NO991677L - Aspartate ester inhibitors for interleukin 1- <beta> conversion enzyme - Google Patents

Aspartate ester inhibitors for interleukin 1- <beta> conversion enzyme

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Publication number
NO991677L
NO991677L NO991677A NO991677A NO991677L NO 991677 L NO991677 L NO 991677L NO 991677 A NO991677 A NO 991677A NO 991677 A NO991677 A NO 991677A NO 991677 L NO991677 L NO 991677L
Authority
NO
Norway
Prior art keywords
interleukin
beta
conversion enzyme
aspartate ester
ester inhibitors
Prior art date
Application number
NO991677A
Other languages
Norwegian (no)
Other versions
NO991677D0 (en
Inventor
Hans-Peter Albrecht
Hamish John Allen
Kenneth Dale Brady
Bradley William Caprathe
John Lodge Gilmore
William Glen Harter
Sheryl Jeanne Hays
Catherine Rose Kostlan
Elizabeth Ann Lunney
Kimberly Suzanne Para
Anthony Jerome Thomas
Nigel Walker
Original Assignee
Warner Lambert Co
Basf Ag
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 Warner Lambert Co, Basf Ag filed Critical Warner Lambert Co
Publication of NO991677D0 publication Critical patent/NO991677D0/en
Publication of NO991677L publication Critical patent/NO991677L/en

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    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
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    • C07D333/24—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • 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
    • C07K5/0202—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-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • C07C2601/10—Systems containing only non-condensed rings with a five-membered ring the ring being unsaturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/36—Systems containing two condensed rings the rings having more than two atoms in common
    • C07C2602/42—Systems containing two condensed rings the rings having more than two atoms in common the bicyclo ring system containing seven carbon atoms

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NO991677A 1996-10-11 1999-04-09 Aspartate ester inhibitors for interleukin 1- <beta> conversion enzyme NO991677L (en)

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US2832296P 1996-10-11 1996-10-11
PCT/US1997/018514 WO1998016502A1 (en) 1996-10-11 1997-10-09 ASPARTATE ESTER INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME

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Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2214037T3 (en) 1998-07-08 2004-09-01 Harbor Branch Oceanographic Institution, Inc. ALCALOID COMPOUNDS OF AMINOIMIQUINONE AND AMINOQUININE AS CASPASA INHIBITORS.
US6339101B1 (en) * 1998-08-14 2002-01-15 Gpi Nil Holdings, Inc. N-linked sulfonamides of N-heterocyclic carboxylic acids or isosteres for vision and memory disorders
KR20020005665A (en) * 1999-04-09 2002-01-17 추후보정 Caspase inhibitors and the use thereof
ATE277923T1 (en) * 1999-05-07 2004-10-15 Texas Biotechnology Corp PROPANE ACID DERIVATIVES THAT PREVENT THE BINDING OF INTEGRINS TO THEIR RECEPTORS
US6723711B2 (en) 1999-05-07 2004-04-20 Texas Biotechnology Corporation Propanoic acid derivatives that inhibit the binding of integrins to their receptors
AR026748A1 (en) 1999-12-08 2003-02-26 Vertex Pharma A CASPASE INHIBITING COMPOUND, A PHARMACEUTICAL COMPOSITION THAT INCLUDES IT, A METHOD FOR THE SYNTHESIS OF THE SAME AND AN INTERMEDIATE COMPOUND PARADICHA SYNTHESIS
EP1923386A3 (en) 2000-03-29 2008-05-28 Vertex Pharmceuticals Incorporated Carbamate caspase inhibitors and uses thereof
IL151829A0 (en) 2000-03-29 2003-04-10 Vertex Pharma Carbamate derivatives and pharmaceutical compositions containing the same
PE20011350A1 (en) 2000-05-19 2002-01-15 Vertex Pharma PROPHARMAC OF AN INHIBITOR OF INTERLEUKIN-1ß CONVERTER ENZYME (ICE)
WO2001094351A1 (en) * 2000-06-07 2001-12-13 Vertex Pharmaceuticals Incorporated Caspase inhibitors and uses thereof
US6355666B1 (en) 2000-06-23 2002-03-12 Medinox, Inc. Protected forms of pharmacologically active agents and uses therefor
JP2004521080A (en) * 2000-09-08 2004-07-15 メルク フロスト カナダ アンド カンパニー Gamma-keto acid dipeptides as caspase-3 inhibitors
PE20020500A1 (en) * 2000-09-13 2002-06-25 Vertex Pharma DERIVATIVES OF PIPERIDINE, TETRAHYDROQUINOLINE, TETRAHYDROISOQUINOLINE AS DANDRUFF INHIBITORS
AU2007201841B2 (en) * 2000-09-13 2008-09-04 Vertex Pharmaceuticals Incorporated Caspase Inhibitors and Uses Thereof
KR100896664B1 (en) 2000-09-15 2009-05-14 버텍스 파마슈티칼스 인코포레이티드 Pyrazole compounds useful as protein kinase inhibitors
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
WO2002068415A1 (en) 2000-12-21 2002-09-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
CA2443600A1 (en) 2001-04-19 2002-10-31 Vertex Pharmaceuticals Incorporated Heterocyclyldicarbamides as caspase inhibitors
EP1392289A2 (en) 2001-05-23 2004-03-03 Vertex Pharmaceuticals Incorporated Caspase inhibitors and uses thereof
US6878743B2 (en) 2001-09-18 2005-04-12 Sunesis Pharmaceuticals, Inc. Small molecule inhibitors of caspases
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
RU2005102094A (en) 2002-06-28 2006-02-27 Вертекс Фармасьютикалз Инкорпорейтед (Us) CASPASE INHIBITORS AND THEIR APPLICATION
PL374967A1 (en) 2002-08-02 2005-11-14 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of gsk-3
CN100366612C (en) 2002-12-20 2008-02-06 沃泰克斯药物股份有限公司 4-oxo-3-(1-oxo-1h-isoquinolin-2-ylacetylamino)-pentanoic acid ester and amide derivatives and their use as aspartic specifity cysteine proteinase inhibitors
PE20050159A1 (en) * 2003-05-27 2005-04-19 Vertex Pharma DERIVATIVES OF 3- [2- (3-AMINO-2-OXO-2H-PYRIDIN-1-IL) -ACETILAMINO] -4-OXO-PENTANOICO AS CASPASE INHIBITORS
DK2399916T3 (en) 2004-03-12 2015-03-02 Vertex Pharma A process and intermediates for the preparation of asparaginacetal-caspase inhibitors
CA2566362C (en) 2004-05-15 2013-09-10 Vertex Pharmaceuticals Incorporated Treating seizures using ice inhibitors
JP2008500374A (en) 2004-05-27 2008-01-10 バーテックス　ファーマシューティカルズ　インコーポレイテッド ICE inhibitors for the treatment of autoinflammatory diseases
ATE543803T1 (en) 2004-11-24 2012-02-15 Vertex Pharma 3-Ä2-(3-AZYLAMINO-2-OXO-2H-PYRIDINE-1-YL)ACETYLAMINOÜ-4-OXOPENTANIC ACID DERIVATIVES AND THEIR USE AS CASPASE INHIBITORS
CN101268084A (en) 2005-07-28 2008-09-17 沃泰克斯药物股份有限公司 Caspase inhibitor prodrugs
US7507842B2 (en) 2005-08-12 2009-03-24 Radiorx, Inc. Cyclic nitro compounds, pharmaceutical compositions thereof and uses thereof
RU2423361C2 (en) 2005-11-03 2011-07-10 Вертекс Фармасьютикалз Инкорпорейтед Aminopyrimidines as kinase inhibitors
CN101209976B (en) * 2006-12-29 2012-01-11 中国人民解放军军事医学科学院毒物药物研究所 Substituted tartaric acid derivatives and use thereof for preparing beta-secretase inhibitor
CA2685876A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
CN101790532B (en) 2007-07-31 2013-11-20 沃泰克斯药物股份有限公司 Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof
JP2012501971A (en) 2008-09-03 2012-01-26 バーテックス ファーマシューティカルズ インコーポレイテッド Co-crystals and pharmaceutical formulations containing co-crystals
WO2012061785A2 (en) 2010-11-05 2012-05-10 Brandeis University Ice inhibiting compounds and uses thereof
US9956260B1 (en) 2011-07-22 2018-05-01 The J. David Gladstone Institutes Treatment of HIV-1 infection and AIDS
US20140308260A1 (en) 2011-10-07 2014-10-16 Radiorx, Inc. Methods and compositions comprising a nitrite-reductase promoter for treatment of medical disorders and preservation of blood products
US9987270B1 (en) 2015-10-29 2018-06-05 Epicentrix, Inc. Treatment of gliomas using organonitro compound combination therapy
EA201891606A1 (en) 2016-01-11 2019-02-28 Эписентарикс, Инк. COMPOSITIONS AND METHODS FOR INTRAVENOUS INTRODUCTION OF 2-BROM-1- (3,3-DINITROAZETIDIN-1-IL) ETHANON
KR20190128619A (en) * 2016-10-14 2019-11-18 에피센트알엑스, 인코포레이티드 Sulfoxyalkyl organononitro and related compounds and pharmaceutical compositions for use in medicine
US11744859B2 (en) 2017-07-07 2023-09-05 Epicentrx, Inc. Compositions and methods for parenteral administration of therapeutic agents
US11510901B2 (en) 2018-01-08 2022-11-29 Epicentrx, Inc. Methods and compositions utilizing RRx-001 combination therapy for radioprotection
CN108997155A (en) * 2018-09-17 2018-12-14 吉尔生化（上海）有限公司 A kind of polypeptide raw material aspartic acid β-tert-butyl ester α-methyl ester hydrochloride preparation method

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0618223A3 (en) * 1993-03-08 1996-06-12 Sandoz Ltd Peptides inhibiting interleukin 1-bêta release useful as antiinflammatory agents.
CA2122227A1 (en) * 1993-04-29 1994-10-30 Roland E. Dolle Peptide analogs as irreversible interleukin-1.beta. protease inhibitors

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WO1998016502A1 (en) 1998-04-23
BR9712530A (en) 1999-10-19
AU4902397A (en) 1998-05-11
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NO991677D0 (en) 1999-04-09

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