TW444020B - Nucleotide analogs - Google Patents

Nucleotide analogs Download PDF

Info

Publication number
TW444020B
TW444020B TW086110757A TW86110757A TW444020B TW 444020 B TW444020 B TW 444020B TW 086110757 A TW086110757 A TW 086110757A TW 86110757 A TW86110757 A TW 86110757A TW 444020 B TW444020 B TW 444020B
Authority
TW
Taiwan
Prior art keywords
alkyl
independently
alkenyl
alkynyl
aryl
Prior art date
Application number
TW086110757A
Other languages
English (en)
Inventor
Murty N Arimilli
Kenneth C Cundy
Joseph P Dougherty
Reza Oliyai
Choung Un Kim
Original Assignee
Gilead Sciences Inc
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=26696272&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TW444020(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Application granted granted Critical
Publication of TW444020B publication Critical patent/TW444020B/zh

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509—Six-membered rings
    • C07F9/6512—Six-membered rings having the nitrogen atoms in positions 1 and 3

Description

444020 A8 B8 C8 六、申請專利範圍
與L-CHR2-0-C(0)-0R /反應後回收式（1)化合物，其中B是 鳥糞嘌呤-9-基，腺嘌呤-9-基，2,6-二胺基嘌呤-9-基，2-胺基 嘌玲-9-基或其1-去氮，3-去氮，或8-氮基類似物，或b是 胞嘧啶-1-基； R1 是氫，-CH3, -CH2〇H, -CH2F，-CH = CH2, -CH2N3 或 R1 與R8連結形成-CH2-;及 R8 是氫，-CHR2-0-C(0)-0R > 或 R8 與 R1 連結形成 _CH2_; R2是H.CVCu烷基，芳基，烯基，炔基，烯芳基，炔芳 基，烷芳基，芳炔基，芳烯基或芳烷基，其係未經取代或 經鹵基，疊氮基，硝基或〇113(113爲Ci-Cu烷基）取代； R /分別是H，G-Cu烷基，芳基，烯基，炔基，烯芳基， 炔芳基，烷芳基，芳炔基，芳烯基或芳烷基，其係未經取 代或經鹵基，疊氮基，硝基或OR3取代，惟至少一個R-不 是Η ;及 L是離去基。 18.如申請專利範圍第17項之方法，該方法包括用至少 約1.0當量之l-chr2-o-c(o)-〇r/進行反應。 i 9.如申請專利範圍第17項之方法，該方法包括在有機 鹼存在下，於有機溶劑中及反應溫度約4-lOOt：進行反應約 4-72小時。 本紙張尺度適用中國國家梯準（CNS ) A4规格（210X 297公着）-4- (請先聞靖背面之注意事項再填寫本頁) 訂 Ψ. 經濟部智慧財產局員工消費合作社印製 444020 A6 B8 C8 D8 六、申請專利範圍 20. 如申請專利範圍第17項之方法 形成鹽類後沈澱回收。 21. 如申請專利範圍第20項之方法 酸、磷酸、乳酸或檸檬酸。 22.—種具有下式之化合物 其中式（1)化合物 其中該鹽類得自硫
〇 〇、/ 3 CH2〆 c 、CH3 •〇-CH2^C c -ch3 0 \h. (請先閲请背面之注意事項再填寫本頁) 經濟部智慧財產局員工消費合作社印製 本纸張尺度適用中國國家揉準（CNS ) A4規格（210X297公釐）-5 -
TW086110757A 1996-07-26 1997-08-21 Nucleotide analogs TW444020B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US68683896A 1996-07-26 1996-07-26
US2270896P 1996-07-26 1996-07-26

Publications (1)

Publication Number Publication Date
TW444020B true TW444020B (en) 2001-07-01

Family

ID=26696272

Family Applications (2)

Application Number Title Priority Date Filing Date
TW089123708A TW470748B (en) 1996-07-26 1997-08-21 Nucleotide analogs
TW086110757A TW444020B (en) 1996-07-26 1997-08-21 Nucleotide analogs

Family Applications Before (1)

Application Number Title Priority Date Filing Date
TW089123708A TW470748B (en) 1996-07-26 1997-08-21 Nucleotide analogs

Country Status (4)

Country Link
JP (6) JP4033494B2 (zh)
CA (1) CA2261619C (zh)
TW (2) TW470748B (zh)
WO (1) WO1998004569A1 (zh)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4033494B2 (ja) * 1996-07-26 2008-01-16 ギリヤド サイエンシーズ， インコーポレイテッド ヌクレオチドアナログ
PT1256584E (pt) * 1997-07-25 2004-12-31 Gilead Sciences Inc Processo para a preparacao de adefovir-dipivoxil
EP1243593B1 (en) * 1997-07-25 2005-09-21 Gilead Sciences, Inc. Nucleotide analog composition and synthesis method
WO1999005150A1 (en) * 1997-07-25 1999-02-04 Gilead Sciences, Inc. Nucleotide analog composition and synthesis method
AU4716299A (en) * 1998-06-24 2000-01-10 Emory University Use of 3'-azido-2',3'-dideoxyuridine in combination with further anti-hiv drugs for the manufacture of a medicament for the treatment of hiv
CZ304734B6 (cs) * 2000-07-21 2014-09-10 Gilead Sciences, Inc. Způsob přípravy 9-[2-(fosfonomethoxy)propyl]adeninu a 9-[2-(fosfonomethoxy)ethyl]adeninu
CA2481449A1 (en) 2002-04-26 2003-11-06 Gilead Sciences, Inc. Method and compositions for identifying anti-hiv therapeutic compounds
EP1923063A3 (en) 2003-01-14 2009-04-08 Gilead Sciences, Inc. Compositions and methods for combination antiviral therapy
US7432261B2 (en) 2003-04-25 2008-10-07 Gilead Sciences, Inc. Anti-inflammatory phosphonate compounds
US7452901B2 (en) 2003-04-25 2008-11-18 Gilead Sciences, Inc. Anti-cancer phosphonate analogs
US7273716B2 (en) 2003-04-25 2007-09-25 Gilead Sciences, Inc. Methods and compositions for identifying therapeutic compounds with GS-7340 ester hydrolase
US7427636B2 (en) 2003-04-25 2008-09-23 Gilead Sciences, Inc. Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
WO2004096285A2 (en) 2003-04-25 2004-11-11 Gilead Sciences, Inc. Anti-infective phosphonate conjugates
CN101410120A (zh) * 2003-04-25 2009-04-15 吉里德科学公司 抗炎的膦酸酯化合物
US7470724B2 (en) 2003-04-25 2008-12-30 Gilead Sciences, Inc. Phosphonate compounds having immuno-modulatory activity
US7407965B2 (en) 2003-04-25 2008-08-05 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
EP1620109A2 (en) 2003-04-25 2006-02-01 Gilead Sciences, Inc. Kinase inhibitor phosphonate conjugates
NZ542342A (en) 2003-04-25 2009-05-31 Gilead Sciences Inc Antiviral phosphonate analogs
WO2005002626A2 (en) 2003-04-25 2005-01-13 Gilead Sciences, Inc. Therapeutic phosphonate compounds
ATE496056T1 (de) 2003-06-16 2011-02-15 Acad Of Science Czech Republic Pyrimidinverbindungen mit phosphonatgruppen als antivirale nucleotidanaloga
WO2005044279A1 (en) 2003-10-24 2005-05-19 Gilead Sciences, Inc. Purine nucleoside phosphonate conjugates
WO2005044308A1 (en) 2003-10-24 2005-05-19 Gilead Sciences, Inc. Phosphonate analogs of antimetabolites
EP1715871A1 (en) * 2003-12-22 2006-11-02 Gilead Sciences, Inc. Kinase inhibitor phosphonate conjugates
WO2005063751A1 (en) 2003-12-22 2005-07-14 Gilead Sciences, Inc. 4’-substituted carbovir-and abacavir-derivatives as well as related compounds with hiv and hcv antiviral activity
AU2005330489B2 (en) 2004-07-27 2011-08-25 Gilead Sciences, Inc. Nucleoside phosphonate conjugates as anti HIV agents
CN102228463B (zh) * 2005-06-13 2012-12-19 博瑞生物医药技术(苏州)有限公司 泰诺福韦的晶体
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
CA2681267C (en) 2007-04-13 2013-11-19 Southern Research Institute Anti-angiogenic agents and methods of use
CN101778855A (zh) * 2007-05-22 2010-07-14 阿尔迪默菲克斯技术有限责任公司 替诺福韦酯半富马酸共晶体
WO2009064174A1 (en) * 2007-11-14 2009-05-22 Ultimorphix Technologies B.V. Polymorphic form of tenofovir disoproxil fumarate, method for its preparation and use
EP2937356A1 (en) * 2008-04-25 2015-10-28 Cipla Limited Crystalline form of tenofovir disoproxil and a process for its preparation
WO2010005986A1 (en) 2008-07-08 2010-01-14 Gilead Sciences, Inc. Salts of hiv inhibitor compounds
CN102093422B (zh) 2009-12-10 2015-02-25 中国人民解放军军事医学科学院毒物药物研究所 无环核苷膦酸酯衍生物及其医药用途
WO2012152317A1 (en) * 2011-05-10 2012-11-15 Okapi Sciences Nv Compounds for use in the treatment of feline retroviral infections
CA2845553C (en) 2011-08-16 2019-05-28 Gilead Sciences, Inc. Tenofovir alafenamide hemifumarate
CN103626802A (zh) * 2012-08-23 2014-03-12 重庆药友制药有限责任公司 一种制备替诺福韦的新方法
CN103665043B (zh) 2012-08-30 2017-11-10 江苏豪森药业集团有限公司 一种替诺福韦前药及其在医药上的应用
WO2014068265A1 (en) 2012-10-29 2014-05-08 Cipla Limited Antiviral phosphonate analogues and process for preparation thereof
EP2860184B1 (en) 2013-10-09 2018-08-29 Zentiva, k.s. Dihydrogenphosphate salt of Tenofovir disoproxil
EP2860185A1 (en) 2013-10-09 2015-04-15 Zentiva, k.s. An improved process for the preparation of Tenofovir disoproxil and pharmaceutically acceptable salts thereof
TWI660965B (zh) * 2014-01-15 2019-06-01 美商基利科學股份有限公司 泰諾福韋之固體形式
SI3661937T1 (sl) 2017-08-01 2021-11-30 Gilead Sciences, Inc. Kristalinične oblike etil((S)-((((2R,5R)-5-(6-amino-9H-purin-9-IL)-4- fluoro-2,5-dihidrofuran-2-IL)oksi)metil)(fenoksi)fosforil)-L-alaninata (GS-9131) za zdravljenje virusnih okužb
CN107805202A (zh) * 2017-12-01 2018-03-16 内蒙古圣氏化学股份有限公司 一种氯甲基异丙基碳酸酯连续化反应装置及方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ222553A (en) * 1986-11-18 1991-07-26 Bristol Myers Co Phosphonomethoxyalkylene purine and pyrimidine derivatives and pharmaceutical compositions
EP0481214B1 (en) * 1990-09-14 1998-06-24 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Prodrugs of phosphonates
GB9026164D0 (en) * 1990-12-01 1991-01-16 Beecham Group Plc Pharmaceuticals
AU691527B2 (en) * 1993-09-17 1998-05-21 Gilead Sciences, Inc. Nucleotide analogs
JP4033494B2 (ja) * 1996-07-26 2008-01-16 ギリヤド サイエンシーズ， インコーポレイテッド ヌクレオチドアナログ

Also Published As

Publication number Publication date
TW470748B (en) 2002-01-01
CA2261619A1 (en) 1998-02-05
JP2017031212A (ja) 2017-02-09
CA2261619C (en) 2006-05-23
JP2015164934A (ja) 2015-09-17
JP2011016847A (ja) 2011-01-27
JP2007297406A (ja) 2007-11-15
JP2000515866A (ja) 2000-11-28
JP4033494B2 (ja) 2008-01-16
JP2014159450A (ja) 2014-09-04
WO1998004569A1 (en) 1998-02-05

Similar Documents

Publication Publication Date Title
TW444020B (en) Nucleotide analogs
JPH0586792B2 (zh)
JP5863789B2 (ja) ピラゾール誘導体の製造方法
JP5805880B2 (ja) １−（４−（４−（３，４−ジクロロ−２−フルオロフェニルアミノ）−７−メトキシキナゾリン−６−イルオキシ）ピペリジン−１−イル）−プロパ−２−エン−１−オン塩酸塩の製造方法および該方法で用いられる中間体
SK743188A3 (en) 2',3'-dideoxy-2'-fluoronucleosides, method of production and pharmaceutical agents containing them
IE59713B1 (en) Amino-thiazole and oxazole derivatives
EP0520574A1 (en) Thioxanthone derivatives
CA2436665A1 (en) Nucleic acid derivatives
US8119800B2 (en) Processes for preparing HIV reverse transcriptase inhibitors
JP7109056B2 (ja) Ｓ－ｉｃａリボシルホモシステインの製造方法
CS259896B2 (en) Method of aryloxypropanolamine's new salts production with diphenyl acetic acid
KR830007510A (ko) 심장질환 치료제의 제조방법
YU47906B (sh) Proces za sintezu optički aktivnih aminokiselina
JP4245490B2 (ja) ２−（ジクロロフェニル）−４−フェニルイミダゾール化合物
AU2006282428A1 (en) Method for producing 1-substituted-5-acylimidazole compound
NL8007126A (nl) Werkwijze ter bereiding van watervrij 2-hydroxy-3-chloorpropyltrimethylammoniumchloride.
CA2883263C (en) Photocleavable linker molecules with diarylsulphid backbone for transient bioconjugate synthesis
CN1189158A (zh) 用于合成四唑的新的试剂和使用该试剂合成四唑的方法
US2856405A (en) Mecuration products of 1-(2-pyrimidyl)-3-allylurea
JPH013178A (ja) アミン誘導体の製造方法
WO1996034861A1 (fr) Nouveau procede de n2-tritylation de cycles tetrazole
JP2017178811A (ja) γターン構造を有する化合物及びそれを用いたＬＳＤ１阻害剤
CA1067099A (en) Process for the production of substituted benzyl cyanides
PL104471B1 (pl) Sposob wytwarzania pochodnych 1-karbamylouracylu
ES2352958T3 (es) Un proceso para la preparación de base de imatinib.

Legal Events

Date Code Title Description
GD4A Issue of patent certificate for granted invention patent
MK4A Expiration of patent term of an invention patent