Plural Chalcogens Bonded Directly To Carbocyclic Rings Of The Tetracyclo Ring System (e.g., Pyridoanthraquinones, Etc.) Patents (Class 546/78)
-
Publication number: 20130296279Abstract: 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: ApplicationFiled: May 10, 2013Publication date: November 7, 2013Inventor: Adam Morgan
-
Patent number: 8486959Abstract: 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: GrantFiled: January 14, 2011Date of Patent: July 16, 2013Assignee: National Health Research InstitutesInventors: Shiow-Ju Lee, Cheng-Wei Yang, Yue-Zhi Lee, Yu-Sheng Chao
-
Patent number: 8367654Abstract: 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: GrantFiled: May 7, 2010Date of Patent: February 5, 2013Assignee: Tetraphase Pharmaceuticals, Inc.Inventors: Roger B. Clark, Minsheng He, Louis Plamondon, Xiao-Yi Xiao, Magnus P. Rönn
-
Publication number: 20120108569Abstract: 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: ApplicationFiled: May 7, 2010Publication date: May 3, 2012Inventors: Roger B. Clark, Minsheng He, Louis Plamondon, Xiao-Yi Xiao, Magnus P. Rönn
-
Publication number: 20110172261Abstract: 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: ApplicationFiled: January 14, 2011Publication date: July 14, 2011Applicant: National Health Research InstitutesInventors: Shiow-Ju Lee, Cheng-Wei Yang, Yue-Zhi Lee, Yu-Sheng Chao
-
Patent number: 7968561Abstract: 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: GrantFiled: August 28, 2008Date of Patent: June 28, 2011Assignee: Sterix LimitedInventors: Barry Victor Lloyd Potter, Michael John Reed, Lok Wai Lawrence Woo, Atul Purohit, Paul Foster
-
Publication number: 20110009371Abstract: 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: ApplicationFiled: May 12, 2010Publication date: January 13, 2011Inventors: Andrew G. Myers, Mark G. Charest, Christian D. Lerner, Jason D. Brubaker, Dionicio R. Siegel
-
Publication number: 20090182000Abstract: 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: ApplicationFiled: August 28, 2008Publication date: July 16, 2009Inventors: Barry Victor Lloyd Potter, Michael John Reed, Lok Wai Lawrence Woo, Atul Purohit, Paul Foster
-
Publication number: 20080312266Abstract: 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: ApplicationFiled: September 14, 2007Publication date: December 18, 2008Inventors: Barry Victor Lloyd Potter, Michael John Reed, Lok Wai Lawrence Woo
-
Publication number: 20080305082Abstract: 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: ApplicationFiled: September 14, 2005Publication date: December 11, 2008Inventors: John G. Curd, Robert L. Capizzi, John F.W. Keana
-
Patent number: 6506765Abstract: 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: GrantFiled: March 29, 2001Date of Patent: January 14, 2003Assignee: TAP Pharmaceutical Products, Inc.Inventors: Pramod K. Gupta, Deborah Milkowski, Debra Sutkowski-Markmann
-
Patent number: 6365597Abstract: 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: GrantFiled: February 11, 1997Date of Patent: April 2, 2002Assignee: Aventis Pharmaceuticals Inc.Inventors: James R. Pribish, Cynthia A. Gates, Philip M. Weintraub
-
Patent number: 6352997Abstract: 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: GrantFiled: May 3, 1999Date of Patent: March 5, 2002Assignee: Merck & Co., Inc.Inventors: Joanne Waldstreicher, Georgianna S. Harris
-
Patent number: 6204273Abstract: 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: GrantFiled: January 29, 1999Date of Patent: March 20, 2001Assignee: 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: 6180794Abstract: 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: GrantFiled: October 15, 1999Date of Patent: January 30, 2001Assignee: Ligand Pharmacueticals IncorparatedInventors: James P. Edwards, Todd K. Jones, Josef D. Riggenberg, Erick M. Carreira
-
Patent number: 6143887Abstract: 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: GrantFiled: May 11, 1999Date of Patent: November 7, 2000Assignee: Merck & Co., Inc.Inventors: Dominick F. Gratale, Richard L. Tolman, Soumya P. Sahoo
