[go: up one dir, main page]

ES2580481T3 - Derivados de aminoquinazolina y sus sales, y métodos de uso - Google Patents

Derivados de aminoquinazolina y sus sales, y métodos de uso Download PDF

Info

Publication number
ES2580481T3
ES2580481T3 ES12850573.2T ES12850573T ES2580481T3 ES 2580481 T3 ES2580481 T3 ES 2580481T3 ES 12850573 T ES12850573 T ES 12850573T ES 2580481 T3 ES2580481 T3 ES 2580481T3
Authority
ES
Spain
Prior art keywords
agent
therapeutic agent
pharmaceutically acceptable
pharmaceutical composition
combination
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.)
Active
Application number
ES12850573.2T
Other languages
English (en)
Inventor
Jiancun Zhang
Yingjun Zhang
Weihong Zhang
Bing Liu
Jiquan Zhang
Jinlei Liu
Lu Zhang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sunshine Lake Pharma Co Ltd
Original Assignee
Sunshine Lake Pharma Co Ltd
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 Sunshine Lake Pharma Co Ltd filed Critical Sunshine Lake Pharma Co Ltd
Application granted granted Critical
Publication of ES2580481T3 publication Critical patent/ES2580481T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/535—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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • 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
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • 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
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Un compuesto que tiene la formula (III)**Fórmula** en la que cada uno de X9, X10 y X11 es independientemente CReRf, NRe, O o S, con la condicion de que al menos uno de X9, X10 y X11 sea CReRf; D es un enlace, metileno o etileno; cada uno de Re y Rf es independientemente H, alquilo C1-6, alquilacilo C1-6, cicloalquilo C3-8, arilo C6-10-alquilo C1- 6 o haloalquilo C1-6; y n es 1 o 2; o que tiene una de las siguientes estructuras:**Fórmula** o un estereoisomero, un isomero geometrico, un tautomero, un N-oxido 5 o una sal farmaceuticamente aceptable de los mismos.

Description

imagen1
imagen2
imagen3
imagen4
imagen5
puede ser:
imagen6
6
imagen7
imagen8
imagen9
imagen10
imagen11
imagen12
imagen13
imagen14
imagen15
imagen16
imagen17
imagen18
imagen19
imagen20
Además, Ra puede tener la Fórmula (II):
imagen21
en la que cada uno de R3 yR4 es independientemente H, F, Cl, Br, I, alquenilo, alquinilo, alquilo, cicloalquilo,
5 haloalquilo, heteroalquilo, alcoxi, alquilamino, heterociclilo, hidroxi, amino, nitro, carboxi, ciano, arilo, heteroarilo, aralquilo, heteroarilalquilo, aminosulfonilo, carbamoílo, arilamino, heteroarilamino, arilalquilamino, heteroarilalquilamino, heterociclilamino, heterociclilalquilamino, heteroariloxi, arilalcoxi, heteroarilalcoxi, heterocicliloxi
o heterociclilalcoxi.
10 Además, cada uno de R3 y R4 puede ser independientemente H, F, Cl, Br, I, alquenilo C2-6, alquinilo C2-6, alquilo C16, haloalquilo C1-6, hidroxi, amino, nitro, carboxi, ciano, arilo C6-10 o heteroarilo C1-9.
Ra puede ser:
imagen22
Rb puede ser H o alquilo C1-6. Rc puede ser H, alquilo C1-6, haloalquilo C1-6, éter de alquilo C210, heteroalquilo C16, cicloalquilo C3-8,
20 heterocicloalquilo C210, arilo C6-10, arilo C6-10-alquilo C1-6, heteroarilo C1-9 o heteroarilo C1-9-alquilo C1-6. Rc puede ser metilo, etilo, propilo, isopropilo, trifluorometilo, metoxietilo, ciclopropilo, ciclopentilo, fenilo o fenilmetilo. En un aspecto, en el presente documento se proporcionan compuestos que tienen la Fórmula (III) según se muestra
25 a continuación:
imagen23
en la que cada uno de X9,X10 y X11 es independientemente CReRf, NRe, O o S, con la condición de que al menos 30 unodeX9,X10 y X11 sea CReRf;
D es un enlace, metileno o etileno;
cada uno de Re y Rf es independientemente H, alquilo, alquilacilo C16, cicloalquilo C3-8, arilo C6-10-alquilo C1-6, 35 heteroarilo C1-9- alquilo C1-6 o haloalquilo C1-6;y
n es1 o2.
En otras realizaciones, algunos ejemplos no limitantes de los compuestos divulgados en el presente documento, y 40 de las sales y los solvatos farmacéuticamente aceptables de los mismos (los compuestos 30, 31,32 y 88 son
compuestos de referencia y no son parte de la invención), incluyen:
21
imagen24
imagen25
imagen26
24
imagen27
imagen28
imagen29
imagen30
imagen31
imagen32
imagen33
imagen34
imagen35
imagen36
imagen37
imagen38
imagen39
imagen40
imagen41
imagen42
imagen43
imagen44
imagen45
imagen46
imagen47
imagen48
imagen49
imagen50
imagen51
imagen52
imagen53
imagen54
imagen55
imagen56
imagen57
imagen58
imagen59
imagen60
imagen61
imagen62
imagen63
imagen64
imagen65
imagen66
imagen67
imagen68
imagen69
imagen70
imagen71
imagen72
imagen73
imagen74
imagen75
imagen76
imagen77
imagen78
imagen79
imagen80
imagen81
imagen82
imagen83
imagen84
imagen85
imagen86
imagen87
imagen88
imagen89
imagen90
imagen91
imagen92
imagen93
imagen94
imagen95
imagen96
imagen97
imagen98
imagen99
imagen100
imagen101
imagen102
imagen103
imagen104
imagen105
imagen106
imagen107
imagen108
imagen109
imagen110
imagen111
imagen112
imagen113
imagen114
imagen115
imagen116

