WO2001052892A3 - Jak/stat pathway inhibitors and the uses thereof - Google Patents

Jak/stat pathway inhibitors and the uses thereof Download PDF

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Publication number
WO2001052892A3
WO2001052892A3 PCT/US2001/002033 US0102033W WO0152892A3 WO 2001052892 A3 WO2001052892 A3 WO 2001052892A3 US 0102033 W US0102033 W US 0102033W WO 0152892 A3 WO0152892 A3 WO 0152892A3
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WO
WIPO (PCT)
Prior art keywords
jak
jak3
downregulate
therapeutics
steady state
Prior art date
Application number
PCT/US2001/002033
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French (fr)
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WO2001052892A2 (en
Inventor
George Vasios
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Genzyme 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.)
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Publication date
Application filed by Genzyme Corp filed Critical Genzyme Corp
Priority to CA002397774A priority Critical patent/CA2397774A1/en
Priority to IL15076301A priority patent/IL150763A0/en
Priority to DE60129926T priority patent/DE60129926T2/en
Priority to EP01942563A priority patent/EP1250137B1/en
Priority to JP2001552939A priority patent/JP5512909B2/en
Priority to AU29687/01A priority patent/AU2968701A/en
Publication of WO2001052892A2 publication Critical patent/WO2001052892A2/en
Publication of WO2001052892A3 publication Critical patent/WO2001052892A3/en
Priority to IL150763A priority patent/IL150763A/en

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    • 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
    • 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
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • 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
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    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
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  • Veterinary Medicine (AREA)
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  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Immunology (AREA)
  • Pulmonology (AREA)
  • Zoology (AREA)
  • Marine Sciences & Fisheries (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicinal Preparation (AREA)

Abstract

The role of JAK/STAT signal transduction pathway cellular mechanisms that lead to the onset and progression of degenerative joint diseases or disorders such as osteoarthritis (OA) is disclosed. Certain known effective OA therapeutics such as hymenialdisine, debromohymenialdisine, and its variants and derivatives are shown to function as JAK3-specific inhibitors, which downregulate steady state mRNA levels of key cellular components involved in cartilage degradation. Another JAK3-specific inhibitor, not previously known as an OA therapeutic, is shown to downregulate steady state mRNA levels of various cellular components involved in cartilage degradation in a manner identical to that of the known OA therapeutics.
PCT/US2001/002033 2000-01-24 2001-01-22 Jak/stat pathway inhibitors and the uses thereof WO2001052892A2 (en)

Priority Applications (7)

Application Number Priority Date Filing Date Title
CA002397774A CA2397774A1 (en) 2000-01-24 2001-01-22 Jak/stat pathway inhibitors and the uses thereof
IL15076301A IL150763A0 (en) 2000-01-24 2001-01-22 Jak/stat inhibitors and pharmaceutical compositions containing the same
DE60129926T DE60129926T2 (en) 2000-01-24 2001-01-22 INHIBITORS OF THE JAK / STAT PATH AND ITS USE IN TREATING GENERAL PRIMARY OSTEOARTHRITIS
EP01942563A EP1250137B1 (en) 2000-01-24 2001-01-22 Jak/stat pathway inhibitors and the use thereof for the treatment of primary generalized osteoarthritis
JP2001552939A JP5512909B2 (en) 2000-01-24 2001-01-22 JAK / STAT pathway inhibitors and uses thereof
AU29687/01A AU2968701A (en) 2000-01-24 2001-01-22 Jak/stat pathway inhibitors and the uses thereof
IL150763A IL150763A (en) 2000-01-24 2002-07-16 Jak/stat inhibitors and pharmaceutical compositions containing the same

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US17787200P 2000-01-24 2000-01-24
US60/177,872 2000-01-24
US72349000A 2000-11-28 2000-11-28
US09/723,490 2000-11-28

Publications (2)

Publication Number Publication Date
WO2001052892A2 WO2001052892A2 (en) 2001-07-26
WO2001052892A3 true WO2001052892A3 (en) 2002-01-24

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/002033 WO2001052892A2 (en) 2000-01-24 2001-01-22 Jak/stat pathway inhibitors and the uses thereof

Country Status (11)

Country Link
US (2) US20040209799A1 (en)
EP (1) EP1250137B1 (en)
JP (2) JP5512909B2 (en)
AT (1) ATE369844T1 (en)
AU (1) AU2968701A (en)
CA (1) CA2397774A1 (en)
DE (1) DE60129926T2 (en)
ES (1) ES2452696T3 (en)
IL (2) IL150763A0 (en)
PT (1) PT1782800E (en)
WO (1) WO2001052892A2 (en)

Cited By (1)

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US9248190B2 (en) 2005-06-08 2016-02-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway

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WO2001052892A2 (en) * 2000-01-24 2001-07-26 Genzyme Corporation Jak/stat pathway inhibitors and the uses thereof
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
US20040175384A1 (en) * 2003-12-12 2004-09-09 Mohapatra Shyam S. Protein kinase C as a target for the treatment of respiratory syncytial virus
KR101201603B1 (en) 2003-07-30 2012-11-14 리겔 파마슈티칼스, 인크. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
US8592368B2 (en) * 2003-12-19 2013-11-26 University Of South Florida JAK/STAT inhibitors and MAPK/ERK inhibitors for RSV infection
EP1704145B1 (en) * 2004-01-12 2012-06-13 YM BioSciences Australia Pty Ltd Selective kinase inhibitors
AU2005233582B2 (en) * 2004-04-12 2009-01-29 Sanbio, Inc. Cells exhibiting neuronal progenitor cell characteristics
WO2005102332A1 (en) * 2004-04-27 2005-11-03 Santen Pharmaceutical Co., Ltd. Therapeutic agent for arthrosis deformans
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
EP1734118A1 (en) * 2005-06-15 2006-12-20 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts Identification of JAK/STAT pathway modulating genes by genome wide RNAi screening
US8962643B2 (en) 2006-02-24 2015-02-24 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
CA2650140A1 (en) 2006-04-14 2007-10-25 Mriganka Sur Identifying and modulating molecular pathways that mediate nervous system plasticity
JP2009544750A (en) * 2006-07-28 2009-12-17 ザ ユニヴァーシティ コート オブ ザ ユニヴァーシティ オブ エディンバラ Treatment
CN102007124B (en) 2008-02-15 2014-06-18 里格尔制药公司 Pyrimidine-2-amine compounds and their use as inhibitors of jak kinases
US8063058B2 (en) 2008-04-16 2011-11-22 Portola Pharmaceuticals, Inc. Inhibitors of syk and JAK protein kinases
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
US8258144B2 (en) 2008-04-22 2012-09-04 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
TW201300360A (en) 2010-11-01 2013-01-01 Portola Pharm Inc Nicotinamides as JAK kinase modulators
US20140112913A1 (en) * 2011-02-10 2014-04-24 Genqual Corporation Methods of prognosing and administering treatment for inflammatory disorders
BR112014012396B1 (en) 2011-11-23 2020-08-25 Portola Pharmaceuticals, Inc pyrazine kinase inhibitors, composition, in vitro method for inhibiting kinase syk or signal transduction pathway, use of said inhibitors and kit
JP2015505669A (en) * 2011-11-25 2015-02-26 シンガポール ヘルス サービシーズ ピーティーイー リミテッド Natural killer / T cell lymphoma (NKTCL) sensitivity prediction, diagnosis and treatment
EP2903970A4 (en) 2012-10-08 2016-11-30 Portola Pharm Inc Substituted pyrimidinyl kinase inhibitors
KR101632111B1 (en) * 2014-07-30 2016-06-20 원광대학교산학협력단 Composition for preventing and treating osteoporosis
US20220143049A1 (en) 2019-03-21 2022-05-12 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
JP2023500906A (en) 2019-11-08 2023-01-11 インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） Methods of treating cancers with acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use

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Cited By (1)

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Publication number Priority date Publication date Assignee Title
US9248190B2 (en) 2005-06-08 2016-02-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway

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