PE20181020A1 - MUCLEAR RECEIVER MODULATORS - Google Patents
MUCLEAR RECEIVER MODULATORSInfo
- Publication number
- PE20181020A1 PE20181020A1 PE2017002535A PE2017002535A PE20181020A1 PE 20181020 A1 PE20181020 A1 PE 20181020A1 PE 2017002535 A PE2017002535 A PE 2017002535A PE 2017002535 A PE2017002535 A PE 2017002535A PE 20181020 A1 PE20181020 A1 PE 20181020A1
- Authority
- PE
- Peru
- Prior art keywords
- cra
- muclear
- nra
- present
- halo
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
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- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D235/16—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic 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
- C07D405/10—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 linked by a carbon chain containing aromatic 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
- C07D405/14—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
- 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
- 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
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presenten invencion refiere un compuesto de formula (I) en donde W es C o CRa; A y E son independientemente C o N con la condicion de que no sean ambos N; V es CR3 o N; X es CRa, NRa, N u O; Y es C, CRa, NRa,N, O o S; Z es CR3 o N; Cy es un anillo aromatico de 6 miembros, heteroaromatico o parcialmente sustituido con R1 o R2; L1 es -CH(Rb)-, -C(O)-, entre otros; L2 es -C(O)-, -O-, entre otros; R1 y R2 son independientemente halo, cicloalquilo (C3-C6), entre otros; R3 es H, CF3, CN, halo, entre otros; R4 es H, -OH, entre otros; Ra es H, -C(O)CH3, alquilo (C1-C6), entre otros: Rb es H,F,OH, entre otros. Es compuesto preferido: acido 1-(2,4-dicloro-3-((1,4-dimetil-6-(trifluorometil)-1H-indol-2-il)metil)benzoil)piperidin-4-carboxilico; entre otros. La presente invencion es util para el tratamiento de enfermedades inflamatorias y autoinmunes, como es el caso de artritis reumatoide, colitis ulcerosa, entre otras referidas en la invencionThe present invention relates to a compound of formula (I) wherein W is C or CRa; A and E are independently C or N provided they are not both N; V is CR3 or N; X is CRa, NRa, N or O; Y is C, CRa, NRa, N, O, or S; Z is CR3 or N; Cy is a 6-membered aromatic ring, heteroaromatic or partially substituted with R1 or R2; L1 is -CH (Rb) -, -C (O) -, among others; L2 is -C (O) -, -O-, among others; R1 and R2 are independently halo, (C3-C6) cycloalkyl, among others; R3 is H, CF3, CN, halo, among others; R4 is H, -OH, among others; Ra is H, -C (O) CH3, (C1-C6) alkyl, among others: Rb is H, F, OH, among others. The preferred compound is: 1- (2,4-dichloro-3 - ((1,4-dimethyl-6- (trifluoromethyl) -1H-indol-2-yl) methyl) benzoyl) piperidine-4-carboxylic acid; among others. The present invention is useful for the treatment of inflammatory and autoimmune diseases, such as rheumatoid arthritis, ulcerative colitis, among others referred to in the invention.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/IB2015/001693 WO2016198908A1 (en) | 2015-06-09 | 2015-06-09 | Ror nuclear receptor modulators |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20181020A1 true PE20181020A1 (en) | 2018-06-27 |
Family
ID=54293273
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2017002535A PE20181020A1 (en) | 2015-06-09 | 2016-06-08 | MUCLEAR RECEIVER MODULATORS |
Country Status (3)
Country | Link |
---|---|
AR (1) | AR104934A1 (en) |
PE (1) | PE20181020A1 (en) |
WO (1) | WO2016198908A1 (en) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN108689942B (en) * | 2017-04-11 | 2023-06-09 | 广东东阳光药业有限公司 | Nitrogen-containing bicyclic compound, and preparation method and application thereof |
US11427596B2 (en) * | 2019-07-19 | 2022-08-30 | Indian Institute of Technology Indore | Metal-free solvent-free synthesis of fused-pyrido heterocycles and biomedical applications |
US11834441B2 (en) | 2019-12-06 | 2023-12-05 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofurans as modulators of sodium channels |
BR112022020131A2 (en) | 2020-04-06 | 2022-11-29 | Basf Se | COMPOUND OF THE FORMULA, MIXTURE OF PESTICIDES, USE OF COMPOUNDS OF THE FORMULA, METHODS FOR COMBAT OR CONTROL OF INVERTEBRATE PEST AND PROTECTION OF GROWING PLANTS AND SEEDS |
EP4347031A1 (en) | 2021-06-04 | 2024-04-10 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamides as modulators of sodium channels |
CN116283753A (en) * | 2023-03-20 | 2023-06-23 | 武汉朗克环境科技有限公司 | Trifluoromethyl pyridine amide derivative and preparation method and application thereof |
Family Cites Families (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20070129334A1 (en) | 2001-10-30 | 2007-06-07 | Conforma Therapeutics Corporation | Orally Active Purine-Based Inhibitors of Heat Shock Protein 90 |
WO2003060078A2 (en) | 2001-12-21 | 2003-07-24 | X-Ceptor Therapeutics, Inc. | Heterocyclic modulators of nuclear receptors |
BR0317525A (en) | 2002-12-20 | 2005-11-16 | Pharmacia Corp | Acyclic pyrazole compounds, therapeutic and pharmaceutical composition, kit, as well as their uses |
US7312215B2 (en) | 2003-07-29 | 2007-12-25 | Bristol-Myers Squibb Company | Benzimidazole C-2 heterocycles as kinase inhibitors |
UY28526A1 (en) | 2003-09-24 | 2005-04-29 | Boehringer Ingelheim Pharma | GLUCOCORTICOID MIMETICS, METHODS OF PREPARATION PHARMACEUTICAL COMPOSITIONS AND USES OF THE SAME |
JP2008504266A (en) | 2004-06-24 | 2008-02-14 | イーライ リリー アンド カンパニー | Compounds and methods for treating dyslipidemia |
WO2006050076A1 (en) | 2004-10-29 | 2006-05-11 | Janssen Pharmaceutica, N.V. | Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders |
PL1807072T3 (en) | 2004-10-29 | 2009-06-30 | Lilly Co Eli | Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 |
US8026257B2 (en) | 2007-07-11 | 2011-09-27 | Bristol-Myers Squibb Company | Substituted heterocyclic ethers and their use in CNS disorders |
BRPI1007923A2 (en) | 2009-02-06 | 2020-08-25 | Elan Pharmaceuticals, Inc | compound, pharmaceutical composition, methods for treating a neurodegenerative disease, and for reducing the concentration of p-cjun in brain tissue of an individual in need thereof, use of a compound, and, in vitro method |
AU2010295481A1 (en) | 2009-09-18 | 2012-03-08 | Zalicus Pharmaceuticals Ltd. | Aryl sulphone derivatives as calcium channel blockers |
US8466186B2 (en) * | 2010-12-10 | 2013-06-18 | Boehringer Ingelheim International Gmbh | Compounds |
EP2487159A1 (en) * | 2011-02-11 | 2012-08-15 | MSD Oss B.V. | RorgammaT inhibitors |
KR20140082643A (en) | 2011-07-25 | 2014-07-02 | 알러간, 인코포레이티드 | N-(IMIDAZOLIDIN-2-YLIDENE)-HETEROCYCLOPENTA[b]PYRIDINE DERIVATIVES AS MODULATORS OF ALPHA 2 ADRENERGIC RECEPTORS |
WO2013038381A1 (en) | 2011-09-16 | 2013-03-21 | Novartis Ag | Pyridine/pyrazine amide derivatives |
US9957271B2 (en) | 2011-10-20 | 2018-05-01 | Glaxosmithkline Llc | Substituted bicyclic aza-heterocycles and analogues as sirtuin modulators |
EP2647628A1 (en) | 2012-04-02 | 2013-10-09 | Almirall, S.A. | Substituted tricyclic compounds with activity towards ep1 receptors |
WO2014026328A1 (en) * | 2012-08-15 | 2014-02-20 | Merck Sharp & Dohme Corp. | 3-cyclohexenyl substituted indole and indazole compounds as rorgammat inhibitors and uses thereof |
CN105531274A (en) * | 2013-09-11 | 2016-04-27 | 豪夫迈·罗氏有限公司 | Keto-imidazopyridine derivatives as rorc modulators |
-
2015
- 2015-06-09 WO PCT/IB2015/001693 patent/WO2016198908A1/en active Application Filing
-
2016
- 2016-06-08 PE PE2017002535A patent/PE20181020A1/en unknown
- 2016-06-08 AR ARP160101700A patent/AR104934A1/en unknown
Also Published As
Publication number | Publication date |
---|---|
AR104934A1 (en) | 2017-08-23 |
WO2016198908A1 (en) | 2016-12-15 |
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