PE20171649A1 - ALCOHOLES TRIFLUOROMETILICOS COMO MODULADORES DE ROR(gamma)T - Google Patents
ALCOHOLES TRIFLUOROMETILICOS COMO MODULADORES DE ROR(gamma)TInfo
- Publication number
- PE20171649A1 PE20171649A1 PE2017000795A PE2017000795A PE20171649A1 PE 20171649 A1 PE20171649 A1 PE 20171649A1 PE 2017000795 A PE2017000795 A PE 2017000795A PE 2017000795 A PE2017000795 A PE 2017000795A PE 20171649 A1 PE20171649 A1 PE 20171649A1
- Authority
- PE
- Peru
- Prior art keywords
- gamma
- alkyl
- compounds
- formula
- ror
- Prior art date
Links
- -1 TRIFLUOROMETHYL ALCOHOLS Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002393 azetidinyl group Chemical group 0.000 abstract 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
Classifications
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
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- 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
- C07D417/06—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 carbon chain containing only aliphatic carbon atoms
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- 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
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- 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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P3/00—Drugs for disorders of the metabolism
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- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- 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
- C07D277/32—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 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
- C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/10—Spiro-condensed systems
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Neurosurgery (AREA)
- Endocrinology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Emergency Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Otolaryngology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
Referida a un compuesto de formula I, donde: X es CH, CR1 o N; A1 es alquilo C1-C2; A2 es ciclobutilo o alquilo C1-C4 opcionalmente sustituido o A1 y A2 juntos con el nitrogeno al que estan unidos forman un anillo azetidinilo, piperidinilo, entre otros; R1 es Cl, C(CH3)3, entre otros; R2 es H, F o Cl, o R1 y R2 juntos con el fenilo al que estan unidos forman un grupo naftalenilo o quinolinilo; R3 es CF3 o CH2CH3; A3 es H; A4 es H, alquilo C1-C5, entre otros. Son compuestos preferidos los compuestos de formula i), ii), iii), entre otros. Tambien se refiere a una composicion farmaceutica y a un procedimiento de obtencion. Dichos compuestos son moduladores del receptor nuclear ROR(gamma)t, siendo utiles en el tratamiento de enfermedades inflamatorias, artritis reumatoide, soriasis, entre otros.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462072563P | 2014-10-30 | 2014-10-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20171649A1 true PE20171649A1 (es) | 2017-11-13 |
Family
ID=54754732
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2017000795A PE20171649A1 (es) | 2014-10-30 | 2015-10-30 | ALCOHOLES TRIFLUOROMETILICOS COMO MODULADORES DE ROR(gamma)T |
| PE2017002473A PE20180250A1 (es) | 2014-10-30 | 2015-10-30 | ALCOHOLES TRIFLUOROMETILICOS COMO MODULADORES DE RORyT |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2017002473A PE20180250A1 (es) | 2014-10-30 | 2015-10-30 | ALCOHOLES TRIFLUOROMETILICOS COMO MODULADORES DE RORyT |
Country Status (40)
| Country | Link |
|---|---|
