CN104428300B - 酶的抑制 - Google Patents
酶的抑制 Download PDFInfo
- Publication number
- CN104428300B CN104428300B CN201380036973.4A CN201380036973A CN104428300B CN 104428300 B CN104428300 B CN 104428300B CN 201380036973 A CN201380036973 A CN 201380036973A CN 104428300 B CN104428300 B CN 104428300B
- Authority
- CN
- China
- Prior art keywords
- phenyl
- methyl
- trifluoromethyl
- base
- pyridine
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
- 0 *C(C(Br)=C(*)N(C1=NN2)C2=O)=C1C1=CC=CCC1 Chemical compound *C(C(Br)=C(*)N(C1=NN2)C2=O)=C1C1=CC=CCC1 0.000 description 1
- YJXQLSZMFGMNID-OUBWWKSTSA-N CC(C(/C(/N(c(cc1)ccc1C#N)N)=C/C=C)=CN(C1=NN2CC(NC)=O)C2=O)=C1c1cc(C(F)(F)F)ccc1 Chemical compound CC(C(/C(/N(c(cc1)ccc1C#N)N)=C/C=C)=CN(C1=NN2CC(NC)=O)C2=O)=C1c1cc(C(F)(F)F)ccc1 YJXQLSZMFGMNID-OUBWWKSTSA-N 0.000 description 1
- DYUGRFPEKXFPLU-UHFFFAOYSA-N CC(Nc1n[n](cc(C(N)=O)c(C)c2-c3cc(C(F)(F)F)ccc3)c2n1)=O Chemical compound CC(Nc1n[n](cc(C(N)=O)c(C)c2-c3cc(C(F)(F)F)ccc3)c2n1)=O DYUGRFPEKXFPLU-UHFFFAOYSA-N 0.000 description 1
- DPLUAKYCHXRWTJ-UHFFFAOYSA-N CC(Nc1n[n](cc(c(C)c2-c3cc(C(F)(F)F)ccc3)Br)c2n1)=O Chemical compound CC(Nc1n[n](cc(c(C)c2-c3cc(C(F)(F)F)ccc3)Br)c2n1)=O DPLUAKYCHXRWTJ-UHFFFAOYSA-N 0.000 description 1
- PTLRJWFVZCOBOV-UHFFFAOYSA-N CC1C(c2ccn[n]2-c(cc2)ccc2N)=C[n]2nc(NC(NC(CC3)CCN3C(OC(C)(C)C)=O)O)nc2C1C1C=C(C(F)(F)F)C=CC1 Chemical compound CC1C(c2ccn[n]2-c(cc2)ccc2N)=C[n]2nc(NC(NC(CC3)CCN3C(OC(C)(C)C)=O)O)nc2C1C1C=C(C(F)(F)F)C=CC1 PTLRJWFVZCOBOV-UHFFFAOYSA-N 0.000 description 1
- GATVXKDTEWPUKL-UHFFFAOYSA-N CS(c1cc(C#N)ccc1NN)(=O)=O Chemical compound CS(c1cc(C#N)ccc1NN)(=O)=O GATVXKDTEWPUKL-UHFFFAOYSA-N 0.000 description 1
- CPGWEUYHMMXUIA-UHFFFAOYSA-N Cc(c(-c1ccn[n]1-c(cc1)ccc1C#N)c[n]1c2ncc1)c2-c1cc(C(F)(F)F)ccc1 Chemical compound Cc(c(-c1ccn[n]1-c(cc1)ccc1C#N)c[n]1c2ncc1)c2-c1cc(C(F)(F)F)ccc1 CPGWEUYHMMXUIA-UHFFFAOYSA-N 0.000 description 1
- CEKMGNTXNFQPIB-UHFFFAOYSA-N Cc(c(-c1ccn[n]1-c(cc1)ccc1C#N)c[n]1nc(NC(CCSC)=O)nc11)c1-c1cc(C(F)(F)F)ccc1 Chemical compound Cc(c(-c1ccn[n]1-c(cc1)ccc1C#N)c[n]1nc(NC(CCSC)=O)nc11)c1-c1cc(C(F)(F)F)ccc1 CEKMGNTXNFQPIB-UHFFFAOYSA-N 0.000 description 1
- ATUJAUNBXASJTJ-UHFFFAOYSA-N Cc(c(-c1ccn[n]1-c(cc1)ccc1N)c[n]1nc(NCCCCO)nc11)c1-c1cc(C(F)(F)F)ccc1 Chemical compound Cc(c(-c1ccn[n]1-c(cc1)ccc1N)c[n]1nc(NCCCCO)nc11)c1-c1cc(C(F)(F)F)ccc1 ATUJAUNBXASJTJ-UHFFFAOYSA-N 0.000 description 1
- YWSHCHGNLJLOJI-UHFFFAOYSA-N Cc(c(Br)c[n]1c2ncc1)c2-c1cc(C(F)(F)F)ccc1 Chemical compound Cc(c(Br)c[n]1c2ncc1)c2-c1cc(C(F)(F)F)ccc1 YWSHCHGNLJLOJI-UHFFFAOYSA-N 0.000 description 1
- MTMHQBUTTWCAJK-UHFFFAOYSA-N Cc(c(Br)c[n]1nc(NCCCSC)nc11)c1-c1cc(C(F)(F)F)ccc1 Chemical compound Cc(c(Br)c[n]1nc(NCCCSC)nc11)c1-c1cc(C(F)(F)F)ccc1 MTMHQBUTTWCAJK-UHFFFAOYSA-N 0.000 description 1
- UNUVSCZZIKWWRU-UHFFFAOYSA-N Cc(c(Br)c[n]1ncnc11)c1-c1cc(C(F)(F)F)ccc1 Chemical compound Cc(c(Br)c[n]1ncnc11)c1-c1cc(C(F)(F)F)ccc1 UNUVSCZZIKWWRU-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/4196—1,2,4-Triazoles
