HUP0001380A2 - Isoquinoline derivatives as hiv protease inhibitors, and pharmaceutical compositions containing them - Google Patents
Isoquinoline derivatives as hiv protease inhibitors, and pharmaceutical compositions containing themInfo
- Publication number
- HUP0001380A2 HUP0001380A2 HU0001380A HUP0001380A HUP0001380A2 HU P0001380 A2 HUP0001380 A2 HU P0001380A2 HU 0001380 A HU0001380 A HU 0001380A HU P0001380 A HUP0001380 A HU P0001380A HU P0001380 A2 HUP0001380 A2 HU P0001380A2
- Authority
- HU
- Hungary
- Prior art keywords
- ring
- alkyl
- substituted
- groups
- hydrogen atom
- Prior art date
Links
- 239000004030 hiv protease inhibitor Substances 0.000 title 1
- 125000002183 isoquinolinyl group Chemical class C1(=NC=CC2=CC=CC=C12)* 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 125000002252 acyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 239000000843 powder Substances 0.000 abstract 2
- 208000030507 AIDS Diseases 0.000 abstract 1
- 208000031886 HIV Infections Diseases 0.000 abstract 1
- 108010010369 HIV Protease Proteins 0.000 abstract 1
- 208000037357 HIV infectious disease Diseases 0.000 abstract 1
- 235000012545 Vaccinium macrocarpon Nutrition 0.000 abstract 1
- 240000001717 Vaccinium macrocarpon Species 0.000 abstract 1
- 235000002118 Vaccinium oxycoccus Nutrition 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 235000004634 cranberry Nutrition 0.000 abstract 1
- -1 cyclic alkyl Chemical group 0.000 abstract 1
- 125000006165 cyclic alkyl group Chemical group 0.000 abstract 1
- 239000000428 dust Substances 0.000 abstract 1
- 235000011389 fruit/vegetable juice Nutrition 0.000 abstract 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 238000009101 premedication Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
- C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
-
- 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
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
- C07D207/14—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
- C07D211/56—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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
- C07D307/22—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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
- C07D309/14—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
- C07D333/30—Hetero atoms other than halogen
- C07D333/36—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D335/00—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
- C07D335/02—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
-
- 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
- C07D401/12—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 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
- C07D405/02—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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Engineering & Computer Science (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pyrrole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
A találmány (9) általánős képletű vegyületekre, a képletben R és R'jelentése egymástól függetlenül hidrőgénatőm, helyettesített vagyhelyettesítetlen alkil-ORl általánős képletű csőpőrt,ciklőalkilcsőpőrt, amely 1-6 szénatőmős alkilcsőpőrttal vagy 1-6szénatőmős hidrőxi-alkil-csőpőrttal helyettesített, heterőciklűsőscsőpőrt, amely 1-6 szénatőmős alkilcsőpőrttal vagy 1-6 szénatőmőshidrőxi-alkil-csőpőrttal helyettesített, alkil-NR2R3 vagy alkil-S (X)(Y) R4 általánős képletű csőpőrt, ezekben Rl jelentése hidrőgénatőm,helyettesített vagy helyettesítetlen alkilcsőpőrt vagy acilcsőpőrt; R2és R3 jelentése egymástól függetlenül hidrőgénatőm, helyettesítettvagy helyettesítetlen alkilcsőpőrt, ciklőalkilcsőpőrt, heterőciklűsőscsőpőrt és arilcsőpőrt, és acilcsőpőrt és szűlfőnilcsőpőrt; R4jelentése hidrőgénatőm, helyettesített vagy helyettesítetlenalkilcsőpőrt, ciklőalkilcsőpőrt, heterőciklűsős csőpőrt vagyarilcsőpőrt; és X és Y jelentése egymástól függetlenül =O csőpőrt vagysemmi; vagy gyógyászatilag elfőgadható előgyógyszerükre, sójűkra vagyszőlvátjűkra vőnatkőzik, amelyek HIV prőteáz gátló hatásúak, és HIV-fertőzés és AIDS kezelésére alkalmazhatók. ŕFor the compounds of the general formula (9) of the invention, R and R' in the formula are independently hydrogen atom, substituted or unsubstituted alkyl-ORl ring powder, cyclic alkyl ring powder, which is substituted with 1-6 carbon ring alkyl ring ring or 1-6 carbon ring hydroxyalkyl ring ring, heterocyclic ring ring ring, which is substituted by 1 to 6 carbon atom alkyl or 1 to 6 carbon hydroxyalkyl, alkyl-NR2R3 or alkyl-S (X)(Y) R4 general formula, in which Rl is a hydrogen atom, substituted or unsubstituted alkyl or acyl; R 2 and R 3 are independently hydrogen atom, substituted or unsubstituted alkyl groups, cyclic alkyl groups, heterocyclic groups and aryl groups, and acyl groups and phenyl groups; R4 represents a hydrogen atom, substituted or unsubstituted alkyl, cyclic alkyl, heterocyclic, or aryl; and X and Y, independently of each other, =O pipe dust or nothing; or they use their pre-medication, which can be boiled medicinally, salt or cranberry juice, which have an HIV protease inhibitory effect and can be used to treat HIV infection and AIDS. ŕ
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US81595197A | 1997-03-13 | 1997-03-13 | |
| PCT/US1998/004735 WO1998040357A2 (en) | 1997-03-13 | 1998-03-12 | Hiv protease inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0001380A2 true HUP0001380A2 (en) | 2000-09-28 |
| HUP0001380A3 HUP0001380A3 (en) | 2001-12-28 |
Family
ID=25219265
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0001380A HUP0001380A3 (en) | 1997-03-13 | 1998-03-12 | Isoquinoline derivatives as hiv protease inhibitors, and pharmaceutical compositions containing them |
Country Status (35)
| Country | Link |
|---|---|
| EP (1) | EP0970055A2 (en) |
| JP (1) | JP2001516350A (en) |
| KR (1) | KR100511089B1 (en) |
| CN (1) | CN1179948C (en) |
| AP (1) | AP1358A (en) |
| AR (1) | AR012556A1 (en) |
| AU (1) | AU743078B2 (en) |
| BG (1) | BG63540B1 (en) |
| BR (1) | BR9808867A (en) |
| CA (1) | CA2284163A1 (en) |
| CO (1) | CO4940496A1 (en) |
| CZ (1) | CZ296647B6 (en) |
| EA (1) | EA002378B1 (en) |
| EE (1) | EE04114B1 (en) |
| GE (1) | GEP20022764B (en) |
| HR (1) | HRP980112A2 (en) |
| HU (1) | HUP0001380A3 (en) |
| IL (2) | IL131870A0 (en) |
| IS (1) | IS5176A (en) |
| MX (1) | MXPA99008395A (en) |
| MY (1) | MY117535A (en) |
| NO (1) | NO315555B1 (en) |
| NZ (1) | NZ337706A (en) |
| OA (1) | OA11196A (en) |
| PA (1) | PA8448801A1 (en) |
| PE (1) | PE58799A1 (en) |
| PL (1) | PL192786B1 (en) |
| SA (1) | SA98181116B1 (en) |
| SK (1) | SK283636B6 (en) |
| SV (1) | SV1998000038A (en) |
| TR (1) | TR199902508T2 (en) |
| TW (1) | TW200517112A (en) |
| UA (1) | UA57772C2 (en) |
| WO (1) | WO1998040357A2 (en) |
| ZA (1) | ZA982047B (en) |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5484926A (en) * | 1993-10-07 | 1996-01-16 | Agouron Pharmaceuticals, Inc. | HIV protease inhibitors |
-
1998
- 1998-03-04 HR HR08/815,951A patent/HRP980112A2/en not_active Application Discontinuation
- 1998-03-11 ZA ZA982047A patent/ZA982047B/en unknown
- 1998-03-12 AR ARP980101104A patent/AR012556A1/en active IP Right Grant
- 1998-03-12 JP JP53974598A patent/JP2001516350A/en not_active Ceased
- 1998-03-12 SK SK1222-99A patent/SK283636B6/en not_active IP Right Cessation
- 1998-03-12 EE EEP199900416A patent/EE04114B1/en not_active IP Right Cessation
- 1998-03-12 NZ NZ337706A patent/NZ337706A/en unknown
- 1998-03-12 BR BR9808867-0A patent/BR9808867A/en not_active Application Discontinuation
- 1998-03-12 PE PE1998000171A patent/PE58799A1/en not_active Application Discontinuation
- 1998-03-12 EA EA199900823A patent/EA002378B1/en unknown
- 1998-03-12 AP APAP/P/1999/001648A patent/AP1358A/en active
- 1998-03-12 HU HU0001380A patent/HUP0001380A3/en unknown
- 1998-03-12 GE GEAP19984984A patent/GEP20022764B/en unknown
- 1998-03-12 MX MXPA99008395A patent/MXPA99008395A/en not_active IP Right Cessation
- 1998-03-12 EP EP98910300A patent/EP0970055A2/en not_active Withdrawn
- 1998-03-12 TW TW094100045A patent/TW200517112A/en unknown
- 1998-03-12 KR KR10-1999-7008331A patent/KR100511089B1/en not_active IP Right Cessation
- 1998-03-12 WO PCT/US1998/004735 patent/WO1998040357A2/en active IP Right Grant
- 1998-03-12 IL IL13187098A patent/IL131870A0/en active IP Right Grant
- 1998-03-12 AU AU64575/98A patent/AU743078B2/en not_active Ceased
- 1998-03-12 CZ CZ0319199A patent/CZ296647B6/en not_active IP Right Cessation
- 1998-03-12 PL PL335672A patent/PL192786B1/en not_active IP Right Cessation
- 1998-03-12 TR TR1999/02508T patent/TR199902508T2/en unknown
- 1998-03-12 CN CNB988045389A patent/CN1179948C/en not_active Expired - Fee Related
- 1998-03-12 CA CA002284163A patent/CA2284163A1/en not_active Abandoned
- 1998-03-12 MY MYPI98001071A patent/MY117535A/en unknown
- 1998-03-13 CO CO98014251A patent/CO4940496A1/en unknown
- 1998-03-13 PA PA19988448801A patent/PA8448801A1/en unknown
- 1998-03-13 SV SV1998000038A patent/SV1998000038A/en not_active Application Discontinuation
- 1998-04-21 SA SA98181116A patent/SA98181116B1/en unknown
- 1998-12-03 UA UA99095049A patent/UA57772C2/en unknown
-
1999
- 1999-09-10 NO NO19994415A patent/NO315555B1/en not_active IP Right Cessation
- 1999-09-10 IL IL131870A patent/IL131870A/en not_active IP Right Cessation
- 1999-09-10 IS IS5176A patent/IS5176A/en unknown
- 1999-09-13 OA OA9900207A patent/OA11196A/en unknown
- 1999-09-13 BG BG103727A patent/BG63540B1/en unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD9A | Lapse of provisional protection due to non-payment of fees |