AR018915A1 - INHIBITORS OF DIACIL HYDRAZINIC PROTEASES, PHARMACEUTICAL COMPOSITION THAT INCLUDE IT, USES OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT, A MANUFACTURING MANUFACTURE OF SUCH COMPOUNDS - Google Patents

INHIBITORS OF DIACIL HYDRAZINIC PROTEASES, PHARMACEUTICAL COMPOSITION THAT INCLUDE IT, USES OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT, A MANUFACTURING MANUFACTURE OF SUCH COMPOUNDS

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Publication number
AR018915A1
AR018915A1 ARP990102984A ARP990102984A AR018915A1 AR 018915 A1 AR018915 A1 AR 018915A1 AR P990102984 A ARP990102984 A AR P990102984A AR P990102984 A ARP990102984 A AR P990102984A AR 018915 A1 AR018915 A1 AR 018915A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
het
alkenyl
manufacture
Prior art date
Application number
ARP990102984A
Other languages
Spanish (es)
Original Assignee
Smithkline Beecham Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of AR018915A1 publication Critical patent/AR018915A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P19/08—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Furan Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Inhibidores de proteasas diacil-hidrazínicos, que comprenden un compuesto de formula (I) en la cual: L se selecciona del grupo constituido por: alquiloC2-6, Ar-alquilo C0-6, Het-alquilo C0-6, CH(R4)NR5R6, CH(R4)Ar, CH(R4)OAr, y NR4R7; X, Y, Z se seleccionan independientemente del grupo constituido por: N, O,S y CR10, con la condicion de que al menos dos de X, Y y Z son heteroátomos y al menos unode X, Y y Z es N, o uno de X, Y y Z es C=N, C=C o N=N y los otros dosson CR10 o N, con la condicion de que X, Y y Z juntos comprenden al menos dos N; --indica un enlace simple o doble en el heterociclo de cinco miembros; R, R1,R2, R5, R10 R12, R16 y R17 se seleccionan independientemente del grupo constituido por: H, alquilo, C1-6, alquenilo C2-6, Ar-alquilo C0-6; y Het-alquilo C0-6;R3 se selecciona del grupo constituido por: alquilo C3-6, Ar, Het, CH(R11)Ar, CH(R11)OAr, NR12R12, CH(R11) NR12R13; y formula II, R4, R11 y R15 se seleccionanindependientemente del grupo constituido por: H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquil C3-11-alquilo C0-6, Ar-alquilo C0-6, Ar-alqueniloC2-6, Ar-alquinilo C2-6, Het-alquilo C0-6, Het-alquenilo C2-6, Het-alquinilo C2-6, alquilo C1-6, sustituido opcionalmente con OR8, SR8, NR8R9, N(R)CO2RMCI2R, CONR10R11, y N(C=NH)NH2; R6 y R13 se seleccionan independientemente del grupo constituido por: R14, R14C(O), R14C(S), R14OC(O), Y r14OC-(O)NR9CH(R15)(O); R7se selecciona del grupo constituido por: alquilo C1-6, alquenilo C1-6, cicloalquil C3-6-alquilo C0-6, Ar-alquilo C0-6, y Het-alquilo C0-6; R4 y R7 puedencombinarse