RU2362775C1 - Хиназолиновые соединения - Google Patents

Хиназолиновые соединения Download PDF

Info

Publication number
RU2362775C1
RU2362775C1 RU2008100767/04A RU2008100767A RU2362775C1 RU 2362775 C1 RU2362775 C1 RU 2362775C1 RU 2008100767/04 A RU2008100767/04 A RU 2008100767/04A RU 2008100767 A RU2008100767 A RU 2008100767A RU 2362775 C1 RU2362775 C1 RU 2362775C1
Authority
RU
Russia
Prior art keywords
bromo
azaindole
azaindoline
obtaining
stage
Prior art date
Application number
RU2008100767/04A
Other languages
English (en)
Other versions
RU2008100767A (ru
Inventor
Лоран Франсуа Андре ЭННЕКЕН (GB)
Лоран Франсуа Андре ЭННЕКЕН
Original Assignee
Астразенека Аб
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 Астразенека Аб filed Critical Астразенека Аб
Publication of RU2008100767A publication Critical patent/RU2008100767A/ru
Application granted granted Critical
Publication of RU2362775C1 publication Critical patent/RU2362775C1/ru

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Reproductive Health (AREA)
  • Emergency Medicine (AREA)
  • Oncology (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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Изобретение относится к способу получения 5-бром-7-азаиндола, который предусматривает: стадия 1: восстановление 7-азаиндола, получая 7-азаиндолин; стадия 2: бромирование 7-азаиндолина, получая 5-бром-7-азаиндолин; стадия 3: окисление 5-бром-7-азаиндолина, получая 5-бром-7-азаиндол.

Description

Текст описания приведен в факсимильном виде.
Figure 00000001
Figure 00000002
Figure 00000003
Figure 00000004
Figure 00000005
Figure 00000006
Figure 00000007
Figure 00000008
Figure 00000009
Figure 00000010
Figure 00000011
Figure 00000012
Figure 00000013
Figure 00000014
Figure 00000015
Figure 00000016
Figure 00000017
Figure 00000018
Figure 00000019
Figure 00000020
Figure 00000021
Figure 00000022
Figure 00000023
Figure 00000024
Figure 00000025
Figure 00000026
Figure 00000027
Figure 00000028
Figure 00000029
Figure 00000030
Figure 00000031
Figure 00000032
Figure 00000033
Figure 00000034
Figure 00000035
Figure 00000036
Figure 00000037
Figure 00000038
Figure 00000039
Figure 00000040
Figure 00000041
Figure 00000042
Figure 00000043
Figure 00000044
Figure 00000045
Figure 00000046
Figure 00000047
Figure 00000048
Figure 00000049
Figure 00000050
Figure 00000051
Figure 00000052
Figure 00000053
Figure 00000054
Figure 00000055
Figure 00000056
Figure 00000057
Figure 00000058
Figure 00000059
Figure 00000060
Figure 00000061
Figure 00000062
Figure 00000063
Figure 00000064
Figure 00000065
Figure 00000066
Figure 00000067
Figure 00000068
Figure 00000069
Figure 00000070
Figure 00000071
Figure 00000072
Figure 00000073
Figure 00000074
Figure 00000075
Figure 00000076
Figure 00000077
Figure 00000078
Figure 00000079
Figure 00000080
Figure 00000081
Figure 00000082
Figure 00000083
Figure 00000084
Figure 00000085
Figure 00000086
Figure 00000087
Figure 00000088
Figure 00000089
Figure 00000090
Figure 00000091
Figure 00000092
Figure 00000093
Figure 00000094
Figure 00000095
Figure 00000096
Figure 00000097
Figure 00000098
Figure 00000099
Figure 00000100
Figure 00000101
Figure 00000102
Figure 00000103
Figure 00000104
Figure 00000105
Figure 00000106
Figure 00000107
Figure 00000108
Figure 00000109
Figure 00000110
Figure 00000111
Figure 00000112
Figure 00000113
Figure 00000114
Figure 00000115
Figure 00000116
Figure 00000117
Figure 00000118
Figure 00000119
Figure 00000120
Figure 00000121
Figure 00000122
Figure 00000123
Figure 00000124
Figure 00000125
Figure 00000126
Figure 00000127
Figure 00000128
Figure 00000129
Figure 00000130
Figure 00000131
Figure 00000132
Figure 00000133
Figure 00000134
Figure 00000135
Figure 00000136
Figure 00000137
Figure 00000138
Figure 00000139
Figure 00000140
Figure 00000141
Figure 00000142
Figure 00000143
Figure 00000144
Figure 00000145
Figure 00000146
Figure 00000147
Figure 00000148
Figure 00000149
Figure 00000150
Figure 00000151
Figure 00000152
Figure 00000153
Figure 00000154
Figure 00000155
Figure 00000156
Figure 00000157
Figure 00000158
Figure 00000159
Figure 00000160
Figure 00000161
Figure 00000162
Figure 00000163
Figure 00000164
Figure 00000165
Figure 00000166
Figure 00000167
Figure 00000168
Figure 00000169
Figure 00000170
Figure 00000171
Figure 00000172
Figure 00000173
Figure 00000174
Figure 00000175
Figure 00000176
Figure 00000177
Figure 00000178
Figure 00000179
Figure 00000180
Figure 00000181
Figure 00000182
Figure 00000183
Figure 00000184
Figure 00000185
Figure 00000186
Figure 00000187
Figure 00000188
Figure 00000189
Figure 00000190
Figure 00000191
Figure 00000192

