CN102176827B - 抗真菌制剂 - Google Patents
抗真菌制剂 Download PDFInfo
- Publication number
- CN102176827B CN102176827B CN200980140485.1A CN200980140485A CN102176827B CN 102176827 B CN102176827 B CN 102176827B CN 200980140485 A CN200980140485 A CN 200980140485A CN 102176827 B CN102176827 B CN 102176827B
- Authority
- CN
- China
- Prior art keywords
- mmol
- compound
- intermediate compound
- reaction
- added
- 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.)
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Links
- 0 *=*[n]1ncnc1-c1nnccc1 Chemical compound *=*[n]1ncnc1-c1nnccc1 0.000 description 29
- OKKPTYPQFAFGOT-MLCCFXAWSA-N CC(C)(C)[C@](C)(C1)N1S(c1ccc(C)cc1)(=O)=O Chemical compound CC(C)(C)[C@](C)(C1)N1S(c1ccc(C)cc1)(=O)=O OKKPTYPQFAFGOT-MLCCFXAWSA-N 0.000 description 1
- JMMIHGCIDBAMMW-VYRBHSGPSA-N CC(C)(C)[C@](C)(C1)N1[S@@](C)(c1ccc(C)cc1)O Chemical compound CC(C)(C)[C@](C)(C1)N1[S@@](C)(c1ccc(C)cc1)O JMMIHGCIDBAMMW-VYRBHSGPSA-N 0.000 description 1
- IPJUGSRSRYBXTA-UHFFFAOYSA-N CC(C)(C1)C(C)(C)OB1c1c[o]cc1 Chemical compound CC(C)(C1)C(C)(C)OB1c1c[o]cc1 IPJUGSRSRYBXTA-UHFFFAOYSA-N 0.000 description 1
- ZCSJZRUISUMERF-CNNPROEUSA-N CC(C)[C@@H](C)[C@@](C)(CC[C@](C)([C@H]1CC2)[C@@]3(C)CC=C1[C@](CC([C@@H](C1(C)C)OC[C@@](C)(C(C)C)N)[n]4nccc4C(N)=O)([C@H](C)O)[C@@]21N)[C@H]3C(O)=O Chemical compound CC(C)[C@@H](C)[C@@](C)(CC[C@](C)([C@H]1CC2)[C@@]3(C)CC=C1[C@](CC([C@@H](C1(C)C)OC[C@@](C)(C(C)C)N)[n]4nccc4C(N)=O)([C@H](C)O)[C@@]21N)[C@H]3C(O)=O ZCSJZRUISUMERF-CNNPROEUSA-N 0.000 description 1
- LUHOYIOMQYPHNU-KEHUTRCWSA-N CC(C)[C@@H](C)[C@@](C)(CC[C@](C)([C@H]1CC2)[C@@]3(C)CC=C1[C@](CC1[n](nc4C(N)=O)nc4N)([C@H](C)O)[C@@H]2C(C)(C)[C@H]1OC[C@@](C)(C(C)C)N)[C@H]3C(O)=O Chemical compound CC(C)[C@@H](C)[C@@](C)(CC[C@](C)([C@H]1CC2)[C@@]3(C)CC=C1[C@](CC1[n](nc4C(N)=O)nc4N)([C@H](C)O)[C@@H]2C(C)(C)[C@H]1OC[C@@](C)(C(C)C)N)[C@H]3C(O)=O LUHOYIOMQYPHNU-KEHUTRCWSA-N 0.000 description 1
- XWKRUKWXCQSRIO-NMJILFDFSA-N CC(C)[C@@H](C)[C@@](C)(CC[C@](C)([C@H]1CC2)[C@@]3(C)CC=C1[C@](C[C@H]1O)([C@H](C)O)[C@@H]2C(C)(C)[C@H]1O[C@@H](C(C)(C)C)N)[C@H]3C(O)=O Chemical compound CC(C)[C@@H](C)[C@@](C)(CC[C@](C)([C@H]1CC2)[C@@]3(C)CC=C1[C@](C[C@H]1O)([C@H](C)O)[C@@H]2C(C)(C)[C@H]1O[C@@H](C(C)(C)C)N)[C@H]3C(O)=O XWKRUKWXCQSRIO-NMJILFDFSA-N 0.000 description 1
- GXSBTOZTKSMCCW-NMIBEJMRSA-N CC(C)[C@@H](C)[C@@](C)(CC[C@](C)([C@H]1CC2)[C@@]3(C)CC=C1[C@](C[C@H]1[n]4ncnc4Br)([C@H](C)O)[C@@H]2C(C)(C)[C@H]1OCC1(CCOCC1)N)[C@H]3C(O)=O Chemical compound CC(C)[C@@H](C)[C@@](C)(CC[C@](C)([C@H]1CC2)[C@@]3(C)CC=C1[C@](C[C@H]1[n]4ncnc4Br)([C@H](C)O)[C@@H]2C(C)(C)[C@H]1OCC1(CCOCC1)N)[C@H]3C(O)=O GXSBTOZTKSMCCW-NMIBEJMRSA-N 0.000 description 1
- CGKPFYHZXUIMKN-ADGPQGAUSA-N CC(C)[C@@H](C)[C@@](C)(CC[C@](C)([C@H]1CC2)[C@@]3(C)CC=C1[C@](C[C@H]1[n]4ncnc4C#N)([C@H](C)OC4)[C@@H]2[C@]4(C)[C@H]1OC[C@@](C)(C(C)C)N)[C@H]3C(O)=O Chemical compound CC(C)[C@@H](C)[C@@](C)(CC[C@](C)([C@H]1CC2)[C@@]3(C)CC=C1[C@](C[C@H]1[n]4ncnc4C#N)([C@H](C)OC4)[C@@H]2[C@]4(C)[C@H]1OC[C@@](C)(C(C)C)N)[C@H]3C(O)=O CGKPFYHZXUIMKN-ADGPQGAUSA-N 0.000 description 1
- GXMZKSUWPJHWHY-UHFFFAOYSA-N CCC(c1n[nH]cc1)=O Chemical compound CCC(c1n[nH]cc1)=O GXMZKSUWPJHWHY-UHFFFAOYSA-N 0.000 description 1
- NHTKJBCNJJVEAN-YRNVUSSQSA-N CN(C)/C=N/C(c1ccncc1)=O Chemical compound CN(C)/C=N/C(c1ccncc1)=O NHTKJBCNJJVEAN-YRNVUSSQSA-N 0.000 description 1
- XTHROVVOMBQSJD-UHFFFAOYSA-N C[n]1ncnc1-c(ccnc1)c1F Chemical compound C[n]1ncnc1-c(ccnc1)c1F XTHROVVOMBQSJD-UHFFFAOYSA-N 0.000 description 1
- BUKHIOLKKWIACI-UHFFFAOYSA-N C[n]1ncnc1-c1c[nH]cn1 Chemical compound C[n]1ncnc1-c1c[nH]cn1 BUKHIOLKKWIACI-UHFFFAOYSA-N 0.000 description 1
- XRSSMBJTADRELB-UHFFFAOYSA-N C[n]1ncnc1-c1ccncc1 Chemical compound C[n]1ncnc1-c1ccncc1 XRSSMBJTADRELB-UHFFFAOYSA-N 0.000 description 1
- AFZPZXWXZLJGEX-UHFFFAOYSA-N C[n]1ncnc1-c1cnc[s]1 Chemical compound C[n]1ncnc1-c1cnc[s]1 AFZPZXWXZLJGEX-UHFFFAOYSA-N 0.000 description 1
- XHVVCVIGSLINKN-UHFFFAOYSA-N C[n]1ncnc1-c1cnccc1 Chemical compound C[n]1ncnc1-c1cnccc1 XHVVCVIGSLINKN-UHFFFAOYSA-N 0.000 description 1
- GCWZAPNPSHBILS-UHFFFAOYSA-N C[n]1ncnc1-c1cncnc1 Chemical compound C[n]1ncnc1-c1cncnc1 GCWZAPNPSHBILS-UHFFFAOYSA-N 0.000 description 1
- ADKKGTCEODQBAL-UHFFFAOYSA-N C[n]1ncnc1-c1cnncc1 Chemical compound C[n]1ncnc1-c1cnncc1 ADKKGTCEODQBAL-UHFFFAOYSA-N 0.000 description 1
- BTTNIGVWGUOKOM-UHFFFAOYSA-N C[n]1ncnc1-c1nccnc1 Chemical compound C[n]1ncnc1-c1nccnc1 BTTNIGVWGUOKOM-UHFFFAOYSA-N 0.000 description 1
- KNSLFGDZXYVILK-UHFFFAOYSA-N C[n]1ncnc1-c1ncncc1 Chemical compound C[n]1ncnc1-c1ncncc1 KNSLFGDZXYVILK-UHFFFAOYSA-N 0.000 description 1
- KSPVCDBCHFVORA-UHFFFAOYSA-N Cc(cc1)ccc1[S@](C)(N)O Chemical compound Cc(cc1)ccc1[S@](C)(N)O KSPVCDBCHFVORA-UHFFFAOYSA-N 0.000 description 1
- YGQJQEDHXMRPBB-UHFFFAOYSA-N Cc(cncc1)c1-c1ncn[n]1C Chemical compound Cc(cncc1)c1-c1ncn[n]1C YGQJQEDHXMRPBB-UHFFFAOYSA-N 0.000 description 1
- MNKBSXULTGYFFR-UHFFFAOYSA-N NC(c1c(N)nn[nH]1)=O Chemical compound NC(c1c(N)nn[nH]1)=O MNKBSXULTGYFFR-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0005—Oxygen-containing hetero ring
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/64—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with three nitrogen atoms as the only ring hetero atoms
- A01N43/647—Triazoles; Hydrogenated triazoles
- A01N43/653—1,2,4-Triazoles; Hydrogenated 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
-
- 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
-
- 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
- A61P31/10—Antimycotics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Dentistry (AREA)
- Environmental Sciences (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- Emergency Medicine (AREA)
- Engineering & Computer Science (AREA)
- Agronomy & Crop Science (AREA)
- Pest Control & Pesticides (AREA)
- Plant Pathology (AREA)
- Communicable Diseases (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Steroid Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510182454.XA CN104877001B (zh) | 2008-08-12 | 2009-08-07 | 抗真菌制剂 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13610108P | 2008-08-12 | 2008-08-12 | |
| US61/136,101 | 2008-08-12 | ||
| PCT/US2009/004560 WO2010019204A1 (en) | 2008-08-12 | 2009-08-07 | Antifungal agents |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510182454.XA Division CN104877001B (zh) | 2008-08-12 | 2009-08-07 | 抗真菌制剂 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102176827A CN102176827A (zh) | 2011-09-07 |
| CN102176827B true CN102176827B (zh) | 2015-05-20 |
Family
ID=41669133
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510182454.XA Active CN104877001B (zh) | 2008-08-12 | 2009-08-07 | 抗真菌制剂 |
| CN200980140485.1A Active CN102176827B (zh) | 2008-08-12 | 2009-08-07 | 抗真菌制剂 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510182454.XA Active CN104877001B (zh) | 2008-08-12 | 2009-08-07 | 抗真菌制剂 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US8188085B2 (enExample) |
| EP (1) | EP2326181A4 (enExample) |
| JP (1) | JP5548875B2 (enExample) |
| CN (2) | CN104877001B (enExample) |
| AU (1) | AU2009282474B2 (enExample) |
| CA (1) | CA2731941C (enExample) |
| WO (1) | WO2010019204A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103180301B (zh) | 2010-08-26 | 2015-11-25 | 拜耳知识产权有限责任公司 | 5-碘代三唑衍生物 |
| DK3247711T3 (da) | 2015-01-19 | 2022-05-09 | Scynexis Inc | Hidtil ukendte salte og polymorfer af scy-078 |
| KR20240110109A (ko) | 2017-04-10 | 2024-07-12 | 싸이넥시스, 인크. | 조합하여 사용되는 항진균제 |
| WO2019028034A1 (en) | 2017-08-04 | 2019-02-07 | Scynexis, Inc. | Antifungal agents with enhanced activity in acidic ph |
| BR112020013448A2 (pt) * | 2018-01-02 | 2020-12-01 | Scynexis, Inc. | composição injetável, métodos para tratar uma infecção fúngica e para preparar uma composição injetável. |
| US12053486B2 (en) | 2018-03-09 | 2024-08-06 | Therazure LLC | Compositions for the treatment of infections in feet |
| WO2020160316A1 (en) | 2019-01-30 | 2020-08-06 | Scynexis, Inc. | Triterpenoid antifungals for the treatment of fungal osteo-articular infections |
| JP7581219B2 (ja) | 2019-02-27 | 2024-11-12 | サイネクシス，インコーポレーテッド | ニューモシスチス属種（Ｐｎｅｕｍｏｃｙｓｔｉｓ ｓｐｐ．）肺炎を治療又は予防するためのトリテルペノイド系抗真菌薬 |
| WO2020232037A1 (en) | 2019-05-16 | 2020-11-19 | Scynexis, Inc. | Antifungal agents, like ibrexafungerp for candida auris decolonization |
| WO2021092349A1 (en) | 2019-11-08 | 2021-05-14 | Scynexis, Inc. | Lipid-based formulations of scy-078 salts |
| US20220409651A1 (en) * | 2019-11-15 | 2022-12-29 | The Research Foundation For The State University Of New York | Anti-fungal compositions and methods for using same |
| CN118724779B (zh) * | 2024-06-05 | 2025-09-23 | 浙江瑞博制药有限公司 | 一种醛基化合物的制备方法 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6960600B2 (en) * | 2001-05-04 | 2005-11-01 | Aventis Pharma S.A. | Azole or triazole derivatives, method for preparing the same and use thereof as antifungal medicaments |
| US7230023B2 (en) * | 2001-02-22 | 2007-06-12 | Sankyo Company, Limited | Water-soluble triazole fungicide |
| US20080009504A1 (en) * | 2006-04-03 | 2008-01-10 | Balkovec James M | Antifungal agents |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3834062B2 (ja) | 1996-01-31 | 2006-10-18 | メルク エンド カンパニー インコーポレーテッド | 抗真菌剤 |
| US5756472A (en) | 1996-01-31 | 1998-05-26 | Merck & Co., Inc. | Antifungal agent obtained from hormonema |
| AU2002253456A1 (en) | 2002-04-17 | 2003-10-27 | Ranbaxy Laboratories Limited | Azole derivatives as antifungal agents |
-
2009
- 2009-08-07 US US12/461,318 patent/US8188085B2/en active Active
- 2009-08-07 AU AU2009282474A patent/AU2009282474B2/en active Active
- 2009-08-07 CA CA2731941A patent/CA2731941C/en active Active
- 2009-08-07 WO PCT/US2009/004560 patent/WO2010019204A1/en not_active Ceased
- 2009-08-07 JP JP2011522975A patent/JP5548875B2/ja active Active
- 2009-08-07 EP EP09806945A patent/EP2326181A4/en not_active Withdrawn
- 2009-08-07 CN CN201510182454.XA patent/CN104877001B/zh active Active
- 2009-08-07 CN CN200980140485.1A patent/CN102176827B/zh active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7230023B2 (en) * | 2001-02-22 | 2007-06-12 | Sankyo Company, Limited | Water-soluble triazole fungicide |
| US6960600B2 (en) * | 2001-05-04 | 2005-11-01 | Aventis Pharma S.A. | Azole or triazole derivatives, method for preparing the same and use thereof as antifungal medicaments |
| US20080009504A1 (en) * | 2006-04-03 | 2008-01-10 | Balkovec James M | Antifungal agents |
Non-Patent Citations (1)
| Title |
|---|
| 唑类抗真菌药物结构修饰的研发进展;王思袭等;《中国医药工业杂志》;20071231;第38卷(第1期) * |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2009282474B2 (en) | 2014-03-20 |
| WO2010019204A1 (en) | 2010-02-18 |
| CA2731941A1 (en) | 2010-02-18 |
| CA2731941C (en) | 2016-09-27 |
| EP2326181A4 (en) | 2012-11-28 |
| CN102176827A (zh) | 2011-09-07 |
| EP2326181A1 (en) | 2011-06-01 |
| US8188085B2 (en) | 2012-05-29 |
| HK1214271A1 (zh) | 2016-07-22 |
| JP5548875B2 (ja) | 2014-07-16 |
| CN104877001A (zh) | 2015-09-02 |
| AU2009282474A1 (en) | 2010-02-18 |
| US20100113439A1 (en) | 2010-05-06 |
| JP2011530593A (ja) | 2011-12-22 |
| CN104877001B (zh) | 2020-07-03 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| ASS | Succession or assignment of patent right |
Free format text: FORMER OWNER: SCYNEXIS INC. Effective date: 20140911 Owner name: SCYNEXIS INC. Free format text: FORMER OWNER: MERCK + CO. INC Effective date: 20140911 |
|
| C41 | Transfer of patent application or patent right or utility model | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20140911 Address after: North Carolina Applicant after: Scynexis Inc. Address before: new jersey Applicant before: Merck Sharp & Dohme Applicant before: Scynexis Inc. |
|
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant |