AU2012299218A1 - Crystal forms of a HCV protease inhibitor - Google Patents

Crystal forms of a HCV protease inhibitor Download PDF

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Publication number
AU2012299218A1
AU2012299218A1 AU2012299218A AU2012299218A AU2012299218A1 AU 2012299218 A1 AU2012299218 A1 AU 2012299218A1 AU 2012299218 A AU2012299218 A AU 2012299218A AU 2012299218 A AU2012299218 A AU 2012299218A AU 2012299218 A1 AU2012299218 A1 AU 2012299218A1
Authority
AU
Australia
Prior art keywords
hydrate
compound
diffraction pattern
radiation
powder diffraction
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.)
Abandoned
Application number
AU2012299218A
Other languages
English (en)
Inventor
Juan D. Arredondo
Laura Artino
Gregory L. Beutner
Eric J. Choi
Jeremy Scott
Clinton Scott Shultz
Robert M. Wenslow Jr.
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.)
Organon Pharma UK Ltd
Merck Sharp and Dohme LLC
Original Assignee
Merck Sharp and Dohme Ltd
Merck Sharp and Dohme LLC
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 Merck Sharp and Dohme Ltd, Merck Sharp and Dohme LLC filed Critical Merck Sharp and Dohme Ltd
Publication of AU2012299218A1 publication Critical patent/AU2012299218A1/en
Abandoned legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C35/00Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C07C35/02Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring monocyclic
    • C07C35/04Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring monocyclic containing a three or four-membered rings
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C269/04Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups from amines with formation of carbamate groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/32Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C271/34Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of rings other than six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00Preparation of carboxylic acid esters
    • C07C67/14Preparation of carboxylic acid esters from carboxylic acid halides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/013Esters of alcohols having the esterified hydroxy group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/02Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
    • C07C69/12Acetic acid esters
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/16Peri-condensed systems
    • 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
    • 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
    • C07K5/12Cyclic peptides with only normal peptide bonds in the ring
    • C07K5/126Tetrapeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Communicable Diseases (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Oncology (AREA)
  • Veterinary Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Cephalosporin Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2012299218A 2011-08-19 2012-08-16 Crystal forms of a HCV protease inhibitor Abandoned AU2012299218A1 (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201161525462P 2011-08-19 2011-08-19
US61/525,462 2011-08-19
US201161533439P 2011-09-12 2011-09-12
US61/533,439 2011-09-12
US201161533915P 2011-09-13 2011-09-13
US61/533,915 2011-09-13
US201161539540P 2011-09-27 2011-09-27
US61/539,540 2011-09-27
PCT/US2012/051168 WO2013028465A1 (en) 2011-08-19 2012-08-16 Crystal forms of a hcv protease inhibitor

Publications (1)

Publication Number Publication Date
AU2012299218A1 true AU2012299218A1 (en) 2014-02-20

Family

ID=47746773

Family Applications (2)

Application Number Title Priority Date Filing Date
AU2012299218A Abandoned AU2012299218A1 (en) 2011-08-19 2012-08-16 Crystal forms of a HCV protease inhibitor
AU2012299223A Abandoned AU2012299223A1 (en) 2011-08-19 2012-08-16 Process and intermediates for preparing macrolactams

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU2012299223A Abandoned AU2012299223A1 (en) 2011-08-19 2012-08-16 Process and intermediates for preparing macrolactams

Country Status (11)

Country Link
US (3) US9238604B2 (https=)
EP (3) EP2744336B1 (https=)
JP (2) JP2014521750A (https=)
KR (2) KR20140053330A (https=)
CN (2) CN103874414A (https=)
AU (2) AU2012299218A1 (https=)
BR (2) BR112014003802A2 (https=)
CA (2) CA2844386A1 (https=)
MX (2) MX2014001944A (https=)
RU (2) RU2014110399A (https=)
WO (3) WO2013028470A1 (https=)

