SG10201912040RA - Synthesis of polycyclic-carbamoylpyridone compounds - Google Patents

Synthesis of polycyclic-carbamoylpyridone compounds

Info

Publication number
SG10201912040RA
SG10201912040RA SG10201912040RA SG10201912040RA SG10201912040RA SG 10201912040R A SG10201912040R A SG 10201912040RA SG 10201912040R A SG10201912040R A SG 10201912040RA SG 10201912040R A SG10201912040R A SG 10201912040RA SG 10201912040R A SG10201912040R A SG 10201912040RA
Authority
SG
Singapore
Prior art keywords
polycyclic
synthesis
carbamoylpyridone compounds
carbamoylpyridone
compounds
Prior art date
Application number
SG10201912040RA
Other languages
English (en)
Inventor
Anna Chiu
John Enquist
Nolan Griggs
Christopher Hale
Norihiro Ikemoto
Katie Ann Keaton
Matt Kraft
Scott E Lazerwith
Michel Leeman
Zhihui Peng
Kate Schrier
Jonathan Trinidad
Jochem Van Herpt
Andrew W Waltman
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
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of SG10201912040RA publication Critical patent/SG10201912040RA/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/02—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
    • 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
    • C07D498/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/10—Separation; Purification; Stabilisation; Use of additives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/02—Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/72—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
    • C07C235/80—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms having carbon atoms of carboxamide groups and keto groups bound to the same carbon atom, e.g. acetoacetamides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/16—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and unsaturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/20—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C269/06—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/34—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D309/36—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
    • C07D309/40—Oxygen atoms attached in positions 3 and 4, e.g. maltol
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/04—1,3-Dioxanes; Hydrogenated 1,3-dioxanes
    • C07D319/06—1,3-Dioxanes; Hydrogenated 1,3-dioxanes not condensed with other rings
    • 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
    • C07D471/02—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 two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • 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
    • C07D471/22—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 systems contains four or more hetero rings
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyrane Compounds (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
SG10201912040RA 2014-06-20 2015-06-16 Synthesis of polycyclic-carbamoylpyridone compounds SG10201912040RA (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201462015081P 2014-06-20 2014-06-20

Publications (1)

Publication Number Publication Date
SG10201912040RA true SG10201912040RA (en) 2020-02-27

Family

ID=53674256

Family Applications (2)

Application Number Title Priority Date Filing Date
SG10201912040RA SG10201912040RA (en) 2014-06-20 2015-06-16 Synthesis of polycyclic-carbamoylpyridone compounds
SG11201609945SA SG11201609945SA (en) 2014-06-20 2015-06-16 Synthesis of polycyclic-carbamoylpyridone compounds

Family Applications After (1)

Application Number Title Priority Date Filing Date
SG11201609945SA SG11201609945SA (en) 2014-06-20 2015-06-16 Synthesis of polycyclic-carbamoylpyridone compounds

Country Status (21)

