ZA201307332B - Aminopyrazine compounds useful as inhibitors of tra kinase - Google Patents

Aminopyrazine compounds useful as inhibitors of tra kinase

Info

Publication number
ZA201307332B
ZA201307332B ZA2013/07332A ZA201307332A ZA201307332B ZA 201307332 B ZA201307332 B ZA 201307332B ZA 2013/07332 A ZA2013/07332 A ZA 2013/07332A ZA 201307332 A ZA201307332 A ZA 201307332A ZA 201307332 B ZA201307332 B ZA 201307332B
Authority
ZA
South Africa
Prior art keywords
tra
kinase
inhibitors
compounds useful
aminopyrazine compounds
Prior art date
Application number
ZA2013/07332A
Other languages
English (en)
Inventor
Jean-Damien Charrier
Somhairle Maccormick
Pierre-Henri Storck
Joanne Pinder
Michael Edward O'donnell
Ronald Marcellus Alphonsus Knegtel
Stephen Clinton Young Young
David Kay
Philip Michael Reaper
Steven John Durrant
Heather Clare Twin
Christopher John Davis
Original Assignee
Vertex Pharmaceutical Incorporated
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 Vertex Pharmaceutical Incorporated filed Critical Vertex Pharmaceutical Incorporated
Publication of ZA201307332B publication Critical patent/ZA201307332B/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/555—Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/24—Heavy metals; Compounds thereof
    • A61K33/243—Platinum; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Inorganic Chemistry (AREA)
  • Dermatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
ZA2013/07332A 2011-04-05 2013-10-01 Aminopyrazine compounds useful as inhibitors of tra kinase ZA201307332B (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201161471937P 2011-04-05 2011-04-05
US201161541862P 2011-09-30 2011-09-30
US201161554167P 2011-11-01 2011-11-01
PCT/US2012/032438 WO2012138938A1 (en) 2011-04-05 2012-04-05 Aminopyrazine compounds useful as inhibitors of tra kinase

Publications (1)

Publication Number Publication Date
ZA201307332B true ZA201307332B (en) 2015-03-25

Family

ID=46001773

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA2013/07332A ZA201307332B (en) 2011-04-05 2013-10-01 Aminopyrazine compounds useful as inhibitors of tra kinase

Country Status (11)

Country Link
US (1) US8877759B2 (OSRAM)
EP (1) EP2694498B1 (OSRAM)
JP (1) JP2014510151A (OSRAM)
KR (1) KR20140027974A (OSRAM)
CN (1) CN103562204A (OSRAM)
AU (1) AU2012240030A1 (OSRAM)
CA (1) CA2832100A1 (OSRAM)
IL (1) IL228715A0 (OSRAM)
MX (1) MX2013011450A (OSRAM)
WO (1) WO2012138938A1 (OSRAM)
ZA (1) ZA201307332B (OSRAM)

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2376485T3 (pl) 2008-12-19 2018-05-30 Vertex Pharmaceuticals Incorporated Pochodne pirazyny użyteczne jako inhibitory kinazy ATR
EP2569287B1 (en) 2010-05-12 2014-07-09 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
WO2011143423A2 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
MX2012013082A (es) 2010-05-12 2013-05-09 Vertex Pharma Derivados de 2-aminopiridina utiles como iinhibidores de cinasa atr.
CA2798763A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2011143419A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Pyrazines useful as inhibitors of atr kinase
US8969356B2 (en) 2010-05-12 2015-03-03 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
MX2013000103A (es) 2010-06-23 2013-06-13 Vertex Pharma Derivados de pirrolo-pirazina utiles como inhibidores de cinasa art.
KR20140027974A (ko) 2011-04-05 2014-03-07 버텍스 파마슈티칼스 인코포레이티드 Ｔｒａ 키나제의 억제제로서 유용한 아미노피라진 화합물
JP2014517079A (ja) 2011-06-22 2014-07-17 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 Ａｔｒキナーゼ阻害剤として有用な化合物
JP2014520161A (ja) 2011-06-22 2014-08-21 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 Ａｔｒキナーゼ阻害剤として有用な化合物
EP2723747A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
MX392542B (es) 2011-09-30 2025-03-24 Vertex Pharma Tratamiento del cancer de pancreas y del cancer de pulmon de celulas no pequeñas con inhibidores de atr.
US8853217B2 (en) 2011-09-30 2014-10-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
JP2014528419A (ja) 2011-09-30 2014-10-27 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ａｔｒキナーゼ阻害剤として有用な化合物
WO2013049719A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
HUE046429T2 (hu) 2011-09-30 2020-03-30 Vertex Pharma ATR kináz inhibítoraként használható vegyületek elõállítására szolgáló eljárás
WO2013071085A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
WO2013071094A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2776422A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2013071088A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2776420A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
CN108478577A (zh) 2012-04-05 2018-09-04 沃泰克斯药物股份有限公司 可用作atr激酶抑制剂的化合物及其组合疗法
IN2014KN02601A (OSRAM) 2012-04-24 2015-05-08 Vertex Pharma
US8999632B2 (en) 2012-10-04 2015-04-07 Vertex Pharmaceuticals Incorporated Method for measuring ATR inhibition mediated increases in DNA damage
WO2014062604A1 (en) 2012-10-16 2014-04-24 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
RU2655964C2 (ru) * 2012-11-20 2018-05-30 Спектрум Фармасьютикалз, Инк. Улучшенный способ получения инкапсулированного в липосомы винкристина для терапевтического применения
SMT202000713T1 (it) * 2012-12-07 2021-03-15 Vertex Pharma Pirazolo [1,5-a] pirimidine utili come inibitori dell'atr chinasi per il trattamento di malattie del cancro
CA2895162C (en) * 2012-12-14 2021-03-09 D. Lynn Kirkpatrick Methods and compositions for inhibiting cnksr1
US9663519B2 (en) 2013-03-15 2017-05-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
PL3424920T3 (pl) 2013-10-17 2020-11-16 Vertex Pharmaceuticals Incorporated Kokryształy (S)-N-metylo-8-(1-((2'-metylo-4’,6'-dideutero-[4,5'-bipirymidyn]-6-ylo)amino)propan-2-ylo)chinolino-4-karboksyamidu i ich deuterowane pochodne jako inhibitory DNA-PK
ES2768678T3 (es) 2013-12-06 2020-06-23 Vertex Pharma Compuesto de 2-amino-6-fluoro-N-[5-fluoro-piridin-3-il]pirazolo[1,5-a]pirimidin-3-carboxamida útil como inhibidor de la ATR quinasa, su preparación, diferentes formas sólidas y derivados radiomarcados de las mismas
SG10201902206QA (en) 2014-06-05 2019-04-29 Vertex Pharma Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof
AU2015277212B2 (en) 2014-06-17 2020-07-02 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of Chk1 and ATR inhibitors
TWI700283B (zh) 2014-08-04 2020-08-01 德商拜耳製藥公司 ２-(嗎啉-４-基)-１,７-萘啶
TWI678213B (zh) 2015-07-22 2019-12-01 美商史倍壯製藥公司 用於長春新鹼硫酸鹽脂質體注射之即可使用的調配物
RU2768621C1 (ru) 2015-09-30 2022-03-24 Вертекс Фармасьютикалз Инкорпорейтед Способ лечения рака с использованием комбинации повреждающих днк средств и ингибиторов atr
EP3190103A1 (en) * 2016-01-08 2017-07-12 Rijksuniversiteit Groningen Inhibitors of the pd-1/pd-l1 protein/protein interaction
MA43870A (fr) 2016-01-11 2021-05-26 Celator Pharmaceuticals Inc Inhibition de la protéine associée à l'ataxie télangiectasie et à rad3 (atr)
MX394860B (es) 2016-09-27 2025-03-24 Vertex Pharma Metodo para tratar cancer usando una combinacion de agentes que dañan adn e inhibidores de proteina cinasa dependiente de adn (adn-pk).
MD3558990T2 (ro) * 2016-12-22 2023-02-28 Incyte Corp Derivați tetrahidro imidazo[4,5-c]piridină ca inductori de internalizare a PD-L1
CA3047991A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Bicyclic heteroaromatic compounds as immunomodulators
JOP20190197A1 (ar) 2017-02-24 2019-08-22 Bayer Pharma AG مثبط كيناز ايه تي آر للاستخدام في طريقة لعلاج مرض فرط التكاثر
AR110995A1 (es) 2017-02-24 2019-05-22 Bayer Ag Combinación de inhibidores de quinasa atr con sal de radio-223
WO2018153972A1 (en) 2017-02-24 2018-08-30 Bayer Pharma Aktiengesellschaft Combination of atr kinase inhibitors and antiandrogens
WO2018206547A1 (en) 2017-05-12 2018-11-15 Bayer Pharma Aktiengesellschaft Combination of bub1 and atr inhibitors
US11690911B2 (en) 2017-08-04 2023-07-04 Bayer Aktiengesellschaft Combination of ATR kinase inhibitors and PD-1/PD-L1 inhibitors
EP3461480A1 (en) 2017-09-27 2019-04-03 Onxeo Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer
CA3084863A1 (en) 2017-12-08 2019-06-13 Bayer Aktiengesellschaft Predictive markers for atr kinase inhibitors
WO2019226213A2 (en) 2018-03-08 2019-11-28 Incyte Corporation AMINOPYRAZINE DIOL COMPOUNDS AS PI3K-y INHIBITORS
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
CN113286614A (zh) 2018-09-26 2021-08-20 默克专利股份有限公司 用于治疗癌症的pd-1拮抗剂、atr抑制剂和铂化物质的组合
CA3116234A1 (en) 2018-10-15 2020-04-23 Merck Patent Gmbh Combination therapy utilizing dna alkylating agents and atr inhibitors
US20210369724A1 (en) 2018-10-16 2021-12-02 Bayer Aktiengesellschaft Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds
BR112021008336A2 (pt) 2018-10-30 2021-08-03 Repare Therapeutics Inc. compostos, composições farmacêuticas, e métodos de preparação de compostos e de seu uso como inibidores de atr quinase
SG11202108636SA (en) * 2019-02-11 2021-09-29 Merck Patent Gmbh Indazolyl-isoxazole derivatives for the treatment of diseases such as cancer
CN120247907A (zh) * 2020-05-04 2025-07-04 大塚制药株式会社 Iap拮抗剂化合物和中间体及其合成方法
WO2022099071A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process for making a pd-1/pd-l1 inhibitor and salts and crystalline forms thereof
CN117024413B (zh) * 2023-10-07 2024-01-09 天津匠新致成科技有限公司 3-氨基吡嗪-2-甲酰胺类靶向蛋白水解嵌合体及其制备方法、药物组合物和应用

