[go: up one dir, main page]

AR100809A1 - Inhibidores de fosfatidilinositol 3-quinasa - Google Patents

Inhibidores de fosfatidilinositol 3-quinasa

Info

Publication number
AR100809A1
AR100809A1 ARP150101859A ARP150101859A AR100809A1 AR 100809 A1 AR100809 A1 AR 100809A1 AR P150101859 A ARP150101859 A AR P150101859A AR P150101859 A ARP150101859 A AR P150101859A AR 100809 A1 AR100809 A1 AR 100809A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
carbon atoms
alkyl
substituted carbon
haloalkyl
Prior art date
Application number
ARP150101859A
Other languages
English (en)
Inventor
Chung Yeung Suet
j watkins William
Van Veldhuizen Joshua
Phillips Gary
W Phillips Barton
Naduthambi Devan
A Loyer-Drew Jennifer
Kaplan Joshua
Du Zhimin
Cai Shaopei
Original Assignee
Gilead Sciences Inc
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
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of AR100809A1 publication Critical patent/AR100809A1/es

Links

Classifications

    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K31/505—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
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • 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
    • A61P9/10—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/04—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/90—Oxygen atoms with acyclic radicals attached in position 2 or 3
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • 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
    • 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
    • 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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Reproductive Health (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Child & Adolescent Psychology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)

Abstract

Reivindicación 1: Un compuesto caracterizado porque tiene la estructura de fórmula (1), en donde: n es 0, 1, 2, ó 3; m es 0, 1, ó 2; A es un enlace sencillo o C(O); B es heterocicloalquilo de tres a diez miembros que tiene al menos un heteroátomo seleccionado de N ó O, en donde heterocicloalquilo está sustituido opcionalmente con halo, alquilo de uno a seis átomos de carbono sustituido opcionalmente, heterocicloalquilo de tres a ocho átomos de carbono sustituido opcionalmente, C₁₋₆ haloalquilo, y cicloalquilo de tres a ocho átomos de carbono sustituido opcionalmente; cada R¹ es seleccionado independientemente de halo, ciano, alquilo de uno a seis átomos de carbono sustituido opcionalmente, haloalquilo de uno a seis átomos de carbono sustituido opcionalmente, alcoxi de uno a seis átomos de carbono sustituido opcionalmente, sulfonilo sustituido opcionalmente, arilo de tres a ocho átomos de carbono sustituido opcionalmente, heteroarilo de tres a ocho átomos de carbono sustituido opcionalmente, cicloalquilo de tres a ocho átomos de carbono sustituido opcionalmente, y heterocicloalquilo de tres a ocho átomos de carbono sustituido opcionalmente; cada R² es independientemente halo, alquilo de uno a seis átomos de carbono sustituido opcionalmente, haloalquilo de uno a seis átomos de carbono sustituido opcionalmente, y -NH₂; R³ es hidrógeno, alquilo de uno a seis átomos de carbono sustituido opcionalmente, C₃₋₈ cicloalquilo, o C₆₋₁₀ arilo; R⁴ es un heteroarilo de seis a doce miembros que tiene al menos un grupo aromático y al menos dos heteroátomos seleccionados de N, O, o S, en donde el heteroarilo está sustituido opcionalmente con uno, dos o tres miembros seleccionados independientemente de halo, ciano, haloalquilo de uno a seis átomos de carbono sustituido opcionalmente, alquilo de uno a seis átomos de carbono sustituido opcionalmente, alquinilo de dos a cuatro átomos de carbono sustituido opcionalmente, y -NH₂; y R⁵ es hidrógeno o alquilo de uno a seis átomos de carbono sustituido opcionalmente, en donde R⁵ y R³ junto con los átomos a los cuales están enlazados forman un anillo heterocíclico de cuatro a ocho miembros; o una sal, isómero, o una mezcla de los mismos, farmacéuticamente aceptables.
ARP150101859A 2014-06-13 2015-06-11 Inhibidores de fosfatidilinositol 3-quinasa AR100809A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201462012222P 2014-06-13 2014-06-13

