IL115790A - Esters of boronic acid and pharmaceutical preparations containing them - Google Patents

Esters of boronic acid and pharmaceutical preparations containing them

Info

Publication number
IL115790A
IL115790A IL11579095A IL11579095A IL115790A IL 115790 A IL115790 A IL 115790A IL 11579095 A IL11579095 A IL 11579095A IL 11579095 A IL11579095 A IL 11579095A IL 115790 A IL115790 A IL 115790A
Authority
IL
Israel
Prior art keywords
compound
boronic
mmol
leu
independently
Prior art date
Application number
IL11579095A
Other languages
English (en)
Hebrew (he)
Other versions
IL115790A0 (en
Original Assignee
Millenium Pharmaceuticals 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26987313&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=IL115790(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Millenium Pharmaceuticals Inc filed Critical Millenium Pharmaceuticals Inc
Priority to IL13383195A priority Critical patent/IL133831A/en
Priority to IL13772695A priority patent/IL137726A/en
Publication of IL115790A0 publication Critical patent/IL115790A0/xx
Priority to IL13383199A priority patent/IL133831A0/xx
Priority to IL13772600A priority patent/IL137726A0/xx
Publication of IL115790A publication Critical patent/IL115790A/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/26Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/04Heterocyclic 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
    • C07D295/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/04Esters of boric acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043Leu-amino acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06191Dipeptides containing heteroatoms different from O, S, or N
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0827Tripeptides containing heteroatoms different from O, S, or N
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Transplantation (AREA)
  • AIDS & HIV (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
IL11579095A 1994-10-28 1995-10-27 Esters of boronic acid and pharmaceutical preparations containing them IL115790A (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
IL13383195A IL133831A (en) 1994-10-28 1995-10-27 Pharmaceutical preparations containing protease inhibitors
IL13772695A IL137726A (en) 1994-10-28 1995-10-27 Aster and boric acid compounds
IL13383199A IL133831A0 (en) 1994-10-28 1999-12-30 Pharmaceutical compositions containing proteasome inhibitors
IL13772600A IL137726A0 (en) 1994-10-28 2000-08-07 Bronic ester and acid compounds

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US33052594A 1994-10-28 1994-10-28
US08/442,581 US6083903A (en) 1994-10-28 1995-05-16 Boronic ester and acid compounds, synthesis and uses

Publications (2)

Publication Number Publication Date
IL115790A0 IL115790A0 (en) 1996-01-19
IL115790A true IL115790A (en) 2002-12-01

Family

ID=26987313

Family Applications (5)

Application Number Title Priority Date Filing Date
IL11579095A IL115790A (en) 1994-10-28 1995-10-27 Esters of boronic acid and pharmaceutical preparations containing them
IL13383195A IL133831A (en) 1994-10-28 1995-10-27 Pharmaceutical preparations containing protease inhibitors
IL13772695A IL137726A (en) 1994-10-28 1995-10-27 Aster and boric acid compounds
IL13383199A IL133831A0 (en) 1994-10-28 1999-12-30 Pharmaceutical compositions containing proteasome inhibitors
IL13772600A IL137726A0 (en) 1994-10-28 2000-08-07 Bronic ester and acid compounds

Family Applications After (4)

Application Number Title Priority Date Filing Date
IL13383195A IL133831A (en) 1994-10-28 1995-10-27 Pharmaceutical preparations containing protease inhibitors
IL13772695A IL137726A (en) 1994-10-28 1995-10-27 Aster and boric acid compounds
IL13383199A IL133831A0 (en) 1994-10-28 1999-12-30 Pharmaceutical compositions containing proteasome inhibitors
IL13772600A IL137726A0 (en) 1994-10-28 2000-08-07 Bronic ester and acid compounds

Country Status (25)

Country Link
US (16) US6083903A (de)
EP (4) EP1312609B1 (de)
JP (1) JP3717934B2 (de)
KR (1) KR100398944B1 (de)
CN (2) CN1305475C (de)
AT (3) ATE411324T1 (de)
AU (1) AU710564B2 (de)
CA (2) CA2496538C (de)
CH (1) CH0788360H1 (de)
CY (1) CY2484B1 (de)
DE (5) DE122004000025I2 (de)
DK (3) DK0788360T5 (de)
ES (3) ES2314540T3 (de)
FI (2) FI114801B (de)
FR (1) FR04C0014I2 (de)
HK (2) HK1002059A1 (de)
IL (5) IL115790A (de)
LU (1) LU91083I2 (de)
MX (1) MX9703063A (de)
NL (1) NL300151I2 (de)
NO (2) NO310558B1 (de)
NZ (2) NZ296717A (de)
PT (3) PT1312609E (de)
TW (1) TW318850B (de)
WO (1) WO1996013266A1 (de)

