Plural Chalcogens Bonded Directly To Carbocyclic Rings Of The Tetracyclo Ring System (e.g., Pyridoanthraquinones, Etc.) Patents (Class 546/78)
  • Publication number: 20130296279
    Abstract: The invention in one embodiment is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof. The invention is also directed to a composition comprising the compound of formula I or a pharmaceutically acceptable salt, and methods of treating the indications listed herein.
    Type: Application
    Filed: May 10, 2013
    Publication date: November 7, 2013
    Inventor: Adam Morgan
  • Patent number: 8486959
    Abstract: A group of novel dibenzo[f,h]isoquinoline derivatives as shown in the specification. Also disclosed are methods of using the compounds for treating a disease associated with NO overproduction, cancer, or viral infection.
    Type: Grant
    Filed: January 14, 2011
    Date of Patent: July 16, 2013
    Assignee: National Health Research Institutes
    Inventors: Shiow-Ju Lee, Cheng-Wei Yang, Yue-Zhi Lee, Yu-Sheng Chao
  • Patent number: 8367654
    Abstract: The present invention is directed to a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.
    Type: Grant
    Filed: May 7, 2010
    Date of Patent: February 5, 2013
    Assignee: Tetraphase Pharmaceuticals, Inc.
    Inventors: Roger B. Clark, Minsheng He, Louis Plamondon, Xiao-Yi Xiao, Magnus P. Rönn
  • Publication number: 20120108569
    Abstract: The present invention is directed to a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.
    Type: Application
    Filed: May 7, 2010
    Publication date: May 3, 2012
    Inventors: Roger B. Clark, Minsheng He, Louis Plamondon, Xiao-Yi Xiao, Magnus P. Rönn
  • Publication number: 20110172261
    Abstract: A group of novel dibenzo[f,h]isoquinoline derivatives as shown in the specification. Also disclosed are methods of using the compounds for treating a disease associated with NO overproduction, cancer, or viral infection.
    Type: Application
    Filed: January 14, 2011
    Publication date: July 14, 2011
    Applicant: National Health Research Institutes
    Inventors: Shiow-Ju Lee, Cheng-Wei Yang, Yue-Zhi Lee, Yu-Sheng Chao
  • Patent number: 7968561
    Abstract: There is provided a compound having Formula I wherein G is a fluorocarbyl group, and wherein R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group.
    Type: Grant
    Filed: August 28, 2008
    Date of Patent: June 28, 2011
    Assignee: Sterix Limited
    Inventors: Barry Victor Lloyd Potter, Michael John Reed, Lok Wai Lawrence Woo, Atul Purohit, Paul Foster
  • Publication number: 20110009371
    Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.
    Type: Application
    Filed: May 12, 2010
    Publication date: January 13, 2011
    Inventors: Andrew G. Myers, Mark G. Charest, Christian D. Lerner, Jason D. Brubaker, Dionicio R. Siegel
  • Publication number: 20090182000
    Abstract: There is provided a compound having Formula I wherein G is a fluorocarbyl group, and wherein R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group.
    Type: Application
    Filed: August 28, 2008
    Publication date: July 16, 2009
    Inventors: Barry Victor Lloyd Potter, Michael John Reed, Lok Wai Lawrence Woo, Atul Purohit, Paul Foster
  • Publication number: 20080312266
    Abstract: There is provided a compound having Formula (I) wherein G is H or a substituent, and wherein R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group, capable of inhibiting steroid sulphatase.
    Type: Application
    Filed: September 14, 2007
    Publication date: December 18, 2008
    Inventors: Barry Victor Lloyd Potter, Michael John Reed, Lok Wai Lawrence Woo
  • Publication number: 20080305082
    Abstract: Disclosed are compounds having Formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, A, and B are as defined herein, for use in methods for treating, preventing or ameliorating hyperproliferative disorders, such as cancer and other diseases and conditions. The invention also relates to pharmaceutical compositions and formulations comprising a compound having Formula I, and in combination with one or more other active agents and/or treatments.