Family Cites Families (127)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4309430A (en) 1980-06-27 1982-01-05 Merck & Co., Inc. Pyrazinyl-1,2,4-oxadiazole-5-ones, for treatment of edema, and processes for preparing same
US5329012A (en) 1987-10-29 1994-07-12 The Research Foundation Of State University Of New York Bis(acyloxmethyl)imidazole compounds
JP2597917B2 (ja) 1990-04-26 1997-04-09 富士写真フイルム株式会社 新規な色素形成カプラー及びそれを用いたハロゲン化銀カラー写真感光材料
JP2002241379A (ja) 1997-03-21 2002-08-28 Dainippon Pharmaceut Co Ltd ３−オキサジアゾリルキノキサリン誘導体
KR20010071936A (ko) 1998-07-16 2001-07-31 시오노 요시히코 항종양 활성을 갖는 피리미딘 유도체
US6660753B2 (en) 1999-08-19 2003-12-09 Nps Pharmaceuticals, Inc. Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
ATE384704T1 (de) 1999-12-17 2008-02-15 Novartis Vaccines & Diagnostic Pyrazin-basierte hemmer der glycogen-synthase- kinase 3
US6849660B1 (en) 2000-08-01 2005-02-01 Isis Pharmaceuticals, Inc. Antimicrobial biaryl compounds
EP1217000A1 (en) 2000-12-23 2002-06-26 Aventis Pharma Deutschland GmbH Inhibitors of factor Xa and factor VIIa
CA2446380A1 (en) 2001-05-08 2002-11-14 Yale University Proteomimetic compounds and methods
SE0102438D0 (sv) 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
SE0102439D0 (sv) 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
DK1446387T3 (da) 2001-11-21 2009-12-21 Pharmacia & Upjohn Co Llc Substituerede aryl, 1,4-pyrazinderivater
US6992087B2 (en) 2001-11-21 2006-01-31 Pfizer Inc Substituted aryl 1,4-pyrazine derivatives
WO2003066629A2 (en) 2002-02-06 2003-08-14 Vertex Pharmaceuticals Incorporated Heteroaryl compounds useful as inhibitors of gsk-3
OA12792A (en) 2002-03-13 2006-07-10 Janssen Pharmaceutica Nv Sulfonyl-derivatives as novel inhibitors of histone deacetylase.
GB0206860D0 (en) 2002-03-22 2002-05-01 Glaxo Group Ltd Compounds
TWI319387B (en) 2002-04-05 2010-01-11 Astrazeneca Ab Benzamide derivatives
GB0209715D0 (en) 2002-04-27 2002-06-05 Astrazeneca Ab Chemical compounds
JP4901102B2 (ja) * 2002-05-03 2012-03-21 エクセリクシス， インク． プロテインキナーゼモジュレーターおよびその使用方法
US7704995B2 (en) 2002-05-03 2010-04-27 Exelixis, Inc. Protein kinase modulators and methods of use
IL164209A0 (en) 2002-05-31 2005-12-18 Eisai Co Ltd Pyrazole derivatives and pharmaceutical compositions containing the same
US7015227B2 (en) 2002-06-21 2006-03-21 Cgi Pharmaceuticals, Inc. Certain amino-substituted monocycles as kinase modulators
WO2004033431A2 (en) 2002-10-04 2004-04-22 Arena Pharmaceuticals, Inc. Hydroxypyrazoles for use against metabolic-related disorders
SE0203752D0 (sv) 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
SE0203754D0 (sv) 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
BRPI0408251A (pt) 2003-03-11 2006-03-01 Pfizer Prod Inc compostos de pirazina como inibidores do fator de crescimento transformante (tgf)
JP2006520794A (ja) 2003-03-21 2006-09-14 スミスクライン ビーチャム コーポレーション 化合物
US20060293339A1 (en) 2003-03-24 2006-12-28 Chakravarty Prasun K Biaryl substituted 6-membered heterocycles as sodium channel blockers
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
EP1625123A4 (en) 2003-05-15 2007-08-29 Merck & Co Inc 3- (2-AMINO-1-AZACYCLYL) -5-ARYL-1,2,4-OXADIAZOLE AS S1P RECEPTOR AGONISTS
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
WO2005034952A2 (en) 2003-10-07 2005-04-21 The Feinstein Institute For Medical Research Isoxazole and isothiazole compounds useful in the treatment of inflammation