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UA119315C2 (uk) 2012-07-03 2019-06-10 Гіліад Фармассет Елелсі Інгібітори вірусу гепатиту с
EA025560B1 (ru) 2012-10-19 2017-01-30 Бристол-Майерс Сквибб Компани Ингибиторы вируса гепатита с
EP2914613B1 (en) 2012-11-02 2017-11-22 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
US9334279B2 (en) 2012-11-02 2016-05-10 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US9643999B2 (en) 2012-11-02 2017-05-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US9409943B2 (en) 2012-11-05 2016-08-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP2764866A1 (en) 2013-02-07 2014-08-13 IP Gesellschaft für Management mbH Inhibitors of nedd8-activating enzyme
JP6342922B2 (ja) 2013-03-07 2018-06-13 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company C型肝炎ウイルス阻害剤
WO2014145095A1 (en) 2013-03-15 2014-09-18 Gilead Sciences, Inc. Macrocyclic and bicyclic inhibitors of hepatitis c virus
SG11201602693QA (en) 2013-10-18 2016-05-30 Merck Sharp & Dohme Methods and intermediates for preparing macrolactams
WO2015095437A1 (en) * 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Methods and intermediates for the preparation of macrolactams
ES2933350T3 (es) * 2014-01-24 2023-02-06 Turning Point Therapeutics Inc Macrociclos de diarilo como moduladores de proteína quinasas
MX373056B (es) 2014-06-06 2020-05-20 Abbvie Inc Formas cristalinas de glecaprevir.
AU2016287568B2 (en) 2015-07-02 2020-08-20 Turning Point Therapeutics, Inc. Chiral diaryl macrocycles as modulators of protein kinases
RU2765181C2 (ru) 2015-07-06 2022-01-26 Тёрнинг Поинт Терапьютикс, Инк. Полиморфная форма диарильного макроцикла
PT3733187T (pt) 2015-07-21 2024-11-08 Turning Point Therapeutics Inc Macrociclo de diarilo quiral e utilização do mesmo no tratamento do cancro
CN109641874A (zh) 2016-05-10 2019-04-16 C4医药公司 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体
EP3454856B1 (en) 2016-05-10 2024-09-11 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
ES2990061T3 (es) 2016-05-10 2024-11-28 C4 Therapeutics Inc Degronímeros espirocíclicos para la degradación de proteínas diana
CN109790143A (zh) 2016-05-10 2019-05-21 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
US10689400B2 (en) 2016-07-28 2020-06-23 Turning Point Therapeutics, Inc. Macrocycle kinase inhibitors
TWI808958B (zh) 2017-01-25 2023-07-21 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
CN110769822A (zh) 2017-06-20 2020-02-07 C4医药公司 用于蛋白降解的n/o-连接的降解决定子和降解决定子体
CN111182903A (zh) 2017-07-28 2020-05-19 特普医药公司 巨环化合物及其用途
LT3728271T (lt) 2017-12-19 2022-12-12 Turning Point Therapeutics, Inc. Makrocikliniai junginiai, skirti ligų gydymui
CN111057045A (zh) * 2019-12-18 2020-04-24 安徽红杉生物医药科技有限公司 Hcv ns3/4a蛋白酶抑制剂中间体及其合成方法、应用
CN112174982A (zh) * 2020-09-10 2021-01-05 上海希迈医药科技有限公司 一种洛普替尼晶型及其制备方法

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Also Published As

Publication number Publication date
EP2744336A4 (en) 2014-12-31
US20140243519A1 (en) 2014-08-28
BR112014003802A2 (pt) 2017-06-13
EP2744507A1 (en) 2014-06-25
WO2013028465A1 (en) 2013-02-28
US9242917B2 (en) 2016-01-26
EP2744331A1 (en) 2014-06-25
KR20140059236A (ko) 2014-05-15
RU2014110400A (ru) 2015-09-27
CA2844388A1 (en) 2013-02-28
AU2012299223A1 (en) 2014-02-27
JP2014521750A (ja) 2014-08-28
KR20140053330A (ko) 2014-05-07
BR112014003798A2 (pt) 2017-03-01
US9073825B2 (en) 2015-07-07
MX2014001945A (es) 2014-03-27
EP2744507A4 (en) 2015-01-28
US20140206605A1 (en) 2014-07-24
US20140200343A1 (en) 2014-07-17
MX2014001944A (es) 2014-03-27
CN103889439A (zh) 2014-06-25
EP2744336A1 (en) 2014-06-25
US9238604B2 (en) 2016-01-19
CN103874414A (zh) 2014-06-18
WO2013028470A1 (en) 2013-02-28
CA2844386A1 (en) 2013-02-28
EP2744336B1 (en) 2017-07-05
EP2744331A4 (en) 2015-01-21
WO2013028471A1 (en) 2013-02-28
RU2014110399A (ru) 2015-09-27
JP2014524442A (ja) 2014-09-22

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