AR018370A1 - Inhibidores de proteasas, composiciones farmaceuticas que lo comprenden, uso de los mismos para la manufactura de un medicamento - Google Patents

Inhibidores de proteasas, composiciones farmaceuticas que lo comprenden, uso de los mismos para la manufactura de un medicamento

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Publication number
AR018370A1
AR018370A1 ARP990102442A ARP990102442A AR018370A1 AR 018370 A1 AR018370 A1 AR 018370A1 AR P990102442 A ARP990102442 A AR P990102442A AR P990102442 A ARP990102442 A AR P990102442A AR 018370 A1 AR018370 A1 AR 018370A1
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AR
Argentina
Prior art keywords
alkyl
phenyl
thiophene
alkoxy
benzoxazole
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ARP990102442A
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English (en)
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Smithkline Beecham Corp
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Publication date
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Publication of AR018370A1 publication Critical patent/AR018370A1/es

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/89—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
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    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
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    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/84—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
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    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Furan Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Quinoline Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)

Abstract

Se proporciona inhibidores de proteasa de bis-aminometil-carbonilo, que comprenden un compuesto de la formula(I):R1 y R2 son independientemente H o alquiloC1-6,siempre y cuando R1 y R2 no sean ambos alquilo C1-6;formula(II)R3 se elige entre el grupoformado pr CH2CH(CH3)2, CH2CH2CH3, CH3CH=CH2 o CH2Ph;R4 se eligeentre el grupo formado por: alquilo C0-6; N-piperizina; N-tetrahidroisoquinoleína; alquilo C0-6 sustituido con fenilo, tiofeno, benzotiazol, 2-, 3-, 4-, 5-, 6-o 7-quinoleína, naftilo, 1-(7-nitro-2, 1, 3-benzoxadiazol-4-il)-L-prolilo, alquil(C0-6)pirazol, N-Cbz-2-(N,N-dimetilamino)etilglicil-, N-metilpirrol,benzoxazol, benciloxi, alcoxi C1-6; 2, 3, o 4-piridiniloxi; adamantilo, tieno [3,2-b]tiofeno; fenilo; tiofeno; benzotiofeno; benozofurano; benzotiazol; 2-, 3-,4-, 5-, 6- o 7-quinoleína; naftilo; y benzoxazol, cada uno de ellos independientemente sustituido con uno o más de los grupos alquilo C1-6, halogeno, nitro,ciano, hidroxi, alcoxi C1-6, trifluormetilo, carboxil, éster carboxi-alquilo (C1-6), alquil(C0-6)2N-alquilo C0-6, alquil (C0-6) 2N-alcoxi C0-6, N-(C0-C6)-N-piperizina, N-(N-alquil(C0-C6)N-piperidina)-4-alquil (C0-6)-amina, (alquil(C0-6) 2N-alquil(C0-6)-amina, N-morfolino-alquilo C0-6, N-morfolino-alquilo C0-6,N-morfolino-alcoxi C0-6, fenilo, tiofeno, benzotiazol, 2, 3, 4, 5, 6 o 7-quinoleína, naftilo, alquil(C0-6) pirazol, N-metil-pirrol, benzoxazol; benciloxisustituido con uno o más grupos alquilo (C1-6), halogeno, nitro, ciano, hidroxi, alcoxi (C1-6), trifluormetilo, carboxilo, éster carboxi alquilo (C1-6), fenilo, tiofeno, bentiazol, 2, 3, 4, 5 o 7 quinoleína, naftilo, alquil (C0-6) pirazol, N-metil-pirrol, y benzoxazol; y pirazina; pirimidina; 2,7-dimetilpirazolo[1,5a]pirimidina y 4,7 dimetilpirazolo[5,1-c][1,2,4]-triazina. R6 se elige entre el grupo formado por fenilo y fenilo sustituido con alquilo C0-6, N-piperidina,benzofurano; o 2,3 o 4 piridina; Q es formula (III)en la que R7 se elige entre el grupo formado por fenilo y fenilo sustituidocon alquilo (C0-C6),N-piperidina, benzofurano; o 2, 3 o 4 piridina; R8 se elige entre el grupo formado por H, CH2Ch(CH3)2, CH2CH2CH3 y CH2CH=CH2, CH2Ph, cuando R9 es H; o R8 y R9
ARP990102442A 1998-05-21 1999-05-21 Inhibidores de proteasas, composiciones farmaceuticas que lo comprenden, uso de los mismos para la manufactura de un medicamento AR018370A1 (es)

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US8655798P 1998-05-21 1998-05-21

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US (1) US6518267B1 (es)
EP (1) EP1067894A4 (es)
JP (1) JP2002515411A (es)
AR (1) AR018370A1 (es)
AU (1) AU4092799A (es)
CA (1) CA2332531A1 (es)
CO (1) CO5080801A1 (es)
DZ (1) DZ2796A1 (es)
MA (1) MA26631A1 (es)
WO (1) WO1999059526A2 (es)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6586466B2 (en) 1995-10-30 2003-07-01 Smithkline Beecham Corporation Carbohydrazide-protease inhibitors
CO5150165A1 (es) * 1998-11-13 2002-04-29 Smithkline Beecham Plc Inhibidores de proteasa: tipo catepsina k
US20030144175A1 (en) 1998-12-23 2003-07-31 Smithkline Beecham Corporation Protease inhibitors
WO2001034599A1 (en) 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
AU1474801A (en) 1999-11-10 2001-06-06 Smithkline Beecham Corporation Protease inhibitors
JP2003513972A (ja) 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション プロテアーゼ阻害剤
CN1416346A (zh) 2000-03-21 2003-05-07 史密丝克莱恩比彻姆公司 蛋白酶抑制剂
FR2832405B1 (fr) * 2001-11-19 2004-12-10 Sanofi Synthelabo Tetrahydropyridyl-alkyl-heterocycles azotes, procede pour leur preparation et compositions pharmaceutiques les contenant
US7282512B2 (en) 2002-01-17 2007-10-16 Smithkline Beecham Corporation Cycloalkyl ketoamides derivatives useful as cathepsin K inhibitors
MXPA04010441A (es) 2002-04-23 2005-02-14 Shionogi & Co Derivado de pirazolo[1,5-a]pirimidina e inhibidor de nad(p)h oxidasa que contiene el mismo.
JP2007503401A (ja) * 2003-08-27 2007-02-22 メルク フロスト カナダ リミテツド カテプシン阻害剤
AR050559A1 (es) * 2004-09-07 2006-11-01 Smithkline Beecham Corp Compuesto de diamina aciclica, composicion farmaceutica que lo comprende y su uso para la preparacion de dicha composicion
WO2009128521A1 (ja) * 2008-04-15 2009-10-22 帝人ファーマ株式会社 システインプロテアーゼ阻害剤
CN104311408B (zh) * 2014-09-12 2019-11-08 沈阳化工研究院有限公司 4,4’-二苯醚二甲酸的制备方法
CN111943818B (zh) * 2020-09-16 2023-01-24 天津均凯农业科技有限公司 一种制备4,4′-双三氟甲基二苯醚的方法

Family Cites Families (2)

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Publication number Priority date Publication date Assignee Title
CZ132798A3 (cs) * 1995-10-30 1999-02-17 Smithkline Beecham Corporation Inhibitory proteázy
MA26618A1 (fr) * 1998-04-09 2004-12-20 Smithkline Beecham Corp Composes et compositions pharmaceutiques pour le traitement du paludisme

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EP1067894A4 (en) 2004-09-08
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JP2002515411A (ja) 2002-05-28
AU4092799A (en) 1999-12-06
WO1999059526A2 (en) 1999-11-25
MA26631A1 (fr) 2004-12-20
CO5080801A1 (es) 2001-09-25
US6518267B1 (en) 2003-02-11
DZ2796A1 (fr) 2003-12-01

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