AU2004289672C1 - Inhibition of FGFR3 and treatment of multiple myeloma - Google Patents
Inhibition of FGFR3 and treatment of multiple myeloma Download PDFInfo
- Publication number
- AU2004289672C1 AU2004289672C1 AU2004289672A AU2004289672A AU2004289672C1 AU 2004289672 C1 AU2004289672 C1 AU 2004289672C1 AU 2004289672 A AU2004289672 A AU 2004289672A AU 2004289672 A AU2004289672 A AU 2004289672A AU 2004289672 C1 AU2004289672 C1 AU 2004289672C1
- Authority
- AU
- Australia
- Prior art keywords
- substituted
- unsubstituted
- groups
- alkyl
- heterocyclyl
- 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.)
- Ceased
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/4353—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 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
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
- C07C51/41—Preparation of salts of carboxylic acids
- C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C59/01—Saturated compounds having only one carboxyl group and containing hydroxy or O-metal groups
- C07C59/08—Lactic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Emergency Medicine (AREA)
- Psychiatry (AREA)
- Physical Education & Sports Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (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)
- Medicinal Preparation (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US51791503P | 2003-11-07 | 2003-11-07 | |
| US60/517,915 | 2003-11-07 | ||
| US52642503P | 2003-12-02 | 2003-12-02 | |
| US52642603P | 2003-12-02 | 2003-12-02 | |
| US60/526,426 | 2003-12-02 | ||
| US60/526,425 | 2003-12-02 | ||
| US54601704P | 2004-02-19 | 2004-02-19 | |
| US60/546,017 | 2004-02-19 | ||
| PCT/US2004/036956 WO2005047244A2 (en) | 2003-11-07 | 2004-11-05 | Inhibition of fgfr3 and treatment of multiple myeloma |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| AU2004289672A1 AU2004289672A1 (en) | 2005-05-26 |
| AU2004289672B2 AU2004289672B2 (en) | 2010-06-24 |
| AU2004289672C1 true AU2004289672C1 (en) | 2010-12-02 |
Family
ID=34596121
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2004289672A Ceased AU2004289672C1 (en) | 2003-11-07 | 2004-11-05 | Inhibition of FGFR3 and treatment of multiple myeloma |
| AU2004288709A Ceased AU2004288709B2 (en) | 2003-11-07 | 2004-11-05 | Methods for synthesizing quinolinone compounds |
| AU2011202249A Ceased AU2011202249B2 (en) | 2003-11-07 | 2011-05-16 | Pharmaceutically acceptable salts of quinolinone compounds having improved pharmaceutical properties |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2004288709A Ceased AU2004288709B2 (en) | 2003-11-07 | 2004-11-05 | Methods for synthesizing quinolinone compounds |
| AU2011202249A Ceased AU2011202249B2 (en) | 2003-11-07 | 2011-05-16 | Pharmaceutically acceptable salts of quinolinone compounds having improved pharmaceutical properties |
Country Status (14)
| Country | Link |
|---|---|
| US (7) | US20050209247A1 (https=) |
| EP (4) | EP2762475A1 (https=) |
| JP (5) | JP4724665B2 (https=) |
| KR (3) | KR20060111520A (https=) |
| CN (1) | CN102225926A (https=) |
| AU (3) | AU2004289672C1 (https=) |
| BR (1) | BRPI0416143A (https=) |
| CA (3) | CA2544492C (https=) |
| EA (1) | EA012621B1 (https=) |
| ES (1) | ES2486240T3 (https=) |
| IL (5) | IL174471A (https=) |
| MX (1) | MXPA06004194A (https=) |
| TW (1) | TWI347940B (https=) |
| WO (3) | WO2005046589A2 (https=) |
Families Citing this family (96)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE448226T1 (de) | 2000-09-01 | 2009-11-15 | Novartis Vaccines & Diagnostic | Aza heterocyclische derivate und ihre therapeutische verwendung |
| DE60115069T2 (de) | 2000-09-11 | 2006-08-03 | Chiron Corp., Emeryville | Chinolinonderivate als tyrosin-kinase inhibitoren |
| US20030028018A1 (en) * | 2000-09-11 | 2003-02-06 | Chiron Coporation | Quinolinone derivatives |
| EP1539754A4 (en) | 2002-08-23 | 2009-02-25 | Novartis Vaccines & Diagnostic | BENZIMIDAZOCHINOLINONE AND ITS USE |
| US7825132B2 (en) * | 2002-08-23 | 2010-11-02 | Novartis Vaccines And Diagnostics, Inc. | Inhibition of FGFR3 and treatment of multiple myeloma |
| SG148864A1 (en) * | 2002-11-13 | 2009-01-29 | Chiron Corp | Methods of treating cancer and related methods |
| US20050209247A1 (en) * | 2003-11-07 | 2005-09-22 | Chiron Corporation | Pharmaceutically acceptable salts of quinolinone compounds having improved pharmaceutical properties |
| EP1718306A2 (en) * | 2004-02-20 | 2006-11-08 | Chiron Corporation | Modulation of inflammatory and metastatic processes |
| EP2301546B1 (en) * | 2005-01-27 | 2014-09-10 | Novartis AG | Treatment of metastasized tumors |
| US8034823B2 (en) * | 2005-02-22 | 2011-10-11 | Savvipharm Inc | Method of increasing drug oral bioavailability and compositions of less toxic orotate salts |
| ES2732251T3 (es) * | 2005-04-25 | 2019-11-21 | Enterin Inc | Dilactato de escualamina cristalino |
| EP1885187B1 (en) * | 2005-05-13 | 2013-09-25 | Novartis AG | Methods for treating drug resistant cancer |
| EP2465857B1 (en) * | 2005-05-17 | 2014-06-04 | Novartis AG | Methods for synthesizing heterocyclic compounds |
| AU2012258324B2 (en) * | 2005-05-17 | 2014-07-24 | Novartis Ag | Methods for synthesizing heterocyclic compounds |
| BRPI0611375A2 (pt) * | 2005-05-23 | 2010-08-31 | Novartis Ag | formas cristalinas e outras de sais de ácido láctico de 4-amino-5-flúor-3-[6-(4-metilpiperazin-1-il)-1h-benzimid azol-2-il]-1h-quinolin-2-ona |
| US20080207572A1 (en) * | 2005-07-14 | 2008-08-28 | Ab Science | Use of Dual C-Kit/Fgfr3 Inhibitors for Treating Multiple Myeloma |
| CN101316593B (zh) * | 2005-11-29 | 2012-05-02 | 诺瓦提斯公司 | 喹啉酮类的制剂 |
| NZ567550A (en) * | 2005-11-29 | 2011-08-26 | Novartis Ag | Formulations of lactic acid salts of 4-amino-5-fluoro-3-[6-(4-methyl-piperazin-1-yl)-1 H-benzimidazol-2-yl]1H-quinolin-2-one |
| KR20080080525A (ko) | 2005-12-08 | 2008-09-04 | 노파르티스 아게 | 유전자 전사에 대한 fgfr3의 억제제의 효과 |
| CN100488960C (zh) * | 2006-03-09 | 2009-05-20 | 中国药科大学 | 2-位取代的喹诺酮类化合物及其在制药中的应用 |
| WO2008044041A1 (en) | 2006-10-12 | 2008-04-17 | Astex Therapeutics Limited | Pharmaceutical combinations |
| EP2073807A1 (en) | 2006-10-12 | 2009-07-01 | Astex Therapeutics Limited | Pharmaceutical combinations |
| CA2679268A1 (en) * | 2007-03-09 | 2008-09-18 | Novartis Ag | Treatment of melanoma |
| EP2170859A1 (en) | 2007-06-25 | 2010-04-07 | F. Hoffmann-Roche AG | Benzimidazole amido derivatives as kinase inhibitors |
| GB0800855D0 (en) | 2008-01-17 | 2008-02-27 | Syngenta Ltd | Herbicidal compounds |
| JPWO2009113436A1 (ja) * | 2008-03-14 | 2011-07-21 | 国立大学法人 千葉大学 | Fgfr3遺伝子阻害剤の放射線照射併用による放射線の抗癌作用増強法および副作用軽減法 |
| PE20091628A1 (es) * | 2008-03-19 | 2009-11-19 | Novartis Ag | Formas cristalinas y dos formas solvatadas de sales de acido lactico de 4-amino-5-fluoro-3-[5-(4-metilpiperazin-1-il)-1h-benzimidazol-2-il]quinolin-2(1h)-ona |
| JP2012509321A (ja) * | 2008-11-21 | 2012-04-19 | ミレニアム ファーマシューティカルズ, インコーポレイテッド | 癌および他の疾患または障害の処置のための、4−[6−メトキシ−7−(3−ピペリジン−1−イル−プロポキシ)キナゾリン−4−イル]ピペラジン−1−カルボン酸(4−イソプロポキシフェニル)−アミドの乳酸塩およびその薬学的組成物 |
| WO2010075443A1 (en) * | 2008-12-22 | 2010-07-01 | Burnham Institute For Medical Research | Selective inhibitors of akt and methods of using same |
| NZ779754A (en) | 2009-01-16 | 2023-04-28 | Exelixis Inc | 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 |
| UA108618C2 (uk) | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
| MX2012011090A (es) | 2010-03-26 | 2012-10-10 | Novartis Ag | Preparacion de polimorfos hidratados de sal de acido lactico de la 4-amino-5-fluoro-3-[6-(4-metil-piperazin-1-il)-1h-bencimidazol- 2-il]-1h-quinolin-2-ona. |
| CN102834094B (zh) * | 2010-04-16 | 2015-05-06 | 诺华有限公司 | 有机化合物的组合产品及其制药用途 |
| GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| EA030435B1 (ru) * | 2010-07-16 | 2018-08-31 | Экселиксис, Инк. | ТАБЛЕТКА, СОДЕРЖАЩАЯ МОДУЛЯТОР c-MET В ФОРМЕ КРИСТАЛЛИЧЕСКОЙ L-МАЛАТНОЙ СОЛИ (ВАРИАНТЫ), СПОСОБ ЕЕ ПРОИЗВОДСТВА И СПОСОБ ЛЕЧЕНИЯ ОНКОЛОГИЧЕСКОГО ЗАБОЛЕВАНИЯ С ЕЕ ИСПОЛЬЗОВАНИЕМ |
| GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| BR112013020362A2 (pt) | 2011-02-10 | 2018-05-29 | Exelixis Inc | processos para a preparação de compostos de quinolina, compostos e combinações farmacêuticas que os contem |
| EP2524915A1 (en) * | 2011-05-20 | 2012-11-21 | Sanofi | 2-Amino-3-(imidazol-2-yl)-pyridin-4-one derivatives and their use as VEGF receptor kinase inhibitors |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| GB201118652D0 (en) * | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
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| WO2013088191A1 (en) | 2011-12-12 | 2013-06-20 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Antagonist of the fibroblast growth factor receptor 3 (fgfr3) for use in the treatment or the prevention of skeletal disorders linked with abnormal activation of fgfr3 |
| EP2809312A1 (en) | 2012-01-31 | 2014-12-10 | Novartis AG | Combination of a rtk inhibitor with an anti - estrogen and use thereof for the treatment of cancer |
| PL2824181T3 (pl) | 2012-03-08 | 2019-02-28 | Astellas Pharma Inc. | Nowa fuzja fgfr3 |
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| ES2670550T3 (es) | 2013-10-14 | 2018-05-30 | Eisai R&D Management Co., Ltd. | Derivados de quinolina selectivamente sustituidos |
| SG10202103278TA (en) | 2013-10-14 | 2021-04-29 | Eisai R&D Man Co Ltd | Selectively substituted quinoline compounds |
| US9458169B2 (en) | 2013-11-01 | 2016-10-04 | 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 |
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