[go: up one dir, main page]

PE20120508A1 - Inhibidores de la replicacion de los virus de la gripe - Google Patents

Inhibidores de la replicacion de los virus de la gripe

Info

Publication number
PE20120508A1
PE20120508A1 PE2011002120A PE2011002120A PE20120508A1 PE 20120508 A1 PE20120508 A1 PE 20120508A1 PE 2011002120 A PE2011002120 A PE 2011002120A PE 2011002120 A PE2011002120 A PE 2011002120A PE 20120508 A1 PE20120508 A1 PE 20120508A1
Authority
PE
Peru
Prior art keywords
alkyl
halogen
aromatic
optionally replaced
ilamino
Prior art date
Application number
PE2011002120A
Other languages
English (en)
Inventor
Paul Charifson
Michael P Clark
Upul K Bandarage
Randy S Bethiel
John J Court
Hongo Deng
Iona Drutu
John P Duffy
Luc Farmer
Huai Gao
Wexin Gu
Dylan H Jacobs
Joseph M Kennedy
Mark W Ledeboer
Brian Ledford
Francois Maltais
Emanuele Perola
Tiansheng Wang
M Woods Wannamaker
Randal Byrn
Yi Zhou
Chao Lin
Min Jiang
Steven Jones
Ursula A Germann
Francesco G Salituro
Ann Dak-Yee Kwong
Original Assignee
Vertex Pharma
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=42537408&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20120508(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of PE20120508A1 publication Critical patent/PE20120508A1/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • A61P31/14Antivirals for RNA viruses
    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/30Halogen atoms or nitro radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

REFERIDA A UN DERIVADO DE PIRROLOPIRIDINA DE FORMULA (IA), DONDE Z1 ES F, Cl, CN, NO2, ENTRE OTROS; Z2 ES R*, OR*, CO2R*, ENTRE OTROS; Z3 ES H, OH, NH2, HALOGENO, ENTRE OTROS; R1 ES H O ALQUILO C1-C6; R2 ES H, F, NH2, NH(ALQUILO C1-C4), ENTRE OTROS; R3 ES H, Cl, F, OH, O(ALQUILO C1-C4), ENTRE OTROS; R4 ES (a), (b) O (c); T ES UN CARBOCICLO NO AROMATICO C3-C10 OPCIONALMENTE SUSTITUIDO CON JA O UN HETEROCICLO NO AROMATICO DE 3 A 10 MIEMBROS OPCIONALMENTE SUSTITUIDO CON JB; J ES UN HETEROCICLO NO AROMATICO DE 3 A 10 MIEMBROS OPCIONALMENTE SUSTITUIDO CON JB; D ES UN HETEROCICLO NO AROMATICO DE 4 A 10 MIEMBROS OPCIONALMENTE SUSTITUIDO CON JD1; JA Y JB SON HALOGENO, CN, NCO, ENTRE OTROS; R9 ES H, HALOGENO, CN, OH, AMINO, ALQUILO C1-C6, ENTRE OTROS; R* ES H, ALQUILO C1-C6, CARBOCICLO C3-C8 NO AROMATICO, ENTRE OTROS; JD1 ES HALOGENO, CN, OXO, ENTRE OTROS; R13 Y R14 SON H, HALOGENO, ALQUILO C1-C6, ENTRE OTROS; j Y z SON 1 O 2; t ES 0, 1 O 2. SON COMPUESTOS PREFERIDOS: ACIDO (R)-3-(3-((2-(5-CLORO-1H-PIRROLO[2,3-b]PIRIDIN-3-IL)-5-FLUOROPIRIMIDIN-4-ILAMINO)METIL)PIPERIDINA-1-CARBONIL)PIRAZINA-2-CARBOXILICO, (S)-1-(3-((2-(5-CLORO-1H-PIRROLO[2,3-b]PIRIDIN-3-IL)-5-FLUOROPIRIMIDIN-4-ILAMINO)METIL)PIPERIDIN-1-IL)-2-METOXIETANONA, (S)-1-(3-((2-(5-CLORO-1H-PIRROLO[2,3-b]PIRIDIN-3-IL)-5-FLUOROPIRIMIDIN-4-ILAMINO)METIL)PIPERIDIN-1-IL)PROPAN-1-ONA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS INHIBEN LA REPLICACION DEL VIRUS DE LA INFLUENZA
PE2011002120A 2009-06-17 2010-06-17 Inhibidores de la replicacion de los virus de la gripe PE20120508A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US18771309P 2009-06-17 2009-06-17
US28778109P 2009-12-18 2009-12-18

Publications (1)

Publication Number Publication Date
PE20120508A1 true PE20120508A1 (es) 2012-05-09

