EA201270540A1 - Макроциклические ингибиторы интегразы - Google Patents

Макроциклические ингибиторы интегразы

Info

Publication number
EA201270540A1
EA201270540A1 EA201270540A EA201270540A EA201270540A1 EA 201270540 A1 EA201270540 A1 EA 201270540A1 EA 201270540 A EA201270540 A EA 201270540A EA 201270540 A EA201270540 A EA 201270540A EA 201270540 A1 EA201270540 A1 EA 201270540A1
Authority
EA
Eurasian Patent Office
Prior art keywords
integrases
macrocyclic inhibitors
inhibitors
macrocyclic
piperazine
Prior art date
Application number
EA201270540A
Other languages
English (en)
Other versions
EA019558B1 (ru
Inventor
Йоханнес Вильхельмус Й. Тюринг
Жан-Франсуа Бонфанти
Жером Мишель Клод Фортэн
Original Assignee
Эланко Энимал Хэлс Аиэлэнд Лимитед
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
Application filed by Эланко Энимал Хэлс Аиэлэнд Лимитед filed Critical Эланко Энимал Хэлс Аиэлэнд Лимитед
Publication of EA201270540A1 publication Critical patent/EA201270540A1/ru
Publication of EA019558B1 publication Critical patent/EA019558B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/18—Bridged systems
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D515/18—Bridged systems

Abstract

Соединение, имеющее формулу (I)где W представляет собой -NH-, -N(CH)- или пиперазин, Х представляет собой связь, -С(=O)- или -S(=O)-, Y представляет собой Cалкилен и Z представляет собой -NH-C(=O)- или -О-, и его фармацевтически приемлемые соли, фармацевтические композиции и их применение в качестве ингибиторов ВИЧ.
EA201270540A 2009-10-13 2010-10-13 Макроциклические ингибиторы интегразы EA019558B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09172853 2009-10-13
PCT/EP2010/065300 WO2011045330A1 (en) 2009-10-13 2010-10-13 Macrocyclic integrase inhibitors

Publications (2)

Publication Number Publication Date
EA201270540A1 true EA201270540A1 (ru) 2012-09-28
EA019558B1 EA019558B1 (ru) 2014-04-30

Family

ID=41720665

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201270540A EA019558B1 (ru) 2009-10-13 2010-10-13 Макроциклические ингибиторы интегразы

Country Status (15)

Country Link
US (1) US8497270B2 (ru)
EP (1) EP2488521B1 (ru)
JP (1) JP5624148B2 (ru)
KR (1) KR20120087916A (ru)
CN (1) CN102574854B (ru)
AU (1) AU2010305805B2 (ru)
BR (1) BR112012008586A2 (ru)
CA (1) CA2777664C (ru)
EA (1) EA019558B1 (ru)
ES (1) ES2446720T3 (ru)
IL (1) IL218845A0 (ru)
MX (1) MX2012004426A (ru)
NZ (1) NZ598766A (ru)
WO (1) WO2011045330A1 (ru)
ZA (1) ZA201202516B (ru)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2487176A1 (en) * 2011-02-14 2012-08-15 Elanco Animal Health Ireland Limited Macrocyclic integrase inhibitors for use in the treatment of feline immunodeficiency virus
WO2014008636A1 (en) * 2012-07-11 2014-01-16 Merck Sharp & Dohme Corp. Macrocyclic compounds as hiv integrase inhibitors
EP2931730B1 (en) 2012-12-17 2019-08-07 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as hiv integrase inhibitors
EP2986291B1 (en) 2013-04-16 2020-05-27 Merck Sharp & Dohme Corp. 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors
US9643982B2 (en) 2013-05-17 2017-05-09 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as HIV integrase inhibitors
WO2014200880A1 (en) 2013-06-13 2014-12-18 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
JP6081662B2 (ja) 2013-09-27 2017-02-15 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． Ｈｉｖインテグラーゼ阻害薬として有用な置換されたキノリジン誘導体
WO2016187788A1 (en) 2015-05-25 2016-12-01 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds useful for treating hiv infection
MX2017017097A (es) * 2015-07-02 2018-05-23 Tp Therapeutics Inc Macrociclos diarílicos quirales como moduladores de proteínas quinasas.
MX2018000718A (es) 2015-07-21 2020-01-20 Turning Point Therapeutics Inc Macrociclos de diarilo quirales y usos de los mismos.
US10548910B2 (en) 2015-11-17 2020-02-04 Merck Sharp & Dohme Corp. Amido-substituted pyridotriazine derivatives useful as HIV integrase inhibitors
EP3389380B1 (en) 2015-12-15 2021-07-21 Merck Sharp & Dohme Corp. Spirocyclic quinolizine derivatives useful as hiv integrase inhibitors
WO2017113288A1 (en) 2015-12-31 2017-07-06 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
CA3042314A1 (en) 2016-12-02 2018-06-07 Merck Sharp & Dohme Corp. Tricyclic heterocycle compounds useful as hiv integrase inhibitors
JOP20190130A1 (ar) 2016-12-02 2019-06-02 Merck Sharp & Dohme مركبات حلقية غير متجانسة رباعية الحلقات مفيدة كمثبطات إنزيم مدمج لفيروس نقص المناعة البشرية (hiv)
TWI808958B (zh) 2017-01-25 2023-07-21 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
US10786488B2 (en) 2017-01-26 2020-09-29 Merck Sharp & Dohme Corp. Substituted quinolizine derivatives useful as HIV integrase inhibitors
WO2019023417A1 (en) 2017-07-28 2019-01-31 Tp Therapeutics, Inc. MACROCYCLIC COMPOUNDS AND USES THEREOF
CN111511746B (zh) 2017-12-19 2024-01-09 特普医药公司 用于治疗疾病的巨环化合物
CA3128961A1 (en) 2019-03-22 2020-10-01 Hang CHU Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use
CR20220418A (es) 2020-02-24 2022-10-10 Gilead Sciences Inc Compuestos tetracíclicos para el tratamiento de infecciones por vih
CN112358477A (zh) * 2020-11-10 2021-02-12 牡丹江医学院 一种用于治疗胆囊炎的药物及其制备方法
LT4196479T (lt) 2021-01-19 2023-12-11 Gilead Sciences, Inc. Pakeistieji piridotriazino junginiai ir jų panaudojimo būdai

