HUP0302862A2 - HIV reverz transzkriptáz inhibitorokként alkalmazható triciklikus 2-piridon-származékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények - Google Patents
HIV reverz transzkriptáz inhibitorokként alkalmazható triciklikus 2-piridon-származékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0302862A2 HUP0302862A2 HU0302862A HUP0302862A HUP0302862A2 HU P0302862 A2 HUP0302862 A2 HU P0302862A2 HU 0302862 A HU0302862 A HU 0302862A HU P0302862 A HUP0302862 A HU P0302862A HU P0302862 A2 HUP0302862 A2 HU P0302862A2
- Authority
- HU
- Hungary
- Prior art keywords
- general formula
- group
- carbonyl
- nitrogen atom
- reverse transcriptase
- Prior art date
Links
- 108010078851 HIV Reverse Transcriptase Proteins 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- UBQKCCHYAOITMY-UHFFFAOYSA-N pyridin-2-ol Chemical class OC1=CC=CC=N1 UBQKCCHYAOITMY-UHFFFAOYSA-N 0.000 title abstract 2
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 6
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 abstract 1
- 239000013067 intermediate product Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- -1 phenyl-amino-carbonyl- Chemical group 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 239000011593 sulfur Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
- A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Communicable Diseases (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
A találmány tárgyát a HIV-reverz transzkriptáz inhibitoraikénthasználható általános képletű triciklusos piridonszármazékok - ahol Aegy általános képletű gyűrű; P jelentése oxigén- vagy kénatom; Wnitrogénatom vagy CR3 általános képletű csoport; X nitrogénatom vagyCR3a általános képletű csoport; Y nitrogénatom vagy CR3b általánosképletű csoport; Z nitrogénatom vagy CR3c általános képletű csoport;azzal a feltétellel, hogy ha W, X, Y és Z közül kettőnek a jelentésenitrogénatom, akkor a többi szubsztituens nitrogénatomtól eltérőjelentésű; R1 adott esetben halogénatommal szubsztituált alkilcsoport,ciklopropil-, hidroxi-metil- vagy cianocsoport; R2 adott esetbenszubsztituált alkil-, alkenil-, alkinil-, cikloalkil-, fenilcsoportvagy heterogyűrű; R8 hidrogénatom, alkil-karbonil-, alkoxi-, alkoxi-karbonil-, aril-oxi-, aril-oxi-karbonil-, aril-metil-karbonil-,(alkilkarbonil-oxi)-karbonil-, (aril-karbonil-oxi)-(alkoxi-karbonil)-,alkil-amino-karbonil-, fenil-amino-karbonil-, fenil-alkoxi-karbonil-vagy -NR5R5a-alkil-karbonilcsoport - ezeket tartalmazógyógyszerkészítmények és készletek, alkalmazásuk, valamint avegyületek előállítására szolgáló eljárások és azok közbenső termékeiképezik. Ó
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US21953200P | 2000-07-20 | 2000-07-20 | |
| US28485601P | 2001-04-19 | 2001-04-19 | |
| PCT/US2001/022827 WO2002008226A2 (en) | 2000-07-20 | 2001-07-20 | Tricyclic 2-pyridone compounds useful as hiv reverse transcriptase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HUP0302862A2 true HUP0302862A2 (hu) | 2003-12-29 |
Family
ID=26913986