Family

ID=42537408

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2011002120A PE20120508A1 (es) 2009-06-17 2010-06-17 Inhibidores de la replicacion de los virus de la gripe
PE2015002683A PE20160127A1 (es) 2009-06-17 2010-06-17 COMPUESTO ACIDO (2S,3S)-3-((2-(5-FLUORO-1H-PIRROLO[2,3-B]PIRIDIN-3-IL)-5-FLUOROPIRIMIDIN-4-IL)AMINO)BICICLO[2.2.2]OCTANO-2-CARBOXILICO COMO INHIBIDOR DE LA REPLICACION DEL VIRUS DE LA GRIPE A H1N1, H2N2, H3N2 o H5N1

Family Applications After (1)

Application Number Title Priority Date Filing Date
PE2015002683A PE20160127A1 (es) 2009-06-17 2010-06-17 COMPUESTO ACIDO (2S,3S)-3-((2-(5-FLUORO-1H-PIRROLO[2,3-B]PIRIDIN-3-IL)-5-FLUOROPIRIMIDIN-4-IL)AMINO)BICICLO[2.2.2]OCTANO-2-CARBOXILICO COMO INHIBIDOR DE LA REPLICACION DEL VIRUS DE LA GRIPE A H1N1, H2N2, H3N2 o H5N1

Country Status (37)

Country Link
US (7) US20120171245A1 (es)
EP (3) EP3141252B8 (es)
JP (6) JP5721706B2 (es)
KR (3) KR102050712B1 (es)
CN (5) CN104940202B (es)
AP (1) AP3631A (es)
AR (1) AR077130A1 (es)
AU (1) AU2010262905B2 (es)
BR (1) BRPI1011993A2 (es)
CA (1) CA2764177C (es)
CL (1) CL2011003192A1 (es)
CO (1) CO6491048A2 (es)
CY (2) CY1118246T1 (es)
DK (2) DK3141252T3 (es)
EA (3) EA025276B1 (es)
EC (1) ECSP12011610A (es)
ES (2) ES2692396T3 (es)
GE (3) GEP20207129B (es)
HR (2) HRP20161577T1 (es)
HU (1) HUE031048T2 (es)
IL (2) IL216980B (es)
LT (2) LT3141252T (es)
ME (1) ME02558B (es)
MX (3) MX348066B (es)
NZ (2) NZ597059A (es)
PE (2) PE20120508A1 (es)
PH (1) PH12015501678B1 (es)
PL (2) PL3141252T3 (es)
PT (2) PT2442809T (es)
RS (2) RS55341B1 (es)
SG (3) SG10201405827PA (es)
SI (2) SI2442809T1 (es)
TR (1) TR201815272T4 (es)
TW (4) TWI666209B (es)
UY (1) UY32717A (es)
WO (1) WO2010148197A1 (es)
ZA (2) ZA201109127B (es)

Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2006251623A1 (en) * 2005-05-20 2006-11-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
JP5721706B2 (ja) 2009-06-17 2015-05-20 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated インフルエンザウイルス複製の阻害剤
WO2012083117A1 (en) * 2010-12-16 2012-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
RU2013132717A (ru) * 2010-12-16 2015-01-27 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы репликации вирусов гриппа
CN103562205A (zh) * 2010-12-16 2014-02-05 沃泰克斯药物股份有限公司 流感病毒复制的抑制剂
CA2839116C (en) 2011-07-04 2019-07-16 Rottapharm S.P.A. Cyclic amine derivatives as ep4 receptor antagonists
KR20140058547A (ko) * 2011-07-05 2014-05-14 버텍스 파마슈티칼스 인코포레이티드 아자인돌을 제조하기 위한 방법 및 중간체
UA118010C2 (uk) * 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
US10323012B2 (en) * 2012-06-05 2019-06-18 Hong Kong Baptist University Miliusanes as antiviral agents
WO2013184985A1 (en) * 2012-06-08 2013-12-12 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
HK1215032A1 (zh) * 2012-11-21 2016-08-12 Ptc Therapeutics, Inc. 取代的反向嘧啶bmi-1抑制劑
AU2013399092A1 (en) 2013-08-30 2016-03-17 Ptc Therapeutics, Inc. Substituted pyrimidine Bmi-1 inhibitors
US9296727B2 (en) 2013-10-07 2016-03-29 Vertex Pharmaceuticals Incorporated Methods of regioselective synthesis of 2,4-disubstituted pyrimidines
KR20160084465A (ko) * 2013-11-13 2016-07-13 버텍스 파마슈티칼스 인코포레이티드 아자인돌 화합물의 제형
CN110156779A (zh) 2013-11-13 2019-08-23 沃泰克斯药物股份有限公司 流感病毒复制抑制剂
KR102338461B1 (ko) 2013-11-13 2021-12-13 버텍스 파마슈티칼스 인코포레이티드 인플루엔자 바이러스 복제 억제제의 제조 방법
WO2015076800A1 (en) 2013-11-21 2015-05-28 Ptc Therapeutics, Inc. Substituted pyridine and pyrazine bmi-1 inhibitors
JP6594949B2 (ja) 2014-04-04 2019-10-23 サイロス ファーマシューティカルズ, インコーポレイテッド サイクリン依存性キナーゼ7(cdk7)の阻害剤
MX381488B (es) * 2014-08-08 2025-03-12 Janssen Sciences Ireland Uc Indoles para su uso en la infección por el virus de la gripe.
US9932346B2 (en) * 2014-09-08 2018-04-03 Janssen Sciences Ireland Uc Pyrrolopyrimidines for use in influenza virus infection
MA40773A (fr) 2014-10-02 2017-08-08 Vertex Pharma Variants du virus influenza a
MA40772A (fr) 2014-10-02 2017-08-08 Vertex Pharma Variants du virus de la grippe a
EP3245190B1 (en) * 2015-01-16 2018-12-26 Bayer CropScience Aktiengesellschaft Method for preparing 4-cyanopiperidine hydrochloride
WO2016183116A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
EP3294735B8 (en) 2015-05-13 2022-01-05 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
US20180134730A1 (en) * 2015-05-26 2018-05-17 BoroPharm Inc. Improved process for preparing boryl 7-azaindole compounds
KR20180087290A (ko) * 2015-11-27 2018-08-01 얀센 사이언시즈 아일랜드 유씨 인플루엔자 바이러스 감염에서 사용하기 위한 복소환식 인돌
US10717732B2 (en) * 2015-12-09 2020-07-21 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication, application methods and uses thereof
MA43583A (fr) * 2016-01-07 2021-05-19 Janssen Sciences Ireland Unlimited Co Dérivés d'acide pentanoïque substitués par pyrrolo-[2,3-b]pyrimidne-pyridines pour traiter des infections par le virus de la grippe
CN108473477B (zh) * 2016-01-20 2021-10-22 爱尔兰詹森科学公司 用于在流感病毒感染中使用的芳基取代的嘧啶
WO2017133667A1 (en) * 2016-02-05 2017-08-10 Savira Pharmaceuticals Gmbh Pyrimidine and pyridine derivatives and use in treatment, amelioration or prevention of influenza thereof
CN109071567B (zh) * 2016-05-19 2021-03-23 四川大学 抗流感小分子化合物及其制备方法和用途
CN107759571B (zh) * 2016-08-16 2021-03-02 广东东阳光药业有限公司 流感病毒复制抑制剂及其使用方法和用途
CN109641868B (zh) 2016-08-30 2021-12-03 广东东阳光药业有限公司 流感病毒复制抑制剂及其使用方法和用途
WO2018041263A1 (zh) * 2016-09-05 2018-03-08 广东众生药业股份有限公司 抗流感病毒嘧啶衍生物
JP7071383B2 (ja) * 2016-11-08 2022-05-18 キャンサー・リサーチ・テクノロジー・リミテッド cdc7阻害剤としてのピリミジノン誘導体
EP3555095B1 (en) 2016-12-15 2023-04-12 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication and uses thereof
JP7299837B2 (ja) 2016-12-23 2023-06-28 アクイナ ファーマシューティカルズ, インコーポレイテッド 化合物、組成物、および使用方法
US11098042B2 (en) 2017-01-05 2021-08-24 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication and uses thereof
CN110446711B (zh) 2017-03-02 2022-02-15 广东东阳光药业有限公司 流感病毒复制抑制剂及其用途
WO2018191475A1 (en) 2017-04-12 2018-10-18 Vertex Pharmaceuticals Incorporated Combination therapies for treating influenza virus infection
PL3615545T3 (pl) * 2017-04-24 2022-01-10 Cocrystal Pharma, Inc. Pochodne pirolopirymidyny użyteczne jako inhibitory replikacji wirusa grypy
CN108727369B (zh) * 2017-04-25 2023-06-09 广东东阳光药业有限公司 流感病毒复制抑制剂及其用途
US11236100B2 (en) 2017-08-09 2022-02-01 Denali Therapeutics Inc. Modulators of eukaryotic initiation factor 2B, compositions and methods
EP4248965A3 (en) 2017-09-01 2023-11-22 Denali Therapeutics Inc. Compounds, compositions and methods
CN109745309B (zh) * 2017-11-03 2022-01-28 香港浸会大学 作为抗病毒剂的密瘤杀
CN110117285B (zh) * 2018-02-07 2023-02-03 广东东阳光药业有限公司 流感病毒复制抑制剂及其用途
US11535613B2 (en) 2018-03-05 2022-12-27 Guangdong Raynovent Biotech Co., Ltd. Crystal form and salt form of pyridoimidazole compound and preparation method therefor
EP3774794A1 (en) 2018-04-06 2021-02-17 Janssen Pharmaceuticals, Inc. Isothermal reactive crystallisation process for the preparation of a crystalline form of pimodivir hydrochloride hemihydrate
CN110590768B (zh) * 2018-06-13 2021-02-26 银杏树药业(苏州)有限公司 杂环化合物、其组合物及其作为抗流感病毒药物的应用
WO2020023813A1 (en) * 2018-07-27 2020-01-30 Cocrystal Pharma, Inc. Pyrrolo[2,3-b]pyridin derivatives as inhibitors of influenza virus replication
AU2019340402B2 (en) 2018-08-17 2025-04-03 Ptc Therapeutics, Inc. Method for treating pancreatic cancer
EP3924341A4 (en) 2019-02-13 2022-11-02 Denali Therapeutics Inc. Compounds, compositions and methods
MX2021009669A (es) 2019-02-13 2021-10-13 Denali Therapeutics Inc Compuestos, composiciones y métodos.
US20220177456A1 (en) * 2019-03-06 2022-06-09 Denali Therapeutics Inc. Compounds, compositions and methods
WO2020212399A1 (en) 2019-04-15 2020-10-22 Janssen Pharmaceutica Nv Method for preparing an alkyl trans-3-aminobicyclo[2.2.2]octane-2-carboxylic acid ester compound
US20200397784A1 (en) 2019-06-20 2020-12-24 Janssen Pharmaceuticals, Inc. Formulations of azaindole compounds
EP3992192A4 (en) * 2019-07-22 2022-08-17 Guangdong Raynovent Biotech Co., Ltd. DOMINANT SALT FORMS OF PYRIMIDINE DERIVATIVES AND CRYSTAL FORMS THEREOF
CA3148490C (en) * 2019-08-30 2024-04-30 Jae Won Lee Imidazopyridine derivative and pharmaceutical composition comprising same as active ingredient
WO2021047437A1 (zh) * 2019-09-10 2021-03-18 广东众生睿创生物科技有限公司 一种用于治疗病毒性感冒的药物组合物及其制剂
RU2726119C1 (ru) * 2019-11-22 2020-07-09 Общество С Ограниченной Ответственностью "Валента - Интеллект" Новые производные полиолов, их применение, фармацевтическая композиция на их основе
CN115698011B (zh) 2020-07-10 2023-10-20 四川海思科制药有限公司 Pb2抑制剂及其制备方法和用途
CN112979647B (zh) * 2021-03-12 2022-05-20 浙江大学 含氮杂氨基酸的氮杂吲哚衍生物及制备和应用

