YU49439B - Benzoksazinoni kao inhibitori hiv reverzne transkriptaze - Google Patents
Benzoksazinoni kao inhibitori hiv reverzne transkriptazeInfo
- Publication number
- YU49439B YU49439B YU53093A YU53093A YU49439B YU 49439 B YU49439 B YU 49439B YU 53093 A YU53093 A YU 53093A YU 53093 A YU53093 A YU 53093A YU 49439 B YU49439 B YU 49439B
- Authority
- YU
- Yugoslavia
- Prior art keywords
- reverse transcriptase
- benzoxazinones
- hiv
- inhibitors
- hiv reverse
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
- C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
- C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
- C07D265/18—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in position 2
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
-
- 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
- A61P27/00—Drugs for disorders of the senses
-
- 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
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
-
- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Transplantation (AREA)
- AIDS & HIV (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Heat Sensitive Colour Forming Recording (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Primena jedinjenja formule II gde, X je halo; X1 je trihalometil; pentahaloetil; C2-5 alkil; C2-5 alkinil; C3-5 cikloalkil; ili fenil, naftil, tetrahidronaftil, bifenil, fenetil, antril ili acenaftil; Z je O ili S; R je (a) C1-8 alkil, nesupstituisan ili supstituisan sa A, a A je halo, C3-6 cikloalkil, CN, hidroksi, C1-4 alkoksi, C2-4 alkinil-C1-4 alkoksi, fenoksi, naftoksi, tetrahidronaftoksi, bifenoksi, fenetoksi, antroksi, acenaftoksi, C1-4 alkilkarbonil, nitro, di(C1-2 alkil)amino, C1-4 alkilamino-C1-2 alkil, heterociklican prsten, ili feniltio, naftiltio, tetrahidronaftiltio, bifeniltio, fenetiltio, antriltio ili acenaftiltio; gde heterociklican prsten oznacava stabilan 5- do 7-clani monociklican ili stabilan 8- do 11-clani biciklican heterociklican prsten koji je ili nezasicen, delimicno nezasicen ili zasicen i koji se sastoji od ugljenikovih atoma i od jednog do cetiri heteroatoma koji su izabrani od N, O i S, gde heteroatomi azota i sumpora mogu biti izborno oksidovani, a ukljucujuci tu i bilo koju biciklicnu grupu u kojoj je bilo koji od prethodno odredjenih heterociklicnih prstenova fuzionisan za benzenov prsten; (b) C2-4 alkenil, nesupstituisan ili supstituisan sa (i) A, ili (c) C2-5 alkinil, nesupstituisan ili supstituisan sa (i) A, ili (ii) fenil, naftil, tetrahidronaftnil, bifenil, fenetil, antril ili acenaftil, nesupstituisan ili supstituisan sa A; ili (d) C3-4 cikloalkil, nesupstituisan ili supstituisan sa (i) A; ili (ii) fenil, naftil, tetrahidronaftil, bifenil, fenetil, antril ili acenaftil, nesupstituisan ili supstituisan sa A, ili njegove farmaceutski prihvatljive soli, naznacena time, sto se koristi za pripremanje leka za inhibiciju HIV reverzne transkriptaze, za prevenciju HIV infekcije, za lecenje infekcije izazvane HIV-om, ili za lecenje SIDA-e ili ARC-a. Prijava sadrzi jos 11 nezavisna i 5 zavisna patentna zatheva.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US92660792A | 1992-08-07 | 1992-08-07 | |
| US5480593A | 1993-04-27 | 1993-04-27 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| YU53093A YU53093A (sh) | 1996-10-09 |
| YU49439B true YU49439B (sh) | 2006-03-03 |
Family
ID=26733517
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| YU53093A YU49439B (sh) | 1992-08-07 | 1993-08-05 | Benzoksazinoni kao inhibitori hiv reverzne transkriptaze |
Country Status (37)
| Country | Link |
|---|---|
| EP (1) | EP0582455B1 (sh) |
| JP (1) | JPH0780860B2 (sh) |
| KR (1) | KR100272387B1 (sh) |
| CN (3) | CN1318031C (sh) |
| AT (1) | ATE197295T1 (sh) |
| AU (1) | AU670300B2 (sh) |
| BG (1) | BG62612B1 (sh) |
| CA (1) | CA2101572C (sh) |
| CZ (1) | CZ290447B6 (sh) |
| DE (4) | DE10199013I1 (sh) |
| DK (1) | DK0582455T3 (sh) |
| DZ (1) | DZ1707A1 (sh) |
| ES (1) | ES2151897T3 (sh) |
| FI (1) | FI115457B (sh) |
| GR (1) | GR3034754T3 (sh) |
| HK (1) | HK1009267A1 (sh) |
| HR (1) | HRP931102B1 (sh) |
| HU (1) | HU223076B1 (sh) |
| IL (1) | IL106507A (sh) |
| LU (2) | LU90709I2 (sh) |
| LV (1) | LV12719B (sh) |
| MX (1) | MX192812B (sh) |
| MY (1) | MY109834A (sh) |
| NL (2) | NL300032I2 (sh) |
| NO (3) | NO304886B1 (sh) |
| NZ (1) | NZ255216A (sh) |
| PL (2) | PL175615B1 (sh) |
| PT (1) | PT582455E (sh) |
| RO (1) | RO113641B1 (sh) |
| RU (1) | RU2186775C2 (sh) |
| SG (1) | SG52698A1 (sh) |
| SI (1) | SI9300419B (sh) |
| SK (1) | SK282276B6 (sh) |
| TW (2) | TWI233436B (sh) |
| UA (1) | UA42699C2 (sh) |
| WO (1) | WO1994003440A1 (sh) |
| YU (1) | YU49439B (sh) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5633405A (en) * | 1995-05-25 | 1997-05-27 | Merck & Co., Inc. | Asymmetric synthesis of (-)-6-chloro-4-cyclopropyl-ethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxanzin-2-one |
| US6147210A (en) * | 1996-07-26 | 2000-11-14 | Dupont Pharmaceuticals Company | Practical synthesis of benzoxazinones useful as HIV reverse transcriptase inhibitors |
| WO1998004535A1 (en) * | 1996-07-26 | 1998-02-05 | Du Pont Pharmaceuticals Company | A practical synthesis of benzoxazinones useful as hiv reverse transcriptase inhibitors |
| US5932726A (en) * | 1996-12-16 | 1999-08-03 | Dupont Pharmaceuticals Company | Asymmetric synthesis of benzoxazinones |
| ZA9711256B (en) | 1996-12-16 | 1999-06-15 | Du Pont Merck Pharma | Asymmetric synthesis of benzoxazinones |
| PL197740B1 (pl) * | 1997-02-05 | 2008-04-30 | Merck & Co Inc | Postać krystaliczna I (-)-6-chloro-4-cyklopropyloetynylo-4-trifluorometylo-1,4-dihydro-2H-3,1-benzoksazyn-2-onu i sposób krystalizacji postaci I (-)-6-chloro-4-cyklopropylo-etynylo-4-trifluorometylo-1,4-dihydro-2H-3,1-benzoksazyn-2-onu |
| US5965729A (en) | 1997-02-05 | 1999-10-12 | Merck & Co., Inc. | Process for the crystallization of a reverse transcriptase inhibitor using an anti-solvent |
| CA2285000A1 (en) * | 1997-04-07 | 1998-10-15 | Dupont Pharmaceuticals Company | Asymmetric synthesis of benzoxazinones via new intermediates |
| US6124302A (en) | 1997-04-09 | 2000-09-26 | Dupont Pharmaceuticals | 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones useful as HIV reverse transcriptase inhibitors |
| US5952528A (en) * | 1997-09-03 | 1999-09-14 | Merck & Co., Inc. | Process for enhancing the optical purity |
| JP4157272B2 (ja) * | 1997-09-03 | 2008-10-01 | メルク エンド カムパニー インコーポレーテッド | ２ｒ−［１−ヒドロキシ−１−トリフルオロメチル−３−シクロプロピルプロピン−２−イル］−４−クロロアニリンの光学純度を高める方法 |
| US20010014352A1 (en) | 1998-05-27 | 2001-08-16 | Udit Batra | Compressed tablet formulation |
| HRP990182A2 (en) * | 1998-06-11 | 2000-02-29 | Du Pont Pharm Co | Crystalline efavirenz |
| US6673372B1 (en) | 1998-06-11 | 2004-01-06 | Bristol-Myers Squibb Pharma Company | Crystalline Efavirenz |
| EP1091939A1 (en) * | 1998-06-30 | 2001-04-18 | Du Pont Pharmaceuticals Company | Substituted quinolin-2(1h)-ones useful as hiv reverse transcriptase inhibitors |
| SE9904652D0 (sv) * | 1999-12-17 | 1999-12-17 | Astra Pharma Prod | Novel Compounds |
| UA73119C2 (en) | 2000-04-19 | 2005-06-15 | American Home Products Corpoir | Derivatives of cyclic thiocarbamates, pharmaceutical composition including noted derivatives of cyclic thiocarbamates and active ingredients of medicines as modulators of progesterone receptors |
| WO2002081456A1 (en) | 2001-03-28 | 2002-10-17 | Bristol-Myers Squibb Company | Cyanamide, alkoxyamino, and urea derivatives of 4, 4-disubstituted-3, 4-dihydro-2 (1h)- quinazolinones as hiv reverse transcriptase inhibitors |
| EP1608629A1 (en) | 2003-03-24 | 2005-12-28 | F. Hoffmann-La Roche Ag | Benzyl-pyridazinons as reverse transcriptase inhibitors |
| ES2549084T3 (es) * | 2007-10-05 | 2015-10-22 | Msd K.K. | Derivados de benzoxazinona |
| GB0720503D0 (en) | 2007-10-22 | 2007-11-28 | Angeletti P Ist Richerche Bio | New compound |
| EP2448917A2 (de) | 2009-07-03 | 2012-05-09 | Archimica GmbH | Verfahren zur enantioselektiven addition von organometallischen kohlenstoffnukleophilen an trifluormethylketone und verwendung des verfahrens in der synthese von hiv reverse transcriptase inhibitoren |
| KR20170078868A (ko) | 2010-01-27 | 2017-07-07 | 비이브 헬쓰케어 컴퍼니 | 항바이러스 치료 |
| EP2471783A1 (en) | 2010-12-23 | 2012-07-04 | Esteve Química, S.A. | Novel polymorphic form of efavirenz |
| CN103664816B (zh) * | 2011-01-06 | 2016-03-02 | 中国科学院上海有机化学研究所 | Hiv逆转录酶抑制剂依法韦伦类化合物的一锅法不对称合成工艺 |
| CN102675125B (zh) * | 2011-03-15 | 2015-02-18 | 中国科学院上海有机化学研究所 | 一种4-氯-2-三氟乙酰基苯胺及其类似物的简便高效合成方法 |
| JP7071036B2 (ja) | 2019-02-15 | 2022-05-18 | 福建永晶科技股▲ふん▼有限公司 | Ｆｒｉｅｄｅｌ－Ｃｒａｆｔｓ反応の新しい新方法及び当該方法に用いられる触媒 |
| CN110372625B (zh) * | 2019-08-06 | 2022-11-01 | 常州大学 | 蓝光照射制备4-烷甲基-4-芳基-1,3-苯并噁嗪-2(4h)-酮的方法 |
| CN113106473B (zh) * | 2021-04-14 | 2022-02-18 | 南京工业大学 | 一种通过连续电化学微反应器装置制备1,3-苯并噁嗪衍生物的方法 |
| WO2023064196A1 (en) * | 2021-10-15 | 2023-04-20 | Merck Sharp & Dohme Llc | Benzoxazinone derivatives as selective cytotoxic agents |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3526621A (en) * | 1966-08-03 | 1970-09-01 | Farmaceutical Italia Soc | Substituted 3,1-benzoxazin-2-one |
| US3562621A (en) * | 1967-07-26 | 1971-02-09 | Technipower Inc | Inrush current limiting circuit for rectifier circuits with capacitive load |
| DE3217012A1 (de) * | 1982-05-06 | 1983-11-10 | Dr. Karl Thomae Gmbh, 7950 Biberach | Benzoxazin-2-one, deren herstellung und diese verbindungen enthaltende arzneimittel |
| CA2032259A1 (en) * | 1989-12-18 | 1991-06-19 | Wayne J. Thompson | Hiv protease inhibitors useful for the treatment of aids |
| IL99843A0 (en) * | 1990-11-01 | 1992-08-18 | Merck & Co Inc | Synergistic combination of hiv reverse transcriptase inhibitors |
-
1993
- 1993-07-28 IL IL106507A patent/IL106507A/xx not_active IP Right Cessation