Country Link
US (3) US20150368264A1 (enExample)
EP (3) EP3527573B9 (enExample)
JP (2) JP6581607B2 (enExample)
KR (2) KR101975912B1 (enExample)
CN (3) CN106470975B (enExample)
AR (2) AR100904A1 (enExample)
AU (3) AU2015277312B2 (enExample)
BR (2) BR112016029333B1 (enExample)
CA (2) CA2950300C (enExample)
EA (2) EA034169B1 (enExample)
ES (2) ES2718409T3 (enExample)
IL (3) IL249134B (enExample)
MX (2) MX363532B (enExample)
NZ (1) NZ726859A (enExample)
PL (2) PL3157933T3 (enExample)
PT (2) PT3527573T (enExample)
SG (2) SG10201912040RA (enExample)
SI (2) SI3157933T1 (enExample)
TR (1) TR201906366T4 (enExample)
TW (2) TWI744723B (enExample)
WO (1) WO2015195656A2 (enExample)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI3067358T1 (sl) 2012-12-21 2019-12-31 Gilead Sciences, Inc. Policiklične spojine karbamoilpiridona in njihova farmacevtska uporaba
IN2014CH00247A (enExample) 2014-01-21 2015-08-14 Laurus Labs Private Ltd
TWI744723B (zh) * 2014-06-20 2021-11-01 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
TW201613936A (en) 2014-06-20 2016-04-16 Gilead Sciences Inc Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
NO2717902T3 (enExample) 2014-06-20 2018-06-23
CN108348473B (zh) 2015-11-09 2021-06-18 吉利德科学公司 治疗人免疫缺陷病毒的治疗组合物
ZA201803942B (en) 2017-06-13 2021-05-26 Cipla Ltd Novel processes for preparation of integrase inhibitor
CN109020911B (zh) * 2018-04-16 2022-06-28 常州制药厂有限公司 用于制备bictegravir的中间体及其制备方法
CN108774145A (zh) * 2018-05-23 2018-11-09 安徽华昌高科药业有限公司 一种(1r,3s)-3-氨基环戊醇盐酸盐的制备方法
US11623933B2 (en) 2018-06-28 2023-04-11 Honour Lab Limited Process for the preparation of sodium (2R,5S,13AR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl) carbamoyl)-2,3,4,5,7,9,13,13A-octahydro-2,5-Methanopyrido[1 ′,2′:4,5]pyrazino[2,1 -b] [1,3] oxazepin-8-olate and its polymorphic form
US11634431B2 (en) 2018-07-12 2023-04-25 Laurus Labs Limited Process for purification of protected polycyclic carbamoylpyridone derivatives
CN110862325B (zh) * 2018-08-28 2020-08-25 重庆博腾制药科技股份有限公司 一种(1r,3s)-3-氨基-1-环戊醇及其盐的制备方法
CN111018725B (zh) * 2018-10-09 2023-07-07 上海迪赛诺化学制药有限公司 一种（1r,3s）-3-氨基环戊醇手性酸盐的制备方法
MX2021008661A (es) 2019-01-18 2021-08-19 Astrazeneca Ab Inhibidores de la pcsk9 y metodos de uso de los mismos.
CN109868293A (zh) * 2019-01-22 2019-06-11 湖南理工学院 一种酶催化酯交换动力学拆分2-氯扁桃酸对映体的方法
CN110041210A (zh) * 2019-05-06 2019-07-23 凯瑞斯德生化(苏州)有限公司 一种Bictegravir中间体及其制备方法
US11248005B2 (en) 2019-07-08 2022-02-15 Lupin Limited Process for preparation of intermediates used for the synthesis of HIV integrase inhibitor
CN111056939B (zh) * 2019-10-16 2022-08-05 弈柯莱生物科技(上海)股份有限公司 一种(1r,3s)-3-氨基环戊醇及其中间体的制备方法
CN112174929A (zh) * 2020-10-13 2021-01-05 台州市生物医化产业研究院有限公司 一种西他列汀关键中间体热解杂质及其制备方法和应用
WO2025184448A2 (en) 2024-03-01 2025-09-04 Gilead Sciences, Inc. Methods and intermediates for preparing therapeutic compounds

