ZA200110177B - Inhibitors of aspartyl protease. - Google Patents
Inhibitors of aspartyl protease. Download PDFInfo
- Publication number
- ZA200110177B ZA200110177B ZA200110177A ZA200110177A ZA200110177B ZA 200110177 B ZA200110177 B ZA 200110177B ZA 200110177 A ZA200110177 A ZA 200110177A ZA 200110177 A ZA200110177 A ZA 200110177A ZA 200110177 B ZA200110177 B ZA 200110177B
- Authority
- ZA
- South Africa
- Prior art keywords
- alkyl
- optionally substituted
- membered saturated
- aryl
- unsaturated
- Prior art date
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- 239000003112 inhibitor Substances 0.000 title claims description 24
- 108010017640 Aspartic Acid Proteases Proteins 0.000 title claims description 13
- 102000004580 Aspartic Acid Proteases Human genes 0.000 title claims description 13
- 125000000217 alkyl group Chemical group 0.000 claims description 130
- 229920006395 saturated elastomer Polymers 0.000 claims description 108
- 229910052757 nitrogen Inorganic materials 0.000 claims description 84
- 125000000623 heterocyclic group Chemical group 0.000 claims description 68
- 229910052717 sulfur Inorganic materials 0.000 claims description 66
- 150000001875 compounds Chemical class 0.000 claims description 65
- 125000003342 alkenyl group Chemical group 0.000 claims description 51
- 125000005842 heteroatom Chemical group 0.000 claims description 49
- -1 methylenedioxy Chemical group 0.000 claims description 42
- 125000003118 aryl group Chemical group 0.000 claims description 40
- 229910052760 oxygen Inorganic materials 0.000 claims description 38
- 229910052799 carbon Inorganic materials 0.000 claims description 37
- 239000000203 mixture Substances 0.000 claims description 31
- 229910020008 S(O) Inorganic materials 0.000 claims description 29
- 125000001424 substituent group Chemical group 0.000 claims description 29
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 28
- 125000005843 halogen group Chemical group 0.000 claims description 25
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 24
- 125000000304 alkynyl group Chemical group 0.000 claims description 23
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 23
- 125000003545 alkoxy group Chemical group 0.000 claims description 16
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 15
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- 125000004122 cyclic group Chemical group 0.000 claims description 6
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- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 6
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- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 5
- GOWMBYUZXIZENX-CAUSLRQDSA-N 1-[(2r,3s,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-4-(hexadecylamino)pyrimidin-2-one Chemical compound O=C1N=C(NCCCCCCCCCCCCCCCC)C=CN1[C@H]1[C@@H](O)[C@H](O)[C@@H](CO)O1 GOWMBYUZXIZENX-CAUSLRQDSA-N 0.000 claims description 4
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Classifications
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
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- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
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- A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
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- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
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- C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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- C07C311/39—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
- C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
- C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
- C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
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- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
