated disorders. Also described is a method for the use of the diaminopropanols in ameliorating or treating renin related disorders in a subject in need thereof.
    Type: Application
    Filed: April 5, 2007
    Publication date: July 23, 2009
    Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty
  • Patent number: 7556751
    Abstract: Photochromic materials comprising indeno-fused naphthopyrans having a first electron-withdrawing substituent and, in certain non-limiting embodiments, a second electron-withdrawing substituent are disclosed. The photochromic materials according to the various embodiments may display faster fade rates, bathochromic shift, and higher performance ratings compared to comparable indeno-fused naphthopyrans without the electron-withdrawing substituents. Photochromic compositions and articles, such as optical elements, incorporating the photochromic materials are also disclosed.
    Type: Grant
    Filed: December 21, 2005
    Date of Patent: July 7, 2009
    Assignee: Transitions Optical, Inc.
    Inventors: Anu Chopra, Beon-Kyu Kim, Barry Van Gemert
  • Patent number: 7527754
    Abstract: Photochromic materials comprising indeno-fused naphthopyrans having substituents comprising a 4-fluorophenyl group and a 4-aminophenyl group bonded to the 3-position of the indeno-fused naphthopyran are disclosed. The photochromic materials may exhibit faster fade rates as compared to similar indeno-fused naphthopyrans without a 4-fluorophenyl group and a 4-aminophenyl group bonded to the 3-position of the indeno-fused naphthopyran. Substituted 2-propyn-1-ols utilized for the synthesis of the indeno-fused naphthopyrans disclosed herein are disclosed. Photochromic compositions and articles, such as optical elements, incorporating the photochromic materials disclosed herein are also disclosed.
    Type: Grant
    Filed: December 21, 2005
    Date of Patent: May 5, 2009
    Assignee: Transitions Optical, Inc.
    Inventor: Anu Chopra
  • Publication number: 20090062533
    Abstract: Described are naphthols useful in the manufacture of novel indeno-fused photochromic naphthopyran materials.
    Type: Application
    Filed: November 11, 2008
    Publication date: March 5, 2009
    Applicant: TRANSITIONS OPTICAL, INC.
    Inventors: Robert W. Walters, Anil Kumar, Clara E. Nelson, Anu Chopra
  • Patent number: 7481955
    Abstract: Various non-limiting embodiments of the present invention relate to photochromic materials having a metallocenyl group. More particularly, various non-limiting embodiments disclosed herein provide photochromic materials including an indeno-fused naphthopyran, such as an indeno[2?,3?:3,4]naphtho[1,2-b]pyran, and a metallocenyl group bonded to at least one available position on the indeno-fused naphthopyran. Other non-limiting embodiments disclosed herein provide photochromic composition and photochromic articles, such as but not limited to ophthalmic lens, which include the disclosed photochromic materials and method of making the same.
    Type: Grant
    Filed: May 31, 2006
    Date of Patent: January 27, 2009
    Assignee: Transitions Optical, Inc.
    Inventor: Wenjing Xiao
  • Patent number: 7446196
    Abstract: Leptomycin-type compounds according to Formula I wherein R0, R1, R2, R10, R11, R12, R13, R14, and m are as defined herein, exhibit anti-tumor activity.
    Type: Grant
    Filed: June 1, 2005
    Date of Patent: November 4, 2008
    Assignee: Kosan Biosciences, Incorporated
    Inventors: Steven Dong, Daniel V. Santi, David C. Myles, Brian Hearn
  • Publication number: 20080234258
    Abstract: A compound of formula (1) wherein X is H or —OCR1 and Y is H or —OCR2, provided that X and Y are not both H; and R is CH2OR9, CONR11R12, CN, tetrazole or COOR17; or a salt thereof, has therapeutic utility.
    Type: Application
    Filed: August 10, 2006
    Publication date: September 25, 2008
    Inventors: Andrew Douglas Baxter, Andrea Walmsley
  • Patent number: 7423037
    Abstract: Compounds of the general formula (I) are inhibitors of the reuptake of norepinephrine. As such, they may be useful for the treatment of disorders of the central and/or peripheral nervous system.
    Type: Grant
    Filed: October 28, 2004
    Date of Patent: September 9, 2008
    Assignee: Eli Lilly and Company
    Inventors: Gordon Iain Campbell, Manuel Javier Cases-Thomas, Teresa Man, John Joseph Masters, Hélène Catherine Eugénie Rudyk, Magnus Wilhelm Walter
  • Patent number: 7312211
    Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and other diseases.
    Type: Grant
    Filed: August 26, 2004
    Date of Patent: December 25, 2007
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, Yancey David Ward
  • Publication number: 20070278461
    Abstract: Various non-limiting embodiments of the present invention relate to photochromic materials which include a haloalkyl group. More particularly, various non-limiting embodiments disclosed herein provide photochromic materials including an indeno-fused naphthopyran, such as, an indeno[2?,3?:3,4]naphtho[1,2-b] pyran, and a haloalkyl group bonded at the 13-position thereof, wherein the haloalkyl group is a perhalogenated group or a group represented by —O(CH2)a(CX2)bCT3, wherein T is a halogen, each X is independently hydrogen or halogen, a is an integer ranging from 1 to 10, and b is an integer ranging from 1 to 10. Other non-limiting embodiments disclosed herein provide photochromic composition and photochromic articles, such as, but not limited to ophthalmic lens, which include the disclosed photochromic materials and methods of making the same.
    Type: Application
    Filed: April 2, 2007
    Publication date: December 6, 2007
    Applicant: TRANSITIONS OPTICAL, INC.
    Inventors: Olga G. Petrovskaia, Anu Chopra, Patrick M. Brown
  • Patent number: 7189714
    Abstract: Compounds useful for the treatment of pain in accord with the following structural diagram, wherein R1, R2 and R3 are any of a number of groups as defined in the specification and pharmaceutical compositions and methods of treatment utilising such compounds.
    Type: Grant
    Filed: October 31, 2001
    Date of Patent: March 13, 2007
    Assignee: Astrazeneca AB
    Inventors: Marc Chapdelaine, Lucius Kemp, John McCauley
  • Patent number: 7053212
    Abstract: The present invention provides estrogen receptor (ER) ligands of structural formula (I) the pharmaceutically acceptable salts, stereoisomers, and prodrugs thereof, and the pharmaceutically acceptable salts of the prodrugs, wherein R1, R2, R3, R4, R5, X, and Q are as defined herein. The invention further provides pharmaceutical compositions comprising the compounds of formula (I), and methods for treating or preventing diseases, disorders, conditions, or symptoms mediated by an ER which comprise administering to a mammalian subject in need of treatment therewith, an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt, stereoisomer, or prodrug thereof, or a pharmaceutically acceptable salt of the prodrug, or a pharmaceutical composition comprising a compound of formula (I), or a pharmaceutically acceptable salt, stereoisomer, or prodrug thereof, or a pharmaceutically acceptable salt of the prodrug.
    Type: Grant
    Filed: September 17, 2003
    Date of Patent: May 30, 2006
    Assignee: Pfizer Inc.
    Inventors: Kimberly O. Cameron, Richard Chesworth
  • Patent number: 7026352
    Abstract: The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution of Streptomyces sp. Mer.
    Type: Grant
    Filed: February 1, 2002
    Date of Patent: April 11, 2006
    Assignees: Mercian Corporation, Eisai Co., Ltd.
    Inventors: Yoshiharu Mizui, Takashi Sakai, Satoshi Yamamoto, Keisuke Komeda, Masanori Fujita, Akifumi Okuda, Kumiko Kishi, Jun Niijima, Mitsuo Nagai, Kiyoshi Okamoto, Masao Iwata, Yoshihiko Kotake, Toshimitsu Uenaka, Naoki Asai, Motoko Matsufuji, Tomohiro Sameshima, Naoto Kawamura, Kazuyuki Dobashi, Takashi Nakashima, Masashi Yoshida, Toshio Tsuchida, Susumu Takeda, Tomonari Yamada, Koji Norihisa, Takao Yamori
  • Patent number: 6927217
    Abstract: The present invention relates to novel dihydropyrones of Formula I wherein X is NH or NR8, which inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS.