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pulmonology (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12176079.7 | 2012-07-12 | ||
| EP12176079 | 2012-07-12 | ||
| EP13158756.0 | 2013-03-12 | ||
| EP13158756 | 2013-03-12 | ||
| PCT/EP2013/064603 WO2014009425A1 (en) | 2012-07-12 | 2013-07-10 | Inhibition of enzymes |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104428300A CN104428300A (zh) | 2015-03-18 |
| CN104428300B true CN104428300B (zh) | 2016-11-09 |
Family
ID=48953361
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380036973.4A Expired - Fee Related CN104428300B (zh) | 2012-07-12 | 2013-07-10 | 酶的抑制 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9199984B2 (enExample) |
| EP (1) | EP2872509B1 (enExample) |
| KR (1) | KR20150031318A (enExample) |
| CN (1) | CN104428300B (enExample) |
| AR (1) | AR091737A1 (enExample) |
| BR (1) | BR112015000507A2 (enExample) |
| CA (1) | CA2878792A1 (enExample) |
| IN (1) | IN2015DN00202A (enExample) |
| RU (1) | RU2638537C2 (enExample) |
| WO (1) | WO2014009425A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2933725A1 (en) | 2013-12-16 | 2015-06-25 | Chiesi Farmaceutici S.P.A. | Tetrahydrotriazolopyrimidine derivatives as human neutrophil elastase inhibitors |
| US9487528B2 (en) | 2014-06-09 | 2016-11-08 | Chiesi Farmaceutici S.P.A. | Compounds |
| US9440930B2 (en) | 2014-07-31 | 2016-09-13 | Boehringer Ingelheim International Gmbh | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| US9475779B2 (en) | 2014-07-31 | 2016-10-25 | Boehringer Ingelheim International Gmbh | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| US9657015B2 (en) | 2014-07-31 | 2017-05-23 | Boehringer Ingelheim International Gmbh | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| US9409870B2 (en) * | 2014-12-15 | 2016-08-09 | Chiesi Farmaceutici S.P.A. | Compounds |
| AR108609A1 (es) * | 2016-05-31 | 2018-09-05 | Chiesi Farm Spa | Derivados de imidazolona y pirazolona como inhibidores de la elastasa de neutrófilos humana (hne) |
| BR112018074608B1 (pt) * | 2016-05-31 | 2024-01-23 | Chiesi Farmaceutici S.P.A | Composto, composição farmacêutica e uso de um composto |
| WO2017207432A1 (en) * | 2016-05-31 | 2017-12-07 | Chiesi Farmaceutici S.P.A. | Novel compounds |
| US11106356B2 (en) | 2017-02-27 | 2021-08-31 | Géza Bálint | Smart device with a display that enables simultaneous multi-functional handling of the displayed information and/or data |
| CN118496198A (zh) | 2019-07-23 | 2024-08-16 | 拜耳公司 | 作为农药的新的杂芳基-三唑化合物 |
| PH12022550166A1 (en) | 2019-07-23 | 2022-11-14 | Bayer Ag | Novel heteroaryl-triazole compounds as pesticides |
| 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 |
| DK4041721T3 (da) | 2019-10-09 | 2024-05-27 | Bayer Ag | Hidtil ukendte heteroaryltriazolforbindelser som pesticider |
| TW202128664A (zh) | 2019-10-09 | 2021-08-01 | 德商拜耳廠股份有限公司 | 作為除害劑之新穎雜芳基三唑化合物 |
| US20230117470A1 (en) * | 2019-11-01 | 2023-04-20 | Bristol-Myers Squibb Company | Substituted pyrazole compounds as toll receptor inhibitors |
| TW202134226A (zh) | 2019-11-18 | 2021-09-16 | 德商拜耳廠股份有限公司 | 作為殺蟲劑之新穎雜芳基-三唑化合物 |
| ES2962498T3 (es) | 2020-04-16 | 2024-03-19 | Mereo Biopharma 4 Ltd | Métodos que implican el inhibidor de elastasa de neutrófilos alvelestat para el tratamiento de enfermedades respiratorias mediadas por deficiencia de alfa-1 antitripsina |
| JP2023542789A (ja) * | 2020-09-28 | 2023-10-12 | シチュアン ケルン-バイオテック バイオファーマシューティカル カンパニー リミテッド | ピラゾール化合物並びにその調製方法及び使用 |
| CN113480486B (zh) * | 2021-07-30 | 2022-05-24 | 赣南师范大学 | 一种3-胺基-1,2,4-三唑类衍生物及其制备方法和应用 |
| KR20240090272A (ko) | 2021-10-20 | 2024-06-21 | 메레오 바이오파마 4 리미티드 | 섬유화 치료에 사용하기 위한 호중구 엘라스테이스 억제제 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011039528A1 (en) * | 2009-10-02 | 2011-04-07 | Astrazeneca Ab | 2-pyridone compounds used as inhibitors of neutrophil elastase |
| CN102131805A (zh) * | 2008-06-20 | 2011-07-20 | 百时美施贵宝公司 | 用作激酶抑制剂的咪唑并吡啶和咪唑并吡嗪化合物 |
| US20120004203A1 (en) * | 2009-01-09 | 2012-01-05 | Bayer Schering Pharma Aktiengesellschaft | Triazolo and tetrazolo pyrimidine derivatives as hne inhibitors for treating copd |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4259504A (en) | 1979-08-27 | 1981-03-31 | American Cyanamid Company | Substituted 1H-1,2,4-triazoles |
| US4451471A (en) | 1981-03-18 | 1984-05-29 | Ciba-Geigy Corporation | Certain 2,4,5-tri-substituted thiazoles, pharmaceutical compositions containing same and methods of using same |
| US4576958A (en) | 1984-01-23 | 1986-03-18 | E. I. Du Pont De Nemours And Company | Antihypertensive 4,5-diaryl-1H-imidazole-2-methanol derivatives |
| AU650953B2 (en) | 1991-03-21 | 1994-07-07 | Novartis Ag | Inhaler |
| ES2184633B1 (es) | 2001-08-07 | 2004-08-01 | J. URIACH & CIA, S.A. | Procedimiento para la preparacion de derivados de 4-(imidazol-1-il) bencenosulfonamida. |
| US6693116B2 (en) * | 2001-10-08 | 2004-02-17 | Hoffmann-La Roche Inc. | Adenosine receptor ligands |
| WO2006038116A2 (en) | 2004-10-07 | 2006-04-13 | Warner-Lambert Company Llc | Triazolopyridine derivatives as antibacterial agents |
| US7902374B2 (en) | 2005-05-06 | 2011-03-08 | Universal Display Corporation | Stability OLED materials and devices |
| WO2007139952A2 (en) | 2006-05-25 | 2007-12-06 | Synta Pharmaceuticals Corp. | Method for the preparation of triazole compounds with hsp90 modulating activity |
| EA017297B1 (ru) * | 2007-11-06 | 2012-11-30 | Астразенека Аб | Некоторые производные 2-пиразинона и их применение в качестве ингибиторов нейтрофильной эластазы |
| PE20091953A1 (es) | 2008-05-08 | 2010-01-09 | Du Pont | Azoles sustituidos como fungicidas |
| US8410128B2 (en) * | 2008-06-20 | 2013-04-02 | Bristol-Myers Squibb Company | Triazolopyridine compounds useful as kinase inhibitors |
-
2013
- 2013-07-10 BR BR112015000507A patent/BR112015000507A2/pt not_active IP Right Cessation