Family Cites Families (122)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE788516A (fr) 1971-09-10 1973-03-07 Lonza Ag Procede de fabrication d'esters alcoxyacetylacetiques
GB1528382A (en) 1974-12-26 1978-10-11 Teijin Ltd Cyclopentene diols and acyl esters thereof and processes for their preparation
DE2658401A1 (de) 1976-12-23 1978-07-06 Merck Patent Gmbh Cyclopentan-1-amine, verfahren zu ihrer herstellung und diese verbindungen enthaltende mittel
US4575694A (en) 1984-03-05 1986-03-11 Allied Corporation Coaxial connector
GB8729994D0 (en) 1987-12-23 1988-02-03 Glaxo Group Ltd Chemical compounds
DE3900735A1 (de) * 1989-01-12 1990-07-26 Hoechst Ag Neue mehrfunktionelle (alpha)-diazo-(beta)-ketoester, verfahren zu ihrer herstellung und deren verwendung
US6642245B1 (en) 1990-02-01 2003-11-04 Emory University Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane
US5204466A (en) 1990-02-01 1993-04-20 Emory University Method and compositions for the synthesis of bch-189 and related compounds
US6703396B1 (en) 1990-02-01 2004-03-09 Emory University Method of resolution and antiviral activity of 1,3-oxathiolane nuclesoside enantiomers
DE4014649A1 (de) * 1990-05-08 1991-11-14 Hoechst Ag Neue mehrfunktionelle verbindungen mit (alpha)-diazo-ss-ketoester- und sulfonsaeureester-einheiten, verfahren zu ihrer herstellung und deren verwendung
GB9301000D0 (en) 1993-01-20 1993-03-10 Glaxo Group Ltd Chemical compounds
FR2734822B1 (fr) 1995-05-30 1997-07-04 Rhone Poulenc Rorer Sa Nouveaux derives du 2-azabicyclo(2.2.1)heptane, leur preparation et leur application
US5922695A (en) 1996-07-26 1999-07-13 Gilead Sciences, Inc. Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability
SE9603285D0 (sv) 1996-09-10 1996-09-10 Astra Ab New compounds
CN1254335A (zh) 1997-04-04 2000-05-24 辉瑞产品公司 烟酰胺衍生物
SE9702772D0 (sv) 1997-07-22 1997-07-22 Astra Pharma Prod Novel compounds
US5935946A (en) 1997-07-25 1999-08-10 Gilead Sciences, Inc. Nucleotide analog composition and synthesis method
WO1999025345A1 (en) * 1997-11-14 1999-05-27 Merck & Co., Inc. Alpha-1a adrenergic receptor antagonists
PL347591A1 (en) * 1998-11-09 2002-04-08 Gastrin and cholecystokinin receptor ligands
GB2345058A (en) 1998-12-01 2000-06-28 Cerebrus Pharm Ltd Hydroxypyridone compounds useful in the treatment of oxidative damage to the central nervous system
PL348596A1 (en) 1998-12-25 2002-06-03 Shionogi & Co Aromatic heterocycle compounds having hiv integrase inhibiting activities
US20040039060A1 (en) 2000-06-14 2004-02-26 Ryuichi Kiyama Inhibitor for enzyme having two divalent metal ions as active centers
KR20030017655A (ko) 2000-07-27 2003-03-03 에프. 호프만-라 로슈 아게 글리코겐 신타아제 키나아제-3베타의 억제제로서의3-인돌릴-4-페닐-1ｈ-피롤-2,5-디온 유도체
US7250518B2 (en) 2001-01-31 2007-07-31 Pfizer Inc. Nicotinamide acids, amides, and their mimetics active as inhibitors of PDE4 isozymes
DK2266958T1 (da) 2001-08-10 2016-04-04 Shionogi & Co Antiviralt middel
TWI335221B (en) 2001-09-27 2011-01-01 Alcon Inc Inhibtors of glycogen synthase kinase-3 (gsk-3) for treating glaucoma
HUP0402503A2 (hu) 2001-10-03 2005-03-29 Ucb, S.A. Pirrolidinonszármazékok és a vegyületeket tartalmazó gyógyászati készítmények
SI1441735T1 (sl) 2001-10-26 2006-06-30 Angeletti P Ist Richerche Bio N-substituirani hidroksipirimidinon-karboksamidniinhibitorji HIV-integraze
WO2004004657A2 (en) 2002-07-09 2004-01-15 Bristol-Myers Squibb Company Hiv integrase inhibitors
EP1549315A4 (en) 2002-09-11 2007-05-23 Merck & Co Inc DIHYDROXYPYRIDOPYRAZINE-1,6-DION COMPOUNDS AS HIV INTEGRASE INHIBITORS
US7390803B2 (en) 2002-10-30 2008-06-24 Merck & Co., Inc. Tetrahydropyranyl cyclopentyl benzylamide modulators of chemokine receptor activity
BRPI0306214B1 (pt) 2002-11-20 2017-08-08 Japan Tobacco Inc. 4-oxoquinoline compound and use of this as a hiv integrase inhibitor
AU2004206821C1 (en) 2003-01-14 2009-10-01 Gilead Sciences, Inc. Compositions and methods for combination antiviral therapy
TW200510425A (en) 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
TW200528440A (en) 2003-10-31 2005-09-01 Fujisawa Pharmaceutical Co 2-cyanopyrrolidinecarboxamide compound
EP1713773A4 (en) 2004-01-30 2009-09-23 Merck & Co Inc N-BENZYL-3,4-DIHYDROXYPYRIDINE-2-CARBOXYLIC AMID AND N-BENZYL-2,3-DIHYDROXYPYRIDINE-4-CARBOXYLIC AMIDE COMPOUNDS SUITABLE AS INHIBITORS OF THE HIV INTEGRASE
AU2005220767A1 (en) 2004-03-09 2005-09-22 Merck & Co., Inc. HIV integrase inhibitors
WO2005110399A2 (en) 2004-04-29 2005-11-24 The Regents Of The University Of California Zinc-binding groups for metalloprotein inhibitors
EP1755586A2 (en) 2004-04-29 2007-02-28 The Regents of the University of California Hydroxypyridinone, hydroxypyridinethione, pyrone, and thiopyrone metalloprotein inhibitors
CN1964975B (zh) 2004-05-07 2011-11-30 默沙东公司 Hiv整合酶抑制剂
US7273859B2 (en) 2004-05-12 2007-09-25 Bristol-Myers Squibb Company HIV integrase inhibitors: cyclic pyrimidinone compounds
WO2005113509A1 (en) 2004-05-20 2005-12-01 Japan Tobacco Inc. Novel 4-oxoquinoline compound and use thereof as hiv integrase inhibitor
MY134672A (en) 2004-05-20 2007-12-31 Japan Tobacco Inc Stable crystal of 4-oxoquinoline compound
EP3287130A1 (en) 2004-05-21 2018-02-28 Japan Tobacco Inc. Combinations comprising a 4-isoquinolone derivative and protease inhibitors
US7550463B2 (en) 2004-09-15 2009-06-23 Shionogi & Co., Ltd. Carbamoylpyridone derivatives having inhibitory activity against HIV integrase
JP2006118669A (ja) 2004-10-25 2006-05-11 Sanoh Industrial Co Ltd 樹脂チューブ
WO2006066414A1 (en) 2004-12-23 2006-06-29 Virochem Pharma Inc. Hydroxydihydropyridopy razine-1,8-diones and methods for inhibiting hiv integrase
US7858788B2 (en) 2005-02-21 2010-12-28 Shionogi & Co., Ltd. Bicyclic carbamoylpyridone derivative having HIV integrase inhibitory activity
PL3372281T3 (pl) * 2005-04-28 2021-12-27 Viiv Healthcare Company Policykliczne pochodne karbamoilopirydonu o aktywności inhibitorowej wobec integrazy HIV
WO2006125048A2 (en) 2005-05-16 2006-11-23 Gilead Sciences, Inc. Hiv-integrase inhibitor compounds
EP1906971A2 (en) 2005-07-27 2008-04-09 Gilead Sciences, Inc. Antiviral compounds
BRPI0617842A2 (pt) 2005-10-27 2011-08-09 Shionogi & Co composto ou um sal farmaceuticamente aceitável ou um solvato do mesmo, e, composição farmacêutica
US7888376B2 (en) 2005-11-23 2011-02-15 Bristol-Myers Squibb Company Heterocyclic CETP inhibitors
KR101524165B1 (ko) 2005-12-30 2015-06-01 길리애드 사이언시즈, 인코포레이티드 Ｈｉｖ 인테그라제 억제제의 약동학을 개선하기 위한 방법
US7601844B2 (en) 2006-01-27 2009-10-13 Bristol-Myers Squibb Company Piperidinyl derivatives as modulators of chemokine receptor activity
US20090018162A1 (en) 2006-02-01 2009-01-15 Yuji Matsuzaki Use of 6-(3-chloro-2-fluorobenzyl)-1-[(2s)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or salt thereof for treating retrovirus infection
WO2007099385A1 (en) 2006-03-01 2007-09-07 Glenmark Pharmaceuticals S.A. Dipeptidyl peptidase iv inhibitor compounds and compositions
