PL2387563T5 - 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 - Google Patents

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

Info

Publication number
PL2387563T5
PL2387563T5 PL10701175.1T PL10701175T PL2387563T5 PL 2387563 T5 PL2387563 T5 PL 2387563T5 PL 10701175 T PL10701175 T PL 10701175T PL 2387563 T5 PL2387563 T5 PL 2387563T5
Authority
PL
Poland
Prior art keywords
cycloproane
methyloxy
quinolin
fluorophenyl
oxy
Prior art date
Application number
PL10701175.1T
Other languages
English (en)
Other versions
PL2387563T3 (pl
Inventor
Adrian St. Clair BROWN
Peter Lamb
William P. Gallagher
Original Assignee
Exelixis, 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41820137&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PL2387563(T5) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Exelixis, Inc. filed Critical Exelixis, Inc.
Publication of PL2387563T3 publication Critical patent/PL2387563T3/pl
Publication of PL2387563T5 publication Critical patent/PL2387563T5/pl

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61P35/00—Antineoplastic 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
PL10701175.1T 2009-01-16 2010-01-15 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 PL2387563T5 (pl)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US14542109P 2009-01-16 2009-01-16
PCT/US2010/021194 WO2010083414A1 (en) 2009-01-16 2010-01-15 Malate salt of n- (4- { [ 6, 7-bis (methyloxy) quin0lin-4-yl] oxy}phenyl-n' - (4 -fluorophenyl) cyclopropane-1-dicarboxamide, and crystalline forms therof for the treatment of cancer
EP10701175.1A EP2387563B2 (en) 2009-01-16 2010-01-15 Malate salt of n- (4- { [ 6, 7-bis (methyloxy) quinolin-4-yl]oxy}phenyl-n' - (4 -fluorophenyl) cyclopropane-1,1-dicarboxamide, and crystalline forms thereof for the treatment of cancer

Publications (2)

Publication Number Publication Date
PL2387563T3 PL2387563T3 (pl) 2013-08-30
PL2387563T5 true PL2387563T5 (pl) 2023-03-13

Family

ID=41820137

Family Applications (1)

Application Number Title Priority Date Filing Date
PL10701175.1T PL2387563T5 (pl) 2009-01-16 2010-01-15 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

Country Status (24)

Country Link
US (15) US8877776B2 (pl)
EP (1) EP2387563B2 (pl)
JP (6) JP5677318B2 (pl)
KR (9) KR20230008268A (pl)
CN (3) CN106083714B (pl)
AR (1) AR075025A1 (pl)
AU (3) AU2010204619B2 (pl)
BR (1) BRPI1006812B8 (pl)
CA (2) CA2995880C (pl)
DK (1) DK2387563T4 (pl)
EA (3) EA019959B1 (pl)
ES (1) ES2402524T5 (pl)
HR (1) HRP20130458T4 (pl)
IL (2) IL214086A (pl)
MX (3) MX350898B (pl)
NZ (3) NZ779754A (pl)
PL (1) PL2387563T5 (pl)
PT (1) PT2387563E (pl)
RS (1) RS52754B2 (pl)
SG (1) SG173014A1 (pl)
SM (1) SMT201300050B (pl)
TW (7) TW202112751A (pl)
WO (1) WO2010083414A1 (pl)
ZA (1) ZA201105167B (pl)

