KR101097623B1 - Ｈｉｖ 인테그라제 억제제로서의 비시클릭 헤테로사이클 - Google Patents

Ｈｉｖ 인테그라제 억제제로서의 비시클릭 헤테로사이클 Download PDF

Info

Publication number
KR101097623B1
KR101097623B1 KR1020067027455A KR20067027455A KR101097623B1 KR 101097623 B1 KR101097623 B1 KR 101097623B1 KR 1020067027455 A KR1020067027455 A KR 1020067027455A KR 20067027455 A KR20067027455 A KR 20067027455A KR 101097623 B1 KR101097623 B1 KR 101097623B1
Authority
KR
South Korea
Prior art keywords
oxo
methyl
oxazine
dimethyl
hydroxy
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
KR1020067027455A
Other languages
English (en)
Korean (ko)
Other versions
KR20070039502A (ko
Inventor
비. 나라시물루 나이두
자크. 방빌
프란시스 베를류
티모시 피. 콘놀리
마크 알. 크리스탈
존 디. 마티스켈라
칼 월렛
서지 플라몬돈
로저 레밀라드
마가렛 이. 소렌손
야스쯔구 우에다
마이클 에이. 워커
Original Assignee
브리스톨-마이어스 스큅 컴퍼니
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 브리스톨-마이어스 스큅 컴퍼니 filed Critical 브리스톨-마이어스 스큅 컴퍼니
Publication of KR20070039502A publication Critical patent/KR20070039502A/ko
Application granted granted Critical
Publication of KR101097623B1 publication Critical patent/KR101097623B1/ko
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • 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
    • C07D498/02—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 two hetero rings
    • C07D498/04—Ortho-condensed 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • 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
    • 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
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020067027455A 2004-05-28 2006-12-27 Ｈｉｖ 인테그라제 억제제로서의 비시클릭 헤테로사이클 Expired - Fee Related KR101097623B1 (ko)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US57551304P 2004-05-28 2004-05-28
US60/575,513 2004-05-28
US60337104P 2004-08-20 2004-08-20
US60/603,371 2004-08-20
US11/126,891 US7176196B2 (en) 2004-05-28 2005-05-11 Bicyclic heterocycles as HIV integrase inhibitors
US11/126,891 2005-05-11
PCT/US2005/016473 WO2005118593A1 (en) 2004-05-28 2005-05-12 Bicyclic heterocycles as hiv integrase inhibitors

Publications (2)

Publication Number Publication Date
KR20070039502A KR20070039502A (ko) 2007-04-12
KR101097623B1 true KR101097623B1 (ko) 2011-12-22

Family

ID=35456854

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020067027455A Expired - Fee Related KR101097623B1 (ko) 2004-05-28 2006-12-27 Ｈｉｖ 인테그라제 억제제로서의 비시클릭 헤테로사이클

Country Status (26)

Country Link
US (2) US7176196B2 (https=)
EP (1) EP1749011B1 (https=)
JP (1) JP4874959B2 (https=)
KR (1) KR101097623B1 (https=)
AR (1) AR049124A1 (https=)
AT (1) ATE412656T1 (https=)
AU (1) AU2005250356C1 (https=)
BR (1) BRPI0511623A (https=)
CA (1) CA2568356C (https=)
CY (1) CY1110266T1 (https=)
DE (1) DE602005010690D1 (https=)
DK (1) DK1749011T3 (https=)
ES (1) ES2315875T3 (https=)
HR (1) HRP20090005T3 (https=)
IL (1) IL179455A (https=)
MX (1) MXPA06013835A (https=)
NO (1) NO20065879L (https=)
NZ (1) NZ551282A (https=)
PE (1) PE20060242A1 (https=)
PL (1) PL1749011T3 (https=)
PT (1) PT1749011E (https=)
RS (1) RS50700B (https=)
RU (1) RU2381228C2 (https=)
SI (1) SI1749011T1 (https=)
TW (1) TWI366567B (https=)
WO (1) WO2005118593A1 (https=)

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7115601B2 (en) 2004-05-18 2006-10-03 Bristol-Myers Squibb Company HIV integrase inhibitors
CA2600832C (en) * 2005-03-31 2011-12-13 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Hiv integrase inhibitors
US7494984B2 (en) * 2005-08-31 2009-02-24 Bristol-Myers Squibb Company Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors
US7939537B2 (en) 2005-10-04 2011-05-10 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. HIV integrase inhibitors
US7902182B2 (en) * 2005-11-16 2011-03-08 Bristol-Myers Squibb Company HIV integrase inhibitors
WO2007064316A1 (en) * 2005-11-30 2007-06-07 Bristol-Myers Squibb Company Bicyclic heterocycles as hiv integrase inhibitors
US20070129379A1 (en) * 2005-12-01 2007-06-07 Bristol-Myers Squibb Company Hiv integrase inhibitors
WO2007064502A1 (en) * 2005-12-01 2007-06-07 Bristol-Myers Squibb Company Forms of n-[(4-fluorophenyl)methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide
WO2007143446A1 (en) * 2006-05-30 2007-12-13 Bristol-Myers Squibb Company Spiro-condensed heterotricyclic compounds as hiv integrase inhibitors
US7893055B2 (en) * 2006-06-28 2011-02-22 Bristol-Myers Squibb Company HIV integrase inhibitors
JP2009543865A (ja) * 2006-07-19 2009-12-10 ユニバーシティ オブ ジョージア リサーチ ファウンデーション， インコーポレーテッド ピリジノンジケト酸：併用療法におけるｈｉｖ複製の阻害剤
US7763630B2 (en) * 2007-06-06 2010-07-27 Bristol-Myers Squibb Company HIV integrase inhibitors
US8129398B2 (en) * 2008-03-19 2012-03-06 Bristol-Myers Squibb Company HIV integrase inhibitors
WO2009120841A1 (en) * 2008-03-27 2009-10-01 Bristol-Myers Squibb Company Crystalline form of n-[[4-fluoro-2-(5-methyl-1h-1,2,4-triazol-1-yl)phenyl]methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide, sodium salt monohydrate
WO2010042391A2 (en) * 2008-10-06 2010-04-15 Merck Sharp & Dohme Corp. Hiv integrase inhibitors
US8143244B2 (en) * 2009-02-26 2012-03-27 Bristol-Myers Squibb Company Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
ES2446720T3 (es) 2009-10-13 2014-03-10 Elanco Animal Health Ireland Limited Inhibidores de la integrasa macrocíclica
US8383639B2 (en) 2009-10-15 2013-02-26 Bristol-Myers Squibb Company HIV integrase inhibitors
EA201270651A1 (ru) 2009-12-07 2013-01-30 Юниверсити Оф Джорджия Рисерч Фаундейшн, Инк. Карбоксамиды пиридинон гидроксициклопентила: ингибиторы вич интегразы и области терапевтического применения
LT3494972T (lt) 2010-01-27 2024-03-12 Viiv Healthcare Company Dolutegraviro ir lamivudino kompozicija živ infekcijai gydyti
WO2011121105A1 (en) 2010-04-02 2011-10-06 Tibotec Pharmaceuticals Macrocyclic integrase inhibitors
JP5996532B2 (ja) 2010-07-15 2016-09-21 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 有害生物防除剤としての新規複素環式化合物
US8791108B2 (en) 2011-08-18 2014-07-29 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
ES3018133T3 (en) 2011-11-30 2025-05-14 Univ Emory Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae
WO2013111118A2 (en) * 2012-01-26 2013-08-01 Cro Consulting Limited Agents for treating neurodegenerative disorders
EP2931730B1 (en) 2012-12-17 2019-08-07 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as hiv integrase inhibitors
US9493479B2 (en) 2013-04-16 2016-11-15 Merck Sharp & Dohme Corp. Substituted pyrido[1,2-a]pyrazines as HIV integrase inhibitors
RS56701B1 (sr) 2013-05-17 2018-03-30 Merck Sharp & Dohme Fuzionisana triciklična heterociklična jedinjenja kao inhibitori hiv integraze
EP3008044B1 (en) 2013-06-13 2018-11-21 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
UA117499C2 (uk) 2013-09-27 2018-08-10 Мерк Шарп Енд Доум Корп. Заміщені похідні хінолізину, які можна використовувати як інгібітори інтегрази віл
WO2016187788A1 (en) 2015-05-25 2016-12-01 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds useful for treating hiv infection
US10548910B2 (en) 2015-11-17 2020-02-04 Merck Sharp & Dohme Corp. Amido-substituted pyridotriazine derivatives useful as HIV integrase inhibitors
US10544155B2 (en) 2015-12-15 2020-01-28 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
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)
CA3042314A1 (en) 2016-12-02 2018-06-07 Merck Sharp & Dohme Corp. Tricyclic heterocycle compounds useful as hiv integrase inhibitors
EP3573984A4 (en) 2017-01-26 2020-07-29 Merck Sharp & Dohme Corp. USEFUL SUBSTITUTE QUINOLIZINE DERIVATIVES AS HIV INTEGRASE INHIBITORS
WO2021050555A1 (en) * 2019-09-10 2021-03-18 X-Chem, Inc. Compositions and uses thereof
CN113912622B (zh) * 2020-07-10 2023-12-01 上海纽思克生物科技有限公司 三环嘧啶酮类化合物、其制备方法、其组合物和用途

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003035077A1 (en) 2001-10-26 2003-05-01 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5693641A (en) * 1996-08-16 1997-12-02 Berlex Laboratories Inc. Bicyclic pyrimidine derivatives and their use as anti-coagulants
ATE355064T1 (de) 2001-10-26 2006-03-15 Angeletti P Ist Richerche Bio Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase
EP1539762A2 (en) 2002-06-26 2005-06-15 Bristol-Myers Squibb Company Bicyclic pyrimidinones as coagulation cascade inhibitors
NZ540729A (en) 2002-12-27 2008-03-28 Angeletti P Ist Richerche Bio Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds useful as HIV integrase inhibitors
AR046938A1 (es) 2003-12-12 2006-01-04 Merck & Co Inc Procedimiento para preparar hexahidropirimido[1,2-a]azepin-2-carboxilatos y compuetos similares
TW200526635A (en) 2003-12-22 2005-08-16 Shionogi & Co Hydroxypyrimidinone derivative having HIV integrase inhibitory activity
BRPI0518741A2 (pt) 2004-12-03 2008-12-02 Merck & Co Inc uso de uma combinaÇço de uma droga diretamente metabolizada por ugt1a1 ou um seu sal farmaceuticamente aceitÁvel e atazanavir ou um seu sal farmaceuticamente aceitÁvel, e, combinaÇço farmacÊutica para administraÇço oral a um mamÍfero
CA2600832C (en) 2005-03-31 2011-12-13 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Hiv integrase inhibitors

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003035077A1 (en) 2001-10-26 2003-05-01 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase

Also Published As

Publication number Publication date
AR049124A1 (es) 2006-06-28
EP1749011A1 (en) 2007-02-07
EP1749011B1 (en) 2008-10-29
AU2005250356B2 (en) 2011-03-17
IL179455A (en) 2011-10-31
SI1749011T1 (sl) 2009-08-31
US20060276466A1 (en) 2006-12-07
RS50700B (sr) 2010-06-30
PL1749011T3 (pl) 2009-04-30
CY1110266T1 (el) 2015-01-14
US7511037B2 (en) 2009-03-31
WO2005118593A1 (en) 2005-12-15
JP2008501018A (ja) 2008-01-17
RU2381228C2 (ru) 2010-02-10
TWI366567B (en) 2012-06-21
NZ551282A (en) 2009-05-31
JP4874959B2 (ja) 2012-02-15
TW200600503A (en) 2006-01-01
CA2568356A1 (en) 2005-12-15
HK1107343A1 (en) 2008-04-03
PE20060242A1 (es) 2006-03-31
DK1749011T3 (da) 2009-02-16
NO20065879L (no) 2007-02-20
RU2006146970A (ru) 2008-07-10
PT1749011E (pt) 2008-11-27
KR20070039502A (ko) 2007-04-12
US7176196B2 (en) 2007-02-13
HRP20090005T3 (hr) 2009-02-28
IL179455A0 (en) 2007-05-15
US20050267105A1 (en) 2005-12-01
BRPI0511623A (pt) 2008-03-11
DE602005010690D1 (de) 2008-12-11
MXPA06013835A (es) 2007-02-02
ES2315875T3 (es) 2009-04-01
CA2568356C (en) 2012-07-03
ATE412656T1 (de) 2008-11-15
AU2005250356C1 (en) 2011-10-06
AU2005250356A1 (en) 2005-12-15

Similar Documents

Publication Publication Date Title
KR101097623B1 (ko) Ｈｉｖ 인테그라제 억제제로서의 비시클릭 헤테로사이클
US8039458B2 (en) HIV integrase inhibitors
US7157447B2 (en) Bicyclic heterocycles as HIV integrase inhibitors
US7897593B2 (en) HIV integrase inhibitors
US7419969B2 (en) HIV integrase inhibitors: cyclic pyrimidinone compounds
AU2006315446A1 (en) HIV integrase inhibitors
US20070129379A1 (en) Hiv integrase inhibitors
US7763630B2 (en) HIV integrase inhibitors
US7491819B1 (en) N-[4-Fluorophenyl)methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide as an HIV integrase inhibitor
WO2007064316A1 (en) Bicyclic heterocycles as hiv integrase inhibitors
CN1989141B (zh) 作为hiv整合酶抑制剂的双环杂环
HK1107343B (en) Bicyclic heterocycles as hiv integrase inhibitors

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

A201 Request for examination
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

FPAY Annual fee payment

Payment date: 20141126

Year of fee payment: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

FPAY Annual fee payment

Payment date: 20151118

Year of fee payment: 5

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 5

LAPS Lapse due to unpaid annual fee
PC1903 Unpaid annual fee

St.27 status event code: A-4-4-U10-U13-oth-PC1903

Not in force date: 20161216

Payment event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

PC1903 Unpaid annual fee

St.27 status event code: N-4-6-H10-H13-oth-PC1903

Ip right cessation event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

Not in force date: 20161216

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000