ES2531190T3 (es) 2006-03-06 2015-03-11 Japan Tobacco Inc Método para producir un compuesto de 4-oxoquinolina
WO2007102499A1 (ja) 2006-03-06 2007-09-13 Japan Tobacco Inc. ４－オキソキノリン化合物の製造方法
US7893055B2 (en) 2006-06-28 2011-02-22 Bristol-Myers Squibb Company HIV integrase inhibitors
MX2009000661A (es) 2006-07-19 2009-03-27 Univ Georgia Res Found Piridinon-diceto-acidos: inhibidores de replicacion de vih en terapia de combinacion.
HRP20090213B1 (hr) 2006-09-12 2016-12-02 Gilead Sciences, Inc. Postupak i međuprodukti u pripravi inhibitora integraze
EP2084160A1 (en) 2006-10-18 2009-08-05 Merck & Co., Inc. Hiv integrase inhibitors
UA98777C2 (en) 2006-11-20 2012-06-25 Эли Лилли Энд Компани Tetrahydrocyclopenta[b]indole compounds as androgen receptor modulators
ES2779826T3 (es) 2007-02-23 2020-08-20 Gilead Sciences Inc Moduladores de propiedades farmacocinéticas de agentes terapéuticos
US20080280945A1 (en) 2007-05-09 2008-11-13 Sachin Lohani Crystalline forms of an HIV integrase inhibitor
CN103356622A (zh) 2007-06-29 2013-10-23 吉里德科学公司 治疗用组合物及其用途
CN101686972B (zh) 2007-06-29 2013-08-14 吉里德科学公司 治疗用组合物和方法
EP2182801A4 (en) 2007-07-31 2011-04-13 Limerick Biopharma Inc COMPOSITIONS OF PYRONE ANALOGS AND METHODS
AR068403A1 (es) 2007-09-11 2009-11-18 Gilead Sciences Inc Proceso e intermediarios para la preparacion de inhibidores de integrasa
GB0803019D0 (en) 2008-02-19 2008-03-26 Btg Int Ltd Fluorinated compounds
US8129398B2 (en) 2008-03-19 2012-03-06 Bristol-Myers Squibb Company HIV integrase inhibitors
WO2009130496A1 (en) * 2008-04-22 2009-10-29 Astrazeneca Ab Substituted pyrimidin-5-carboxamides 281
WO2010011813A1 (en) 2008-07-23 2010-01-28 Alkermes, Inc. Complex of trospium and pharmaceutical compositions thereof
WO2010011818A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
WO2010011819A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
PL2320908T3 (pl) 2008-07-25 2014-06-30 Viiv Healthcare Co Proleki dolutegrawiru
KR101772610B1 (ko) 2008-07-25 2017-09-12 비이브 헬쓰케어 컴퍼니 화합물
WO2010011816A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
WO2010011815A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
JP5572168B2 (ja) * 2008-12-11 2014-08-13 ビーブ・ヘルスケア・カンパニー カルバモイルピリドンｈｉｖインテグラーゼ阻害剤の製造方法および中間体
US8624023B2 (en) 2008-12-11 2014-01-07 Shionogi & Co., Ltd. Synthesis of carbamoylpyridone HIV integrase inhibitors and intermediates
US8835461B2 (en) 2009-03-26 2014-09-16 Shionogi & Co., Ltd. Substituted 3-hydroxy-4-pyridone derivative
TWI518084B (zh) 2009-03-26 2016-01-21 鹽野義製藥股份有限公司 哌喃酮與吡啶酮衍生物之製造方法
PL2444400T3 (pl) 2009-06-15 2018-08-31 Shionogi & Co., Ltd. Podstawiona policykliczna pochodna karbamoilopirydonowa
US8637674B2 (en) * 2009-09-02 2014-01-28 Ewha University-Industry Collaboration Foundation Pyrazole derivatives, preparation method thereof, and composition for prevention and treatment of osteoporosis containing same
EA032868B1 (ru) 2010-01-27 2019-07-31 Вайв Хелткер Компани Комбинация для лечения вич-инфекции
NZ601847A (en) 2010-02-26 2014-03-28 Japan Tobacco Inc 1,3,4,8-tetrahydro-2h-pyrido[1,2-a]pyrazine derivative and use of same as hiv integrase inhibitor
TWI582097B (zh) 2010-03-23 2017-05-11 Ｖｉｉｖ醫療保健公司 製備胺甲醯吡啶酮衍生物及中間體之方法
WO2012009009A2 (en) 2010-07-14 2012-01-19 Addex Pharma S.A. Novel 2-amino-4-pyrazolyl-thiazole derivatives and their use as allosteric modulators of metabotropic glutamate receptors
DK3456721T3 (da) 2010-08-05 2021-04-26 Shionogi & Co Fremgangsmåde til at fremstille forbindelser som har hiv-integrase-inhiberende aktivitet.