EP1715867A4 (en) 2004-02-12 2009-04-15 Merck & Co Inc BIPYRIDYLAMIDE AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR-5
EP1773807A2 (en) 2004-06-14 2007-04-18 Takeda San Diego, Inc. Kinase inhibitors
US7626021B2 (en) 2004-07-27 2009-12-01 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
CA2573573A1 (en) 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
WO2006053342A2 (en) 2004-11-12 2006-05-18 Osi Pharmaceuticals, Inc. Integrin antagonists useful as anticancer agents
CN101098872B (zh) 2004-11-22 2012-09-05 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的吡咯并吡嗪和吡唑并吡嗪
GB0428235D0 (en) 2004-12-23 2005-01-26 Glaxo Group Ltd Novel compounds
BRPI0519508A2 (pt) 2004-12-27 2009-03-17 Alcon Inc análogos de aminopirazina para tratamento de glaucoma e outras doenças ou condições mediadas por rho cinase
GB0500492D0 (en) 2005-01-11 2005-02-16 Cyclacel Ltd Compound
US7622583B2 (en) 2005-01-14 2009-11-24 Chemocentryx, Inc. Heteroaryl sulfonamides and CCR2
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
KR20070107046A (ko) 2005-02-16 2007-11-06 쉐링 코포레이션 Ｃｘｃｒ3 길항제 활성을 지닌 헤테로사이클릭 치환된피페라진
ATE524467T1 (de) 2005-04-25 2011-09-15 Merck Patent Gmbh Neuartige aza-heterozyklen als kinase-inhibitoren
WO2007015632A1 (en) 2005-08-04 2007-02-08 Cgk Co., Ltd. Atm and atr inhibitor
AR056786A1 (es) 2005-11-10 2007-10-24 Smithkline Beecham Corp Compuesto de 1h- imidazo ( 4,5-c) piridin-2-ilo, composicion farmaceutica que lo comprende, procedimiento para preparar dicha composicion, su uso para preparar unmedicamento, uso de una combinacion que omprende al compuesto y al menos un agente antineoplasico para preparar un medicamento y dicha com
RU2396269C2 (ru) 2005-12-01 2010-08-10 Ф.Хоффманн-Ля Рош Аг Производные гетероарилзамещенного пиперидина в качестве ингибиторов печеночной карнитин пальмитоилтрансферазы (l-cpt1)
EP1970377A4 (en) 2005-12-09 2013-02-27 Meiji Seika Kaisha LINCOMYCIN DERIVATIVE AND ANTIBACTERIAL AGENT CONTAINING THIS AS AN ACTIVE SUBSTANCE
EP1962853A1 (en) 2005-12-22 2008-09-03 Alcon Research, Ltd. (indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)- pyrazines for treating rho kinase-mediated diseases and conditions
ITMI20060311A1 (it) 2006-02-21 2007-08-22 Btsr Int Spa Dispositivo perfezionato di alimentazione di filo o filatio ad una macchina tessile e metodo per attuare tale alimentazione
GB0603684D0 (en) 2006-02-23 2006-04-05 Novartis Ag Organic compounds
WO2007096764A2 (en) 2006-02-27 2007-08-30 Glenmark Pharmaceuticals S.A. Bicyclic heteroaryl derivatives as cannabinoid receptor modulators
TW200800203A (en) 2006-03-08 2008-01-01 Astrazeneca Ab New use
WO2007111904A2 (en) 2006-03-22 2007-10-04 Vertex Pharmaceuticals Incorporated C-met protein kinase inhibitors for the treatment of proliferative disorders
CA2648124A1 (en) 2006-03-31 2007-11-08 Schering Corporation Kinase inhibitors
US9216963B2 (en) 2006-06-22 2015-12-22 Medibeacon Inc. Pyrazine derivatives with extended conjugation and methods of using the same in optical applications
BRPI0713328A2 (pt) 2006-06-22 2012-10-30 Biovitrum Ab derivados de piridina e pirazina como inibidores de cinase mnk
AU2007302263A1 (en) 2006-09-29 2008-04-03 Novartis Ag Pyrazolopyrimidines as P13K lipid kinase inhibitors
GB0619342D0 (en) 2006-09-30 2006-11-08 Vernalis R&D Ltd New chemical compounds
EP2074096B1 (en) 2006-10-04 2012-06-27 F. Hoffmann-La Roche AG 3-pyridinecarboxamide and 2-pyrazinecarboxamide derivatives as hdl-cholesterol raising agents
EP2081928B1 (en) 2006-11-10 2014-02-26 Bristol-Myers Squibb Company Pyrrolo-pyridine kinase inhibitors
US20090062273A1 (en) 2006-12-15 2009-03-05 Ingo Hartung 3-H-pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same.
US7687522B2 (en) 2006-12-20 2010-03-30 Amgen Inc. Substituted pyridines and pyrimidines and their use in treatment of cancer
PE20121126A1 (es) 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
GB0625659D0 (en) 2006-12-21 2007-01-31 Cancer Rec Tech Ltd Therapeutic compounds and their use
US8314087B2 (en) 2007-02-16 2012-11-20 Amgen Inc. Nitrogen-containing heterocyclyl ketones and methods of use
CA2679659C (en) 2007-03-01 2016-01-19 Novartis Ag Pim kinase inhibitors and methods of their use
AU2008235089B8 (en) 2007-04-10 2014-04-10 Bayer Intellectual Property Gmbh Insecticidal aryl isoxazoline derivatives
EP2150255A4 (en) 2007-05-10 2011-10-05 Glaxosmithkline Llc CHINOXALINE DERIVATIVES AS P13 KINASE INHIBITORS
PE20090717A1 (es) 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
UY31137A1 (es) 2007-06-14 2009-01-05 Smithkline Beecham Corp Derivados de quinazolina como inhibidores de la pi3 quinasa
US20100190980A1 (en) 2007-06-21 2010-07-29 Taisho Pharmaceutical Co., Ltd Pyrazinamide compound
EA201070058A1 (ru) 2007-06-26 2010-06-30 Лексикон Фармасьютикалз, Инк. Способы лечения опосредованных серотонином заболеваний и расстройств
GB0713259D0 (en) 2007-07-09 2007-08-15 Astrazeneca Ab Pyrazine derivatives 954
SG187396A1 (en) 2007-07-19 2013-02-28 Lundbeck & Co As H 5-membered heterocyclic amides and related compounds
RU2474580C2 (ru) 2007-07-19 2013-02-10 Шеринг Корпорейшн Гетероциклические амидные соединения как ингибиторы протеинкиназ
EA201000113A1 (ru) 2007-08-01 2010-08-30 Пфайзер Инк. Пиразольные соединения
WO2009024825A1 (en) 2007-08-21 2009-02-26 Astrazeneca Ab 2-pyrazinylbenzimidazole derivatives as receptor tyrosine kinase inhibitors
EP2203436A1 (en) 2007-09-17 2010-07-07 Neurosearch A/S Pyrazine derivatives and their use as potassium channel modulators
JP2011500778A (ja) 2007-10-25 2011-01-06 アストラゼネカ・アクチエボラーグ ピリジン及びピラジン誘導体−０８３
ATE517107T1 (de) 2008-02-25 2011-08-15 Hoffmann La Roche Pyrrolopyrazinkinaseinhibitoren
EP2250172B1 (en) 2008-02-25 2011-08-31 F. Hoffmann-La Roche AG Pyrrolopyrazine kinase inhibitors
RU2503676C2 (ru) 2008-02-25 2014-01-10 Ф.Хоффманн-Ля Рош Аг Пирролопиразиновые ингибиторы киназы
WO2009106444A1 (en) 2008-02-25 2009-09-03 F. Hoffmann-La Roche Ag Pyrrolopyrazine kinase inhibitors
TW200940537A (en) 2008-02-26 2009-10-01 Astrazeneca Ab Heterocyclic urea derivatives and methods of use thereof
WO2009152087A1 (en) 2008-06-10 2009-12-17 Plexxikon, Inc. Bicyclic heteroaryl compounds and methods for kinase modulation, and indications therefor
GB0814364D0 (en) 2008-08-05 2008-09-10 Eisai London Res Lab Ltd Diazaindole derivatives and their use in the inhibition of c-Jun N-terminal kinase
MX2011004188A (es) 2008-10-21 2011-06-09 Vertex Pharma Inhibidores de la proteina cinasa c-met.
KR101712576B1 (ko) 2008-11-10 2017-03-06 버텍스 파마슈티칼스 인코포레이티드 Ａｔｒ 키나제의 억제제로서 유용한 화합물
AU2009324894B2 (en) 2008-11-25 2015-04-09 University Of Rochester MLK inhibitors and methods of use
AU2009324210A1 (en) 2008-12-05 2010-06-10 F. Hoffmann-La Roche Ag Pyrrolopyrazinyl urea kinase inhibitors
