BR112014007721A2 - processos para preparar compostos úteis como inibidores de atr quinase - Google Patents
processos para preparar compostos úteis como inibidores de atr quinaseInfo
- Publication number
- BR112014007721A2 BR112014007721A2 BR112014007721A BR112014007721A BR112014007721A2 BR 112014007721 A2 BR112014007721 A2 BR 112014007721A2 BR 112014007721 A BR112014007721 A BR 112014007721A BR 112014007721 A BR112014007721 A BR 112014007721A BR 112014007721 A2 BR112014007721 A2 BR 112014007721A2
- Authority
- BR
- Brazil
- Prior art keywords
- compounds
- processes
- inhibitors
- relates
- preparing
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 18
- 238000000034 method Methods 0.000 title abstract 8
- 239000003112 inhibitor Substances 0.000 title abstract 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 4
- 239000000543 intermediate Substances 0.000 abstract 4
- TVOUADZSZLEFQO-UHFFFAOYSA-N 1,2-oxazole;pyrazin-2-amine Chemical class C=1C=NOC=1.NC1=CN=CC=N1 TVOUADZSZLEFQO-UHFFFAOYSA-N 0.000 abstract 2
- 102000001253 Protein Kinase Human genes 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000035475 disorder Diseases 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 108060006633 protein kinase Proteins 0.000 abstract 2
- 239000007787 solid Substances 0.000 abstract 2
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 abstract 1
- 239000003909 protein kinase inhibitor Substances 0.000 abstract 1
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
- C07D413/02—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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C251/00—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
- C07C251/32—Oximes
- C07C251/34—Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
- C07C251/48—Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with the carbon atom of at least one of the oxyimino groups bound to a carbon atom of a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C269/06—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/20—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D309/14—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrane Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Catalysts (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
abstract [00282] the present invention relates to processes and intermediates for preparing compounds useful as inhibitors of atr kinase, such as aminopyrazine-isoxazole derivatives and related molecules. the present invention also relates to compounds useful as inhibitors of atr protein kinase. the invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention. [00283] the compounds of this invention have formula i or ii: i ii wherein the variables are as defined herein. -------------------------------------------------------------------------- tradução do resumo resumo patente de invenção "processos para preparar compostos úteis como inibidores de atr quinase". a presente invenção refere-se a processos e intermediários para preparar compostos úteis como inibidores de atr quinase, tais como derivados aminopirazina-isoxazol e moléculas relacionadas. a presente invenção refere-se também a compostos úteis como inibidores de atr proteína quinase. ta invenção refere-se a compo¬sições farmaceuticamente aceitáveis que compreendem os compostos desta invenção; métodos para tratamento de várias doenças, distúr¬bios e condições com o uso de compostos desta invenção; processos para preparar os compostos desta invenção; intermediários para a preparação dos compostos desta invenção; e formas sólidas dos compostos desta invenção. os compostos desta invenção têm fórmula i ou ii: i ii em que as variáveis são como definidas aqui.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161541865P | 2011-09-30 | 2011-09-30 | |
US61/541,865 | 2011-09-30 | ||
PCT/US2012/058127 WO2013049726A2 (en) | 2011-09-30 | 2012-09-28 | Processes for making compounds useful as inhibitors of atr kinase |
Publications (2)
Publication Number | Publication Date |
