BG62612B1 - Съединения, фармацевтични състави и методи за инхибиране наhiv обратна транскриптаза и за лечение на hiv инфекции, спин илиarc и методи за получаване на съединенията - Google Patents

Съединения, фармацевтични състави и методи за инхибиране наhiv обратна транскриптаза и за лечение на hiv инфекции, спин илиarc и методи за получаване на съединенията Download PDF

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Publication number
BG62612B1
BG62612B1 BG99383A BG9938395A BG62612B1 BG 62612 B1 BG62612 B1 BG 62612B1 BG 99383 A BG99383 A BG 99383A BG 9938395 A BG9938395 A BG 9938395A BG 62612 B1 BG62612 B1 BG 62612B1
Authority
BG
Bulgaria
Prior art keywords
substituted
unsubstituted
chloro
hiv
aids
Prior art date
Application number
BG99383A
Other languages
Bulgarian (bg)
English (en)
Other versions
BG99383A (bg
Inventor
Steven D. Young
Susan F. Britcher
Linda S. Payne
Lekhanh O. Tran
William C. Lumma Jun.
Original Assignee
Merck & Co.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26733517&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BG62612(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck & Co. filed Critical Merck & Co.
Publication of BG99383A publication Critical patent/BG99383A/bg
Publication of BG62612B1 publication Critical patent/BG62612B1/bg

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/041,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/121,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C07D265/141,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D265/181,3-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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs 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)
BG99383A 1992-08-07 1995-01-30 Съединения, фармацевтични състави и методи за инхибиране наhiv обратна транскриптаза и за лечение на hiv инфекции, спин илиarc и методи за получаване на съединенията BG62612B1 (bg)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US92660792A 1992-08-07 1992-08-07
US5480593A 1993-04-27 1993-04-27
PCT/US1993/007376 WO1994003440A1 (fr) 1992-08-07 1993-08-06 Benzoxazinones en tant qu'inhibiteurs de la transcriptase inverse du vih

Publications (2)

Publication Number Publication Date
BG99383A BG99383A (bg) 1995-09-29
BG62612B1 true BG62612B1 (bg) 2000-03-31

Family

ID=26733517

Family Applications (1)

Application Number Title Priority Date Filing Date
BG99383A BG62612B1 (bg) 1992-08-07 1995-01-30 Съединения, фармацевтични състави и методи за инхибиране наhiv обратна транскриптаза и за лечение на hiv инфекции, спин илиarc и методи за получаване на съединенията

Country Status (37)

Country Link
EP (1) EP0582455B1 (fr)
JP (1) JPH0780860B2 (fr)
KR (1) KR100272387B1 (fr)
CN (3) CN1318031C (fr)
AT (1) ATE197295T1 (fr)
AU (1) AU670300B2 (fr)
BG (1) BG62612B1 (fr)
CA (1) CA2101572C (fr)
CZ (1) CZ290447B6 (fr)
DE (4) DE10199013I1 (fr)
DK (1) DK0582455T3 (fr)
DZ (1) DZ1707A1 (fr)
ES (1) ES2151897T3 (fr)
FI (1) FI115457B (fr)
GR (1) GR3034754T3 (fr)
HK (1) HK1009267A1 (fr)
HR (1) HRP931102B1 (fr)
HU (1) HU223076B1 (fr)
IL (1) IL106507A (fr)
LU (2) LU90709I2 (fr)
LV (1) LV12719B (fr)
MX (1) MX192812B (fr)
MY (1) MY109834A (fr)
NL (2) NL300032I2 (fr)
NO (3) NO304886B1 (fr)
NZ (1) NZ255216A (fr)
PL (2) PL175615B1 (fr)
PT (1) PT582455E (fr)
RO (1) RO113641B1 (fr)
RU (1) RU2186775C2 (fr)
SG (1) SG52698A1 (fr)
SI (1) SI9300419B (fr)
SK (1) SK282276B6 (fr)
TW (2) TWI233436B (fr)
UA (1) UA42699C2 (fr)
WO (1) WO1994003440A1 (fr)
YU (1) YU49439B (fr)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
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 (fr) * 1996-07-26 1998-02-05 Du Pont Pharmaceuticals Company Synthese pratique de benzoxazinones utiles comme inhibiteurs de la transcriptase inverse du vih
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 (fr) * 1997-04-07 1998-10-15 Dupont Pharmaceuticals Company Synthese asymetrique de benzoxazinones via de nouveaux intermediaires
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 (fr) * 1998-06-30 2001-04-18 Du Pont Pharmaceuticals Company Quinoline-2(1h)-ones substituees utiles comme inhibiteurs de la transcriptase inverse du vih
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 (fr) 2001-03-28 2002-10-17 Bristol-Myers Squibb Company Cyanamide, alcoxyamino, et derives uree de quinazolinones 4, 4-bisubstituees-3, 4-dihydro-2 (1h)- utiles en tant qu'inhibiteurs de la transcriptase inverse du vih
EP1608629A1 (fr) 2003-03-24 2005-12-28 F. Hoffmann-La Roche Ag Benzyl-pyridazinones en tant qu inhibiteurs de transcriptase inverse
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 (fr) 2009-07-03 2012-05-09 Archimica GmbH Procédé d addition énantiosélective de nucléophiles carbonés organométalliques sur des trifluorométhylcétones et utilisation du procédé dans la synthèse d inhibiteurs de la transcriptase inverse du vih
KR20170078868A (ko) 2010-01-27 2017-07-07 비이브 헬쓰케어 컴퍼니 항바이러스 치료
EP2471783A1 (fr) 2010-12-23 2012-07-04 Esteve Química, S.A. Nouvelle forme polymorphe de l'éfavirenz
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 (fr) * 2021-10-15 2023-04-20 Merck Sharp & Dohme Llc Dérivés de benzoxazinone utilisés comme agents cytotoxiques sélectifs

Family Cites Families (5)

* Cited by examiner, † Cited by third party
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 (fr) * 1989-12-18 1991-06-19 Wayne J. Thompson Inhibiteurs de la protease du vih utiles dans le traitement du sida
IL99843A0 (en) * 1990-11-01 1992-08-18 Merck & Co Inc Synergistic combination of hiv reverse transcriptase inhibitors

Also Published As

Publication number Publication date
YU53093A (sh) 1996-10-09
ES2151897T3 (es) 2001-01-16
HRP931102B1 (en) 2001-06-30
LV12719A (lv) 2001-09-20
DE69329608D1 (de) 2000-12-07
JPH06184124A (ja) 1994-07-05
NZ255216A (en) 1996-05-28
AU4449693A (en) 1994-02-10
NO2008008I1 (no) 2008-06-30
CN1318031C (zh) 2007-05-30
CA2101572A1 (fr) 1994-02-08
CN1250652A (zh) 2000-04-19
NO950424D0 (no) 1995-02-06
EP0582455B1 (fr) 2000-11-02
WO1994003440A1 (fr) 1994-02-17
LV12719B (lv) 2001-12-20
DE10199013I1 (de) 2001-05-23
JPH0780860B2 (ja) 1995-08-30
DZ1707A1 (fr) 2002-02-17
IL106507A0 (en) 1993-11-15
FI950508A0 (fi) 1995-02-06
NO2000004I1 (no) 2000-06-16
CN1090277A (zh) 1994-08-03
RU2186775C2 (ru) 2002-08-10
KR950702970A (ko) 1995-08-23
HRP931102A2 (en) 1997-10-31
SG52698A1 (en) 1998-09-28
MX192812B (es) 1999-07-30
CA2101572C (fr) 2001-08-28
KR100272387B1 (ko) 2000-11-15
CN1107505C (zh) 2003-05-07
YU49439B (sh) 2006-03-03
CN1221608A (zh) 1999-07-07
TW382014B (en) 2000-02-11
DE122008000034I1 (de) 2008-10-02
DE10199013I2 (de) 2007-05-24
LU90709I2 (fr) 2002-02-04
BG99383A (bg) 1995-09-29
FI115457B (fi) 2005-05-13
GR3034754T3 (en) 2001-02-28
HUT71219A (en) 1995-11-28
SI9300419A (en) 1994-06-30
PL176679B1 (pl) 1999-07-30
HU223076B1 (hu) 2004-03-01
MX9304775A (es) 1994-05-31
DE69329608T2 (de) 2001-05-03
IL106507A (en) 1997-11-20
RO113641B1 (ro) 1998-09-30
CZ290447B6 (cs) 2002-07-17
UA42699C2 (uk) 2001-11-15
RU95107403A (ru) 1996-11-20
SK16195A3 (en) 1995-07-11
SI9300419B (sl) 2002-10-31
SK282276B6 (sk) 2002-01-07
ATE197295T1 (de) 2000-11-15
NL300347I1 (nl) 2008-07-01
AU670300B2 (en) 1996-07-11
FI950508A (fi) 1995-02-06
NL300032I1 (fr) 2001-02-01
CN1051767C (zh) 2000-04-26
MY109834A (en) 1997-08-30
PT582455E (pt) 2001-03-30
EP0582455A1 (fr) 1994-02-09
NO950424L (no) 1995-04-06
NO304886B1 (no) 1999-03-01
CZ28695A3 (en) 1995-09-13
HU9500366D0 (en) 1995-03-28
PL175615B1 (pl) 1999-01-29
LU91446I2 (fr) 2008-07-28
TWI233436B (en) 2005-06-01
PL307348A1 (en) 1995-05-15
DK0582455T3 (da) 2000-11-27
HK1009267A1 (en) 1999-05-28
NL300032I2 (nl) 2001-04-02

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