para formar un anillo carbocíclico o heterocíclico monocíclico de 3-7 miembros o bicíclico de 7-10 miembros, sustituido opcionalmente con 1-4 dealquilo C1-6, Ar-alquilo C0-6, Het-alquilo C0-6, alcoxi C1-6, Ar-alcoxi C0-6, Het-alcoxi C0-6. OH, (CH2)1-6NR8R9, O(CH2)1-6NR8R9; R8 y R9 se seleccionanindependientemente del grupo constituido por: H, alquilo C1-6, alquenilo C2-6, Ar-alquilo C0-6, Het-alquilo C0-6, y R16R17-alquilo C2-6; R14 se seleccionadel grupo consitutuido por: alquilo C1-6, alquenilo C2-6, Ar-alquilo C0-6, y Het-alquilo C0-6; y sus sales, hidratos y solvatos farmacéuticamente aceptables,Diacyl hydrazine protease inhibitors, comprising a compound of formula (I) in which: L is selected from the group consisting of: C2-6 alkyl, Ar-C0-6 alkyl, Het-C0-6 alkyl, CH (R4) NR5R6, CH (R4) Ar, CH (R4) OAr, and NR4R7; X, Y, Z are independently selected from the group consisting of: N, O, S and CR10, with the proviso that at least two of X, Y and Z are heteroatoms and at least one of X, Y and Z is N, or one of X, Y and Z is C = N, C = C or N = N and the other two are CR10 or N, with the proviso that X, Y and Z together comprise at least two N; - indicates a single or double bond in the five-member heterocycle; R, R1, R2, R5, R10 R12, R16 and R17 are independently selected from the group consisting of: H, alkyl, C1-6, C2-6 alkenyl, Ar-C0-6 alkyl; and Het-C0-6 alkyl; R3 is selected from the group consisting of: C3-6 alkyl, Ar, Het, CH (R11) Ar, CH (R11) OAr, NR12R12, CH (R11) NR12R13; and formula II, R4, R11 and R15 are independently selected from the group consisting of: H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-11 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, C2-6 ar-alkenyl, C2-6 alkynyl, H0-6 alkyl, C2-6 alkynyl, C2-6 alkynyl, C1-6 alkyl, optionally substituted with OR8, SR8, NR8R9, N ( R) CO2RMCI2R, CONR10R11, and N (C = NH) NH2; R6 and R13 are independently selected from the group consisting of: R14, R14C (O), R14C (S), R14OC (O), and r14OC- (O) NR9CH (R15) (O); R7 is selected from the group consisting of: C1-6 alkyl, C1-6 alkenyl, C3-6 cycloalkyl-C0-6 alkyl, Ar-C0-6 alkyl, and Het-C0-6 alkyl; R4 and R7 can be combined to form a 3-7 membered monocyclic carbocyclic or heterocyclic ring or 7-10 membered bicyclic, optionally substituted with 1-4 C1-6 alkyl, Ar-C0-6 alkyl, Het-C0-6 alkyl, C1-6 alkoxy, Ar-C0-6 alkoxy, Het-C0-6 alkoxy. OH, (CH2) 1-6NR8R9, O (CH2) 1-6NR8R9; R8 and R9 are independently selected from the group consisting of: H, C1-6 alkyl, C2-6 alkenyl, Ar-C0-6 alkyl, Het-C0-6 alkyl, and R16R17-C2-6 alkyl; R14 is selected from the group consisting of: C1-6 alkyl, C2-6 alkenyl, Ar-C0-6 alkyl, and Het-C0-6 alkyl; and its pharmaceutically acceptable salts, hydrates and solvates,

