NO324066B1 - Multikatalytiske proteaseinhibitorer, farmasoytiske sammensetninger omfattende disse og deres anvendelse - Google Patents

Multikatalytiske proteaseinhibitorer, farmasoytiske sammensetninger omfattende disse og deres anvendelse Download PDF

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Publication number
NO324066B1
NO324066B1 NO19972104A NO972104A NO324066B1 NO 324066 B1 NO324066 B1 NO 324066B1 NO 19972104 A NO19972104 A NO 19972104A NO 972104 A NO972104 A NO 972104A NO 324066 B1 NO324066 B1 NO 324066B1
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NO
Norway
Prior art keywords
mmol
group
compound
mcp
arginyl
Prior art date
Application number
NO19972104A
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English (en)
Norwegian (no)
Other versions
NO972104L (no
NO972104D0 (no
Inventor
James C Kauer
Robert Siman
Mohamed Iqbal
James Diebold
Sankar Chatterjee
Original Assignee
Cephalon Inc
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
Priority claimed from US08/337,795 external-priority patent/US5550262A/en
Application filed by Cephalon Inc filed Critical Cephalon Inc
Publication of NO972104D0 publication Critical patent/NO972104D0/no
Publication of NO972104L publication Critical patent/NO972104L/no
Publication of NO324066B1 publication Critical patent/NO324066B1/no

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/275—Nitriles; Isonitriles
    • A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035—Isoindoles, e.g. phthalimide
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/30—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to nitro or nitroso groups
    • C07C279/32—N-nitroguanidines
    • C07C279/36—Substituted N-nitroguanidines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/09—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton the carbon skeleton being further substituted by at least two halogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
    • C07C311/47—Y being a hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • C07C311/50—Compounds containing any of the groups, X being a hetero atom, Y being any atom
    • C07C311/52—Y being a hetero atom
    • C07C311/64—X and Y being nitrogen atoms, e.g. N-sulfonylguanidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C337/00—Derivatives of thiocarbonic acids containing functional groups covered by groups C07C333/00 or C07C335/00 in which at least one nitrogen atom of these functional groups is further bound to another nitrogen atom not being part of a nitro or nitroso group
    • C07C337/06—Compounds containing any of the groups, e.g. thiosemicarbazides
    • C07C337/08—Compounds containing any of the groups, e.g. thiosemicarbazides the other nitrogen atom being further doubly-bound to a carbon atom, e.g. thiosemicarbazones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
    • C07D311/70—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4 with two hydrocarbon radicals attached in position 2 and elements other than carbon and hydrogen in position 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07K5/06086—Dipeptides with the first amino acid being basic
    • C07K5/06095—Arg-amino acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated

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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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Emergency Medicine (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrane Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Macromonomer-Based Addition Polymer (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
NO19972104A 1994-11-14 1997-05-07 Multikatalytiske proteaseinhibitorer, farmasoytiske sammensetninger omfattende disse og deres anvendelse NO324066B1 (no)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US08/337,795 US5550262A (en) 1994-11-14 1994-11-14 Multicatalytic protease inhibitors
US46439895A 1995-06-05 1995-06-05
US08/552,794 US5614649A (en) 1994-11-14 1995-11-03 Multicatalytic protease inhibitors
PCT/US1995/014921 WO1996014857A1 (en) 1994-11-14 1995-11-14 Multicatalytic protease inhibitors

Publications (3)

Publication Number Publication Date
NO972104D0 NO972104D0 (no) 1997-05-07
NO972104L NO972104L (no) 1997-06-13
NO324066B1 true NO324066B1 (no) 2007-08-06

Family

ID=27407222

Family Applications (1)

Application Number Title Priority Date Filing Date
NO19972104A NO324066B1 (no) 1994-11-14 1997-05-07 Multikatalytiske proteaseinhibitorer, farmasoytiske sammensetninger omfattende disse og deres anvendelse

Country Status (18)

Country Link
US (3) US5614649A (ja)
EP (1) EP0789578B1 (ja)
JP (2) JP3056258B2 (ja)
KR (1) KR100420774B1 (ja)
CN (1) CN1166403C (ja)
AT (1) ATE241998T1 (ja)
BR (1) BR9509665A (ja)
CA (1) CA2202760A1 (ja)
DE (1) DE69530993T2 (ja)
DK (1) DK0789578T3 (ja)
ES (1) ES2200010T3 (ja)
FI (1) FI118325B (ja)
HK (1) HK1004638A1 (ja)
MX (1) MX9703564A (ja)
NO (1) NO324066B1 (ja)
NZ (1) NZ296479A (ja)
PT (1) PT789578E (ja)
WO (1) WO1996014857A1 (ja)