-
Patent number: 6127354Abstract: 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: GrantFiled: March 17, 1999Date of Patent: October 3, 2000Assignee: Novo Nordisk A/SInventors: Bernd Peschke, Michael Ankersen, Thomas Kruse Hansen, Henning Th.o slashed.gersen
-
Patent number: 6001846Abstract: 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: GrantFiled: February 17, 1998Date of Patent: December 14, 1999Assignee: Ligand Pharmaceuticals IncorporatedInventors: James P. Edwards, Todd K. Jones, Josef D. Riggenberg, Erick M. Carreira
-
Patent number: 5935968Abstract: 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: GrantFiled: March 12, 1998Date of Patent: August 10, 1999Assignee: Merck & Co., Inc.Inventors: Joanne Waldstreicher, Georgianna S. Harris
-
Patent number: 5886005Abstract: 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: GrantFiled: May 6, 1997Date of Patent: March 23, 1999Assignee: Merck & Co., Inc.Inventors: Susan D. Aster, Donald W. Graham
-
Patent number: 5854273Abstract: 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: GrantFiled: July 23, 1997Date of Patent: December 29, 1998Assignee: ADIR et CompagnieInventors: Gilbert Lavielle, Patrick Hautefaye, Ghanem Atassi, Alain Pierre, Laurence Kraus-Berthier, Stephane Leonce
-
Patent number: 5739137Abstract: 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: GrantFiled: February 28, 1996Date of Patent: April 14, 1998Assignee: 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: 5719158Abstract: 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: GrantFiled: June 5, 1995Date of Patent: February 17, 1998Assignee: 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: 5710275Abstract: Described are new 7.beta.-substituted 4-aza-5.alpha.-androstan-3-ones and related compounds as 5.alpha.-reductase inhibitors.Type: GrantFiled: April 3, 1995Date of Patent: January 20, 1998Assignee: 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: 5696266Abstract: 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: GrantFiled: July 28, 1995Date of Patent: December 9, 1997Assignee: Merck & Co., Inc.Inventors: Guy R. Humphrey, Ross A. Miller
-
Patent number: 5693809Abstract: 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: GrantFiled: May 12, 1995Date of Patent: December 2, 1997Assignee: 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: 5693647Abstract: 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: GrantFiled: June 5, 1995Date of Patent: December 2, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Lin Zhi, Christopher M. Tegley, David T. Winn, Lawrence G. Hamann, James P. Edwards, Sarah J. West
-
Patent number: 5688808Abstract: 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: GrantFiled: June 5, 1995Date of Patent: November 18, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, David T. Winn, Lin Zhi, Lawrence G. Hamann, Christopher M. Tegley, Charlotte L. F. Pooley
-
Patent number: 5610162Abstract: 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: GrantFiled: November 17, 1994Date of Patent: March 11, 1997Assignee: Merck & Co., Inc.Inventors: Bruce E. Witzel, Gary H. Rasmusson, Richard L. Tolman, Shu Shu Yang
-
Patent number: 5597832Abstract: 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: GrantFiled: November 10, 1994Date of Patent: January 28, 1997Assignee: Abbott LaboratoriesInventors: Michael R. Michaelides, Yufeng Hong
-
Patent number: 5578726Abstract: 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: GrantFiled: November 10, 1994Date of Patent: November 26, 1996Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Gary H. Rasmusson
-
Patent number: 5536727Abstract: 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: GrantFiled: November 17, 1994Date of Patent: July 16, 1996Assignee: Merck & Co., Inc.Inventors: Bruce E. Witzel, Richard L. Tolman, Gary H. Rasmusson, Raman K. Bakshi, Shu Shu Yang
-
Patent number: 5525608Abstract: 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: GrantFiled: April 20, 1994Date of Patent: June 11, 1996Assignee: Merck & Co., Inc.Inventors: Alan D. Adams, Gary H. Rasmusson, Nathan G. Steinberg
-
Patent number: 5516779Abstract: 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: GrantFiled: June 8, 1994Date of Patent: May 14, 1996Assignee: Merck & Co., Inc.Inventors: Derek Von Langen, Donald W. Graham, Richard L. Tolman
-
Patent number: 5359071Abstract: 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: GrantFiled: March 12, 1993Date of Patent: October 25, 1994Assignee: Merck & Co., Inc.Inventors: Philippe L. Durette, Craig K. Esser, William Hagmann, Ihor E. Kopka
-
Patent number: 5294701Abstract: 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: GrantFiled: May 6, 1992Date of Patent: March 15, 1994Assignee: Pharmachemie B.V.Inventors: Johan W. Scheeren, Joannes F. M. de Bie, Dirk de Vos
-
Patent number: 5276053Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: October 6, 1992Date of Patent: January 4, 1994Assignee: Warner-Lambert CompanyInventor: Graham Johnson
-
Patent number: 5180736Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: May 17, 1991Date of Patent: January 19, 1993Assignee: Warner-Lambert CompanyInventor: Graham Johnson
-
Patent number: 5116983Abstract: 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: GrantFiled: May 8, 1990Date of Patent: May 26, 1992Assignee: Merck & Co., Inc.Inventors: Apurba Bhattacharya, Alan W. Douglas, Edward J. Grabowski, Ulf H. Dolling
-
Patent number: 5071853Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: February 27, 1990Date of Patent: December 10, 1991Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
-
Patent number: 4914106Abstract: 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: GrantFiled: August 4, 1988Date of Patent: April 3, 1990Assignee: Teikoku Hormone Mfg. Co., Ltd.Inventors: Kenyu Shibata, Nobuaki Yamakoshi, Naoyuki Koizumi, Shigehiro Takegawa, Eiichiro Shimazawa, Mamoru Mieda
-
Patent number: 4888336Abstract: 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: GrantFiled: July 28, 1987Date of Patent: December 19, 1989Assignee: SmithKline Beckman CorporationInventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
-
Patent number: 4874803Abstract: 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: GrantFiled: September 21, 1987Date of Patent: October 17, 1989Assignee: Pennwalt CorporationInventors: Arthur L. Baron, Terry N. Myers, Jerome Wicher
-
Patent number: 4863918Abstract: 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: GrantFiled: July 19, 1988Date of Patent: September 5, 1989Assignee: BOC, Inc.Inventors: Kanti J. Gala, Ross C. Terrell
-
Patent number: 4785103Abstract: 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: GrantFiled: February 27, 1986Date of Patent: November 15, 1988Assignee: Teikoku Hormone Mfg. Co., Ltd.Inventors: Kenyu Shibata, Nobuaki Yamakoshi, Naoyuki Koizumi, Shigehiro Takegawa, Eiichiro Shimazawa, Mamoru Mieda
-
Patent number: 4739062Abstract: 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: GrantFiled: June 27, 1986Date of Patent: April 19, 1988Assignee: Consiglio Nazionale Delle RicercheInventors: Franca Bigi, Giovanni Casiraghi, Giuseppe Casnati, Giovanni Sartori
-
Patent number: 4732897Abstract: 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: GrantFiled: February 3, 1986Date of Patent: March 22, 1988Assignees: Farmitalia Carlo Erba, S.p.A., Consiglio Nazionale Delle RicercheInventors: Gianfranco Cainelli, Giorgio Martelli, Mauro Panunzio, Giuseppe Spunta, Giuliano Nannini, Enrico di Salle
-
Patent number: 4377584Abstract: 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: GrantFiled: September 23, 1980Date of Patent: March 22, 1983Assignee: Merck & Co., Inc.Inventors: Gary H. Rasmusson, David B. R. Johnston, Glen E. Arth, deceased
-
Patent number: 4158059Abstract: 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: GrantFiled: June 23, 1978Date of Patent: June 12, 1979Assignee: Akzona IncorporatedInventor: Willem J. van der Burg
-
Patent number: 4158058Abstract: 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: GrantFiled: June 26, 1978Date of Patent: June 12, 1979Assignee: Akzona IncorporatedInventor: Willem J. van der Burg