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0302862A HUP0302862A2 (hu) | 2000-07-20 | 2001-07-20 | HIV reverz transzkriptáz inhibitorokként alkalmazható triciklikus 2-piridon-származékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US6596729B2 (hu) |
| EP (1) | EP1303515A2 (hu) |
| JP (1) | JP2004532793A (hu) |
| KR (1) | KR20030065454A (hu) |
| CN (1) | CN1464878A (hu) |
| AR (1) | AR031861A1 (hu) |
| AU (1) | AU2001280641A1 (hu) |
| BG (1) | BG107439A (hu) |
| BR (1) | BR0112606A (hu) |
| CA (1) | CA2418194A1 (hu) |
| EE (1) | EE200300027A (hu) |
| HU (1) | HUP0302862A2 (hu) |
| IL (1) | IL153683A0 (hu) |
| IS (1) | IS6690A (hu) |
| LT (1) | LT2003003A (hu) |
| LV (1) | LV13024B (hu) |
| MX (1) | MXPA03000434A (hu) |
| NO (1) | NO20030248L (hu) |
| PL (1) | PL365958A1 (hu) |
| SI (1) | SI21139A (hu) |
| SK (1) | SK392003A3 (hu) |
| WO (1) | WO2002008226A2 (hu) |
| YU (1) | YU3203A (hu) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8101629B2 (en) | 2001-08-13 | 2012-01-24 | Janssen Pharmaceutica N.V. | Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile |
| US7638522B2 (en) | 2001-08-13 | 2009-12-29 | Janssen Pharmaceutica N.V. | Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino] benzonitrile |
| JO3429B1 (ar) | 2001-08-13 | 2019-10-20 | Janssen Pharmaceutica Nv | مشتقات برميدينات مثبطة فيروس الايدز |
| TW200306192A (en) | 2002-01-18 | 2003-11-16 | Bristol Myers Squibb Co | Tricyclic 2-pyrimidone compounds useful as HIV reverse transcriptase inhibitors |
| AR039540A1 (es) | 2002-05-13 | 2005-02-23 | Tibotec Pharm Ltd | Compuestos microbicidas con contenido de pirimidina o triazina |
| KR101086678B1 (ko) * | 2002-08-09 | 2011-11-25 | 얀센 파마슈티카 엔.브이. | 4-[[4-[[4-(2-시아노에테닐)-2,6-디메틸페닐]아미노]-2-피리미디닐]아미노]벤조니트릴의 제조방법 |
| ES2598404T3 (es) * | 2003-02-07 | 2017-01-27 | Janssen Pharmaceutica Nv | Derivados de pirimidina para la prevención de infección por el VIH |
| BRPI0511175A (pt) | 2004-05-17 | 2007-12-04 | Tibotec Pharm Ltd | 1-hetero-ciclil-1,5-diidro-pirido[3,2-b]indol-2-onas |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3700673A (en) * | 1971-02-12 | 1972-10-24 | Morton Norwich Products Inc | 3-4-dihydrobenzo(b) (1,7)naphthyridin-1(2h)-ones |
| GB9023289D0 (en) | 1990-10-25 | 1990-12-05 | Ici Plc | Herbicides |
| IL102764A0 (en) | 1991-08-16 | 1993-01-31 | Merck & Co Inc | Quinazoline derivatives,and pharmaceutical compositions containing them |
| WO1993004047A1 (en) * | 1991-08-16 | 1993-03-04 | Merck & Co., Inc. | Quinazoline derivatives as inhibitors of hiv reverse transcriptase |
| DE4320347A1 (de) | 1993-06-19 | 1994-12-22 | Boehringer Mannheim Gmbh | Quinazolin-Derivate und diese enthaltende Arzneimittel |
| AU1046895A (en) | 1993-11-05 | 1995-05-23 | Merck & Co., Inc. | New quinazolines as inhibitors of hiv reverse transcriptase |
| DE4344452A1 (de) | 1993-12-24 | 1995-06-29 | Hoechst Ag | Aza-4-iminochinoline, Verfahren zu ihrer Herstellung und ihre Verwendung |
| ID18046A (id) | 1996-08-20 | 1998-02-19 | Takeda Chemical Industries Ltd | Senyawa siklik campuran, pembuatan dan penngunaannya. |
| EP0929533B1 (en) | 1996-10-02 | 2003-09-03 | Bristol-Myers Squibb Pharma Company | 4,4-disubstituted-1,4-dihydro-2h-3,1-benzoxazin-2-ones useful as hiv reverse transcriptase inhibitors and intermediates and processes for making the same |
| HRP980143A2 (en) | 1997-04-09 | 1999-02-28 | Soo Sung Ko | 4,4-disubstituted-3,4-dihydro-2 (1h)-quinazolinones useful as hiv reverse transcriptase inhibitors |
| US6593337B1 (en) | 1999-10-19 | 2003-07-15 | Bristol-Myers Squibb Pharma Company | Tricyclic compounds useful as HIV reverse transcriptase inhibitors |
-
2001
- 2001-07-19 US US09/908,995 patent/US6596729B2/en not_active Expired - Lifetime
- 2001-07-20 EP EP01959047A patent/EP1303515A2/en not_active Withdrawn
- 2001-07-20 EE EEP200300027A patent/EE200300027A/xx unknown
- 2001-07-20 HU HU0302862A patent/HUP0302862A2/hu unknown
- 2001-07-20 JP JP2002514132A patent/JP2004532793A/ja active Pending
- 2001-07-20 SI SI200120050A patent/SI21139A/sl not_active IP Right Cessation
- 2001-07-20 PL PL01365958A patent/PL365958A1/xx not_active Application Discontinuation
- 2001-07-20 MX MXPA03000434A patent/MXPA03000434A/es unknown
- 2001-07-20 YU YU3203A patent/YU3203A/sh unknown
- 2001-07-20 CN CN01815629A patent/CN1464878A/zh active Pending
- 2001-07-20 SK SK39-2003A patent/SK392003A3/sk unknown
- 2001-07-20 AU AU2001280641A patent/AU2001280641A1/en not_active Abandoned
- 2001-07-20 AR ARP010103492A patent/AR031861A1/es unknown
- 2001-07-20 BR BR0112606-7A patent/BR0112606A/pt not_active Application Discontinuation
- 2001-07-20 CA CA002418194A patent/CA2418194A1/en not_active Abandoned
- 2001-07-20 KR KR10-2003-7000800A patent/KR20030065454A/ko not_active Application Discontinuation
- 2001-07-20 WO PCT/US2001/022827 patent/WO2002008226A2/en not_active Application Discontinuation
- 2001-07-20 IL IL15368301A patent/IL153683A0/xx unknown
-
2003
- 2003-01-06 BG BG107439A patent/BG107439A/bg unknown
- 2003-01-15 LT LT2003003A patent/LT2003003A/xx not_active Application Discontinuation
- 2003-01-17 IS IS6690A patent/IS6690A/is unknown
- 2003-01-17 NO NO20030248A patent/NO20030248L/no not_active Application Discontinuation
- 2003-02-18 LV LVP-03-16A patent/LV13024B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US6596729B2 (en) | 2003-07-22 |
| EP1303515A2 (en) | 2003-04-23 |
| SI21139A (sl) | 2003-08-31 |
| EE200300027A (et) | 2004-10-15 |
| NO20030248L (no) | 2003-03-17 |
| WO2002008226A2 (en) | 2002-01-31 |
| SK392003A3 (en) | 2003-10-07 |
| LV13024B (en) | 2003-10-20 |
| IS6690A (is) | 2003-01-17 |
| BR0112606A (pt) | 2004-06-29 |
| CA2418194A1 (en) | 2002-01-31 |
| AU2001280641A1 (en) | 2002-02-05 |
| PL365958A1 (en) | 2005-01-24 |
| NO20030248D0 (no) | 2003-01-17 |
| CN1464878A (zh) | 2003-12-31 |
| IL153683A0 (en) | 2003-07-06 |
| AR031861A1 (es) | 2003-10-08 |
| US20020107261A1 (en) | 2002-08-08 |
| WO2002008226A3 (en) | 2002-06-20 |
| BG107439A (bg) | 2003-09-30 |
| YU3203A (sh) | 2006-01-16 |
| MXPA03000434A (es) | 2003-06-24 |
| JP2004532793A (ja) | 2004-10-28 |
| LT2003003A (en) | 2003-11-25 |
| KR20030065454A (ko) | 2003-08-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD9A | Lapse of provisional protection due to non-payment of fees |