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WO2016029216A3 - Method for producing amidine derivatives - Google Patents

Method for producing amidine derivatives Download PDF

Info

Publication number
WO2016029216A3
WO2016029216A3 PCT/US2015/046582 US2015046582W WO2016029216A3 WO 2016029216 A3 WO2016029216 A3 WO 2016029216A3 US 2015046582 W US2015046582 W US 2015046582W WO 2016029216 A3 WO2016029216 A3 WO 2016029216A3
Authority
WO
WIPO (PCT)
Prior art keywords
amidine derivatives
producing
producing amidine
derivatives
prodrug
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US2015/046582
Other languages
French (fr)
Other versions
WO2016029216A2 (en
Inventor
Pravin L. Kotian
Vivekanand P. Kamath
Venkat R. CHINTAREDDY
Ahmed Abdel-Magid
Pooran Chand
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Biocryst Pharmaceuticals Inc
Original Assignee
Biocryst 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
Application filed by Biocryst Pharmaceuticals Inc filed Critical Biocryst Pharmaceuticals Inc
Publication of WO2016029216A2 publication Critical patent/WO2016029216A2/en
Publication of WO2016029216A3 publication Critical patent/WO2016029216A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—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
    • C07D213/56—Amides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen 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
    • C07D213/61—Halogen atoms or nitro radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention provides methods and intermediates useful in the synthesis of a compound of formula (I): or a pharmaceutically acceptable salt, solvate, ester or prodrug thereof; wherein the variables are as defined herein.
PCT/US2015/046582 2014-08-22 2015-08-24 Method for producing amidine derivatives Ceased WO2016029216A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462040818P 2014-08-22 2014-08-22
US62/040,818 2014-08-22

Publications (2)

Publication Number Publication Date
WO2016029216A2 WO2016029216A2 (en) 2016-02-25
WO2016029216A3 true WO2016029216A3 (en) 2016-05-12

Family

ID=54012342

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2015/046582 Ceased WO2016029216A2 (en) 2014-08-22 2015-08-24 Method for producing amidine derivatives

Country Status (1)

Country Link
WO (1) WO2016029216A2 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA46642A (en) 2016-10-31 2021-04-21 Biocryst Pharm Inc KALLICREIN INHIBITOR MEDICINAL PRODUCTS
CN106749358B (en) * 2016-11-22 2019-05-10 雅本化学股份有限公司 A method of synthesis 5- methoxyl group -4- hydroxyl -2- aldehyde radical phenyl boric acid pinacol ester
WO2023160509A1 (en) * 2022-02-25 2023-08-31 中国科学院上海药物研究所 Amidine derivative compound, and preparation method therefor and use thereof

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002042273A2 (en) * 2000-11-07 2002-05-30 Bristol-Myers Squibb Company Acid derivatives useful as serine protease inhibitors
US6699994B1 (en) * 2001-04-06 2004-03-02 Biocryst Pharmaceuticals, Inc. Biaryl compounds as serine protease inhibitors
WO2006110173A2 (en) * 2004-10-05 2006-10-19 Smithkline Beecham Corporation Novel compounds
WO2008084223A2 (en) * 2007-01-11 2008-07-17 Astrazeneca Ab Chemical compounds 637: pyridopyrimidinediones as pde4 inhibitors
WO2011094450A1 (en) * 2010-01-27 2011-08-04 Anacor Pharmaceuticals, Inc Boron-containing small molecules

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002042273A2 (en) * 2000-11-07 2002-05-30 Bristol-Myers Squibb Company Acid derivatives useful as serine protease inhibitors
US6699994B1 (en) * 2001-04-06 2004-03-02 Biocryst Pharmaceuticals, Inc. Biaryl compounds as serine protease inhibitors
WO2006110173A2 (en) * 2004-10-05 2006-10-19 Smithkline Beecham Corporation Novel compounds
WO2008084223A2 (en) * 2007-01-11 2008-07-17 Astrazeneca Ab Chemical compounds 637: pyridopyrimidinediones as pde4 inhibitors
WO2011094450A1 (en) * 2010-01-27 2011-08-04 Anacor Pharmaceuticals, Inc Boron-containing small molecules

Non-Patent Citations (7)

* Cited by examiner, † Cited by third party
Title
DATABASE REGISTRY [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 12 January 2014 (2014-01-12), "5-(aminocarbonyl)-2-fluoro-benzoic acid methyl ester", XP002754741, Database accession no. 1517885-05-0 *
DATABASE REGISTRY [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 17 January 2014 (2014-01-17), "5-[(cyclopropylamino)carbonyl]-2-fluoro-benzoic acid methyl ester", XP002754740, Database accession no. 1523183-73-4 *
ERAN SELLA ET AL: "Hydroquinone-quinone oxidation by molecular oxygen: a simple tool for signal amplification through auto-generation of hydrogen peroxide", ORGANIC & BIOMOLECULAR CHEMISTRY, vol. 11, no. 31, 1 January 2013 (2013-01-01), GB, pages 5074, XP055225744, ISSN: 1477-0520, DOI: 10.1039/c3ob40962g *
IMAKURA Y ET AL: "REGIOSELECTIVE CLEAVAGE REACTION OF THE AROMATIC METHYLENEDIOXY RING. V. CLEAVAGE WITH SODIUM ALKOXIDES-ALCOHOLS, POTASSIUM TERT-BUTOXIDE-ALCOHOLS, DIMSYL ANION-METHYL ALCOHOL, METALLIC SODIUM-ALCOHOLS, AND SODIUM CYANIDE IN DIPOLAR APROTIC SOLVENTS", CHEMICAL AND PHARMACEUTICAL BULLETIN, PHARMACEUTICAL SOCIETY OF JAPAN, JP, vol. 40, no. 7, 1 July 1992 (1992-07-01), pages 1691 - 1696, XP001148863, ISSN: 0009-2363 *
KOTIAN P L ET AL: "Design, parallel synthesis, and crystal structures of biphenyl antithrombotics as selective inhibitors of tissue factor FVIIa complex. Part 1: Exploration of S2 pocket pharmacophores", BIOORGANIC & MEDICINAL CHEMISTRY, PERGAMON, GB, vol. 17, no. 11, 1 June 2009 (2009-06-01), pages 3934 - 3958, XP026118942, ISSN: 0968-0896, [retrieved on 20090412], DOI: 10.1016/J.BMC.2009.04.013 *
MIMI L. QUAN ET AL: "Tetrahydroquinoline Derivatives as Potent and Selective Factor XIa Inhibitors", JOURNAL OF MEDICINAL CHEMISTRY, vol. 57, no. 3, 13 February 2014 (2014-02-13), pages 955 - 969, XP055156150, ISSN: 0022-2623, DOI: 10.1021/jm401670x *
ZHANG J ET AL: "Discovery of Highly Potent Small Molecule Kallikrein Inhibitors", MEDICINAL CHEMISTRY, BENTHAM SCIENCE PUBLISHERS LTD, NL, vol. 2, 1 January 2006 (2006-01-01), pages 545 - 533, XP009186844, ISSN: 1573-4064 *

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Publication number Publication date
WO2016029216A2 (en) 2016-02-25

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