    Type: Application
    Filed: September 14, 2005
    Publication date: December 11, 2008
    Inventors: John G. Curd, Robert L. Capizzi, John F.W. Keana
  • Patent number: 6506765
    Abstract: Apomorphine derivative compounds; pharmaceutically active compositions of apomorphine derivative compounds; and the use of apomorphine derivative compounds in methods for treating sexual dysfunction or for enhancing apomorphine effectiveness for patients treated with apomorphine are disclosed. The apomorphine derivatives may be esters, ethers, amides, mixed anhydrides, hemiacetals, glucuronates, sulfates or phosphonates. A preferred apomorphine derivative is norapomorphine.
    Type: Grant
    Filed: March 29, 2001
    Date of Patent: January 14, 2003
    Assignee: TAP Pharmaceutical Products, Inc.
    Inventors: Pramod K. Gupta, Deborah Milkowski, Debra Sutkowski-Markmann
  • Patent number: 6365597
    Abstract: The invention related to 4-aza-17&bgr;-(cyclopropoxy)-androst-5&agr;-androstan-3-one, 4-aza-17&bgr;-(cyclopropylamino)-androst-4-en-3-one and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17-20 lyase, 5&agr;-reductase and C17&agr;-hydroxylase and to the use of these compounds in the treatment of androgen and estrogen mediated disorders, including benign prostatic hyperplasia, androgen mediated prostate cancer, estrogen mediated breast cancer and to DHT-mediated disorders such as acne. Disorders relating to the oversynthesis of cortisol, for example, Cushing's Syndrome, are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide.
    Type: Grant
    Filed: February 11, 1997
    Date of Patent: April 2, 2002
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: James R. Pribish, Cynthia A. Gates, Philip M. Weintraub
  • Patent number: 6352997
    Abstract: The present invention provides for a method of treating polycystic ovary syndrome in a subject in need of such treatment comprising the administration of a therapeutically effective amount of a compound of structural formula I: to the subject. The present invention further provides for a method for improving fertility and the response to in vitro fertilization (I.V.F.), comprising administration of therapeutically effective amount of compound of structural formula I to the subject. Further, the present invention provides for compositions useful in the methods of the present invention, as well as a method of manufacture of a medicament useful for treating polycystic ovary syndrome or for improving fertility or the response to in vitro fertilization (I.V.F.).
    Type: Grant
    Filed: May 3, 1999
    Date of Patent: March 5, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Joanne Waldstreicher, Georgianna S. Harris
  • Patent number: 6204273
    Abstract: Compounds of the Formula I are inhibitors of the 5&agr;-reductase 1 isozyme, and are useful alone, or in combination with a 5&agr;-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.
    Type: Grant
    Filed: January 29, 1999
    Date of Patent: March 20, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, William K. Hagmann, Thomas J. Lanza, Jr., Soumya P. Sahoo, Gary H. Rasmusson, Richard L. Tolman, Derek Von Langen
  • Patent number: 6180794
    Abstract: A method for preparing 1,2-dihydroquinolines that is more flexible than the Skraup reaction is provided. The method comprises treating an ortho-alkenyl aniline with a ketone in the presence of a Lewis acid. Novel intermediates and products of this method useful as steroid receptor modulators, as well as pharmaceutical compositions and methods of use thereof are also claimed.
    Type: Grant
    Filed: October 15, 1999
    Date of Patent: January 30, 2001
    Assignee: Ligand Pharmacueticals Incorparated
    Inventors: James P. Edwards, Todd K. Jones, Josef D. Riggenberg, Erick M. Carreira
  • Patent number: 6143887
    Abstract: The novel process of the present invention involves the stereoselective synthesis of certain 16.beta.-substituted 4-aza-5.alpha.-androstan-3-ones and the useful intermediates obtained therein.