| US (2) | US9850236B2 (es) |
| EP (2) | EP3354651B1 (es) |
| JP (3) | JP6998204B2 (es) |
| KR (2) | KR20170127580A (es) |
| CN (3) | CN107108599A (es) |
| AR (2) | AR102480A1 (es) |
| AU (2) | AU2015339087B2 (es) |
| BR (2) | BR112017008816A2 (es) |
| CA (1) | CA2965512C (es) |
| CL (3) | CL2017001042A1 (es) |
| CO (1) | CO2017005014A2 (es) |
| CR (2) | CR20170166A (es) |
| CY (1) | CY1121716T1 (es) |
| DK (1) | DK3212643T3 (es) |
| EA (2) | EA033699B1 (es) |
| EC (1) | ECSP17033054A (es) |
| ES (2) | ES2724556T3 (es) |
| GT (1) | GT201700090A (es) |
| HR (1) | HRP20190900T1 (es) |
| HU (1) | HUE043624T2 (es) |
| IL (2) | IL251865A0 (es) |
| JO (2) | JOP20200117A1 (es) |
| LT (1) | LT3212643T (es) |
| MA (1) | MA40873B1 (es) |
| ME (1) | ME03426B (es) |
| MX (2) | MX369567B (es) |
| PE (2) | PE20171649A1 (es) |
| PH (2) | PH12017500800A1 (es) |
| PL (1) | PL3212643T3 (es) |
| PT (1) | PT3212643T (es) |
| RS (1) | RS58613B1 (es) |
| SG (2) | SG10201805355YA (es) |
| SI (1) | SI3212643T1 (es) |
| SM (1) | SMT201900290T1 (es) |
| SV (1) | SV2017005429A (es) |
| TR (1) | TR201907763T4 (es) |
| TW (2) | TWI705057B (es) |
| UY (2) | UY36377A (es) |
| WO (1) | WO2016069974A1 (es) |
| ZA (3) | ZA201703679B (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201803869A (zh) * | 2016-04-27 | 2018-02-01 | 健生藥品公司 | 作為ＲＯＲγＴ調節劑之６－胺基吡啶－３－基噻唑 |
| BR112020018718A2 (pt) | 2018-03-12 | 2021-03-09 | Escalier Biosciences B.V. | Moduladores de ror-gama espirocíclicos |
| CN112292124A (zh) * | 2018-03-12 | 2021-01-29 | 爱思凯利尔生物科学私人有限责任公司 | 双环ROR-γ调节剂 |
| US10975057B2 (en) | 2018-06-18 | 2021-04-13 | Janssen Pharmaceutica Nv | 6-aminopyridin-3-yl pyrazoles as modulators of RORgT |
| JP2021528405A (ja) | 2018-06-18 | 2021-10-21 | ヤンセン ファーマシューティカ エヌ．ベー． | ＲＯＲγｔのモジュレータとしてのアミド置換チアゾール |
| US11034658B2 (en) | 2018-06-18 | 2021-06-15 | Janssen Pharmaceutica Nv | Pyridinyl pyrazoles as modulators of RORγT |
| CA3103770A1 (en) | 2018-06-18 | 2019-12-26 | Janssen Pharmaceutica Nv | Phenyl and pyridinyl substituted imidazoles as modulators of roryt |
| WO2023232870A1 (en) | 2022-05-31 | 2023-12-07 | Immunic Ag | Rorg/rorgt modulators for the treatment of virus infections like covid-19 |
| WO2024089216A1 (en) | 2022-10-27 | 2024-05-02 | Syngenta Crop Protection Ag | Novel sulfur-containing heteroaryl carboxamide compounds |
| CN119528866B (zh) * | 2024-11-28 | 2025-10-17 | 河南农业大学 | 一种含双三氟甲基的香豆素叔醇类化合物及其制备方法和应用 |
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|---|---|---|---|---|
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| CA2195847A1 (en) | 1994-07-27 | 1996-02-08 | John J. Talley | Substituted thiazoles for the treatment of inflammation |
| BR0208956A (pt) | 2001-04-16 | 2004-07-13 | Tanabe Seiyaku Co | Abridor de canais de k ativados por cálcio de grande condutância |
| HUP0401160A3 (en) | 2001-08-13 | 2008-01-28 | Janssen Pharmaceutica Nv | 2,4,5-trisubstituted thiazolyl derivatives having antiinflammatory activity, process for their preparation and pharmaceutical compositions containing them |
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| US8188128B2 (en) | 2005-05-12 | 2012-05-29 | The University Of Medicine And Dentistry Of New Jersey | Opioid receptor subtype-selective agents |
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| WO2008064318A2 (en) | 2006-11-22 | 2008-05-29 | University Of Medicine And Dentistry Of New Jersey | Peripheral opioid receptor active compounds |
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