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ATE230275T1 (de) 1995-10-25 2003-01-15 Senju Pharma Co Angiogense-inhibitor
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EP1006798A4 (en) 1996-09-05 2003-03-05 Massachusetts Inst Technology COMPOSITIONS AND METHODS FOR TREATING NEUROLOGICAL DISORDERS AND NEURODEGENERATIVE DISEASES
US5939581A (en) * 1997-08-20 1999-08-17 First Chemical Corporation Processes for preparing hydrocinnamic acid
US6096778A (en) * 1997-10-07 2000-08-01 Cephalon, Inc. α-ketoamide multicatalytic protease inhibitors
US6150378A (en) 1997-10-07 2000-11-21 Cephalon, Inc. Peptidyl-containing α-ketoamide cysteine and serine protease inhibitors
US6083944A (en) * 1997-10-07 2000-07-04 Cephalon, Inc. Quinoline-containing α-ketoamide cysteine and serine protease inhibitors
GB9723407D0 (en) * 1997-11-05 1998-01-07 Ciba Geigy Ag Organic compounds
US20010012854A1 (en) * 1997-12-16 2001-08-09 Robert Siman Multicatalytic protease inhibitors for use as anti-tumor agents
US6803357B1 (en) 1998-02-02 2004-10-12 New England Medical Center Hospitals, Inc. Method of regulating glucose metabolism, and reagents related thereto
US6096711A (en) * 1998-02-25 2000-08-01 Sherman; Michael Hsp72 induction and applications
WO2000023614A1 (en) 1998-10-20 2000-04-27 Millennium Pharmaceuticals, Inc. Method for monitoring proteasome inhibitor drug action
US20030054977A1 (en) * 1999-10-12 2003-03-20 Cell Therapeutics, Inc. Manufacture of polyglutamate-therapeutic agent conjugates
US6358928B1 (en) 1999-11-22 2002-03-19 Enzyme Systems Products Peptidyl sulfonyl imidazolides as selective inhibitors of serine proteases
GB0003111D0 (en) * 2000-02-10 2000-03-29 Novartis Ag Organic compounds
DK1355910T3 (da) * 2001-01-25 2011-06-27 Us Of America Represented By The Secretary Dept Of Health And Human Services Formulering af borsyreforbindelser
JP4416501B2 (ja) 2001-05-30 2010-02-17 ノバルティス アクチエンゲゼルシャフト ２−｛［ｎ−（２−アミノ−３−（ヘテロアリールまたはアリール）プロピオニル）−アミノアシル］−アミノ｝−アルキルボロン酸誘導体
CA2466870A1 (en) 2001-11-26 2003-06-05 Trustees Of Tufts College Methods for treating autoimmune disorders, and reagents related thereto
EP1469873A4 (en) 2001-11-26 2007-10-03 Tufts College PEPTIDOMIMETIC INHIBITORS OF POST-PROLINE CLEAVAGE ENZYMES
US7223745B2 (en) * 2003-08-14 2007-05-29 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7576206B2 (en) * 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7468383B2 (en) * 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
FR2914920B1 (fr) 2007-04-11 2011-09-09 Clariant Specialty Fine Chem F Procede de deacetalisation d'alpha-aminoacetals.
EP3434259A1 (en) * 2007-05-04 2019-01-30 Marina Biotech, Inc. Amino acid lipids and uses thereof
FR2916441B1 (fr) 2007-05-22 2009-08-28 Clariant Specialty Fine Chem Procede de racemisation d'alpha-aminoacetals optiquement actifs.
US7442830B1 (en) 2007-08-06 2008-10-28 Millenium Pharmaceuticals, Inc. Proteasome inhibitors
FR2927900B1 (fr) 2008-02-27 2010-09-17 Clariant Specialty Fine Chem Procede de preparation d'alpha-aminoacetals optiquement actifs.
EP2733147A1 (en) 2008-06-17 2014-05-21 Millennium Pharmaceuticals, Inc. Boronate ester compounds and pharmaceutical compositions thereof
AU2009282117B2 (en) * 2008-08-11 2016-05-12 Banyan Biomarkers, Inc. Biomarker detection process and assay of neurological condition
AR075090A1 (es) 2008-09-29 2011-03-09 Millennium Pharm Inc Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden.
MX2012003770A (es) 2009-09-30 2012-08-03 Harvard College Metodos para la modulacion de autofagia a traves de la modulacion de productos de genes que aumentan la autofagia.
CA2785300A1 (en) 2009-12-22 2011-07-21 Cephalon, Inc. Proteasome inhibitors and processes for their preparation, purification and use
US8354548B2 (en) * 2010-02-19 2013-01-15 Bristol-Myers Squibb Company Glycine chroman-6-sulfonamides for use as inhibitors of diacylglycerol lipase
KR20130036228A (ko) 2010-03-31 2013-04-11 밀레니엄 파머슈티컬스 인코퍼레이티드 1-아미노-2-사이클로프로필에틸보론산의 유도체
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Publication number Publication date
FI118325B (fi) 2007-10-15
AU710437B2 (en) 1999-09-23
MX9703564A (es) 1997-08-30
CN1166403C (zh) 2004-09-15
FI972029A0 (fi) 1997-05-13
US5614649A (en) 1997-03-25
BR9509665A (pt) 1997-10-28
HK1004638A1 (en) 1998-11-13
US5990083A (en) 1999-11-23
US5830870A (en) 1998-11-03
NO972104L (no) 1997-06-13
DE69530993D1 (de) 2003-07-10
JP2000290197A (ja) 2000-10-17
PT789578E (pt) 2003-10-31
KR100420774B1 (ko) 2004-07-05
DE69530993T2 (de) 2004-05-19
WO1996014857A1 (en) 1996-05-23
ES2200010T3 (es) 2004-03-01
AU4110496A (en) 1996-06-06
CA2202760A1 (en) 1996-05-23
DK0789578T3 (da) 2003-09-22
NZ296479A (en) 1999-06-29
EP0789578A1 (en) 1997-08-20
ATE241998T1 (de) 2003-06-15
EP0789578B1 (en) 2003-06-04
EP0789578A4 (en) 2000-09-20
JPH10507465A (ja) 1998-07-21
FI972029A (fi) 1997-05-13
CN1164192A (zh) 1997-11-05
JP3056258B2 (ja) 2000-06-26
NO972104D0 (no) 1997-05-07

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