Acyclic Nitrogen Bonded Directly To The -c(=x)- Group Patents (Class 546/169)
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Patent number: 5700821Abstract: The present invention is directed to compounds having the formula: ##STR1## The invention further provides a method of making the compounds. The compounds are useful as inhibitors of protein phosphatases, for example PP1, PP2A, PP3, CDC25A and CDC25B. The invention is further directed to a method of inhibiting a protein phosphatase, a method of inhibiting cell proliferation, and pharmaceutical compositions comprising the subject compounds.Type: GrantFiled: July 30, 1996Date of Patent: December 23, 1997Assignee: University of PittsburghInventors: John S. Lazo, Robert L. Rice, April Cunningham, Peter Wipf
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Patent number: 5698569Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 7, 1995Date of Patent: December 16, 1997Assignee: G. D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, John N. Freskos, Ko-Chung Lin, Robert M. Heintz, Donald J. Rogier, Jr., Deborah E. Bertenshaw
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Patent number: 5691366Abstract: A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)-alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, andR.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4 wherein Y is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.Type: GrantFiled: October 31, 1995Date of Patent: November 25, 1997Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masayuki Kato, Shigetaka Nishino, Mitsuko Hamano, Hisashi Takasugi
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Patent number: 5679688Abstract: The present invention discloses the compounds of general formula (1) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 are optionally substituted carbonyl and amide derivatives which are useful as inhibitors of retroviral proteases, and are effective in treating conditions characterized by unwanted activity of these enzymes, such as acquired immune deficiency syndrome.Type: GrantFiled: November 4, 1994Date of Patent: October 21, 1997Assignee: Narhex LimitedInventor: Damian Wojciech Grobelny
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Patent number: 5679687Abstract: The present invention relates to novel compounds of formula (I) which have inhibitory activity against human immunodeficiency virus ("HIV") protease, a process for the preparation thereof, and compositions for prevention or treatment of AIDS by HIV infection comprising the above compounds as active ingredients. ##STR1## wherein: R.sup.1 is an aromatic group, a nitrogen-containing aromatic group, C.sub.1-4 alkyl group optionally substituted with an aromatic group or a nitrogen-containing aromatic group, C.sub.1-4 alkoxy group optionally substituted with an aromatic group or a nitrogen-containing aromatic group;R.sup.2 is an amino acid residue or a C.sub.1-8 alkyl group substituted with a C.sub.1-4 alkylsulfonyl group;R.sup.3 is a C.sub.1-4 alkyl group optionally substituted with an aromatic group;R.sup.4 is hydrogen or a C.sub.1-4 alkyl group;R.sup.5 is an aromatic group, a C.sub.1-10 alkyl group or a C.sub.1-4 alkyl groups optionally substituted with an aromatic group; andn is 1 or 2.Type: GrantFiled: June 6, 1996Date of Patent: October 21, 1997Assignee: LG Chemical LimitedInventors: Nakyen Choy, Hoil Choi, Chi-Hyo Park, Young-Chan Son, Chang-Sun Lee, Heungsik Yoon, Sung-Chun Kim, Jong-Sung Koh, Chung-Ryeol Kim
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Patent number: 5670511Abstract: Indolepiperidine derivatives of the formula I ##STR1## and their physiologically acceptable salts exhibit action on the central nervous system, in particular dopamine-agonistic or dopamine-antagonistic action.Type: GrantFiled: January 16, 1996Date of Patent: September 23, 1997Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Joachim Marz, Hartmut Greiner, Christoph Seyfried, Gerd Bartoszyk
