EA199800899A1 - Гетероциклические азагексановые производные с антивирусным действием - Google Patents

Гетероциклические азагексановые производные с антивирусным действием

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Publication number
EA199800899A1
EA199800899A1 EA199800899A EA199800899A EA199800899A1 EA 199800899 A1 EA199800899 A1 EA 199800899A1 EA 199800899 A EA199800899 A EA 199800899A EA 199800899 A EA199800899 A EA 199800899A EA 199800899 A1 EA199800899 A1 EA 199800899A1
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EA
Eurasian Patent Office
Prior art keywords
denotes
ness
substituted
alkyl
phenyl
Prior art date
Application number
EA199800899A
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English (en)
Other versions
EA001794B1 (ru
Inventor
Александр Фэсслер
Гвидо Болд
Ханс-Георг Капраро
Марк Ланг
Сатиш Ханна
Original Assignee
Новартис Аг
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27171723&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA199800899(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Новартис Аг filed Critical Новартис Аг
Publication of EA199800899A1 publication Critical patent/EA199800899A1/ru
Publication of EA001794B1 publication Critical patent/EA001794B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36Radicals substituted by singly-bound nitrogen atoms
    • C07D213/42Radicals substituted by singly-bound nitrogen atoms having hetero atoms attached to the substituent nitrogen atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C281/00Derivatives of carbonic acid containing functional groups covered by groups C07C269/00 - C07C279/00 in which at least one nitrogen atom of these functional groups is further bound to another nitrogen atom not being part of a nitro or nitroso group
    • C07C281/02Compounds containing any of the groups, e.g. carbazates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C281/00Derivatives of carbonic acid containing functional groups covered by groups C07C269/00 - C07C279/00 in which at least one nitrogen atom of these functional groups is further bound to another nitrogen atom not being part of a nitro or nitroso group
    • C07C281/02Compounds containing any of the groups, e.g. carbazates
    • C07C281/04Compounds containing any of the groups, e.g. carbazates the other nitrogen atom being further doubly-bound to a carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/12Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D257/00Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04Five-membered rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/28Radicals substituted by nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/20Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Virology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Communicable Diseases (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Indole Compounds (AREA)

Abstract

В заявке описаны соединения формулы (I*),где Rобозначает (низш.)алкоксикарбонил, Rобозначает вторичный или третичный (низш.)алкил или (низш.)алкилтио(низш.)алкил, Rобозначает фенил, который не замещен или замещен одним или несколькими (низш.)алкоксирадикалами, или С-Сциклоалкил, Rобозначает фенил или циклогексил, каждый из которых замещен в 4-м положении ненасыщенным гетероциклилом, который связан с помощью кольцевого углеродного атома, включает 5-8 кольцевых атомов, содержит 1-4 гетероатома, выбранных из азота, кислорода, серы, серы в виде сульфинила (-SO-) и сульфонила (-SO-), и не замещен или замещен (низш.)алкилом или фенил (низш.)алкилом, Rнезависимо от Rимеет одно из значений, указанных для R, a Rнезависимо от Rобозначает (низш.)алкоксикарбонил, или его соли при условии наличия, по меньшей мере, одной солеобразующей группы. Эти соединения являются ингибиторами ретровирусной аспартатпротеазы и могут быть использованы, например, при лечении СПИДа. Они обладают исключительно ценными фармакокинетическими свойствами.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA199800899A 1996-04-22 1997-04-14 Гетероциклические азагексановые производные с антивирусным действием EA001794B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CH101896 1996-04-22
CH2997 1997-01-08
CH22397 1997-01-31
PCT/EP1997/001860 WO1997040029A1 (en) 1996-04-22 1997-04-14 Antivirally active heterocyclic azahexane derivatives

Publications (2)

Publication Number Publication Date
EA199800899A1 true EA199800899A1 (ru) 1999-10-28
EA001794B1 EA001794B1 (ru) 2001-08-27

Family

ID=27171723

Family Applications (1)

Application Number Title Priority Date Filing Date
EA199800899A EA001794B1 (ru) 1996-04-22 1997-04-14 Гетероциклические азагексановые производные с антивирусным действием

Country Status (28)

Country Link
EP (1) EP0900210B1 (ru)
JP (1) JP3174347B2 (ru)
CN (3) CN1082508C (ru)
AR (1) AR006720A1 (ru)
AT (1) ATE288903T1 (ru)
AU (1) AU706183B2 (ru)
BR (1) BR9701877A (ru)
CA (3) CA2250840C (ru)
CY (1) CY2596B2 (ru)
CZ (1) CZ296135B6 (ru)
DE (2) DE122005000003I1 (ru)
DK (1) DK0900210T3 (ru)
EA (1) EA001794B1 (ru)
ES (1) ES2238720T3 (ru)
FR (1) FR05C0030I2 (ru)
HK (2) HK1018788A1 (ru)
HU (1) HU224125B1 (ru)
IL (1) IL126381A (ru)
LU (1) LU91189I2 (ru)
MY (1) MY114457A (ru)
NL (1) NL300203I2 (ru)
NO (2) NO313330B1 (ru)
NZ (3) NZ332118A (ru)
PT (1) PT900210E (ru)
SI (1) SI0900210T1 (ru)
SK (1) SK285048B6 (ru)
TW (1) TW409125B (ru)
WO (1) WO1997040029A1 (ru)

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US6096894A (en) * 1998-07-29 2000-08-01 Sumika Fine Chemicals Co., Ltd. Production method of 2-(p-alkylphenyl)pyridine compound
DK0979820T3 (da) 1998-08-07 2003-06-02 Sumika Fine Chemicals Co Ltd 2-phenylpyridinderivater og fremgangsmåder til deres fremstilling
US6255349B1 (en) 1998-12-09 2001-07-03 American Home Products Corporation Alph-methylbenzyl-containing thiourea inhibitors of herpes viruses containing a phenylenediamine group
US6335350B1 (en) 1998-12-09 2002-01-01 American Home Products Corporation Acetamide and substituted acetamide-containing thiourea inhibitors of herpes viruses
US6197803B1 (en) 1998-12-09 2001-03-06 American Home Products Corporation Heterocyclic carboxamide-containing thiourea inhibitors of herpes viruses containing phenylenediamine group
US6207715B1 (en) 1998-12-09 2001-03-27 American Home Products Corporation Alpha-methylbenzyl-containing thiourea inhibitors of herpes viruses containing a substituted phenylene-diamine group
JP4222671B2 (ja) * 1999-02-15 2009-02-12 住友化学株式会社 ヒドラジン誘導体の製造方法
IT1313664B1 (it) * 1999-10-12 2002-09-09 Norpharma S P A Processo per la preparazione di un composto aril-piridinico.
US6365745B1 (en) 2000-07-14 2002-04-02 Sumika Fine Chemicals Co., Ltd. Method for producing hydrazine derivative
JP4278316B2 (ja) * 2000-07-14 2009-06-10 住友化学株式会社 ヒドラジン誘導体の製造方法
WO2004037790A1 (en) 2002-10-02 2004-05-06 Euticals Prime European Therapeuticals Spa Process for the preparation of aryl-piridyl compounds
US7943593B2 (en) * 2002-12-06 2011-05-17 Vertex Pharmaceuticals Incorporated Compositions comprising inhibitors of IMPDH enzyme
ITMI20032338A1 (it) * 2003-11-28 2005-05-29 Dinamite Dipharma S P A In Forma A Bbreviata Diph Composti feniltetrazolici.
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WO2013014633A1 (en) * 2011-07-27 2013-01-31 Ranbaxy Laboratories Limited Process for preparation of atazanavir or its bisulfate salt
JP2015536940A (ja) 2012-10-29 2015-12-24 シプラ・リミテッド 抗ウイルス性ホスホネート類似体及びその製造方法
CN104250224A (zh) * 2013-06-28 2014-12-31 上海威智医药科技有限公司 阿扎那韦富马酸盐及其制备和应用
CN104163787A (zh) * 2014-08-08 2014-11-26 山东威智医药工业有限公司 阿扎那韦及其硫酸盐的制备方法
CN107459496B (zh) * 2016-06-03 2022-07-19 华东理工大学 噻唑类衍生物在治疗病毒感染中的应用
JOP20180009A1 (ar) 2017-02-06 2019-01-30 Gilead Sciences Inc مركبات مثبط فيروس hiv
CN107245052A (zh) * 2017-06-21 2017-10-13 连云港杰瑞药业有限公司 一种阿扎那韦制备方法
TWI829205B (zh) * 2018-07-30 2024-01-11 美商基利科學股份有限公司 抗hiv化合物
CN109251165B (zh) * 2018-10-02 2022-09-23 国药集团川抗制药有限公司 阿扎那韦达二4-氨基苯磺酸盐及其制备方法
CN109574916A (zh) * 2018-12-29 2019-04-05 常州吉恩药业有限公司 阿扎那韦中间体2-[4-(2-吡啶基)苄基]-肼羧酸叔丁酯的工业化生产方法
US20230218644A1 (en) 2020-04-16 2023-07-13 Som Innovation Biotech, S.A. Compounds for use in the treatment of viral infections by respiratory syndrome-related coronavirus
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Also Published As

Publication number Publication date
CA2250840A1 (en) 1997-10-30
AU706183B2 (en) 1999-06-10
PT900210E (pt) 2005-06-30
IL126381A0 (en) 1999-05-09
CY2596B2 (en) 2010-03-03
FR05C0030I1 (ru) 2005-08-12
JP3174347B2 (ja) 2001-06-11
TW409125B (en) 2000-10-21
DE69732483D1 (de) 2005-03-17
CA2510945A1 (en) 1997-10-30
DE122005000003I1 (de) 2005-05-25
CA2568104C (en) 2009-08-04
NO313330B1 (no) 2002-09-16
HK1018788A1 (en) 2000-01-07
NZ509046A (en) 2002-05-31
AR006720A1 (es) 1999-09-08
LU91189I2 (fr) 2005-10-03
CN1319587A (zh) 2001-10-31
CZ296135B6 (cs) 2006-01-11
ATE288903T1 (de) 2005-02-15
FR05C0030I2 (fr) 2007-04-27
CA2250840C (en) 2006-07-04
DE69732483T2 (de) 2005-07-28
ES2238720T3 (es) 2005-09-01
CN1216539A (zh) 1999-05-12
CA2510945C (en) 2007-01-16
EP0900210B1 (en) 2005-02-09
EA001794B1 (ru) 2001-08-27
NZ509045A (en) 2002-09-27
WO1997040029A1 (en) 1997-10-30
HUP9901612A3 (en) 2000-06-28
CN1193010C (zh) 2005-03-16
CN1082508C (zh) 2002-04-10
CZ337398A3 (cs) 1999-01-13
HK1075043A1 (en) 2005-12-02
CA2568104A1 (en) 1997-10-30
MY114457A (en) 2002-10-31
IL126381A (en) 2001-08-26
HUP9901612A2 (hu) 1999-08-30
DK0900210T3 (da) 2005-05-02
HU224125B1 (hu) 2005-05-30
SI0900210T1 (ru) 2005-08-31
SK145298A3 (en) 1999-06-11
NZ332118A (en) 2001-02-23
JPH11511177A (ja) 1999-09-28
NO984900L (no) 1998-12-21
EP0900210A1 (en) 1999-03-10
NL300203I1 (nl) 2005-10-03
AU2385997A (en) 1997-11-12
SK285048B6 (sk) 2006-05-04
CN1616453A (zh) 2005-05-18
BR9701877A (pt) 1998-09-29
NO984900D0 (no) 1998-10-21
NO2005010I1 (no) 2005-05-02
LU91189I9 (ru) 2018-12-27
NL300203I2 (nl) 2005-11-01
CN1310905C (zh) 2007-04-18

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