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- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Virology (AREA)
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- Communicable Diseases (AREA)
- Bioinformatics & Cheminformatics (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13907099P | 1999-06-11 | 1999-06-11 | |
| US19021100P | 2000-03-17 | 2000-03-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200110177B true ZA200110177B (en) | 2003-01-13 |
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|---|---|---|---|
| ZA200110177A ZA200110177B (en) | 1999-06-11 | 2001-12-11 | Inhibitors of aspartyl protease. |
Country Status (31)
| Country | Link |
|---|---|
| EP (2) | EP1194404B1 (de) |
| JP (2) | JP4503896B2 (de) |
| KR (1) | KR100762188B1 (de) |
| CN (2) | CN100516034C (de) |
| AR (1) | AR031520A1 (de) |
| AT (2) | ATE534622T1 (de) |
| AU (1) | AU779994B2 (de) |
| BR (1) | BR0011745A (de) |
| CA (1) | CA2380858C (de) |
| CO (1) | CO5160337A1 (de) |
| CY (1) | CY1112632T1 (de) |
| CZ (1) | CZ303052B6 (de) |
| DE (1) | DE60027722T2 (de) |
| DK (2) | DK1686113T3 (de) |
| ES (2) | ES2375823T3 (de) |
| HK (1) | HK1046899B (de) |
| HU (1) | HUP0300385A3 (de) |
| IL (3) | IL146918A0 (de) |
| MX (1) | MXPA01012808A (de) |
| MY (1) | MY137777A (de) |
| NO (1) | NO323951B1 (de) |
| NZ (1) | NZ516003A (de) |
| PE (1) | PE20010230A1 (de) |
| PL (1) | PL210227B1 (de) |
| PT (2) | PT1686113E (de) |
| SI (1) | SI1194404T1 (de) |
| TN (1) | TNSN00129A1 (de) |
| TR (3) | TR200200407T2 (de) |
| TW (3) | TW593248B (de) |
| WO (1) | WO2000076961A1 (de) |
| ZA (1) | ZA200110177B (de) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999065870A2 (en) | 1998-06-19 | 1999-12-23 | Vertex Pharmaceuticals Incorporated | Sulfonamide inhibitors of aspartyl protease |
| AR031520A1 (es) * | 1999-06-11 | 2003-09-24 | Vertex Pharma | Un compuesto inhibidor de aspartilo proteasa, una composicion que lo comprende y un metodo para tratar un paciente con dicha composicion |
| ATE343567T1 (de) | 2001-02-14 | 2006-11-15 | Tibotec Pharm Ltd | Breitspektrum 2-(substituierte-amino)- benzothiazol-sulfonamide hiv protease inhibitoren |
| US7285566B2 (en) * | 2002-01-07 | 2007-10-23 | Erickson John W | Resistance-repellent retroviral protease inhibitors |
| MY142238A (en) * | 2002-03-12 | 2010-11-15 | Tibotec Pharm Ltd | Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors |
| AU2003231766A1 (en) * | 2002-04-26 | 2003-11-10 | Gilead Sciences, Inc. | Non nucleoside reverse transcriptase inhibitors |
| US6632816B1 (en) * | 2002-12-23 | 2003-10-14 | Pharmacor Inc. | Aromatic derivatives as HIV aspartyl protease inhibitors |
| JP2007521277A (ja) * | 2003-06-27 | 2007-08-02 | スミスクライン ビーチャム コーポレーション | 化合物の製造 |
| US7767683B2 (en) | 2003-08-18 | 2010-08-03 | H. Lundbeck A/S | Hydrogen succinate salts of trans-4-((1R, 3S)-6-chloro-3-phenylindan-1-YL)-1,2,2-trimethylpiperazine and the use as a medicament |
| CN102627609B (zh) * | 2003-12-15 | 2016-05-04 | 默沙东公司 | 杂环天冬氨酰蛋白酶抑制剂 |
| CN1953964A (zh) | 2004-03-11 | 2007-04-25 | 塞阔伊亚药品公司 | 抗耐药性反转录病毒蛋白酶抑制剂 |
| TWI383975B (zh) | 2004-03-31 | 2013-02-01 | Tibotec Pharm Ltd | 製備（３Ｒ，３ａＳ，６ａＲ）六氫-呋喃并〔２，３-ｂ〕呋喃-３-醇之方法 |
| US7388008B2 (en) | 2004-08-02 | 2008-06-17 | Ambrilia Biopharma Inc. | Lysine based compounds |
| TWI376373B (en) | 2005-02-16 | 2012-11-11 | Lundbeck & Co As H | Crystalline base of a pharmaceutical compound |
| TWI453198B (zh) | 2005-02-16 | 2014-09-21 | Lundbeck & Co As H | 製造反式-1-((1r,3s)-6-氯基-3-苯基茚滿-1-基) -3 , 3 -二甲基六氫吡與其鹽類之方法及製造4-((1r , 3s）-6 -氯基-3-苯基茚滿-1-基 )-1,2,2-三甲基六氫吡與其鹽類之方法 |
| JP2008533017A (ja) * | 2005-03-11 | 2008-08-21 | スミスクライン ビーチャム コーポレーション | Ｈｉｖプロテアーゼ阻害薬 |
| US8227450B2 (en) | 2005-11-30 | 2012-07-24 | Ambrilia Biopharma Inc. | Lysine-based prodrugs of aspartyl protease inhibitors and processes for their preparation |