    Type: Grant
    Filed: October 16, 2002
    Date of Patent: August 9, 2005
    Assignee: Warner-Lambert Company
    Inventors: Frederick Earl Boyer, Jr., John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Elizabeth Ann Lunney, Alexander Pavlovsky, Vara Prasad Venkata Nagendra Josyula, Bradley Dean Tait
  • Patent number: 6833367
    Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B and C are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.
    Type: Grant
    Filed: November 12, 2002
    Date of Patent: December 21, 2004
    Assignee: Novartis AC
    Inventors: Frederick R. Kinder, Jr., Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
  • Publication number: 20040254184
    Abstract: The present invention relates compounds of the formula (I); wherein R1, R2, R3, R4, R5, R6, R7, R8, and R10 represent a variety of substituents; A represents NR9 or O; B represents a bond, CH2, NR9 or O, wherein one or both hydrogen atoms in said CH2 moiety may be replaced with one or both of R7 and R8, or alternatively, one of the hydrogen atoms in said CH2 moiety together with a hydrogen atom from an adjacent carbon are replaced by a double bond; with the proviso that when A is O, then B is NR9; n is zero, 1 or 2; and pharmaceutically acceptable salts thereof. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.
    Type: Application
    Filed: March 4, 2004
    Publication date: December 16, 2004
    Inventors: Jose Luis Castro Pineiro, Duncan Shaw, Brian Williams
  • Patent number: 6756372
    Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.
    Type: Grant
    Filed: November 2, 2001
    Date of Patent: June 29, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Michel Jose Emmanuel, Weimin Liu, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey David Ward
  • Patent number: 6743788
    Abstract: Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or conditions such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
    Type: Grant
    Filed: May 17, 2002
    Date of Patent: June 1, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier Francesco Cirillo, Victor Kamhi, John Robinson Regan, Michele Tsang
  • Publication number: 20040053921
    Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.
    Type: Application
    Filed: October 24, 2002
    Publication date: March 18, 2004
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, Yancey David Ward
  • Publication number: 20040006227
    Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 4-pyrone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
    Type: Application
    Filed: January 31, 2003
    Publication date: January 8, 2004
    Inventors: Michael S. South, Chun C Ma, Kevin J Koeller, Hayat K Rahman, William L Neumann
  • Publication number: 20040002492
    Abstract: The application concerns a compound of formula I: 1
    Type: Application
    Filed: February 24, 2003
    Publication date: January 1, 2004
    Applicant: Kudos Pharmaceuticals Ltd
    Inventors: Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Stephen Philip Jackson, Mark James O'Connor, Alan Yin Kai Lau, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Laurent Jean Martin Rigoreau, Marc Geoffery Hummersone, Roger John Griffin
  • Publication number: 20030186976
    Abstract: There is provided benzofuryl-&agr;-pyrone derivative represented by the following structural formula (I): 1
    Type: Application
    Filed: May 12, 2003
    Publication date: October 2, 2003
    Applicant: TEIJIN LIMITED, MICROBIAL CHEMISTRY RESEARCH FOUNDATION
    Inventors: Yoshimitsu Naniwa, Hiroshi Imai, Tomohide Ida, Emiko Muratani, Kazuo Kitai, Yoshinori Sugimoto, Tomomi Kosugi, Akiko Takeuchi, Kunihito Watanabe, Takami Tomiyama, Tomio Takeuchi, Masa Hamada
  • Publication number: 20030186962
    Abstract: of the formula (IV): 1
    Type: Application
    Filed: November 16, 2001
    Publication date: October 2, 2003
    Inventors: Martin Quibell, Steven Taylor, Urszula Grabowska, Magnus Nilsson, Veronique Morrison
  • Patent number: 6586428
    Abstract: The present invention relates to combined preparations comprising a morpholinyl anthracycline administered in combination anticancer agents chosen from an alkylating agent, an antimetabolite, a topoisomerase II inihbitor, a topoisomerase I inhibitor, an antimitotic drug and a platinum derivative, which are useful anticancer therapy, particularly in the treatment of a primary or metastatic liver cancer.
    Type: Grant
    Filed: October 31, 2002
    Date of Patent: July 1, 2003
    Assignee: Pharmacia Italia, S.p.A.
    Inventors: Maria Cristina Geroni, Marina Ripamonti, Michele Caruso, Antonino Suarato
  • Patent number: 6537990
    Abstract: The present invention relates to combined preparations comprising a morpholinyl anthracycline administered in combination anticancer agents chosen from an alkylating agent, an antimetabolite, a topoisomerase II inhibitor, a topoisomerase I inhibitor, an antimitotic drug and a platinum derivative, which are useful anticancer therapy, particularly in the treatment of a primary or metastatic liver cancer.
    Type: Grant
    Filed: October 25, 2001
    Date of Patent: March 25, 2003
    Assignee: Pharmacia Italia S.p.A.
    Inventors: Maria Cristina Geroni, Marina Ripamonti, Michele Caruso, Antonino Suarato
  • Patent number: 6458830
    Abstract: The present invention relates to compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n are defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis and postherpetic neuralgia.
    Type: Grant
    Filed: September 10, 2001
    Date of Patent: October 1, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Simon Neil Owen, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • Patent number: 6316505
    Abstract: Block copolymers containing a fluorinated hydrocarbon unit, a hydrocarbon unit, and a poly(oxyethylene) unit are useful in fluid formulations of pharmaceutical agents. A typical embodiment is: C11H23—CONHC2H4NHCO—C8F16—CONHC2H4NHCOO—(C2H4O)34—H.
    Type: Grant
    Filed: August 5, 1999
    Date of Patent: November 13, 2001
    Assignee: Supratek Pharma, Inc.
    Inventors: Alexander V. Kabanov, Serguei V. Vinogradov
  • Patent number: 6265446
    Abstract: Hydrazine derivatives of the formula wherein R1 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R2 represents heterocyclyl or NR5R6, R3 represents hydrogen, lower alkyl, halo-lower alkyl, cyano-lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, lower alkoxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, heterocyclyl-lower alkyl, heterocyclylcarbonyl-lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl, heteroaryl or aryl-lower alkyl, R4 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a grouping of the formula -Z-aryl, -Z-heterocyclyl or —(CH2)n—, CH═CR7R8, R5 and R6 each independently represent hydrogen or lower alkyl, R7 and R8 each independently represent hydrogen or lower alkyl or R7 and R8 together represent lower alkylene in which one CH2 group is optionally replaced by a hetero atom, X and Z each repres
    Type: Grant
    Filed: November 22, 1999
    Date of Patent: July 24, 2001
    Assignee: Hoffmann-La Roche Inc..
    Inventors: Michael John Broadhurst, William Henry Johnson, Daryl Simon Walter
  • Patent number: 6117870
    Abstract: A cyclic amide derivative of formula (I): ##STR1## wherein R.sup.1 represents a substituted alkyl group, a substituted alkenyl group, a substituted amino group, a substituted alkoxyl group, a substituted alkylthio group, a substituted carbamoyl group, a substituted sulfonamide group or a substituted amide group; the ring A represents a saturated cyclic alkyl group with 5 to 7 carbon atoms or a hetero-atom-containing saturated heterocyclic group with 3 to 6 carbon atoms; R.sup.2 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aromatic hydrocarbon group or a substituted or unsubstituted heterocyclic group; R.sup.3 represents a hydrogen atom, a group represented by the general formula R.sup.4 O-- or a group represented by the general formula R.sup.5 (R.sup.6)N-- wherein R.sup.
    Type: Grant
    Filed: November 10, 1999
    Date of Patent: September 12, 2000
    Assignee: Fujirebio Kabushiki Kaisha
    Inventors: Akihiko Hosoda, Nobuo Kobayashi, Naoko Tanabe, Tsuneo Koji, Masahiro Shibata, Akihiro Sekine, Masaharu Dozen
  • Patent number: 6113812
    Abstract: A photochromic article that includes a host material and a photochromic amount of a benzopyran compound, the benzopyran compound represented by one of the formulas: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are selected from hydrogen, a stable organic radical, a heterocyclic group, halogen, a nitrogen-substituted group, and a nitrogen-substituted ring compound.
    Type: Grant
    Filed: August 4, 1997
    Date of Patent: September 5, 2000
    Assignee: Vision-Ease Lens, Inc.
    Inventor: Frank J. Hughes
  • Patent number: 6087359
    Abstract: A thioaryl sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated thioaryl sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: September 10, 1999
    Date of Patent: July 11, 2000
    Inventors: Daniel P. Getman, Daniel P. Becker, Thomas E. Barta, Clara I. Villamil, Susan L. Hockerman, Louis J. Bedell, Hui Li, John N. Freskos, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo
  • Patent number: 6005103
    Abstract: The present invention relates to novel tri- and tetrasubstituted pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The pyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized pyrones and of related structures.
    Type: Grant
    Filed: October 12, 1994
    Date of Patent: December 21, 1999
    Assignee: Warner-Lambert Company
    Inventors: John Michael Domagala, Elizabeth Lunney, Kimberly Suzanne Para, Josyula Venkata Nagendra Vara Prasad, Bradley Dean Tait
  • Patent number: 5969140
    Abstract: Naphthalene derivatives of the formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are each H, protected or unprotected OH, one of R.sup.3 and R.sup.4 is protected or unprotected hydroxymethyl, and the other is H, lower alkyl, or protected or unprotected hydroxymethyl, R.sup.5 and R.sup.6 are the same or different and are each H, substituted or unsubstituted lower alkyl, substituted or unsubstituted phenyl or protected or unprotected NH.sub.2, or both combine together with the adjacent N to form substituted or unsubstituted heterocyclic group, and pharmaceutically acceptable salts thereof, these compounds showing excellent bronchoconstriction inhibitory activity, and hence, being useful in the prophylaxis or treatment of asthma.
    Type: Grant
    Filed: July 2, 1998
    Date of Patent: October 19, 1999
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Tatsuzo Ukita, Katsuo Ikezawa, Shinsuke Yamagata
  • Patent number: 5914351
    Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.
    Type: Grant
    Filed: December 12, 1997
    Date of Patent: June 22, 1999
    Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.
    Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
  • Patent number: 5869662
    Abstract: Benzopyran compounds represented by the formulas: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are selected from hydrogen, a stable organic radical, a heterocyclic group, halogen, a nitrogen-substituted group, and a nitrogen-substituted ring compound.
    Type: Grant
    Filed: July 17, 1997
    Date of Patent: February 9, 1999
    Assignee: Vision-Ease Lens, Inc.
    Inventor: Frank J. Hughes
  • Patent number: 5808062
    Abstract: The present invention relates to novel tri- and tetrasubstituted pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The pyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized pyrones and of related structures.
    Type: Grant
    Filed: October 12, 1994
    Date of Patent: September 15, 1998
    Assignee: Warner-Lambert Company
    Inventors: John Michael Domagala, Edmund Lee Ellsworth, Elizabeth Lunney, Daniel Fred Ortwine, Kimberly Suzanne Para, Josyula Venkata Nagendra Vara Prasad, Tomi Sawyer, Bradley Dean Tait
  • Patent number: 5795981
    Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.
    Type: Grant
    Filed: December 16, 1996
    Date of Patent: August 18, 1998
    Assignee: Polaroid Corporation
    Inventors: John W. Lee, Donald A. McGowan, Mark R. Mischke, Socorro M. Ramos, Stephen J. Telfer
  • Patent number: 5789440
    Abstract: The present invention relates to novel 5,6-dihydropyrone derivatives and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The 5,6-dihydropyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized 5,6-dihydropyrones and of related structures.
    Type: Grant
    Filed: October 12, 1994
    Date of Patent: August 4, 1998
    Assignee: Warner-Lambert Company
    Inventors: Edmund Lee Ellsworth, Elizabeth Lunney, Bradley Dean Tait
  • Patent number: 5714484
    Abstract: Cysteine protease inhibitors which deactivate the protease by covalently bonding to the cysteine protease and releasing the enolate of a 1,3-dicarbonyl (or its enolic form). The cysteine protease inhibitors of the present invention accordingly comprise a first portion which targets a desired cysteine protease and positions the inhibitor near the thiolate anion portion of the active site of the protease, and a second portion which covalently bonds to the cysteine protease and irreversibly deactivates that protease by providing a carbonyl or carbonyl-equivalent which is attacked by the thiolate anion of the active site of the cysteine protease to sequentially cleave a .beta.-dicarbonyl enol ether leaving group.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: February 3, 1998
    Assignee: Prototek, Inc.
    Inventors: Mary P. Zimmerman, Robert E. Smith, Mark Becker