EA009700B1 - Ненуклеозидные ингибиторы обратной транскриптазы - Google Patents
Ненуклеозидные ингибиторы обратной транскриптазы Download PDFInfo
- Publication number
- EA009700B1 EA009700B1 EA200601289A EA200601289A EA009700B1 EA 009700 B1 EA009700 B1 EA 009700B1 EA 200601289 A EA200601289 A EA 200601289A EA 200601289 A EA200601289 A EA 200601289A EA 009700 B1 EA009700 B1 EA 009700B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- alkyl
- mmol
- compound according
- cis
- tetrahydrocycloprop
- Prior art date
Links
- 239000002773 nucleotide Substances 0.000 title 1
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 32
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 4
- 125000001424 substituent group Chemical group 0.000 claims abstract 4
- 229910052799 carbon Inorganic materials 0.000 claims abstract 3
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 3
- 125000005842 heteroatom Chemical group 0.000 claims abstract 3
- 239000003443 antiviral agent Substances 0.000 claims abstract 2
- 125000003118 aryl group Chemical group 0.000 claims abstract 2
- 239000000651 prodrug Substances 0.000 claims abstract 2
- 229940002612 prodrug Drugs 0.000 claims abstract 2
- 150000003839 salts Chemical class 0.000 claims abstract 2
- 229910052731 fluorine Inorganic materials 0.000 claims 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 6
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 5
- -1 cyano-C1 -C6 alkyl Chemical group 0.000 claims 5
- 125000001153 fluoro group Chemical group F* 0.000 claims 5
- 125000005843 halogen group Chemical group 0.000 claims 5
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 4
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 4
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- 208000031886 HIV Infections Diseases 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 125000000468 ketone group Chemical group 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 102000002004 Cytochrome P-450 Enzyme System Human genes 0.000 claims 1
- 108010015742 Cytochrome P-450 Enzyme System Proteins 0.000 claims 1
- 241000725303 Human immunodeficiency virus Species 0.000 claims 1
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 1
- NCDNCNXCDXHOMX-UHFFFAOYSA-N Ritonavir Natural products C=1C=CC=CC=1CC(NC(=O)OCC=1SC=NC=1)C(O)CC(CC=1C=CC=CC=1)NC(=O)C(C(C)C)NC(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-UHFFFAOYSA-N 0.000 claims 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 1
- 239000004202 carbamide Substances 0.000 claims 1
- 125000001589 carboacyl group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 1
- 230000001747 exhibiting effect Effects 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 150000004702 methyl esters Chemical class 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 230000003287 optical effect Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- NCDNCNXCDXHOMX-XGKFQTDJSA-N ritonavir Chemical compound N([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1SC=NC=1)CC=1C=CC=CC=1)C(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-XGKFQTDJSA-N 0.000 claims 1
- 229960000311 ritonavir Drugs 0.000 claims 1
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 1
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 abstract 1
- 229940121357 antivirals Drugs 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 150000002170 ethers Chemical class 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Virology (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Enzymes And Modification Thereof (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE0400021A SE0400021D0 (sv) | 2004-01-08 | 2004-01-08 | Non-nucleoside reverse transcriptase inhibitors |
| SE0400585A SE0400585D0 (sv) | 2004-03-09 | 2004-03-09 | NNRTI Antivirals |
| PCT/SE2004/002034 WO2005066131A1 (en) | 2004-01-08 | 2004-12-30 | Non-nucleotide reverse transcriptase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200601289A1 EA200601289A1 (ru) | 2006-12-29 |
| EA009700B1 true EA009700B1 (ru) | 2008-02-28 |
Family
ID=34752289
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200601289A EA009700B1 (ru) | 2004-01-08 | 2004-12-30 | Ненуклеозидные ингибиторы обратной транскриптазы |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US7915295B2 (OSRAM) |
| EP (1) | EP1701942B1 (OSRAM) |
| JP (1) | JP4762917B2 (OSRAM) |
| AT (1) | ATE451357T1 (OSRAM) |
| AU (1) | AU2004312284B2 (OSRAM) |
| BR (1) | BRPI0418306B8 (OSRAM) |
| CA (1) | CA2550187C (OSRAM) |
| DE (1) | DE602004024584D1 (OSRAM) |
| DK (1) | DK1701942T3 (OSRAM) |
| EA (1) | EA009700B1 (OSRAM) |
| ES (1) | ES2337794T3 (OSRAM) |
| IL (1) | IL176740A (OSRAM) |
| NZ (1) | NZ548367A (OSRAM) |
| SG (1) | SG149070A1 (OSRAM) |
| WO (1) | WO2005066131A1 (OSRAM) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1694700A (zh) * | 2002-09-05 | 2005-11-09 | 美迪维尔公司 | 非核苷逆转录酶抑制剂 |
| US7388008B2 (en) | 2004-08-02 | 2008-06-17 | Ambrilia Biopharma Inc. | Lysine based compounds |
| EP1877091B1 (en) * | 2005-04-27 | 2015-03-25 | TaiMed Biologics, Inc. | Method for improving pharmacokinetics of protease inhibitors and protease inhibitor precursors |
| WO2007062526A1 (en) | 2005-11-30 | 2007-06-07 | Ambrilia Biopharma Inc. | Lysine-based prodrugs of aspartyl protease inhibitors and processes for their preparation |
| GB0608876D0 (en) * | 2006-05-05 | 2006-06-14 | Medivir Ab | Combination therapy |
| WO2007136572A2 (en) * | 2006-05-15 | 2007-11-29 | Merck & Co., Inc. | Antidiabetic bicyclic compounds |
| CA2664118A1 (en) | 2006-09-21 | 2008-07-03 | Ambrilia Biopharma Inc. | Protease inhibitors |
| EP3250552B1 (en) * | 2015-01-30 | 2019-03-27 | Genentech, Inc. | Therapeutic compounds and uses thereof |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999036406A1 (en) * | 1998-01-16 | 1999-07-22 | Medivir Ab | Antivirals |
| WO2000047561A1 (en) * | 1999-02-12 | 2000-08-17 | Medivir Ab | Non-nucleoside reverse transcriptase inhibitors |
| WO2002070516A2 (en) * | 2001-03-05 | 2002-09-12 | Medivir Ab | Cyclopropaheterocycles as non-nucleoside reverse transcriptase inhibitors |
| WO2003020705A1 (en) * | 2001-08-28 | 2003-03-13 | Medivir Ab | Urea and thiourea derivatives as non-nucleoside reverse transcriptase inhibitors |
| WO2004021969A2 (en) * | 2002-09-05 | 2004-03-18 | Medivir Ab | Non-nucleoside reverse transcriptase inhibitors |
-
2004
- 2004-12-30 EP EP04809207A patent/EP1701942B1/en not_active Expired - Lifetime
- 2004-12-30 WO PCT/SE2004/002034 patent/WO2005066131A1/en not_active Ceased
- 2004-12-30 EA EA200601289A patent/EA009700B1/ru not_active IP Right Cessation
- 2004-12-30 SG SG200809639-8A patent/SG149070A1/en unknown
- 2004-12-30 BR BRPI0418306A patent/BRPI0418306B8/pt not_active IP Right Cessation
- 2004-12-30 AU AU2004312284A patent/AU2004312284B2/en not_active Ceased
- 2004-12-30 DE DE602004024584T patent/DE602004024584D1/de not_active Expired - Lifetime
- 2004-12-30 NZ NZ548367A patent/NZ548367A/en not_active IP Right Cessation
- 2004-12-30 CA CA2550187A patent/CA2550187C/en not_active Expired - Fee Related
- 2004-12-30 US US10/584,933 patent/US7915295B2/en not_active Expired - Fee Related
- 2004-12-30 AT AT04809207T patent/ATE451357T1/de not_active IP Right Cessation
- 2004-12-30 ES ES04809207T patent/ES2337794T3/es not_active Expired - Lifetime
- 2004-12-30 DK DK04809207.6T patent/DK1701942T3/da active
- 2004-12-30 JP JP2006549182A patent/JP4762917B2/ja not_active Expired - Fee Related
-
2006
- 2006-07-06 IL IL176740A patent/IL176740A/en not_active IP Right Cessation
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999036406A1 (en) * | 1998-01-16 | 1999-07-22 | Medivir Ab | Antivirals |
| WO2000047561A1 (en) * | 1999-02-12 | 2000-08-17 | Medivir Ab | Non-nucleoside reverse transcriptase inhibitors |
| WO2002070516A2 (en) * | 2001-03-05 | 2002-09-12 | Medivir Ab | Cyclopropaheterocycles as non-nucleoside reverse transcriptase inhibitors |
| WO2003020705A1 (en) * | 2001-08-28 | 2003-03-13 | Medivir Ab | Urea and thiourea derivatives as non-nucleoside reverse transcriptase inhibitors |
| WO2004021969A2 (en) * | 2002-09-05 | 2004-03-18 | Medivir Ab | Non-nucleoside reverse transcriptase inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| EA200601289A1 (ru) | 2006-12-29 |
| DK1701942T3 (da) | 2010-04-06 |
| WO2005066131A1 (en) | 2005-07-21 |
| BRPI0418306A (pt) | 2007-05-02 |
| BRPI0418306B8 (pt) | 2021-05-25 |
| ATE451357T1 (de) | 2009-12-15 |
| DE602004024584D1 (de) | 2010-01-21 |
| JP4762917B2 (ja) | 2011-08-31 |
| AU2004312284A2 (en) | 2005-07-21 |
| EP1701942B1 (en) | 2009-12-09 |
| AU2004312284A1 (en) | 2005-07-21 |
| NZ548367A (en) | 2010-06-25 |
| IL176740A (en) | 2011-09-27 |
| SG149070A1 (en) | 2009-01-29 |
| HK1101400A1 (en) | 2007-10-18 |
| US7915295B2 (en) | 2011-03-29 |
| BRPI0418306B1 (pt) | 2018-09-18 |
| US20080070951A1 (en) | 2008-03-20 |
| JP2007519640A (ja) | 2007-07-19 |
| AU2004312284B2 (en) | 2010-08-05 |
| ES2337794T3 (es) | 2010-04-29 |
| EP1701942A1 (en) | 2006-09-20 |
| IL176740A0 (en) | 2006-10-31 |
| CA2550187A1 (en) | 2005-07-21 |
| CA2550187C (en) | 2012-08-07 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM |
|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): RU |