| EP2069356A1 (de) * | 2006-07-24 | 2009-06-17 | Gilead Sciences, Inc. | Bisfuranylproteasehemmer |
| PL2089371T3 (pl) | 2006-11-09 | 2011-06-30 | Janssen Sciences Ireland Uc | Sposoby wytwarzania heksahydrofuro[2,3-b]furan-3-olu |
| EP2120562A4 (de) * | 2006-11-21 | 2010-01-13 | Purdue Research Foundation | Verfahren und zusammensetzungen zur behandlung von hiv-infektionen |
| PT2152667E (pt) | 2007-04-27 | 2011-04-06 | Tibotec Pharm Ltd | Processos para a preparação de derivados de n-isobutil-n- (2-hidroxi-3-amino-4-fenilbutil)-p-nitrobenzenosulfonilamida |
| GB2452952A (en) * | 2007-09-20 | 2009-03-25 | Npil Pharmaceuticals | N-[2-Hydroxy-3-(hydroxycarbonylamino)-3-methyl]-N-methyl-sulphonamide derivatives via N-[2-oxo-3-(hydroxycarbonylamino)-3-methyl]-N-methyl-imine skeleton |
| US8592487B2 (en) | 2007-10-26 | 2013-11-26 | Concert Pharmaceuticals, Inc. | Deuterated darunavir |
| MX2012003424A (es) | 2009-09-22 | 2012-05-08 | Tibotec Pharm Ltd | Tratamiento y prevencion de infeccion por el virus de inmunodeficiencia humana. |
| WO2011061590A1 (en) | 2009-11-17 | 2011-05-26 | Hetero Research Foundation | Novel carboxamide derivatives as hiv inhibitors |
| CN103193570B (zh) * | 2013-04-09 | 2014-01-22 | 湖北来凤腾升香料化工有限公司 | 一种羟基高选择性保护方法 |
| JPWO2016039403A1 (ja) * | 2014-09-11 | 2017-06-29 | 塩野義製薬株式会社 | 持続性ｈｉｖプロテアーゼ阻害剤 |
| US11116737B1 (en) | 2020-04-10 | 2021-09-14 | University Of Georgia Research Foundation, Inc. | Methods of using probenecid for treatment of coronavirus infections |
| US12083099B2 (en) | 2020-10-28 | 2024-09-10 | Accencio LLC | Methods of treating symptoms of coronavirus infection with viral protease inhibitors |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3635907A1 (de) * | 1986-10-22 | 1988-04-28 | Merck Patent Gmbh | Hydroxy-aminosaeurederivate |
| CA2032259A1 (en) * | 1989-12-18 | 1991-06-19 | Wayne J. Thompson | Hiv protease inhibitors useful for the treatment of aids |
| HU9301447D0 (en) * | 1990-11-19 | 1993-11-29 | Monsanto Co | Inhibitors of retrovirus protease |
| US5475013A (en) * | 1990-11-19 | 1995-12-12 | Monsanto Company | Retroviral protease inhibitors |
| KR100336699B1 (ko) * | 1992-08-25 | 2002-05-13 | 윌리암스 로저 에이 | 레트로바이러스 프로테아제 저해제로서 유용한히드록시에틸아미노 술폰아미드 |
| IS2334B (is) * | 1992-09-08 | 2008-02-15 | Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) | Aspartyl próteasi hemjari af nýjum flokki súlfonamíða |
| US5723490A (en) * | 1992-09-08 | 1998-03-03 | Vertex Pharmaceuticals Incorporated | THF-containing sulfonamide inhibitors of aspartyl protease |
| CA2143191A1 (en) * | 1992-10-30 | 1994-05-11 | Michael L. Vazquez | Sulfonylalkanoylamino hydroxyethylamino sulfamic acids useful as retroviral protease inhibitors |
| ES2127938T3 (es) * | 1993-08-24 | 1999-05-01 | Searle & Co | Hidroxietilamino sulfonamidas utiles como inhibidores de proteasas retroviricas. |
| CA2210889C (en) * | 1995-01-20 | 2007-08-28 | G.D. Searle & Co. | Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors |
| US5756533A (en) * | 1995-03-10 | 1998-05-26 | G.D. Searle & Co. | Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
| US6150556A (en) * | 1995-03-10 | 2000-11-21 | G. D. Dearle & Co. | Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
| PL184771B1 (pl) * | 1995-03-10 | 2002-12-31 | Searle & Co | Związek stanowiący hydroksyetyloaminosulfonamid pirolidynokarbonyloaminokwasu, kompozycja zawierająca ten związek, jego zastosowanie do wytwarzania kompozycji do leczenia infekcji retrowirusowej i sposób zapobiegania replikacji retrowirusa in vitro |
| US5705500A (en) * | 1995-03-10 | 1998-01-06 | G.D. Searle & Co. | Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
| US5691372A (en) * | 1995-04-19 | 1997-11-25 | Vertex Pharmaceuticals Incorporated | Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease |
| AU7722296A (en) * | 1995-11-15 | 1997-06-05 | G.D. Searle & Co. | Substituted sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
| GB9712504D0 (en) * | 1997-06-17 | 1997-08-20 | Dundee Teaching Hospitals Nhs | Thermal imaging method and apparatus |
| US6316405B1 (en) * | 1997-08-26 | 2001-11-13 | Wisconsin Alumni Research Foundation | Cyclosporin a conjugates and uses therefor |
| AR031520A1 (es) * | 1999-06-11 | 2003-09-24 | Vertex Pharma | Un compuesto inhibidor de aspartilo proteasa, una composicion que lo comprende y un metodo para tratar un paciente con dicha composicion |
-
2000
- 2000-06-07 AR ARP000102852A patent/AR031520A1/es active IP Right Grant
- 2000-06-08 TR TR2002/00407T patent/TR200200407T2/xx unknown
- 2000-06-08 TW TW089111145A patent/TW593248B/zh not_active IP Right Cessation
- 2000-06-08 PE PE2000000573A patent/PE20010230A1/es not_active Application Discontinuation
- 2000-06-08 CN CNB008104395A patent/CN100516034C/zh not_active Expired - Fee Related
- 2000-06-08 AU AU56006/00A patent/AU779994B2/en not_active Ceased
- 2000-06-08 PL PL352830A patent/PL210227B1/pl not_active IP Right Cessation
- 2000-06-08 HU HU0300385A patent/HUP0300385A3/hu unknown
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- 2000-06-08 CN CNA2008100096668A patent/CN101245058A/zh active Pending
- 2000-06-08 BR BR0011745-5A patent/BR0011745A/pt not_active Application Discontinuation
- 2000-06-08 IL IL14691800A patent/IL146918A0/xx unknown
- 2000-06-08 DK DK06009072.7T patent/DK1686113T3/da active
- 2000-06-08 TR TR2006/03871T patent/TR200603871T2/xx unknown
- 2000-06-08 CA CA2380858A patent/CA2380858C/en not_active Expired - Fee Related
- 2000-06-08 DE DE60027722T patent/DE60027722T2/de not_active Expired - Lifetime
- 2000-06-08 JP JP2001503821A patent/JP4503896B2/ja not_active Expired - Fee Related
- 2000-06-08 AT AT06009072T patent/ATE534622T1/de active
- 2000-06-08 ES ES06009072T patent/ES2375823T3/es not_active Expired - Lifetime
- 2000-06-08 CO CO00042752A patent/CO5160337A1/es unknown
- 2000-06-08 EP EP00941279A patent/EP1194404B1/de not_active Expired - Lifetime
- 2000-06-08 DK DK00941279T patent/DK1194404T3/da active
- 2000-06-08 CZ CZ20014431A patent/CZ303052B6/cs not_active IP Right Cessation
- 2000-06-08 AT AT00941279T patent/ATE325091T1/de active
- 2000-06-08 MX MXPA01012808A patent/MXPA01012808A/es active IP Right Grant
- 2000-06-08 TW TW093114799A patent/TWI299000B/zh not_active IP Right Cessation
- 2000-06-08 EP EP06009072A patent/EP1686113B1/de not_active Expired - Lifetime
- 2000-06-08 TN TNTNSN00129A patent/TNSN00129A1/fr unknown
- 2000-06-08 MY MYPI20002595A patent/MY137777A/en unknown
- 2000-06-08 PT PT06009072T patent/PT1686113E/pt unknown
- 2000-06-08 SI SI200030872T patent/SI1194404T1/sl unknown
- 2000-06-08 PT PT00941279T patent/PT1194404E/pt unknown
- 2000-06-08 TR TR2002/02528T patent/TR200202528T2/xx unknown
- 2000-06-08 NZ NZ516003A patent/NZ516003A/xx not_active IP Right Cessation
- 2000-06-08 WO PCT/US2000/015781 patent/WO2000076961A1/en active Application Filing
- 2000-06-08 ES ES00941279T patent/ES2263478T3/es not_active Expired - Lifetime
- 2000-06-08 KR KR1020017016293A patent/KR100762188B1/ko not_active IP Right Cessation
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2001
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- 2001-12-10 NO NO20016034A patent/NO323951B1/no not_active IP Right Cessation
- 2001-12-11 ZA ZA200110177A patent/ZA200110177B/en unknown
-
2002
- 2002-09-23 HK HK02106939.9A patent/HK1046899B/zh not_active IP Right Cessation
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2008
- 2008-09-08 JP JP2008230351A patent/JP2009046493A/ja not_active Withdrawn
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2009
- 2009-12-09 IL IL202633A patent/IL202633A/en not_active IP Right Cessation
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2012
- 2012-02-22 CY CY20121100182T patent/CY1112632T1/el unknown
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