DK0871454T3 - Phosphorholdige inhibitorer af cystein- og serinprotease - Google Patents
Phosphorholdige inhibitorer af cystein- og serinproteaseInfo
- Publication number
- DK0871454T3 DK0871454T3 DK96923756T DK96923756T DK0871454T3 DK 0871454 T3 DK0871454 T3 DK 0871454T3 DK 96923756 T DK96923756 T DK 96923756T DK 96923756 T DK96923756 T DK 96923756T DK 0871454 T3 DK0871454 T3 DK 0871454T3
- Authority
- DK
- Denmark
- Prior art keywords
- cysteine
- phosphorus
- serine protease
- containing inhibitors
- inhibitors
- Prior art date
Links
- 102000005927 Cysteine Proteases Human genes 0.000 title abstract 2
- 108010005843 Cysteine Proteases Proteins 0.000 title abstract 2
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 title abstract 2
- 102000012479 Serine Proteases Human genes 0.000 title abstract 2
- 108010022999 Serine Proteases Proteins 0.000 title abstract 2
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 title abstract 2
- 235000018417 cysteine Nutrition 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 title 1
- 229910052698 phosphorus Inorganic materials 0.000 title 1
- 239000011574 phosphorus Substances 0.000 title 1
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 abstract 1
- BHEPBYXIRTUNPN-UHFFFAOYSA-N hydridophosphorus(.) (triplet) Chemical compound [PH] BHEPBYXIRTUNPN-UHFFFAOYSA-N 0.000 abstract 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/08—Esters of oxyacids of phosphorus
- C07F9/09—Esters of phosphoric acids
- C07F9/091—Esters of phosphoric acids with hydroxyalkyl compounds with further substituents on alkyl
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
- C07F9/32—Esters thereof
- C07F9/3205—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
- C07F9/3211—Esters of acyclic saturated acids which can have further substituents on alkyl
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
- C07F9/32—Esters thereof
- C07F9/3205—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
- C07F9/3247—Esters of acids containing the structure -C(=X)-P(=X)(R)(XH) or NC-P(=X)(R)(XH), (X = O, S, Se)
- C07F9/3252—Esters of acids containing the structure -C(=X)-P(=X)(R)(XH) or NC-P(=X)(R)(XH), (X = O, S, Se) containing the structure -C(=X)-P(=X)(R)(XR), (X = O, S, Se)
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
- C07F9/32—Esters thereof
- C07F9/3258—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
- C07F9/3264—Esters with hydroxyalkyl compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
- C07F9/40—Esters thereof
- C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
- C07F9/4006—Esters of acyclic acids which can have further substituents on alkyl
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
- C07F9/40—Esters thereof
- C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
- C07F9/4062—Esters of acids containing the structure -C(=X)-P(=X)(XR)2 or NC-P(=X)(XR)2, (X = O, S, Se)
- C07F9/4065—Esters of acids containing the structure -C(=X)-P(=X)(XR)2, (X = O, S, Se)
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
- C07F9/40—Esters thereof
- C07F9/4071—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
- C07F9/4075—Esters with hydroxyalkyl compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/572—Five-membered rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6527—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms
- C07F9/6533—Six-membered rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
- C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
- C07F9/657163—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
- C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
- C07F9/6574—Esters of oxyacids of phosphorus
- C07F9/65742—Esters of oxyacids of phosphorus non-condensed with carbocyclic rings or heterocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biochemistry (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Crystallography & Structural Chemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Medicinal Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Cosmetics (AREA)
- Detergent Compositions (AREA)
- Enzymes And Modification Thereof (AREA)
- Peptides Or Proteins (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US149195P | 1995-07-17 | 1995-07-17 | |
| US08/679,342 US5639732A (en) | 1996-07-10 | 1996-07-10 | Phosphorous-containing cysteine and serine protease inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK0871454T3 true DK0871454T3 (da) | 2004-03-22 |
Family
ID=26669094
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK96923756T DK0871454T3 (da) | 1995-07-17 | 1996-07-12 | Phosphorholdige inhibitorer af cystein- og serinprotease |
Country Status (10)
| Country | Link |
|---|---|
| EP (1) | EP0871454B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JPH11509231A (cg-RX-API-DMAC7.html) |
| AT (1) | ATE253920T1 (cg-RX-API-DMAC7.html) |
| AU (1) | AU6458396A (cg-RX-API-DMAC7.html) |
| CA (1) | CA2226414A1 (cg-RX-API-DMAC7.html) |
| DE (1) | DE69630701T2 (cg-RX-API-DMAC7.html) |
| DK (1) | DK0871454T3 (cg-RX-API-DMAC7.html) |
| ES (1) | ES2210377T3 (cg-RX-API-DMAC7.html) |
| PT (1) | PT871454E (cg-RX-API-DMAC7.html) |
| WO (1) | WO1997003679A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2002514192A (ja) * | 1996-11-13 | 2002-05-14 | セフアロン・インコーポレーテツド | ベンゾチアゾおよび関連の複素環基を含有するシステインおよびセリンプロテアーゼ阻害剤 |
| US6312662B1 (en) | 1998-03-06 | 2001-11-06 | Metabasis Therapeutics, Inc. | Prodrugs phosphorus-containing compounds |
| CA2322487C (en) * | 1998-03-06 | 2010-07-20 | Metabasis Therapeutics, Inc. | Novel prodrugs for phosphorus-containing compounds |
| WO2000051624A2 (en) | 1999-03-05 | 2000-09-08 | The Trustees Of University Technology Corporation | Methods and compositions useful in inhibiting apoptosis |
| WO2000051623A2 (en) | 1999-03-05 | 2000-09-08 | The Trustees Of University Technology Corporation | Inhibitors of serine protease activity, methods and compositions for treatment of nitric oxide-induced clinical conditions |
| US7205404B1 (en) | 1999-03-05 | 2007-04-17 | Metabasis Therapeutics, Inc. | Phosphorus-containing prodrugs |
| WO2000055124A2 (en) * | 1999-03-15 | 2000-09-21 | Axys Pharmaceuticals, Inc. | Novel compounds and compositions as protease inhibitors |
| US7030116B2 (en) | 2000-12-22 | 2006-04-18 | Aventis Pharmaceuticals Inc. | Compounds and compositions as cathepsin inhibitors |
| IL156577A0 (en) | 2000-12-22 | 2004-01-04 | Axys Pharm Inc | Selective cathepsin s inhibitors and pharmaceutical compositions containing the same |
| KR20040044920A (ko) | 2001-09-14 | 2004-05-31 | 아벤티스 파마슈티칼스 인크. | 카뎁신 억제제로서 신규한 화합물 및 조성물 |
| US7459461B2 (en) | 2001-10-19 | 2008-12-02 | Ortho-Mcneil Pharmaceutical, Inc. | Phosphonic acid compounds as inhibitors of serine proteases |
| MXPA04003707A (es) * | 2001-10-19 | 2005-04-08 | Johnson & Johnson | Compuestos de acido fosforico como inhibidores de serina proteasas. |
| PL372105A1 (en) | 2001-11-14 | 2005-07-11 | Aventis Pharmaceuticals Inc. | Oligopeptides and compositions containing them as cathepsin s inhibitors |
| CA2485597C (en) | 2002-05-13 | 2013-07-02 | Metabasis Therapeutics, Inc. | Process for preparation of cyclic prodrugs of pmea and pmpa |
| NZ536328A (en) | 2002-05-13 | 2007-11-30 | Metabasis Therapeutics Inc | Novel phosphonic acid based prodrugs of PMEA and its analogues |
| EP1556393B1 (en) | 2002-10-31 | 2013-12-25 | Metabasis Therapeutics, Inc. | Novel cyclic phosphate diesters of 1,3-propane-1-aryl diols and their use in preparing prodrugs |
| ES2622522T3 (es) | 2003-08-26 | 2017-07-06 | The Regents Of The University Of Colorado, A Body Corporate | Inhibidores de la actividad proteasa de serina y su uso en métodos y composiciones para el tratamiento de infecciones bacterianas |
| EP1753762B1 (en) | 2004-06-08 | 2014-03-19 | Metabasis Therapeutics, Inc. | Lewis acid mediated synthesis of cyclic esters |
| CA2937548C (en) | 2014-02-13 | 2022-10-25 | Ligand Pharmaceuticals, Inc. | Prodrug compounds and their uses |
| WO2016003812A1 (en) | 2014-07-02 | 2016-01-07 | Ligand Pharmaceuticals, Inc. | Prodrug compounds and uses therof |
| RU2020126177A (ru) | 2018-01-09 | 2022-02-10 | Лиганд Фармасьютикалз, Инк. | Ацетальные соединения и их терапевтическое применение |
| CN113354679A (zh) * | 2021-07-05 | 2021-09-07 | 南京恒远科技开发有限公司 | 一种二硬脂酰磷脂酰甘油钠的制备工艺 |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK0644197T3 (da) * | 1993-06-04 | 1999-06-07 | Vertex Pharma | Peptidphosphinyloxymethylketoner som inhibitorer af interleukin-1beta-konverterende enzymer |
-
1996
- 1996-07-12 DK DK96923756T patent/DK0871454T3/da active
- 1996-07-12 WO PCT/US1996/011625 patent/WO1997003679A1/en not_active Ceased
- 1996-07-12 JP JP9506762A patent/JPH11509231A/ja not_active Ceased
- 1996-07-12 DE DE69630701T patent/DE69630701T2/de not_active Expired - Lifetime
- 1996-07-12 PT PT96923756T patent/PT871454E/pt unknown
- 1996-07-12 CA CA002226414A patent/CA2226414A1/en not_active Abandoned
- 1996-07-12 AU AU64583/96A patent/AU6458396A/en not_active Abandoned
- 1996-07-12 ES ES96923756T patent/ES2210377T3/es not_active Expired - Lifetime
- 1996-07-12 AT AT96923756T patent/ATE253920T1/de not_active IP Right Cessation
- 1996-07-12 EP EP96923756A patent/EP0871454B1/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| JPH11509231A (ja) | 1999-08-17 |
| ES2210377T3 (es) | 2004-07-01 |
| DE69630701D1 (de) | 2003-12-18 |
| PT871454E (pt) | 2004-03-31 |
| HK1016495A1 (en) | 1999-11-05 |
| ATE253920T1 (de) | 2003-11-15 |
| WO1997003679A1 (en) | 1997-02-06 |
| CA2226414A1 (en) | 1997-02-06 |
| DE69630701T2 (de) | 2004-08-19 |
| EP0871454A4 (cg-RX-API-DMAC7.html) | 1998-11-25 |
| AU6458396A (en) | 1997-02-18 |
| EP0871454B1 (en) | 2003-11-12 |
| EP0871454A1 (en) | 1998-10-21 |
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