Publications (1)

Publication Number Publication Date
AR100809A1 true AR100809A1 (es) 2016-11-02

Family

ID=53674247

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP150101859A AR100809A1 (es) 2014-06-13 2015-06-11 Inhibidores de fosfatidilinositol 3-quinasa

Country Status (18)

Country Link
US (1) US10092563B2 (es)
EP (1) EP3154958B1 (es)
JP (1) JP6454736B2 (es)
KR (1) KR20170012557A (es)
CN (1) CN106458932A (es)
AR (1) AR100809A1 (es)
AU (1) AU2015274635B2 (es)
BR (1) BR112016028818A2 (es)
CA (1) CA2952037A1 (es)
EA (1) EA201692249A1 (es)
ES (1) ES2833025T3 (es)
HK (1) HK1231477A1 (es)
IL (1) IL249078A0 (es)
MX (1) MX2016016516A (es)
NZ (1) NZ726608A (es)
SG (1) SG11201610095SA (es)
TW (1) TW201625561A (es)
WO (1) WO2015191752A1 (es)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA201692265A1 (ru) 2014-06-13 2017-05-31 Джилид Сайэнс, Инк. Ингибиторы фосфатидилинозитол-3-киназы
NZ726360A (en) * 2014-06-13 2018-04-27 Gilead Sciences Inc Phosphatidylinositol 3-kinase inhibitors
CN106458932A (zh) 2014-06-13 2017-02-22 吉利德科学公司 磷脂酰肌醇3‑激酶抑制剂
ES2763103T3 (es) 2014-06-13 2020-05-27 Gilead Sciences Inc Inhibidor de la fosfatidilinositol 3-quinasa
EA201692266A1 (ru) 2014-06-13 2017-06-30 Джилид Сайэнс, Инк. Ингибиторы фосфатидилинозитол-3-киназы
MX2017000208A (es) 2014-07-04 2017-05-01 Lupin Ltd Derivados de quinolizinona como inhibidores de pi3k.
CN118286245A (zh) 2014-12-26 2024-07-05 埃莫里大学 N4-羟基胞苷和衍生物及与其相关的抗病毒用途
PL3321265T3 (pl) 2015-03-04 2020-11-16 Gilead Sciences, Inc. Związki 4,6-diamino-pirydo[3,2-d]pirymidynowe i ich wykorzystanie jako modulatorów receptorów toll-podobnych
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療
EP3507288B1 (en) 2016-09-02 2020-08-26 Gilead Sciences, Inc. 4,6-diamino-pyrido[3,2-d]pyrimidine derivaties as toll like receptor modulators
CA3035346A1 (en) 2016-09-02 2018-03-08 Gilead Sciences, Inc. Toll like receptor modulator compounds
AU2018363482A1 (en) * 2017-11-13 2020-06-25 Luoxin Pharmaceutical (Shanghai) Co., Ltd. Quinazolinone compound and application thereof
US11331331B2 (en) 2017-12-07 2022-05-17 Emory University N4-hydroxycytidine and derivatives and anti-viral uses related thereto
US10751339B2 (en) 2018-01-20 2020-08-25 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine compounds and methods of use
CN108546268B (zh) * 2018-05-28 2019-04-09 西安培华学院 用于治疗动脉粥样硬化的化合物及其应用
CN109593066B (zh) * 2018-12-21 2020-06-19 上海交通大学 一种用于治疗肠道细菌感染的叶酸拮抗剂及其制备与应用
TW202212339A (zh) 2019-04-17 2022-04-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TW202210480A (zh) 2019-04-17 2022-03-16 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TWI879779B (zh) 2019-06-28 2025-04-11 美商基利科學股份有限公司 類鐸受體調節劑化合物的製備方法