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JP2001511814A (ja) * 1997-02-15 2001-08-14 プロスクリプト・インコーポレイテッド NF−κBの阻害を介する梗塞の治療
US6221888B1 (en) * 1997-05-29 2001-04-24 Merck & Co., Inc. Sulfonamides as cell adhesion inhibitors
JP2001517631A (ja) * 1997-09-25 2001-10-09 ミレニアム・ファーマシューティカルズ・インコーポレイテッド 炎症疾患および自己免疫疾患を治療するためのプロテアソーム阻害剤、ユビキチン経路阻害剤、またはユビキチンプロテアソーム経路を介したNF−κBの活性化に干渉する剤
KR100458403B1 (ko) * 1997-09-29 2004-11-26 포인트 써러퓨틱스, 인크. 생체외 조혈세포의 자극방법
US6831057B2 (en) * 1997-10-28 2004-12-14 The University Of North Carolina At Chapel Hill Use of NF-κB inhibition in combination therapy for cancer
CA2219867A1 (en) * 1997-10-31 1999-04-30 Jiangping Wu The use of proteasome inhibitors for treating cancer, inflammation, autoimmune disease, graft rejection and septic shock
DE19802450A1 (de) * 1998-01-23 1999-07-29 Hoechst Marion Roussel De Gmbh Ustilipide, Verfahren zu deren Herstellung sowie deren Verwendung
US6075150A (en) * 1998-01-26 2000-06-13 Cv Therapeutics, Inc. α-ketoamide inhibitors of 20S proteasome
US6617171B2 (en) * 1998-02-27 2003-09-09 The General Hospital Corporation Methods for diagnosing and treating autoimmune disease
FR2779653B1 (fr) * 1998-06-11 2002-12-20 Inst Nat Sante Rech Med Utilisation de composes modulateurs du proteasome en therapie
US6902721B1 (en) 1998-07-10 2005-06-07 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6462019B1 (en) 1998-07-10 2002-10-08 Osteoscreen, Inc. Inhibitors of proteasomal activity and production for stimulating bone growth
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US6979697B1 (en) * 1998-08-21 2005-12-27 Point Therapeutics, Inc. Regulation of substrate activity
EP0982317A1 (de) * 1998-08-26 2000-03-01 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Bivalente Proteasome Inhibitore
WO2000023614A1 (en) * 1998-10-20 2000-04-27 Millennium Pharmaceuticals, Inc. Method for monitoring proteasome inhibitor drug action
US6492333B1 (en) * 1999-04-09 2002-12-10 Osteoscreen, Inc. Treatment of myeloma bone disease with proteasomal and NF-κB activity inhibitors
US6890904B1 (en) * 1999-05-25 2005-05-10 Point Therapeutics, Inc. Anti-tumor agents
US6649593B1 (en) * 1999-10-13 2003-11-18 Tularik Inc. Modulators of SREBP processing
AU2001287399A1 (en) * 2000-08-16 2002-02-25 University Of Alberta Non-pressurized methods for the preparation of conjugated solid supports for boronic acids
US6919382B2 (en) 2000-08-31 2005-07-19 The Governors Of The University Of Alberta Preparation and uses of conjugated solid supports for boronic acids
ATE338564T1 (de) * 2000-10-12 2006-09-15 Viromics Gmbh Proteasome inhibitoren zur behandlung von hepatitis-virus infektionen
DK1355910T3 (da) 2001-01-25 2011-06-27 Us Of America Represented By The Secretary Dept Of Health And Human Services Formulering af borsyreforbindelser
US7112588B2 (en) * 2001-05-21 2006-09-26 Alcon, Inc. Use of proteasome inhibitors to treat dry eye disorders
DE60218153T2 (de) 2001-05-21 2007-06-28 Alcon Inc. Verwendung von proteasom-inhibitoren zur behandlung des trockenen auges
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
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