AR078201A1 - Compuestos de 2-piridona y su uso en el tratamiento de enfermedades mediadas por la elastasa de neutrofilos - Google Patents
Compuestos de 2-piridona y su uso en el tratamiento de enfermedades mediadas por la elastasa de neutrofilosInfo
- Publication number
- AR078201A1 AR078201A1 ARP100103564A ARP100103564A AR078201A1 AR 078201 A1 AR078201 A1 AR 078201A1 AR P100103564 A ARP100103564 A AR P100103564A AR P100103564 A ARP100103564 A AR P100103564A AR 078201 A1 AR078201 A1 AR 078201A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- fluoro
- group
- ring
- substituted
- Prior art date
Links
Classifications
-
- 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
-
- 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
-
- 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
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/62—Oxygen or sulfur atoms
- C07D213/63—One oxygen atom
- C07D213/64—One oxygen atom attached in position 2 or 6
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
Abstract
Procesos e intermediarios para prepararlos, composiciones farmacéuticas que los contienen y su uso en terapia. Los compuestos son inhibidores de la elastasa de neutrofilos humanos. Reivindicacion 1. Un compuesto caracterizado porque tiene la formula (1) donde R1 representa hidrogeno o alquilo C1-4; R7 representa un anillo de fenilo o piridinilo, donde dicho anillo está 4- (para) sustituido con fluoro, cloro o CN; X representa N o CR2, donde R2 representa H o fluoro; R3 representa un grupo fenilo sustituido con uno o dos sustituyentes seleccionados de manera independiente entre fluor, cloro y trifluorometilo; L representa alquileno C2-4; R4, R5 y R6 representan independientemente alquilo C1-6; o R4 y R5 pueden estar unidos de manera que el grupo NR4R5 representa un grupo cíclico amonio de 5 o 6 miembros; y Y representa un anion farmacéuticamente aceptable. Reivindicacion 18: Un compuesto caracterizado porque es de la formula (2) donde R1 representa hidrogeno o alquilo C1-4; R7 representa un anillo de fenilo o piridinilo; donde dicho anillo está 4- (para) sustituido con fluoro, cloro o CN; X representa N o CR2, donde R2 representa H o fluoro; R3 representa un grupo fenilo sustituido con uno o dos sustituyentes seleccionados de manera independiente entre fluor, cloro y trifluorometilo; L representa alquileno C2-4; R4 y R5 representan independientemente alquilo C1-6; o R4 y R5 pueden estar unidos de manera que el grupo NR4R5 representa un grupo cíclico de 5 o 6 miembros; o una sal de éste. Reivindicacion 19: Un compuesto caracterizado porque es de la formula (8), o una sal de éste donde R1' representa alquilo C1-4; X representa N o CR2, donde R2 representa H o fluoro; L representa alquileno C2-4; R4' y R5' representan independientemente alquilo C1-6; o R4' y R5' pueden estar unidos de manera que el grupo NR4'R5' representa un anillo heterocíclico no aromático saturado o parcialmente saturado de 5 o 6 miembros que contiene 1 nitrogeno y opcionalmente 1, 2 o 3 heteroátomos seleccionados entre oxígeno, azufre y nitrogeno; y R9 es halo; o una sal de éste.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US24808109P | 2009-10-02 | 2009-10-02 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR078201A1 true AR078201A1 (es) | 2011-10-19 |
Family
ID=42983551
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100103564A AR078201A1 (es) | 2009-10-02 | 2010-09-30 | Compuestos de 2-piridona y su uso en el tratamiento de enfermedades mediadas por la elastasa de neutrofilos |
Country Status (14)
Country | Link |
---|---|
US (1) | US8436024B2 (es) |
EP (1) | EP2483244A1 (es) |
JP (1) | JP2013506649A (es) |
KR (1) | KR20120099639A (es) |
CN (1) | CN102639505A (es) |
AR (1) | AR078201A1 (es) |
AU (1) | AU2010302420B2 (es) |
BR (1) | BR112012007322A2 (es) |
CA (1) | CA2773618A1 (es) |
MX (1) | MX2012003644A (es) |
RU (1) | RU2012116877A (es) |
TW (1) | TW201118078A (es) |
UY (1) | UY32918A (es) |
WO (1) | WO2011039528A1 (es) |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TW200808771A (en) * | 2006-05-08 | 2008-02-16 | Astrazeneca Ab | Novel compounds II |
US10105356B2 (en) * | 2011-01-31 | 2018-10-23 | Avalyn Pharma Inc. | Aerosol pirfenidone and pyridone analog compounds and uses thereof |
EP4059499A1 (en) | 2011-01-31 | 2022-09-21 | Avalyn Pharma Inc. | Aerosol pirfenidone and pyridone analog compounds and uses thereof |
US9388137B2 (en) | 2011-10-31 | 2016-07-12 | Purdue Pharma L.P. | Quaternized amines as sodium channel blockers |
EP2872509B1 (en) * | 2012-07-12 | 2016-09-14 | Chiesi Farmaceutici S.p.A. | Inhibition of enzymes |
