JP2016512816A - Atrキナーゼの阻害剤として有用な化合物 - Google Patents
Atrキナーゼの阻害剤として有用な化合物 Download PDFInfo
- Publication number
- JP2016512816A JP2016512816A JP2016500121A JP2016500121A JP2016512816A JP 2016512816 A JP2016512816 A JP 2016512816A JP 2016500121 A JP2016500121 A JP 2016500121A JP 2016500121 A JP2016500121 A JP 2016500121A JP 2016512816 A JP2016512816 A JP 2016512816A
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- JP
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- Prior art keywords
- compound
- cancer
- alkyl
- compound according
- independently selected
- 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.)
- Pending
Links
- 0 *c1c(*)ncc(NC(CC#N)=O)c1* Chemical compound *c1c(*)ncc(NC(CC#N)=O)c1* 0.000 description 4
- CZFWHCXSHJKWCN-UHFFFAOYSA-N C=Cc(cn1)ccc1O Chemical compound C=Cc(cn1)ccc1O CZFWHCXSHJKWCN-UHFFFAOYSA-N 0.000 description 1
- SBOKGMDCMMOASX-UHFFFAOYSA-N CCOc1ccncc1NC(c1c2nc(C(F)(F)F)cc[n]2nc1N)=O Chemical compound CCOc1ccncc1NC(c1c2nc(C(F)(F)F)cc[n]2nc1N)=O SBOKGMDCMMOASX-UHFFFAOYSA-N 0.000 description 1
- QWNAULJLHZHMPS-UHFFFAOYSA-N CN(C)CCOc1nc2c(C(Nc(c(OC)c3)cnc3Cl)=O)c(N)n[n]2cc1 Chemical compound CN(C)CCOc1nc2c(C(Nc(c(OC)c3)cnc3Cl)=O)c(N)n[n]2cc1 QWNAULJLHZHMPS-UHFFFAOYSA-N 0.000 description 1
- SWGQBHFYMNXZRZ-UHFFFAOYSA-N CN(CC1)CCN1C(C(CC1)CCN1c(c(F)cnc1)c1Br)=O Chemical compound CN(CC1)CCN1C(C(CC1)CCN1c(c(F)cnc1)c1Br)=O SWGQBHFYMNXZRZ-UHFFFAOYSA-N 0.000 description 1
- STCHKJRPCYSJPY-UHFFFAOYSA-N CN(CC1)CCN1C(C(CC1)CCN1c(c(F)cnc1)c1N)=O Chemical compound CN(CC1)CCN1C(C(CC1)CCN1c(c(F)cnc1)c1N)=O STCHKJRPCYSJPY-UHFFFAOYSA-N 0.000 description 1
- GDHWXQQENDWPIY-UHFFFAOYSA-N CN(CC1)CCN1C(C1CCNCC1)=O Chemical compound CN(CC1)CCN1C(C1CCNCC1)=O GDHWXQQENDWPIY-UHFFFAOYSA-N 0.000 description 1
- YQJQELXJQQXGFE-UHFFFAOYSA-N CNCCOc1nc2c(C(Nc3cnccc3OC)=O)c(N)n[n]2cc1 Chemical compound CNCCOc1nc2c(C(Nc3cnccc3OC)=O)c(N)n[n]2cc1 YQJQELXJQQXGFE-UHFFFAOYSA-N 0.000 description 1
- GMDNXQJQRDQHOF-UHFFFAOYSA-N COc(ccnc1)c1NC(c(c(N)n[n]1cc2)c1nc2OC1COC1)=O Chemical compound COc(ccnc1)c1NC(c(c(N)n[n]1cc2)c1nc2OC1COC1)=O GMDNXQJQRDQHOF-UHFFFAOYSA-N 0.000 description 1
- JNPZBGCRNZYAMR-UHFFFAOYSA-N COc1ccncc1NC(c(c(N)n[n]1cc2)c1nc2OCCN1CCC1)=O Chemical compound COc1ccncc1NC(c(c(N)n[n]1cc2)c1nc2OCCN1CCC1)=O JNPZBGCRNZYAMR-UHFFFAOYSA-N 0.000 description 1
- GMYNISBQODDWSA-UHFFFAOYSA-N COc1ccncc1NC(c1c2nc(C(F)(F)F)cc[n]2nc1N)=O Chemical compound COc1ccncc1NC(c1c2nc(C(F)(F)F)cc[n]2nc1N)=O GMYNISBQODDWSA-UHFFFAOYSA-N 0.000 description 1
- AAHGMJZGBAOSKP-UHFFFAOYSA-N Cc(cncc1F)c1Cl Chemical compound Cc(cncc1F)c1Cl AAHGMJZGBAOSKP-UHFFFAOYSA-N 0.000 description 1
- DAAOIZUFYABULM-UHFFFAOYSA-N Nc1n[n](ccc(C(F)(F)F)n2)c2c1C(Nc1cnccc1OCC(F)(F)F)=O Chemical compound Nc1n[n](ccc(C(F)(F)F)n2)c2c1C(Nc1cnccc1OCC(F)(F)F)=O DAAOIZUFYABULM-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361788644P | 2013-03-15 | 2013-03-15 | |
| US61/788,644 | 2013-03-15 | ||
| PCT/US2013/073477 WO2014143242A1 (en) | 2013-03-15 | 2013-12-06 | Compounds useful as inhibitors of atr kinase |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016512816A true JP2016512816A (ja) | 2016-05-09 |
| JP2016512816A5 JP2016512816A5 (cg-RX-API-DMAC7.html) | 2017-01-26 |
Family
ID=49881040
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016500121A Pending JP2016512816A (ja) | 2013-03-15 | 2013-12-06 | Atrキナーゼの阻害剤として有用な化合物 |
Country Status (4)
| Country | Link |
|---|---|
| US (2) | US8969360B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2970288A1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2016512816A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2014143242A1 (cg-RX-API-DMAC7.html) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2016539155A (ja) * | 2013-12-06 | 2016-12-15 | 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2−アミノ−6−フルオロ−N−[5−フルオロ−ピリジン−3−イル]ピラゾロ[1,5−a]ピリミジン−3−カルボキサミド化合物、その調製、その異なる固体形態および放射性標識された誘導体 |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| EP3418281B1 (en) | 2012-12-07 | 2020-09-30 | Vertex Pharmaceuticals Inc. | Pyrazolo[1,5-a]pyrimidines useful as inhibitors of atr kinase for the treatment of cancer diseases |
| EP2970286A1 (en) | 2013-03-15 | 2016-01-20 | Vertex Pharmaceuticals Inc. | Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase |
| SG11201608303QA (en) | 2014-04-04 | 2016-11-29 | Del Mar Pharmaceuticals | Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer |
| ES2777608T3 (es) | 2014-06-05 | 2020-08-05 | Vertex Pharma | Derivados radiomarcados de un compuesto de 2-amino-6-fluoro-N-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida útiles como inhibidores de ATR cinasa, la preparación de dicho compuesto y diferentes formas sólidas del mismo |
| CA2950780C (en) | 2014-06-17 | 2023-05-16 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of chk1 and atr inhibitors |
| WO2017059357A1 (en) | 2015-09-30 | 2017-04-06 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of dna damaging agents and atr inhibitors |
| IL260487B2 (en) | 2016-01-11 | 2024-11-01 | Merrimack Pharmaceuticals Inc | Inhibition of ataxia capillary dilation and related protein- (ATR) RAD3 |
| AU2017348826B2 (en) * | 2016-10-28 | 2021-12-02 | Centaurus Biopharma Co., Ltd. | Amino pyrazolopyrimidine compound used as neurotrophic factor tyrosine kinase receptor inhibitor |
| WO2018153972A1 (en) | 2017-02-24 | 2018-08-30 | Bayer Pharma Aktiengesellschaft | Combination of atr kinase inhibitors and antiandrogens |
| JOP20190197A1 (ar) | 2017-02-24 | 2019-08-22 | Bayer Pharma AG | مثبط كيناز ايه تي آر للاستخدام في طريقة لعلاج مرض فرط التكاثر |
| WO2018153969A1 (en) | 2017-02-24 | 2018-08-30 | Bayer Aktiengesellschaft | Combination of atr kinase inhibitors with radium-223 salt |
| WO2018206547A1 (en) | 2017-05-12 | 2018-11-15 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and atr inhibitors |
| WO2019023468A1 (en) | 2017-07-28 | 2019-01-31 | Nimbus Lakshmi, Inc. | TYK2 INHIBITORS AND USES THEREOF |
| CA3071760A1 (en) | 2017-08-04 | 2019-02-07 | Bayer Pharma 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 |
| CA3114024A1 (en) | 2018-09-26 | 2020-04-02 | Merck Patent Gmbh | Combination of a pd-1 antagonist, an atr inhibitor and a platinating agent for the treatment of cancer |
| CN113164447A (zh) | 2018-10-15 | 2021-07-23 | 默克专利股份公司 | 利用dna烷化剂和atr抑制剂的组合疗法 |
| EP3866805A1 (en) | 2018-10-16 | 2021-08-25 | Bayer Aktiengesellschaft | Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds |
| CN115884776B (zh) * | 2021-06-15 | 2024-07-23 | 中国医药研究开发中心有限公司 | 杂环大环化合物及其医药用途 |
| WO2023006057A1 (zh) * | 2021-07-30 | 2023-02-02 | 正大天晴药业集团股份有限公司 | 氨基吡唑并嘧啶化合物的晶体 |
Citations (5)
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|---|---|---|---|---|
| WO2003091256A1 (en) * | 2002-04-23 | 2003-11-06 | Shionogi & Co., Ltd. | PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVE AND NAD(P)H OXIDASE INHIBITOR CONTAINING THE SAME |
| JP2008519059A (ja) * | 2004-11-04 | 2008-06-05 | 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 | プロテインキナーゼのインヒビターとして有用なピラゾロ[1,5−α]ピリミジン |
| JP2009511478A (ja) * | 2005-10-06 | 2009-03-19 | シェーリング コーポレイション | プロテインキナーゼインヒビターとしてのピラゾロピリミジン |
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| JP2012532112A (ja) * | 2009-07-02 | 2012-12-13 | ジェネンテック, インコーポレイテッド | ピラゾロピリミジンjak阻害剤化合物及び方法 |
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Also Published As
| Publication number | Publication date |
|---|---|
| US8969360B2 (en) | 2015-03-03 |
| WO2014143242A1 (en) | 2014-09-18 |
| EP2970288A1 (en) | 2016-01-20 |
| WO2014143242A8 (en) | 2015-03-05 |
| US20140275021A1 (en) | 2014-09-18 |
| US20150299205A1 (en) | 2015-10-22 |
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