Claims (2)

  1. imagen1
    imagen2
    imagen3
    imagen4
    imagen5
    imagen6
    imagen7
    imagen8
    o un estereoisómero, un isómero geométrico, un tautómero, un N-óxido o una sal farmacéuticamente aceptable de
    los mismos. 10
  2. 6. Una composición farmacéutica que comprende un compuesto de acuerdo con la reivindicación 5 y un soporte, un excipiente, un diluyente, un adyuvante, un vehículo farmacéuticamente aceptables o una combinación de los mismos.
    15 7. La composición farmacéutica de acuerdo con la reivindicación 6 que comprende adicionalmente un agente terapéutico, en donde el agente terapéutico se selecciona entre un agente quimioterapéutico, un agente antiproliferativo, un agente para el tratamiento del cáncer pulmonar no microcítico o del carcinoma epidermoide, o una combinación de los mismos; o en donde el agente terapéutico es adriamicina, rapamicina, temsirolimus, everolimus, ixabepilona, gemcitabina, ciclofosfamida, dexametasona, etopósido, fluorouracilo, imatinibmesilato,
    20 dasatinib, nilotinib, erlotinib, lapatinib, gefitinib, sorafenib, sunitinib, un interferón, carboplatino, topotecán, taxol,
    122
    imagen9
ES12850573.2T 2011-11-14 2012-11-14 Derivados de aminoquinazolina y sus sales, y métodos de uso Active ES2580481T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201110359739 2011-11-14
CN201110359739 2011-11-14
PCT/CN2012/001545 WO2013071697A1 (en) 2011-11-14 2012-11-14 Aminoquinazoline derivatives and their salts and methods of use

Publications (1)

Publication Number Publication Date
ES2580481T3 true ES2580481T3 (es) 2016-08-24

Family

ID=48310576

Family Applications (1)

Application Number Title Priority Date Filing Date
ES12850573.2T Active ES2580481T3 (es) 2011-11-14 2012-11-14 Derivados de aminoquinazolina y sus sales, y métodos de uso

Country Status (11)

Country Link
US (1) US9181277B2 (es)
EP (1) EP2780342B1 (es)
JP (1) JP6126613B2 (es)
KR (1) KR101965271B1 (es)
CN (1) CN103102344B (es)
AR (1) AR092289A1 (es)
AU (1) AU2012339499B2 (es)
CA (1) CA2851151C (es)
ES (1) ES2580481T3 (es)
TW (1) TWI577671B (es)
WO (1) WO2013071697A1 (es)

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9546179B2 (en) * 2011-12-20 2017-01-17 Wei Qian Heterocycle amido alkyloxy substituted quinazoline derivative and use thereof
US8906900B2 (en) 2012-12-21 2014-12-09 Epizyme, Inc. PRMT5 inhibitors and uses thereof
SI2935222T1 (sl) 2012-12-21 2019-02-28 Epizyme Inc. Inhibitorji PRMT5 in njihove uporabe
CA2894157A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
CA2899363A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
EP2935243B1 (en) 2012-12-21 2018-03-14 Epizyme, Inc. Prmt5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof
EP2956138B1 (en) 2013-02-15 2022-06-22 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof
ES2831625T3 (es) 2013-02-20 2021-06-09 Kala Pharmaceuticals Inc Compuestos terapéuticos y sus usos
US9688688B2 (en) 2013-02-20 2017-06-27 Kala Pharmaceuticals, Inc. Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof
CN104513237A (zh) * 2013-09-30 2015-04-15 重庆药友制药有限责任公司 一种制备n-甲基莫西沙星的新方法
CN108530458A (zh) 2013-11-01 2018-09-14 卡拉制药公司 治疗化合物的结晶形式及其用途
US9890173B2 (en) 2013-11-01 2018-02-13 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
CN104744446B (zh) * 2013-12-30 2019-06-25 广东东阳光药业有限公司 杂芳化合物及其在药物中的应用
WO2015200677A2 (en) * 2014-06-25 2015-12-30 Epizyme, Inc. Prmt5 inhibitors and uses thereof
DK3172212T3 (en) * 2014-07-24 2018-08-27 Boehringer Ingelheim Int Aldosterone synthase inhibitors.
EP3177288A4 (en) 2014-08-04 2018-04-04 Epizyme, Inc. Prmt5 inhibitors and uses thereof
DK3212637T3 (da) 2014-10-31 2021-07-12 Indivior Uk Ltd Dopamin-d3-receptorantagonistforbindelser
AU2016214923A1 (en) * 2015-02-03 2017-08-24 Trillium Therapeutics Inc. Novel fluorinated derivatives as EGFR inhibitors useful for treating cancers
CN106146412B (zh) * 2015-03-31 2019-05-24 广州市恒诺康医药科技有限公司 喹唑啉衍生物及其制备方法和应用
KR102627044B1 (ko) * 2015-10-19 2024-01-18 선샤인 레이크 파르마 컴퍼니 리미티드 Egfr 저해제의 염, 이의 결정질 형태 및 용도
CN105294719B (zh) * 2015-11-18 2017-12-22 乳源瑶族自治县大众药品贸易有限公司 一种氨基喹唑啉类衍生物的二对甲苯磺酸盐及其晶型
CN105294716B (zh) * 2015-11-18 2017-12-22 乳源瑶族自治县大众药品贸易有限公司 一种氨基喹唑啉类衍生物的二水杨酸盐及其晶型
CN105461729B (zh) * 2015-11-18 2017-12-05 乳源瑶族自治县大众药品贸易有限公司 一种egfr抑制剂的盐、晶型及其用途
CN105294717B (zh) * 2015-11-18 2017-12-22 乳源瑶族自治县大众药品贸易有限公司 一种egfr抑制剂的盐、晶型及其用途
CN105294718B (zh) * 2015-11-18 2018-01-23 乳源瑶族自治县大众药品贸易有限公司 一种氨基喹唑啉类衍生物的马来酸盐及其晶型
CN105294715B (zh) * 2015-11-18 2017-12-22 乳源瑶族自治县大众药品贸易有限公司 一种氨基喹唑啉类衍生物的富马酸盐及其晶型
EP3241830A1 (de) 2016-05-04 2017-11-08 Bayer CropScience Aktiengesellschaft Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel
EP3509423A4 (en) 2016-09-08 2020-05-13 Kala Pharmaceuticals, Inc. CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF
EP3509421A4 (en) 2016-09-08 2020-05-20 Kala Pharmaceuticals, Inc. CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF
US10253036B2 (en) 2016-09-08 2019-04-09 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
CN107793420A (zh) * 2017-12-11 2018-03-13 康化（上海）新药研发有限公司 一种3,4‑二氢‑2H‑吡喃[3,2‑b]吡啶的合成方法
JP2021512959A (ja) 2018-02-06 2021-05-20 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司Ｊｉａｎｇｓｕ Ｈｅｎｇｒｕｉ Ｍｅｄｉｃｉｎｅ Ｃｏ．， Ｌｔｄ． ピラゾロ［１，５−ａ］［１，３，５］トリアジン−２−アミン誘導体、その製造法、およびその医薬用途
WO2019236884A1 (en) 2018-06-07 2019-12-12 Disarm Therapeutics, Inc. Inhibitors of sarm1
CA3123215C (en) 2018-12-19 2024-04-02 Disarm Therapeutics, Inc. Inhibitors of sarm1 in combination with neuroprotective agents
CN113549063B (zh) * 2020-04-23 2024-04-05 南京药石科技股份有限公司 一种光学异构的八氢-2H-吡咯并[3,4-c]吡啶-2-羧酸叔丁酯的制备方法
CN114380841A (zh) * 2020-10-19 2022-04-22 南京正大天晴制药有限公司 作为akt抑制剂的三环喹唑啉或二氢喹唑啉化合物
CN118715216A (zh) * 2022-03-28 2024-09-27 江苏恒瑞医药股份有限公司 含氮杂环类化合物、其制备方法及其在医药上的应用
CN116969961B (zh) * 2023-07-25 2025-06-27 乳源东阳光药业有限公司 氨基喹唑啉类酪氨酸激酶抑制剂化合物(a)的合成方法
CN117924316B (zh) * 2023-12-28 2024-11-22 乐威医药（江苏）股份有限公司 四氢吡咯并恶嗪酮环的制备方法

Family Cites Families (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
UA71945C2 (en) * 1999-01-27 2005-01-17 Pfizer Prod Inc Substituted bicyclic derivatives being used as anticancer agents
US20060063752A1 (en) 2000-03-14 2006-03-23 Boehringer Ingelheim Pharma Gmbh & Co. Kg Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them
DE10042059A1 (de) * 2000-08-26 2002-03-07 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
US6617329B2 (en) * 2000-08-26 2003-09-09 Boehringer Ingelheim Pharma Kg Aminoquinazolines and their use as medicaments
US6924285B2 (en) 2002-03-30 2005-08-02 Boehringer Ingelheim Pharma Gmbh & Co. Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them
JP2005536486A (ja) 2002-07-09 2005-12-02 アストラゼネカ アクチボラグ 癌の処置に使用するためのキナゾリン誘導体
JP4703183B2 (ja) 2002-07-15 2011-06-15 シンフォニー エボルーション， インク． 受容体型キナーゼモジュレーターおよびその使用方法
WO2004018430A1 (ja) 2002-08-23 2004-03-04 Kirin Beer Kabushiki Kaisha ＴＧＦβ阻害活性を有する化合物およびそれを含んでなる医薬組成物
NZ539408A (en) * 2002-11-04 2007-09-28 Astrazeneca Ab Quinazoline derivatives as SRC tyrosine kinase inhibitors for treating solid tumours
CN100354278C (zh) * 2002-11-04 2007-12-12 阿斯利康(瑞典)有限公司 作为src酪氨酸激酶抑制剂的喹唑啉衍生物
GB0226434D0 (en) * 2002-11-13 2002-12-18 Astrazeneca Ab Combination product
CA2522079A1 (en) * 2003-04-16 2004-11-04 Astrazeneca Ab Quinazoline derivatives for treatment of cancer
WO2004108710A1 (en) * 2003-06-05 2004-12-16 Astrazeneca Ab 4-pyrimidinyl quinazoline derivatives for use in the treatment of tumours
WO2004108711A1 (en) * 2003-06-05 2004-12-16 Astrazeneca Ab Pyrazinil quinazoline derivatives for use in the treatment of tumours
WO2004108707A1 (en) * 2003-06-05 2004-12-16 Astrazeneca Ab Pyridazinil quinazoline derivatives for use in the treatment of tumours
GB0318423D0 (en) * 2003-08-06 2003-09-10 Astrazeneca Ab Chemical compounds
PL1667992T3 (pl) 2003-09-19 2007-05-31 Astrazeneca Ab Pochodne chinazoliny
GB0322409D0 (en) 2003-09-25 2003-10-29 Astrazeneca Ab Quinazoline derivatives
ES2651730T3 (es) 2003-09-26 2018-01-29 Exelixis, Inc. Moduladores c-Met y métodos de uso
WO2006081741A1 (en) 2005-02-05 2006-08-10 Piaoyang Sun Quinazoline compounds or their medical salts and preparation and medical usage thereof
LT2229369T (lt) * 2008-01-18 2016-09-26 Natco Pharma Limited 6,7-dialkoksi-chinazolino dariniai, tinkami panaudoti su vėžiu susijusių susirgimų gydymui
US8426430B2 (en) * 2008-06-30 2013-04-23 Hutchison Medipharma Enterprises Limited Quinazoline derivatives
CN101619043B (zh) * 2008-06-30 2013-06-05 和记黄埔医药（上海）有限公司 喹唑啉衍生物及其医药用途
CN101367793B (zh) * 2008-09-26 2013-09-11 中国科学院广州生物医药与健康研究院 一种具有抗肿瘤活性的氨基喹唑啉衍生物及其盐类
WO2011084796A2 (en) 2009-12-21 2011-07-14 Qiang Zhang Novel quinazoline derivatives
CN101836992A (zh) * 2010-05-27 2010-09-22 东南大学 4-苯并噻酚氨基喹唑啉衍生物在制备治疗肿瘤药物方面的应用
WO2012000182A1 (en) 2010-06-30 2012-01-05 Hutchison Medipharma Limited Quinazoline compounds
CN102452988B (zh) 2010-10-27 2016-01-27 中国科学院化学研究所 一种喹唑啉衍生物及其制备方法
US9546179B2 (en) * 2011-12-20 2017-01-17 Wei Qian Heterocycle amido alkyloxy substituted quinazoline derivative and use thereof

Also Published As

Publication number Publication date
US20140228361A1 (en) 2014-08-14
JP6126613B2 (ja) 2017-05-10
AR092289A1 (es) 2015-04-15
WO2013071697A1 (en) 2013-05-23
HK1196609A1 (zh) 2014-12-19
TW201319055A (zh) 2013-05-16
KR101965271B1 (ko) 2019-04-03
EP2780342B1 (en) 2016-06-01
US9181277B2 (en) 2015-11-10
CA2851151A1 (en) 2013-05-23
KR20140093271A (ko) 2014-07-25
CA2851151C (en) 2017-09-12
CN103102344B (zh) 2015-10-14
AU2012339499A1 (en) 2014-06-05
TWI577671B (zh) 2017-04-11
EP2780342A1 (en) 2014-09-24
EP2780342A4 (en) 2015-04-08
CN103102344A (zh) 2013-05-15
AU2012339499B2 (en) 2015-09-10
JP2014534975A (ja) 2014-12-25

Similar Documents

Publication Publication Date Title
ES2580481T3 (es) Derivados de aminoquinazolina y sus sales, y métodos de uso
RU2018121499A (ru) Гипоксантины в качестве ингибиторов убиквитин-специфической протеазы 1
AR059957A1 (es) DERIVADOS DE ESPIROINDOLINONA, MÉTODOS PARA SU PREPARACIoN, UNA COMPOSICIoN FARMACÉUTICA QUE LOS CONTIENE Y SU USO EN LA FABRICACIoN DE MEDICAMENTOS PARA EL TRATAMIENTO DEL CÁNCER.
AR064608A1 (es) Derivados de pirazolo-quinazolina sustituidos, composiciones farmaceuticas que los contienen. proceso para su preparacion y uso de los mismos como agentes anticancer.
UA107954C2 (xx) Заміщені піролідин-2-карбоксаміди
AR084408A1 (es) Compuestos de purina y 7-deazapurina substituidos
AR079205A1 (es) Morfolinotiazoles como moduladores alostericos positivos alfa 7
JP2014511892A5 (es)
AR081058A1 (es) Derivados de arilmetoxi isoindolina, composiciones que los comprenden y su uso en el tratamiento del cancer.
JP2010522194A5 (es)
AR075366A1 (es) Compuestos heterociclicos biciclicos sustituidos como modulares de la gamma secretasa
AR094262A1 (es) Compuestos antivirales para el tratamiento de la hepatitis c
AR088175A1 (es) 3-pirimidin-4-il-oxazolidin-2-onas utiles para tratar cancer y composiciones farmaceuticas que las contienen
JP2013544268A5 (es)
UA113541C2 (xx) Заміщені піролідин-2-карбоксаміди
JP2013510120A5 (es)
JP2015537008A5 (es)
AR054612A1 (es) Derivados de espiroquetas y composiciones farmaceuticas para su utilizacion como agente terapeutico para diabetes
JP2016506958A5 (es)
JP2017509586A5 (es)
AR070136A1 (es) Pirimidil ciclopentanos como inhibidores de la akt proteina quinasa
JP2016501223A5 (es)
AR085489A1 (es) Derivados de triazolopiridinas, composiciones farmaceuticas que los contienen, proceso para prepararlos, intermediarios de dicho proceso y uso de los mismos para el tratamiento de enfermedades autoinmunes e inflamatorias
RU2014121205A (ru) Производные азолов
WO2013004995A8 (en) Pyrimidinone compounds and their use