JP6501264B2 (ja) * | 2012-07-24 | 2019-04-17 | アヴァリン ファーマ インク. | エアロゾルのピルフェニドン及びピリドンのアナログの化合物、及び、その使用 |
US20140057920A1 (en) | 2012-08-23 | 2014-02-27 | Boehringer Ingelheim International Gmbh | Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity |
US9102624B2 (en) | 2012-08-23 | 2015-08-11 | Boehringer Ingelheim International Gmbh | Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity |
US20140057926A1 (en) | 2012-08-23 | 2014-02-27 | Boehringer Ingelheim International Gmbh | Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity |
CN105339780A (zh) | 2013-03-15 | 2016-02-17 | 拜耳医药保健有限公司 | 蛋白酶在中性粒细胞胞外诱捕网中的底物性质 |
JP7066321B2 (ja) | 2014-01-10 | 2022-05-13 | アヴァリン ファーマ インク. | エアロゾルのピルフェニドン及びピリドンのアナログの化合物、及び、その使用 |
US9221807B2 (en) | 2014-02-21 | 2015-12-29 | Boehringer Ingelheim International Gmbh | Substituted pyridones and pyrazinones and their use as inhibitors of neutrophil elastase activity |
GEP20207130B (en) * | 2016-05-31 | 2020-07-10 | Chiesi Farm Spa | Imidazolone compounds as human neutrophil elastase inhibitors |
KR20200020210A (ko) | 2018-08-16 | 2020-02-26 | 서울대학교산학협력단 | 식물 추출물을 함유하는 호중구 엘라스타아제 억제용 조성물 |
AU2020349353A1 (en) | 2019-09-17 | 2022-04-14 | Duke University | Alvelestat for use in the treatment of graft rejection, bronchiolitis obliterans syndrome and graft versus host disease |
EP4125891A1 (en) * | 2020-03-27 | 2023-02-08 | Aclaris Therapeutics, Inc. | Process, compositions, and crystalline forms of substituted pyridinone-pyridinyl compounds |
PL4106757T3 (pl) | 2020-04-16 | 2024-01-22 | Mereo Biopharma 4 Limited | Sposoby z udziałem inhibitora elastazy neutrofilowej, alwelestatu, do leczenia choroby układu oddechowego, w której pośredniczy niedobór alfa-1 antytrypsyny |
AU2022373971A1 (en) | 2021-10-20 | 2024-04-04 | Mereo Biopharma 4 Limited | Neutrophil elastase inhibitors for use in the treatment of fibrosis |
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TW200808771A (en) * | 2006-05-08 | 2008-02-16 | Astrazeneca Ab | Novel compounds II |
TW200801513A (en) | 2006-06-29 | 2008-01-01 | Fermiscan Australia Pty Ltd | Improved process |
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WO2008104752A1 (en) | 2007-02-26 | 2008-09-04 | Astrazeneca Ab | Dihydropyridones as elastase inhibitors |
WO2009058076A1 (en) | 2007-11-02 | 2009-05-07 | Astrazeneca Ab | 2-pyrazinone derivatives and their use as inhibitors of neutrophile elastase |
AR069206A1 (es) * | 2007-11-06 | 2010-01-06 | Astrazeneca Ab | Derivados de 2-pirazinona, proceso para preparalos, composiciones farmaceuticas que los comprenden, proceso de preparacion de las mismas y usos en el tratamiento de trastornos osteoarticularesy del aparato respiratorio, entre otros. |
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TW201036957A (en) * | 2009-02-20 | 2010-10-16 | Astrazeneca Ab | Novel salt 628 |
-
2010
- 2010-09-22 MX MX2012003644A patent/MX2012003644A/es unknown
- 2010-09-22 RU RU2012116877/04A patent/RU2012116877A/ru not_active Application Discontinuation
- 2010-09-22 KR KR1020127008238A patent/KR20120099639A/ko not_active Application Discontinuation
- 2010-09-22 BR BR112012007322A patent/BR112012007322A2/pt not_active IP Right Cessation
- 2010-09-22 CN CN2010800548567A patent/CN102639505A/zh active Pending
- 2010-09-22 CA CA2773618A patent/CA2773618A1/en not_active Abandoned
- 2010-09-22 EP EP10760396A patent/EP2483244A1/en not_active Withdrawn
- 2010-09-22 JP JP2012531500A patent/JP2013506649A/ja active Pending
- 2010-09-22 WO PCT/GB2010/051589 patent/WO2011039528A1/en active Application Filing
- 2010-09-22 AU AU2010302420A patent/AU2010302420B2/en not_active Ceased
- 2010-09-30 UY UY0001032918A patent/UY32918A/es unknown
- 2010-09-30 AR ARP100103564A patent/AR078201A1/es unknown
- 2010-10-01 US US12/895,995 patent/US8436024B2/en not_active Expired - Fee Related
- 2010-10-01 TW TW099133516A patent/TW201118078A/zh unknown
Also Published As
Publication number | Publication date |
---|---|
US8436024B2 (en) | 2013-05-07 |
KR20120099639A (ko) | 2012-09-11 |
AU2010302420B2 (en) | 2013-07-04 |
CN102639505A (zh) | 2012-08-15 |
WO2011039528A1 (en) | 2011-04-07 |
MX2012003644A (es) | 2012-04-30 |
AU2010302420A1 (en) | 2012-04-19 |
US20110082155A1 (en) | 2011-04-07 |
BR112012007322A2 (pt) | 2017-06-06 |
UY32918A (es) | 2011-04-29 |
RU2012116877A (ru) | 2013-11-10 |
JP2013506649A (ja) | 2013-02-28 |
TW201118078A (en) | 2011-06-01 |
CA2773618A1 (en) | 2011-04-07 |
EP2483244A1 (en) | 2012-08-08 |
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