KR920702682A - 1, 3-옥사티오란 뉴클레오시드 동족체 - Google Patents

1, 3-옥사티오란 뉴클레오시드 동족체

Info

Publication number
KR920702682A
KR920702682A KR1019910702025A KR910702025A KR920702682A KR 920702682 A KR920702682 A KR 920702682A KR 1019910702025 A KR1019910702025 A KR 1019910702025A KR 910702025 A KR910702025 A KR 910702025A KR 920702682 A KR920702682 A KR 920702682A
Authority
KR
South Korea
Prior art keywords
compound
enantiomer
enzyme
amount
present
Prior art date
Application number
KR1019910702025A
Other languages
English (en)
Other versions
KR960007532B1 (ko
Inventor
알란 빅터 코우츠 죠다난
마틴 머튼 이안
리차드 펜 차알스
스토러 리차드
윌리암슨 크리스토퍼
Original Assignee
원본미기재
아이에이 에프 바이오켐 인터내쇼날 인코오포레이티드
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=10675345&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=KR920702682(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 원본미기재, 아이에이 에프 바이오켐 인터내쇼날 인코오포레이티드 filed Critical 원본미기재
Publication of KR920702682A publication Critical patent/KR920702682A/ko
Application granted granted Critical
Publication of KR960007532B1 publication Critical patent/KR960007532B1/ko

Links

Classifications

    • 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D411/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

Abstract

내용 없음

Description

1,3-옥사티오란 뉴클레오시드 동족체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (18)

  1. (-)-시스-4-아미노-1-(2-히드록시메틸-1,3-옥사티오란-5-일)-(1H)-피리미딘-2-온 또는 그의 약학적 허용 유도체.
  2. 제1항에 있어서, 상응하는 (+)-엔안티오머가 거의 없는 화합물.
  3. 제1항 또는 제2항에 있어서, 상기 (+)-엔안티오머는 약 5% w/w이하의 양으로 존재하는 화합물.
  4. 제1항 내지 제3항중 어느 한항에 있어서, 상기 (+)-엔안티오머는 약 2% w/w이하의 양으로 존재하는 화합물.
  5. 제1항 내지 제4항중의 어느 한항에 있어서, 상기 (+)-엔안티오머 약 1% w/w이하의 양으로 존재하는 화합물.
  6. 제1항에 있어서, 거의 순수한 형태의 화합물.
  7. 제1항 내지 제6항중 어느 한항에 의한 화합물 및 그의 약학적 허용담체을 포함하는 약학 조성물.
  8. 제1항 내지 제6항중 어느 한항에 있어서, 치료용으로 사용되는 화합물.
  9. 비루스 감염질환의 치료용 약제를 제조하기 위해 제1항 내지 제6항중 어느 한항에 의한 화합물을 사용하는 방법.
  10. 제1항 내지 제6항중 어느 한항의 유효량 투여함을 포함하는 비루스 감염질환으로 고통받는 인체를 포함하는 포유류를 치료하는 방법.
  11. (+)-엔안티오머를 함유하고 있는 혼합물로 부터(-)-엔안티오머를 분리함을 포함하는 제1항 내지 제6항중 어느 한항의 화합물을 제조하기 위한 방법.
  12. 제11항에 있어서, 상기 화합물의 혼합물은 라셈 혼합물인 방법.
  13. 제11항 또는 제12항에 있어서, 상기 분리방법은 키랄 HPLC로 실시하는 것을 특징으로하는 방법.
  14. 제13항에 있어서, 상기 HPLC는 고정상으로 아세틸화된 β-시클로덱스트린 또는 셀룰로오즈 트리아세테이트를 사용하는 것을 특징으로 하는 방법.
  15. 제11항 또는 제12항에 있어서, 상기 방법은 효소 매개된 엔안티오 선택성 이화작용(enantioselective catabolism)에 의해 실시되는 것을 특징으로 하는 방법.
  16. 제15항에 있어서, 상기 효소는 고정화된 형태로 사용되는 방법.
  17. 제15항 또는 제16항에 있어서, 상기 효소는 시티딘 디아미나제인 방법.
  18. 제15항 또는 제16항에 있어서, 상기 효소는 5'-뉴크레오티다제인 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019910702025A 1990-05-02 1991-05-02 1,3-옥사티오란 뉴클레오시드 동족체 KR960007532B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB90098617 1990-05-02
GB900986 1990-05-02
GB909009861A GB9009861D0 (en) 1990-05-02 1990-05-02 Chemical compounds
PCT/GB1991/000706 WO1991017159A1 (en) 1990-05-02 1991-05-02 1,3-oxathiolane nucleoside analogues

Publications (2)

Publication Number Publication Date
KR920702682A true KR920702682A (ko) 1992-10-06
KR960007532B1 KR960007532B1 (ko) 1996-06-05

Family

ID=10675345

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019910702025A KR960007532B1 (ko) 1990-05-02 1991-05-02 1,3-옥사티오란 뉴클레오시드 동족체

Country Status (35)

Country Link
US (3) US6180639B1 (ko)
EP (2) EP1062950A3 (ko)
JP (3) JP2927546B2 (ko)
KR (1) KR960007532B1 (ko)
CN (3) CN1036196C (ko)
AP (1) AP182A (ko)
BG (1) BG60679B1 (ko)
CA (2) CA2337748A1 (ko)
CZ (1) CZ288499B6 (ko)
EG (1) EG19958A (ko)
FI (1) FI111722B (ko)
GB (1) GB9009861D0 (ko)
GE (1) GEP19991705B (ko)
HK (1) HK1043940B (ko)
HU (2) HUT64335A (ko)
IE (1) IE911482A1 (ko)
IL (1) IL98025A (ko)
MA (1) MA22144A1 (ko)
MD (1) MD809C2 (ko)
MY (1) MY109796A (ko)
NO (1) NO180377B (ko)
NZ (1) NZ238017A (ko)
OA (1) OA09559A (ko)
PL (1) PL167682B1 (ko)
PT (1) PT97520B (ko)
RO (1) RO112616B1 (ko)
RU (1) RU2099338C1 (ko)
SG (1) SG46383A1 (ko)
SK (1) SK283430B6 (ko)
TN (1) TNSN91029A1 (ko)
TW (2) TW366346B (ko)
UA (1) UA40589C2 (ko)
WO (1) WO1991017159A1 (ko)
YU (1) YU78291A (ko)
ZA (1) ZA913293B (ko)

Families Citing this family (82)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5466806A (en) * 1989-02-08 1995-11-14 Biochem Pharma Inc. Processes for preparing substituted 1,3-oxathiolanes with antiviral properties
US7119202B1 (en) 1989-02-08 2006-10-10 Glaxo Wellcome Inc. Substituted-1,3-oxathiolanes and substituted-1,3-dioxolanes with antiviral properties
US5684164A (en) * 1988-04-11 1997-11-04 Biochem Pharma Inc. Processes for preparing substituted 1,3-oxathiolanes with antiviral properties
DE69233014T2 (de) * 1989-02-08 2004-01-08 Biochem Pharma Inc., Laval Verfahren für die herstellung von antiviralen substituierten 1, 3-oxathiolanen
US5276151A (en) * 1990-02-01 1994-01-04 Emory University Method of synthesis of 1,3-dioxolane nucleosides
US5914331A (en) * 1990-02-01 1999-06-22 Emory University Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane
US5827727A (en) * 1990-02-01 1998-10-27 Emory University Method of resolution of 1,3-oxathiolane nucleoside enantiomers
US6703396B1 (en) 1990-02-01 2004-03-09 Emory University Method of resolution and antiviral activity of 1,3-oxathiolane nuclesoside enantiomers
US5204466A (en) * 1990-02-01 1993-04-20 Emory University Method and compositions for the synthesis of bch-189 and related compounds
US5444063A (en) * 1990-12-05 1995-08-22 Emory University Enantiomerically pure β-D-dioxolane nucleosides with selective anti-Hepatitis B virus activity
US5925643A (en) * 1990-12-05 1999-07-20 Emory University Enantiomerically pure β-D-dioxolane-nucleosides
IL100502A (en) * 1991-01-03 1995-12-08 Iaf Biochem Int PHARMACEUTICAL PREPARATIONS CONTAINING CIS-4-AMINO-1-) 2-HYDROXIMETHIL-1,3-OXETYOLEN-5-IL (-
US5817667A (en) * 1991-04-17 1998-10-06 University Of Georgia Research Foudation Compounds and methods for the treatment of cancer
SK279262B6 (sk) * 1991-05-16 1998-08-05 Glaxo Group Limited Protivírusová zmes, farmaceutický prostriedok s je
GB9110874D0 (en) * 1991-05-20 1991-07-10 Iaf Biochem Int Medicaments
ZA923640B (en) * 1991-05-21 1993-02-24 Iaf Biochem Int Processes for the diastereoselective synthesis of nucleosides
GB9111902D0 (en) * 1991-06-03 1991-07-24 Glaxo Group Ltd Chemical compounds
GB9116601D0 (en) * 1991-08-01 1991-09-18 Iaf Biochem Int 1,3-oxathiolane nucleoside analogues
US6177435B1 (en) 1992-05-13 2001-01-23 Glaxo Wellcome Inc. Therapeutic combinations
GB9215178D0 (en) * 1992-07-16 1992-08-26 Glaxo Group Ltd Antiviral combinations
GB9215176D0 (en) * 1992-07-16 1992-08-26 Glaxo Group Ltd Antiviral combinations
GB9226927D0 (en) * 1992-12-24 1993-02-17 Iaf Biochem Int Dideoxy nucleoside analogues
GB9311709D0 (en) * 1993-06-07 1993-07-21 Iaf Biochem Int Stereoselective synthesis of nucleoside analogues using bicycle intermediate
US20020120130A1 (en) 1993-09-10 2002-08-29 Gilles Gosselin 2' or 3' -deoxy and 2', 3' -dideoxy-beta-L-pentofuranonucleo-side compounds, method of preparation and application in therapy, especially as anti- viral agents
US5587362A (en) * 1994-01-28 1996-12-24 Univ. Of Ga Research Foundation L-nucleosides
IL113432A (en) * 1994-04-23 2000-11-21 Glaxo Group Ltd Process for the diastereoselective synthesis of nucleoside analogues
IL115156A (en) * 1994-09-06 2000-07-16 Univ Georgia Pharmaceutical compositions for the treatment of cancer comprising 1-(2-hydroxymethyl-1,3-dioxolan-4-yl) cytosines
US6391859B1 (en) 1995-01-27 2002-05-21 Emory University [5-Carboxamido or 5-fluoro]-[2′,3′-unsaturated or 3′-modified]-pyrimidine nucleosides
US5703058A (en) * 1995-01-27 1997-12-30 Emory University Compositions containing 5-fluoro-2',3'-didehydro-2',3'-dideoxycytidine or a mono-, di-, or triphosphate thereof and a second antiviral agent
US5808040A (en) * 1995-01-30 1998-09-15 Yale University L-nucleosides incorporated into polymeric structure for stabilization of oligonucleotides
MY115461A (en) 1995-03-30 2003-06-30 Wellcome Found Synergistic combinations of zidovudine, 1592u89 and 3tc
PT831852E (pt) 1995-06-07 2007-02-28 Uab Research Foundation Nucleósidos com actividade anti-vírus da hepatite b
GB9605293D0 (en) * 1996-03-13 1996-05-15 Glaxo Group Ltd Medicaments
BR9709939A (pt) 1996-06-25 1999-08-10 Glaxo Group Ltd Combinação formulação farmacêutica processo de tratamento de uma infecção por hiv em um animal infectado usos de éster tetraidro-3-furanila do ácido 3s[3r*(1r*,2s*)]-[-3-[[4-amino-fenil)sulfonil](2-metilprop ril)-amino]-2-hidroxi-1-fenilmetil)propil]-carbâmico de zidovudina e de (2r,cis)-4-amino-1-(2-hidroximetil-1,3-oxatiolan-5-il)-(1h)-pirimidin-2-ona e pacote para paciente
US5753789A (en) * 1996-07-26 1998-05-19 Yale University Oligonucleotides containing L-nucleosides
US6113920A (en) * 1996-10-31 2000-09-05 Glaxo Wellcome Inc. Pharmaceutical compositions
IT1290447B1 (it) * 1997-03-28 1998-12-03 Zambon Spa Derivati 1,3-ossatiolanici ad attivita' antivirale
CN1141305C (zh) 1998-08-12 2004-03-10 三角药物公司 生产1,3-氧硫戊环核苷的方法
