CR20150489A - Derivados de 1-acil-4-amino-1,2,3,4-tetrahidroquinolina 2,3 - disustituidos y su uso como inhibidores del bromodominio - Google Patents
Derivados de 1-acil-4-amino-1,2,3,4-tetrahidroquinolina 2,3 - disustituidos y su uso como inhibidores del bromodominioInfo
- Publication number
- CR20150489A CR20150489A CR20150489A CR20150489A CR20150489A CR 20150489 A CR20150489 A CR 20150489A CR 20150489 A CR20150489 A CR 20150489A CR 20150489 A CR20150489 A CR 20150489A CR 20150489 A CR20150489 A CR 20150489A
- Authority
- CR
- Costa Rica
- Prior art keywords
- bromodominum
- acil
- tetrahydroquinoline
- inhibitors
- derivatives
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
Classifications
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed 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
- A61K31/435—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
- A61K31/4706—4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
-
- 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
- A61K31/495—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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines 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
- A61K31/535—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
- A61K31/535—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
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
- C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
-
- 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
- C07D215/38—Nitrogen atoms
- C07D215/42—Nitrogen atoms attached in position 4
- C07D215/44—Nitrogen atoms attached in position 4 with aryl radicals attached to said nitrogen atoms
-
- 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
- C07D215/38—Nitrogen atoms
- C07D215/42—Nitrogen atoms attached in position 4
- C07D215/46—Nitrogen atoms attached in position 4 with hydrocarbon radicals, substituted by nitrogen atoms, attached to said nitrogen atoms
-
- 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
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- 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
-
- 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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
- C07D471/02—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 two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- C07D471/02—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 two hetero rings
- C07D471/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Virology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Immunology (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)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Quinoline Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
La presente invención se refiere a compuestos novedosos defórmula (I), en donde R1 es alquilo de C1 - 4 ; R2 es alquilo de C1 - 4 , cicloalquilo de C3 - 7 , -CH2CF3 , -CH2OCH3 o heterociclilo; 5 R3 es alquilo de C1 - 4 , -CH2F, -CH2OH o -CH2O(O)CH3 ; R4 , cuando está presente, es como se define en la reivindicación 1; R5 , cuando está presente, es H,
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361781583P | 2013-03-14 | 2013-03-14 | |
US201361882798P | 2013-09-26 | 2013-09-26 | |
PCT/EP2014/054795 WO2014140076A1 (en) | 2013-03-14 | 2014-03-12 | 2,3-disubstituted 1 -acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
CR20150489A true CR20150489A (es) | 2015-11-20 |
Family
ID=50390051
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CR20150489A CR20150489A (es) | 2013-03-14 | 2015-09-14 | Derivados de 1-acil-4-amino-1,2,3,4-tetrahidroquinolina 2,3 - disustituidos y su uso como inhibidores del bromodominio |
Country Status (32)
Country | Link |
---|---|
US (5) | US9637456B2 (es) |
EP (2) | EP2970127B1 (es) |
JP (2) | JP6093046B2 (es) |
KR (1) | KR101780784B1 (es) |
CN (1) | CN105189461B (es) |
AU (1) | AU2014230815B2 (es) |
CA (1) | CA2901537C (es) |
CL (1) | CL2015002658A1 (es) |
CR (1) | CR20150489A (es) |
CY (1) | CY1121095T1 (es) |
DK (1) | DK2970127T3 (es) |
DO (1) | DOP2015000239A (es) |
EA (1) | EA028174B1 (es) |
ES (2) | ES2704048T3 (es) |
HK (1) | HK1219954A1 (es) |
HR (1) | HRP20182179T1 (es) |
HU (1) | HUE043568T2 (es) |
IL (2) | IL240463B (es) |
LT (1) | LT2970127T (es) |
MX (1) | MX369324B (es) |
MY (1) | MY187479A (es) |
NZ (1) | NZ710765A (es) |
PE (1) | PE20151596A1 (es) |
PH (1) | PH12015502038B1 (es) |
PL (1) | PL2970127T3 (es) |
PT (1) | PT2970127T (es) |
RS (1) | RS58264B1 (es) |
SG (1) | SG11201506245QA (es) |
SI (1) | SI2970127T1 (es) |
UA (1) | UA118549C2 (es) |
WO (1) | WO2014140076A1 (es) |
ZA (1) | ZA201505877B (es) |
Families Citing this family (49)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US9765039B2 (en) | 2012-11-21 | 2017-09-19 | Zenith Epigenetics Ltd. | Biaryl derivatives as bromodomain inhibitors |
WO2014080290A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Cyclic amines as bromodomain inhibitors |
MX2015007921A (es) | 2012-12-21 | 2016-03-03 | Zenith Epigenetics Corp | Compuestos heterociclicos novedosos como inhibidores de bromodominio. |
WO2014152537A1 (en) | 2013-03-14 | 2014-09-25 | Janssen Pharmaceutica Nv | P2x7 modulators |
JO3773B1 (ar) | 2013-03-14 | 2021-01-31 | Janssen Pharmaceutica Nv | معدلات p2x7 |
AU2014230815B2 (en) | 2013-03-14 | 2016-12-08 | Glaxosmithkline Intellectual Property (No.2) Limited | 2,3-disubstituted 1 -acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors |
US9604982B2 (en) | 2013-03-14 | 2017-03-28 | Janssen Pharmaceutica Nv | P2X7 modulators |
JO3509B1 (ar) | 2013-03-14 | 2020-07-05 | Janssen Pharmaceutica Nv | معدلات p2x7 |
ES2755827T3 (es) | 2013-03-15 | 2020-04-23 | Incyte Holdings Corp | Heterciclos tricíclicos como inhibidores de proteína BET |
CN105492439B (zh) | 2013-06-21 | 2019-11-22 | 齐尼思表观遗传学有限公司 | 作为溴结构域抑制剂的取代的双环化合物 |
KR102307566B1 (ko) | 2013-06-21 | 2021-10-05 | 제니쓰 에피제네틱스 리미티드 | 신규한 바이사이클릭 브로모도메인 억제제 |
JP2016523964A (ja) | 2013-07-08 | 2016-08-12 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Betタンパク質阻害剤としての三環式複素環 |
WO2015015318A2 (en) | 2013-07-31 | 2015-02-05 | Zenith Epigenetics Corp. | Novel quinazolinones as bromodomain inhibitors |
WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
WO2015095492A1 (en) | 2013-12-19 | 2015-06-25 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
UA119870C2 (uk) | 2014-04-23 | 2019-08-27 | Інсайт Корпорейшн | 1H-ПІРОЛО[2,3-c]ПІРИДИН-7(6H)-ОНИ ТА ПІРАЗОЛО[3,4-c]ПІРИДИН-7(6H)-ОНИ ЯК ІНГІБІТОРИ БІЛКІВ BET |