US8987441B2 (en) 2010-09-24 2015-03-24 Shionogi & Co., Ltd. Substituted polycyclic carbamoyl pyridone derivative prodrug
WO2012106534A2 (en) 2011-02-02 2012-08-09 The Regents Of The University Of California Hiv integrase inhibitors
US20140213553A1 (en) 2011-05-03 2014-07-31 Concert Pharmaceuticals Inc. Carbamoylpyridone derivatives
US9328075B2 (en) 2011-05-05 2016-05-03 St. Jude Children's Research Hospital Pyrimidinone compounds and methods for treating influenza
US9121496B2 (en) 2011-06-29 2015-09-01 Arvinmeritor Technology, Llc Drive axle system and a method of control
ES2613180T3 (es) 2011-09-14 2017-05-23 Mapi Pharma Limited Forma amorfa de la sal sódica dolutegravir
US9246434B2 (en) 2011-09-26 2016-01-26 First Solar, Inc System and method for estimating the short circuit current of a solar device
RU2014113230A (ru) 2011-10-12 2015-11-20 Шионоги Энд Ко., Лтд. Полициклическое производное пиридона, обладающее ингибирующей активностью в отношении интегразы
EP2804864B1 (en) * 2011-12-12 2017-09-06 Bayer Intellectual Property GmbH Amino-substituted imidazopyridazines
CN106957282B (zh) 2011-12-21 2019-08-30 诺维拉治疗公司 B型肝炎抗病毒剂
WO2014008636A1 (en) 2012-07-11 2014-01-16 Merck Sharp & Dohme Corp. Macrocyclic compounds as hiv integrase inhibitors
WO2014014933A1 (en) 2012-07-20 2014-01-23 Merck Sharp & Dohme Corp. Hiv treatment with amido-substituted pyrimidinone derivatives
WO2014018449A1 (en) 2012-07-25 2014-01-30 Merck Sharp & Dohme Corp. Substituted naphthyridinedione derivatives as hiv integrase inhibitors
AU2013296289B2 (en) 2012-08-03 2017-10-05 Gilead Sciences, Inc. Process and intermediates for preparing integrase inhibitors
CA2890983A1 (en) * 2012-11-08 2014-05-15 Bristol-Myers Squibb Company Heteroaryl substituted pyridyl compounds useful as kinase modulators
KR20150093819A (ko) 2012-12-14 2015-08-18 글락소스미스클라인 엘엘씨 약제 조성물
EP2931730B1 (en) 2012-12-17 2019-08-07 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as hiv integrase inhibitors
US20160000721A1 (en) 2012-12-21 2016-01-07 Merck Sharp & Dohme Corp. Gastro-retentive formulations
SI3067358T1 (sl) 2012-12-21 2019-12-31 Gilead Sciences, Inc. Policiklične spojine karbamoilpiridona in njihova farmacevtska uporaba
US20140221355A1 (en) 2012-12-21 2014-08-07 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
AR094311A1 (es) 2012-12-27 2015-07-22 Japan Tobacco Inc Derivados de tetrahidroespiro-ciclopropil-pirido[1,2-a]pirazina inhibidores de la integrasa del hiv
EP3008044B1 (en) 2013-06-13 2018-11-21 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
AU2014286993B2 (en) 2013-07-12 2018-10-25 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their use for the treatment of HIV infections
WO2015039348A1 (en) 2013-09-23 2015-03-26 Merck Sharp & Dohme Corp. Tetracyclic heterocycle compounds useful as hiv integrase inhibitors
HK1221648A1 (zh) 2013-09-27 2017-06-09 Merck Sharp & Dohme Corp. 用作hiv整合酶抑制劑的取代喹嗪衍生物
WO2015076492A1 (ko) 2013-11-25 2015-05-28 주식회사 케이티 홈 네트워크 전송 선로의 간섭 완화 장치, 간섭 완화 방법 및 이를 이용한 통신 시스템
WO2015089847A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Spirocyclic heterocycle compounds useful as hiv integrase inhibitors
IN2014CH00247A (enExample) 2014-01-21 2015-08-14 Laurus Labs Private Ltd
NO2717902T3 (enExample) 2014-06-20 2018-06-23
TW201613936A (en) 2014-06-20 2016-04-16 Gilead Sciences Inc Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
TWI744723B (zh) * 2014-06-20 2021-11-01 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成

Also Published As

Publication number Publication date
MX363532B (es) 2019-03-27
WO2015195656A3 (en) 2016-03-24
MX2020001278A (es) 2020-03-12
TWI677489B (zh) 2019-11-21
KR102159892B1 (ko) 2020-09-25
WO2015195656A2 (en) 2015-12-23
PT3527573T (pt) 2020-10-07
CN114394983A (zh) 2022-04-26
NZ736697A (en) 2023-08-25
EP3157933B1 (en) 2019-02-27
AU2018217236B2 (en) 2020-03-05
EP3527573B9 (en) 2022-07-06
EA201992183A3 (ru) 2020-04-30
AR100904A1 (es) 2016-11-09
CA3059135C (en) 2023-12-05
EA201692412A1 (ru) 2017-06-30
CN110317212A (zh) 2019-10-11
KR101975912B1 (ko) 2019-05-09
PL3527573T3 (pl) 2020-12-28
US10975096B2 (en) 2021-04-13
US10519168B2 (en) 2019-12-31
KR20190049937A (ko) 2019-05-09
CA3059135A1 (en) 2015-12-23
AU2015277312A1 (en) 2016-12-15
PT3157933T (pt) 2019-05-31
IL260675B (en) 2020-03-31
JP2017521398A (ja) 2017-08-03
ES2821143T9 (es) 2022-10-11
EP3527573A1 (en) 2019-08-21
EP3527573B1 (en) 2020-08-12
CN106470975B (zh) 2019-04-26
JP6581607B2 (ja) 2019-09-25
JP2019218391A (ja) 2019-12-26
US20150368264A1 (en) 2015-12-24
IL273230A (en) 2020-04-30
US20200223866A1 (en) 2020-07-16
BR122021009062B1 (pt) 2022-10-11
TW202014400A (zh) 2020-04-16
EA201992183A2 (ru) 2020-01-16
US20180022757A1 (en) 2018-01-25
AU2018217236A1 (en) 2018-08-30
KR20170018063A (ko) 2017-02-15
SI3157933T1 (sl) 2019-05-31
EP3783001A1 (en) 2021-02-24
BR112016029333A2 (pt) 2017-08-22
CA2950300A1 (en) 2015-12-23
NZ726859A (en) 2017-12-22
CN110317212B (zh) 2022-10-21
TW201613853A (en) 2016-04-16
CN106470975A (zh) 2017-03-01
AR132627A2 (es) 2025-07-16
PL3157933T3 (pl) 2019-09-30
AU2020201369A1 (en) 2020-03-12
IL249134B (en) 2018-08-30
SG11201609945SA (en) 2017-01-27
SI3527573T1 (sl) 2020-10-30
MX2016016065A (es) 2017-03-28
AU2015277312B2 (en) 2018-08-30
TR201906366T4 (tr) 2019-05-21
EP3157933A2 (en) 2017-04-26
ES2821143T3 (es) 2021-04-23
CA2950300C (en) 2019-12-24
EA034169B1 (ru) 2020-01-14
IL249134A0 (en) 2017-01-31
BR112016029333B1 (pt) 2023-03-28
TWI744723B (zh) 2021-11-01
ES2718409T3 (es) 2019-07-01
JP6880127B2 (ja) 2021-06-02

Similar Documents

Publication Publication Date Title
IL273230A (en) Preparation of carbamoylpyridone-polycyclic compounds
IL255817B (en) Synthesis of heterocyclic compounds
ZA201701246B (en) Synthesis of dna
ZA201700880B (en) Polymorphs of selinexor
GB201416754D0 (en) Novel compounds
GB201417011D0 (en) Novel compounds
GB201405991D0 (en) Novel compounds
GB201417018D0 (en) Novel compounds
AP2016009432A0 (en) Novel compounds
GB201411239D0 (en) Novel compounds
GB201411236D0 (en) Novel compounds
GB201404002D0 (en) Novel compounds
IL258408B (en) Improved synthesis of honokiol
GB201512678D0 (en) Methods of chemical synthesis
PL3174849T3 (pl) Synteza pochodnych pirolidyny
HK40066086A (zh) 多环氨基甲醯基吡啶酮化合物的合成
GB201416951D0 (en) Method of synthesis
GB201408729D0 (en) Synthesis
SG11201605485QA (en) Synthesis method of 9-allylcamptothecin derivatives
GB201417021D0 (en) Novel compounds
GB201417041D0 (en) Novel compounds
GB201414614D0 (en) Novel compounds
GB201413451D0 (en) Novel compounds
GB201413260D0 (en) Novel compounds
GB201412689D0 (en) Novel compounds