US6979561B1 (en) 1998-10-09 2005-12-27 Gilead Sciences, Inc. Non-homogeneous systems for the resolution of enantiomeric mixtures
DK1382343T3 (da) 1998-11-02 2010-04-26 Gilead Sciences Inc Kombinationsterapi til behandling af hepatitis B-virus
ID30477A (id) 1998-12-23 2001-12-13 Shire Biochem Inc Analog nukleosida antivirus
GB9909154D0 (en) * 1999-04-22 1999-06-16 Nippon Glaxo Limited Pharmaceutical formulation
US6432966B2 (en) 1999-10-29 2002-08-13 Smithkline Beecham Corporation Antiviral combinations
US6436948B1 (en) 2000-03-03 2002-08-20 University Of Georgia Research Foundation Inc. Method for the treatment of psoriasis and genital warts
EP1903041B1 (en) 2001-03-01 2015-02-18 AbbVie Inc. Polymorphic and other crystalline forms of cis-FTC
US6720000B2 (en) * 2001-03-19 2004-04-13 Three Rivers Pharmaceutical, Llc Process for producing wet ribavirin pellets
US6649607B2 (en) 2001-05-18 2003-11-18 Vela Pharmaceuticals, Inc. Compositions and methods for treating or preventing convulsions or seizures
CA2351049C (en) 2001-06-18 2007-03-13 Brantford Chemicals Inc. Process for recovery of the desired cis-1,3-oxathiolane nucleosides from their undesired trans-isomers
WO2003039517A1 (en) * 2001-11-02 2003-05-15 Sandoz Inc. Process for preparing quick dissolving, high loading ribavirin compositions
US7538094B2 (en) * 2002-09-19 2009-05-26 Three Rivers Pharmacueticals, Llc Composition containing ribavirin and use thereof
WO2004043433A2 (en) * 2002-11-08 2004-05-27 Glaxo Group Limited Pharmaceutical antiviral compositions
EP1923063A3 (en) 2003-01-14 2009-04-08 Gilead Sciences, Inc. Compositions and methods for combination antiviral therapy
FR2855822B1 (fr) * 2003-06-05 2005-07-22 Univ Grenoble 1 Acides nucleiques en tant que nouveaux selecteurs chiraux specifiques
GB0317009D0 (en) 2003-07-21 2003-08-27 Univ Cardiff Chemical compounds
TWI375560B (en) 2005-06-13 2012-11-01 Gilead Sciences Inc Composition comprising dry granulated emtricitabine and tenofovir df and method for making the same
TWI471145B (zh) 2005-06-13 2015-02-01 Bristol Myers Squibb & Gilead Sciences Llc 單一式藥學劑量型
LV13544B (en) 2005-08-15 2007-05-20 Grindeks As Pharmaceutical composition containing reverse transcriptase inhibitor and meldonium
CN100360528C (zh) * 2005-08-31 2008-01-09 四川大学 4-氨基-1-(2-羟甲基-1,3-氧硫杂环戊烷-5-基)-2(1h)-嘧啶酮的制备方法
ATE485292T1 (de) 2006-04-18 2010-11-15 Lupin Ltd Neue kristalline form von lamivudin
US20100196273A1 (en) * 2007-02-12 2010-08-05 Board Of Regents, University Of Texas System Novel agent for in vivo pet imaging of tumor proliferation
DE602008000255D1 (de) 2007-06-12 2009-12-17 Concert Pharmaceuticals Inc Azapeptid-Derivate als HIV-Protease-Inhibitoren
SI2225232T1 (sl) 2007-11-29 2012-12-31 Ranbaxy Laboratories Limited Postopek za pripravo substituiranih 1,3-oksatiolanov
RU2446807C2 (ru) * 2007-12-20 2012-04-10 Н.В. Нютрисиа Жидкий продукт, содержащий нуклеотиды/нуклеозиды
US8536151B2 (en) 2008-09-01 2013-09-17 Hetero Research Foundation Process for preparing lamivudine polymorph form
SG172361A1 (en) 2008-12-23 2011-07-28 Pharmasset Inc Nucleoside analogs
AU2009329872B2 (en) 2008-12-23 2016-07-07 Gilead Pharmasset Llc Synthesis of purine nucleosides
AR074897A1 (es) 2008-12-23 2011-02-23 Pharmasset Inc Fosforamidatos de nucleosidos
US20110282046A1 (en) 2009-01-19 2011-11-17 Rama Shankar Process for preparation of cis-nucleoside derivative
MX367937B (es) 2010-01-27 2019-09-12 Viiv Healthcare Co Combinaciones de compuestos que comprenden inhibidores de la integrasa de vih y otros agentes terapéuticos.
AU2011215878A1 (en) 2010-02-12 2012-08-09 Merck Sharp & Dohme Corp. Preparation of lamivudine Form I
CN102167696B (zh) 2010-02-25 2013-09-18 南京正大天晴制药有限公司 拉米夫定草酸盐及其制备方法
EP2752422B1 (en) 2010-03-31 2017-08-16 Gilead Pharmasset LLC Stereoselective synthesis of phosphorus containing actives
CN102234269B (zh) * 2010-04-29 2015-09-16 重庆医药工业研究院有限责任公司 拉米夫定的工业化制备方法
WO2011156594A2 (en) 2010-06-09 2011-12-15 Vaccine Technologies, Incorporated Therapeutic immunization in hiv infected subjects receiving stable antiretroviral treatment
NZ607996A (en) 2010-09-22 2014-07-25 Alios Biopharma Inc Substituted nucleotide analogs
CN104321333A (zh) 2012-03-21 2015-01-28 沃泰克斯药物股份有限公司 硫代氨基磷酸酯核苷酸前药的固体形式
WO2013142157A1 (en) 2012-03-22 2013-09-26 Alios Biopharma, Inc. Pharmaceutical combinations comprising a thionucleotide analog
WO2013168066A1 (en) 2012-05-05 2013-11-14 Lupin Limited An improved process for the manufacture of lamivudine form i.
WO2014068265A1 (en) 2012-10-29 2014-05-08 Cipla Limited Antiviral phosphonate analogues and process for preparation thereof
CN103315963A (zh) * 2013-06-21 2013-09-25 北京阜康仁生物制药科技有限公司 一种稳定的拉米夫定颗粒剂
US11116737B1 (en) 2020-04-10 2021-09-14 University Of Georgia Research Foundation, Inc. Methods of using probenecid for treatment of coronavirus infections
WO2021209563A1 (en) 2020-04-16 2021-10-21 Som Innovation Biotech, S.A. Compounds for use in the treatment of viral infections by respiratory syndrome-related coronavirus

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4211773A (en) * 1978-10-02 1980-07-08 Sloan Kettering Institute For Cancer Research 5-Substituted 1-(2'-Deoxy-2'-substituted-β-D-arabinofuranosyl)pyrimidine nucleosides
JPS5668674A (en) 1979-11-08 1981-06-09 Shionogi & Co Ltd 5-fluorouracil derivative
IT1212737B (it) * 1983-05-06 1989-11-30 Daniele Gatti Derivati pirimidinici ad azione antivirale.
HU196607B (en) * 1985-05-15 1988-12-28 Wellcome Found Process for producing dideoxy-nucleosides and pharmaceutics comprising such compounds
DE3529263A1 (de) 1985-08-16 1987-02-19 Hoechst Ag Verfahren zur herstellung von 2-oxo-1,3-dioxolanen
CA1327000C (en) 1987-08-07 1994-02-15 David L.J. Tyrrell Antiviral therapy for hepatitis b
US4997926A (en) 1987-11-18 1991-03-05 Scripps Clinic And Research Foundation Deaminase-stable anti-retroviral 2-halo-2',3'-dideoxy
US5047407A (en) * 1989-02-08 1991-09-10 Iaf Biochem International, Inc. 2-substituted-5-substituted-1,3-oxathiolanes with antiviral properties
US5466806A (en) * 1989-02-08 1995-11-14 Biochem Pharma Inc. Processes for preparing substituted 1,3-oxathiolanes with antiviral properties
NZ228645A (en) * 1988-04-11 1991-09-25 Iaf Biochem Int 1,3-dioxolane derivatives substituted in the 5th position by a purine or pyrimidine radical; treatment of viral infections
GB8815265D0 (en) 1988-06-27 1988-08-03 Wellcome Found Therapeutic nucleosides
DE3827134A1 (de) 1988-08-10 1990-03-15 Bayer Ag Substituierte triazolyl- bzw. imidazolyl-hydroxyalkyldioxolane, verfahren zu ihrer herstellung und ihre verwendung als mikrobizide, oxiranyldioxolane, dioxolanylketone, oxiranylketone und (alpha)-halogenketone als zwischenprodukte und verfahren zu deren herstellung
NZ233197A (en) 1989-04-13 1991-11-26 Richard Thomas Walker Aromatically substituted nucleotide derivatives, intermediates therefor and pharmaceutical compositions
DK0479822T3 (da) 1989-06-27 2000-03-20 Wellcome Found Terapeutiske nucleosider
NZ234534A (en) 1989-07-17 1994-12-22 Univ Birmingham Pyrimidine 4'-thionucleoside derivatives and their preparation; intermediates therefor
IE74701B1 (en) 1989-10-04 1997-07-30 Univ Birmingham Further antiviral pyrimidine nucleosides
US5039567A (en) 1989-12-04 1991-08-13 Supracor Systems, Inc. Resilient panel having anisotropic flexing characteristics and method of making same
US5204466A (en) 1990-02-01 1993-04-20 Emory University Method and compositions for the synthesis of bch-189 and related compounds
SK279262B6 (sk) 1991-05-16 1998-08-05 Glaxo Group Limited Protivírusová zmes, farmaceutický prostriedok s je
US5869461A (en) 1995-03-16 1999-02-09 Yale University Reducing toxicity of L-nucleosides with D-nucleosides

Also Published As

Publication number Publication date
IL98025A (en) 1996-10-16
GB9009861D0 (en) 1990-06-27
JP2927546B2 (ja) 1999-07-28
MA22144A1 (fr) 1991-12-31
FI916165A0 (fi) 1991-12-30
HU9200302D0 (en) 1992-04-28
MD809B2 (en) 1997-08-31
EP1062950A2 (en) 2000-12-27
CN1108655A (zh) 1995-09-20
CS125191A3 (en) 1992-01-15
US20030004175A1 (en) 2003-01-02
SG46383A1 (en) 1998-02-20
AP9100255A0 (en) 1991-07-31
EP0625150A1 (en) 1994-11-23
HK1043940B (zh) 2005-03-24
YU78291A (sh) 1994-06-10
EP1062950A3 (en) 2003-05-02
TW366346B (en) 1999-08-11
CA2059263A1 (en) 1991-11-03
CN1036196C (zh) 1997-10-22
US20050250950A1 (en) 2005-11-10
GEP19991705B (en) 1999-08-05
HK1043940A1 (en) 2002-10-04
UA40589C2 (uk) 2001-08-15
PL293181A1 (ko) 1993-02-08
NO180377B (no) 1996-12-30
PL167682B1 (pl) 1995-10-31
TNSN91029A1 (fr) 1992-10-25
AU651345B2 (en) 1994-07-21
HUT64335A (en) 1993-12-28
AP182A (en) 1992-06-30
CZ288499B6 (en) 2001-06-13
OA09559A (fr) 1993-01-31
EG19958A (en) 1996-10-31
CA2059263C (en) 2001-04-10
WO1991017159A1 (en) 1991-11-14
JPH05501117A (ja) 1993-03-04
JP2000128787A (ja) 2000-05-09
JP3062475B2 (ja) 2000-07-10
KR960007532B1 (ko) 1996-06-05
IL98025A0 (en) 1992-06-21
US6180639B1 (en) 2001-01-30
IE911482A1 (en) 1991-11-06
CN1056145C (zh) 2000-09-06
NZ238017A (en) 1994-06-27
CN1326743A (zh) 2001-12-19
PT97520A (pt) 1992-01-31
NO920018L (no) 1992-01-02
HU210803A9 (en) 1995-07-28
RU2099338C1 (ru) 1997-12-20
CA2337748A1 (en) 1991-11-14
ZA913293B (en) 1992-02-26
MY109796A (en) 1997-07-30
MD809C2 (ro) 1998-07-31
JPH1180153A (ja) 1999-03-26
FI111722B (fi) 2003-09-15
NO920018D0 (no) 1992-01-02
SK283430B6 (sk) 2003-07-01
BG60679B1 (bg) 1995-12-29
CN1154500C (zh) 2004-06-23
PT97520B (pt) 1998-08-31
AU7771991A (en) 1991-11-27
RO112616B1 (ro) 1997-11-28
TWI222448B (en) 2004-10-21
CN1058214A (zh) 1992-01-29

Similar Documents

Publication Publication Date Title
KR920702682A (ko) 1, 3-옥사티오란 뉴클레오시드 동족체
CA2114221A1 (en) 1, 3-oxathiolane nucleoside analogues
BR0012136A (pt) Inibidores de reabsorção de norepinefrina altamente seletivos e métodos de uso dos mesmos
KR900014367A (ko) 피롤리딘 유도체
HUT47217A (en) Process for producing pharmaceutical compositions containing indol derivatives as active components
BR0214967A (pt) Composto, sal famaceuticamente aceitável, processo para a preparação de um composto, composição farmacêutica, uso de um composto e método de tratar um distúrbio de um paciente
KR960033460A (ko) 심장의 염증성 질병 치료용 약제학적 조성물
UA41446C2 (uk) Застосування фумагілолу та його похідних для одержання ліків, призначених для боротьби з кишковими інфекціями, та фармацевтична композиція на їх основі
ATE73331T1 (de) Verwendung von tetrahydrobiopterinen zur herstellung eines medikaments zur behandlung von kinderautismus.
EA199800943A1 (ru) Производные мочевины и их применение в качестве ингибиторов инозин-5`-монофосфат- дегидрогеназы
BR9808953A (pt) Composto, processo para tratar um distúrbio mediado pela ciclooxigenase-2 em um paciente, e, composição farmacêutica
RU94042935A (ru) Водорастворенные комплексы включения соединений бензотиофена с водорастворимыми циклодекстринами, способ их получения и фармацевтический состав
PT98735A (pt) Processo de preparacao de compostos azaciclicos e de composicoes farmaceuticas que os contem
UA45942A (uk) 1,3-оксатіолан, його похідні, спосіб (варіанти) його одержання та фармацевтична композиція
JPH0825890B2 (ja) 抗ウイルス剤
BR0109602A (pt) Glóbulos de liberação controlada contendo estavudina
TNSN00250A1 (fr) Composes nouveaux inhibiteurs de pcp, procede pour leur preparation et compositions les contenant
DE3682811D1 (de) Pharmazeutische zusammensetzung zur heilung und verhuetung kardiovaskularer krankheiten und verfahren zu ihrer herstellung.
PT1194415E (pt) Novos derivados da piperazinil-alquil-tiopirimidina composicoes farmaceuticas que os contem e um processo de preparacao da substancia activa
Franco et al. Self-aggregation of the transmembrane glycoprotein CD38 purified from human erythrocytes
KR880013927A (ko) 피리미딘 유도체
Hunskaar A case of ecthyma contagiosum (human orf) treated with idoxuridine
KR890012942A (ko) 5-치환된 오르니틴 유도체
PT98538A (pt) Processo de preparacao de factor de crescimento humano epidermico (hegf) dos seus congeneres e de composicoes farmaceuticas que os contem
BR9916733A (pt) Derivados de arilalcanoìla, processos para sua preparação, seu uso e composições farmacêuticas que os contêm

Legal Events

Date Code Title Description
A201 Request for examination
E902 Notification of reason for refusal
G160 Decision to publish patent application
E701 Decision to grant or registration of patent right
GRNT Written decision to grant
J204 Request for invalidation trial [patent]
J121 Written withdrawal of request for trial
J206 Request for trial to confirm the scope of a patent right
J121 Written withdrawal of request for trial
FPAY Annual fee payment

Payment date: 20110922

Year of fee payment: 16

EXPY Expiration of term