JP6592510B2 (ja) | 2014-09-12 | 2019-10-16 | ヤンセン ファーマシューティカ エヌ.ベー. | P2x7調節因子 |
ES2705623T3 (es) * | 2014-09-12 | 2019-03-26 | Glaxosmithkline Ip No 2 Ltd | Derivados de tetrahidroquinolina como inhibidores del bromodominio |
US9527864B2 (en) | 2014-09-15 | 2016-12-27 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
US10710992B2 (en) | 2014-12-01 | 2020-07-14 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
WO2016087942A1 (en) | 2014-12-01 | 2016-06-09 | Zenith Epigenetics Corp. | Substituted pyridines as bromodomain inhibitors |
CN107207474B (zh) | 2014-12-11 | 2021-05-07 | 恒翼生物医药科技(上海)有限公司 | 被取代的杂环作为溴结构域抑制剂 |
US10231953B2 (en) | 2014-12-17 | 2019-03-19 | Zenith Epigenetics Ltd. | Inhibitors of bromodomains |
GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
TW201711999A (zh) | 2015-09-03 | 2017-04-01 | 佛瑪治療公司 | ﹝6,6﹞稠合雙環組蛋白脫乙醯基酶8(hdac8)抑制劑 |
RU2018112312A (ru) | 2015-09-22 | 2019-10-23 | ГлаксоСмитКлайн Интеллекчуал Проперти (N2) Лимитед | Пиридинондикарбоксамиды для применения в качестве ингибиторов бромодомена |
AR106520A1 (es) | 2015-10-29 | 2018-01-24 | Incyte Corp | Forma sólida amorfa de un inhibidor de proteína bet |
WO2017093272A1 (en) * | 2015-12-03 | 2017-06-08 | Bayer Pharma Aktiengesellschaft | Furane derivatives as inhibitors of atad2 |
JP7160688B2 (ja) * | 2016-05-24 | 2022-10-25 | ジェネンテック, インコーポレイテッド | Cbp/ep300の複素環式インヒビターおよびがんの処置におけるそれらの使用 |
CN114366748A (zh) | 2016-06-20 | 2022-04-19 | 因赛特公司 | Bet抑制剂的结晶固体形式 |
WO2018075908A1 (en) * | 2016-10-21 | 2018-04-26 | University Of Miami | Materials and methods for treating ophthalmic inflammation |
CN109983019B (zh) * | 2017-08-08 | 2021-12-21 | 江苏恒瑞医药股份有限公司 | 一种咪唑并异吲哚类衍生物的制备方法 |
CN110041253B (zh) * | 2018-01-17 | 2022-03-29 | 上海翰森生物医药科技有限公司 | 吡啶类n-氧化衍生物及其制备方法和应用 |
MX2020009967A (es) * | 2018-03-30 | 2021-01-08 | Kyowa Kirin Co Ltd | Compuesto con actividad anticancerigena. |
JOP20210058A1 (ar) | 2018-09-28 | 2021-03-24 | Janssen Pharmaceutica Nv | مُعدلات ليباز أُحادِيُّ الجلِيسِريد |
CA3111309A1 (en) | 2018-09-28 | 2020-04-02 | Janssen Pharmaceutica Nv | Monoacylglycerol lipase modulators |
CN113226322A (zh) | 2018-10-30 | 2021-08-06 | 诺维逊生物股份有限公司 | 作为bet抑制剂的杂环化合物 |
CN109836385B (zh) * | 2019-04-04 | 2021-12-17 | 上海翰森生物医药科技有限公司 | 四氢喹啉类n-氧化衍生物及其制备方法和应用 |
EP3997070A4 (en) | 2019-07-02 | 2023-07-26 | Nuvation Bio Inc. | HETEROCYCLIC COMPOUNDS USED AS BET INHIBITORS |
AU2020360170A1 (en) | 2019-09-30 | 2022-05-19 | Kyowa Kirin Co., Ltd. | Bet degrader |
EP4038070A1 (en) | 2019-09-30 | 2022-08-10 | Janssen Pharmaceutica NV | Radiolabelled mgl pet ligands |
CA3176946A1 (en) | 2020-03-26 | 2021-09-30 | Janssen Pharmaceutica Nv | Monoacylglycerol lipase modulators |
TWI783480B (zh) * | 2020-05-27 | 2022-11-11 | 美商美國禮來大藥廠 | 用於抑制cdk7之化合物 |
US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
EP4095128A1 (en) | 2021-05-25 | 2022-11-30 | Centre national de la recherche scientifique | Tetrahydroquinoline (thq) coumpounds |
WO2023274418A1 (zh) * | 2021-07-02 | 2023-01-05 | 南京明德新药研发有限公司 | 蛋白降解靶向嵌合体类化合物 |
WO2023196512A1 (en) * | 2022-04-08 | 2023-10-12 | Plexium, Inc. | Propargyl compounds and pharmaceutical compositions that modulate brd4 |
WO2024073072A1 (en) | 2022-09-30 | 2024-04-04 | Bp Asset Iii, Inc. | Topical pharmaceutical formulations for bd2-preferential bromodomain and extra terminal inhibitor |
Family Cites Families (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB9004781D0 (en) | 1990-03-02 | 1990-04-25 | Glaxo Group Ltd | Device |
SE0101161D0 (sv) | 2001-03-30 | 2001-03-30 | Astrazeneca Ab | New compounds |
US20050228016A1 (en) | 2002-06-13 | 2005-10-13 | Enrique Michelotti | Tetrahydroquinolines for modulating the expression of exogenous genes via an ecdysone receptor complex |
AU2003277285B2 (en) * | 2002-10-04 | 2007-12-13 | Millennium Pharmaceuticals, Inc. | PGD2 receptor antagonists for the treatment of inflammatory diseases |
JPWO2004052863A1 (ja) | 2002-12-06 | 2006-04-13 | 協和醗酵工業株式会社 | 抗炎症剤 |
WO2004072042A2 (en) | 2003-02-12 | 2004-08-26 | Carex S.A. | Quinoline derivative and their use for modulation of lxr activity |
WO2005007094A2 (en) | 2003-07-09 | 2005-01-27 | Tularik Inc. | Asthma and allergic inflammation modulators |
CN102028994B (zh) | 2003-11-03 | 2013-04-24 | 葛兰素集团有限公司 | 流体分配装置 |
US8604030B2 (en) * | 2009-03-27 | 2013-12-10 | Kowa Company, Ltd. | Fused piperidine compound and pharmaceutical containing same |
WO2010113498A1 (ja) * | 2009-03-31 | 2010-10-07 | 興和株式会社 | テトラヒドロキノリン化合物を有効成分とする貧血の予防及び/又は治療剤 |
GB0919431D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
GB0919434D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
GB201106743D0 (en) | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
GB201106750D0 (en) | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
GB201107325D0 (en) | 2011-05-04 | 2011-06-15 | Glaxosmithkline Llc | Novel compounds |
WO2013027168A1 (en) | 2011-08-22 | 2013-02-28 | Pfizer Inc. | Novel heterocyclic compounds as bromodomain inhibitors |
AU2014230815B2 (en) * | 2013-03-14 | 2016-12-08 | Glaxosmithkline Intellectual Property (No.2) Limited | 2,3-disubstituted 1 -acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors |
-
2014
- 2014-03-12 AU AU2014230815A patent/AU2014230815B2/en active Active
- 2014-03-12 PT PT14713394T patent/PT2970127T/pt unknown
- 2014-03-12 EA EA201591429A patent/EA028174B1/ru not_active IP Right Cessation
- 2014-03-12 RS RS20181568A patent/RS58264B1/sr unknown
- 2014-03-12 EP EP14713394.6A patent/EP2970127B1/en active Active
- 2014-03-12 PE PE2015002004A patent/PE20151596A1/es active IP Right Grant
- 2014-03-12 ES ES14713394T patent/ES2704048T3/es active Active
- 2014-03-12 ES ES18201850T patent/ES2915658T3/es active Active
- 2014-03-12 SG SG11201506245QA patent/SG11201506245QA/en unknown
- 2014-03-12 UA UAA201507943A patent/UA118549C2/uk unknown
- 2014-03-12 SI SI201431018T patent/SI2970127T1/sl unknown
- 2014-03-12 KR KR1020157029457A patent/KR101780784B1/ko active IP Right Grant
- 2014-03-12 EP EP18201850.7A patent/EP3511323B1/en active Active
- 2014-03-12 HU HUE14713394A patent/HUE043568T2/hu unknown
- 2014-03-12 MX MX2015012815A patent/MX369324B/es active IP Right Grant
- 2014-03-12 MY MYPI2015703150A patent/MY187479A/en unknown
- 2014-03-12 WO PCT/EP2014/054795 patent/WO2014140076A1/en active Application Filing
- 2014-03-12 CA CA2901537A patent/CA2901537C/en active Active
- 2014-03-12 LT LTEP14713394.6T patent/LT2970127T/lt unknown
- 2014-03-12 DK DK14713394.6T patent/DK2970127T3/en active
- 2014-03-12 CN CN201480026886.5A patent/CN105189461B/zh active Active