    Type: Grant
    Filed: May 11, 1999
    Date of Patent: November 7, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Dominick F. Gratale, Richard L. Tolman, Soumya P. Sahoo
  • Patent number: 6127354
    Abstract: Novel peptide derivatives, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are disclosed. The peptides have the formula (I): ##STR1## wherein a, b, A, R.sup.1, L.sup.1, D, R.sup.3, R.sup.4, R.sup.2, L.sup.2, E and G are as defined in the specification. These peptides exhibit improved resistance to proteolytic degradation, and hence, improved bioavailability.
    Type: Grant
    Filed: March 17, 1999
    Date of Patent: October 3, 2000
    Assignee: Novo Nordisk A/S
    Inventors: Bernd Peschke, Michael Ankersen, Thomas Kruse Hansen, Henning Th.o slashed.gersen
  • Patent number: 6001846
    Abstract: A method for preparing 1,2-dihydroquinolines that is more flexible than the Skraup reaction is provided. The method comprises treating an ortho-alkenyl aniline with a ketone in the presence of a Lewis acid. Novel intermediates and products of this method useful as steroid receptor modulators, as well as pharmaceutical compositions and methods of use thereof are also claimed.
    Type: Grant
    Filed: February 17, 1998
    Date of Patent: December 14, 1999
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: James P. Edwards, Todd K. Jones, Josef D. Riggenberg, Erick M. Carreira
  • Patent number: 5935968
    Abstract: The present invention provides for a method of treating polycystic ovary syndrome in a subject in need of such treatment comprising the administration of a therapeutically effective amount of a compound of structural formula I: ##STR1## to the subject. The present invention further provides for a method for improving fertility and the response to in vitro fertilization (I.V.F.), comprising administration of therapeutically effective amount of compound of structural formula I to the subject. Further, the present invention provides for compositions useful in the methods of the present invention, as well as a method of manufacture of a medicament useful for treating polycystic ovary syndrome or for improving fertility or the response to in vitro fertilization (I.V.F.).
    Type: Grant
    Filed: March 12, 1998
    Date of Patent: August 10, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Joanne Waldstreicher, Georgianna S. Harris
  • Patent number: 5886005
    Abstract: Compounds of the formula ##STR1## are inhibitors of 5.alpha.-reductase and are useful alone or in combination with other active agents for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.
    Type: Grant
    Filed: May 6, 1997
    Date of Patent: March 23, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Susan D. Aster, Donald W. Graham
  • Patent number: 5854273
    Abstract: A compound of formula (I) ##STR1## in which: X and Y, which may be identical or different, represent hydrogen or halogen or alkyl, trihaloalkyl, alkoxy, hydroxyl, cyano, nitro, amino, alkylamino, or dialkylamino,Z represent a linear or branched C.sub.4 to C.sub.12 alkylene chain in which one or more --CH.sub.2 -- are optionally replaced by any one of the following atoms or groups: --NR--, --O--, --S--, --SO--, --SO.sub.2 --, or --CONH--,A forms, with two adjacent carbon atoms of the phenyl ring, a phenyl, naphthyl or tetrahydronaphthyl ring or a heterocycle, ##STR2## represents any one of the groups as defined in the description, its optical isomers and its addition salts with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful as anticancer agents.
    Type: Grant
    Filed: July 23, 1997
    Date of Patent: December 29, 1998
    Assignee: ADIR et Compagnie
    Inventors: Gilbert Lavielle, Patrick Hautefaye, Ghanem Atassi, Alain Pierre, Laurence Kraus-Berthier, Stephane Leonce
  • Patent number: 5739137
    Abstract: Compounds of formula (I) are inhibitors of the 5.alpha.-reductase 1 isozyme, and are useful alone, or in combination with a 5.alpha.-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.
    Type: Grant
    Filed: February 28, 1996
    Date of Patent: April 14, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, William K. Hagmann, Thomas J. Lanza, Jr., Soumya P. Sahoo, Gary H. Rasmusson, Richard L. Tolman, Derek Von Langen
  • Patent number: 5719158
    Abstract: Compounds of the Formula I ##STR1## are inhibitors of the 5.alpha.-reductase 1 isozyme, and are useful alone, or in combination with a 5.alpha.-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: February 17, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, William K. Hagmann, Thomas J. Lanza, Jr., Soumya P. Sahoo, Gary H. Rasmusson, Richard L. Tolman, Derek von Langen
  • Patent number: 5710275
    Abstract: Described are new 7.beta.-substituted 4-aza-5.alpha.-androstan-3-ones and related compounds as 5.alpha.-reductase inhibitors.
    Type: Grant
    Filed: April 3, 1995
    Date of Patent: January 20, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Raman K. Bakshi, Gary H. Rasmusson, Richard L. Tolman, Gool F. Patel, Georgianna S. Harris, Donald W. Graham, Bruce E. Witzel
  • Patent number: 5696266
    Abstract: The novel process of this invention involves the reduction of certain .DELTA.-5 steroidal alkenes to selectively produce either the 5.alpha. or 5.beta. reduction products. Particularly, this invention involves reduction of .DELTA.-5 steroidal alkenes using a rhodium based catalyst in the presence of hydrogen to selectively yield 5.alpha. steroids or alternatively reduction of .DELTA.-5 steroidal alkenes in an ionizing medium with a trialkylsilane to selectively yield 5.beta. steroids.
    Type: Grant
    Filed: July 28, 1995
    Date of Patent: December 9, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Guy R. Humphrey, Ross A. Miller
  • Patent number: 5693809
    Abstract: Described are new 16-substituted and 7,16-disubstituted 4-aza-5.alpha.-androstan-3-ones and related compounds as 5.alpha.-reductase inhibitors.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: December 2, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, William Hagmann, Gary H. Rasmusson, Richard L. Tolman, Ihor E. Kopka, Soumya P. Sahoo, Craig K. Esser, Nathan G. Steinberg, Donald W. Graham, Bruce E. Witzel
  • Patent number: 5693647
    Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: December 2, 1997
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Todd K. Jones, Lin Zhi, Christopher M. Tegley, David T. Winn, Lawrence G. Hamann, James P. Edwards, Sarah J. West
  • Patent number: 5688808
    Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: November 18, 1997
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Todd K. Jones, David T. Winn, Lin Zhi, Lawrence G. Hamann, Christopher M. Tegley, Charlotte L. F. Pooley
  • Patent number: 5610162
    Abstract: Compounds of Formula (I), ##STR1## wherein X is sulfur or oxygen are inhibitors of the 5.alpha.-reductase enzyme and isozymes thereof. The compounds are useful for the treatment of hyperandrogenic disease conditions and diseases of the skin and scalp.
    Type: Grant
    Filed: November 17, 1994
    Date of Patent: March 11, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Bruce E. Witzel, Gary H. Rasmusson, Richard L. Tolman, Shu Shu Yang
  • Patent number: 5597832
    Abstract: A tetracyclic compound of the formula: ##STR1## wherein A and the atoms to which it is attached and the optional double bond represent a mono- or di-heterocyclic ring selected from: ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X are specifically defined, which compounds are useful in the treatment of dopamine-related neurological, psychological and cardiovascular disorders as well as in the treatment of substance abuse and other addictive behavior disorders, cognitive impairment and attention deficit disorder.
    Type: Grant
    Filed: November 10, 1994
    Date of Patent: January 28, 1997
    Assignee: Abbott Laboratories
    Inventors: Michael R. Michaelides, Yufeng Hong
  • Patent number: 5578726
    Abstract: Described is a new process for producing 7.beta.-substituted-4-aza-5.alpha.-androstan-3-ones and related compounds which are 5.alpha.-reductase inhibitors, consisting of reducing the corresponding androsteneone with lithium and liquid ammonia, contacting the product with an isomerizing agent, oxidizing the product to a seco acid and reacting that seco acid with an amine to cyclize to form 4-aza-5.alpha.-androstan-3-ones.
    Type: Grant
    Filed: November 10, 1994
    Date of Patent: November 26, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Raman K. Bakshi, Gary H. Rasmusson
  • Patent number: 5536727
    Abstract: Compounds of Formula I ##STR1## wherein Z contains an ether or thioether moeity, are inhibitors of the 5.alpha.-reductase enzyme and isozymes thereof. The compounds are useful for the treatment of hyperandrogenic disease conditions and diseases of the skin and scalp.
    Type: Grant
    Filed: November 17, 1994
    Date of Patent: July 16, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Bruce E. Witzel, Richard L. Tolman, Gary H. Rasmusson, Raman K. Bakshi, Shu Shu Yang
  • Patent number: 5525608
    Abstract: Compounds of the formula ##STR1## are inhibitors of 5.alpha.-reductase and are useful alone or in combination with other active agents for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.
    Type: Grant
    Filed: April 20, 1994
    Date of Patent: June 11, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Alan D. Adams, Gary H. Rasmusson, Nathan G. Steinberg
  • Patent number: 5516779
    Abstract: Compounds of the formula ##STR1## are inhibitors of 5 .alpha.-reductase and are useful alone or in combination with other active agents for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.
    Type: Grant
    Filed: June 8, 1994
    Date of Patent: May 14, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Derek Von Langen, Donald W. Graham, Richard L. Tolman
  • Patent number: 5359071
    Abstract: Compounds of the formula ##STR1## or a pharmaceutically acceptable salt or ester thereof, wherein R.sup.1 is selected from the group consisting of hydrogen and C.sub.1-10 alkyl;R.sup.2 is selected from the group consisting of hydrogen and C.sub.1-10 alkyl;R.sup.3 is selected from the group consisting of C.sub.1-10 alkoxyl, C.sub.1-10 alkyl and cyano;R.sup.4 is selected from the group consisting of C.sub.1-10 alkenyloxyl, C.sub.1-10 alkoxyl, C.sub.1-10 alkyl, C.sub.1-10 alkylcarbamic, C.sub.1-10 alkylcarbonyloxyl, carbonyl, hydroxyl, and --NHR.sup.5, andR.sup.5 is selected from the group consisting of hydrogen and C.sub.1-10 alkylcarbonyl. Such compounds are useful as selective antagonists of testosterone 5.alpha.-reductase 1.
    Type: Grant
    Filed: March 12, 1993
    Date of Patent: October 25, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, Craig K. Esser, William Hagmann, Ihor E. Kopka
  • Patent number: 5294701
    Abstract: This invention provides novel anti-tumour compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or together form an alkyl-, alkoxy- or OH-substituted aromatic group, which optionally contains an N atom as a hetero-atom; R is --COCH.sub.3 or --C.tbd.C--R.sub.4 and R.sub.4 is H or trimethylsilyl; and R.sub.3 is H or --COCF.sub.3 ; and acid addition salts thereof; as well as compositions containing these compounds.
    Type: Grant
    Filed: May 6, 1992
    Date of Patent: March 15, 1994
    Assignee: Pharmachemie B.V.
    Inventors: Johan W. Scheeren, Joannes F. M. de Bie, Dirk de Vos
  • Patent number: 5276053
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: January 4, 1994
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5180736
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: January 19, 1993
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5116983
    Abstract: A process for dehydrogenating a compound of the formula ##STR1## which comprises reacting the compound with a silylating agent in the presence of a quinone to introduce a .DELTA..sup.1 double bond.
    Type: Grant
    Filed: May 8, 1990
    Date of Patent: May 26, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Apurba Bhattacharya, Alan W. Douglas, Edward J. Grabowski, Ulf H. Dolling
  • Patent number: 5071853
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: February 27, 1990
    Date of Patent: December 10, 1991
    Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
  • Patent number: 4914106
    Abstract: A compound represented by the following formula ##STR1## wherein A represents a hydrogen atom or a lower alkanoyl group, Z represents an oxygen atom or the group ##STR2## in which R represents a hydrogen atom or a lower alkyl group, and X represents a halogen atom, the compound being useful for controlling androgen-dependent diseases, particularly for preventing abortion or for contraception.
