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)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (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 (OSRAM) | 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 (OSRAM) |
| EP (1) | EP2970288A1 (OSRAM) |
| JP (1) | JP2016512816A (OSRAM) |
| WO (1) | WO2014143242A1 (OSRAM) |
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 |
| 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 |
| US9663519B2 (en) | 2013-03-15 | 2017-05-30 | Vertex Pharmaceuticals Incorporated | Compounds 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 |
| 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 |
| RU2768621C1 (ru) | 2015-09-30 | 2022-03-24 | Вертекс Фармасьютикалз Инкорпорейтед | Способ лечения рака с использованием комбинации повреждающих днк средств и ингибиторов atr |
| MA43870A (fr) | 2016-01-11 | 2021-05-26 | Celator Pharmaceuticals Inc | Inhibition de la protéine associée à l'ataxie télangiectasie et à rad3 (atr) |
| JP7046940B2 (ja) | 2016-10-28 | 2022-04-04 | チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド | 神経栄養因子チロシンキナーゼ受容体阻害剤として用いられるアミノピラゾロピリミジン化合物 |
| WO2018153972A1 (en) | 2017-02-24 | 2018-08-30 | Bayer Pharma Aktiengesellschaft | Combination of atr kinase inhibitors and antiandrogens |
| AR110995A1 (es) | 2017-02-24 | 2019-05-22 | Bayer Ag | Combinación de inhibidores de quinasa atr con sal de radio-223 |
| JOP20190197A1 (ar) | 2017-02-24 | 2019-08-22 | Bayer Pharma AG | مثبط كيناز ايه تي آر للاستخدام في طريقة لعلاج مرض فرط التكاثر |
| WO2018206547A1 (en) | 2017-05-12 | 2018-11-15 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and atr inhibitors |
| DK3658557T3 (da) | 2017-07-28 | 2024-07-29 | Takeda Pharmaceuticals Co | Tyk2-inhibitorer og anvendelser deraf |
| 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 |
| 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 |
| WO2022262671A1 (zh) * | 2021-06-15 | 2022-12-22 | 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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2012007375A1 (en) * | 2010-07-13 | 2012-01-19 | F. Hoffmann-La Roche Ag | Pyrazolo [1, 5a] pyrimidine and thieno [3, 2b] pyrimidine derivatives as irak4 modulators |
| 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 |
Family Cites Families (113)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0824533B1 (de) | 1995-05-09 | 2001-11-14 | Basf Aktiengesellschaft | PYRAZOLO- 1,5a]-PYRIMIDINE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG |
| US6191131B1 (en) | 1997-07-23 | 2001-02-20 | Dupont Pharmaceuticals Company | Azolo triazines and pyrimidines |
| US6060478A (en) | 1996-07-24 | 2000-05-09 | Dupont Pharmaceuticals | Azolo triazines and pyrimidines |
| JPH10218881A (ja) | 1997-02-03 | 1998-08-18 | Pola Chem Ind Inc | 新規なピロロピラゾロピリミジン誘導体 |
| GB2323861B (en) | 1997-02-05 | 2001-06-20 | Sector Exhibiting Systems | Artificial wall structure |
| US6235741B1 (en) | 1997-05-30 | 2001-05-22 | Merck & Co., Inc. | Angiogenesis inhibitors |
| CA2291709A1 (en) | 1997-05-30 | 1998-12-03 | Merck & Co., Inc. | Novel angiogenesis inhibitors |
| US6245759B1 (en) | 1999-03-11 | 2001-06-12 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| JP2001302666A (ja) | 1999-09-21 | 2001-10-31 | Nissan Chem Ind Ltd | アゾール縮合ヘテロ環アニライド化合物及び除草剤 |
| MY125533A (en) | 1999-12-06 | 2006-08-30 | Bristol Myers Squibb Co | Heterocyclic dihydropyrimidine compounds |
| AU2001264932A1 (en) | 2000-05-26 | 2001-12-11 | Neurogen Corporation | Oxo-imidazopyrimidine-carboxamides and their use as gaba brain receptor ligands |
| US20020041880A1 (en) | 2000-07-05 | 2002-04-11 | Defeo-Jones Deborah | Method of treating cancer |
| US7067520B2 (en) | 2000-11-17 | 2006-06-27 | Ishihara Sangyo Kaisha, Ltd. | Preventive or therapeutic medicines for diabetes containing fused-heterocyclic compounds or their salts |
| GB0103926D0 (en) | 2001-02-17 | 2001-04-04 | Astrazeneca Ab | Chemical compounds |
| EP1463742A4 (en) | 2001-06-21 | 2006-05-10 | Ariad Pharma Inc | NEW PYRAZOLO AND PYRROLO PYRIMIDINES AND THEIR USES |
| ATE541847T1 (de) | 2001-11-01 | 2012-02-15 | Icagen Inc | Pyrazolopyrimidine als natriumkanalblocker |
| JP4602076B2 (ja) | 2002-06-04 | 2010-12-22 | ネオジェネシス ファーマシューティカルズ インコーポレイテッド | 抗ウイルス剤としてのピラゾロ[1,5a]ピリミジン化合物 |
| US7449488B2 (en) | 2002-06-04 | 2008-11-11 | Schering Corporation | Pyrazolopyrimidines as protein kinase inhibitors |
| US7074924B2 (en) | 2002-09-04 | 2006-07-11 | Schering Corporation | Pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| US7601724B2 (en) | 2002-09-04 | 2009-10-13 | Schering Corporation | Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors |
| US7196092B2 (en) | 2002-09-04 | 2007-03-27 | Schering Corporation | N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| US7563798B2 (en) | 2002-09-04 | 2009-07-21 | Schering Corporation | Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors |
| US8580782B2 (en) | 2002-09-04 | 2013-11-12 | Merck Sharp & Dohme Corp. | Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors |
| US7119200B2 (en) | 2002-09-04 | 2006-10-10 | Schering Corporation | Pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| AU2003263071B2 (en) | 2002-09-04 | 2007-03-15 | Merck Sharp & Dohme Llc | Pyrazolopyrimidines as cyclin-dependent kinase inhibitors |
| US7067661B2 (en) | 2002-09-04 | 2006-06-27 | Schering Corporation | Pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| CA2497444C (en) | 2002-09-04 | 2010-11-30 | Schering Corporation | Pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| US7205308B2 (en) | 2002-09-04 | 2007-04-17 | Schering Corporation | Trisubstituted 7-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors |
| US7196078B2 (en) | 2002-09-04 | 2007-03-27 | Schering Corpoartion | Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| US8673924B2 (en) | 2002-09-04 | 2014-03-18 | Merck Sharp & Dohme Corp. | Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors |
| US7550470B2 (en) | 2002-12-11 | 2009-06-23 | Merck & Co. Inc. | Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors |
| BRPI0407834A (pt) | 2003-02-28 | 2006-02-14 | Teijin Pharma Ltd | composto, processo para a manufatura do mesmo, composição, processo para a manufatura da mesma, método de tratamento ou prevenção de um distúrbio mediado por proteìna quinase em um indivìduo, uso de um composto, ensaio para determinar a atividade dos compostos, e, método de inibição da atividade ou função de uma proteìna quinase |
| US7138401B2 (en) | 2003-09-18 | 2006-11-21 | Conforma Therapeutics Corporation | 2-aminopurine analogs having HSP90-inhibiting activity |
| ATE495155T1 (de) | 2003-11-19 | 2011-01-15 | Array Biopharma Inc | Heterocyclische inhibitoren von mek |
| JP2007523939A (ja) | 2004-02-25 | 2007-08-23 | ビーエーエスエフ アクチェンゲゼルシャフト | アゾロピリミジン化合物及び寄生性菌類を駆除するためのその使用 |
| US8076338B2 (en) | 2004-04-23 | 2011-12-13 | Exelixis, Inc. | Kinase modulators and methods of use |
| US7635699B2 (en) | 2004-12-29 | 2009-12-22 | Bristol-Myers Squibb Company | Azolopyrimidine-based inhibitors of dipeptidyl peptidase IV and methods |
| US20060156482A1 (en) | 2005-01-14 | 2006-07-20 | The Procter & Gamble Company | Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof |
| DE102005007534A1 (de) | 2005-02-17 | 2006-08-31 | Bayer Cropscience Ag | Pyrazolopyrimidine |
| AU2006251989B2 (en) | 2005-05-20 | 2010-05-27 | Alantos-Pharmaceuticals, Inc. | Pyrimidine or triazine fused bicyclic metalloprotease inhibitors |
| US20070155738A1 (en) | 2005-05-20 | 2007-07-05 | Alantos Pharmaceuticals, Inc. | Heterobicyclic metalloprotease inhibitors |
| US20070155737A1 (en) | 2005-05-20 | 2007-07-05 | Alantos Pharmaceuticals, Inc. | Heterobicyclic metalloprotease inhibitors |
| TWI333953B (en) | 2005-10-06 | 2010-12-01 | Schering Corp | Pyrazolopyrimidines as protein kinase inhibitors |
| US7776865B2 (en) | 2005-10-06 | 2010-08-17 | Schering Corporation | Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors |
| WO2007044441A2 (en) | 2005-10-06 | 2007-04-19 | Schering Corporation | Use of pyrazolo [1 , 5 -a] pyrimidine derivatives for inhibiting protein kinases methods for inhibiting protein kinases |
| KR101071438B1 (ko) | 2005-10-21 | 2011-10-10 | 미쓰비시 타나베 파마 코퍼레이션 | 카나비노이드 수용체 길항제로서의피라졸로[1,5-a]피리미딘 화합물 |
| ATE517874T1 (de) | 2005-10-21 | 2011-08-15 | Exelixis Inc | Pyrimidinone als modulatoren von caseinkinase ii (ck2) |
| JP2009531443A (ja) | 2006-03-29 | 2009-09-03 | フォールドアールエックス ファーマシューティカルズ インコーポレーティッド | α−シヌクレイン毒性の抑制 |
| US20070275963A1 (en) | 2006-05-22 | 2007-11-29 | Schering Corporation | PYRAZOLO[1,5-a]PYRIMIDINES |
| AR061793A1 (es) | 2006-07-05 | 2008-09-24 | Mitsubishi Tanabe Pharma Corp | Compuesto de pirazolo[1,5-a] pirimidina y composicion farmaceutica |
| US8198448B2 (en) | 2006-07-14 | 2012-06-12 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
| US8217177B2 (en) | 2006-07-14 | 2012-07-10 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
| PE20121506A1 (es) | 2006-07-14 | 2012-11-26 | Amgen Inc | Compuestos triazolopiridinas como inhibidores de c-met |
| CA2670083A1 (en) | 2006-11-20 | 2008-05-29 | Alantos Pharmaceuticals Holding, Inc. | Heterobicyclic metalloprotease inhibitors |
| EP2014661A1 (de) | 2007-06-13 | 2009-01-14 | Bayer CropScience AG | Heterocyclisch substituierte Heterocyclyl-carbonsäurederivate |
| US20090012103A1 (en) | 2007-07-05 | 2009-01-08 | Matthew Abelman | Substituted heterocyclic compounds |
| WO2009006580A1 (en) | 2007-07-05 | 2009-01-08 | Cv Therapeutics, Inc. | Optionally condensed dihydropyridine, dihydropyrimidine and dihydropyrane derivatives acting as late sodium channel blockers |
| WO2009017954A1 (en) | 2007-08-01 | 2009-02-05 | Phenomix Corporation | Inhibitors of jak2 kinase |
| JP2011504931A (ja) | 2007-11-28 | 2011-02-17 | シェーリング コーポレイション | プロテインキナーゼ阻害剤としての2−フルオロピラゾロ[1,5−a]ピリミジン |
| WO2009075790A1 (en) | 2007-12-07 | 2009-06-18 | Alantos Pharmaceuticals Holding, Inc. | Metalloprotease inhibitors for intra-articular application |
| WO2009088990A1 (en) | 2008-01-04 | 2009-07-16 | Intellikine, Inc. | Certain chemical entities, compositions and methods |
| EP2085398A1 (en) | 2008-02-01 | 2009-08-05 | Merz Pharma GmbH & Co. KGaA | Pyrazolopyrimidines, a process for their preparation and their use as medicine |
| CA2716856C (en) | 2008-03-20 | 2013-02-19 | Amgen Inc. | Aurora kinase modulators and method of use |
| BRPI0915231A2 (pt) | 2008-07-08 | 2018-06-12 | Intellikine Inc | compostos inibidores de quinase e métodos de uso |
| EP2320907A4 (en) | 2008-08-05 | 2012-09-05 | Merck Sharp & Dohme | THERAPEUTIC COMPOUNDS |
| BRPI0919085B1 (pt) | 2008-09-24 | 2021-05-11 | Basf Se | métodos não terapêuticos para controlar pragas invertebradas e para proteger material de propagação de plantas e/ou plantas que se desenvolvem dos mesmos, compostos de pirazol ou um sal ou um n-óxido dos mesmos, e, composição agrícola |
| JP5769199B2 (ja) | 2008-10-31 | 2015-08-26 | 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阻害剤化合物と方法 |
| WO2010059836A1 (en) | 2008-11-20 | 2010-05-27 | Decode Genetics Ehf | Substituted aza-bridged bicyclics for cardiovascular and cns disease |
| WO2010086040A1 (en) | 2009-01-29 | 2010-08-05 | Biomarin Iga, Ltd. | Pyrazolo-pyrimidines for treatment of duchenne muscular dystrophy |
| US20100204265A1 (en) | 2009-02-09 | 2010-08-12 | Genelabs Technologies, Inc. | Certain Nitrogen Containing Bicyclic Chemical Entities for Treating Viral Infections |
| CN101537007A (zh) | 2009-03-18 | 2009-09-23 | 中国医学科学院血液病医院(血液学研究所) | N-(噻吩-2)吡唑并[1,5-a]嘧啶-3-甲酰胺类化合物在制备抗恶性肿瘤药物方面的应用 |
| US9085560B2 (en) | 2009-08-17 | 2015-07-21 | Intellikine, Inc. | Heterocyclic compounds and uses thereof |
| CN101671336B (zh) | 2009-09-23 | 2013-11-13 | 辽宁利锋科技开发有限公司 | 芳杂环并嘧啶衍生物和类似物及其制备方法和用途 |
| AU2010326268B2 (en) | 2009-12-04 | 2016-11-03 | Senhwa Biosciences, Inc. | Pyrazolopyrimidines and related heterocycles as CK2 inhibitors |
| NZ602311A (en) | 2010-03-18 | 2014-08-29 | Pasteur Institut Korea | Anti-infective compounds |
| WO2011121096A1 (en) | 2010-03-31 | 2011-10-06 | Dkfz Deutsches Krebsforschungszentrum | PYRAZOL[1,5-a]PYRIMIDINE DERIVATIVES AS WNT PATHWAY ANTAGONISTS |
| MX2013000103A (es) | 2010-06-23 | 2013-06-13 | Vertex Pharma | Derivados de pirrolo-pirazina utiles como inhibidores de cinasa art. |
| DK2585467T3 (en) | 2010-06-24 | 2016-06-13 | Gilead Sciences Inc | PYRAZOLO [1,5-A] PYRIMIDINES AND TRIAZINES AS ANTIVIRAL AGENTS |
| WO2012022045A1 (en) | 2010-08-20 | 2012-02-23 | Hutchison Medipharma Limited | Pyrrolopyrimidine compounds and uses thereof |
| EP2608669B1 (en) | 2010-08-23 | 2016-06-22 | Merck Sharp & Dohme Corp. | NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS |
| WO2012067822A1 (en) | 2010-11-16 | 2012-05-24 | Abbott Laboratories | Pyrazolo [1, 5 -a] pyrimidin potassium channel modulators |
| PT3366688T (pt) | 2010-12-08 | 2022-05-11 | Us Health | Pirazolopirimidinas substituídas como ativadores de glucocerebrosidase |
| WO2012143510A1 (de) | 2011-04-21 | 2012-10-26 | Bayer Intellectual Property Gmbh | Fluoralkyl-substituierte pyrazolopyridine und ihre verwendung |
| WO2012143796A2 (en) | 2011-04-21 | 2012-10-26 | Institut Pasteur Korea | Anti-inflammation compounds |
| 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 |
| CN103764166B (zh) | 2011-06-22 | 2017-10-24 | 通用医疗公司 | 蛋白质病的治疗 |
| 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 |
| EA201490265A1 (ru) | 2011-07-13 | 2014-12-30 | Фармасайкликс, Инк. | Ингибиторы тирозинкиназы брутона |
| WO2013052263A2 (en) | 2011-09-16 | 2013-04-11 | Microbiotix, Inc. | Antifungal compounds |
| US9193725B2 (en) | 2012-03-14 | 2015-11-24 | Bristol-Meyers Squibb Company | Cyclic hydrazine derivatives as HIV attachment inhibitors |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| MX354965B (es) | 2012-04-02 | 2018-03-27 | Cytokinetics Inc | Metodo para mejorar la funcion del diafragma. |
| US8940742B2 (en) | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| CN103373996A (zh) | 2012-04-20 | 2013-10-30 | 山东亨利医药科技有限责任公司 | 作为crth2受体拮抗剂的二并环衍生物 |
| WO2013174931A1 (en) | 2012-05-23 | 2013-11-28 | Savira Pharmaceuticals Gmbh | 7-oxo-4,7 -dihydro- pyrazolo [1, 5 -a] pyrimidine derivatives which are useful in the treatment, amelioration or prevention of a viral disease |
| EP2864338B1 (en) | 2012-05-23 | 2016-12-14 | Savira Pharmaceuticals GmbH | 7-oxo-thiazolopyridine carbonic acid derivatives and their use in the treatment, amelioration or prevention of a viral disease |
| WO2014011911A2 (en) | 2012-07-11 | 2014-01-16 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| WO2014015523A1 (en) | 2012-07-27 | 2014-01-30 | Hutchison Medipharma Limited | Novel heteroaryl and heterocycle compounds, compositions and methods |
| EP2885289A1 (en) | 2012-08-06 | 2015-06-24 | Savira Pharmaceuticals GmbH | Dihydroxypyrimidine carbonic acid derivatives and their use in the treatment, amelioration or prevention of a viral disease |
| ES2616492T3 (es) | 2012-08-09 | 2017-06-13 | VIIV Healthcare UK (No.5) Limited | Derivados de piperidina amida como inhibidores de la fijación del VIH |
| EP2895472B1 (en) | 2012-08-09 | 2016-11-23 | VIIV Healthcare UK (No.5) Limited | Tricyclic alkene derivatives as HIV attachment inhibitors |
| ES2614034T3 (es) | 2012-08-09 | 2017-05-29 | VIIV Healthcare UK (No.5) Limited | Derivados de amidina tricíclica como inhibidores de la unión del VIH |
| BR112015003098A2 (pt) | 2012-08-17 | 2017-08-22 | Bayer Cropscience Ag | Azaindolecarboxamidas e azaindoletiocarboxamidas como inseticidas e acaricidas. |
| RU2648247C2 (ru) | 2012-08-24 | 2018-03-23 | Ф. Хоффманн-Ля Рош Аг | Бициклические производные пиридина, полезные в качестве ингибитора белков, связывающих жирные кислоты (FABP) 4 и/или 5 |
| WO2014035140A2 (en) | 2012-08-30 | 2014-03-06 | Kainos Medicine, Inc. | Compounds and compositions for modulating histone methyltransferase activity |
| EP2909212B1 (en) | 2012-09-07 | 2017-02-22 | Takeda Pharmaceutical Company Limited | Substituted 1,4-dihydropyrazolo[4,3-b]indoles |
| WO2014042433A2 (en) | 2012-09-14 | 2014-03-20 | Kainos Medicine, Inc. | Compounds and compositions for modulating adenosine a3 receptor activity |
| TW201412740A (zh) | 2012-09-20 | 2014-04-01 | Bayer Pharma AG | 經取代之吡咯并嘧啶胺基苯并噻唑酮 |
| WO2014047648A1 (en) | 2012-09-24 | 2014-03-27 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| JP6465803B2 (ja) | 2012-10-22 | 2019-02-06 | シティ・オブ・ホープCity of Hope | Etp誘導体 |
| EP2912464B1 (en) | 2012-10-24 | 2017-04-26 | Becton Dickinson and Company | Hydroxamate substituted azaindoline-cyanine dyes and bioconjugates of the same |
| 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 |
-
2013
- 2013-12-06 US US14/098,655 patent/US8969360B2/en not_active Expired - Fee Related
- 2013-12-06 EP EP13812337.7A patent/EP2970288A1/en not_active Withdrawn
- 2013-12-06 JP JP2016500121A patent/JP2016512816A/ja active Pending
- 2013-12-06 WO PCT/US2013/073477 patent/WO2014143242A1/en not_active Ceased
-
2015
- 2015-01-21 US US14/601,442 patent/US20150299205A1/en not_active Abandoned
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| WO2012007375A1 (en) * | 2010-07-13 | 2012-01-19 | F. Hoffmann-La Roche Ag | Pyrazolo [1, 5a] pyrimidine and thieno [3, 2b] pyrimidine derivatives as irak4 modulators |
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 |
Also Published As
| Publication number | Publication date |
|---|---|
| US8969360B2 (en) | 2015-03-03 |
| US20140275021A1 (en) | 2014-09-18 |
| WO2014143242A1 (en) | 2014-09-18 |
| WO2014143242A8 (en) | 2015-03-05 |
| EP2970288A1 (en) | 2016-01-20 |
| US20150299205A1 (en) | 2015-10-22 |
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