Families Citing this family (66)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2888102B2 (ja) 1993-08-26 1999-05-10 三菱電機株式会社 時間ダイバーシティ通信装置用送信機および受信機、並びに時間ダイバーシティ通信装置
PL2210607T3 (pl) * 2003-09-26 2012-01-31 Exelixis Inc N-[3-fluoro-4-({6-(metyloksy)-7-[(3-morfolin-4-ylopropylo)oksy]chinolin-4-ylo} oxy)fenylo]-N'-(4-fluorofenylo)cyklopropano-1,1-dikarboksamid do leczenia raka
US8877776B2 (en) 2009-01-16 2014-11-04 Exelixis, Inc. (L)-malate salt of N-(4-{[6,7-bis(methyloxy) quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
US20120070368A1 (en) * 2010-04-16 2012-03-22 Exelixis, Inc. Methods of Using C-Met Modulators
CN114209699A (zh) 2010-07-16 2022-03-22 埃克塞里艾克西斯公司 C-met调节剂药物组合物
PL2621481T5 (pl) * 2010-09-27 2023-03-13 Exelixis, Inc. Podwójne inhibitory MET i VEGF do leczenia opornego na kastrację raka prostaty i osteoblastycznych przerzutów do kości
KR20200031711A (ko) * 2011-02-10 2020-03-24 엑셀리시스, 인코포레이티드 퀴놀린 화합물들의 제조 방법들 및 상기 화합물들을 함유하는 약학 조성물들
US20120252840A1 (en) * 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
TW201806598A (zh) 2011-05-02 2018-03-01 艾克塞里克斯公司 治療癌症及骨癌疼痛之方法
AU2012312364B2 (en) * 2011-09-22 2017-11-09 Exelixis, Inc. Method for treating osteoporosis
TWI642650B (zh) 2011-10-20 2018-12-01 艾克塞里克斯公司 用於製備喹啉衍生物之方法
JP6238311B2 (ja) 2012-01-13 2017-11-29 エックススプレイ ファーマ パブリーク・アクチエボラグＸＳｐｒａｙ Ｐｈａｒｍａ ＡＢ（ｐｕｂｌ） 少なくとも１種のプロテインキナーゼ阻害剤及び少なくとも１種のポリマー性安定化マトリックス形成性成分の安定な非晶質のハイブリッドナノ粒子を含む医薬組成物
EP2844254A1 (en) 2012-05-02 2015-03-11 Exelixis, Inc. A dual met - vegf modulator for treating osteolytic bone metastases
EP2892532B1 (en) * 2012-09-07 2019-02-13 Exelixis, Inc. Inhibitors of met, vegfr and ret for use in the treatment of lung adenocarcinoma
CN103664776B (zh) * 2012-09-26 2016-05-04 正大天晴药业集团股份有限公司 一种酪氨酸激酶抑制剂及其中间体的制备方法
UA119321C2 (uk) 2013-03-15 2019-06-10 Екселіксіс, Інк. Метаболіти n-(4-{[6,7-біс(метилокси)хінолін-4-іл]окси}феніл)-n'-(4-фторфеніл)циклопропан-1,1-дикарбоксаміду
ES2927651T3 (es) * 2013-04-04 2022-11-10 Exelixis Inc Forma de dosificación de cabozantinib y uso en el tratamiento del cáncer
HK1221424A1 (zh) * 2013-04-04 2017-06-02 Exelixis, Inc. 治疗癌症的药物组合
CN104109124B (zh) * 2013-04-19 2016-08-31 正大天晴药业集团股份有限公司 卡博替尼·0.5苹果酸盐的晶体
CN104370811B (zh) * 2013-08-15 2019-02-12 广东东阳光药业有限公司 一种喹啉化合物的新晶型及其制备方法
CN104649969B (zh) * 2013-11-22 2019-02-12 广东东阳光药业有限公司 一种替尼类药物的盐及其制备方法
CN106068255A (zh) 2014-02-14 2016-11-02 埃克塞里艾克西斯公司 结晶固体形式的n‑{4‑[(6，7‑二甲氧基喹啉‑4‑基)氧基]苯基}‑n′‑(4‑氟苯基)环丙烷‑1，1‑二甲酰胺、制备方法以及使用方法
EA201691850A1 (ru) * 2014-03-17 2016-12-30 Экселиксис, Инк. Дозирование составов, содержащих кабозантиниб
BR112016024672A2 (pt) * 2014-04-25 2021-02-02 Exelixis, Inc método para o tratamento de adenocarcinoma de pulmão
WO2015177758A1 (en) 2014-05-23 2015-11-26 Mylan Laboratories Ltd Novel polymorphs of cabozantinib (s)-malate and cabozantinib free base
CN104788372B (zh) * 2014-07-25 2018-01-30 上海圣考医药科技有限公司 一种氘代卡博替尼衍生物、其制备方法、应用及其中间体
CN106715397B (zh) 2014-07-31 2021-07-23 埃克塞里艾克西斯公司 制备氟-18标记的卡博替尼及其类似物的方法
UA121482C2 (uk) 2014-08-05 2020-06-10 Екселіксіс, Інк. Комбінація інгібітору протеасом, яким є бортезоміб, та інгібітору c-met для лікування множинної мієломи
CN105503717A (zh) * 2014-09-24 2016-04-20 江苏奥赛康药业股份有限公司 一种苹果酸卡博替尼化合物及其药物组合物
CN104961680B (zh) * 2014-11-07 2017-09-12 苏州晶云药物科技有限公司 N‑(4‑{[6,7‑双(甲基氧基)喹啉‑4‑基]氧基}苯基)‑n’‑(4‑氟苯基)环丙烷‑1,1‑二甲酰胺的盐酸盐及其多晶型
CN104961681B (zh) * 2014-11-13 2017-06-13 苏州晶云药物科技有限公司 卡博替尼的粘酸盐及其晶型
US10206916B2 (en) 2015-03-25 2019-02-19 Sandoz Ag Cabozantinib salts and their use as anti-cancer agents
ES2716633T3 (es) 2015-03-25 2019-06-13 Sandoz Ag Formas cristalinas de fosfato de cabozantinib e hidrocloruro de cabozantinib
