AR066978A1 - Compuestos derivados de quinazolina, composicion farmaceutica que los comprende y su uso para reparar un medicamento util como inhibidores de la p13 quinasa - Google Patents
Compuestos derivados de quinazolina, composicion farmaceutica que los comprende y su uso para reparar un medicamento util como inhibidores de la p13 quinasaInfo
- Publication number
- AR066978A1 AR066978A1 ARP080102512A ARP080102512A AR066978A1 AR 066978 A1 AR066978 A1 AR 066978A1 AR P080102512 A ARP080102512 A AR P080102512A AR P080102512 A ARP080102512 A AR P080102512A AR 066978 A1 AR066978 A1 AR 066978A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- cycloalkyl
- heterocycloalkyl
- alkyl
- heteroaryl
- Prior art date
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- A—HUMAN NECESSITIES
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- 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
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- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P9/12—Antihypertensives
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- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
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- C07D401/14—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 three or more hetero rings
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Pulmonology (AREA)
- Biomedical Technology (AREA)
- Oncology (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Reproductive Health (AREA)
- Communicable Diseases (AREA)
- Virology (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Vascular Medicine (AREA)
- Endocrinology (AREA)
- Dermatology (AREA)
Abstract
Un compuesto derivado de quinazolina de formula (1) donde R2 es un sistema de anillos opcionalmente sustituido seleccionado entre un grupo que consiste en los anillos (2), (3), (4), (5), (6), (7) y (8), R1 se selecciona entre un grupo que consiste en: heterocicloalquilo, heterocicloalquilo sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, hidrogeno, cicloalquilo C3-7, cicloalquilo C3-7 sustituido, amino, amino sustituido, arilamino, acilamino, heterocicloalquilamino, alcoxi, alquilo C1-6 y alquilo C1-6 sustituido; cada R3 y R4 se selecciona independientemente entre: hidrogeno, halogeno, acilo, amino, amino sustituido, alquilo C1-6, alquilo C1-6 sustituido, cicloalquilo C3-7, cicloalquilo C3-7 sustituido, heterocicloalquilo C3-7, heterocicloalquilo C3-7 sustituido, alquilcarboxi, arilamino, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, arilalquilo, arilalquilo sustituido, arilcicloalquilo, arilcicloalquilo sustituido, heteroarilalquilo, heteroarilalquilo sustituido, ciano, hidroxilo, alcoxi, nitro, aciloxi y ariloxi; n es 1 o 2; X es C o N; Y es C, O, N oS; y una sal farmacéuticamente aceptable del mismo; con la condicion de que en las formulas (5), (6), (7) y (8) al menos un X o Y no sea carbono; con la condicion adicional de que la formula (3) no contenga más de dos nitrogenos. Composicion farmacéutica que lo comprende. Su uso para preparar un medicamento util para inhibir una o más fosfatoinosítidos 3-quinasas (PI3K) en un ser humano y para tratar trastornos autoinmunes, enfermedades inflamatorias, enfermedades cardiovasculares, enfermedades neurodegenerativas, alergia, asma, pancreatitis, fallo multiorgánico, enfermedades renales, agregacion plaquetaria, cáncer, motilidad de los espermatozoides, rechazo de trasplantes, rechazo de injertos y lesiones pulmonares, incluyendo cáncer.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US94389907P | 2007-06-14 | 2007-06-14 |
Publications (1)
Publication Number | Publication Date |
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AR066978A1 true AR066978A1 (es) | 2009-09-23 |
Family
ID=40156899
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP080102512A AR066978A1 (es) | 2007-06-14 | 2008-06-12 | Compuestos derivados de quinazolina, composicion farmaceutica que los comprende y su uso para reparar un medicamento util como inhibidores de la p13 quinasa |
Country Status (9)
Country | Link |
---|---|
US (2) | US20100179144A1 (es) |
EP (1) | EP2167092A4 (es) |
JP (1) | JP2010532320A (es) |
AR (1) | AR066978A1 (es) |
CL (1) | CL2008001743A1 (es) |
PE (1) | PE20090835A1 (es) |
TW (1) | TW200918068A (es) |
UY (1) | UY31137A1 (es) |
WO (1) | WO2008157191A2 (es) |
Families Citing this family (64)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
UY31137A1 (es) * | 2007-06-14 | 2009-01-05 | Smithkline Beecham Corp | Derivados de quinazolina como inhibidores de la pi3 quinasa |
WO2009017822A2 (en) | 2007-08-02 | 2009-02-05 | Amgen Inc. | Pi3 kinase modulators and methods of use |
US20100311736A1 (en) * | 2007-10-22 | 2010-12-09 | Glaxosmithkline Llc | Pyridosulfonamide derivatives as p13 kinase inhibitors |
JP5520831B2 (ja) | 2007-12-19 | 2014-06-11 | アムジエン・インコーポレーテツド | Pi3キナーゼの阻害薬 |
CA2725014C (en) | 2008-05-30 | 2014-06-17 | Amgen Inc. | Inhibitors of pi3 kinase |
RU2011123647A (ru) | 2008-11-10 | 2012-12-20 | Вертекс Фармасьютикалз Инкорпорейтед | Соединения, полезные в качестве ингибиторов atr киназы |
EP3354650B1 (en) | 2008-12-19 | 2022-02-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
CN102388041B (zh) * | 2009-02-12 | 2014-12-24 | 默克雪兰诺有限公司 | 2-吗啉代-吡啶并[3,2-d]嘧啶 |
AU2010247414B2 (en) * | 2009-05-15 | 2013-08-01 | Novartis Ag | Aryl pyridine as aldosterone synthase inhibitors |
WO2011143423A2 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
US8962631B2 (en) | 2010-05-12 | 2015-02-24 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
US8969356B2 (en) | 2010-05-12 | 2015-03-03 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
US9630956B2 (en) | 2010-05-12 | 2017-04-25 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
US9334244B2 (en) | 2010-05-12 | 2016-05-10 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
AU2011253021A1 (en) | 2010-05-12 | 2012-11-29 | Vertex Pharmaceuticals Incorporated | 2 -aminopyridine derivatives useful as inhibitors of ATR kinase |
MX2013000103A (es) | 2010-06-23 | 2013-06-13 | Vertex Pharma | Derivados de pirrolo-pirazina utiles como inhibidores de cinasa art. |
DE102010049595A1 (de) * | 2010-10-26 | 2012-04-26 | Merck Patent Gmbh | Chinazolinderivate |
WO2012125668A1 (en) * | 2011-03-17 | 2012-09-20 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
JP2014510151A (ja) | 2011-04-05 | 2014-04-24 | 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(trakinase)阻害剤として有用なアミノピラジン化合物 |
US8822469B2 (en) | 2011-06-22 | 2014-09-02 | Vertex Pharmaceuticals Incorporated | Pyrrolo[2,3-B]pyrazines useful as inhibitors of ATR kinase |
WO2012178124A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
WO2012178125A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
US8853217B2 (en) | 2011-09-30 | 2014-10-07 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
KR102184246B1 (ko) | 2011-09-30 | 2020-12-01 | 버텍스 파마슈티칼스 인코포레이티드 | Atr 키나제의 억제제로서 유용한 화합물의 제조 방법 |
SG10201602515QA (en) | 2011-09-30 | 2016-05-30 | Vertex Pharma | Treating pancreatic cancer and non-small cell lung cancer with atr inhibitors |
WO2013049719A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
MX2014003796A (es) | 2011-09-30 | 2015-01-16 | Vertex Pharma | Compuestos utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr). |
WO2013057711A1 (en) * | 2011-10-21 | 2013-04-25 | Novartis Ag | Quinazoline derivatives as pi3k modulators |
WO2013071094A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | 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 |
US8841449B2 (en) | 2011-11-09 | 2014-09-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
EP2776421A1 (en) | 2011-11-09 | 2014-09-17 | 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 |
PL2790705T3 (pl) | 2011-12-15 | 2018-06-29 | Novartis Ag | Zastosowanie inhibitorów czynności lub funkcji PI3K |
RU2014128387A (ru) * | 2012-02-06 | 2016-03-27 | ГлаксоСмитКлайн Интеллекчуал Проперти (N 2) Лимитед | Ингибиторы рi3к для лечения фиброзных заболеваний |
RU2014128386A (ru) * | 2012-02-06 | 2016-03-27 | ГлаксоСмитКлайн Интеллекчуал Проперти (N 2) Лимитед | Ингибиторы PI3K для лечения кашля |
EP2833973B1 (en) | 2012-04-05 | 2017-09-13 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase and combination therapies thereof |
CN102746241B (zh) * | 2012-07-02 | 2014-11-05 | 西安交通大学 | 2,3,5-三取代苯甲酰胺类化合物及其制备方法和用途 |
DK2904406T3 (en) | 2012-10-04 | 2018-06-18 | Vertex Pharma | METHOD OF DETERMINING THE ATR INHIBITION, INCREASED DNA DAMAGE |
EP2909202A1 (en) | 2012-10-16 | 2015-08-26 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
AP2015008328A0 (en) | 2012-10-16 | 2015-03-31 | Almirall Sa | Pyrrolotriazinone derivatives as pi3k inhibitors |
TR201807740T4 (tr) | 2012-12-07 | 2018-06-21 | Vertex Pharma | ATR kinaz inhibitörü olarak 2-amino-6-fluoro-n-(5-fluoro-4-(4-(4-(oksetan-3-il)piperazin-1-karbonil)piperidin-1-il)piridin-3-il)pirazolo[1,5alfa]pirimidin-3-karboksamid. |
US9663519B2 (en) | 2013-03-15 | 2017-05-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
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UY31137A1 (es) * | 2007-06-14 | 2009-01-05 | Smithkline Beecham Corp | Derivados de quinazolina como inhibidores de la pi3 quinasa |
US20100311736A1 (en) * | 2007-10-22 | 2010-12-09 | Glaxosmithkline Llc | Pyridosulfonamide derivatives as p13 kinase inhibitors |
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- 2008-06-12 EP EP08770759A patent/EP2167092A4/en not_active Withdrawn
- 2008-06-12 PE PE2008001006A patent/PE20090835A1/es not_active Application Discontinuation
- 2008-06-12 AR ARP080102512A patent/AR066978A1/es not_active Application Discontinuation
- 2008-06-12 JP JP2010512333A patent/JP2010532320A/ja active Pending
- 2008-06-12 US US12/664,496 patent/US20100179144A1/en not_active Abandoned
- 2008-06-12 TW TW097121826A patent/TW200918068A/zh unknown
- 2008-06-12 CL CL2008001743A patent/CL2008001743A1/es unknown
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- 2008-06-12 WO PCT/US2008/066619 patent/WO2008157191A2/en active Application Filing
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UY31137A1 (es) | 2009-01-05 |
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PE20090835A1 (es) | 2009-07-25 |
WO2008157191A2 (en) | 2008-12-24 |
WO2008157191A3 (en) | 2011-07-14 |
US20090018131A1 (en) | 2009-01-15 |
JP2010532320A (ja) | 2010-10-07 |
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