---|---|
BR112014007721A2 true BR112014007721A2 (pt) | 2017-04-25 |
BR112014007721B1 BR112014007721B1 (pt) | 2022-11-01 |
Family
ID=47019163
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112014007721-5A BR112014007721B1 (pt) | 2011-09-30 | 2012-09-28 | Processos para preparar compostos úteis como inibidores de atr quinase |
Country Status (24)
Country | Link |
---|---|
US (4) | US9035053B2 (pt) |
EP (4) | EP2751097A2 (pt) |
JP (4) | JP6212045B2 (pt) |
KR (2) | KR102013133B1 (pt) |
CN (2) | CN106496173A (pt) |
AR (1) | AR088092A1 (pt) |
AU (3) | AU2012315615A1 (pt) |
BR (1) | BR112014007721B1 (pt) |
CA (2) | CA2850566C (pt) |
ES (1) | ES2751741T3 (pt) |
HK (2) | HK1201259A1 (pt) |
HR (1) | HRP20191641T1 (pt) |
HU (1) | HUE046429T2 (pt) |
IL (3) | IL231771A0 (pt) |
IN (1) | IN2014KN00929A (pt) |
MX (1) | MX353461B (pt) |
PL (1) | PL2940017T3 (pt) |
PT (1) | PT2940017T (pt) |
RS (1) | RS59337B1 (pt) |
RU (2) | RU2677292C2 (pt) |
SG (2) | SG10201606774UA (pt) |
TW (3) | TWI625328B (pt) |
WO (1) | WO2013049726A2 (pt) |
ZA (1) | ZA201402625B (pt) |
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KR101755216B1 (ko) | 2008-12-19 | 2017-07-07 | 버텍스 파마슈티칼스 인코포레이티드 | Atr 키나제의 억제제로서 유용한 피라진 유도체 |
EP2569286B1 (en) | 2010-05-12 | 2014-08-20 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
RU2012153675A (ru) | 2010-05-12 | 2014-06-20 | Вертекс Фармасьютикалз Инкорпорейтед | Соединения, пригодные в качестве ингибиторов atr киназы |
US9334244B2 (en) | 2010-05-12 | 2016-05-10 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
WO2011143422A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | 2 -aminopyridine derivatives useful as inhibitors of atr kinase |
US8962631B2 (en) | 2010-05-12 | 2015-02-24 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
WO2011143399A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
US8623869B2 (en) | 2010-06-23 | 2014-01-07 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
CN103562204A (zh) * | 2011-04-05 | 2014-02-05 | 沃泰克斯药物股份有限公司 | 可用作tra激酶的抑制剂的氨基吡嗪化合物 |
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 |
US9096602B2 (en) | 2011-06-22 | 2015-08-04 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-B]pyrazines as ATR kinase inhibitors |
EP2723746A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
CN103958507A (zh) | 2011-09-30 | 2014-07-30 | 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 |
US8853217B2 (en) | 2011-09-30 | 2014-10-07 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
WO2013049719A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
KR102013133B1 (ko) | 2011-09-30 | 2019-08-22 | 버텍스 파마슈티칼스 인코포레이티드 | Atr 키나제의 억제제로서 유용한 화합물의 제조 방법 |
IN2014CN02501A (pt) | 2011-09-30 | 2015-06-26 | Vertex Pharma | |
US8846917B2 (en) | 2011-11-09 | 2014-09-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
US8841449B2 (en) | 2011-11-09 | 2014-09-23 | Vertex Pharmaceuticals Incorporated | 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 |
EP2776420A1 (en) | 2011-11-09 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
US8841337B2 (en) | 2011-11-09 | 2014-09-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
CA2869309C (en) | 2012-04-05 | 2021-02-09 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase and combination therapies thereof |
WO2014055756A1 (en) | 2012-10-04 | 2014-04-10 | Vertex Pharmaceuticals Incorporated | Method for measuring atr inhibition mediated increases in dna damage |
US8912198B2 (en) | 2012-10-16 | 2014-12-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
LT3486245T (lt) | 2012-12-07 | 2021-08-25 | Vertex Pharmaceuticals Incorporated | 2-amino-n-(piperidin-1-il-piridin-3-il)pirazolo[1,5alfa]pirimidin-3-karboksamidas, kaip atr kinazės inhibitorius |
US9663519B2 (en) | 2013-03-15 | 2017-05-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
EP3077397B1 (en) | 2013-12-06 | 2019-09-18 | Vertex Pharmaceuticals Inc. | 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof |
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