AR109042A1 - COMPUESTOS MODULARES DE RORg - Google Patents
COMPUESTOS MODULARES DE RORgInfo
- Publication number
- AR109042A1 AR109042A1 ARP170101950A ARP170101950A AR109042A1 AR 109042 A1 AR109042 A1 AR 109042A1 AR P170101950 A ARP170101950 A AR P170101950A AR P170101950 A ARP170101950 A AR P170101950A AR 109042 A1 AR109042 A1 AR 109042A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- haloalkyl
- heterocyclyl
- cycloalkyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 101100091494 Mus musculus Rorc gene Proteins 0.000 title abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 150000002431 hydrogen Chemical group 0.000 abstract 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 3
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 125000004043 oxo group Chemical group O=* 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000001831 (C6-C10) heteroaryl group Chemical group 0.000 abstract 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- -1 C3− cycloalkyl 6 Chemical group 0.000 abstract 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000004475 heteroaralkyl group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000001841 imino group Chemical group [H]N=* 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 238000006467 substitution reaction Methods 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
-
- 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
- A61P37/02—Immunomodulators
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
- C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
- C07D263/56—Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente solicitud provee compuestos que son moduladores de RORg y su uso para el tratamiento de enfermedades o afecciones mediadas por RORg. Asimismo, la presente se refiere a procesos para preparar dichos compuestos, sus formas tautoméricas, intermediarios que participan en su síntesis, sus sales farmacéuticamente aceptables, métodos para usar dichos compuestos, y composiciones farmacéuticas que los contienen. Reivindicación 1: Compuesto que tiene la estructura de fórmula general (1), en la que: A es un sistema de anillos heterocíclicos bicíclicos o monocíclicos; cada R¹ y R² se seleccionan independientemente entre halógeno, alquilo C₁₋₃, alcoxi, CF₃; Y y Z se seleccionan independientemente entre CH o un átomo de N; R³ se selecciona entre hidrógeno, halógeno, alquilo C₁₋₆, haloalquilo C₁₋₆, arilo C₆₋₁₀, heteroarilo C₆₋₁₀, cicloalquilo C₃₋₆, heterociclilo C₄₋₆, NR⁷R⁸; R⁴ se selecciona entre hidrógeno, halógeno, alquilo C₁₋₃; R⁵ se selecciona entre alquilo C₁₋₃; R⁶ se selecciona entre alquilo C₁₋₆, haloalquilo C₁₋₆, cicloalcanilalquilo, heterociclilo C₄₋₆, heterociclilalquilo; R⁴ y R⁶ junto con el átomo de N pueden ciclarse para formar un anillo heterocíclico de 5 miembros con 0 - 1 enlace doble y 1 - 2 átomos de N; la sustitución en R³ se selecciona entre el grupo conformado por hidrógeno, hidroxi, ciano, halógeno, COOH, oxo, haloalquilo C₁₋₆, alquilo C₁₋₆ opcionalmente sustituido, -O(alquilo C₁₋₆), -OCF₃, cicloalquilo C₃₋₆, NR⁷R⁸; en donde R⁷ y R⁸ se seleccionan independientemente entre hidrógeno o alquilo C₁₋₆; el grupo alquilo, tal como se usó más arriba, está opcionalmente sustituido con hidrógeno, hidroxi, -COOH, ciano, halo, oxo, imino, haloalquilo, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₆, arilo, heterociclilo, heteroarilo, aralquilo, heteroaralquilo, heterociclilalquilo; m se selecciona entre los números enteros de 1 - 4; n se selecciona entre los números enteros de 1 - 2.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN201621024155 | 2016-07-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR109042A1 true AR109042A1 (es) | 2018-10-24 |
Family
ID=59581978
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP170101950A AR109042A1 (es) | 2016-07-14 | 2017-07-13 | COMPUESTOS MODULARES DE RORg |
Country Status (3)
| Country | Link |
|---|---|
| AR (1) | AR109042A1 (es) |
| TW (1) | TW201815388A (es) |
| WO (1) | WO2018011747A1 (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11208407B2 (en) * | 2017-08-02 | 2021-12-28 | Merck Sharp & Dohme Corp. | Substituted phenyl compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors |
| CN113527172B (zh) * | 2020-04-21 | 2022-10-25 | 上海交通大学医学院附属仁济医院 | M2乙酰胆碱受体拮抗剂及其用途 |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005034837A2 (en) | 2003-10-08 | 2005-04-21 | Cardiome Pharma Corporation | 7H-IMIDAZO [1,2-α] PYRAZIN-8-ONE COMPOUNDS AS ION CHANNEL MODULATORS |
| WO2012027965A1 (en) | 2010-09-01 | 2012-03-08 | Glaxo Group Limited | Novel compounds |
| WO2012100734A1 (en) | 2011-01-24 | 2012-08-02 | Glaxo Group Limited | Compounds useful as retinoid-related orphan receptor gamma modulators |
| WO2012100732A1 (en) | 2011-01-24 | 2012-08-02 | Glaxo Group Limited | Retinoid-related orphan receptor gamma modulators, composition containing them and uses thereof |
| WO2013029338A1 (en) | 2011-09-01 | 2013-03-07 | Glaxo Group Limited | Novel compounds |
| WO2013171729A2 (en) | 2013-01-08 | 2013-11-21 | Glenmark Pharmaceuticals S.A. | Aryl and heteroaryl amide compounds as rorgamat modulator |
| WO2014125426A1 (en) | 2013-02-15 | 2014-08-21 | Aurigene Discovery Technologies Limited | Trisubstituted heterocyclic derivatives as ror gamma modulators |
| US9868748B2 (en) | 2013-05-01 | 2018-01-16 | Vitae Pharmaceuticals, Inc. | Thiazolopyrrolidine inhibitors of ROR- γ |
| HUE043258T2 (hu) * | 2013-12-05 | 2019-08-28 | Lead Pharma Holding Bv | ROR gamma (RORy) modulátorok |
| WO2015083130A1 (en) | 2013-12-06 | 2015-06-11 | Aurigene Discovery Technologies Limited | Fused pyridine and pyrimidine derivatives as ror gamma modulators |
| WO2015101928A1 (en) | 2013-12-31 | 2015-07-09 | Aurigene Discovery Technologies Limited | Fused thiophene and thiazole derivatives as ror gamma modulators |
| UA121309C2 (uk) | 2014-02-03 | 2020-05-12 | Вітае Фармасьютікалс, Ллс | Дигідропіролопіридинові інгібітори ror-гамма |
| EP3119774A1 (en) | 2014-03-17 | 2017-01-25 | reMynd NV | Oxadiazole compounds |
| WO2015145371A1 (en) | 2014-03-27 | 2015-10-01 | Piramal Enterprises Limited | Ror-gamma modulators and uses thereof |
| SG11201607518RA (en) | 2014-04-16 | 2016-10-28 | Glenmark Pharmaceuticals Sa | Aryl and heteroaryl ether compounds as ror gamma modulators |
| EP3101006A1 (en) | 2015-06-05 | 2016-12-07 | Lead Pharma Cel Models IP B.V. | Ror gamma (rory) modulators |
| EP3101009A1 (en) | 2015-06-05 | 2016-12-07 | Lead Pharma Cel Models IP B.V. | Ror gamma (rory) modulators |
| EP3101007A1 (en) | 2015-06-05 | 2016-12-07 | Lead Pharma Cel Models IP B.V. | Ror gamma (rory) modulators |
| EP3101005A1 (en) | 2015-06-05 | 2016-12-07 | Lead Pharma Cel Models IP B.V. | Ror gamma (rory) modulators |
| EP3101008A1 (en) | 2015-06-05 | 2016-12-07 | Lead Pharma Cel Models IP B.V. | Ror gamma (rory) modulators |
| ES2856931T3 (es) | 2015-08-05 | 2021-09-28 | Vitae Pharmaceuticals Llc | Moduladores de ROR-gamma |
| MX385332B (es) | 2015-11-20 | 2025-03-18 | Vitae Pharmaceuticals Llc | Moduladores de ror-gamma. |
-
2017
- 2017-07-13 TW TW106123418A patent/TW201815388A/zh unknown
- 2017-07-13 AR ARP170101950A patent/AR109042A1/es unknown
- 2017-07-13 WO PCT/IB2017/054240 patent/WO2018011747A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| TW201815388A (zh) | 2018-05-01 |
| WO2018011747A1 (en) | 2018-01-18 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |