GR3020814T3 - Method for making intermediates useful in synthesis of retroviral protease inhibitors. - Google Patents
Method for making intermediates useful in synthesis of retroviral protease inhibitors.Info
- Publication number
- GR3020814T3 GR3020814T3 GR960402048T GR960402048T GR3020814T3 GR 3020814 T3 GR3020814 T3 GR 3020814T3 GR 960402048 T GR960402048 T GR 960402048T GR 960402048 T GR960402048 T GR 960402048T GR 3020814 T3 GR3020814 T3 GR 3020814T3
- Authority
- GR
- Greece
- Prior art keywords
- substituted
- alkyl
- synthesis
- arylalkyl
- protease inhibitors
- Prior art date
Links
- 230000015572 biosynthetic process Effects 0.000 title abstract 2
- 239000000543 intermediate Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 238000003786 synthesis reaction Methods 0.000 title abstract 2
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 title 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 title 1
- 230000001177 retroviral effect Effects 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 3
- -1 epoxide compound Chemical class 0.000 abstract 3
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 abstract 2
- CLAHOZSYMRNIPY-UHFFFAOYSA-N 2-hydroxyethylurea Chemical compound NC(=O)NCCO CLAHOZSYMRNIPY-UHFFFAOYSA-N 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000006242 amine protecting group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 239000003153 chemical reaction reagent Substances 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 239000004030 hiv protease inhibitor Substances 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 229940031575 hydroxyethyl urea Drugs 0.000 abstract 1
- 125000002524 organometallic group Chemical group 0.000 abstract 1
- 125000001181 organosilyl group Chemical group [SiH3]* 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
- C07C213/02—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
- C07C213/08—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
- C07C275/04—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms
- C07C275/20—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
- C07C275/22—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings other than six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
- C07C275/04—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms
- C07C275/20—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
- C07C275/24—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
- C07D303/02—Compounds containing oxirane rings
- C07D303/36—Compounds containing oxirane rings with hydrocarbon radicals, substituted by nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Crystallography & Structural Chemistry (AREA)
- Molecular Biology (AREA)
- Health & Medical Sciences (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Epoxy Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US88655892A | 1992-05-20 | 1992-05-20 | |
| PCT/US1993/004804 WO1993023388A1 (en) | 1992-05-20 | 1993-05-20 | Method for making intermediates useful in synthesis of retroviral protease inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| GR3020814T3 true GR3020814T3 (en) | 1996-11-30 |
Family
ID=25389250
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GR960402048T GR3020814T3 (en) | 1992-05-20 | 1996-08-16 | Method for making intermediates useful in synthesis of retroviral protease inhibitors. |
Country Status (11)
| Country | Link |
|---|---|
| EP (1) | EP0641333B1 (el) |
| JP (3) | JP3492362B2 (el) |
| KR (1) | KR100290516B1 (el) |
| AT (1) | ATE141265T1 (el) |
| AU (2) | AU4253193A (el) |
| CA (1) | CA2131182C (el) |
| DE (1) | DE69304051T2 (el) |
| DK (1) | DK0641333T3 (el) |
| ES (1) | ES2091000T3 (el) |
| GR (1) | GR3020814T3 (el) |
| WO (2) | WO1993023368A1 (el) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040122000A1 (en) | 1981-01-07 | 2004-06-24 | Vertex Pharmaceuticals Incorporated. | Inhibitors of aspartyl protease |
| US6878728B1 (en) | 1999-06-11 | 2005-04-12 | Vertex Pharmaceutical Incorporated | Inhibitors of aspartyl protease |
| ATE218541T1 (de) | 1992-08-25 | 2002-06-15 | Searle & Co | Hydroxyethylaminosulfonamide verwendbar als inhibitoren retroviraler proteasen |
| US7141609B2 (en) | 1992-08-25 | 2006-11-28 | G.D. Searle & Co. | α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors |
| US5723490A (en) * | 1992-09-08 | 1998-03-03 | Vertex Pharmaceuticals Incorporated | THF-containing sulfonamide inhibitors of aspartyl protease |
| US5783701A (en) * | 1992-09-08 | 1998-07-21 | Vertex Pharmaceuticals, Incorporated | Sulfonamide inhibitors of aspartyl protease |
| IS2334B (is) * | 1992-09-08 | 2008-02-15 | Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) | Aspartyl próteasi hemjari af nýjum flokki súlfonamíða |
| ATE273700T1 (de) * | 1993-05-21 | 2004-09-15 | Us Gov Health & Human Serv | Neues verfahen zur hemmung der replication der virus - abhängigen reverse transciptase durch verwendung von dideoxydenucleotide-synthese inhibitoren |
| AU7518694A (en) * | 1993-08-20 | 1995-03-21 | G.D. Searle & Co. | Retroviral protease inhibitors and combinations thereof |
| US6093702A (en) * | 1993-12-20 | 2000-07-25 | The United States Of America As Represented By The Department Of Health And Human Services | Mixtures of dideoxy-nucleosides and hydroxycarbamide for inhibiting retroviral spread |
| JPH10500938A (ja) * | 1994-03-07 | 1998-01-27 | バーテックス ファーマシューティカルズ インコーポレイテッド | アスパラチルプロテアーゼインヒビターとしてのスルホンアミド誘導体 |
| US5475138A (en) * | 1994-07-07 | 1995-12-12 | Pharm-Eco Laboratories Incorporated | Method preparing amino acid-derived diaminopropanols |
| CA2137406C (en) * | 1994-12-06 | 2005-09-13 | Pierre Louis Beaulieu | Process for key intermediates for hiv protease inhibitors |
| US5481011A (en) * | 1994-12-13 | 1996-01-02 | Bristol-Myers Squibb Company | Process for preparing N-protected amino acid α-halomethyl ketones and alcohols from N-protected amino acid esters |
| US5831117A (en) | 1995-01-20 | 1998-11-03 | G. D. Searle & Co. | Method of preparing retroviral protease inhibitor intermediates |
| US6143747A (en) | 1995-01-20 | 2000-11-07 | G. D. Searle & Co. | Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors |
| US5693847A (en) * | 1995-04-19 | 1997-12-02 | Vertex Pharmaceuticals Incorporated | Heteroatom functionalized α-methyl ketones |
| US5691372A (en) * | 1995-04-19 | 1997-11-25 | Vertex Pharmaceuticals Incorporated | Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease |
| US6004957A (en) * | 1995-06-07 | 1999-12-21 | Vertex Pharmaceuticals, Incorporated | Sulfonamide inhibitors of aspartyl protease |
| US6037157A (en) | 1995-06-29 | 2000-03-14 | Abbott Laboratories | Method for improving pharmacokinetics |
| US6063963A (en) * | 1995-07-05 | 2000-05-16 | Pharm-Eco Laboratories, Inc. | Amino acid-derived diaminopropanols |
| PT861233E (pt) | 1995-11-16 | 2000-09-29 | Searle & Co | Beta-amino-hidroxissulfonatos n-protegidos/n-substituidos |
| US5767316A (en) | 1995-11-17 | 1998-06-16 | Ajinomoto Co., Inc. | Process for producing 3-amino-2-oxo-1-halogenopropane derivatives |
| US5914332A (en) | 1995-12-13 | 1999-06-22 | Abbott Laboratories | Retroviral protease inhibiting compounds |
| US5919956A (en) * | 1996-10-18 | 1999-07-06 | Roche Vitamins Inc. | Process for the C1 -homologization of protected phorenol |
| ZA9710071B (en) * | 1996-11-21 | 1998-05-25 | Abbott Lab | Pharmaceutical composition. |
| US6232333B1 (en) | 1996-11-21 | 2001-05-15 | Abbott Laboratories | Pharmaceutical composition |
| US6127556A (en) * | 1996-12-31 | 2000-10-03 | G. D. Searle & Co. | Epoxide formation by continuous in-situ synthesis process |
| US6436989B1 (en) | 1997-12-24 | 2002-08-20 | Vertex Pharmaceuticals, Incorporated | Prodrugs of aspartyl protease inhibitors |
| BR9912169A (pt) | 1998-06-19 | 2001-04-10 | Vertex Pharma | Inibidores de sulfonamida de protease de aspartil |
| DK2269591T3 (en) | 2000-01-19 | 2018-07-16 | Abbvie Inc | IMPROVED PHARMACEUTICAL FORMULATIONS |
| FR2820136A1 (fr) * | 2001-01-26 | 2002-08-02 | Aventis Pharma Sa | Nouveaux derives de l'uree, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilisation |
| FR2885129B1 (fr) | 2005-04-29 | 2007-06-15 | Proskelia Sas | Nouveaux derives de l'ureee substituee parun thiazole ou benzothiazole, leur procede de preparation, leur application a titre de medicaments, les compositions pharmaceutiques les renfermant et utilisation. |
| CA2630860A1 (en) | 2005-11-25 | 2007-05-31 | Galapagos Sas | Urea derivatives useful as calcium receptor modulators |
| CN101631568B (zh) | 2007-03-12 | 2012-08-22 | 尼克塔治疗公司 | 低聚物-蛋白酶抑制剂偶联物 |
| US9095620B2 (en) | 2008-03-12 | 2015-08-04 | Nektar Therapeutics | Reagents |
| JP2012530069A (ja) | 2009-06-12 | 2012-11-29 | ネクター セラピューティックス | プロテアーゼ阻害剤、水溶性非ペプチドオリゴマーおよび親油性部分を含む共有結合体 |
| CN112546969B (zh) * | 2020-12-07 | 2022-12-23 | 安徽贝克制药股份有限公司 | 催化加氢连续生产装置和利托那韦中间体的制备方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA1297631C (en) * | 1985-12-23 | 1992-03-17 | Sesha I. Natarajan | Ureido renin inhibitors |
| DE3635907A1 (de) * | 1986-10-22 | 1988-04-28 | Merck Patent Gmbh | Hydroxy-aminosaeurederivate |
| GB2200115B (en) * | 1987-01-21 | 1990-11-14 | Sandoz Ltd | Novel peptide derivatives, their production and use |
| USH725H (en) * | 1987-02-26 | 1990-01-02 | E. R. Squibb & Sons, Inc. | Ureido amino and imino acids, compositions and methods for use |
| DE3711911A1 (de) * | 1987-04-08 | 1988-10-20 | Bayer Ag | Optisch aktive (alpha)-aminoaldehyde, verfahren zu ihrer herstellung und ihre verwendung zur stereoselektiven herstellung optisch aktiver ss-aminoalkohole |
| EP0374097A3 (de) * | 1988-12-15 | 1991-06-12 | Ciba-Geigy Ag | Verwendung von Peptidisosteren als retrovirale Proteasehemmer |
| EP0813868B1 (en) * | 1990-11-19 | 2005-06-01 | Monsanto Company | Retroviral protease inhibitors |
-
1993
- 1993-05-20 WO PCT/US1993/004806 patent/WO1993023368A1/en not_active Ceased
- 1993-05-20 EP EP93911369A patent/EP0641333B1/en not_active Expired - Lifetime
- 1993-05-20 DK DK93911369.2T patent/DK0641333T3/da active
- 1993-05-20 AU AU42531/93A patent/AU4253193A/en not_active Abandoned
- 1993-05-20 AU AU42530/93A patent/AU676479B2/en not_active Ceased
- 1993-05-20 WO PCT/US1993/004804 patent/WO1993023388A1/en not_active Ceased
- 1993-05-20 JP JP50384794A patent/JP3492362B2/ja not_active Expired - Fee Related
- 1993-05-20 CA CA002131182A patent/CA2131182C/en not_active Expired - Fee Related
- 1993-05-20 ES ES93911369T patent/ES2091000T3/es not_active Expired - Lifetime
- 1993-05-20 AT AT93911369T patent/ATE141265T1/de not_active IP Right Cessation
- 1993-05-20 DE DE69304051T patent/DE69304051T2/de not_active Expired - Fee Related
- 1993-05-20 KR KR1019940703377A patent/KR100290516B1/ko not_active Expired - Fee Related
-
1996
- 1996-08-16 GR GR960402048T patent/GR3020814T3/el unknown
-
2002
- 2002-11-21 JP JP2002337346A patent/JP2003192648A/ja active Pending
- 2002-11-21 JP JP2002337347A patent/JP2003160545A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| WO1993023388A1 (en) | 1993-11-25 |
| DE69304051D1 (de) | 1996-09-19 |
| JP3492362B2 (ja) | 2004-02-03 |
| AU4253193A (en) | 1993-12-13 |
| EP0641333B1 (en) | 1996-08-14 |
| DK0641333T3 (da) | 1996-09-02 |
| ATE141265T1 (de) | 1996-08-15 |
| KR100290516B1 (ko) | 2001-09-17 |
| KR950700893A (ko) | 1995-02-20 |
| AU676479B2 (en) | 1997-03-13 |
| DE69304051T2 (de) | 1997-01-23 |
| AU4253093A (en) | 1993-12-13 |
| JP2003160545A (ja) | 2003-06-03 |
| EP0641333A1 (en) | 1995-03-08 |
| ES2091000T3 (es) | 1996-10-16 |
| WO1993023368A1 (en) | 1993-11-25 |
| CA2131182A1 (en) | 1993-11-25 |
| JPH07508041A (ja) | 1995-09-07 |
| JP2003192648A (ja) | 2003-07-09 |
| CA2131182C (en) | 2005-04-26 |
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