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)
Abstract
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 21 November 2013 (21.11.2013) WIPOIPCT (10) International Publication Number WO 2013/171470 A1 (51) International Patent Classification: C07D 401/12 (2006.01) A61P 35/00 (2006.01) A61K31/506 (2006.01) (21) International Application Number: PCT/GB2013/051233 (22) International Filing Date: 14 May 2013 (14.05.2013) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 61/647,200 15 May 2012 (15.05.2012) US (71) Applicant: CANCER RESEARCH TECHNOLOGY LIMITED [GB/GB]; Angel Building, 407 St John Street, London Greater London EC IV 4AD (GB). (72) Inventors: COLLINS, Ian; The Institute of Cancer Re search, 15 Cotswold Road, Sutton Surrey SM2 5NG (GB). MATTHEWS, Thomas Peter; The Institute of Cancer Re- search, 15 Cotswold Road, Sutton Surrey SM2 5NG (GB). FARIA DA FONSECA MCHARDY, Tatiana; The Insti- ~~ tute of Cancer Research, 15 Cotswold Road, Sutton Surrey = SM2 5NG (GB). OSBORNE, James; Biofocus, Chester- _ ford Research Park, Chesterford Park, Saffron Walden Es- sex CB10 1XL (GB). LAINCHBURY, Michael; Argenta Discovery 2009 Limited, 8-9 Spire Green Centre, Flex [Continued on next page] (54) Title: 5-[[4-[[MORPHOLIN-2-YL]METHYLAMINO]-5-(TRIFLUOROMETHYL)-2-PYRIDYL]AMINO]PYRAZINE-2- = CARBONITRILE AND THERAPEUTIC USES THEREOF (57) Abstract: The present invention pertains gen erally to the field of therapeutic compounds. More specifically the present invention pertains to 5-[[4- [ [morpholin-2 -yljmethylamino] - - 5 (trifluoro - methyl)-2-pyridyl]amino]pyrazine-2-carbonitrile compounds (referred to herein as \"TFM com pounds\") which, inter alia, inhibit Checkpoint Kinase (CHK1) 1 kinase function. The present in vention also pertains to pharmaceutical composi tions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the in hibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., op tionally in combination with another agent, for ex ample, (a) DNA a topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or a thymidylate synthase (TS) inhibitor; (d) a mi crotubule targeted agent; (e) ionising radiation; (f) an inhibitor of a mitosis regulator or a mitotic checkpoint regulator; (g) an inhibitor of a DNA damage signal transducer; or (h) an inhibitor of a DNA damage repair enzyme. CJ o & Meadow, Harlow Essex CM 19 5TR (GB). WALTON, Mi chael Ian; The Institute of Cancer Research, 15 Cotswold Road, Sutton Surrey SM2 5NG (GB). GARRETT, Michelle Dawn; The Institute of Cancer Research, 15 Cotswold Road, Sutton Surrey SM2 5NG (GB). (74) Agent: WYTENBURG, Wilhelmus; Mewburn Ellis LLP, 33 Gutter Lane, London Greater London EC2V 8AS (GB). (81) Designated States (unless otherwise indicated, for every kind of national protection available)'. AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available)'. ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, WO 2013/171470 Al I lllll llllllll II llllll III lllll lllll lllll III III III lllll lllll lllll lllll llll lllllll llll llll llll TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, Published: ML, MR, NE, SN, TD, TG). — -with international search report (Art. 21(3)) Declarations under Rule 4.17: — of inventorship (Rule 4.17 (iv))
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 (en) |
EP (2) | EP3210980B1 (en) |
JP (2) | JP6027230B2 (en) |
KR (6) | KR102635954B1 (en) |
CN (2) | CN106279142B (en) |
AU (2) | AU2013261605B2 (en) |
BR (1) | BR112014026801B1 (en) |
CA (1) | CA2870837C (en) |
DK (1) | DK2855448T3 (en) |
ES (1) | ES2624307T3 (en) |
HK (2) | HK1203529A1 (en) |
IL (1) | IL235133A (en) |
IN (1) | IN2014DN09221A (en) |
MX (1) | MX358819B (en) |
NZ (1) | NZ702050A (en) |
PL (1) | PL2855448T3 (en) |
RU (1) | RU2659786C2 (en) |
SG (1) | SG11201407238VA (en) |