EP3337786B1 (en) 2015-08-19 2019-12-11 Sandoz AG Asymmetric bisamidation of malonic ester derivatives
CN109069499A (zh) * 2016-04-15 2018-12-21 埃克塞里艾克西斯公司 使用 n-(4-(6,7-二甲氧基喹啉-4-基氧基)苯基)-n’-(4-氟苯基)环丙烷-1,1-二甲酰胺,(2s)-羟基丁二酸盐治疗肾细胞癌的方法
US10980792B2 (en) 2016-09-12 2021-04-20 Zhuhai Beihai Biotech Co., Ltd. Formulations of Cabozantinib
KR101829706B1 (ko) * 2016-09-21 2018-02-19 씨제이헬스케어 주식회사 벤즈이미다졸 유도체의 산부가염
MX389966B (es) * 2017-01-20 2025-03-20 Exelixis Inc Combinaciones de cabozantinib y atezolizumab para tratar cancer.
CN108341773A (zh) * 2017-01-21 2018-07-31 南京华威医药科技开发有限公司 卡博替尼苹果酸盐的晶型ii
ES2909390T3 (es) 2017-05-26 2022-05-06 Exelixis Inc Formas sólidas cristalinas de sales de N-{4-[(6,7-dimetoxiquinolin-4-il)oxi]fenil}-N'-(4-fluorofenil)ciclopropano-1,1-dicarboxamida, procedimientos de fabricación y procedimientos de uso
JP7249962B2 (ja) 2017-06-09 2023-03-31 エグゼリクシス， インコーポレイテッド がんを治療するための液体剤形
CN109836382B (zh) * 2017-11-29 2021-11-05 江苏豪森药业集团有限公司 苹果酸卡博替尼及其中间体的制备方法
DK3743070T3 (da) 2018-01-26 2025-09-29 Exelixis Inc Forbindelser til behandling af kinaseafhængige lidelser
WO2019234761A1 (en) * 2018-06-05 2019-12-12 Natco Pharma Limited An improved process for the preparation of cabozantinib and its pharmaceutically acceptable salts thereof
TWI770624B (zh) 2018-06-15 2022-07-11 漢達生技醫藥股份有限公司 尼洛替尼十二烷基硫酸鹽在製備用於治療慢性骨髓性白血病之劑型的用途
WO2020075196A1 (en) 2018-10-11 2020-04-16 Cipla Limited Polymorphs of n-(4-(6,7-dimethoxyquinolin-4-yloxy) phenyl)-n'-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide, (s)- malate, methods of production and pharmaceutical uses thereof
AU2019395419B2 (en) 2018-12-13 2025-06-26 Exelixis, Inc. Crystalline forms and salt forms of a kinase inhibitor
IL289941B2 (en) 2019-07-19 2025-07-01 Biosynth Ag Method of making nicotinamide ribofuranoside salts, nicotinamide ribofuranoside salts as such, and uses thereof
CN112979544B (zh) * 2019-12-17 2024-06-28 江苏先声药业有限公司 一种卡博替尼或其盐的制备方法
WO2021209940A1 (en) * 2020-04-14 2021-10-21 Msn Laboratories Private Limited, R&D Center Pharmaceutical composition containing n-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, (2s)-hydroxybutanedioate
CA3176042A1 (en) * 2020-04-30 2021-11-04 Exelixis, Inc. Processes for the preparation of a kinase inhibitor
CN114456109B (zh) * 2020-11-09 2025-11-28 北京轩升制药有限公司 一种高纯度卡博替尼苹果酸盐的制备方法及其应用
IT202000027678A1 (it) 2020-11-18 2022-05-18 Indena Spa Dispersioni solide amorfe di cabozantinib-(s)-malato e processi per la loro preparazione
WO2022115464A1 (en) 2020-11-25 2022-06-02 Nanocopoeia, Llc Amorphous cabozantinib particles and uses thereof
WO2022177983A1 (en) 2021-02-19 2022-08-25 Slayback Pharma Llc Pharmaceutical compositions of cabozantinib
US20240190825A1 (en) * 2021-03-24 2024-06-13 Biocon Limited Process for preparation of cabozantinib
CN115215797B (zh) * 2021-04-15 2024-04-12 成都苑东生物制药股份有限公司 一种苹果酸卡博替尼新晶型及其制备方法
CN118339144A (zh) * 2021-12-03 2024-07-12 湖南湘源美东医药科技有限公司 卡博替尼共晶及制备方法以及作为药物或在药物制剂中的应用
WO2023165948A1 (en) 2022-03-01 2023-09-07 Synthon B.V. Cabozantinib salt with l-(+)-tartaric acid and solid forms thereof
WO2023222946A1 (en) 2022-05-18 2023-11-23 Fermion Oy Process for the preparation of cabozantinib
AU2024215796A1 (en) 2023-01-31 2025-05-15 Handa Oncology, Llc Improved cabozantinib compositions and methods of use
US11814356B1 (en) 2023-03-29 2023-11-14 Apotex Inc. Salt of cabozantinib
WO2025079089A1 (en) * 2023-10-09 2025-04-17 Msn Laboratories Private Limited, R&D Center Pharmaceutical composition of cabozantinib
WO2025090032A1 (en) * 2023-10-24 2025-05-01 Deva Holding Novel polymorph of cabozantinib l-tartrate (form a) and method of preparation
CN120058603A (zh) * 2025-03-04 2025-05-30 鲁南制药集团股份有限公司 一种卡博替尼新晶型