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CS210880B1 (cs) 1979-10-19 1982-01-29 Jiri Krepelka Substituované imidy kyselin 4-arylnaftalen-2,3-dikarboxylových
CS225002B1 (cs) 1980-12-12 1984-02-13 Krepelka Jiri Deriváty 9-fenyl-1H-benzo/f/isoindol-1,3-dionu a způsob jejich výroby
JPH04217684A (ja) 1990-05-30 1992-08-07 Shionogi & Co Ltd アルド−ス還元酵素阻害物質
CA2176011A1 (en) * 1994-09-13 1996-03-21 Yoshiaki Nonomura Anti-hiv drug
WO2002036734A2 (en) 2000-10-12 2002-05-10 Merck & Co., Inc. Aza-and polyaza-naphthalenyl ketones useful as hiv integrase inhibitors
EP1326610B1 (en) 2000-10-12 2006-11-15 Merck & Co., Inc. Aza-and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
CA2425440C (en) * 2000-10-12 2010-04-13 Merck & Co., Inc. Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
WO2002030426A1 (en) 2000-10-12 2002-04-18 Merck & Co., Inc. Aza- and polyaza-naphthalenyl-carboxamides useful as hiv integrase inhibitors
US20040157804A1 (en) 2002-10-16 2004-08-12 Gilead Sciences, Inc. Pre-organized tricyclic integrase inhibitor compounds
TR200401663T1 (tr) 2002-11-20 2005-04-21 Japan Tobacco Inc. 4-oksokuinolin bileşiği ve bunun HIV integraz inhibitörü olarak kullanımı.
JP4733986B2 (ja) 2002-12-27 2011-07-27 イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・ピー・アー ＨＩＶインテグラーゼ阻害薬として有用なテトラヒドロ−４Ｈ−ピリド［１，２−ａ］ピリミジン類および関連する化合物
US6890942B2 (en) 2003-05-16 2005-05-10 Bristol-Myers Squibb Company Acyl sulfonamides as inhibitors of HIV integrase
AU2004274493A1 (en) 2003-09-19 2005-03-31 Gilead Sciences, Inc. Aza-quinolinol phosphonate integrase inhibitor compounds
CN1930161A (zh) 2004-03-09 2007-03-14 P·安杰莱蒂分子生物学研究所 Hiv整合酶抑制剂
US7176196B2 (en) 2004-05-28 2007-02-13 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
AU2006239177B8 (en) 2005-04-28 2012-02-16 Shionogi & Co., Ltd. Polycyclic carbamoylpyridone derivative having HIV integrase inhibitory activity
EP1910363A4 (en) * 2005-08-04 2010-05-26 Glaxosmithkline Llc INHIBITORS OF HIV INTEGRASE
AU2006307101A1 (en) * 2005-10-27 2007-05-03 Shionogi & Co., Ltd. Polycyclic carbamoylpyridone derivative having inhibitory activity on HIV integrase
US8039458B2 (en) * 2005-11-17 2011-10-18 Bristol-Myers Squibb Company HIV integrase inhibitors
TW200811153A (en) 2006-06-23 2008-03-01 Japan Tobacco Inc 6-(heterocyclyl-substituted benzyl)-4-oxoquinoline compound and use thereof as HIV integrase inhibitor
DK2283024T3 (da) * 2008-03-10 2013-08-05 Janssen Pharmaceutica Nv 4-aryl-2-anilinpyrimidiner som PLK-kinaseinhibitorer

Also Published As

Publication number Publication date
NZ598766A (en) 2013-09-27
ES2446720T3 (es) 2014-03-10
AU2010305805B2 (en) 2014-04-03
EP2488521A1 (en) 2012-08-22
JP2013507423A (ja) 2013-03-04
EP2488521B1 (en) 2013-12-18
AU2010305805A1 (en) 2012-04-19
CN102574854A (zh) 2012-07-11
IL218845A0 (en) 2012-06-28
CA2777664A1 (en) 2011-04-21
US8497270B2 (en) 2013-07-30
MX2012004426A (es) 2012-07-30
ZA201202516B (en) 2013-09-25
EA019558B1 (ru) 2014-04-30
WO2011045330A1 (en) 2011-04-21
CA2777664C (en) 2014-06-10
BR112012008586A2 (pt) 2016-11-29
US20120172367A1 (en) 2012-07-05
JP5624148B2 (ja) 2014-11-12
KR20120087916A (ko) 2012-08-07
CN102574854B (zh) 2014-04-16

Similar Documents

Publication Publication Date Title
EA201270540A1 (ru) Макроциклические ингибиторы интегразы
UA108640C2 (ru) Производные n-(имидазопиримидин 7-ил) гетероариламидов и их применение в качестве ингибиторов pde10a
BR112012024796A2 (pt) inibidores de integrase macrocíclicos
CO6460772A2 (es) Inhibidores de la replicación del virus de la inmunodeficiencia humana
EA201170434A1 (ru) Макроциклические ингибиторы сериновых протеаз гепатита с
DK2235017T3 (da) Spiroindolinonderivater som anticancermidler
RS54123B1 (en) THERAPEUTIC COMBINATION CONTAINING DOLUTEGRAVIR, ABACAVIR AND LAMIVUDINE
ATE519764T1 (de) Spiroindolinon-derivate
RS53503B1 (en) AMORPHIC AND CRYSTAL FORM GENZ 112638 HEMITARTARATE AS A GLYCOSILKERAMIDE SYNTHASIS INHIBITOR
CO6571861A2 (es) Derivado de 1,3,4,8-tetrahidro-2h-pirido[1,2-a]pirazina y su uso como inhibidor de la integrasa del vih
EA200801144A1 (ru) Полициклическое карбамоилпиридоновое производное, обладающее ингибиторной активностью в отношении интегразы вич
BRPI1009333B8 (pt) compostos inibidores de beta-secretase, seus usos, bem como composição farmacêutica
TW200833324A (en) Sulfonamide derivatives
MY150661A (en) Pyridin-3-yl derivatives as immunomodulating agents
MX2011013771A (es) Derivados de imidazolidin-2-ona 1,3-disustituida como inhibidores de cyp17.
MX2011013884A (es) Sulfonamidas heterociclicas, usos y composiciones farmaceuticas de las mismas.
CY1117792T1 (el) Ανταγωνιστες toy trpv4
ATE495176T1 (de) Spiroindolinon-derivate
IN2012DN03337A (ru)
EA201201050A1 (ru) Пиразолы в качестве антагонистов crth2
MY183312A (en) Pharmaceutical formulation
EA200900924A1 (ru) Циклизованные производные как ингибиторы eg-5
IN2012DN01232A (ru)
MY161749A (en) Compound, certain novel forms thereof, pharmaceutical compositions thereof and methods for preparation and use
UY30001A1 (es) Alquilsulfonamida quinolinas

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU