AR109042A1 - RORg MODULAR COMPOUNDS - Google Patents
RORg MODULAR COMPOUNDSInfo
- 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)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (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.The present application provides compounds that are modulators of RORg and their use for the treatment of diseases or conditions mediated by RORg. Likewise, this refers to processes for preparing said compounds, their tautomeric forms, intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using said compounds, and pharmaceutical compositions containing them. Claim 1: Compound having the structure of general formula (1), wherein: A is a bicyclic or monocyclic heterocyclic ring system; each R¹ and R² are independently selected from halogen, C₁₋₃ alkyl, alkoxy, CF₃; Y and Z are independently selected from CH or an N atom; R³ is selected from hydrogen, halogen, C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₆₋₁₀ aryl, C₆₋₁₀ heteroaryl, C₃₋₆ cycloalkyl, C₄₋₆ heterocyclyl, NR⁷R⁸; R⁴ is selected from hydrogen, halogen, C₁₋₃ alkyl; R⁵ is selected from C₁₋₃ alkyl; R⁶ is selected from C₁₋₆ alkyl, C₁₋₆ haloalkyl, cycloalkyl alkyl, C₄₋₆ heterocyclyl, heterocyclyl alkyl; R⁴ and R⁶ together with the N atom can be cyclized to form a 5-membered heterocyclic ring with 0-1 double bond and 1-2 N atoms; the substitution in R³ is selected from the group consisting of hydrogen, hydroxy, cyano, halogen, COOH, oxo, C₁₋₆ haloalkyl, optionally substituted C₁₋₆ alkyl, -O (C₁₋₆ alkyl), -OCF₃, C₃₋ cycloalkyl ₆, NR⁷R⁸; wherein R⁷ and R⁸ are independently selected from hydrogen or C₁₋₆ alkyl; the alkyl group, as used above, is optionally substituted with hydrogen, hydroxy, -COOH, cyano, halo, oxo, imino, haloalkyl, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋ cycloalkyl ₆, aryl, heterocyclyl, heteroaryl, aralkyl, heteroaralkyl, heterocyclylalkyl; m is selected from the whole numbers of 1-4; n is selected from the whole numbers of 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 (en) | 2018-10-24 |
Family
ID=59581978
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP170101950A AR109042A1 (en) | 2016-07-14 | 2017-07-13 | RORg MODULAR COMPOUNDS |
Country Status (3)
| Country | Link |
|---|---|
| AR (1) | AR109042A1 (en) |
| TW (1) | TW201815388A (en) |
| WO (1) | WO2018011747A1 (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019027855A1 (en) * | 2017-08-02 | 2019-02-07 | Merck Sharp & Dohme Corp. | Novel substituted phenyl compounds as indoleamine 2,3-dioxygenase (ido) inhibitors |
| CN113527172B (en) * | 2020-04-21 | 2022-10-25 | 上海交通大学医学院附属仁济医院 | M2 acetylcholine receptor antagonists and uses thereof |
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 |
| WO2012100732A1 (en) | 2011-01-24 | 2012-08-02 | Glaxo Group Limited | Retinoid-related orphan receptor gamma modulators, composition containing them and uses thereof |
| WO2012100734A1 (en) | 2011-01-24 | 2012-08-02 | Glaxo Group Limited | Compounds useful as retinoid-related orphan receptor gamma modulators |
| 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 |
| EP2991994B1 (en) | 2013-05-01 | 2018-08-15 | Vitae Pharmaceuticals, Inc. | Thiazolopyrrolidine inhibitors of ror-gamma |
| DK3077372T3 (en) * | 2013-12-05 | 2019-04-23 | Lead Pharma Holding Bv | ROR GAMMA MODULATORS |
| 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 |
| JP6466461B2 (en) | 2014-02-03 | 2019-02-06 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | Dihydropyrrolopyridine inhibitors of ROR gamma |
| EP3119774A1 (en) | 2014-03-17 | 2017-01-25 | reMynd NV | Oxadiazole compounds |
| CA2942871A1 (en) | 2014-03-27 | 2015-10-01 | Piramal Enterprises Limited | Ror-gamma modulators and uses thereof |
| CN106232582A (en) | 2014-04-16 | 2016-12-14 | 格兰马克药品股份有限公司 | Aryl and heteroaryl ether compound as ROR gamma modulators |
| EP3101007A1 (en) | 2015-06-05 | 2016-12-07 | Lead Pharma Cel Models IP B.V. | Ror gamma (rory) modulators |
| EP3101006A1 (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 |
| EP3101005A1 (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 |
| EP3331876B1 (en) | 2015-08-05 | 2020-10-07 | Vitae Pharmaceuticals, LLC | Modulators of ror-gamma |
| JP6914257B2 (en) | 2015-11-20 | 2021-08-04 | ヴァイティー ファーマシューティカルズ，エルエルシー | ROR-gamma modulator |
-
2017
- 2017-07-13 AR ARP170101950A patent/AR109042A1/en unknown
- 2017-07-13 WO PCT/IB2017/054240 patent/WO2018011747A1/en not_active Ceased
- 2017-07-13 TW TW106123418A patent/TW201815388A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2018011747A1 (en) | 2018-01-18 |
| TW201815388A (en) | 2018-05-01 |
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