Family Cites Families (208)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2160201B (en) 1984-06-14 1988-05-11 Wyeth John & Brother Ltd Quinazoline and cinnoline derivatives
US5123951A (en) 1986-03-31 1992-06-23 Rhone-Poulenc Nederland B.V. Synergistic plant growth regulator compositions
JPS646261A (en) 1987-03-31 1989-01-10 Nisshin Flour Milling Co 4-thioquinazoline derivative, its production and antiulcer agent containing said derivative as active component
US5143854A (en) 1989-06-07 1992-09-01 Affymax Technologies N.V. Large scale photolithographic solid phase synthesis of polypeptides and receptor binding screening thereof
US5034393A (en) 1989-07-27 1991-07-23 Dowelanco Fungicidal use of pyridopyrimidine, pteridine, pyrimidopyrimidine, pyrimidopyridazine, and pyrimido-1,2,4-triazine derivatives
US5238951A (en) 1991-02-01 1993-08-24 E. R. Squibb & Sons, Inc. Heterocyclic amido prostaglandin analogs
DE4114733A1 (de) 1991-05-06 1992-11-12 Huels Chemische Werke Ag Verfahren zur herstellung von substituierten malonesteraniliden und malonsaeure-monoaniliden
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
US6057344A (en) 1991-11-26 2000-05-02 Sepracor, Inc. Methods for treating hypertension, and angina using optically pure (-) amlodipine
US6498144B1 (en) 1993-10-18 2002-12-24 North Shore - Long Island Jewish Research Institute Use of scatter factor to enhance angiogenesis
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
GB9510757D0 (en) 1994-09-19 1995-07-19 Wellcome Found Therapeuticaly active compounds
TW321649B (pl) 1994-11-12 1997-12-01 Zeneca Ltd
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
WO1996040648A1 (en) 1995-06-07 1996-12-19 Sugen, Inc. Quinazolines and pharmaceutical compositions
US5650415A (en) 1995-06-07 1997-07-22 Sugen, Inc. Quinoline compounds
DE69531558T2 (de) 1995-06-07 2004-03-18 Pfizer Inc. Heterocyclische kondensierte pyrimidin-derivate
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
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
GB9526546D0 (en) 1995-12-23 1996-02-28 Pfizer Ltd Compounds useful in therapy
DK0880508T3 (da) 1996-02-13 2003-06-30 Astrazeneca Ab Quinazolinderivater som VEGF-inhibitorer
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
CN1116286C (zh) 1996-03-05 2003-07-30 曾尼卡有限公司 4－苯胺基喹唑啉衍生物
US6514971B1 (en) 1996-03-15 2003-02-04 Zeneca Limited Cinnoline derivatives and use as medicine
US6107300A (en) 1996-03-27 2000-08-22 Dupont Pharmaceuticals Arylamino fused pyrimidines
SK284073B6 (sk) 1996-04-12 2004-09-08 Warner-Lambert Company Polycyklické zlúčeniny, ich použitie a farmaceutické kompozície na ich báze
CZ370298A3 (cs) 1996-05-20 1999-05-12 G. D. Searle Co. Draselné, sodné a trisoxaprozinové soli farmaceutických formulací
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
ATE227283T1 (de) 1996-07-13 2002-11-15 Glaxo Group Ltd Kondensierte heterozyklische verbindungen als protein kinase inhibitoren
US5962407A (en) 1996-07-26 1999-10-05 Kelly; Michael T. Loloatin derivatives and analogs
ATE300521T1 (de) 1996-09-25 2005-08-15 Astrazeneca Ab Chinolin-derivate die den effekt von wachstumsfaktoren wie vegf vezögern
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
JP4073961B2 (ja) 1996-10-01 2008-04-09 協和醗酵工業株式会社 含窒素複素環化合物
GB9700504D0 (en) 1997-01-11 1997-02-26 Pfizer Ltd Pharmaceutical compounds
GB9705361D0 (en) 1997-03-14 1997-04-30 Celltech Therapeutics Ltd Chemical compounds
UA73073C2 (uk) 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
EP0990647B1 (en) 1997-04-18 2003-07-02 Kirin Beer Kabushiki Kaisha Process for producing quinolone derivatives
NZ335822A (en) 1997-04-22 2001-05-25 Neurocrine Biosciences Inc Preparation and use of 2-methyl-4-dipropylamino-8(2',4'-dichlorophenyl)-quinoline and 2-methyl-4-(N-propyl-N-cyclopropanemethyl)amino-8(2',4'-dichlorophenyl)-quinoline for treating corticotropin-releasing factor related diseases
GB9708917D0 (en) 1997-05-01 1997-06-25 Pfizer Ltd Compounds useful in therapy
AR012634A1 (es) 1997-05-02 2000-11-08 Sugen Inc Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion
ZA986732B (en) 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitiors of tyrosine kinases
ATE368665T1 (de) 1997-08-22 2007-08-15 Astrazeneca Ab Oxindolylchinazolinderivate als angiogenesehemmer
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
WO1999061428A1 (en) 1998-05-28 1999-12-02 Parker Hughes Institute Quinazolines for treating brain tumor
PT1107964E (pt) 1998-08-11 2010-06-11 Novartis Ag Derivados de isoquinolina com actividade inibidora da angiogénese
JP2002523403A (ja) 1998-08-21 2002-07-30 パーカー ヒューズ インスティテュート キナゾリン誘導体
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
US6740326B1 (en) 1998-09-10 2004-05-25 Bioequal Ag Topical nail care compositions
US6288082B1 (en) 1998-09-29 2001-09-11 American Cyanamid Company Substituted 3-cyanoquinolines
CA2344169C (en) 1998-09-29 2011-07-19 American Cyanamid Company Substituted 3-cyanoquinolines as protein tyrosine kinases inhibitors
JP2002526538A (ja) 1998-10-01 2002-08-20 アストラゼネカ アクチボラグ 化学化合物
FR2784030B1 (fr) 1998-10-02 2002-12-20 Inst Nat Sante Rech Med Utilisation de bloqueurs des canaux calciques et/ou cgmp-dependants pour le traitement de pathologies de la retine
DK1119567T3 (da) 1998-10-08 2005-07-25 Astrazeneca Ab Quinazolinderivater
JP3687900B2 (ja) 1998-11-19 2005-08-24 ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー チロシンキナーゼの不可逆的阻害剤であるｎ−［４−（３−クロロ−４−フルオロフェニルアミノ）−７−（３−モルホリン−４−イルプロポキシ）キナゾリン−６−イル］アクリルアミド
WO2000043366A1 (en) 1999-01-22 2000-07-27 Kirin Beer Kabushiki Kaisha Quinoline derivatives and quinazoline derivatives
KR20080015482A (ko) 1999-02-10 2008-02-19 아스트라제네카 아베 혈관형성 억제제로서의 퀴나졸린 유도체
GB9904103D0 (en) 1999-02-24 1999-04-14 Zeneca Ltd Quinoline derivatives
US6080747A (en) 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
DE19911509A1 (de) 1999-03-15 2000-09-21 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
WO2000056338A1 (en) 1999-03-19 2000-09-28 Parker Hughes Institute Quinazoline formulations and therapeutic use thereof
US6258820B1 (en) 1999-03-19 2001-07-10 Parker Hughes Institute Synthesis and anti-tumor activity of 6,7-dialkoxy-4-phenylamino-quinazolines
YU13200A (sh) 1999-03-31 2002-10-18 Pfizer Products Inc. Postupci i intermedijeri za dobijanje anti-kancernih jedinjenja
EP1169041A2 (en) 1999-03-31 2002-01-09 The Procter & Gamble Company Use of carbamic acid derivatives for the treatment of viral infections
GB9910580D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
GB9910577D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
US6126917A (en) 1999-06-01 2000-10-03 Hadasit Medical Research Services And Development Ltd. Epidermal growth factor receptor binding compounds for positron emission tomography
CA2375259C (en) 1999-06-21 2009-04-28 Boehringer Ingelheim Pharma Kg Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them
GB9922171D0 (en) 1999-09-21 1999-11-17 Zeneca Ltd Chemical compounds
JP4870304B2 (ja) 1999-09-21 2012-02-08 アストラゼネカ アクチボラグ キナゾリン誘導体およびそれらの医薬品としての使用
US6759410B1 (en) 1999-11-23 2004-07-06 Smithline Beecham Corporation 3,4-dihydro-(1H)-quinazolin-2-ones and their use as CSBP/p38 kinase inhibitors
CA2392554A1 (en) 1999-11-30 2001-06-28 Parker Hughes Institute Inhibitors of thrombin induced platelet aggregation
US20020002169A1 (en) 1999-12-08 2002-01-03 Griffin John H. Protein kinase inhibitors
US7135466B2 (en) 1999-12-24 2006-11-14 Kirin Beer Kabushiki Kaisha Quinoline and quinazoline derivatives and drugs containing the same
US6525046B1 (en) 2000-01-18 2003-02-25 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as antiinflammatory agents
US6977259B2 (en) 2000-01-28 2005-12-20 Astrazeneca Ab Quinoline derivatives and their use as aurora 2 kinase inhibitors
US6664390B2 (en) 2000-02-02 2003-12-16 Warner-Lambert Company Llc Method for the simplified production of (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-nitro-quinazoline-4-yl]-amine or (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-amino-quinazoline-4-yl]-amine
KR20020084116A (ko) 2000-02-07 2002-11-04 애보트 게엠베하 운트 콤파니 카게 2-벤조티아졸릴 우레아 유도체 및 이의 단백질 키나제억제제로서의 용도
CZ303705B6 (cs) 2000-02-15 2013-03-27 Sugen, Inc. Pyrrolem substituovaná 2-indolinonová sloucenina pro pouzití jako inhibitor proteinkináz a farmaceutická kompozice s jejím obsahem
HUP0300547A2 (hu) 2000-03-13 2003-07-28 American Cyanamid Co. Ciano-kinolin vegyületek alkalmazása vastagbél polipok kezelésére és gátlására alkalmas gyógyszerkészítmények előállítására
US6521618B2 (en) 2000-03-28 2003-02-18 Wyeth 3-cyanoquinolines, 3-cyano-1,6-naphthyridines, and 3-cyano-1,7-naphthyridines as protein kinase inhibitors
US6608048B2 (en) 2000-03-28 2003-08-19 Wyeth Holdings Tricyclic protein kinase inhibitors
US6627634B2 (en) 2000-04-08 2003-09-30 Boehringer Ingelheim Pharma Kg Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them
UA73993C2 (uk) 2000-06-06 2005-10-17 Астразенека Аб Хіназолінові похідні для лікування пухлин та фармацевтична композиція
PT1292591E (pt) 2000-06-22 2005-06-30 Pfizer Prod Inc Derivados biciclicos substituidos para o tratamento de crescimento de celula anormal
EP1174118A1 (de) 2000-06-28 2002-01-23 Cognis France S.A. Verwendung von Inulinen und Inulinderivaten
PL360439A1 (pl) 2000-06-28 2004-09-06 Astrazeneca Ab Podstawione pochodne chinazoliny i ich zastosowanie jako inhibitorów
FR2811658B1 (fr) 2000-07-17 2004-07-02 Cfpi Nufarm Reacteur biologique a lit fixe immerge et procede de traitement d'effluents liquides
JP2002030083A (ja) * 2000-07-18 2002-01-29 Kirin Brewery Co Ltd Ｎ−（２−クロロ−４−｛［６−メトキシ−７−（３−ピリジルメトキシ）−４−キノリル］オキシ｝フェニル）−ｎ’−プロピルウレアの二塩酸塩
US7427689B2 (en) 2000-07-28 2008-09-23 Georgetown University ErbB-2 selective small molecule kinase inhibitors
KR100821446B1 (ko) 2000-08-21 2008-04-10 아스트라제네카 아베 퀴나졸린 유도체
FR2813307B1 (fr) 2000-08-23 2002-11-08 Sanofi Synthelabo Aminoalkenylbenzoyl-benzofurannes ou benzothiophenes, leur procede de preparation et les compositions les contenant
DE10042058A1 (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
US6403580B1 (en) 2000-08-26 2002-06-11 Boehringer Ingelheim Pharma Kg Quinazolines, pharmaceutical compositions containing these compounds, their use and processes for preparing them
US6656946B2 (en) 2000-08-26 2003-12-02 Boehringer Ingelheim Pharma Kg Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases
US6740651B2 (en) 2000-08-26 2004-05-25 Boehringer Ingelheim Pharma Kg Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases
US6653305B2 (en) 2000-08-26 2003-11-25 Boehringer Ingelheim Pharma Kg Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them
JP2004511479A (ja) 2000-10-13 2004-04-15 アストラゼネカ　アクチボラグ キナゾリン誘導体
EP1326860A1 (en) 2000-10-13 2003-07-16 AstraZeneca AB Quinazoline derivatives
DE60137273D1 (de) 2000-10-20 2009-02-12 Eisai R&D Man Co Ltd Verfahren zur Herstellung von 4-Phenoxy chinolin Derivaten
US20040063733A1 (en) 2000-10-25 2004-04-01 Lambert Christine Marie Paul Quinazoline derivatives
US7067532B2 (en) 2000-11-02 2006-06-27 Astrazeneca Substituted quinolines as antitumor agents
EP1340748B1 (en) 2000-11-02 2008-01-16 Nippon Shinyaku Co., Ltd. Quinazoline derivatives and drugs
EP1337513A1 (en) 2000-11-02 2003-08-27 AstraZeneca AB 4-substituted quinolines as antitumor agents
US7019012B2 (en) 2000-12-20 2006-03-28 Boehringer Ingelheim International Pharma Gmbh & Co. Kg Quinazoline derivatives and pharmaceutical compositions containing them
US6900220B2 (en) 2001-01-02 2005-05-31 Syntex (U.S.A.) Llc Quinazolone derivatives as alpha 1A/B adrenergic receptor antagonists
GB0103046D0 (en) 2001-02-07 2001-03-21 Novartis Ag Organic Compounds
JP2002265365A (ja) 2001-03-08 2002-09-18 Koyo Chemical Kk 好中球機能抑制剤
DE60229046D1 (de) 2001-04-19 2008-11-06 Astrazeneca Ab Chinazolin derivate
WO2002088110A1 (en) 2001-04-27 2002-11-07 Kirin Beer Kabushiki Kaisha Quinoline derivative having azolyl group and quinazoline derivative
SE0101675D0 (sv) 2001-05-11 2001-05-11 Astrazeneca Ab Novel composition
WO2002092577A1 (en) 2001-05-14 2002-11-21 Astrazeneca Ab Quinazoline derivatives
WO2002092578A1 (en) 2001-05-14 2002-11-21 Astrazeneca Ab Quinazoline derivatives
WO2002092579A1 (en) 2001-05-14 2002-11-21 Astrazeneca Ab 4-anilinoquinazoline derivatives
US6734303B2 (en) 2001-05-18 2004-05-11 Pfizer Inc. Process for the production of quinazolines
DE10125432A1 (de) 2001-05-25 2002-11-28 Bayer Ag Substituierte Benzoylketone
US7132427B2 (en) 2001-06-21 2006-11-07 Ariad Pharmaceuticals, Inc. Quinazolines and uses thereof
US7425564B2 (en) 2001-06-22 2008-09-16 Kirin Beer Kabushiki Kaisha Quinoline derivative and quinazoline derivative inhibiting self-phosphorylation of hepatocytus prolifertor receptor and medicinal composition containing the same
KR100397792B1 (ko) 2001-06-28 2003-09-13 한국과학기술연구원 4-(페닐아미노)-[1,4]디옥사노[2,3-ｇ]퀴나졸린 유도체 및그의 제조방법
GB0118752D0 (en) 2001-08-01 2001-09-26 Pfizer Ltd Process for the production of quinazolines
US7229774B2 (en) 2001-08-02 2007-06-12 Regents Of The University Of Michigan Expression profile of prostate cancer
EP2332934B1 (en) 2001-08-15 2017-03-01 Pharmacia & Upjohn Company LLC Processes for the preparation of crystals including a malic acid salt of n-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3h-indole-3-ylidene)methyl]-2,4-dimethyl-1h-pyrrole-3-carboxamide.
US20030066060A1 (en) 2001-09-28 2003-04-03 Ford Richard L. Cross profile guided optimization of program execution
EP1447405A4 (en) 2001-10-17 2005-01-12 Kirin Brewery CHINOLIN OR CHINAZOLINE DERIVATIVES THAT PREVENT THE AUTOPHOSPHORYLATION OF RECEPTORS FOR THE FIBROBLAST GROWTH FACTOR
US7169788B2 (en) 2001-10-30 2007-01-30 Merck & Co., Inc. Tyrosine kinase inhibitors
GB0126433D0 (en) 2001-11-03 2002-01-02 Astrazeneca Ab Compounds
US7319107B2 (en) 2001-11-08 2008-01-15 Johnson & Johnson Consumer Companies, Inc. 1,2,4-thiadiazolium derivatives as melanocortin receptor modulators