PL2376485T3 (pl) 2008-12-19 2018-05-30 Vertex Pharmaceuticals Incorporated Pochodne pirazyny użyteczne jako inhibitory kinazy ATR
ES2567047T3 (es) 2008-12-23 2016-04-19 Abbvie Inc. Derivados de pirimidina anti-virales
SG173639A1 (en) 2009-02-11 2011-09-29 Sunovion Pharmaceuticals Inc Histamine h3 inverse agonists and antagonists and methods of use thereof
EP2411007A4 (en) 2009-03-27 2012-12-05 Uab Research Foundation MODULATION OF IRES-MEDIATED TRANSLATION
JP2012533551A (ja) 2009-07-15 2012-12-27 アボット・ラボラトリーズ ピロロピラジン系キナーゼ阻害薬
US8518945B2 (en) 2010-03-22 2013-08-27 Hoffmann-La Roche Inc. Pyrrolopyrazine kinase inhibitors
EP2556060A1 (en) 2010-04-08 2013-02-13 Ah Usa 42 Llc Substituted 3,5- diphenyl-isoxazoline derivatives as insecticides and acaricides
ES2602475T3 (es) 2010-04-15 2017-02-21 Tracon Pharmaceuticals, Inc. Potenciación de la actividad anticáncer por terapia de combinación con inhibidores de la vía BER
US8969356B2 (en) 2010-05-12 2015-03-03 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
CA2798763A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
MX2012013082A (es) 2010-05-12 2013-05-09 Vertex Pharma Derivados de 2-aminopiridina utiles como iinhibidores de cinasa atr.
EP2569287B1 (en) 2010-05-12 2014-07-09 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
WO2011143419A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Pyrazines useful as inhibitors of atr kinase
WO2011143423A2 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
CN103003281A (zh) 2010-05-20 2013-03-27 弗·哈夫曼-拉罗切有限公司 作为JAK和SYK抑制剂的吡咯并[2，3-b]吡嗪-7-甲酰胺衍生物和它们的用途
TWI496785B (zh) 2010-05-20 2015-08-21 Hoffmann La Roche 吡咯并吡激酶抑制劑
MX2013000103A (es) 2010-06-23 2013-06-13 Vertex Pharma Derivados de pirrolo-pirazina utiles como inhibidores de cinasa art.
CN102311396B (zh) 2010-07-05 2015-01-07 暨南大学 一种吡嗪类衍生物和其制备方法及在制药中的应用
EP2407478A1 (en) 2010-07-14 2012-01-18 GENETADI Biotech, S.L. New cyclotetrapeptides with pro-angiogenic properties
KR20140027974A (ko) 2011-04-05 2014-03-07 버텍스 파마슈티칼스 인코포레이티드 Ｔｒａ 키나제의 억제제로서 유용한 아미노피라진 화합물
WO2012158785A1 (en) 2011-05-17 2012-11-22 Principia Biopharma Inc. Azaindole derivatives as tyrosine kinase inhibitors
JP2014520161A (ja) 2011-06-22 2014-08-21 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 Ａｔｒキナーゼ阻害剤として有用な化合物
EP2723747A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
JP2014517079A (ja) 2011-06-22 2014-07-17 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 Ａｔｒキナーゼ阻害剤として有用な化合物
US8853217B2 (en) 2011-09-30 2014-10-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
HUE046429T2 (hu) 2011-09-30 2020-03-30 Vertex Pharma ATR kináz inhibítoraként használható vegyületek elõállítására szolgáló eljárás
WO2013049719A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
JP2014528419A (ja) 2011-09-30 2014-10-27 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ａｔｒキナーゼ阻害剤として有用な化合物
MX392542B (es) 2011-09-30 2025-03-24 Vertex Pharma Tratamiento del cancer de pancreas y del cancer de pulmon de celulas no pequeñas con inhibidores de atr.
WO2013071094A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2776422A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2013071088A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2776420A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
WO2013071085A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase

Also Published As

Publication number Publication date
US8877759B2 (en) 2014-11-04
WO2012138938A1 (en) 2012-10-11
KR20140027974A (ko) 2014-03-07
MX2013011450A (es) 2014-02-03
EP2694498A1 (en) 2014-02-12
AU2012240030A1 (en) 2013-10-24
IL228715A0 (en) 2013-12-31
JP2014510151A (ja) 2014-04-24
CA2832100A1 (en) 2012-10-11
EP2694498B1 (en) 2016-03-30
CN103562204A (zh) 2014-02-05
US20130095193A1 (en) 2013-04-18

Similar Documents

Publication Publication Date Title
ZA201307332B (en) Aminopyrazine compounds useful as inhibitors of tra kinase
IL263262B (en) Atr kinase inhibitor compounds, preparations containing them, their uses and methods for their preparation
IL265007B (en) Pyrazolopyrimidine compounds as kinase inhibitors
AP2013007252A0 (en) Heterocyclic compounds as kinase inhibitors
IL238728A0 (en) Pyrrolopyrimidine compounds as kinase inhibitors
ZA201402625B (en) Processes for making compounds useful as inhibitors of atr kinase
SG10201605196PA (en) Novel Inhibitor Compounds Of Phosphodiesterase Type 10A
ZA201500762B (en) Novel pyrrolopyrimidine compounds as inhibitors of protein kinases
ZA201309128B (en) Macrocyclic compounds as protein kinase inhibitors
PL2693881T3 (pl) Podstawione analogi N-fenylopirymidyno-2-aminy jako inhibitory kinazy AXL
IL228108A0 (en) Triazolopyridine compounds as pim kinase inhibitors
IL228103A0 (en) Amino-quinolines as kinase inhibitors
SI2880035T1 (sl) Nove spojine pirolopirimidina kot inhibitorji protein kinaz
ZA201306025B (en) Phosphorus containing compounds as protein kinase inhibitors
EP2782579A4 (en) PYRAZINKINASEINHIBITOREN
EP2758387A4 (en) Pyridine compounds as kinase inhibitors
IL236946A0 (en) A10-type phosphodiesterase inhibitory compounds