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Patent number: 5670517Abstract: The present invention relates to novel compounds of formula (I) which has inhibitory activities against human immunodeficiency virus ("HIV") protease, a process for the preparation thereof, and compositions for prevention or treatment of AIDS by HIV infection comprising the above compounds as active ingredients. ##STR1## wherein: R.sup.1 is an aromatic group, a nitrogen-containing aromatic group, C.sub.1-4 alkyl group optionally substituted with an aromatic group or a nitrogen-containing aromatic group, C.sub.1-4 alkoxy group optionally substituted with an aromatic group or a nitrogen-containing aromatic group;R.sup.2 is an amino acid residue or a C.sub.1-8 alkyl group substituted with a C.sub.1-4 alkylsulfonyl group;R.sup.3 is a C.sub.1-4 alkyl group optionally substituted with an aromatic group;R.sup.4 is hydrogen or a C.sub.1-2 alkyl group;R.sup.5 is a C.sub.1-10 alkyl group optionally substituted with an aromatic group; andn is 1 or 2.Type: GrantFiled: June 6, 1996Date of Patent: September 23, 1997Assignee: LG Chemical LimitedInventors: Nakyen Choy, Hoil Choi, Chi-Hyo Park, Young-Chan Son, Chang-Sun Lee, Heungsik Yoon, Sung-Chun Kim, Jong-Sung Koh, Chung-Ryeol Kim
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Patent number: 5658933Abstract: The invention relates to compounds of the formula I, ##STR1## to a process for their preparation and to their use as pharmaceuticals. The compounds are employed, in particular, as ester prodrugs of prolyl hydroxylase inhibitors for inhibiting collagen biosynthesis and as fibrosuppressive agents.Type: GrantFiled: October 31, 1994Date of Patent: August 19, 1997Assignee: Hoechst AktiengesellschaftInventors: Klaus Weidmann, Karl-Heinz Baringhaus, Georg Tschank, Martin Bickel
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Patent number: 5650514Abstract: The present invention relates to 3-substituted quinoline-5-carboxylic acid derivatives and processes for their preparation.Type: GrantFiled: July 17, 1995Date of Patent: July 22, 1997Assignee: Bayer AktiengesellschaftInventors: Jurgen Stoltefuss, Michael Negele, Karl-Heinz Wahl, Jan-Bernd Lenfers, Samir Samaan
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Patent number: 5627193Abstract: The present invention relates to quinoline-4-carbonylguanidine derivative represented by formula (1) ##STR1## and pharmaceutically acceptable salt thereof, a process for producing the same, and a Na.sup.+ /H.sup.+ exchanger inhibitor containing the compound as an active ingredient. The compounds of the present invention are useful as an agent for treating or preventing various diseases by hyperfunction of the Na.sup.+ /H.sup.+ exchanger and as a diagnostic agent for these diseases.Type: GrantFiled: January 31, 1996Date of Patent: May 6, 1997Assignee: Mitsui Toatsu Chemicals, Inc.Inventors: Junya Fujiwara, Haruki Mori, Hiroyuki Yamashita, Takashi Kitamori, Junko Hosoya, Hitoshi Banno
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Patent number: 5624939Abstract: Compounds of formula I ##STR1## wherein the substituents are as defined herein, are disclosed as treatments for disorders linked to CCK and gastrin. Processes for preparing the compounds are also taught.Type: GrantFiled: June 28, 1995Date of Patent: April 29, 1997Assignee: Rhone-Poulenc Rorer, S.A.Inventors: Marc Capet, Marie-Christine Dubroeucq
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Patent number: 5616711Abstract: A method of producing an aminobutene derivative of formula (I) by allowing a butenol derivative of formula (II) to react with an amide derivative of formula (III) is disclosed. The aminobutene derivative of formula (I) can be deprotected to produce an aminobutene derivative of formula (I-1) or an aminobutene derivative of formula (I-2): ##STR1## The aminobutene derivative of formula (I-A) can also be deprotected to produce the aminobutene derivative of formula (I-B). Any or all of the above aminobutene derivatives are useful as intermediates for producing anti-ulcer drugs, and anti-ulcer drugs having an inhibitory effect on gastric acid secretion based on the antagonism against histamine H.sub.2 receptor.Type: GrantFiled: August 6, 1993Date of Patent: April 1, 1997Assignee: Fujirebio Inc.Inventors: Hiroshi Ikawa, Hajime Matsumoto, Masakatsu Matsumoto, Yasuo Sekine, Masato Nishimura, Akihiko Hosoda
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Patent number: 5614533Abstract: Disclosed herein are compounds of formula 1 ##STR1## wherein X is a terminal group, for example, an aryloxycarbonyl, an alkanoyl or an optionally mono- or disubstituted carbamoyl; B is absent or an amino acid residue, for example, Val or Ash; R.sup.1 is hydrogen or a ring substituent, for example, fluoro or methyl; R.sup.2 is alkyl; and Y is a ring substituent, for example, phenoxy, 2-pyridinylmethoxy, phenylthio or 2-pyridinylthio. The compounds inhibit the activity of human immunodeficiency virus (HIV) protease and interfere with HIV induced cytopathogenic effects in human cells. These properties render the compounds useful for combating HIV infections.Type: GrantFiled: November 9, 1994Date of Patent: March 25, 1997Assignee: Bio-Mega/Boehringer Ingelheim Research, Inc.Inventors: Paul C. Anderson, Fran.cedilla.ois Soucy, Christiane Yoakim, Pierre Lavall ee, Pierre L. Beaulieu
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Patent number: 5605896Abstract: This invention provides bicyclic heterocyclic derivatives and their pharmaceutically acceptable salts useful for the treatment of hypertension, urethral and lower urinary tract contractions, and other disorders. The compounds are also useful for binding .alpha..sub.1 -adrenergic and 5HT.sub.1A serotonergic receptors, in vitro or in vivo.Type: GrantFiled: August 31, 1994Date of Patent: February 25, 1997Assignee: Recordati S.A., Chemical and Pharmaceutical CompanyInventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
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Patent number: 5587388Abstract: The present invention provides cis-epoxide compounds represented by formula (I-1), (I-2) or (I-3) which are useful for treating or preventing diseases caused by HIV infection: ##STR1## wherein: A, B, D, E, R.sup.1, R.sup.10, R.sup.11, K, G, Q, r and J have the meanings as defined in the specification.Type: GrantFiled: November 30, 1993Date of Patent: December 24, 1996Assignee: Lucky LimitedInventors: Sung C. Kim, Nakyen Choy, Chang S. Lee, Young C. Son, Ho I. Choi, Jong S. Koh, Heungsik Yoon, Chi H. Park, Sang S. Kim
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Patent number: 5585397Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: November 24, 1993Date of Patent: December 17, 1996Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Roger D. Tung, Mark A. Murcko, Govinda R. Bhisetti
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Patent number: 5578606Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: October 30, 1992Date of Patent: November 26, 1996Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 5554653Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.Type: GrantFiled: December 22, 1992Date of Patent: September 10, 1996Assignee: Eli Lilly and CompanyInventors: Kwan Hui, Charles D. Jones, Louis N. Jungheim, Timothy A. Shepherd
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Patent number: 5552405Abstract: Disclosed herein are compounds of formula 1 ##STR1## wherein X is a terminal group, for example, an aryloxycarbonyl or an alkanoyl; B is absent or an amino acid residue, for example, Val or Asn; R.sup.1 is alkyl; and Y is a ring substituent, for example, benzyl, benzyloxy, phenylthio or 2-pyridinylthio. The compounds inhibit the activity of human immunodeficiency virus (HIV) protease and interfere with HIV induced cytopathogenic effects in human cells. These properties render the compounds useful for combating HIV infections.Type: GrantFiled: July 31, 1995Date of Patent: September 3, 1996Assignee: Bio-Mega/Boehringer Ingelheim Research, Inc.Inventors: Vida Gorys, Fran.cedilla.ois Soucy, Christiane Yoakim, Pierre L. Beaulieu
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Patent number: 5545640Abstract: Disclosed herein are compounds which inhibit human immunodeficiency virus (HIV) protease activity and inhibit HIV replication in human cells. Thus, the compounds are indicated for the treatment of HIV infections. The compounds can be represented by the formula ##STR1## wherein X is a terminal group, for example, an aryloxycarbonyl, an alkanoyl or an arylalkyl carbamoyl; A is absent or an amino acid or a derived amino acid; either R.sup.1 or R.sup.2 is hydrogen while the other is alkyl or R.sup.1 and R.sup.2 are joined to form a cyclohexane; Q is hydrogen, hydroxy, halo or lower alkoxy; and Y is a terminal group, for example, an alkylamino, alkoxy or an optionally substituted anilino.Type: GrantFiled: April 4, 1995Date of Patent: August 13, 1996Assignee: Bio-Mega/Boehringer Ingeleheim Research Inc.Inventors: Pierre L. Beaulieu, Ingrid Guse