GB0128108D0 (en) 2001-11-23 2002-01-16 Astrazeneca Ab Therapeutic use
MXPA04004969A (es) 2001-11-27 2004-08-11 Wyeth Corp 3-cianoquinolinas como inhibidores del receptor del factor de crecimiento epidermico y her2 cinasas.
GB0129099D0 (en) 2001-12-05 2002-01-23 Astrazeneca Ab Chemical compounds
AU2002347336A1 (en) 2001-12-05 2003-06-17 Astrazeneca Ab Quinoline derivatives
WO2003047584A1 (en) 2001-12-05 2003-06-12 Astrazeneca Ab Quinoline derivatives
AU2002360582B2 (en) 2001-12-10 2009-06-11 Aryx Therapeutics Novel compounds for the treatment of cardiac arrhythmia, synthesis, and methods of use
AU2002339687A1 (en) 2001-12-12 2003-06-23 Pfizer Products Inc. Quinazoline derivatives for the treatement of abnormal cell growth
GEP20063872B (en) 2001-12-12 2006-07-10 Pfizer Prod Inc Salt forms of e-2-methoxy-n-(3-{4-[3-methyl-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quina-zolin-6-yl}-allyl)-acetamide and method of production
TW200301123A (en) 2001-12-21 2003-07-01 Astrazeneca Uk Ltd New use
WO2003055866A1 (en) 2001-12-21 2003-07-10 Bayer Pharmaceuticals Corporation Quinazoline and quinoline derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents
JP4498741B2 (ja) 2001-12-24 2010-07-07 アストラゼネカ アクチボラグ オーロラキナーゼ阻害剤としての置換キナゾリン誘導体
TW200406410A (en) 2002-01-29 2004-05-01 Glaxo Group Ltd Compounds
JP4508650B2 (ja) 2002-01-29 2010-07-21 グラクソ グループ リミテッド アミノピペリジン化合物、当該化合物の製法および当該化合物を含有する医薬組成物
RU2365588C2 (ru) 2002-02-01 2009-08-27 Астразенека Аб Хиназолиновые соединения
DE10204462A1 (de) 2002-02-05 2003-08-07 Boehringer Ingelheim Pharma Verwendung von Tyrosinkinase-Inhibitoren zur Behandlung inflammatorischer Prozesse
TW200813014A (en) 2002-03-28 2008-03-16 Astrazeneca Ab Quinazoline derivatives
DE10217689A1 (de) 2002-04-19 2003-11-13 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, ihre Verwendung und Verfahren zu ihrer Herstellung
US6693198B2 (en) 2002-04-22 2004-02-17 Xanthus Life Sciences, Inc. Amonafide salts
AU2003235838A1 (en) 2002-05-01 2003-11-17 Kirin Beer Kabushiki Kaisha Quinoline derivatives and quinazoline derivatives inhibiting autophosphorylation of macrophage colony stimulating factor receptor
US7323479B2 (en) 2002-05-17 2008-01-29 Celgene Corporation Methods for treatment and management of brain cancer using 1-oxo-2-(2,6-dioxopiperidin-3-yl)-4-methylisoindoline
US7576074B2 (en) 2002-07-15 2009-08-18 Rice Kenneth D Receptor-type kinase modulators and methods of use
GB0219746D0 (en) 2002-08-23 2002-10-02 Inst Of Ex Botany Ascr Azapurine derivatives
EP1548008A4 (en) 2002-08-23 2008-08-06 Kirin Pharma Kk COMPOUND WITH TGF-BETA-HEMMENDER EFFECT AND THIS MEDICAL COMPOSITION CONTAINING
US7419984B2 (en) 2002-10-17 2008-09-02 Cell Therapeutics, Inc. Pyrimidines and uses thereof
DE60316590T2 (de) 2002-10-21 2008-06-19 Kirin Beer K.K. N-(2-CHLOR-4-((6,7-DIMETHOXY-4-CHINOLYL)OXYÜPHENYLü-N'-(5-METHYL-3-ISOXAZOLYL)HARNSTOFFSALZIN KRISTALLINER FORM
AU2003280599A1 (en) 2002-10-29 2004-05-25 Kirin Beer Kabushiki Kaisha QUINOLINE DERIVATIVES AND QUINAZOLINE DERIVATIVES INHIBITING AUTOPHOSPHORYLATION OF Flt3 AND MEDICINAL COMPOSITIONS CONTAINING THE SAME
CA2503371C (en) 2002-11-04 2011-01-11 Astrazeneca Ab Quinazoline derivatives as src tyrosine kinase inhibitors
EP1569925A1 (en) 2002-12-13 2005-09-07 Neurogen Corporation 2-substituted quinazolin-4-ylamine analogues as capsaicin receptor modulators
PL377686A1 (pl) 2002-12-18 2006-02-06 Pfizer Products Inc. Pochodne 4-anilinochinazoliny do leczenia anormalnego wzrostu komórek
EP1575591A4 (en) 2002-12-23 2007-09-12 Ariad Pharma Inc HETEROCYCLES AND ITS USE
WO2004060373A1 (ja) 2002-12-27 2004-07-22 Santen Pharmaceutical Co., Ltd. 滲出型加齢黄斑変性治療剤
US8176532B1 (en) 2003-03-17 2012-05-08 Sprint Communications Company L.P. Secure access point for scada devices
EP1608373A4 (en) 2003-03-19 2010-09-29 Exelixis Inc TIE-2 MODULATORS AND USE METHOD
KR100559180B1 (ko) 2003-05-20 2006-03-14 김민서 조건부 거래에 따른 전자결제 방법 및 전자결제 서버
WO2005003140A1 (en) 2003-07-02 2005-01-13 Pharmacia & Upjohn Company Llc 4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carboxamides as antiviral agents
WO2005005389A2 (en) 2003-07-07 2005-01-20 Merck Patent Gmbh Malonamide derivatives
JP4299090B2 (ja) * 2003-09-24 2009-07-22 株式会社東海理化電機製作所 車両用空調装置の操作装置
PL2210607T3 (pl) * 2003-09-26 2012-01-31 Exelixis Inc N-[3-fluoro-4-({6-(metyloksy)-7-[(3-morfolin-4-ylopropylo)oksy]chinolin-4-ylo} oxy)fenylo]-N'-(4-fluorofenylo)cyklopropano-1,1-dikarboksamid do leczenia raka
AU2004288709B2 (en) 2003-11-07 2011-01-06 Novartis Vaccines And Diagnostics, Inc. Methods for synthesizing quinolinone compounds
EP2567955A3 (en) 2003-12-25 2013-03-27 Eisai R&D Management Co., Ltd. Crystal of salt of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide or of solvate thereof and processes for producing these
EP1711495A2 (en) 2004-01-23 2006-10-18 Amgen Inc. Quinoline, quinazoline, pyridine and pyrimidine counds and their use in the treatment of inflammation, angiogenesis and cancer
AR047530A1 (es) 2004-02-04 2006-01-25 Novartis Ag Formas de sal de 4-(4-metilpiperazin-1-ilmetil)-n-(4-metil-3-(4-piridin-3-il)pirimidin-2-ilamino)fenil)-benzamida
US20060035940A1 (en) 2004-03-16 2006-02-16 Sepracor Inc. (S)-Amlodipine malate
US7173031B2 (en) 2004-06-28 2007-02-06 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
JP5368701B2 (ja) 2004-07-02 2013-12-18 エクセリクシス、インコーポレイテッド ｃ−Ｍｅｔモジュレーター及び使用方法
EP1853968A2 (en) * 2005-03-04 2007-11-14 Colorlink, Inc. Four panel projection system
AU2006231646A1 (en) 2005-04-06 2006-10-12 Exelixis, Inc. C-Met modulators and methods of use
WO2007062135A2 (en) 2005-11-23 2007-05-31 Junji Shiraishi Computer-aided method for detection of interval changes in successive whole-body bone scans and related computer program product and system
WO2007102074A2 (en) 2006-03-07 2007-09-13 Cadila Healthcare Limited Salts of quetiapine
CA2645137A1 (en) 2006-03-07 2007-09-13 James F. Blake Heterobicyclic pyrazole compounds and methods of use
WO2007109799A2 (en) 2006-03-23 2007-09-27 Teva Pharmaceutical Industries Ltd. Polymorphs of eszopiclone malate
US20080004273A1 (en) 2006-05-30 2008-01-03 Stephane Raeppel Inhibitors of protein tyrosine kinase activity
ES2375284T3 (es) 2006-08-23 2012-02-28 Eisai R&D Management Co., Ltd. Sal de un derivado de fenoxipiridina, o cristal de la misma, y procedimiento de producción de la misma.
US20100074897A1 (en) 2006-12-01 2010-03-25 University Of Utah Research Foundation Methods and Compositions related to HIF-1 alpha
EP2101759B1 (en) 2006-12-14 2018-10-10 Exelixis, Inc. Methods of using mek inhibitors
US20080200515A1 (en) 2006-12-29 2008-08-21 Tap Pharmaceutical Products Inc. Solid state forms of enantiopure ilaprazole
CA2812705C (en) 2007-12-19 2015-08-18 Sunovion Pharmaceuticals Inc. Maleate, besylate and l-malate salts of 6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5h-pyrrolo[3,4-b]pyrazine
UY31800A (es) 2008-05-05 2009-11-10 Smithkline Beckman Corp Metodo de tratamiento de cancer usando un inhibidor de cmet y axl y un inhibidor de erbb
TW201035017A (en) 2008-09-26 2010-10-01 Smithkline Beecham Corp Preparation of a quinolinyloxydiphenylcyclopropanedicarboxamide
AU2009300328A1 (en) 2008-10-01 2010-04-08 Ludwig Institute For Cancer Research Methods for the treatment of cancer
CN102282134B (zh) 2008-11-13 2015-04-01 埃克塞里艾克西斯公司 喹啉衍生物制备方法
TW201028383A (en) 2008-12-04 2010-08-01 Exelixis Inc Methods of preparing quinoline derivatives
US8877776B2 (en) 2009-01-16 2014-11-04 Exelixis, Inc. (L)-malate salt of N-(4-{[6,7-bis(methyloxy) quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
WO2011009095A1 (en) 2009-07-17 2011-01-20 Exelixis, Inc. Crystalline forms of n-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]-quin0lin-4-yl}oxy)phenyl]-n'-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
WO2011031840A1 (en) 2009-09-09 2011-03-17 Quintiles Transnational Corp. Methods and compositions for the treatment of receptor tyrosine kinase mediated diseases or disorders
TW201202228A (en) 2010-03-12 2012-01-16 Exelixis Inc Hydrated crystalline forms of N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]-quinolin-4-yl}oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide
US20120070368A1 (en) 2010-04-16 2012-03-22 Exelixis, Inc. Methods of Using C-Met Modulators
CN114209699A (zh) 2010-07-16 2022-03-22 埃克塞里艾克西斯公司 C-met调节剂药物组合物
PL2621481T5 (pl) 2010-09-27 2023-03-13 Exelixis, Inc. Podwójne inhibitory MET i VEGF do leczenia opornego na kastrację raka prostaty i osteoblastycznych przerzutów do kości
KR20200031711A (ko) 2011-02-10 2020-03-24 엑셀리시스, 인코포레이티드 퀴놀린 화합물들의 제조 방법들 및 상기 화합물들을 함유하는 약학 조성물들
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
AU2012312364B2 (en) 2011-09-22 2017-11-09 Exelixis, Inc. Method for treating osteoporosis
EP2844254A1 (en) 2012-05-02 2015-03-11 Exelixis, Inc. A dual met - vegf modulator for treating osteolytic bone metastases
EP2892532B1 (en) 2012-09-07 2019-02-13 Exelixis, Inc. Inhibitors of met, vegfr and ret for use in the treatment of lung adenocarcinoma
HK1221424A1 (zh) 2013-04-04 2017-06-02 Exelixis, Inc. 治疗癌症的药物组合
EA201691850A1 (ru) 2014-03-17 2016-12-30 Экселиксис, Инк. Дозирование составов, содержащих кабозантиниб

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