AR102967A1 - Derivados de imidazolona inhibidores de elastasas de neutrófilos humanos - Google Patents
Derivados de imidazolona inhibidores de elastasas de neutrófilos humanosInfo
- Publication number
- AR102967A1 AR102967A1 ARP150104032A ARP150104032A AR102967A1 AR 102967 A1 AR102967 A1 AR 102967A1 AR P150104032 A ARP150104032 A AR P150104032A AR P150104032 A ARP150104032 A AR P150104032A AR 102967 A1 AR102967 A1 AR 102967A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- chr6
- cycloalkyl
- neutrófilos
- elastasas
- Prior art date
Links
- WZELXJBMMZFDDU-UHFFFAOYSA-N Imidazol-2-one Chemical class O=C1N=CC=N1 WZELXJBMMZFDDU-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 9
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 5
- 101100244083 Arabidopsis thaliana PKL gene Proteins 0.000 abstract 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 3
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 229910052736 halogen Chemical group 0.000 abstract 2
- 150000002367 halogens Chemical group 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical group F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 abstract 1
- 108010081348 HRT1 protein Hairy Chemical group 0.000 abstract 1
- 102100021881 Hairy/enhancer-of-split related with YRPW motif protein 1 Human genes 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
- C07D233/70—One oxygen atom
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- 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
- 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
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- 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
- A61P11/06—Antiasthmatics
-
- 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
- A61P11/08—Bronchodilators
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
- C07C53/02—Formic acid
- C07C53/06—Salts thereof
-
- 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
- C07D401/14—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 three or more hetero 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
- C07D403/14—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 three or more hetero 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
- C07D405/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Reivindicación 1: Un compuesto caracterizado porque es de fórmula general (1) donde A es -CH o -N-; B es -CH o -N-; D es -CH o -N-; X es -CH o -N-; R³ es -CF₃, CHF₂ o halógeno; W es un anillo heteroarilo de 5 ó 6 miembros, opcionalmente sustituido con uno o más sustituyentes seleccionados entre -CN, -NO₂, -OC₁₋₆ alquilo, -C₁₋₃ alquil-O-C₁₋₆ alquilo, -C₁₋₃ alquilamino, -C₃₋₈ cicloalquilo, -OH, C₁₋₃ alquilo, halo, -CF₃ y -SO₂C₁₋₄ alquilo; R¹ es H o se selecciona entre el grupo que consiste en -C(O)R⁴, -(CH₂)ₜ-(CHR⁶)ₙ-R⁴, -(CH₂)ₜ-(CHR⁶)ₙS(O₂)-NR⁴R⁵, -S(O₂)-R⁴, -(CH₂)ₜ-(CHR⁶)ₙ-C(O)-NR⁴R⁵, -(CH₂)ₜ-(CHR⁶)ₙ-C(O)O-R⁴; R⁴ es H o se selecciona entre el grupo que consiste en -C₁₋₆ alquilo, -C₂₋₆ alquil-NR⁷R⁸, -C₂₋₆ alquil-N⁺R⁷R⁸R⁹, -C₂₋₆ alquil-O-C₁₋₄ alquilo, -C₂₋₆ alquil-S(O₂)C₁₋₄ alquilo, -(CH₂)ₜ-arilo, -(CH₂)ₜ-C₃₋₈ cicloalquilo, -(CH₂)ₜ-C₃₋₈ heterocicloalquilo y -(CH₂)ₜ-heteroarilo, opcionalmente sustituido con uno o más sustituyentes seleccionados entre -CN, -NO₂, -OC₁₋₆ alquilo, -C₁₋₃ alquil-O-C₁₋₆ alquilo,-C₁₋₃ alquilamino, -C₃₋₈ cicloalquilo, -OH, C₁₋₃ alquilo, halo, -CF₃ y -SO₂C₁₋₄ alquilo; n es 0 o un entero seleccionado entre 1, 2 ó 3; t es 0 o un entero seleccionado entre 1, 2 ó 3; R⁵ es H o -C₁₋₆ alquilo; R⁶ es H, -C₁₋₆ alquilo, -CF₃ o -CHF₂; R⁷ es H o -C₁₋₆ alquilo; R⁸ es H o -C₁₋₆ alquilo; R⁹ es H o -C₁₋₆ alquilo; donde de manera alternativa R⁴ y R⁵ junto con él átomo de nitrógeno al cual están unidos pueden formar un sistema de anillo C₃₋₈ heterocicloalquilo o heteroarilo, opcionalmente sustituido con uno o más sustituyentes seleccionados entre -CN, -NO₂, -OC₁₋₆ alquilo, -C₁₋₃ alquil-O-C₁₋₆ alquilo, -C₁₋₃ alquilamino, -C₃₋₈ cicloalquilo, -OH, C₁₋₃ alquilo, halo, -CF₃ y -SO₂C₁₋₄ alquilo, donde los heteroátomos del sistema de anillo C₃₋₈ heterocicloalquilo o heteroarilo son un máximo de tres y se seleccionan entre -N, -NH, -O, -S- y -SO₂; R² es H o se selecciona entre el grupo que consiste de, -SMe, -S(O)R⁷, -S(O₂)R⁷ y halógeno; y sales aceptables farmacéuticamente del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14198044 | 2014-12-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR102967A1 true AR102967A1 (es) | 2017-04-05 |
Family
ID=52133873
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150104032A AR102967A1 (es) | 2014-12-15 | 2015-12-10 | Derivados de imidazolona inhibidores de elastasas de neutrófilos humanos |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US9409870B2 (es) |
| EP (1) | EP3233833B1 (es) |
| KR (1) | KR20170095262A (es) |
| CN (1) | CN107108577A (es) |
| AR (1) | AR102967A1 (es) |
| BR (1) | BR112017012608A2 (es) |
| CA (1) | CA2970664A1 (es) |
| MX (1) | MX2017007676A (es) |
| RU (1) | RU2017120277A (es) |
| TR (1) | TR201907044T4 (es) |
| TW (1) | TW201629040A (es) |
| WO (1) | WO2016096638A1 (es) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017207433A1 (en) * | 2016-05-31 | 2017-12-07 | Chiesi Farmaceutici S.P.A. | Hetetocyclic compounds for use in the treatment of a disease in which hne is implicated |
| AR108610A1 (es) * | 2016-05-31 | 2018-09-05 | Chiesi Farm Spa | Derivados de imidazolona inhibidores de la elastasa de neutrófilos humana |
| US10172830B2 (en) | 2016-05-31 | 2019-01-08 | Chiesi Farmaceutici S.P.A. | Pyrazolone compounds having human neutrophil elastase inhibitory properties |
| KR102872760B1 (ko) | 2019-09-25 | 2025-10-16 | 더 트러스티즈 오브 인디애나 유니버시티 | 펄스 모드 전하 검출 질량 분석을 위한 장치 및 방법 |
| WO2021072186A1 (en) | 2019-10-10 | 2021-04-15 | The Trustees Of Indiana University | System and method for identifying, selecting and purifying particles |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7531560B2 (en) | 2004-11-10 | 2009-05-12 | Boehringer Ingelheim Pharmaceuticals, Inc. | Anti-cytokine heterocyclic compounds |
| TW200808763A (en) | 2006-05-08 | 2008-02-16 | Astrazeneca Ab | Novel compounds I |
| US9040516B2 (en) | 2011-08-01 | 2015-05-26 | Sumitomo Dainippon Pharma Co., Ltd. | Uracil derivative and use thereof for medical purposes |
| CA2878792A1 (en) | 2012-07-12 | 2014-01-16 | Chiesi Farmaceutici S.P.A. | Inhibition of enzymes |
-
2015
- 2015-11-27 US US14/953,183 patent/US9409870B2/en active Active
- 2015-12-10 TW TW104141508A patent/TW201629040A/zh unknown
- 2015-12-10 AR ARP150104032A patent/AR102967A1/es unknown
- 2015-12-11 TR TR2019/07044T patent/TR201907044T4/tr unknown
- 2015-12-11 CA CA2970664A patent/CA2970664A1/en not_active Abandoned
- 2015-12-11 RU RU2017120277A patent/RU2017120277A/ru not_active Application Discontinuation
- 2015-12-11 CN CN201580068314.8A patent/CN107108577A/zh active Pending
- 2015-12-11 BR BR112017012608A patent/BR112017012608A2/pt not_active Application Discontinuation
- 2015-12-11 WO PCT/EP2015/079371 patent/WO2016096638A1/en not_active Ceased
- 2015-12-11 EP EP15816401.2A patent/EP3233833B1/en active Active
- 2015-12-11 MX MX2017007676A patent/MX2017007676A/es unknown
- 2015-12-11 KR KR1020177018071A patent/KR20170095262A/ko not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| US20160168101A1 (en) | 2016-06-16 |
| TW201629040A (zh) | 2016-08-16 |
| EP3233833B1 (en) | 2019-02-20 |
| WO2016096638A1 (en) | 2016-06-23 |
| MX2017007676A (es) | 2017-10-27 |
| US9409870B2 (en) | 2016-08-09 |
| CA2970664A1 (en) | 2016-06-23 |
| EP3233833A1 (en) | 2017-10-25 |
| CN107108577A (zh) | 2017-08-29 |
| TR201907044T4 (tr) | 2019-06-21 |
| KR20170095262A (ko) | 2017-08-22 |
| RU2017120277A (ru) | 2019-01-17 |
| BR112017012608A2 (pt) | 2018-01-16 |
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