ARP990102984A 1998-06-24 1999-06-22 INHIBITORS OF DIACIL HYDRAZINIC PROTEASES, PHARMACEUTICAL COMPOSITION THAT INCLUDE IT, USES OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT, A MANUFACTURING MANUFACTURE OF SUCH COMPOUNDS AR018915A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US9049398P 1998-06-24 1998-06-24

Publications (1)

Publication Number Publication Date
AR018915A1 true AR018915A1 (en) 2001-12-12

Family

ID=22223011

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP990102984A AR018915A1 (en) 1998-06-24 1999-06-22 INHIBITORS OF DIACIL HYDRAZINIC PROTEASES, PHARMACEUTICAL COMPOSITION THAT INCLUDE IT, USES OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT, A MANUFACTURING MANUFACTURE OF SUCH COMPOUNDS

Country Status (6)

Country Link
EP (1) EP1093367A4 (en)
JP (1) JP2002518444A (en)
AR (1) AR018915A1 (en)
AU (1) AU4723799A (en)
CA (1) CA2335876A1 (en)
WO (1) WO1999066925A1 (en)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030144175A1 (en) 1998-12-23 2003-07-31 Smithkline Beecham Corporation Protease inhibitors
JP2003513972A (en) 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 Protease inhibitor
AU1588901A (en) 1999-11-10 2001-06-06 Smithkline Beecham Corporation Protease inhibitors
JP2003513924A (en) 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 Protease inhibitor
SK13632002A3 (en) 2000-03-21 2003-02-04 Smithkline Beecham Corporation C1-6-alkyl-4-amino-azepan-3-one compounds, process for the preparation thereof, pharmaceutical composition comprising the same and intermediates
WO2003062192A1 (en) 2002-01-17 2003-07-31 Smithkline Beecham Corporation Cycloalkyl ketoamides derivatives useful as cathepsin k inhibitors
US7176310B1 (en) 2002-04-09 2007-02-13 Ucb Sa Pyrimidinecarboxamide derivatives and their use as anti-inflammatory agents
US6933308B2 (en) 2002-12-20 2005-08-23 Bristol-Myers Squibb Company Aminoalkyl thiazole derivatives as KCNQ modulators
US7273866B2 (en) 2002-12-20 2007-09-25 Bristol-Myers Squibb Company 2-aryl thiazole derivatives as KCNQ modulators
TWI359017B (en) * 2003-11-10 2012-03-01 Synta Pharmaceuticals Corp Heteroaryl-hydrazone compounds
MY147780A (en) * 2006-12-29 2013-01-31 Abbvie Deutschland Carboxamide compounds and their use as calpain inhibitors
TWI453019B (en) * 2007-12-28 2014-09-21 Abbvie Deutschland Carboxamide compounds
CN102408387A (en) * 2010-09-26 2012-04-11 韩南银 Metal complex with antitumor action
WO2014031784A1 (en) * 2012-08-23 2014-02-27 Alios Biopharma, Inc. Compounds for the treatment of paramoxyvirus viral infections
CN103113300A (en) * 2013-03-06 2013-05-22 广西中医药大学 Preparation method and application of compound with antitumor activity
WO2014179943A1 (en) * 2013-05-08 2014-11-13 Yang Yongliang Maleic amide compound, preparation method therefor and application thereof
CN103242321A (en) * 2013-05-21 2013-08-14 苏州科捷生物医药有限公司 Benzylpiperazine compound and anti-tumor application thereof
AU2014308991B2 (en) 2013-08-21 2019-02-14 Janssen Biopharma, Inc. Antiviral compounds
CN103880703B (en) * 2014-03-14 2016-04-13 浙江工业大学 O-cinnyl-fluorobenzene salicylamide compound and the application in the anti-human placental villi cancer drug of preparation thereof
CN103880701B (en) * 2014-03-14 2016-04-13 浙江工业大学 O-cinnyl-fluorobenzene salicylamide compound and the application in the anti-human uterine neck squamous cell carcinoma medicine of preparation thereof
CN103880702B (en) * 2014-03-14 2016-04-13 浙江工业大学 O-cinnyl-fluorobenzene salicylamide compound and preparing the application in anti-leukemia medicine
MA41614A (en) 2015-02-25 2018-01-02 Alios Biopharma Inc ANTIVIRAL COMPOUNDS

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SK56798A3 (en) * 1995-10-30 1998-12-02 Smithkline Beecham Corp Protease inhibitors, pharmaceutical composition containing them and their use

Also Published As

Publication number Publication date
JP2002518444A (en) 2002-06-25
WO1999066925A1 (en) 1999-12-29
EP1093367A1 (en) 2001-04-25
EP1093367A4 (en) 2003-03-05
AU4723799A (en) 2000-01-10
CA2335876A1 (en) 1999-12-29

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