    Type: Grant
    Filed: August 4, 1988
    Date of Patent: April 3, 1990
    Assignee: Teikoku Hormone Mfg. Co., Ltd.
    Inventors: Kenyu Shibata, Nobuaki Yamakoshi, Naoyuki Koizumi, Shigehiro Takegawa, Eiichiro Shimazawa, Mamoru Mieda
  • Patent number: 4888336
    Abstract: Invented are 4-aza-5-alpha-8(14)-17 substituted-androsten-3-ones having an 8(14), 7(8), or 16(17) double bond, optionally also having a 1(2) double bond, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-alpha-reductase.
    Type: Grant
    Filed: July 28, 1987
    Date of Patent: December 19, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
  • Patent number: 4874803
    Abstract: The present invention comprises reaction products resulting from the reaction of hydrazido-substituted or certain amino-substituted polymer stabilizers and cyclic dianhydrides, as well as the use of such products. The polymer stabilizers of the invention are useful for protecting a large variety of synthetic polymeric organic materials from the degradative effects of heat, light and oxygen. Some of the modifiers are flame retardants and many are metal deactivators in addition to their primary activity.
    Type: Grant
    Filed: September 21, 1987
    Date of Patent: October 17, 1989
    Assignee: Pennwalt Corporation
    Inventors: Arthur L. Baron, Terry N. Myers, Jerome Wicher
  • Patent number: 4863918
    Abstract: Disclosed are novel enamine quaternary compounds of the formula ##STR1## wherein m=1, 2 or 3 and n=1, 2 or 3 with the proviso that m+n=3, 4 or 5; R.sup.1 and R.sup.2 are independently lower alkyl or hydrogen, and R.sup.3 and R.sup.4 are independently selected from the group consisting of lower alkyl, lower cycloalkyl lower alkyl, lower alkenyl, phenyl lower alkyl, thienyl lower alkyl, furyl lower alkyl, lower alkoxy lower alkyl, halogenated lower alkyl, lower alkyloyloxo or lower alkyloyloxy lower alkyl or wherein NR.sup.3 R.sup.4 together comprise a heterocycle ring; and wherein X.sup.- represents a pharmaceutically acceptable anion. Pharmaceutical compositions containing the same when administered to warm-blooded animals exhibit a muscle relaxant effect characterized by excellent onset and recovery times. Also disclosed are methods of making the enamine quaternary compounds.
    Type: Grant
    Filed: July 19, 1988
    Date of Patent: September 5, 1989
    Assignee: BOC, Inc.
    Inventors: Kanti J. Gala, Ross C. Terrell
  • Patent number: 4785103
    Abstract: A compound represented by the following formula ##STR1## wherein A represents a hydrogen atom or a lower alkanoyl group, Z represents an oxygen atom or the group ##STR2## in which R represents a hydrogen atom or a lower alkyl group, and X represents a halogen atom, the compound being useful for controlling androgen-dependent diseases, particularly for preventing prostatic hypertrophy.
    Type: Grant
    Filed: February 27, 1986
    Date of Patent: November 15, 1988
    Assignee: Teikoku Hormone Mfg. Co., Ltd.
    Inventors: Kenyu Shibata, Nobuaki Yamakoshi, Naoyuki Koizumi, Shigehiro Takegawa, Eiichiro Shimazawa, Mamoru Mieda
  • Patent number: 4739062
    Abstract: A new widely-applicable method has been found for synthesis of 9,10-anthraquinones and similar chemical compounds of wide use in industry and pharmacology, by reacting suitable aromatic substrates with activated dicarboxylic acids (more particularly dichlorides) in the presence of metal halides. The special characteristics of the reaction are the good yields, high selectivity, the possibility of operating in a single reactor and the use of starting compounds which are cheap and easily available on the market.