- 2014-03-12 US US14/770,499 patent/US9637456B2/en active Active
- 2014-03-12 NZ NZ710765A patent/NZ710765A/en unknown
- 2014-03-12 PL PL14713394T patent/PL2970127T3/pl unknown
- 2014-03-12 JP JP2015562110A patent/JP6093046B2/ja active Active
-
2015
- 2015-08-10 IL IL240463A patent/IL240463B/en active IP Right Grant
- 2015-08-14 ZA ZA2015/05877A patent/ZA201505877B/en unknown
- 2015-09-10 PH PH12015502038A patent/PH12015502038B1/en unknown
- 2015-09-14 CR CR20150489A patent/CR20150489A/es unknown
- 2015-09-14 CL CL2015002658A patent/CL2015002658A1/es unknown
- 2015-09-14 DO DO2015000239A patent/DOP2015000239A/es unknown
-
2016
- 2016-07-11 HK HK16108056.6A patent/HK1219954A1/zh unknown
-
2017
- 2017-02-09 JP JP2017021745A patent/JP6530773B2/ja active Active
- 2017-03-23 US US15/466,925 patent/US10034881B2/en active Active
-
2018
- 2018-06-25 US US16/016,955 patent/US10583139B2/en active Active
- 2018-11-28 IL IL263354A patent/IL263354B/en unknown
- 2018-12-27 HR HRP20182179TT patent/HRP20182179T1/hr unknown
-
2019
- 2019-01-04 CY CY191100010T patent/CY1121095T1/el unknown
-
2020
- 2020-01-07 US US16/735,956 patent/US11478478B2/en active Active
-
2022
- 2022-08-25 US US17/895,273 patent/US20230040299A1/en active Pending
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
CR20150489A (es) | Derivados de 1-acil-4-amino-1,2,3,4-tetrahidroquinolina 2,3 - disustituidos y su uso como inhibidores del bromodominio | |
CY1119105T1 (el) | Παραγωγα διπυραζολιου ως αναστολεις jak | |
CR20150447A (es) | Nuevos derivados de pirazol | |
CR20140519A (es) | Derivados de benzamida para la inhibición de la actividad de abl 1, abl 2 y bcr-abl 1 | |
CR20200276A (es) | Sulfamoilarilamidas y su uso como medicamentos para el tratamientos de la hepatitis b (divisional exp. 2015-0059) | |
CR20150470A (es) | Derivados de triazolona de piridinilo y piridinilo fusionado | |
CR20130369A (es) | Novedosos derivados heterocíclicos | |
CR20140464A (es) | Compuestos de heterociclilo | |
UY34825A (es) | Síntesis de compuestos heterocíclicos | |
PH12017500048A1 (en) | Pyridone derivative having tetrahydropyranylmethyl group | |
CR20130233A (es) | Derivados que quinazolin-4 (3h)-ona utilizados como inhibidores de pi3 cinaza | |
CR20150061A (es) | Compuesto de pirazolopirimidinas | |
CR20150204A (es) | Nuevos derivados de piridina | |
PH12015501933A1 (en) | Novel pyridine derivatives | |
BR112015029348A2 (pt) | inibidores da bace | |
CR20140322A (es) | Nuevos derivados de bencil sulfonamida útiles como inhibidores de mogat-2 | |
CR20140528A (es) | Difluoro-hexahidro-ciclopentaoxacinilos y difluoro-hexahidro-benzooxacinilos como inhibidores de Bace1 | |
CR20150555A (es) | Nuevos derivados de pirrolo[2,3-d]pirimidina | |
CR20160082A (es) | Nuevo derivado de triazina | |
CY1121116T1 (el) | Νεα μεθοδος για την συνθεση αγομελατινης | |
CR20150087A (es) | Derivados de pirazol-carboxamida | |
CO6852081A2 (es) | Antagonistas de trpv1 que incluyen sustituyentes dihidroxi y sus usos | |
MX2015006930A (es) | Compuestos de isoxazol amina sustituidos como inhibidores de scd1. | |
UY34869A (es) | Derivados de pirimidinonas, su preparación y su aplicación en terapéutica. | |
PH12015502462A1 (en) | Imidazo-triazine derivatives as pde10 inhibitors |