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Patent number: 5534530Abstract: The invention relates to thiadiazole derivatives corresponding to the general formula ##STR1## in which Ar represents a nitrogen-containing aromatic heterocycle, in particular indolyl which is substituted or unsubstituted on the nitrogen atom with CO--(C.sub.1 -C.sub.4)alkyl; with (CH.sub.2).sub.n COR in which n represents 1 or 2 and R represents OR.sub.1 or NR.sub.1 R.sub.2 with R.sub.1 and R.sub.2, which may be identical or different, representing H or (C.sub.1 -C.sub.4)alkyl; with (C.sub.1 -C.sub.4) hydroxyalkyl; with (C.sub.2 -C.sub.6) alkoxyalkyl; tetrahydropyranyl; or with a --(CH.sub.2).sub.3 -- chain, the last carbon of which is attached to the phenyl ring of the indole to form a 6-membered ring;Z represents(a) the group ##STR2## where A and B, independently of each other, represent C, CH or N; and X.sub.1, X.sub.2, X.sub.3 and X.sub.4, which may be identical or different, represent H, (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.Type: GrantFiled: April 13, 1994Date of Patent: July 9, 1996Assignee: Elf SanofiInventors: Daniel Frehel, Danielle Gully, Robert Boigegrain, Alain Badorc, Jean-Pierre Bras, Pierre Despeyroux
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Patent number: 5529978Abstract: Certain N-acetonyl-substituted-amides of the formula: ##STR1## wherein A is a heterocycle, a phenylalkyl, a phenylalkoxy, naphthyl, cycloalkyl, alkoxyalkyl, alkyl, haloalkyl or alkenyl group; X, Y and Z are selected from the group consisting of hydrogen, halo, cyano, thiocyano, isothiocyano, methylsulfonyloxy, thio(C.sub.1 -C.sub.2)alkyl, (C.sub.1 -C.sub.2)alkoxy, carbamoyl, dithiocarbamoyl, hydroxy, azide, trifluoromethylcarboxy, (C.sub.1 -C.sub.4)alkylcarbonyloxy, phenylcarbonyloxy, phenoxy, thiophenyl, imidazolyl or triazolyl group as described herein; R.sup.1 and R.sup.2 are each independently a hydrogen atom or a (C.sub.1 -C.sub.6)alkyl group; and compositions containing these amides are fungicidally active, particularly against phytopathogenic fungi.Type: GrantFiled: May 3, 1994Date of Patent: June 25, 1996Assignee: Rohm and Haas CompanyInventor: Ashok K. Sharma
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Patent number: 5516784Abstract: Compounds of formula ##STR1## wherein Ar, W, Z, Q, R.sub.1, U, and T are as set forth herein, are described. These compounds are active as agents against retroviruses and in particular against HIV.Type: GrantFiled: February 10, 1994Date of Patent: May 14, 1996Assignee: Schering CorporationInventors: Frank Bennett, Ashit Ganguly, Viyyoor Girijavallabhan, Naginbhai Patel
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Patent number: 5514690Abstract: Novel compounds having potassium channel activating activity and useful, for example, as antiischemic agents are disclosed. These compounds have the general formula ##STR1## wherein A is ##STR2## or a single bond to complete an indoline nucleus; X is --O--, --S-- or --NCN; and the R groups are as defined herein.Type: GrantFiled: August 24, 1993Date of Patent: May 7, 1996Assignee: E. R. Squibb & Sons, Inc.Inventors: Karnail S. Atwal, Francis N. Ferrara
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Patent number: 5510487Abstract: Hydroxyethylamine compounds are effective as retrovital protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 25, 1995Date of Patent: April 23, 1996Assignee: G.D. Searle & Co.Inventors: John J. Talley, Kathryn L. Reed
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Patent number: 5510090Abstract: The invention relates to a process for the selective extraction of (III) actinides by means of amides having a nitrogenous heterocyclic substituent of formula: ##STR1## in which R.sup.1 is an alkyl or alkoxy group or a hydrogen atom, R.sup.2 and R.sup.3, which can be the same or different, represent a hydrogen atom, an alkyl or an alkoxy group and R.sup.4 is a hydrogen atom or a group of formula: ##STR2## in which R.sup.5 and R.sup.6, which can be the same or different, represent a hydrogen atom or an alkyl or alkoxy group. This process makes it possible to separate (III) actinides from (III) lanthanides.Type: GrantFiled: July 27, 1993Date of Patent: April 23, 1996Assignee: Commissariat a l'Energie AtomiqueInventors: Christine Cuillerdier, Claude Musikas
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Patent number: 5508407Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of their use.Type: GrantFiled: April 29, 1992Date of Patent: April 16, 1996Assignee: Eli Lilly and CompanyInventors: Stephen W. Kaldor, Marlys Hammond
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Patent number: 5495023Abstract: A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, andR.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4whereinY is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.Type: GrantFiled: May 3, 1994Date of Patent: February 27, 1996Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masayuki Kato, Shigetaka Nishino, Mitsuko Hamano, Hisashi Takasugi
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Patent number: 5492915Abstract: This invention relates to compounds having selective LTB.sub.4 antagonist properties. Therapeutic compositions comprising said compounds and methods for the treatment of disorders involving LTB.sub.4 agonist-mediated activity utilizing said compositions wherein the compounds are described by the formula ##STR1## wherein R.sub.4, X, R, Y, R', Q, m and n are herein defined, and pharmaceutically acceptable salts thereof.Type: GrantFiled: October 6, 1994Date of Patent: February 20, 1996Assignee: Rhone-Poulenc Rorer S.A.Inventors: Norbert Dereu, Wolfram Hendel, Richard Labaudiniere
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Patent number: 5482947Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: November 15, 1993Date of Patent: January 9, 1996Inventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Ko-Chung Lin, Michael L. Vazquez, Richard A. Mueller, Kathryn L. Reed, Robert M. Heintz, Michael Clare, John N. Freskos, Eric T. Sun
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Patent number: 5478845Abstract: Piperidine derivatives of formula ##STR1## wherein A is straight or branched alkyl, alkoxy-alkyl, or alkenyl; X is O or NH; Y is O, S, NH, NCN, or N-alkyl; R.sup.1 is 6-fluoro-1,2-benzisoxazol-3-yl, 6-fluoro-1H-indazol-3-yl, or 6-fluoro-1-methyl-1H-indazol-3-yl; R.sup.2 is alkyl or phenyl; and R.sup.3 is phenyl optionally substituted, or R.sup.3 is ##STR2## wherein Z represents a 5- or 6-membered heterocyclic ring; or R.sup.2 and R.sup.3 together with the nitrogen atom form a fused heterocyclic ring system; or pharmaceutically acceptable salts thereof are useful in the treatment of indications related to the CNS-system, cardiovascular system or to gastrointestinal disorders.Type: GrantFiled: May 23, 1994Date of Patent: December 26, 1995Assignee: Novo Nordisk A/SInventors: John B. Hansen, Frederik C. Gronvald, John P. Mogensen
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Patent number: 5474994Abstract: This invention provides bicyclic heterocyclic derivatives and their pharmaceutically acceptable salts useful for the treatment of hypertension, urethral and lower urinary tract contractions, and other disorders. The compounds are also useful for binding .alpha..sub.1 -adrenergic and 5HT.sub.1A serotonergic receptors, in vitro or in vivo.Type: GrantFiled: May 26, 1993Date of Patent: December 12, 1995Assignee: Recordati S.A., Chemical and Pharmaceutical CompanyInventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
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Patent number: 5475027Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: November 8, 1993Date of Patent: December 12, 1995Assignee: G.D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, Ko-Chung Lin, Gary A. DeCrescenzo, Donald J. Rogier, Jr., John N. Freskos
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Patent number: 5475013Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 20, 1992Date of Patent: December 12, 1995Assignee: Monsanto CompanyInventors: John J. Talley, Daniel P. Getman, John N. Freskos, Ko-Chung Lin, Robert M. Heintz, Donald J. Rogier, Jr., Deborah E. Bertenshaw
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Patent number: 5451605Abstract: Compounds of the formula ##STR1## where R.sub.1 -R.sub.5 are hydrogen, lower alkyl of 1-6 carbons, or halogen; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, or CR.sub.7 OR.sub.13 O, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.Type: GrantFiled: December 30, 1993Date of Patent: September 19, 1995Assignee: Allergan, Inc.Inventors: Roshantha A. Chandraratna, Richard L. Beard
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Patent number: 5434265Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating HIV infection.Type: GrantFiled: December 22, 1992Date of Patent: July 18, 1995Assignee: Eli Lilly and CompanyInventors: James E. Fritz, Marlys Hammond, Stephen W. Kaldor
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Patent number: 5430041Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, aralkanoyl, heterocyclylcarbonyl or a group of the formula: ##STR2## R.sup.2 is alkyl, cycloalkylalkyl or aralkyl; R.sup.3 is hydrogen and R.sup.4 is hydroxy or R.sup.3 and R.sup.4 together are oxo; R.sup.5 is alkoxycarbonyl or alkylcarbamoyl; R.sup.6 and R.sup.7 together are trimethylene or tetramethylene optionally substituted by alkyl or on adjacent carbon atoms by tetramethylene; R.sup.8 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, aroyl, aralkanoyl or heterocyclylcarbonyl; and R.sup.9 is alkyl, cycloalkyl, cycloalkylalkyl, aralkyl, cyanoalkyl, carbamoyl-alkyl, alkylthioalkyl, alkoxyalkyl or alkoxycarbonylalkyl: and pharmaceutically acceptable acid addition salts of those compounds of formula I which are basic, inhibit aspartyl proteases of viral origin and can be used in the form of medicaments for the prophylaxis or treatment of viral infections.Type: GrantFiled: April 21, 1992Date of Patent: July 4, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Joseph A. Martin, Gareth J. Thomas
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Patent number: 5424426Abstract: The invention relates to dithiolanylglycine-containing HIV protease inhibitors of the hydroxyethylene isostere type of the general formula (I) ##STR1## processes for their preparation and their use as retroviral agents.Type: GrantFiled: May 10, 1993Date of Patent: June 13, 1995Assignee: Bayer AktiengesellschaftInventors: Dieter Habich, Wolfgang Bender, Jutta Hansen, Arnold Paessens
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Patent number: 5416117Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: February 28, 1994Date of Patent: May 16, 1995Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5413997Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.Type: GrantFiled: January 21, 1993Date of Patent: May 9, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
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Patent number: 5395849Abstract: The present invention provides novel antitumor agents which are hybrid molecules consisting of a cyclic enediyne unit attached to a DNA-binding unit via a linker unit, and having the general formula (I)D--(OCH.sub.2).sub.m --O--(CH.sub.2).sub.n --Ar--Y--CONH--B(I)wherein D is a cyclic enediyne; B is a residue capable of binding to the minor groove of DNA; n is 0 and m is 1, is or n is 1 and m is 0 or 1; Ar is an aromatic residue selected from the group consisting of phenyl, naphthyl, pyridyl, quinolinyl and indolyl; and Y is a direct bond, --CH.sub.2 -- or --CH.dbd.CH--; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 5, 1993Date of Patent: March 7, 1995Assignee: Bristol-Myers Squibb CompanyInventors: Mark D. Wittman, David Langley, John F. Kadow
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Patent number: 5389645Abstract: The present invention provides substituted tyrosyl diamine amide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable salts thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: August 13, 1992Date of Patent: February 14, 1995Assignee: G. D. Searle & Co.Inventors: Donald W. Hansen, Jr., Nizal S. Chandrakumar, Karen B. Peterson, Sofya Tsymbalov
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Patent number: 5380925Abstract: Novel cyclic amino acids which are useful in preparing biologically active peptides as well as a process for the preparation of D and L enantiomers of the cyclic amino acids are described where an N-protected derivative of the racemic cyclic amino acid is treated with (-)cinchonidine and the resulting salt resolved into the desired enantiomers, as well as derivatives thereof and valuable intermediates used in the process.Type: GrantFiled: August 20, 1993Date of Patent: January 10, 1995Assignee: Warner-Lambert CompanyInventors: Vladimir Beylin, Huai G. Chen, Om P. Goel, Mark E. Marlatt, John G. Topliss
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Patent number: 5346907Abstract: Analogs of CCK-tetrapeptides, which analogs have the formula ##STR1## wherein A, B, D, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are specifically defined, having activity as CCK antagonists, useful in the treatment or prevention of disorders of the gastrointestinal, central nervous, appetite regulating or pain regulating systems.Type: GrantFiled: February 16, 1993Date of Patent: September 13, 1994Assignee: Abbott LaboratoriesInventors: James F. Kerwin, Jr., Mark W. Holladay, Michael J. Bennett
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Patent number: 5334724Abstract: A process for the preparation of a substituted 2-chloropyridine derivatives of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent hydrogen or various other radicals, which comprises reacting a pyridine-1-oxide of the formula ##STR2## with an aromatic carbonyl chloride in the presence of an inert organic solvent and in the presence of an acid acceptor at a temperature between about -20.degree. C. and 200.degree. C.Type: GrantFiled: June 24, 1992Date of Patent: August 2, 1994Assignee: Bayer AktiengesellschaftInventors: Dieter Kaufmann, Klaus Jelich, Rudolf Braden, Winfried Rosen
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Patent number: 5328909Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: June 25, 1992Date of Patent: July 12, 1994Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5326770Abstract: This invention relates to monoamine oxidase-B (MAO-B) inhibitory 5-substituted 2,4-thiazolidinediones, such as Formula I, to pharmaceutical compositions thereof, process of preparation, and methods of use in mammals to treat cognitive disorders, neurological dysfunction, and/or mood disturbances such as, but not limited to degenerative nervous system diseases.Type: GrantFiled: July 17, 1992Date of Patent: July 5, 1994Assignee: The Du Pont Merck Pharmaceutical CompanyInventor: Wendell W. Wilkerson
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Patent number: 5322948Abstract: The present invention pertains to a method of preparing substituted and unsubstituted N-hydroxy-2-aminobutane diacid derivatives. The invention also pertains to the use of N-hydroxy-2-aminoethane derivatives (including the N-hydroxy-2-aminobutane diacid derivatives) in the preparation of pyridine derivatives.Type: GrantFiled: January 2, 1992Date of Patent: June 21, 1994Assignee: Hoechst Celanese CorporationInventors: Varadaraj Elango, Donald R. Larkin, John R. Fritch, Michael P. Bodman, Werner H. Mueller, Bernard F. Gupton, John C. Saukaitis
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Patent number: 5314886Abstract: This invention relates to novel N-substituted lactams having the following formula ##STR1## useful in the treatment and prevention of Cholecystokinin (CCK) related disorders of the gastrointestinal, central nervous and appetite regulatory systems of mammals.Type: GrantFiled: October 29, 1992Date of Patent: May 24, 1994Assignee: G. D. Searle & Co.Inventors: Daniel P. Becker, Daniel L. Flynn, Clara I. Villamil
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Patent number: RE34878Abstract: A compound of D-phenylalanine derivative for hypoglycemic use, represented by the general formula ##STR1## R.sup.1 is selected from hydrogen, alkyl of 1 to 5 carbon atoms, aryl of 6 to 12 carbon atoms, aralkyl of 6 to 12 carbon atoms, ##STR2## --CH.sub.2 CO.sub.2 R.sup.3, --CH(CH.sub.3)--OCO--R.sup.3, and --CH.sub.2 --OCO--C(CH.sub.3).sub.3 ; R.sup.2 is selected from groups comprising aryl of 6 to 12 carbon atoms, a hetero six-membered ring, a hetero five-membered ring, cycloalkyl, or cycloalkenyl, any of which groups may have one or more substituents; and R.sup.3 is selected from hydrogen and alkyl of 1 to 5 carbon atoms; the salts thereof, and precursors which can be converted thereto in the human or animal body.Some of the compounds are novel per se.Type: GrantFiled: November 23, 1993Date of Patent: March 14, 1995Assignee: Ajinomoto Co., Inc.Inventors: Shigeshi Toyoshima, Yoshiko Seto, Hisashi Shinkai, Koji Toi, Izumi Kamashiro