    Type: Grant
    Filed: June 27, 1986
    Date of Patent: April 19, 1988
    Assignee: Consiglio Nazionale Delle Ricerche
    Inventors: Franca Bigi, Giovanni Casiraghi, Giuseppe Casnati, Giovanni Sartori
  • Patent number: 4732897
    Abstract: The present invention relates to new 4-aza-17.beta.-substituted 5.alpha.-androstan-3-ones, to a process for their preparation, to pharmacological compostions containing them, and to the use of said compounds as inhibitors of androgen action by means of testosterone 5-reductase inhibition.
    Type: Grant
    Filed: February 3, 1986
    Date of Patent: March 22, 1988
    Assignees: Farmitalia Carlo Erba, S.p.A., Consiglio Nazionale Delle Ricerche
    Inventors: Gianfranco Cainelli, Giorgio Martelli, Mauro Panunzio, Giuseppe Spunta, Giuliano Nannini, Enrico di Salle
  • Patent number: 4377584
    Abstract: 4-Aza-17.beta.-substituted-5.alpha.-androstan-3-ones and their A-homo analogs of the formula: ##STR1## where Formula (I) may also have the structure of partial Formulas (II) and/or (III);and pharmaceutically acceptable salts of the above compounds are active as testosterone 5.alpha.-reductase inhibitors, and thus useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.
    Type: Grant
    Filed: September 23, 1980
    Date of Patent: March 22, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Gary H. Rasmusson, David B. R. Johnston, Glen E. Arth, deceased
  • Patent number: 4158059
    Abstract: The invention relates to novel dibenzo[1,2;5,6] cyclohepta pyridine or -pyrrole derivatives, dibenzo[2,3;6,7] oxepino pyridine or pyrrole derivatives, dibenzo[2,3;6,7] thiepino pyridine or pyrrole derivatives and dibenzo[b,f] pyrido or pyrrolo azepine derivatives of general formula: ##STR1## as well as the pharmaceutically acceptable salts and nitrogen oxides thereof, whereinR.sub.1, r.sub.2, r.sub.3 and R.sub.4 each represent hydrogen, hydroxy, halogen, an alkyl (1-6 C) group, an alkoxy or alkylthio group in which the alkyl group contains 1-6 C-atoms, or a trifluoromethyl group,R.sub.5 represents hydrogen, an alkyl group with 1-6 carbon atoms or an aralkyl group with 7-10 carbon atoms,M is the number 1 or 2,X represents oxygen, sulphur, the group ##STR2## or the group --CH.sub.2 -- and R.sub.6 represents hydrogen or a lower alkyl group (1-4 C),having CNS-depressant activity and excellent antihistamine and antiserotonin activities.
    Type: Grant
    Filed: June 23, 1978
    Date of Patent: June 12, 1979
    Assignee: Akzona Incorporated
    Inventor: Willem J. van der Burg
  • Patent number: 4158058
    Abstract: The invention relates to novel dibenzo[1,2;5,6]cyclohepta pyridine or -pyrrole derivatives, dibenzo[2,3;6,7]oxepino pyridine or pyrrole derivatives, dibenzo[2,3;6,7]thiepino pyridine or pyrrole derivatives and dibenzo[b,f]pyrido or pyrrolo azepine derivatives of general formula: ##STR1## as well as the pharmaceutically acceptable salts and nitrogen oxides thereof, whereinR.sub.1, r.sub.2, r.sub.3 and R.sub.4 each represent hydrogen, hydroxy, halogen, an alkyl (1-6 C) group, an alkoxy or alkylthio group in which the alkyl group contains 1-6 C-atoms, or a trifluoromethyl group,R.sub.5 represents hydrogen, an alkyl group with 1-6 carbon atoms or an aralkyl group with 7-10 carbon atoms,M is the number 1 or 2,X represents oxygen, sulphur, the group ##STR2## OR THE GROUP --CH.sub.2 -- and R.sub.6 represents hydrogen or a lower alkyl group (1-4 C),having CNS-depressant activity and excellent antihistamine and antiserotonin activities.
    Type: Grant
    Filed: June 26, 1978
    Date of Patent: June 12, 1979
    Assignee: Akzona Incorporated
    Inventor: Willem J. van der Burg