DE69304051T2 - Verfahren zur herstellung von intermediaten in der synthese von retroviralen protease inhibitoren - Google Patents
Verfahren zur herstellung von intermediaten in der synthese von retroviralen protease inhibitorenInfo
- Publication number
- DE69304051T2 DE69304051T2 DE69304051T DE69304051T DE69304051T2 DE 69304051 T2 DE69304051 T2 DE 69304051T2 DE 69304051 T DE69304051 T DE 69304051T DE 69304051 T DE69304051 T DE 69304051T DE 69304051 T2 DE69304051 T2 DE 69304051T2
- Authority
- DE
- Germany
- Prior art keywords
- substituted
- alkyl
- arylalkyl
- synthesis
- protease inhibitors
- 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
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)
- Crystallography & Structural Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Medicinal Chemistry (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (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)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (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 (2)
Publication Number | Publication Date |
---|---|
DE69304051D1 DE69304051D1 (de) | 1996-09-19 |
DE69304051T2 true DE69304051T2 (de) | 1997-01-23 |
Family
ID=25389250
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DE69304051T Expired - Fee Related DE69304051T2 (de) | 1992-05-20 | 1993-05-20 | Verfahren zur herstellung von intermediaten in der synthese von retroviralen protease inhibitoren |
Country Status (11)
Country | Link |
---|---|
EP (1) | EP0641333B1 (de) |
JP (3) | JP3492362B2 (de) |
KR (1) | KR100290516B1 (de) |
AT (1) | ATE141265T1 (de) |
AU (2) | AU4253193A (de) |
CA (1) | CA2131182C (de) |
DE (1) | DE69304051T2 (de) |
DK (1) | DK0641333T3 (de) |
ES (1) | ES2091000T3 (de) |
GR (1) | GR3020814T3 (de) |
WO (2) | WO1993023368A1 (de) |
Families Citing this family (38)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6878728B1 (en) | 1999-06-11 | 2005-04-12 | Vertex Pharmaceutical Incorporated | Inhibitors of aspartyl protease |
US20040122000A1 (en) | 1981-01-07 | 2004-06-24 | Vertex Pharmaceuticals Incorporated. | Inhibitors of aspartyl protease |
US5843946A (en) | 1992-08-25 | 1998-12-01 | G.D. Searle & Co. | α-and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors |
US7141609B2 (en) | 1992-08-25 | 2006-11-28 | G.D. Searle & Co. | α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors |
US5783701A (en) | 1992-09-08 | 1998-07-21 | Vertex Pharmaceuticals, Incorporated | Sulfonamide inhibitors of aspartyl protease |
US5723490A (en) * | 1992-09-08 | 1998-03-03 | Vertex Pharmaceuticals Incorporated | THF-containing 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 |
AU699483B2 (en) * | 1994-03-07 | 1998-12-03 | Vertex Pharmaceuticals Incorporated | Sulphonamide derivatives as aspartyl protease inhibitors |
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 |
ES2303337T3 (es) | 1995-01-20 | 2008-08-01 | G.D. Searle Llc | Inhibidores de la proteasa retroviral de bis-hidroxietilamino sulfonamida. |
US5831117A (en) | 1995-01-20 | 1998-11-03 | G. D. Searle & Co. | Method of preparing retroviral protease inhibitor intermediates |
US5691372A (en) * | 1995-04-19 | 1997-11-25 | Vertex Pharmaceuticals Incorporated | Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease |
US5693847A (en) * | 1995-04-19 | 1997-12-02 | Vertex Pharmaceuticals Incorporated | Heteroatom functionalized α-methyl ketones |
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 |
EP0774453B1 (de) | 1995-11-17 | 2002-02-06 | Ajinomoto Co., Inc. | Verfahren zur Herstellung von 3-Amino-2-oxo-1-Halogenpropan-Derivaten |
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 |
US6232333B1 (en) | 1996-11-21 | 2001-05-15 | Abbott Laboratories | Pharmaceutical composition |
ZA9710071B (en) * | 1996-11-21 | 1998-05-25 | Abbott Lab | 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 |
WO1999065870A2 (en) | 1998-06-19 | 1999-12-23 | Vertex Pharmaceuticals Incorporated | Sulfonamide inhibitors of aspartyl protease |
BR0011864A (pt) | 2000-01-19 | 2004-07-20 | Abbott Lab | Formulações farmacêuticas |
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. |
DE602006010905D1 (de) | 2005-11-25 | 2010-01-14 | Galapagos Sas | Harnstoff-derivate als calcium-rezeptor-modulatoren |
AU2008226823B2 (en) | 2007-03-12 | 2014-03-13 | Nektar Therapeutics | Oligomer-protease inhibitor conjugates |
US9095620B2 (en) | 2008-03-12 | 2015-08-04 | Nektar Therapeutics | Reagents |
EP2440249A2 (de) | 2009-06-12 | 2012-04-18 | Nektar Therapeutics | Kovalente konjugate mit einem protease-inhibitor, einem wasserlöslichen nicht-peptidischen oligomer und einem lipophilen teil |
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 |
CH676988A5 (de) * | 1987-01-21 | 1991-03-28 | Sandoz Ag | |
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 |
WO1992008701A1 (en) * | 1990-11-19 | 1992-05-29 | Monsanto Company | Retroviral protease inhibitors |
-
1993
- 1993-05-20 EP EP93911369A patent/EP0641333B1/de 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 IP Right Cessation
- 1993-05-20 DK DK93911369.2T patent/DK0641333T3/da active
- 1993-05-20 WO PCT/US1993/004806 patent/WO1993023368A1/en active Application Filing
- 1993-05-20 WO PCT/US1993/004804 patent/WO1993023388A1/en active IP Right Grant
- 1993-05-20 JP JP50384794A patent/JP3492362B2/ja not_active Expired - Fee Related
- 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 CA CA002131182A patent/CA2131182C/en not_active Expired - Fee Related
- 1993-05-20 ES ES93911369T patent/ES2091000T3/es not_active Expired - Lifetime
-
1996
- 1996-08-16 GR GR960402048T patent/GR3020814T3/el unknown
-
2002
- 2002-11-21 JP JP2002337347A patent/JP2003160545A/ja active Pending
- 2002-11-21 JP JP2002337346A patent/JP2003192648A/ja active Pending
Also Published As
Publication number | Publication date |
---|---|
JP2003192648A (ja) | 2003-07-09 |
EP0641333B1 (de) | 1996-08-14 |
DE69304051D1 (de) | 1996-09-19 |
CA2131182A1 (en) | 1993-11-25 |
WO1993023388A1 (en) | 1993-11-25 |
DK0641333T3 (da) | 1996-09-02 |
JP2003160545A (ja) | 2003-06-03 |
CA2131182C (en) | 2005-04-26 |
ES2091000T3 (es) | 1996-10-16 |
KR950700893A (ko) | 1995-02-20 |
ATE141265T1 (de) | 1996-08-15 |
WO1993023368A1 (en) | 1993-11-25 |
GR3020814T3 (en) | 1996-11-30 |
JPH07508041A (ja) | 1995-09-07 |
AU4253093A (en) | 1993-12-13 |
KR100290516B1 (ko) | 2001-09-17 |
EP0641333A1 (de) | 1995-03-08 |
AU4253193A (en) | 1993-12-13 |
JP3492362B2 (ja) | 2004-02-03 |
AU676479B2 (en) | 1997-03-13 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
8364 | No opposition during term of opposition | ||
8339 | Ceased/non-payment of the annual fee |