KR20140059236A - Hcv 프로테아제 억제제의 결정 형태 - Google Patents

Hcv 프로테아제 억제제의 결정 형태 Download PDF

Info

Publication number
KR20140059236A
KR20140059236A KR1020147006888A KR20147006888A KR20140059236A KR 20140059236 A KR20140059236 A KR 20140059236A KR 1020147006888 A KR1020147006888 A KR 1020147006888A KR 20147006888 A KR20147006888 A KR 20147006888A KR 20140059236 A KR20140059236 A KR 20140059236A
Authority
KR
South Korea
Prior art keywords
compound
hydrate
diffraction pattern
rti
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.)
Withdrawn
Application number
KR1020147006888A
Other languages
English (en)
Korean (ko)
Inventor
그레고리 엘. 뷰트너
로버트 엠. 주니어 웬슬로우
에릭 제이. 초이
클린턴 스콧 슐츠
제레미 스콧
후안 디. 아레돈도
로라 아르티노
Original Assignee
머크 샤프 앤드 돔 코포레이션
머크 샤프 앤드 돔 리미티드
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 머크 샤프 앤드 돔 코포레이션, 머크 샤프 앤드 돔 리미티드 filed Critical 머크 샤프 앤드 돔 코포레이션
Publication of KR20140059236A publication Critical patent/KR20140059236A/ko
Withdrawn legal-status Critical Current

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C35/00—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C07C35/02—Compounds 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
    • C07C35/04—Compounds 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C269/04—Preparation 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/32—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C271/34—Esters 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00—Preparation of carboxylic acid esters
    • C07C67/14—Preparation of carboxylic acid esters from carboxylic acid halides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/013—Esters of alcohols having the esterified hydroxy group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/02—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
    • C07C69/12—Acetic acid esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic 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
    • C07D498/16—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/12—Cyclic peptides with only normal peptide bonds in the ring
    • C07K5/126—Tetrapeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal 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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Cephalosporin Compounds (AREA)
KR1020147006888A 2011-08-19 2012-08-16 Hcv 프로테아제 억제제의 결정 형태 Withdrawn KR20140059236A (ko)

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
KR20140059236A true KR20140059236A (ko) 2014-05-15

Family

ID=47746773

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020147006888A Withdrawn KR20140059236A (ko) 2011-08-19 2012-08-16 Hcv 프로테아제 억제제의 결정 형태
KR1020147006858A Withdrawn KR20140053330A (ko) 2011-08-19 2012-08-16 마크로락탐의 제조를 위한 방법 및 중간체

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020147006858A Withdrawn KR20140053330A (ko) 2011-08-19 2012-08-16 마크로락탐의 제조를 위한 방법 및 중간체

Country Status (11)

Country Link
US (3) US9073825B2 (enExample)
EP (3) EP2744331A4 (enExample)
JP (2) JP2014521750A (enExample)
KR (2) KR20140059236A (enExample)
CN (2) CN103889439A (enExample)
AU (2) AU2012299223A1 (enExample)
BR (2) BR112014003798A2 (enExample)
CA (2) CA2844388A1 (enExample)
MX (2) MX2014001944A (enExample)
RU (2) RU2014110400A (enExample)
WO (3) WO2013028470A1 (enExample)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8828930B2 (en) 2009-07-30 2014-09-09 Merck Sharp & Dohme Corp. Hepatitis C virus NS3 protease inhibitors
US8957203B2 (en) 2011-05-05 2015-02-17 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
MX2014001944A (es) 2011-08-19 2014-03-27 Merck Sharp & Dohme Formas cristalinas de un inhibidor de la proteasa del virus de la hepatitis c.
UA119315C2 (uk) 2012-07-03 2019-06-10 Гіліад Фармассет Елелсі Інгібітори вірусу гепатиту с
MX360452B (es) 2012-10-19 2018-11-01 Bristol Myers Squibb Co Inhibidores del virus de la hepatitis c.
EP2914613B1 (en) 2012-11-02 2017-11-22 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
US9643999B2 (en) 2012-11-02 2017-05-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP2914598B1 (en) 2012-11-02 2017-10-18 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
ES2735355T3 (es) 2013-03-15 2019-12-18 Gilead Sciences Inc Inhibidores macrocíclicos y bicíclicos de virus de hepatitis C
EP3057926A4 (en) * 2013-10-18 2017-07-12 Merck Sharp & Dohme Corp. 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
EP3636649B1 (en) 2014-01-24 2024-02-14 Turning Point Therapeutics, Inc. Diaryl macrocycles as modulators of protein kinases
EP3151850A4 (en) 2014-06-06 2017-11-29 AbbVie Inc. Crystal forms
RU2732405C2 (ru) 2015-07-02 2020-09-16 Тёрнинг Поинт Терапьютикс, Инк. Хиральные диарильные макроциклы в качестве модуляторов протеинкиназ
WO2017007759A1 (en) * 2015-07-06 2017-01-12 Tp Therapeutics, Inc. Diaryl macrocycle polymorph
US20180325901A1 (en) 2015-07-21 2018-11-15 Tp Therapeutics, Inc. Chiral diaryl macrocycles and uses thereof
WO2017197036A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
EP4491236A3 (en) 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
EP3455218A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
JP2019527230A (ja) 2016-07-28 2019-09-26 ターニング・ポイント・セラピューティクス・インコーポレイテッドＴｕｒｎｉｎｇ Ｐｏｉｎｔ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． 大環状キナーゼ阻害剤
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
CN118440096A (zh) 2017-06-20 2024-08-06 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
LT3658148T (lt) 2017-07-28 2024-09-10 Turning Point Therapeutics, Inc. Makrocikliniai junginiai ir jų panaudojimas
KR102814342B1 (ko) 2017-12-19 2025-05-29 터닝 포인트 테라퓨틱스, 인크. 질병 치료용 대환식 화합물
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

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4871868A (en) * 1987-03-11 1989-10-03 Takeda Chemical Industries, Ltd. Production of substituted acetylenic compounds
GB9207987D0 (en) 1992-04-10 1992-05-27 Smithkline Beecham Plc Novel container and closure
US5716960A (en) * 1995-01-13 1998-02-10 U.S. Bioscience Inc. And Individuals Crystalline trimetrexate salts and the process for making the same
ZA98879B (en) * 1997-02-04 1998-08-03 Ono Pharmaceutical Co Omega-cycloalkyl-prostaglandin e2 derivatives
NO317155B1 (no) 1997-02-04 2004-08-30 Ono Pharmaceutical Co <omega>-cykloalkyl-prostagladin-E<N>2</N>-derivater
EP2602259A3 (en) 2005-02-18 2014-09-10 Mitsubishi Tanabe Pharma Corporation Salt of proline derivative, solvate thereof, and production method thereof
US7834145B2 (en) 2005-03-22 2010-11-16 Merck Sharp & Dohme Corp. HCV protease substrates
AU2006242475B2 (en) 2005-05-02 2011-07-07 Merck Sharp & Dohme Corp. HCV NS3 protease inhibitors
US7470664B2 (en) 2005-07-20 2008-12-30 Merck & Co., Inc. HCV NS3 protease inhibitors
UA90909C2 (en) * 2005-07-20 2010-06-10 Мерк Шарп Энд Домэ Корп. Hcv ns3 protease inhibitors
JP4705984B2 (ja) 2005-08-01 2011-06-22 メルク・シャープ・エンド・ドーム・コーポレイション Ｈｃｖｎｓ３プロテアーゼ阻害剤としての大環状ペプチド
CN101394829A (zh) * 2006-03-07 2009-03-25 宝洁公司 用于氧化性染色角蛋白纤维的组合物和使用此类组合物的方法
GB0609492D0 (en) 2006-05-15 2006-06-21 Angeletti P Ist Richerche Bio Therapeutic agents
GB0612423D0 (en) 2006-06-23 2006-08-02 Angeletti P Ist Richerche Bio Therapeutic agents
EP2079480B1 (en) 2006-10-24 2013-06-05 Merck Sharp & Dohme Corp. Hcv ns3 protease inhibitors
AU2007309546A1 (en) 2006-10-24 2008-05-02 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. HCV NS3 protease inhibitors
AU2007318165B2 (en) 2006-10-27 2011-11-17 Msd Italia S.R.L. HCV NS3 protease inhibitors
EP2083844B1 (en) 2006-10-27 2013-11-27 Merck Sharp & Dohme Corp. Hcv ns3 protease inhibitors
US20090155209A1 (en) 2007-05-03 2009-06-18 Blatt Lawrence M Novel macrocyclic inhibitors of hepatitis c virus replication
US8927569B2 (en) 2007-07-19 2015-01-06 Merck Sharp & Dohme Corp. Macrocyclic compounds as antiviral agents
AU2009217551B2 (en) 2008-02-25 2014-07-31 Msd Italia S.R.L. Therapeutic compounds
WO2009131196A1 (ja) * 2008-04-24 2009-10-29 武田薬品工業株式会社 置換ピロリジン誘導体およびその用途
US8871753B2 (en) 2008-04-24 2014-10-28 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
EP2271345B1 (en) 2008-04-28 2015-05-20 Merck Sharp & Dohme Corp. Hcv ns3 protease inhibitors
EP2540349B1 (en) * 2008-07-22 2014-02-12 Merck Sharp & Dohme Corp. Pharmaceutical compositions comprising a macrocyclic quinoxaline compound which is an hcv ns3 protease inhibitor
US8828930B2 (en) 2009-07-30 2014-09-09 Merck Sharp & Dohme Corp. Hepatitis C virus NS3 protease inhibitors
CN102470158A (zh) * 2009-08-27 2012-05-23 默沙东公司 制备丙型肝炎病毒的蛋白酶抑制剂的工艺方法
MX2014001944A (es) 2011-08-19 2014-03-27 Merck Sharp & Dohme Formas cristalinas de un inhibidor de la proteasa del virus de la hepatitis c.

Also Published As

Publication number Publication date
CN103889439A (zh) 2014-06-25
RU2014110400A (ru) 2015-09-27
CA2844388A1 (en) 2013-02-28
AU2012299223A1 (en) 2014-02-27
BR112014003798A2 (pt) 2017-03-01
MX2014001945A (es) 2014-03-27
EP2744507A1 (en) 2014-06-25
CN103874414A (zh) 2014-06-18
US9242917B2 (en) 2016-01-26
MX2014001944A (es) 2014-03-27
AU2012299218A1 (en) 2014-02-20
EP2744336A1 (en) 2014-06-25
WO2013028465A1 (en) 2013-02-28
RU2014110399A (ru) 2015-09-27
US20140243519A1 (en) 2014-08-28
EP2744336A4 (en) 2014-12-31
JP2014524442A (ja) 2014-09-22
BR112014003802A2 (pt) 2017-06-13
US20140206605A1 (en) 2014-07-24
JP2014521750A (ja) 2014-08-28
EP2744336B1 (en) 2017-07-05
WO2013028470A1 (en) 2013-02-28
US9073825B2 (en) 2015-07-07
EP2744331A1 (en) 2014-06-25
US9238604B2 (en) 2016-01-19
EP2744331A4 (en) 2015-01-21
US20140200343A1 (en) 2014-07-17
CA2844386A1 (en) 2013-02-28
WO2013028471A1 (en) 2013-02-28
EP2744507A4 (en) 2015-01-28
KR20140053330A (ko) 2014-05-07

Similar Documents

Publication Publication Date Title
KR20140059236A (ko) Hcv 프로테아제 억제제의 결정 형태
JP6524355B2 (ja) Ｔｌｒ７アゴニストとしての７−（チアゾール−５−イル）ピロロピリミジン化合物
KR100652535B1 (ko) Ｉｍｐｄｈ 효소의 억제제
ES2470568T3 (es) Inhibidores macroc�clicos del virus de la hepatitis C
CN102414199B (zh) 二芳基醚
JP6034802B2 (ja) 大環状ラクタムの調製のための方法および中間体
TWI542585B (zh) Ｃ型肝炎病毒抑制劑
EP3816163A1 (en) Cell necrosis inhibitor, preparation method therefor and use thereof
AU2014225052A1 (en) Novel nucleoside phosphoramidate compound and use thereof
WO2016127916A1 (zh) 作为长效dpp-iv抑制剂的取代的氨基六元饱和杂脂环类
WO2021047524A1 (zh) 一类靶向蛋白质水解通路的功能分子及其制备和应用
CN114907355A (zh) 一种二氢嘧啶类化合物、其制备方法及其应用
CN106967141B (zh) 核苷氨基磷酸酯化合物及其医药组合物和用途
WO2015095430A1 (en) Methods and intermediates for the preparation of macrolactams
EP3498712B1 (en) Spirocyclic indolone polyethylene glycol carbonate compound, composition, preparation method and use thereof
RU2793918C2 (ru) Ингибитор некроза клеток, способ его получения и применения
WO2025016441A1 (zh) 新型GalNAc的靶向递送片段及其制备和应用
HK1136824B (en) Macrocyclic inhibitors of hepatitis c virus

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20140314

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PC1203 Withdrawal of no request for examination
WITN Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid