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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 quinasa

Info

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
Application number
ARP080102512A
Other languages
English (en)
Original Assignee
Smithkline Beecham Corp
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40156899&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR066978(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of AR066978A1 publication Critical patent/AR066978A1/es

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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
    • A61K31/535—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
    • A61K31/33—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
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    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
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    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00—Drugs for disorders of the nervous system
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    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • 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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
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    • A61P9/12—Antihypertensives
    • 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
    • C07D401/04—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
    • 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
    • C07D401/14—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
    • C—CHEMISTRY; METALLURGY
    • 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)
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  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Psychiatry (AREA)
  • Endocrinology (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.
ARP080102512A 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 AR066978A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US94389907P 2007-06-14 2007-06-14

Publications (1)

Publication Number Publication Date
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) US20090018131A1 (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)

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EP2776429A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
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KR20140127307A (ko) * 2012-02-06 2014-11-03 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 섬유성 질병을 치료하기 위한 pi3k 억제제
CN104093407A (zh) * 2012-02-06 2014-10-08 葛兰素史克知识产权第二有限公司 用于治疗咳嗽的pi3k抑制剂
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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
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EP2909202A1 (en) 2012-10-16 2015-08-26 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
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