Claims (1)

  1. Способ получения 5-бром-7-азаиндола, который предусматривает: стадия 1: восстановление 7-азаиндола, получая 7-азаиндолин; затем стадия 2: бромирование 7-азаиндолина, получая 5-бром-7-азаиндолин; затем стадия 3: окисление 5-бром-7-азаиндолина, получая 5-бром-7-азаиндол.
RU2008100767/04A 2002-02-01 2003-01-28 Хиназолиновые соединения RU2362775C1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP02290242.3 2002-02-01
EP02290242 2002-02-01

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
RU2004126612/04A Division RU2365588C2 (ru) 2002-02-01 2003-01-28 Хиназолиновые соединения

Publications (2)

Publication Number Publication Date
RU2008100767A RU2008100767A (ru) 2009-05-10
RU2362775C1 true RU2362775C1 (ru) 2009-07-27

Family

ID=27635895

Family Applications (3)

Application Number Title Priority Date Filing Date
RU2008100766/04A RU2362774C1 (ru) 2002-02-01 2003-01-28 Хиназолиновые соединения
RU2004126612/04A RU2365588C2 (ru) 2002-02-01 2003-01-28 Хиназолиновые соединения
RU2008100767/04A RU2362775C1 (ru) 2002-02-01 2003-01-28 Хиназолиновые соединения

Family Applications Before (2)

Application Number Title Priority Date Filing Date
RU2008100766/04A RU2362774C1 (ru) 2002-02-01 2003-01-28 Хиназолиновые соединения
RU2004126612/04A RU2365588C2 (ru) 2002-02-01 2003-01-28 Хиназолиновые соединения

Country Status (29)

Country Link
US (3) US7268230B2 (ru)
EP (2) EP1474420B1 (ru)
JP (2) JP4608215B2 (ru)
KR (1) KR101093345B1 (ru)
CN (2) CN101607958A (ru)
AR (1) AR038476A1 (ru)
AT (1) ATE549329T1 (ru)
AU (1) AU2003202094B2 (ru)
BR (1) BR0307151A (ru)
CA (1) CA2473572C (ru)
CY (1) CY1112835T1 (ru)
DK (1) DK1474420T3 (ru)
ES (1) ES2381781T3 (ru)
HK (1) HK1070367A1 (ru)
HU (1) HUP0402588A3 (ru)
IL (2) IL163022A (ru)
IS (1) IS7362A (ru)
MX (1) MXPA04007459A (ru)
MY (1) MY144042A (ru)
NO (1) NO328731B1 (ru)
NZ (1) NZ534171A (ru)
PL (1) PL371486A1 (ru)
PT (1) PT1474420E (ru)
RU (3) RU2362774C1 (ru)
SI (1) SI1474420T1 (ru)
TW (1) TWI337866B (ru)
UA (1) UA81619C2 (ru)
WO (1) WO2003064413A1 (ru)
ZA (1) ZA200405908B (ru)

Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9800569D0 (en) * 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
BRPI0008128B8 (pt) 1999-02-10 2021-05-25 Astrazeneca Ab derivados de quinazolina, composições farmacêuticas contendo os mesmos, e, uso dos mesmos como inibidores de angiogênese
WO2001032651A1 (en) 1999-11-05 2001-05-10 Astrazeneca Ab Quinazoline derivatives as vegf inhibitors
DK1274692T3 (da) * 2000-04-07 2006-10-30 Astrazeneca Ab Quinazolinforbindelser
ATE325795T1 (de) * 2001-03-23 2006-06-15 Bayer Corp Rho-kinase inhibitoren
BR0307151A (pt) 2002-02-01 2004-12-07 Astrazeneca Ab Composto ou um sal do mesmo, processo para a preparação do mesmo, composição farmacêutica, uso do composto ou de um seu sal, método para produzir um efeito antiangiogênico e/ou redutor da permeabilidade vascular em um animal de sangue quente, como um ser humano, que necessita de um tratamento do tipo referido, e, processos para a preparação de 5-bromo-7- azaindol, e para a produção de 5-metóxi-7-azaindol
CA2491191C (en) 2002-07-15 2014-02-04 Exelixis, Inc. Receptor-type kinase modulators and methods of use
JP4593464B2 (ja) * 2002-11-04 2010-12-08 アストラゼネカ アクチボラグ Srcチロシンキナーゼ阻害剤としてのキナゾリン誘導体
GB0316127D0 (en) * 2003-07-10 2003-08-13 Astrazeneca Ab Combination therapy
GB0318422D0 (en) * 2003-08-06 2003-09-10 Astrazeneca Ab Chemical compounds
DE10340485B4 (de) 2003-09-03 2015-05-13 Morphochem AG Aktiengesellschaft für kombinatorische Chemie Verfahren zur Herstellung von Oxazolidinon-Chinolon Hybriden
CN1882570B (zh) * 2003-09-19 2010-12-08 阿斯利康(瑞典)有限公司 喹唑啉衍生物
ES2925655T3 (es) 2003-09-26 2022-10-19 Exelixis Inc Moduladores c-Met y métodos de uso
GB0330002D0 (en) 2003-12-24 2004-01-28 Astrazeneca Ab Quinazoline derivatives
CN1933839A (zh) 2004-01-23 2007-03-21 安进公司 化合物和使用方法
JP2007518823A (ja) 2004-01-23 2007-07-12 アムゲン インコーポレイテッド キノリン、キナゾリン、ピリジン、及びピリミジン化合物と炎症、血管新生、及び癌に対する治療におけるそれら化合物の用途
JP4237242B2 (ja) 2004-10-12 2009-03-11 アストラゼネカ アクチボラグ キナゾリン誘導体
EP1827434B1 (en) 2004-11-30 2014-01-15 Amgen Inc. Quinolines and quinazoline analogs and their use as medicaments for treating cancer
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
US8071768B2 (en) 2005-06-10 2011-12-06 Janssen Pharmaceutica, N.V. Alkylquinoline and alkylquinazoline kinase modulators
US7825244B2 (en) 2005-06-10 2010-11-02 Janssen Pharmaceutica Nv Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis
AR054608A1 (es) 2005-08-08 2007-06-27 Actelion Pharmaceuticals Ltd Derivados de oxazolidinona enlazados a quinolonas como antibacterianos
GB0519879D0 (en) 2005-09-30 2005-11-09 Astrazeneca Ab Chemical process
GB0523810D0 (en) * 2005-11-23 2006-01-04 Astrazeneca Ab Pharmaceutical compositions
AU2007217560B2 (en) 2006-02-22 2012-06-28 4Sc Ag Indolopyridines as Eg5 kinesin modulators
UY30183A1 (es) * 2006-03-02 2007-10-31 Astrazeneca Ab Derivados de quinolina
WO2007099323A2 (en) * 2006-03-02 2007-09-07 Astrazeneca Ab Quinoline derivatives
US7851623B2 (en) * 2006-11-02 2010-12-14 Astrazeneca Ab Chemical process
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
WO2008079909A1 (en) * 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
US7648979B2 (en) 2007-02-07 2010-01-19 Hoffmann-La Roche Inc. 5-amido-(1H-indol-2-yl)-piperazin-1-yl-methanone derivatives
US7507736B2 (en) 2007-02-07 2009-03-24 Hoffmann-La Roche Inc. Indol-2-yl-piperazin-1-yl-methanone derivatives
US20080190689A1 (en) * 2007-02-12 2008-08-14 Ballard Ebbin C Inserts for engine exhaust systems
NZ582772A (en) 2007-07-17 2012-06-29 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
AU2008319366B2 (en) * 2007-10-29 2012-03-01 Amgen Inc. Benzomorpholine derivatives and methods of use
WO2009138781A1 (en) 2008-05-13 2009-11-19 Astrazeneca Ab Fumarate salt of 4- (3-chloro-2-fluoroanilino) -7-methoxy-6- { [1- (n-methylcarbamoylmethyl) piperidin- 4-yl] oxy}quinazoline
PL2387563T5 (pl) 2009-01-16 2023-03-13 Exelixis, Inc. Sól jabłczanowa N-(4-{[6,7-bis(metyloksy)chinolin-4-ylo]oksy}fenylo-N′-(4-fluorofenylo)cykloproano-1,1-dikarboksyamidu oraz jej krystaliczne postaci do leczenia raka
AU2010212590B2 (en) 2009-02-10 2013-01-10 Astrazeneca Ab Triazolo [4,3-b] pyridazine derivatives and their uses for prostate cancer
SG173178A1 (en) 2009-04-03 2011-09-29 Hoffmann La Roche Propane- i-sulfonic acid {3- [5- (4 -chloro-phenyl) -1h-pyrrolo [2, 3-b] pyridine-3-carbonyl] -2, 4-difluoro-pheny l } -amide compositions and uses thereof
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
CA2780190C (en) 2009-11-06 2020-05-05 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
US9624213B2 (en) 2011-02-07 2017-04-18 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
AR085279A1 (es) 2011-02-21 2013-09-18 Plexxikon Inc Formas solidas de {3-[5-(4-cloro-fenil)-1h-pirrolo[2,3-b]piridina-3-carbonil]-2,4-difluor-fenil}-amida del acido propano-1-sulfonico
AR086411A1 (es) * 2011-05-20 2013-12-11 Nippon Soda Co Compuesto heterociclico conteniendo nitrogeno y fungicida para el uso en agricultura y jardineria
TWI557109B (zh) * 2011-12-29 2016-11-11 財團法人生物技術開發中心 喹唑啉化合物作為激酶抑制劑及其應用
CN103288756B (zh) * 2012-02-29 2016-04-20 江苏先声药物研究有限公司 一种喹唑啉中间体的甲醇溶剂合物及其制备方法
US9242355B2 (en) 2012-04-17 2016-01-26 Black & Decker Inc. Illuminated power tool
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
WO2014127214A1 (en) 2013-02-15 2014-08-21 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof
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
KR102277833B1 (ko) 2013-02-20 2021-07-14 칼라 파마슈티컬스, 인크. 치료 화합물 및 그의 용도
CA2928665A1 (en) * 2013-11-01 2015-05-07 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
US9890173B2 (en) 2013-11-01 2018-02-13 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
KR20160099084A (ko) 2013-11-01 2016-08-19 칼라 파마슈티컬스, 인크. 치료 화합물의 결정질 형태 및 그의 용도
MX2018004109A (es) 2015-10-05 2018-09-27 Univ Columbia Activadores de flujo autofágico y fosfolipasa d y depuración de acumulaciones de proteína que incluyen tau y tratamiento de proteinopatías.
CN105461718A (zh) * 2016-01-13 2016-04-06 苏州莱安医药化学技术有限公司 一种5-溴-7-氮杂吲哚的合成工艺
CN113912586B (zh) * 2016-08-31 2023-04-07 江苏恒瑞医药股份有限公司 氧代吡啶酰胺类衍生物、其制备方法及其在医药上的应用
BR112019004463A2 (pt) 2016-09-08 2019-05-28 Kala Pharmaceuticals Inc formas cristalinas de compostos terapêuticos, seus processos de obtenção e seus métodos de uso
CA3036340A1 (en) 2016-09-08 2018-03-15 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
AU2017324713B2 (en) 2016-09-08 2020-08-13 KALA BIO, Inc. Crystalline forms of therapeutic compounds and uses thereof
CN107840843A (zh) * 2017-10-17 2018-03-27 浙江工业大学义乌科学技术研究院有限公司 一种西地尼布中间体的合成方法
KR20200074179A (ko) * 2017-10-20 2020-06-24 칼라 파마슈티컬스, 인크. Ret9 및 vegfr2 억제제
WO2020057403A1 (zh) * 2018-09-18 2020-03-26 北京越之康泰生物医药科技有限公司 吲哚衍生物及其在医药上的应用

Family Cites Families (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU174215B (hu) 1976-12-15 1979-11-28 Richter Gedeon Vegyeszet Sposob poluchenija novykh proizvodnykh piperazina i kislotnykh additivnykh i chetvjortichnykh solej
IL81307A0 (en) 1986-01-23 1987-08-31 Union Carbide Agricult Method for reducing moisture loss from plants and increasing crop yield utilizing nitrogen containing heterocyclic compounds and some novel polysubstituted pyridine derivatives
US5411963A (en) * 1988-01-29 1995-05-02 Dowelanco Quinazoline derivatives
IL89029A (en) 1988-01-29 1993-01-31 Lilly Co Eli Fungicidal quinoline and cinnoline derivatives, compositions containing them, and fungicidal methods of using them
DE4022414A1 (de) * 1990-07-13 1992-01-16 Bayer Ag Substituierte pyrrolo-pyridine
CA2102780C (en) * 1991-05-10 2007-01-09 Alfred P. Spada Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase
US6645969B1 (en) * 1991-05-10 2003-11-11 Aventis Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
US5714493A (en) * 1991-05-10 1998-02-03 Rhone-Poulenc Rorer Pharmaceuticals, Inc. Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
US5710158A (en) * 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5480883A (en) * 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5721237A (en) 1991-05-10 1998-02-24 Rhone-Poulenc Rorer Pharmaceuticals Inc. Protein tyrosine kinase aryl and heteroaryl quinazoline compounds having selective inhibition of HER-2 autophosphorylation properties
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
GB9300059D0 (en) 1992-01-20 1993-03-03 Zeneca Ltd Quinazoline derivatives
FR2687402B1 (fr) * 1992-02-14 1995-06-30 Lipha Nouveaux azaindoles, procedes de preparation et medicaments les contenant.
US5212195A (en) * 1992-05-13 1993-05-18 Syntex (U.S.A.) Inc. Substituted indole antagonists derivatives which are angiotensin II
GB9323290D0 (en) 1992-12-10 1994-01-05 Zeneca Ltd Quinazoline derivatives
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
JP2890267B2 (ja) * 1994-02-23 1999-05-10 ファイザー インク. 4−ヘテロサイクリル−置換キナゾリン誘導体、その調製法および抗癌剤としてのその使用法
AU2096895A (en) 1994-03-07 1995-09-25 Sugen, Incorporated Receptor tyrosine kinase inhibitors for inhibiting cell proliferative disorders and compositions thereof
GB9505651D0 (en) 1995-03-21 1995-05-10 Agrevo Uk Ltd AgrEvo UK Limited
FR2732969B1 (fr) * 1995-04-14 1997-05-16 Adir Nouveaux composes pyridiniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US6046206A (en) * 1995-06-07 2000-04-04 Cell Pathways, Inc. Method of treating a patient having a precancerous lesions with amide quinazoline derivatives
GB9514265D0 (en) * 1995-07-13 1995-09-13 Wellcome Found Hetrocyclic compounds
EP0860433B1 (en) 1995-11-07 2002-07-03 Kirin Beer Kabushiki Kaisha Quinoline derivatives and quinazoline derivatives inhibiting autophosphorylation of growth factor receptor originating in platelet and pharmaceutical compositions containing the same
GB9624482D0 (en) * 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
PT880508E (pt) 1996-02-13 2003-07-31 Astrazeneca Ab Derivados de quinazolina como inibidores de vegf
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
AU719327B2 (en) * 1996-03-05 2000-05-04 Astrazeneca Ab 4-anilinoquinazoline derivatives
WO1997034876A1 (en) 1996-03-15 1997-09-25 Zeneca Limited Cinnoline derivatives and use as medicine
DE19614718A1 (de) 1996-04-15 1997-10-16 Hoechst Schering Agrevo Gmbh Substituierte Pyridine/Pyrimidine, Verfahren zu ihrer Herstellung, und ihre Verwendung als Schädlingsbekämpfungsmittel
GB9707800D0 (en) 1996-05-06 1997-06-04 Zeneca Ltd Chemical compounds
ES2249800T3 (es) 1996-06-24 2006-04-01 Pfizer Inc. Derivados triciclicos sustituidos con fenilamino para el tratamento de enfermedades hiperproliferativas.
ID19609A (id) 1996-07-13 1998-07-23 Glaxo Group Ltd Senyawa-senyawa heterosiklik
CA2263479A1 (en) 1996-09-25 1998-04-02 Zeneca Limited Quinoline derivatives inhibiting the effect of growth factors such as vegf
GB9718972D0 (en) * 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
US6225318B1 (en) * 1996-10-17 2001-05-01 Pfizer Inc 4-aminoquinazolone derivatives
AU734009B2 (en) 1997-05-30 2001-05-31 Merck & Co., Inc. Novel angiogenesis inhibitors
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
ZA986729B (en) * 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitors of tyrosine kinases
WO1999010349A1 (en) 1997-08-22 1999-03-04 Zeneca Limited Oxindolylquinazoline derivatives as angiogenesis inhibitors
US6162804A (en) * 1997-09-26 2000-12-19 Merck & Co., Inc. Tyrosine kinase inhibitors
GB9721437D0 (en) 1997-10-10 1997-12-10 Glaxo Group Ltd Heteroaromatic compounds and their use in medicine
GB9800575D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
GB9800569D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
US6172071B1 (en) 1998-07-30 2001-01-09 Hughes Institute Lipid-lowering quinazoline derivative
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
AU756556B2 (en) 1998-10-08 2003-01-16 Astrazeneca Ab Quinazoline derivatives
GB9900334D0 (en) 1999-01-07 1999-02-24 Angiogene Pharm Ltd Tricylic vascular damaging agents
GB2345486A (en) 1999-01-11 2000-07-12 Glaxo Group Ltd Heteroaromatic protein tyrosine kinase inhibitors
GB9900752D0 (en) 1999-01-15 1999-03-03 Angiogene Pharm Ltd Benzimidazole vascular damaging agents
US6797823B1 (en) 1999-01-22 2004-09-28 Kirin Beer Kabushiki Kaisha Quinoline derivatives and quinazoline derivatives
JP3270834B2 (ja) 1999-01-27 2002-04-02 ファイザー・プロダクツ・インク 抗がん剤として有用なヘテロ芳香族二環式誘導体
UA71945C2 (en) 1999-01-27 2005-01-17 Pfizer Prod Inc Substituted bicyclic derivatives being used as anticancer agents
BRPI0008128B8 (pt) * 1999-02-10 2021-05-25 Astrazeneca Ab derivados de quinazolina, composições farmacêuticas contendo os mesmos, e, uso dos mesmos como inibidores de angiogênese
DE19911509A1 (de) 1999-03-15 2000-09-21 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
TWI262914B (en) * 1999-07-02 2006-10-01 Agouron Pharma Compounds and pharmaceutical compositions for inhibiting protein kinases
AU6578900A (en) 1999-07-07 2001-01-30 Astrazeneca Uk Limited Quinazoline derivatives
SK286628B6 (sk) 1999-10-19 2009-02-05 Merck & Co., Inc. Inhibítory tyrozín-kinázy, farmaceutický prostriedok s ich obsahom a ich použitie
WO2001032651A1 (en) 1999-11-05 2001-05-10 Astrazeneca Ab Quinazoline derivatives as vegf inhibitors
JP2003525897A (ja) * 2000-03-06 2003-09-02 アストラゼネカ アクチボラグ 治 療
GB0008269D0 (en) * 2000-04-05 2000-05-24 Astrazeneca Ab Combination chemotherapy
DK1274692T3 (da) * 2000-04-07 2006-10-30 Astrazeneca Ab Quinazolinforbindelser
IL152682A0 (en) 2000-05-31 2003-06-24 Astrazeneca Ab Indole derivatives with vascular damaging activity
UA73993C2 (ru) * 2000-06-06 2005-10-17 Астразенека Аб Хиназолиновые производные для лечения опухолей и фармацевтическая композиция
SK52003A3 (en) 2000-07-07 2003-07-01 Angiogene Pharm Ltd Colchinol derivatives as angiogenesis inhibitors, method for their preparation and pharmaceutical composition comprising the same
AU6623301A (en) 2000-07-07 2002-01-21 Angiogene Pharm Ltd Colchinol derivatives as vascular damaging agents
WO2002012226A1 (en) 2000-08-09 2002-02-14 Astrazeneca Ab Quinoline derivatives having vegf inhibiting activity
AU7993801A (en) * 2000-08-09 2002-02-18 Astrazeneca Ab Chemical compounds
WO2002012228A1 (en) * 2000-08-09 2002-02-14 Astrazeneca Ab Cinnoline compounds
AU2001278609B2 (en) * 2000-08-21 2005-04-14 Astrazeneca Ab Quinazoline derivatives
AU2002323406A1 (en) 2001-08-30 2003-03-18 Merck And Co., Inc. Tyrosine kinase inhibitors
US7169788B2 (en) 2001-10-30 2007-01-30 Merck & Co., Inc. Tyrosine kinase inhibitors
MXPA04004219A (es) * 2001-11-03 2004-09-10 Astrazeneca Ab Derivados de quinazolina como agentes antitumorales.
GB0126433D0 (en) * 2001-11-03 2002-01-02 Astrazeneca Ab Compounds
GB0126879D0 (en) 2001-11-08 2002-01-02 Astrazeneca Ab Combination therapy
BR0307151A (pt) 2002-02-01 2004-12-07 Astrazeneca Ab Composto ou um sal do mesmo, processo para a preparação do mesmo, composição farmacêutica, uso do composto ou de um seu sal, método para produzir um efeito antiangiogênico e/ou redutor da permeabilidade vascular em um animal de sangue quente, como um ser humano, que necessita de um tratamento do tipo referido, e, processos para a preparação de 5-bromo-7- azaindol, e para a produção de 5-metóxi-7-azaindol
CA2495487A1 (en) * 2002-08-09 2004-02-19 Astrazeneca Ab Combination of zd6474, an inhibitor of the vascular endothelial growth factor receptor, with radiotherapy in the treatment of cancer
GB0305142D0 (en) * 2003-03-06 2003-04-09 Eisai London Res Lab Ltd Synthesis
GB0318423D0 (en) * 2003-08-06 2003-09-10 Astrazeneca Ab Chemical compounds
GB0318422D0 (en) * 2003-08-06 2003-09-10 Astrazeneca Ab Chemical compounds
GB0330002D0 (en) * 2003-12-24 2004-01-28 Astrazeneca Ab Quinazoline derivatives
US7117615B2 (en) * 2004-05-28 2006-10-10 Nike, Inc. Shoe with reversible upper
GB0519879D0 (en) * 2005-09-30 2005-11-09 Astrazeneca Ab Chemical process
US7851623B2 (en) * 2006-11-02 2010-12-14 Astrazeneca Ab Chemical process

Also Published As

Publication number Publication date
ZA200405908B (en) 2005-11-30
RU2362774C1 (ru) 2009-07-27
PL371486A1 (en) 2005-06-13
WO2003064413A1 (en) 2003-08-07
HK1070367A1 (en) 2005-06-17
HUP0402588A3 (en) 2009-09-28
US20050085465A1 (en) 2005-04-21
MXPA04007459A (es) 2005-09-08
NO328731B1 (no) 2010-05-03
JP4608215B2 (ja) 2011-01-12
PT1474420E (pt) 2012-05-10
CN1625555A (zh) 2005-06-08
NO20043162L (no) 2004-07-22
TW200302727A (en) 2003-08-16
NZ534171A (en) 2007-06-29
RU2004126612A (ru) 2005-07-10
RU2008100767A (ru) 2009-05-10
US8293902B2 (en) 2012-10-23
RU2365588C2 (ru) 2009-08-27
US7268230B2 (en) 2007-09-11
SI1474420T1 (sl) 2012-06-29
DK1474420T3 (da) 2012-05-21
RU2008100766A (ru) 2009-05-10
AU2003202094B2 (en) 2009-10-08
IS7362A (is) 2004-07-22
US20090156821A1 (en) 2009-06-18
ES2381781T3 (es) 2012-05-31
ATE549329T1 (de) 2012-03-15
BR0307151A (pt) 2004-12-07
US20080027069A1 (en) 2008-01-31
CN101607958A (zh) 2009-12-23
TWI337866B (en) 2011-03-01
UA81619C2 (ru) 2008-01-25
JP2010100642A (ja) 2010-05-06
IL210785A0 (en) 2011-03-31
HUP0402588A2 (hu) 2005-05-30
EP1474420A1 (en) 2004-11-10
EP2292615A1 (en) 2011-03-09
KR20040077922A (ko) 2004-09-07
AR038476A1 (es) 2005-01-19
EP1474420B1 (en) 2012-03-14
CA2473572C (en) 2011-05-10
JP2005522428A (ja) 2005-07-28
CA2473572A1 (en) 2003-08-07
CY1112835T1 (el) 2016-02-10
MY144042A (en) 2011-07-29
IL163022A (en) 2012-10-31
KR101093345B1 (ko) 2011-12-14

Similar Documents

Publication Publication Date Title
RU2362775C1 (ru) Хиназолиновые соединения
EP2031563A3 (en) Method for rendering a region of a composite glyph
CY1110295T1 (el) Trans-9,10-δεϋδροεποθιλονη c και d, αναλογα αυτων και μεθοδοι παρασκευης
EA201000496A1 (ru) Замещенное соединение миноциклина, способ получения замещенных соединений миноциклина (варианты)
EP1258816A3 (en) Image search method and apparatus
JP2002535332A5 (ru)
JP2004537984A5 (ru)
JP2003339391A5 (ru)
JP2006502250A5 (ru)
MXPA05010855A (es) Metodo para obtener galio-68 y uso del mismo y dispositivo para realizar dicho metodo.
EP1587139A3 (en) Method of making a tantalum layer and apparatus using a tantalum layer
JP2004161990A5 (ru)
JP2004121220A5 (ru)
JP2003221429A5 (ru)
JP2003344223A5 (ru)
JP2004513102A5 (ru)
JP2002053846A5 (ru)
AU2002364417A1 (en) Method and device for notching tubes and the tube thus obtained
TW200420530A (en) Novel method for preparing methyl 2-diphenylmethylsulfinylacetate
JP2003183506A5 (ru)
JP2003154400A5 (ru)
JP2004505899A5 (ru)
JP2005503339A5 (ru)
JP2003156591A5 (ru)
JP2004294750A5 (ru)

Legal Events

Date Code Title Description
MM4A The patent is invalid due to non-payment of fees

Effective date: 20130129