MX349550B - 1,7-diazacarbazoles y metodos de uso. - Google Patents
1,7-diazacarbazoles y metodos de uso.Info
- Publication number
- MX349550B MX349550B MX2012006822A MX2012006822A MX349550B MX 349550 B MX349550 B MX 349550B MX 2012006822 A MX2012006822 A MX 2012006822A MX 2012006822 A MX2012006822 A MX 2012006822A MX 349550 B MX349550 B MX 349550B
- Authority
- MX
- Mexico
- Prior art keywords
- cancer
- compounds
- useful
- treatment
- methods
- Prior art date
Links
- HZIDRGNLSOMQRH-UHFFFAOYSA-N 5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene Chemical class N1=CC=C2C3=CC=CN=C3NC2=C1 HZIDRGNLSOMQRH-UHFFFAOYSA-N 0.000 title abstract 2
- 206010028980 Neoplasm Diseases 0.000 title abstract 2
- 201000011510 cancer Diseases 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 101150050673 CHK1 gene Proteins 0.000 abstract 1
- 102000006459 Checkpoint Kinase 1 Human genes 0.000 abstract 1
- 108010019244 Checkpoint Kinase 1 Proteins 0.000 abstract 1
- 239000012830 cancer therapeutic Substances 0.000 abstract 1
- 238000003745 diagnosis Methods 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000003463 hyperproliferative effect Effects 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 238000011065 in-situ storage Methods 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 229940043355 kinase inhibitor Drugs 0.000 abstract 1
- 210000004962 mammalian cell Anatomy 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—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
- A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Enzymes And Modification Thereof (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La invención se refiere a compuestos 1,7-diazacarbazol de la Fórmula ((I), (I-a) y ((I-b) que son útiles como inhibidores de cinasa, más específicamente útiles como inhibidores de cinasa reguladora de ciclo celular 1 (chk1 = checkpoint kinase 1), de esta manera útiles como agentes terapéuticos de cáncer. La invención también se refiere a composiciones, más específicamente a composiciones farmacéuticas que comprenden estos compuestos y métodos de uso de los mismos para tratar diversas formas de cáncer y desórdenes hiperproliferativos, así como métodos para utilizar los compuestos para diagnóstico o tratamiento in vitro, in situ, e in vivo de células de mamífero, o condiciones patológicas asociadas.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US28441409P | 2009-12-16 | 2009-12-16 | |
US28770209P | 2009-12-17 | 2009-12-17 | |
PCT/EP2010/069771 WO2011073263A1 (en) | 2009-12-16 | 2010-12-15 | 1, 7 - diazacarbazoles and their use in the treatment of cancer |
Publications (2)
Publication Number | Publication Date |
---|---|
MX2012006822A MX2012006822A (es) | 2012-08-17 |
MX349550B true MX349550B (es) | 2017-08-02 |
Family
ID=43535586
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2012006822A MX349550B (es) | 2009-12-16 | 2010-12-15 | 1,7-diazacarbazoles y metodos de uso. |
Country Status (9)
Country | Link |
---|---|
US (3) | US20110183938A1 (es) |
EP (1) | EP2513110B1 (es) |
JP (1) | JP5814931B2 (es) |
KR (1) | KR101496273B1 (es) |
CN (1) | CN102791711A (es) |
BR (1) | BR112012014652A2 (es) |
CA (1) | CA2782213C (es) |
MX (1) | MX349550B (es) |
WO (1) | WO2011073263A1 (es) |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20110183938A1 (en) | 2009-12-16 | 2011-07-28 | Genentech, Inc. | 1,7-diazacarbazoles and methods of use |
JOP20130273B1 (ar) * | 2012-09-11 | 2021-08-17 | Genzyme Corp | مثبطات انزيم (سينثاز) غلوكوسيل سيراميد |
WO2015013579A1 (en) | 2013-07-26 | 2015-01-29 | Update Pharma Inc. | Compositions to improve the therapeutic benefit of bisantrene |
AR097931A1 (es) * | 2013-10-08 | 2016-04-20 | Hoffmann La Roche | Derivados de diazacarbazol como ligandos de tau para pet |
CN103755628B (zh) * | 2014-01-27 | 2015-07-29 | 河北科技大学 | 2-氨基-3-碘-5-溴吡啶的合成方法 |
WO2015115339A1 (ja) * | 2014-01-30 | 2015-08-06 | 住友化学株式会社 | ピリジン化合物の製造方法 |
CN104744353B (zh) * | 2015-03-31 | 2017-11-24 | 山东友帮生化科技有限公司 | 2‑氨基‑3‑碘‑5‑氯吡啶的合成方法 |
CA3035624A1 (en) | 2016-09-09 | 2018-03-15 | F. Hoffmann-La Roche Ag | Process for preparation of 2-(6-nitropyridin-3-yl)-9h-dipyrido[2,3-b;3',4'-d]pyrrole |
WO2020072675A1 (en) | 2018-10-02 | 2020-04-09 | Northwestern University | Beta-carbolines as positive allosteric modulators of the human serotonin receptor 2c (5-ht2c) |