WO (1) | WO2013171470A1 (en) |
ZA (1) | ZA201408452B (en) |
Families Citing this family (23)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2849566C (en) | 2011-11-09 | 2021-02-09 | Cancer Research Technology Limited | 5-(pyridin-2-yl-amino)-pyrazine-2-carbonitrile compounds and their therapeutic use |
ES2624307T3 (en) * | 2012-05-15 | 2017-07-13 | Cancer Research Technology Ltd | 5 - [[4 - [[Morpholin-2-yl] methylamino] -5- (trifluoromethyl) -2-pyridyl] amino] pyrazin-2-carbonitrile and therapeutic uses thereof |
ES2946360T3 (en) | 2012-12-07 | 2023-07-17 | Vertex Pharma | Pyrazolo[1,5-a]pyrimidines useful as ATR kinase inhibitors for the treatment of cancer diseases |
WO2014143240A1 (en) | 2013-03-15 | 2014-09-18 | Vertex Pharmaceuticals Incorporated | Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase |
RU2687276C2 (en) | 2013-12-06 | 2019-05-13 | Вертекс Фармасьютикалз Инкорпорейтед | Compounds suitable for use as atr kinase inhibitors |
LT3152212T (en) | 2014-06-05 | 2020-05-11 | Vertex Pharmaceuticals Inc. | 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 |
SG11201610500WA (en) * | 2014-06-17 | 2017-01-27 | Vertex Pharma | Method for treating cancer using a combination of chk1 and atr inhibitors |
CA3000684A1 (en) | 2015-09-30 | 2017-04-06 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using 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 |
CA3058457A1 (en) * | 2017-03-31 | 2018-10-04 | Seattle Genetics, Inc. | Combinations of chk1- and wee1 - inhibitors |
EP3609884A4 (en) * | 2017-04-10 | 2021-01-06 | Sierra Oncology, Inc. | Chk1 (sra737)/parpi combination methods of inhibiting tumor growth |
WO2018191299A1 (en) * | 2017-04-10 | 2018-10-18 | Sierra Oncology, Inc. | Chk1(sra737)wee1 inhibitor combination methods of inhibiting tumor growth |
CA3065803A1 (en) * | 2017-06-01 | 2018-12-06 | Sierra Oncology, Inc. | Biomarkers and patient selection strategies |
CN107266897B (en) * | 2017-08-04 | 2019-05-14 | 上海跃贝新材料科技股份有限公司 | A kind of low viscosity mineral enhancing PC/PET alloy material and preparation method thereof |
MX2020008881A (en) * | 2018-02-26 | 2021-01-08 | Sierra Oncology Inc | Methods of treatment of cancer comprising chk1 inhibitors. |
JP2022523028A (en) * | 2019-01-25 | 2022-04-21 | ヌメディー, インコーポレイテッド | Methods for treating idiopathic pulmonary fibrosis |
US20220184091A1 (en) * | 2019-03-28 | 2022-06-16 | Sierra Oncology, Inc. | Methods of Treating Cancer with Chk1 Inhibitors |
KR20220066005A (en) * | 2019-05-14 | 2022-05-23 | 시에라 온코로지, 인코퍼레이티드 | Methods for treating cancer using CHK1 inhibitors |
CN110872277B (en) * | 2019-11-14 | 2021-06-04 | 浙江大学 | N-substituted aromatic ring-2-aminopyrimidine compounds and application thereof |
CN110680928B (en) * | 2019-12-06 | 2020-04-28 | 深圳前海港影生物科技有限公司 | Conjugate for inhibiting melanin synthesis and application thereof in medicines and cosmetics |
CN110684083B (en) * | 2019-12-06 | 2020-05-15 | 北京诺赛启研再生医学研究院有限公司 | Conjugate II for inhibiting melanin synthesis and application thereof in medicines and cosmetics |
TW202204348A (en) * | 2020-04-07 | 2022-02-01 | 美商西爾拉癌症醫學公司 | Methods for synthesis of chk1 inhibitors |
WO2023021328A1 (en) * | 2021-08-17 | 2023-02-23 | Bellus Health Cough Inc. | Preparation of a p2x3 antagonist |
Family Cites Families (30)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3773778A (en) | 1972-01-24 | 1973-11-20 | Squibb & Sons Inc | Sulfur derivatives of pyrazolo (3,4-b)pyridines |
IL112248A0 (en) | 1994-01-25 | 1995-03-30 | Warner Lambert Co | Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them |
SK398A3 (en) | 1995-07-06 | 1998-07-08 | Novartis Ag | Pyrrolopyrimidines and processes for the preparation thereof |
US7271261B2 (en) | 2001-10-19 | 2007-09-18 | Ortho-Mcneil Pharmaceutical, Inc. | Substituted benzimidazoles and imidazo-[4,5]-pyridines |
MXPA04003954A (en) | 2001-10-26 | 2004-11-29 | Aventis Pharma Inc | Benzimidazoles and analogues and their use as protein kinases inhibitors. |
CA2464934A1 (en) | 2001-10-31 | 2003-05-08 | Bayer Healthcare Ag | Pyrimido [4,5-b] indole derivatives |
JP4901102B2 (en) | 2002-05-03 | 2012-03-21 | エクセリクシス, インク. | Protein kinase modulator and method of use thereof |
WO2003101444A1 (en) * | 2002-05-29 | 2003-12-11 | Millennium Pharmaceuticals, Inc. | Diarylurea compounds and derivatives as chk-1 inhibitors for the treatment of cancer |
EP1651648A4 (en) | 2003-07-29 | 2009-09-02 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
CA2542105C (en) | 2003-10-08 | 2011-08-02 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
DE602004022318D1 (en) | 2003-10-14 | 2009-09-10 | Supergen Inc | PROTEIN KINASE INHIBITORS |
CA2542329A1 (en) | 2003-10-16 | 2005-04-28 | Chiron Corporation | 2,6-disubstituted quinazolines, quinoxalines, quinolines and isoquinolines as inhibitors of raf kinase for treatment of cancer |
US7163939B2 (en) | 2003-11-05 | 2007-01-16 | Abbott Laboratories | Macrocyclic kinase inhibitors |
US20050096324A1 (en) | 2003-11-05 | 2005-05-05 | Zhi-Fu Tao | Macrocyclic kinase inhibitors |
CA2561831A1 (en) | 2004-04-13 | 2005-12-22 | Icagen, Inc. | Polycyclic pyrazines as potassium ion channel modulators |
US20070054916A1 (en) | 2004-10-01 | 2007-03-08 | Amgen Inc. | Aryl nitrogen-containing bicyclic compounds and methods of use |
WO2006116733A2 (en) | 2005-04-28 | 2006-11-02 | Supergen, Inc. | Protein kinase inhibitors |
AU2006264043B2 (en) | 2005-06-28 | 2012-04-26 | Sanofi-Aventis | Isoquinoline derivatives as inhibitors of Rho-kinase |
PE20070335A1 (en) | 2005-08-30 | 2007-04-21 | Novartis Ag | SUBSTITUTE BENZIMIDAZOLES AND METHODS FOR THEIR PREPARATION |
WO2007041712A1 (en) | 2005-10-06 | 2007-04-12 | Schering Corporation | Pyrazolopyrimidines as protein kinase inhibitors |
US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
GB0616747D0 (en) * | 2006-08-24 | 2006-10-04 | Astrazeneca Ab | Novel compounds |
CA2673920C (en) | 2006-12-27 | 2015-03-24 | Sanofi-Aventis | Cycloalkylamine substituted isoquinoline derivatives |
DK2134689T3 (en) * | 2007-03-16 | 2014-06-30 | Scripps Research Inst | Focal adhesion kinase inhibitors |
WO2008117050A1 (en) | 2007-03-27 | 2008-10-02 | Astrazeneca Ab | Pyrazolyl-amino-substituted pyrazines and their use for the treatment of cancer |
WO2009004329A1 (en) | 2007-07-02 | 2009-01-08 | Cancer Research Technology Limited | 9h-pyrimido[4,5-b]indoles, 9h-pyrido[4',3':4,5]pyrrolo[2,3-d]pyridines, and 9h-1,3,6,9-tetraaza-fluorenes as chk1 kinase function inhibitors |
GB0719644D0 (en) | 2007-10-05 | 2007-11-14 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
GB0803018D0 (en) | 2008-02-19 | 2008-03-26 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
CA2849566C (en) | 2011-11-09 | 2021-02-09 | Cancer Research Technology Limited | 5-(pyridin-2-yl-amino)-pyrazine-2-carbonitrile compounds and their therapeutic use |
ES2624307T3 (en) * | 2012-05-15 | 2017-07-13 | Cancer Research Technology Ltd | 5 - [[4 - [[Morpholin-2-yl] methylamino] -5- (trifluoromethyl) -2-pyridyl] amino] pyrazin-2-carbonitrile and therapeutic uses thereof |
-
2013
- 2013-05-14 ES ES13723910.9T patent/ES2624307T3/en active Active
- 2013-05-14 EP EP17152400.2A patent/EP3210980B1/en active Active
- 2013-05-14 KR KR1020227037439A patent/KR102635954B1/en active IP Right Grant
- 2013-05-14 KR KR1020207007411A patent/KR102246265B1/en active IP Right Grant
- 2013-05-14 BR BR112014026801-0A patent/BR112014026801B1/en active IP Right Grant
- 2013-05-14 IN IN9221DEN2014 patent/IN2014DN09221A/en unknown
- 2013-05-14 JP JP2015512120A patent/JP6027230B2/en active Active
- 2013-05-14 AU AU2013261605A patent/AU2013261605B2/en active Active
- 2013-05-14 CA CA2870837A patent/CA2870837C/en active Active
- 2013-05-14 EP EP13723910.9A patent/EP2855448B1/en active Active
- 2013-05-14 KR KR1020247004407A patent/KR20240023685A/en active Application Filing
- 2013-05-14 CN CN201610652725.8A patent/CN106279142B/en active Active
- 2013-05-14 KR KR1020217041302A patent/KR20210156333A/en not_active Application Discontinuation
- 2013-05-14 MX MX2014012881A patent/MX358819B/en active IP Right Grant
- 2013-05-14 WO PCT/GB2013/051233 patent/WO2013171470A1/en active Application Filing
- 2013-05-14 RU RU2014147105A patent/RU2659786C2/en active
- 2013-05-14 SG SG11201407238VA patent/SG11201407238VA/en unknown
- 2013-05-14 PL PL13723910T patent/PL2855448T3/en unknown
- 2013-05-14 KR KR1020217012299A patent/KR102341637B1/en active IP Right Grant
- 2013-05-14 CN CN201380025541.3A patent/CN104302635B/en active Active
- 2013-05-14 NZ NZ702050A patent/NZ702050A/en unknown
- 2013-05-14 US US14/396,338 patent/US9663503B2/en active Active
- 2013-05-14 DK DK13723910.9T patent/DK2855448T3/en active
- 2013-05-14 KR KR1020147031572A patent/KR102090792B1/en active IP Right Grant
-
2014
- 2014-10-19 IL IL235133A patent/IL235133A/en active IP Right Grant
- 2014-11-18 ZA ZA2014/08452A patent/ZA201408452B/en unknown
-
2015
- 2015-04-28 HK HK15104108.4A patent/HK1203529A1/en unknown
-
2016
- 2016-10-13 JP JP2016201383A patent/JP6362652B2/en active Active
-
2017
- 2017-05-04 US US15/587,270 patent/US10259806B2/en active Active
- 2017-11-28 AU AU2017268508A patent/AU2017268508C1/en active Active
-
2018
- 2018-02-27 HK HK18102805.1A patent/HK1243408A1/en unknown
-
2020
- 2020-12-17 US US17/124,606 patent/US11787792B2/en active Active
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
SG11201407238VA (en) | 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof | |
SG11201808878UA (en) | Heterocyclic compounds as ret kinase inhibitors | |
SG11201408821SA (en) | Selective pi3k delta inhibitors | |
SG11201805044WA (en) | Compounds useful as kinase inhibitors | |
SG11201803920TA (en) | Compounds and compositions useful for treating disorders related to ntrk | |
SG11201810983PA (en) | Novel heterocyclic derivatives useful as shp2 inhibitors | |
SG11201805300QA (en) | Heterocyclic compounds as immunomodulators | |
SG11201408791TA (en) | Dihydropyrimidine compounds and their application in pharmaceuticals | |
SG11201810171SA (en) | Kras g12c inhibitors | |
SG11201408750VA (en) | NOVEL FUSED PYRIDINE DERIVATIVES USEFUL AS c-MET TYROSINE KINASE INHIBITORS | |
SG11201809714TA (en) | Piperidines as menin inhibitors | |
SG11201808907PA (en) | Inhibitors of activin receptor-like kinase | |
SG11201900844UA (en) | Amino pyrimidine ssao inhibitors | |
SG11201807301SA (en) | Spiro-condensed pyrrolidine derivatives as deubiquitylating enzymes (dub) inhibitors | |
SG11201900635QA (en) | Chimeric antigen receptors targeting bcma and methods of use thereof | |
SG11201900163PA (en) | Macrocycle kinase inhibitors | |
SG11201807538PA (en) | Crispr-cpf1-related methods, compositions and components for cancer immunotherapy | |
SG11201907032RA (en) | Amino pyrimidine compounds useful as ssao inhibitors | |
SG11201804152RA (en) | Heterocyclic compounds as immunomodulators | |
CA2859619C (en) | Bromodomain inhibitors | |
SG11201809342YA (en) | Pyrimidine compounds as jak kinase inhibitors | |
SG11201407793TA (en) | Compounds and compositions for modulating egfr activity | |
SG11201408271VA (en) | Substituted pyrrolidines as factor xia inhibitors for the treatment thromboembolic diseases | |
SG11201804223TA (en) | OCTAHYDROPYRROLO [3, 4-c] PYRROLE DERIVATIVES AND USES THEREOF | |
SG11201807593TA (en) | Compositions and methods to program therapeutic cells using targeted nucleic acid nanocarriers |