AR107428A1 - COMPUESTOS DE ISOXAZOL DE ÁCIDO HIDROXÁMICO COMO INHIBIDORES DE LpxC - Google Patents
COMPUESTOS DE ISOXAZOL DE ÁCIDO HIDROXÁMICO COMO INHIBIDORES DE LpxCInfo
- Publication number
- AR107428A1 AR107428A1 ARP150104119A ARP150104119A AR107428A1 AR 107428 A1 AR107428 A1 AR 107428A1 AR P150104119 A ARP150104119 A AR P150104119A AR P150104119 A ARP150104119 A AR P150104119A AR 107428 A1 AR107428 A1 AR 107428A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- halo
- alkoxy
- hydroxy
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- JIUZZEOWWWKQSA-UHFFFAOYSA-N n-hydroxy-1,2-oxazole-3-carboxamide Chemical class ONC(=O)C=1C=CON=1 JIUZZEOWWWKQSA-UHFFFAOYSA-N 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 2
- -1 hydroxy, amino Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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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
- A61K31/42—Oxazoles
-
- 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
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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
- 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
- C07D413/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (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)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable del mismo, donde: X es -NH-, y R¹ es -CH(OH)-Y; o X es -CH₂-, y R¹ es -CH(OH)-Y o -SO₂R² donde R² es C₁₋₃ alquilo; R³ es H o halo; Y se selecciona de un anillo heteroarilo de 5 miembros que contiene 1 - 3 heteroátomos seleccionados de entre N, O y S como miembros del anillo, fenilo y alquilo C₁₋₃ y cada Y está opcionalmente sustituido con uno a tres R⁴; cada R⁴ se selecciona independientemente de halo, alquilo C₁₋₃ y cicloalquilo C₃₋₆, donde el alquilo C₁₋₃ Y el cicloalquilo C₃₋₆ están cada uno opcionalmente sustituido con hasta tres grupos seleccionados de entre halo, CN y -OH; L es -CºC- o -CR⁵=CR⁵-; R⁵ se selecciona independientemente en cada caso entre H, halo y metilo; y Z se selecciona de entre alquilo C₁₋₆, cicloalquilo C₃₋₆. piridinilo y fenilo, cada uno de los cuales está opcionalmente sustituido con hasta tres grupos seleccionados de entre halógeno, hidroxi, alcoxi C₁₋₄, haloalcoxi C₁₋₄ CN y alquilo C₁₋₄, que está opcionalmente sustituido con uno a tres grupos seleccionados de entre halógeno, hidroxi, amino, CN y alcoxi C₁₋₃; o, cuando L es -CR⁵=CR⁵-, Z junto con uno de los grupos R⁵ y cualesquiera átomos que conectan Z con el grupo R⁵ pueden formar un grupo cicloalquilo o cicloalquenilo de 3 a 7 miembros, que está opcionalmente sustituido con hasta tres grupos seleccionados de entre halógeno, hidroxi, alcoxi C₁₋₄, haloalcoxi C₁₋₄, CN y alquilo C₁₋₄ que está opcionalmente sustituido con uno a tres grupos seleccionados de entre halógeno, hidroxi, amino, CN y alcoxi C₁₋₃.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462092402P | 2014-12-16 | 2014-12-16 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR107428A1 true AR107428A1 (es) | 2018-05-02 |
Family
ID=55025302
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150104119A AR107428A1 (es) | 2014-12-16 | 2015-12-16 | COMPUESTOS DE ISOXAZOL DE ÁCIDO HIDROXÁMICO COMO INHIBIDORES DE LpxC |
Country Status (42)
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX385187B (es) | 2013-05-17 | 2025-03-14 | Incyte Holdings Corp | Derivados del bipirazol como inhibidores de janus cinasa (jak) |
| PH12018502523B1 (en) * | 2016-06-14 | 2023-05-12 | Novartis Ag | Crystalline form of (r)-4-(5-(cyclopropylethynyl)isoxazol-3-yl)-n-hydroxy-2-methyl-2-(methylsulfonyl)butanamide as an antibacterial agent |
| CN107434766A (zh) * | 2017-08-09 | 2017-12-05 | 凯莱英医药集团（天津）股份有限公司 | 烷烃羟胺类化合物的合成装置及连续合成方法 |
| BR112020016628A2 (pt) | 2018-02-16 | 2020-12-15 | Incyte Corporation | Inibidores da via de jak1 para o tratamento de distúrbios relacionados a citocinas |
| SG11202102712WA (en) | 2018-09-20 | 2021-04-29 | Forge Therapeutics Inc | Antibacterial compounds |
| WO2020105660A1 (ja) * | 2018-11-21 | 2020-05-28 | 大正製薬株式会社 | 新規イミダゾール誘導体 |
| PL4157831T3 (pl) | 2020-06-02 | 2025-03-03 | Incyte Corporation | Sposoby wytwarzania inhibitora jak1 |
| MX2023006542A (es) | 2020-12-08 | 2023-08-25 | Incyte Corp | Inhibidores de la vía cinasa jano 1 (jak1) para el tratamiento del vitiligo. |
| CN112603936B (zh) * | 2020-12-28 | 2022-08-02 | 仲恺农业工程学院 | 一种抑制气单胞菌属的组合物及其制备方法与应用 |
| US20240150298A1 (en) * | 2021-02-11 | 2024-05-09 | Blacksmith Medicines, Inc. | Antibacterial compounds |
| US20240166609A1 (en) * | 2021-02-11 | 2024-05-23 | Blacksmith Medicines, Inc. | Antibacterial compounds |
| FI4333840T3 (fi) | 2021-05-03 | 2025-12-12 | Incyte Corp | Jak1-reitin estäjiä kyhmykutinan hoitoon |
| CA3233328A1 (en) * | 2021-09-28 | 2023-04-06 | Min Teng | Lpxc inhibitors and uses thereof |
| WO2024067812A1 (zh) * | 2022-09-28 | 2024-04-04 | 浙江海正药业股份有限公司 | 芳香乙炔类衍生物及其制备方法和用途 |
| CN119923396A (zh) * | 2022-09-28 | 2025-05-02 | 浙江海正药业股份有限公司 | 芳香乙炔类衍生物及其制备方法和其医药上的用途 |
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2015
- 2015-12-15 JP JP2017532143A patent/JP6697466B2/ja not_active Expired - Fee Related
- 2015-12-15 US US14/969,930 patent/US9549916B2/en not_active Expired - Fee Related
- 2015-12-15 CN CN201580066726.8A patent/CN107001295B/zh not_active Expired - Fee Related
- 2015-12-15 PL PL15816893T patent/PL3233843T3/pl unknown
- 2015-12-15 SG SG11201704053WA patent/SG11201704053WA/en unknown
- 2015-12-15 EP EP15816893.0A patent/EP3233843B1/en active Active
- 2015-12-15 TW TW104142164A patent/TWI693215B/zh not_active IP Right Cessation
- 2015-12-15 HR HRP20192009TT patent/HRP20192009T1/hr unknown
- 2015-12-15 HU HUE15816893A patent/HUE047225T2/hu unknown
- 2015-12-15 KR KR1020177016102A patent/KR20170094214A/ko not_active Withdrawn
- 2015-12-15 DK DK15816893T patent/DK3233843T3/da active
- 2015-12-15 WO PCT/IB2015/059631 patent/WO2016097995A1/en not_active Ceased
- 2015-12-15 LT LT15816893T patent/LT3233843T/lt unknown
- 2015-12-15 EA EA201791353A patent/EA032138B1/ru not_active IP Right Cessation
- 2015-12-15 CA CA2969803A patent/CA2969803A1/en not_active Abandoned
- 2015-12-15 RS RS20191403A patent/RS59507B1/sr unknown
- 2015-12-15 AU AU2015365455A patent/AU2015365455B2/en not_active Ceased
- 2015-12-15 SI SI201530987T patent/SI3233843T1/sl unknown
- 2015-12-15 PT PT158168930T patent/PT3233843T/pt unknown
- 2015-12-15 UA UAA201705042A patent/UA121225C2/uk unknown
- 2015-12-15 PE PE2017001078A patent/PE20171044A1/es unknown
- 2015-12-15 CR CR20170260A patent/CR20170260A/es unknown
- 2015-12-15 MA MA41185A patent/MA41185B1/fr unknown
- 2015-12-15 ME MEP-2019-305A patent/ME03546B/me unknown
- 2015-12-15 MY MYPI2017701741A patent/MY195743A/en unknown
- 2015-12-15 SM SM20190631T patent/SMT201900631T1/it unknown
- 2015-12-15 MX MX2017007980A patent/MX2017007980A/es active IP Right Grant
- 2015-12-15 ES ES15816893T patent/ES2756300T3/es active Active
- 2015-12-15 TN TN2017000207A patent/TN2017000207A1/en unknown
- 2015-12-15 BR BR112017011422-4A patent/BR112017011422A2/pt not_active IP Right Cessation
- 2015-12-15 CU CU2017000084A patent/CU24443B1/es unknown
- 2015-12-16 UY UY0001036448A patent/UY36448A/es not_active Application Discontinuation
- 2015-12-16 JO JOP/2015/0318A patent/JO3818B1/ar active
- 2015-12-16 AR ARP150104119A patent/AR107428A1/es unknown
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2016
- 2016-12-12 US US15/375,560 patent/US9815804B2/en not_active Expired - Fee Related
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2017
- 2017-05-18 IL IL25237317A patent/IL252373B/en active IP Right Grant
- 2017-06-01 PH PH12017501019A patent/PH12017501019B1/en unknown
- 2017-06-08 CL CL2017001460A patent/CL2017001460A1/es unknown
- 2017-06-14 CO CONC2017/0005870A patent/CO2017005870A2/es unknown
- 2017-06-16 SV SV2017005462A patent/SV2017005462A/es unknown
- 2017-06-16 GT GT201700132A patent/GT201700132A/es unknown
- 2017-07-16 EC ECIEPI201745737A patent/ECSP17045737A/es unknown
- 2017-10-09 US US15/728,351 patent/US10029994B2/en active Active
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2019
- 2019-11-11 CY CY20191101181T patent/CY1122305T1/el unknown
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