BR112014015442A8 - compostos e composições para inibir a interação de bcl2 com parceiros de ligação - Google Patents
compostos e composições para inibir a interação de bcl2 com parceiros de ligaçãoInfo
- Publication number
- BR112014015442A8 BR112014015442A8 BR112014015442A BR112014015442A BR112014015442A8 BR 112014015442 A8 BR112014015442 A8 BR 112014015442A8 BR 112014015442 A BR112014015442 A BR 112014015442A BR 112014015442 A BR112014015442 A BR 112014015442A BR 112014015442 A8 BR112014015442 A8 BR 112014015442A8
- Authority
- BR
- Brazil
- Prior art keywords
- compounds
- bcl
- interaction
- compositions
- binding partners
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 13
- 102100021569 Apoptosis regulator Bcl-2 Human genes 0.000 title abstract 9
- 101000971171 Homo sapiens Apoptosis regulator Bcl-2 Proteins 0.000 title abstract 8
- 230000003993 interaction Effects 0.000 title abstract 7
- 230000002401 inhibitory effect Effects 0.000 title abstract 3
- 239000000203 mixture Substances 0.000 title abstract 3
- 206010028980 Neoplasm Diseases 0.000 abstract 4
- 238000000034 method Methods 0.000 abstract 4
- 230000002424 anti-apoptotic effect Effects 0.000 abstract 2
- 201000011510 cancer Diseases 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 2
- 238000002360 preparation method Methods 0.000 abstract 2
- 102000004169 proteins and genes Human genes 0.000 abstract 2
- 108090000623 proteins and genes Proteins 0.000 abstract 2
- 101150017888 Bcl2 gene Proteins 0.000 abstract 1
Classifications
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero 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
- A61K31/435—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
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
compounds and compositions for inhibiting the interaction of bcl2 with binding partners abstract the present invention relates to compounds of formula i: in which r1, r2, r3 and r4 are as defined in the summary of the invention. compounds of formula i are capable of disrupting the bcl-2 interations with proteins containing a bh3 domain. disrupting this interaction can restore the anti-apoptotic function of bcl-2 in cancer cells and tumor tissue expressing bcl-2. the invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases. tradução do resumo resumo "compostos e composições para inibir a interação de bcl2 com parceiros de ligação" a presente invenção refere-se a compostos de fórmula i: em que r1, r2, r3 e r4 são como definidos no sumário da invenção. os compostos de fórmula i são capazes de perturbar as interações bcl-2 com proteínas contendo um domínio bh3. perturbar esta interação pode restaurar a função antiapoptótica de bcl-2 em células cancerosas e tecido tumoral que expressa bcl-2. a invenção proporciona ainda um processo para a preparação de compostos da invenção, preparações farmacêuticas que compreendem estes compostos e métodos de utilização de tais compostos no tratamento de doenças cancerosas.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161579740P | 2011-12-23 | 2011-12-23 | |
PCT/US2012/069191 WO2013096051A1 (en) | 2011-12-23 | 2012-12-12 | Compounds for inhibiting the interaction of bcl2 with binding partners |
Publications (2)
Publication Number | Publication Date |
---|---|
BR112014015442A2 BR112014015442A2 (pt) | 2017-06-13 |
BR112014015442A8 true BR112014015442A8 (pt) | 2017-07-04 |
Family
ID=47429050
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112014015442A BR112014015442A8 (pt) | 2011-12-23 | 2012-12-12 | compostos e composições para inibir a interação de bcl2 com parceiros de ligação |
Country Status (11)
Country | Link |
---|---|
US (1) | US20140350014A1 (pt) |
EP (1) | EP2794589A1 (pt) |
JP (1) | JP2015503516A (pt) |
KR (1) | KR20140107578A (pt) |
CN (1) | CN104136428A (pt) |
AU (1) | AU2012355615A1 (pt) |
BR (1) | BR112014015442A8 (pt) |
CA (1) | CA2859873A1 (pt) |
EA (1) | EA201491259A1 (pt) |
MX (1) | MX2014007725A (pt) |
WO (1) | WO2013096051A1 (pt) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104125954A (zh) | 2011-12-23 | 2014-10-29 | 诺华股份有限公司 | 用于抑制bcl2与结合配偶体相互作用的化合物 |
US9126980B2 (en) | 2011-12-23 | 2015-09-08 | Novartis Ag | Compounds for inhibiting the interaction of BCL2 with binding partners |
FR3008978A1 (fr) * | 2013-07-23 | 2015-01-30 | Servier Lab | "nouveaux derives d'indole et de pyrrole, leur procede de preparation et les compositions pharmaceutiques qui les contiennent" |
FR3008979B1 (fr) | 2013-07-23 | 2015-07-24 | Servier Lab | Nouveaux derives phosphates, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
FR3008976A1 (fr) | 2013-07-23 | 2015-01-30 | Servier Lab | "nouveaux derives d'indolizine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent" |
US10195213B2 (en) | 2015-03-13 | 2019-02-05 | Unity Biotechnology, Inc. | Chemical entities that kill senescent cells for use in treating age-related disease |
US20190119236A1 (en) | 2016-02-23 | 2019-04-25 | Portola Pharmaceuticals, Inc. | Compounds for binding proprotein convertase subtilisin/kexin type 9 (pcsk9) |
BR112020022092A2 (pt) | 2018-04-29 | 2021-02-02 | Beigene, Ltd. | compostos, método para tratar doenças apoptóticas desreguladas e composição farmacêutica |
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-
2012
- 2012-12-12 BR BR112014015442A patent/BR112014015442A8/pt not_active Application Discontinuation
- 2012-12-12 EP EP12805894.8A patent/EP2794589A1/en not_active Withdrawn
- 2012-12-12 CN CN201280070470.4A patent/CN104136428A/zh active Pending
- 2012-12-12 WO PCT/US2012/069191 patent/WO2013096051A1/en active Application Filing
- 2012-12-12 MX MX2014007725A patent/MX2014007725A/es unknown
- 2012-12-12 JP JP2014549135A patent/JP2015503516A/ja active Pending
- 2012-12-12 EA EA201491259A patent/EA201491259A1/ru unknown
- 2012-12-12 CA CA2859873A patent/CA2859873A1/en not_active Abandoned
- 2012-12-12 KR KR1020147020534A patent/KR20140107578A/ko not_active Application Discontinuation
- 2012-12-12 AU AU2012355615A patent/AU2012355615A1/en not_active Abandoned
- 2012-12-12 US US14/366,860 patent/US20140350014A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
CN104136428A (zh) | 2014-11-05 |
CA2859873A1 (en) | 2013-06-27 |
JP2015503516A (ja) | 2015-02-02 |
EP2794589A1 (en) | 2014-10-29 |
WO2013096051A1 (en) | 2013-06-27 |
EA201491259A1 (ru) | 2014-11-28 |
KR20140107578A (ko) | 2014-09-04 |
BR112014015442A2 (pt) | 2017-06-13 |
AU2012355615A1 (en) | 2014-07-10 |
MX2014007725A (es) | 2015-01-12 |
US20140350014A1 (en) | 2014-11-27 |
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Legal Events
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B11A | Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing | ||
B11Y | Definitive dismissal acc. article 33 of ipl - extension of time limit for request of examination expired | ||
B350 | Update of information on the portal [chapter 15.35 patent gazette] |