- 2013-07-10 CA CA2878792A patent/CA2878792A1/en not_active Abandoned
- 2013-07-10 RU RU2015104644A patent/RU2638537C2/ru not_active IP Right Cessation
- 2013-07-10 CN CN201380036973.4A patent/CN104428300B/zh not_active Expired - Fee Related
- 2013-07-10 EP EP13747801.2A patent/EP2872509B1/en active Active
- 2013-07-10 IN IN202DEN2015 patent/IN2015DN00202A/en unknown
- 2013-07-10 KR KR20157002129A patent/KR20150031318A/ko not_active Withdrawn
- 2013-07-10 WO PCT/EP2013/064603 patent/WO2014009425A1/en not_active Ceased
- 2013-07-11 AR ARP130102470 patent/AR091737A1/es unknown
- 2013-07-12 US US13/940,555 patent/US9199984B2/en not_active Expired - Fee Related
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102131805A (zh) * | 2008-06-20 | 2011-07-20 | 百时美施贵宝公司 | 用作激酶抑制剂的咪唑并吡啶和咪唑并吡嗪化合物 |
| US20120004203A1 (en) * | 2009-01-09 | 2012-01-05 | Bayer Schering Pharma Aktiengesellschaft | Triazolo and tetrazolo pyrimidine derivatives as hne inhibitors for treating copd |
| WO2011039528A1 (en) * | 2009-10-02 | 2011-04-07 | Astrazeneca Ab | 2-pyridone compounds used as inhibitors of neutrophil elastase |
Also Published As
| Publication number | Publication date |
|---|---|
| RU2015104644A (ru) | 2016-08-27 |
| AR091737A1 (es) | 2015-02-25 |
| WO2014009425A1 (en) | 2014-01-16 |
| KR20150031318A (ko) | 2015-03-23 |
| EP2872509A1 (en) | 2015-05-20 |
| IN2015DN00202A (enExample) | 2015-06-12 |
| CN104428300A (zh) | 2015-03-18 |
| EP2872509B1 (en) | 2016-09-14 |
| US20140018345A1 (en) | 2014-01-16 |
| CA2878792A1 (en) | 2014-01-16 |
| BR112015000507A2 (pt) | 2017-06-27 |
| US9199984B2 (en) | 2015-12-01 |
| RU2638537C2 (ru) | 2017-12-14 |
| HK1207078A1 (en) | 2016-01-22 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN104428300B (zh) | 酶的抑制 | |
| AU2022201816B2 (en) | Pyrrolopyrimidines as CFTR potentiators | |
| AU2024227155A1 (en) | Carboxy-benzimidazole GLP-1R modulating compounds. | |
| CN103958500B (zh) | 蛋白激酶抑制剂 | |
| CN102821607B (zh) | 1H-吡唑并[3,4-b]吡啶及其治疗应用 | |
| US20110034441A1 (en) | Indazoles as wnt/b-catenin signaling pathway inhibitors and therapeutic uses thereof | |
| CA3047002A1 (en) | Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase | |
| TW201609733A (zh) | 新穎化合物 | |
| HK1207078B (en) | Inhibition of enzymes | |
| HK40014108A (en) | Pyrrolopyrimidines as cftr potentiators | |
| HK40014108B (en) | Pyrrolopyrimidines as cftr potentiators |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| REG | Reference to a national code |
Ref country code: HK Ref legal event code: DE Ref document number: 1207078 Country of ref document: HK |
|
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| REG | Reference to a national code |
Ref country code: HK Ref legal event code: GR Ref document number: 1207078 Country of ref document: HK |
|
| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20161109 Termination date: 20180710 |