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2388646C (en) 1999-10-27 2009-01-27 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
KR100785363B1 (ko) 2000-04-25 2007-12-18 이코스 코포레이션 인간 포스파티딜-이노시톨 3-키나제 델타의 억제제
US6667300B2 (en) 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
ES2873875T3 (es) 2004-05-13 2021-11-04 Icos Corp Quinazolinonas como inhibidores de fosfatidilinositol 3-quinasa delta humano
ITRM20040139U1 (it) * 2004-08-26 2004-11-26 Salice Arturo Spa Cerniera con spinta in apertura per mobili con cornice.
US20080287469A1 (en) 2005-02-17 2008-11-20 Diacovo Thomas G Phosphoinositide 3-Kinase Inhibitors for Inhibiting Leukocyte Accumulation
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
WO2009088990A1 (en) * 2008-01-04 2009-07-16 Intellikine, Inc. Certain chemical entities, compositions and methods
US8399460B2 (en) 2009-10-27 2013-03-19 Astrazeneca Ab Chromenone derivatives
KR101758046B1 (ko) 2009-12-22 2017-07-14 버텍스 파마슈티칼스 인코포레이티드 포스파티딜이노시톨 3-키나제의 이소인돌리논 억제제
US8604032B2 (en) 2010-05-21 2013-12-10 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
TWI642670B (zh) 2010-09-14 2018-12-01 伊塞利克斯公司 Ｐｉ３ｋ-德爾塔抑制劑以及其應用和生產方法
MA34591B1 (fr) 2010-10-06 2013-10-02 Glaxosmithkline Llc Dérivés de benzimidazole utilisés comme inhibiteurs de pi3 kinase
PL2658844T3 (pl) 2010-12-28 2017-04-28 Sanofi Nowe pochodne pirymidyn, ich wytwarzanie i ich zastosowanie farmaceutyczne jako inhibitorów fosforylacji AKT(pkb)
RU2014111823A (ru) 2011-08-29 2015-10-10 Инфинити Фармасьютикалз, Инк. Гетероциклические соединения и их применения
SG10202003090VA (en) * 2012-08-08 2020-05-28 Kbp Biosciences Co Ltd PI3K δ INHIBITOR
TW201441216A (zh) * 2012-12-21 2014-11-01 Gilead Calistoga Llc 肌醇磷酯３－激酶的抑制劑
CA2895785A1 (en) 2012-12-21 2014-06-26 Jerry Evarts Isoquinolinone or quinazolinone phosphatidylinositol 3-kinase inhibitors
WO2014128612A1 (en) 2013-02-20 2014-08-28 Novartis Ag Quinazolin-4-one derivatives
JP6030783B2 (ja) 2013-06-14 2016-11-24 ギリアード サイエンシーズ， インコーポレイテッド ホスファチジルイノシトール３−キナーゼ阻害剤
UY35675A (es) 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
RU2675105C9 (ru) 2013-09-22 2019-01-09 Саншайн Лейк Фарма Ко., Лтд. Замещенные аминопиримидиновые соединения и способы их использования
WO2015051241A1 (en) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
AU2014354769A1 (en) 2013-11-26 2016-05-26 Gilead Sciences, Inc. Therapies for treating myeloproliferative disorders
CN103728782A (zh) * 2013-12-31 2014-04-16 深圳市华星光电技术有限公司 一种液晶显示装置及相应的制造方法
WO2015168079A1 (en) 2014-04-29 2015-11-05 Infinity Pharmaceuticals, Inc. Pyrimidine or pyridine derivatives useful as pi3k inhibitors
EA201692266A1 (ru) 2014-06-13 2017-06-30 Джилид Сайэнс, Инк. Ингибиторы фосфатидилинозитол-3-киназы
CN106458932A (zh) 2014-06-13 2017-02-22 吉利德科学公司 磷脂酰肌醇3‑激酶抑制剂
ES2763103T3 (es) 2014-06-13 2020-05-27 Gilead Sciences Inc Inhibidor de la fosfatidilinositol 3-quinasa
NZ726360A (en) 2014-06-13 2018-04-27 Gilead Sciences Inc Phosphatidylinositol 3-kinase inhibitors
EA201692265A1 (ru) 2014-06-13 2017-05-31 Джилид Сайэнс, Инк. Ингибиторы фосфатидилинозитол-3-киназы
AR100975A1 (es) 2014-06-24 2016-11-16 Gilead Sciences Inc Inhibidores de fosfatidilinositol 3-quinasa

Also Published As

Publication number Publication date
HK1231477A1 (zh) 2017-12-22
EP3154958A1 (en) 2017-04-19
JP2017517542A (ja) 2017-06-29
KR20170012557A (ko) 2017-02-02
IL249078A0 (en) 2017-01-31
US10092563B2 (en) 2018-10-09
US20150361054A1 (en) 2015-12-17
TW201625561A (zh) 2016-07-16
JP6454736B2 (ja) 2019-01-16
CN106458932A (zh) 2017-02-22
WO2015191752A1 (en) 2015-12-17
CA2952037A1 (en) 2015-12-17
ES2833025T3 (es) 2021-06-14
AU2015274635B2 (en) 2018-04-19
BR112016028818A2 (pt) 2017-08-22
MX2016016516A (es) 2017-05-01
NZ726608A (en) 2018-04-27
EP3154958B1 (en) 2020-10-07
EA201692249A1 (ru) 2017-05-31
AU2015274635A1 (en) 2016-12-08
SG11201610095SA (en) 2016-12-29

Similar Documents

Publication Publication Date Title
AR100809A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR100808A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR100975A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR100806A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR100807A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR100810A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR096684A1 (es) Compuestos para tratar atrofia muscular espinal
AR102177A1 (es) Compuestos de heteroarilo como inhibidores de btk y usos de los mismos
AR106472A1 (es) Inhibidores de acc y usos de los mismos
NI201700020A (es) Compuestos de aminopirimidinilo como inhibidores de jak
AR105845A1 (es) Compuestos de heteroarilo bicíclicos fusionados como moduladores de la función irak4
AR103828A1 (es) INHIBIDORES DEL FACTOR TRANSFORMADOR DEL CRECIMIENTO b
AR094299A1 (es) Derivados de ftalazin-1(2h)-ona sustituidos
AR103138A1 (es) Compuestos de heteroarilo como inhibidores de la irak y usos de los mismos
AR098872A1 (es) Moduladores de tetrahidropiridopirazinas de gpr6
AR100058A1 (es) DERIVADOS DE PIRIMIDIN-PIRAZINAS FUSIONADAS MODULADORES DE RORg
AR095359A1 (es) Compuestos heteroaromáticos y su uso como ligandos d1 de dopamina
AR099379A1 (es) Compuestos tricíclicos como agentes antineoplásicos
AR107170A1 (es) Compuestos heterocíclicos tricíclicos condesados como inhibidores de integrasa del vih
AR103170A1 (es) Compuestos y composiciones farmacéuticas de los mismos para el tratamiento de desordenes inflamatorios y osteoartritis
AR097866A1 (es) Derivados de 4-azaindol
MX2017009625A (es) Compuestos macrociclicos como inhibidores de cinasas asociadas al receptor de interleucina1/4 (irak1/4) y usos de los mismos.
AR099495A1 (es) Derivados de amida, antagonistas de orexina
AR103742A1 (es) Derivados de trifluorometilpropanamida
AR090086A1 (es) COMPUESTO DE 1H-INDAZOL-3-CARBOXAMIDA COMO INHIBIDORES DE LA GLUCOGENO SINTASA CINASA 3 b

Legal Events

Date Code Title Description
FB Suspension of granting procedure