SG11201407238VA - 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof - Google Patents
5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereofInfo
- Publication number
- SG11201407238VA SG11201407238VA SG11201407238VA SG11201407238VA SG11201407238VA SG 11201407238V A SG11201407238V A SG 11201407238VA SG 11201407238V A SG11201407238V A SG 11201407238VA SG 11201407238V A SG11201407238V A SG 11201407238VA SG 11201407238V A SG11201407238V A SG 11201407238VA
- Authority
- SG
- Singapore
- Prior art keywords
- international
- lllll
- sutton
- surrey
- inhibitor
- Prior art date
Links
- 230000001225 therapeutic effect Effects 0.000 title abstract 3
- YBYYWUUUGCNAHQ-UHFFFAOYSA-N 5-[[4-(morpholin-2-ylmethylamino)-5-(trifluoromethyl)pyridin-2-yl]amino]pyrazine-2-carbonitrile Chemical compound C1=C(NCC2OCCNC2)C(C(F)(F)F)=CN=C1NC1=CN=C(C#N)C=N1 YBYYWUUUGCNAHQ-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 abstract 5
- 108091000080 Phosphotransferase Proteins 0.000 abstract 4
- 102000020233 phosphotransferase Human genes 0.000 abstract 4
- 239000003795 chemical substances by application Substances 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 230000006870 function Effects 0.000 abstract 3
- 108010022394 Threonine synthase Proteins 0.000 abstract 2
- 102000005497 Thymidylate Synthase Human genes 0.000 abstract 2
- 102000052567 Anaphase-Promoting Complex-Cyclosome Apc1 Subunit Human genes 0.000 abstract 1
- 108700004581 Anaphase-Promoting Complex-Cyclosome Apc1 Subunit Proteins 0.000 abstract 1
- 102000003915 DNA Topoisomerases Human genes 0.000 abstract 1
- 108090000323 DNA Topoisomerases Proteins 0.000 abstract 1
- 230000005778 DNA damage Effects 0.000 abstract 1
- 231100000277 DNA damage Toxicity 0.000 abstract 1
- 230000005971 DNA damage repair Effects 0.000 abstract 1
- 239000012623 DNA damaging agent Substances 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- LELOWRISYMNNSU-UHFFFAOYSA-N Hydrocyanic acid Natural products N#C LELOWRISYMNNSU-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- -1 TFM com pounds Chemical class 0.000 abstract 1
- 102000007537 Type II DNA Topoisomerases Human genes 0.000 abstract 1
- 108010046308 Type II DNA Topoisomerases Proteins 0.000 abstract 1
- 230000001668 ameliorated effect Effects 0.000 abstract 1
- 230000000340 anti-metabolite Effects 0.000 abstract 1
- 229940100197 antimetabolite Drugs 0.000 abstract 1
- 239000002256 antimetabolite Substances 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 230000011278 mitosis Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- 230000005855 radiation Effects 0.000 abstract 1
- 102220240796 rs553605556 Human genes 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61K31/70—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
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261647200P | 2012-05-15 | 2012-05-15 | |
PCT/GB2013/051233 WO2013171470A1 (en) | 2012-05-15 | 2013-05-14 | 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof |
Publications (1)
Publication Number | Publication Date |
---|---|
SG11201407238VA true SG11201407238VA (en) | 2014-12-30 |
Family
ID=48468659
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
SG11201407238VA SG11201407238VA (en) | 2012-05-15 | 2013-05-14 | 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof |
Country Status (20)
Country | Link |
---|---|
US (3) | US9663503B2 (zh) |
EP (2) | EP2855448B1 (zh) |
JP (2) | JP6027230B2 (zh) |
KR (6) | KR102090792B1 (zh) |
CN (2) | CN106279142B (zh) |
AU (2) | AU2013261605B2 (zh) |
BR (1) | BR112014026801B1 (zh) |
CA (1) | CA2870837C (zh) |
DK (1) | DK2855448T3 (zh) |
ES (1) | ES2624307T3 (zh) |
HK (2) | HK1203529A1 (zh) |
IL (1) | IL235133A (zh) |
IN (1) | IN2014DN09221A (zh) |
MX (1) | MX358819B (zh) |
NZ (1) | NZ702050A (zh) |
PL (1) | PL2855448T3 (zh) |
RU (1) | RU2659786C2 (zh) |
SG (1) | SG11201407238VA (zh) |
WO (1) | WO2013171470A1 (zh) |
ZA (1) | ZA201408452B (zh) |
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BR112014010938A2 (pt) | 2011-11-09 | 2017-05-16 | Cancer Res Tech Ltd | compostos de 5-(piridin-2-il-amino)-pirazina-2-carbonitrila e seu uso terapêutico |
KR102090792B1 (ko) | 2012-05-15 | 2020-03-18 | 캔써 리서치 테크놀로지 리미티드 | 5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴 및 그의 치료적 용도 |
CN104903325B (zh) | 2012-12-07 | 2017-10-20 | 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 |
WO2014143240A1 (en) | 2013-03-15 | 2014-09-18 | Vertex Pharmaceuticals Incorporated | Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase |
CN105934435B (zh) | 2013-12-06 | 2019-02-22 | 沃泰克斯药物股份有限公司 | 用作atr激酶抑制剂的化合物,其制备,及其放射性标记的衍生物 |
KR102575125B1 (ko) | 2014-06-05 | 2023-09-07 | 버텍스 파마슈티칼스 인코포레이티드 | Atr 키나제의 저해제로서 유용한 2-아미노-6-플루오로-n-[5-플루오로-피리딘-3-일]-피라졸로[1,5-a]피리미딘-3-카복스아미드 화합물의 방사성표지된 유도체, 상기 화합물의 제조 및 이의 다양한 고체 형태 |
PL3157566T3 (pl) * | 2014-06-17 | 2019-10-31 | Vertex Pharma | Metoda leczenia nowotworu przy użyciu kombinacji inhibitorów chk1 i atr |
EP3355926A4 (en) | 2015-09-30 | 2019-08-21 | Vertex Pharmaceuticals Inc. | METHOD FOR THE TREATMENT OF CANCER WITH A COMBINATION OF DNA DAMAGING AGENTS AND ATR INHIBITORS |
WO2018094325A1 (en) * | 2016-11-18 | 2018-05-24 | The Trustees Of Columbia University In The City Of New York | Therapeutic modulation of oncogenes by pharmacologic top2 targeting for cancer |
US20200108074A1 (en) * | 2017-03-31 | 2020-04-09 | Seattle Genetics, Inc. | Combinations of chk1- and wee1- inhibitors |
KR102645511B1 (ko) * | 2017-04-10 | 2024-03-08 | 시에라 온코로지 엘엘씨 | 종양 성장을 저해하는 CHK1(SRA737)/PARPi 조합 방법 |
WO2018191299A1 (en) * | 2017-04-10 | 2018-10-18 | Sierra Oncology, Inc. | Chk1(sra737)wee1 inhibitor combination methods of inhibiting tumor growth |
WO2018222970A1 (en) * | 2017-06-01 | 2018-12-06 | Sierra Oncology, Inc. | Biomarkers and patient selection strategies |
CN107266897B (zh) * | 2017-08-04 | 2019-05-14 | 上海跃贝新材料科技股份有限公司 | 一种低粘度矿物增强pc/pet合金材料及其制备方法 |
JP2021514979A (ja) * | 2018-02-26 | 2021-06-17 | シエラ オンコロジー, インコーポレイテッド | Chk1阻害剤を含む癌の治療方法 |
CA3135165A1 (en) * | 2019-03-28 | 2020-10-01 | Sierra Oncology, Inc. | Methods of treating cancer with chk1 inhibitors |
MX2021013905A (es) * | 2019-05-14 | 2022-05-18 | Sierra Oncology Inc | Métodos de tratamiento del cáncer mediante el uso de inhibidores de chk1. |
CN110872277B (zh) * | 2019-11-14 | 2021-06-04 | 浙江大学 | N-取代芳环-2-氨基嘧啶类化合物及用途 |
CN110684083B (zh) * | 2019-12-06 | 2020-05-15 | 北京诺赛启研再生医学研究院有限公司 | 抑制黑色素合成的偶联物ii及其在药品和化妆品中的应用 |
CN110680928B (zh) * | 2019-12-06 | 2020-04-28 | 深圳前海港影生物科技有限公司 | 抑制黑色素合成的偶联物及其在药品和化妆品中的应用 |
TW202204348A (zh) * | 2020-04-07 | 2022-02-01 | 美商西爾拉癌症醫學公司 | Chk1抑制劑之合成方法 |
CN117858870A (zh) * | 2021-08-17 | 2024-04-09 | 葛兰素史密斯克莱知识产权(第3号)有限公司 | P2x3拮抗剂的制备 |
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GB0803018D0 (en) | 2008-02-19 | 2008-03-26 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
BR112014010938A2 (pt) | 2011-11-09 | 2017-05-16 | Cancer Res Tech Ltd | compostos de 5-(piridin-2-il-amino)-pirazina-2-carbonitrila e seu uso terapêutico |
KR102090792B1 (ko) | 2012-05-15 | 2020-03-18 | 캔써 리서치 테크놀로지 리미티드 | 5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴 및 그의 치료적 용도 |
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2013
- 2013-05-14 KR KR1020147031572A patent/KR102090792B1/ko active IP Right Grant
- 2013-05-14 WO PCT/GB2013/051233 patent/WO2013171470A1/en active Application Filing
- 2013-05-14 ES ES13723910.9T patent/ES2624307T3/es active Active
- 2013-05-14 CN CN201610652725.8A patent/CN106279142B/zh active Active
- 2013-05-14 JP JP2015512120A patent/JP6027230B2/ja active Active
- 2013-05-14 KR KR1020217012299A patent/KR102341637B1/ko active IP Right Grant
- 2013-05-14 PL PL13723910T patent/PL2855448T3/pl unknown
- 2013-05-14 KR KR1020247004407A patent/KR20240023685A/ko active Application Filing
- 2013-05-14 KR KR1020207007411A patent/KR102246265B1/ko active IP Right Grant
- 2013-05-14 BR BR112014026801-0A patent/BR112014026801B1/pt active IP Right Grant
- 2013-05-14 NZ NZ702050A patent/NZ702050A/en unknown
- 2013-05-14 DK DK13723910.9T patent/DK2855448T3/en active
- 2013-05-14 CN CN201380025541.3A patent/CN104302635B/zh active Active
- 2013-05-14 EP EP13723910.9A patent/EP2855448B1/en active Active
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