- 1993-07-29 CA CA002101572A patent/CA2101572C/en not_active Expired - Lifetime
- 1993-08-03 DE DE2001199013 patent/DE10199013I1/de active Pending
- 1993-08-03 EP EP93306114A patent/EP0582455B1/en not_active Expired - Lifetime
- 1993-08-03 MY MYPI93001523A patent/MY109834A/en unknown
- 1993-08-03 DE DE122008000034C patent/DE122008000034I1/de active Pending
- 1993-08-03 DK DK93306114T patent/DK0582455T3/da active
- 1993-08-03 SG SG1996008032A patent/SG52698A1/en unknown
- 1993-08-03 PT PT93306114T patent/PT582455E/pt unknown
- 1993-08-03 ES ES93306114T patent/ES2151897T3/es not_active Expired - Lifetime
- 1993-08-03 AT AT93306114T patent/ATE197295T1/de active
- 1993-08-03 DE DE69329608T patent/DE69329608T2/de not_active Expired - Lifetime
- 1993-08-03 DE DE1993629608 patent/DE10199013I2/de active Active
- 1993-08-04 TW TW088117982A patent/TWI233436B/zh not_active IP Right Cessation
- 1993-08-04 DZ DZ930090A patent/DZ1707A1/fr active
- 1993-08-04 TW TW082106237A patent/TW382014B/zh not_active IP Right Cessation
- 1993-08-05 YU YU53093A patent/YU49439B/sh unknown
- 1993-08-05 MX MX9304775A patent/MX192812B/es not_active IP Right Cessation
- 1993-08-05 JP JP5194727A patent/JPH0780860B2/ja not_active Expired - Lifetime
- 1993-08-06 SI SI9300419A patent/SI9300419B/sl unknown
- 1993-08-06 CN CNB991181085A patent/CN1318031C/zh not_active Expired - Lifetime
- 1993-08-06 WO PCT/US1993/007376 patent/WO1994003440A1/en active IP Right Grant
- 1993-08-06 PL PL93307348A patent/PL175615B1/pl unknown
- 1993-08-06 CN CN93117660A patent/CN1051767C/zh not_active Expired - Lifetime
- 1993-08-06 SK SK161-95A patent/SK282276B6/sk active Protection Beyond IP Right Term
- 1993-08-06 CZ CZ1995286A patent/CZ290447B6/cs not_active IP Right Cessation
- 1993-08-06 AU AU44496/93A patent/AU670300B2/en not_active Expired
- 1993-08-06 RO RO95-00190A patent/RO113641B1/ro unknown
- 1993-08-06 NZ NZ255216A patent/NZ255216A/en not_active IP Right Cessation
- 1993-08-06 HU HU9500366A patent/HU223076B1/hu active Protection Beyond IP Right Term
- 1993-08-06 PL PL93325950A patent/PL176679B1/pl unknown
- 1993-08-06 HR HR931102A patent/HRP931102B1/xx not_active IP Right Cessation
- 1993-08-06 UA UA95028099A patent/UA42699C2/uk unknown
- 1993-08-06 RU RU95107403/04A patent/RU2186775C2/ru active
- 1993-08-06 KR KR1019950700472A patent/KR100272387B1/ko not_active IP Right Cessation
-
1995
- 1995-01-30 BG BG99383A patent/BG62612B1/bg unknown
- 1995-02-06 FI FI950508A patent/FI115457B/fi not_active IP Right Cessation
- 1995-02-06 NO NO950424A patent/NO304886B1/no active Protection Beyond IP Right Term
-
1998
- 1998-08-12 HK HK98109866A patent/HK1009267A1/xx not_active IP Right Cessation
- 1998-10-10 CN CN98121309A patent/CN1107505C/zh not_active Expired - Lifetime
-
2000
- 2000-06-16 NO NO2000004C patent/NO2000004I1/no unknown
- 2000-11-03 GR GR20000402341T patent/GR3034754T3/el unknown
- 2000-12-08 NL NL300032C patent/NL300032I2/nl unknown
- 2000-12-20 LU LU90709C patent/LU90709I2/fr unknown
-
2001
- 2001-06-01 LV LVP-01-87A patent/LV12719B/lv unknown
-
2008
- 2008-05-15 NL NL300347C patent/NL300347I1/nl unknown
- 2008-05-27 LU LU91446C patent/LU91446I2/fr unknown
- 2008-06-12 NO NO2008008C patent/NO2008008I1/no unknown
Also Published As
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