EP4185267A1 (en) | 2020-07-24 | 2023-05-31 | Genzyme Corporation | Pharmaceutical compositions comprising venglustat |
Family Cites Families (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
NZ521386A (en) * | 2000-03-15 | 2004-06-25 | Aventis Pharma Gmbh | Substituted beta-carbolines with lkB-kinase inhibiting activity |
WO2001068648A1 (en) | 2000-03-15 | 2001-09-20 | Aventis Pharma Deutschland Gmbh | Substituted beta-carbolines with ikb-kinase inhibiting activity |
GB0121941D0 (en) | 2001-09-11 | 2001-10-31 | Astrazeneca Ab | Chemical compounds |
JP4599501B2 (ja) | 2001-11-07 | 2010-12-15 | 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 | 多発性骨髄腫および他の癌の処置におけるIκBのインヒビターとしてのカルボリン誘導体 |
MXPA05008688A (es) * | 2003-02-17 | 2005-10-05 | Pharmacia Italia Spa | Derivados tetraciclicos de pirazol como inhibidores de la cinasa, procedimiento para su preparacion y composiciones farmaceuticas que los comprenden. |
PE20060526A1 (es) * | 2004-06-15 | 2006-07-13 | Schering Corp | Compuestos triciclicos como antagonistas de mglur1 |
SE0401655D0 (sv) | 2004-06-24 | 2004-06-24 | Astrazeneca Ab | New compounds |
US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
AU2007313961A1 (en) | 2006-10-09 | 2008-05-08 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
WO2008045834A2 (en) | 2006-10-09 | 2008-04-17 | Takeda San Diego, Inc. | Kinase inhibitors |
DE102006062203A1 (de) * | 2006-12-22 | 2008-06-26 | Curacyte Discovery Gmbh | Substituierte 5H-Pyrimido[5,4-b]indole als Induktoren der Apoptose bei B-CLL Zellen |
EP2132177B1 (en) | 2007-03-01 | 2013-07-17 | Novartis AG | Pim kinase inhibitors and methods of their use |
WO2009004329A1 (en) * | 2007-07-02 | 2009-01-08 | Cancer Research Technology Limited | 9h-pyrimido[4,5-b]indoles, 9h-pyrido[4',3':4,5]pyrrolo[2,3-d]pyridines, and 9h-1,3,6,9-tetraaza-fluorenes as chk1 kinase function inhibitors |
JP2009151598A (ja) * | 2007-12-21 | 2009-07-09 | Duaxes Corp | 試験装置 |
US20090312288A1 (en) | 2008-04-16 | 2009-12-17 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
WO2009151598A1 (en) * | 2008-06-11 | 2009-12-17 | Genentech, Inc. | Diazacarbazoles and methods of use |
AR072084A1 (es) * | 2008-06-12 | 2010-08-04 | Sanofi Aventis | Derivados de azacarbolinas, su preparacion y su utilizacion terapeutica como inhibidores de las quinasas pim |
WO2010015589A1 (en) | 2008-08-05 | 2010-02-11 | Nycomed Gmbh | Benzyl-substituted tetracyclic heterocyclic compounds as pde5 inhibitors |
KR20110130504A (ko) * | 2009-03-24 | 2011-12-05 | 사노피 | 9h-피롤로〔2,3-b:5,4-c'〕디피리딘 아자카르볼린 유도체, 그의 제조법, 및 그의 치료 용도 |
US20110183938A1 (en) | 2009-12-16 | 2011-07-28 | Genentech, Inc. | 1,7-diazacarbazoles and methods of use |
-
2010
- 2010-12-14 US US12/967,864 patent/US20110183938A1/en not_active Abandoned
- 2010-12-15 KR KR1020127018196A patent/KR101496273B1/ko active IP Right Grant
- 2010-12-15 CN CN2010800639941A patent/CN102791711A/zh active Pending
- 2010-12-15 WO PCT/EP2010/069771 patent/WO2011073263A1/en active Application Filing
- 2010-12-15 BR BR112012014652-1A patent/BR112012014652A2/pt not_active Application Discontinuation
- 2010-12-15 JP JP2012543723A patent/JP5814931B2/ja active Active
- 2010-12-15 CA CA2782213A patent/CA2782213C/en active Active
- 2010-12-15 MX MX2012006822A patent/MX349550B/es active IP Right Grant
- 2010-12-15 EP EP10795311.9A patent/EP2513110B1/en active Active
-
2014
- 2014-02-17 US US14/182,190 patent/US20140171407A1/en not_active Abandoned
-
2015
- 2015-06-18 US US14/743,835 patent/US9440976B2/en active Active
Also Published As
Publication number | Publication date |
---|---|
MX2012006822A (es) | 2012-08-17 |
CA2782213A1 (en) | 2011-06-23 |
CN102791711A (zh) | 2012-11-21 |
US9440976B2 (en) | 2016-09-13 |
BR112012014652A2 (pt) | 2020-09-15 |
EP2513110B1 (en) | 2018-12-05 |
US20140171407A1 (en) | 2014-06-19 |
KR101496273B1 (ko) | 2015-02-26 |
US20150328195A1 (en) | 2015-11-19 |
KR20120103705A (ko) | 2012-09-19 |
CA2782213C (en) | 2014-10-28 |
US20110183938A1 (en) | 2011-07-28 |
JP5814931B2 (ja) | 2015-11-17 |
EP2513110A1 (en) | 2012-10-24 |
RU2012127877A (ru) | 2014-01-27 |
JP2013514315A (ja) | 2013-04-25 |
WO2011073263A1 (en) | 2011-06-23 |
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