DE69523038D1 - Verfahren zur herstellung von hiv proteasinhibitoren - Google Patents
Verfahren zur herstellung von hiv proteasinhibitorenInfo
- Publication number
- DE69523038D1 DE69523038D1 DE69523038T DE69523038T DE69523038D1 DE 69523038 D1 DE69523038 D1 DE 69523038D1 DE 69523038 T DE69523038 T DE 69523038T DE 69523038 T DE69523038 T DE 69523038T DE 69523038 D1 DE69523038 D1 DE 69523038D1
- Authority
- DE
- Germany
- Prior art keywords
- piperazine
- proteasinhibitors
- optically pure
- derivatives
- enriched
- 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
- 238000004519 manufacturing process Methods 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229940122440 HIV protease inhibitor Drugs 0.000 abstract 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- GLUUGHFHXGJENI-UHFFFAOYSA-N diethylenediamine Natural products C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 abstract 1
- 239000004030 hiv protease inhibitor Substances 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 239000002184 metal Substances 0.000 abstract 1
- -1 piperazine compound Chemical class 0.000 abstract 1
- IVXQBCUBSIPQGU-UHFFFAOYSA-N piperazine-1-carboxamide Chemical class NC(=O)N1CCNCC1 IVXQBCUBSIPQGU-UHFFFAOYSA-N 0.000 abstract 1
- 230000006340 racemization Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61P31/12—Antivirals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Cephalosporin Compounds (AREA)
- Catalysts (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US19291694A | 1994-02-04 | 1994-02-04 | |
| PCT/US1995/001232 WO1995021162A1 (en) | 1994-02-04 | 1995-01-30 | Process for making hiv protease inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE69523038D1 true DE69523038D1 (de) | 2001-11-08 |
| DE69523038T2 DE69523038T2 (de) | 2002-06-06 |
Family
ID=22711555
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE69523038T Expired - Fee Related DE69523038T2 (de) | 1994-02-04 | 1995-01-30 | Verfahren zur herstellung von hiv proteasinhibitoren |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US5663341A (de) |
| EP (1) | EP0741712B1 (de) |
| JP (1) | JPH09508628A (de) |
| KR (1) | KR100337579B1 (de) |
| AT (1) | ATE206407T1 (de) |
| AU (1) | AU691878B2 (de) |
| BR (1) | BR9506727A (de) |
| CA (1) | CA2180947A1 (de) |
| CZ (1) | CZ291774B6 (de) |
| DE (1) | DE69523038T2 (de) |
| ES (1) | ES2161863T3 (de) |
| FI (1) | FI112218B (de) |
| HU (1) | HUT76303A (de) |
| NZ (1) | NZ279734A (de) |
| RO (1) | RO118292B1 (de) |
| RU (1) | RU2135482C1 (de) |
| SK (1) | SK281861B6 (de) |
| TW (1) | TW472047B (de) |
| UA (1) | UA46730C2 (de) |
| WO (1) | WO1995021162A1 (de) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL110255A (en) * | 1993-07-16 | 1998-12-06 | Merck & Co Inc | Formation and resolution of 2-tert-butylcarboxamido-piperazine |
| US5464788A (en) * | 1994-03-24 | 1995-11-07 | Merck & Co., Inc. | Tocolytic oxytocin receptor antagonists |
| DE69527683T2 (de) * | 1994-04-22 | 2003-04-10 | Koei Chemical Co., Ltd. | Verfahren zur herstellung von optisch aktivem n-tert-butyl-2-piperazincarboxamidamid |
| ES2116029T3 (es) * | 1994-11-04 | 1998-07-01 | Yamakawa Chemical Ind | Procedimiento para preparar derivados de piperazina opticamente activos e intermedios para prepararlos. |
| DE59609835D1 (de) * | 1995-01-23 | 2002-12-05 | Lonza Ag Visp | Verfahren zur herstellung von 1,4,5,6-tetrahydropyrazin-2-carbonsäureamiden |
| US5618937A (en) * | 1995-03-15 | 1997-04-08 | Merck & Co., Inc. | Process to make HIV protease inhibitor from (2S)-4-picolyl-2-piperazine-t-butylcarboxamide |
| US5612484A (en) * | 1995-05-18 | 1997-03-18 | Merck & Co., Inc. | Process for making HIV protease inhibitors |
| DE19536658C2 (de) * | 1995-09-30 | 1998-02-19 | Degussa | Verfahren zur kontinuierlichen Herstellung von basischen, cyclischen, optisch aktiven alpha-Aminosäuren |
| CA2201218C (en) * | 1996-04-23 | 2004-09-28 | Rudolf Fuchs | Process for the preparation of optically active piperazine-2-carboxylic acid derivatives |
| AU2004212335A1 (en) * | 2003-02-14 | 2004-08-26 | Merck Serono Sa | Piperazine-2-carboxamide derivatives |
| GB0314260D0 (en) * | 2003-06-19 | 2003-07-23 | Astrazeneca Ab | Therapeutic agents |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB604185A (en) * | 1940-08-08 | 1948-06-30 | Arthur Mandl | Improvements in electric rectifier systems used in power or control systems such as for follow-up systems |
| US3692775A (en) * | 1969-03-17 | 1972-09-19 | Allied Chem | Racemization of d-or l-{60 -amino-caprolactam in the presence of metal ions |
| US3852351A (en) * | 1972-10-02 | 1974-12-03 | Fmc Corp | Chlorination of acetoacetamides |
| JPH01117869A (ja) * | 1987-10-30 | 1989-05-10 | Hokuriku Seiyaku Co Ltd | ２−アミノメチルピペラジン誘導体 |
| CA1340588C (en) * | 1988-06-13 | 1999-06-08 | Balraj Krishan Handa | Amino acid derivatives |
| US5413999A (en) * | 1991-11-08 | 1995-05-09 | Merck & Co., Inc. | HIV protease inhibitors useful for the treatment of AIDS |
| SG52731A1 (en) * | 1991-11-08 | 1998-09-28 | Merck & Co Inc | Hiv protease inhibitors useful for the treatment of aids |
| MX9308016A (es) * | 1992-12-22 | 1994-08-31 | Lilly Co Eli | Compuestos inhibidores de la proteasa del virus de la inmunodeficiencia humana, procedimiento para su preparacion y formulacion farmaceutica que los contiene. |
-
1995
- 1995-01-27 TW TW084100727A patent/TW472047B/zh not_active IP Right Cessation
- 1995-01-30 WO PCT/US1995/001232 patent/WO1995021162A1/en active Search and Examination
- 1995-01-30 SK SK1006-96A patent/SK281861B6/sk unknown
- 1995-01-30 CZ CZ19962272A patent/CZ291774B6/cs not_active IP Right Cessation
- 1995-01-30 RU RU96117468/04A patent/RU2135482C1/ru not_active IP Right Cessation
- 1995-01-30 JP JP7520686A patent/JPH09508628A/ja not_active Withdrawn
- 1995-01-30 EP EP95908747A patent/EP0741712B1/de not_active Expired - Lifetime
- 1995-01-30 KR KR1019960704219A patent/KR100337579B1/ko not_active Expired - Fee Related
- 1995-01-30 BR BR9506727A patent/BR9506727A/pt active Search and Examination
- 1995-01-30 RO RO96-01576A patent/RO118292B1/ro unknown
- 1995-01-30 UA UA96093433A patent/UA46730C2/uk unknown
- 1995-01-30 ES ES95908747T patent/ES2161863T3/es not_active Expired - Lifetime
- 1995-01-30 AT AT95908747T patent/ATE206407T1/de not_active IP Right Cessation
- 1995-01-30 HU HU9602143A patent/HUT76303A/hu unknown
- 1995-01-30 AU AU16967/95A patent/AU691878B2/en not_active Ceased
- 1995-01-30 DE DE69523038T patent/DE69523038T2/de not_active Expired - Fee Related
- 1995-01-30 NZ NZ279734A patent/NZ279734A/en unknown
- 1995-01-30 CA CA002180947A patent/CA2180947A1/en not_active Abandoned
- 1995-06-07 US US08/487,903 patent/US5663341A/en not_active Expired - Fee Related
-
1996
- 1996-08-01 FI FI963054A patent/FI112218B/fi active
Also Published As
| Publication number | Publication date |
|---|---|
| CA2180947A1 (en) | 1995-08-10 |
| DE69523038T2 (de) | 2002-06-06 |
| FI963054L (fi) | 1996-08-01 |
| FI112218B (fi) | 2003-11-14 |
| ES2161863T3 (es) | 2001-12-16 |
| MX9603218A (es) | 1997-07-31 |
| EP0741712B1 (de) | 2001-10-04 |
| ATE206407T1 (de) | 2001-10-15 |
| CZ291774B6 (cs) | 2003-05-14 |
| SK281861B6 (sk) | 2001-08-06 |
| JPH09508628A (ja) | 1997-09-02 |
| HUT76303A (en) | 1997-07-28 |
| HU9602143D0 (en) | 1996-09-30 |
| TW472047B (en) | 2002-01-11 |
| SK100696A3 (en) | 1997-03-05 |
| UA46730C2 (uk) | 2002-06-17 |
| CZ227296A3 (en) | 1997-01-15 |
| AU691878B2 (en) | 1998-05-28 |
| RO118292B1 (ro) | 2003-04-30 |
| EP0741712A1 (de) | 1996-11-13 |
| RU2135482C1 (ru) | 1999-08-27 |
| KR100337579B1 (ko) | 2002-11-13 |
| US5663341A (en) | 1997-09-02 |
| WO1995021162A1 (en) | 1995-08-10 |
| AU1696795A (en) | 1995-08-21 |
| FI963054A0 (fi) | 1996-08-01 |
| BR9506727A (pt) | 1997-09-23 |
| NZ279734A (en) | 1998-05-27 |
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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 |