Family Cites Families (174)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4349552A (en) 1978-10-30 1982-09-14 Fujisawa Pharmaceutical Company, Ltd. 5-Fluorouracil derivatives, and their pharmaceutical compositions
NZ221717A (en) 1986-09-10 1990-08-28 Sandoz Ltd Azaindole and indolizine derivatives and pharmaceutical compositions
MX19185A (es) 1989-01-20 1993-12-01 Pfizer Procedimiento para preparar 3-(1,2,5,6-tretrahidropiridil)-pirrolopiridinas.
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
FR2687402B1 (fr) 1992-02-14 1995-06-30 Lipha Nouveaux azaindoles, procedes de preparation et medicaments les contenant.
DE4304455A1 (de) 1993-02-15 1994-08-18 Bayer Ag Heterocyclisch substituierte Phenyl-cyclohexan-carbonsäurederivate
US5716981A (en) 1993-07-19 1998-02-10 Angiogenesis Technologies, Inc. Anti-angiogenic compositions and methods of use
IL129871A (en) 1994-05-06 2003-11-23 Pharmacia & Upjohn Inc Process for preparing 4-phenyl-substituted octanoyl-oxazolidin-2-one intermediates that are useful for preparing pyran-2-ones useful for treating retroviral infections
WO1995033748A1 (en) 1994-06-09 1995-12-14 Smithkline Beecham Corporation Endothelin receptor antagonists
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
US5821243A (en) 1996-07-22 1998-10-13 Viropharma Incorporated Compounds compositions and methods for treating influenza
US6187713B1 (en) 1996-10-31 2001-02-13 Corning Incorporated Method of making activated carbon bodies having improved adsorption properties
GB9721437D0 (en) 1997-10-10 1997-12-10 Glaxo Group Ltd Heteroaromatic compounds and their use in medicine
WO2000040581A1 (en) 1999-01-07 2000-07-13 American Home Products Corporation 3,4-dihydro-2h-benzo[1,4]oxazine derivatives
US6313126B1 (en) 1999-01-07 2001-11-06 American Home Products Corp Arylpiperazinyl-cyclohexyl indole derivatives for the treatment of depression
CN1166636C (zh) 1999-01-07 2004-09-15 惠氏 用于治疗抑郁症的芳基哌嗪基-环己基吲哚衍生物
US6265403B1 (en) 1999-01-20 2001-07-24 Merck & Co., Inc. Angiogenesis inhibitors
AR028475A1 (es) 1999-04-22 2003-05-14 Wyeth Corp Derivados de azaindol y uso de los mismos para la manufactura de un medicamento para el tratamiento de la depresion.
US20030153560A1 (en) 1999-04-23 2003-08-14 Salituro Francesco G. Inhibitors of c-Jun N-terminal kinases (JNK)
WO2001001986A1 (en) 1999-07-02 2001-01-11 Lipton Stuart A Method of reducing neuronal injury or apoptosis
GB9919843D0 (en) 1999-08-20 1999-10-27 Smithkline Beecham Plc Novel compounds
DE19948417A1 (de) 1999-10-07 2001-04-19 Morphochem Ag Imidazol-Derivate und ihre Verwendung als Arzneimittel
CA2394727A1 (en) 1999-12-28 2001-07-05 Pharmacopeia, Inc. Pyrimidine and triazine kinase inhibitors
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
CN1429222A (zh) 2000-02-17 2003-07-09 安姆根有限公司 激酶抑制剂
US7041277B2 (en) 2000-03-10 2006-05-09 Cadbury Adams Usa Llc Chewing gum and confectionery compositions with encapsulated stain removing agent compositions, and methods of making and using the same
CA2308994A1 (en) 2000-05-19 2001-11-19 Aegera Therapeutics Inc. Neuroprotective compounds
MXPA03001420A (es) 2000-08-14 2004-01-26 Johnson & Johnson Pirazoles sustituidos.
MXPA03001962A (es) 2000-09-06 2004-03-26 Johnson & Johnson Metodo para tratar alergias utilizando pirazoles sustituidos.
WO2002020002A2 (en) 2000-09-06 2002-03-14 Ortho Mcneil Pharmaceutical, Inc. A method for treating allergies
AR031130A1 (es) 2000-09-20 2003-09-10 Abbott Lab N-acilsulfonamidas promotoras de la apoptosis
WO2002024705A1 (en) 2000-09-22 2002-03-28 Eli Lilly And Company Stereoselective process for preparing cyclohexyl amine derivatives
BR0116323A (pt) 2000-12-22 2003-10-14 Wyeth Corp Compostos de heterociclilindazol e -azaindazol como ligandos de 5-hidroxitriptamina-6
EP1975620A3 (en) 2001-03-02 2008-12-24 GPC Biotech AG Three hybrid assay system
PT1392697E (pt) 2001-03-14 2005-01-31 Wyeth Corp Antidepressivos derivados aza-heterociclilmetilo de 2,3- di-hidro-1,4-dioxino[2,3-f]quinolina
US7081454B2 (en) 2001-03-28 2006-07-25 Bristol-Myers Squibb Co. Tyrosine kinase inhibitors
US6559169B2 (en) 2001-04-24 2003-05-06 Wyeth Antidepressant azaheterocyclymethyl derivatives of 2,3-dihydro-1,4-benzodioxan
US6656950B2 (en) 2001-04-25 2003-12-02 Wyeth Antidepressant azaheterocyclylmethyl derivatives of 1,4-dioxino[2,3-b]pyridine
CN1250553C (zh) 2001-04-26 2006-04-12 惠氏公司 抗抑郁的2,3-二氢-1,4-二噁英并[2,3-f]喹喔啉的氮杂环基甲基衍生物
WO2002088129A1 (en) 2001-04-26 2002-11-07 Wyeth Antidepressant azaheterocyclylmethyl derivatives of 2,3-dihydro-1,4-dioxino[2,3-f]quinazoline
US6593350B2 (en) 2001-04-26 2003-07-15 Wyeth Antidepressant indoletetrahydropyridine derivatives of 2,3-dihydro-7H-[1,4]dioxino[2,3-e]indole
CN1267434C (zh) 2001-04-26 2006-08-02 惠氏公司 抗抑郁的(SSSRI)7,8-二氢-3H-6,9-二氧杂-1,3-二氮杂环戊二烯并[a]萘的氮杂环基甲基衍生物
DE60201590T2 (de) 2001-04-26 2005-02-17 Wyeth Antidepressiv wirksame azaheterocyclymethyl-derivative von oxaheterocycyl-anellierten (1,4)-benzodioxanen
EP1392700B1 (en) 2001-04-30 2004-09-29 Wyeth Antidepressant azaheterocyclylmethyl derivatives of 7,8-dihydro-1,6,9-trioxa-3-aza-cyclopenta(a)naphthalene
US6555560B2 (en) 2001-04-30 2003-04-29 Wyeth Antidepressant azaheterocyclylmethyl derivatives of 1,4,5-trioxa-phenanthrene
GB0111186D0 (en) 2001-05-08 2001-06-27 Smithkline Beecham Plc Novel compounds
EP1387845A2 (en) 2001-05-17 2004-02-11 Wyeth PROCESSES FOR THE SYNTHESIS OF DERIVATIVES OF 2,3-DIHYDRO-1,4-DIOXINO-(2,3-f) QUINOLINE
JP4541695B2 (ja) 2001-06-15 2010-09-08 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼインヒビターとしての5−(2−アミノピリミジン−4−イル)ベンズイソキサゾール
GB0115109D0 (en) * 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
AR035083A1 (es) 2001-07-25 2004-04-14 Wyeth Corp Derivados azaheterociclilmetilicos de 7,8-dihidro-6h-5-oxa-1-aza-fenantreno, composiciones farmaceuticas, el uso de dichos derivados para la preparacion de un medicamento antidepresivo e intermediarios
US20040235761A1 (en) 2001-08-14 2004-11-25 Yousuke Furuta Novel virus proliferaton inhibition/virucidal method and novel pyradine nucleotide/pyradine nucleoside analogue
US20040236110A1 (en) 2001-09-26 2004-11-25 Ladouceur Gaetan H Substituted 3-pyridyl indoles and indazoles as c17,20 lyase inhibitors
WO2003031439A1 (en) 2001-10-05 2003-04-17 Wyeth Antidepressant chroman and chromene derivatives of 3-(1,2,3,6-tetrahydro-4-pyridinyl)-1h-indole
US7361671B2 (en) 2001-11-15 2008-04-22 The Institute For Pharmaceutical Discovery, Inc. Substituted heteroarylalkanoic acids
TW200306819A (en) 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
AU2003237121A1 (en) 2002-04-26 2003-11-10 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
BR0308787A (pt) 2002-04-26 2005-01-11 Pfizer Prod Inc Inibidores de metaloproteinase de n-substituìdos-heteroarilóxi-aril-espiro-pirimidina- 2,4,6-triona
TW200406385A (en) 2002-05-31 2004-05-01 Eisai Co Ltd Pyrazole compound and pharmaceutical composition containing the same
UA78999C2 (en) 2002-06-04 2007-05-10 Wyeth Corp 1-(aminoalkyl)-3-sulfonylazaindoles as ligands of 5-hydroxytryptamine-6
KR20050032105A (ko) 2002-08-02 2005-04-06 버텍스 파마슈티칼스 인코포레이티드 Gsk-3의 억제제로서 유용한 피라졸 조성물
WO2004014912A1 (en) 2002-08-08 2004-02-19 Ribapharm Inc. Improved synthesis for hydroxyalkylated heterocyclic bases
SE0202463D0 (sv) 2002-08-14 2002-08-14 Astrazeneca Ab Novel compounds
WO2004037814A1 (en) 2002-10-25 2004-05-06 Vertex Pharmaceuticals Incorporated Indazolinone compositions useful as kinase inhibitors
NZ542498A (en) 2003-02-26 2009-01-31 Boehringer Ingelheim Pharma Dihydropteridinones, method for the production and use thereof in the form of drugs
EP1599475A2 (en) 2003-03-06 2005-11-30 Eisai Co., Ltd. Jnk inhibitors
CA2518318A1 (en) 2003-03-17 2004-09-30 Takeda San Diego, Inc. Histone deacetylase inhibitors
GB0308466D0 (en) 2003-04-11 2003-05-21 Novartis Ag Organic compounds
WO2005000813A1 (en) 2003-05-30 2005-01-06 Imclone Systems Incorporated Heteroarylamino-phenylketone derivatives and their use as kinase inhibitors
WO2004106298A1 (en) 2003-05-30 2004-12-09 Janssen Pharmaceutica N.V. Indole derivatives with an improved antipsychotic activity
CN100549014C (zh) 2003-07-16 2009-10-14 詹森药业有限公司 作为糖原合酶激酶3抑制剂的三唑并嘧啶衍生物
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
WO2005044181A2 (en) 2003-09-09 2005-05-19 Temple University-Of The Commonwealth System Of Higher Education Protection of tissues and cells from cytotoxic effects of ionizing radiation by abl inhibitors
EP1675830A4 (en) 2003-09-30 2008-08-20 Scios Inc HETEROCYCLIC AMIDES AND SULFONAMIDES
CN1897950A (zh) 2003-10-14 2007-01-17 惠氏公司 稠合芳基和杂芳基衍生物及其使用方法
ES2527118T3 (es) 2003-12-19 2015-01-20 Plexxikon Inc. Compuestos y procedimientos de desarrollo de moduladores de Ret
US20070066641A1 (en) 2003-12-19 2007-03-22 Prabha Ibrahim Compounds and methods for development of RET modulators
GB0405055D0 (en) 2004-03-05 2004-04-07 Eisai London Res Lab Ltd JNK inhibitors
PL2332940T3 (pl) 2004-03-30 2013-03-29 Vertex Pharma Azaindole użyteczne jako inhibitory JAK i innych kinaz białkowych
EP1756108A2 (en) 2004-04-02 2007-02-28 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of rock and other protein kinases
ITMI20040874A1 (it) 2004-04-30 2004-07-30 Ist Naz Stud Cura Dei Tumori Derivati indolici ed azaindolici con azione antitumorale
KR100476851B1 (ko) 2004-05-18 2005-03-17 (주)성신엔지니어링 중력식 섬유여과기
TW200616632A (en) 2004-06-17 2006-06-01 Plexxikon Inc Compounds modulating c-kit activity and uses therefor
DE102004029784A1 (de) 2004-06-21 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 2-Benzylaminodihydropteridinone, Verfahren zur deren Herstellung und deren Verwendung als Arzneimittel
US7173031B2 (en) 2004-06-28 2007-02-06 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
US20060122213A1 (en) 2004-06-30 2006-06-08 Francoise Pierard Azaindoles useful as inhibitors of protein kinases
EP1781654A1 (en) 2004-07-27 2007-05-09 SGX Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
CN101068815B (zh) 2004-10-04 2012-09-05 千禧药品公司 有效作为蛋白激酶抑制剂的内酰胺化合物
WO2006038001A1 (en) 2004-10-06 2006-04-13 Celltech R & D Limited Aminopyrimidine derivatives as jnk inhibitors
US7855205B2 (en) 2004-10-29 2010-12-21 Janssen Pharmaceutica Nv Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
US7528138B2 (en) 2004-11-04 2009-05-05 Vertex Pharmaceuticals Incorporated Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases
CN101098872B (zh) 2004-11-22 2012-09-05 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的吡咯并吡嗪和吡唑并吡嗪
PT2522365T (pt) 2004-11-24 2017-02-08 Meda Pharmaceuticals Inc Composições que compreendem azelastina e seus métodos de utilização
US20090233955A1 (en) 2004-12-08 2009-09-17 Frazee James S 1H-Pyrrolo[2,3-B]Pyridnes
RU2423351C2 (ru) 2004-12-16 2011-07-10 Вертекс Фармасьютикалз Инкорпорейтед Пирид-2-оны, применимые как ингибиторы протеинкиназ семейства тес для лечения воспалительных, пролиферативных и иммунологически-опосредованных заболеваний
US20060161001A1 (en) 2004-12-20 2006-07-20 Amgen Inc. Substituted heterocyclic compounds and methods of use
US8633205B2 (en) 2005-02-03 2014-01-21 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-d]pyrimidines as inhibitors of protein kinases
US20080300267A1 (en) 2005-05-16 2008-12-04 Barun Okram Compounds and Compositions as Protein Kinase Inhibitors
AU2006251623A1 (en) 2005-05-20 2006-11-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
MY153898A (en) 2005-06-22 2015-04-15 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
EP1749523A1 (en) 2005-07-29 2007-02-07 Neuropharma, S.A. GSK-3 inhibitors
GB0516156D0 (en) 2005-08-05 2005-09-14 Eisai London Res Lab Ltd JNK inhibitors
US8580802B2 (en) 2005-09-30 2013-11-12 Vertex Pharmaceuticals Incorporated Pyrrolo[2,3-D]pyrimidines as inhibitors of Janus kinases
US20130096302A1 (en) 2005-11-22 2013-04-18 Hayley Binch Pyrrolopyrazines and pyrazolopyrazines useful as inhibitors of protein kinases
EP2559694A3 (en) 2006-01-17 2013-04-03 Vertex Pharmaceuticals, Inc. Azaindoles useful as inhibitors of Janus kinases
CN101374839A (zh) * 2006-01-17 2009-02-25 沃泰克斯药物股份有限公司 适用作詹纳斯激酶抑制剂的吖吲哚类
RU2475488C2 (ru) 2006-02-14 2013-02-20 Вертекс Фармасьютикалз Инкорпорейтед Дигидродиазепины, которые можно использовать в качестве ингибиторов протеинкиназ
WO2007095223A2 (en) 2006-02-14 2007-08-23 Vertex Pharmaceuticals Incorporated Pyrrolo(3,2-c) pyridines useful as inhibitors of protein kinases
DE102006012617A1 (de) 2006-03-20 2007-09-27 Merck Patent Gmbh 4-(Pyrrolopyridinyl)-pyrimidinyl-2-amin-derivate
MX2008012860A (es) 2006-04-05 2009-01-07 Vertex Pharma Desazapurinas de utilidad como inhibidores de janus cinasas.
BRPI0710866A2 (pt) * 2006-04-26 2012-08-14 Hoffmann La Roche compostos farmacÊuticos
WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
US20090017444A1 (en) 2006-06-09 2009-01-15 Wisconsin Alumni Research Foundation Screening method for modulators of viral transcription or replication
JP5642963B2 (ja) 2006-06-30 2014-12-17 スネシス ファーマシューティカルズ,インコーポレイティド ピリジノニルpdk1阻害剤
TW200808325A (en) 2006-07-06 2008-02-16 Astrazeneca Ab Novel compounds
EP2050749B1 (en) 2006-08-08 2017-11-22 Chugai Seiyaku Kabushiki Kaisha Pyrimidine derivative as pi3k inhibitor and use thereof
CA2660758A1 (en) * 2006-08-24 2008-02-27 Astrazeneca Ab Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders
AU2007334379B2 (en) 2006-12-14 2013-04-18 Vertex Pharmaceuticals Incorporated Compounds useful as protein kinase inhibitors
KR20090091350A (ko) 2006-12-21 2009-08-27 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제 억제제로 유용한 5-시아노-4-피롤로[2,3b]피리딘-3-일)-피리디민 유도체
TW200840581A (en) 2007-02-28 2008-10-16 Astrazeneca Ab Novel pyrimidine derivatives
AU2008226461A1 (en) 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyridines useful as inhibitors of protein kinases
CA2679884A1 (en) 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
RU2009137390A (ru) 2007-03-09 2011-04-20 Вертекс Фармасьютикалз Инкорпорейтед (Us) Аминопиримидины, пригодные в качестве ингибиторов протеинкиназ
PL2139892T3 (pl) 2007-03-22 2012-03-30 Takeda Pharmaceuticals Co Podstawione pirymidynodiazepiny użyteczne jako inhibitory plk1
AU2008236872B2 (en) 2007-04-05 2013-01-17 Alla Chem, Llc Substituted 2,3,4,5-tetrahydro-1h-pyrido[4,3-b]indoles, methods for the production and use thereof
RU2339637C1 (ru) 2007-04-05 2008-11-27 Андрей Александрович Иващенко Блокаторы гистаминного рецептора для фармацевтических композиций, обладающих противоаллергическим и аутоиммунным действием
AU2008287339A1 (en) 2007-08-15 2009-02-19 Vertex Pharmaceuticals Incorporated 4-(9-(3, 3-difluorocyclopentyl) -5, 7, 7-trimethyl-6-oxo-6, 7, 8, 9-tetrahydro-5H-pyrimido [4, 5-b][1, 4] diazepin-2-ylamino)-3-methoxybenzamide Derivatives as Inhibitors of the Human Protein Kinases PLK1 to PLK4 for the Treatment of Proliferative Diseases
CN101878216B (zh) 2007-09-28 2013-07-10 西克拉塞尔有限公司 作为蛋白激酶抑制剂的嘧啶衍生物
KR101672554B1 (ko) 2007-10-09 2016-11-03 유럽피안 몰레큘러 바이올로지 래보러토리 Rna 캡에 결합 가능한 인플루엔자 바이러스 pb2 단백질의 가용성 단편
MX2010004819A (es) 2007-11-02 2010-07-05 Vertex Pharma Derivados de [1h-pirazolo[3,4-b]piridin-4-il]-fenilo o piridin-2-ilo como proteina cinasa c-theta.
ATE550333T1 (de) 2007-11-05 2012-04-15 Novartis Ag 4-benzylamino-1-carboxyacyl-piperidinderivate als cetp-hemmer zur behandlung von krankheiten wie hyperlipidämie oder arteriosklerose
CA2713710A1 (en) 2008-02-25 2009-09-03 F. Hoffmann-La Roche Ag Pyrrolopyrazine kinase inhibitors
EP2262498A2 (en) 2008-03-10 2010-12-22 Vertex Pharmceuticals Incorporated Pyrimidines and pyridines useful as inhibitors of protein kinases
WO2009125395A1 (en) 2008-04-09 2009-10-15 Technion Research & Development Foundation Ltd. Anti influenza antibodies and uses thereof
CN102076690A (zh) 2008-06-23 2011-05-25 维泰克斯制药公司 蛋白激酶抑制剂
JP5634990B2 (ja) 2008-06-23 2014-12-03 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated タンパク質キナーゼ阻害剤
JP5542287B2 (ja) 2008-07-23 2014-07-09 バーテックス ファーマシューティカルズ インコーポレイテッド ピラゾロピリジンキナーゼ阻害剤
AU2009274023A1 (en) 2008-07-23 2010-01-28 Vertex Pharmaceuticals Incorporated Tri-cyclic pyrazolopyridine kinase inhibitors
US8569337B2 (en) 2008-07-23 2013-10-29 Vertex Pharmaceuticals Incorporated Tri-cyclic pyrazolopyridine kinase inhibitors
WO2010011756A1 (en) 2008-07-23 2010-01-28 Vertex Pharmaceuticals Incorporated Pyrazolopyridine kinase inhibitors
WO2010129668A1 (en) 2009-05-06 2010-11-11 Vertex Pharmaceuticals Incorporated Pyrazolopyridines
WO2010143207A1 (en) 2009-06-11 2010-12-16 Rubicon Research Private Limited Taste-masked oral formulations of influenza antivirals
JP5721706B2 (ja) 2009-06-17 2015-05-20 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated インフルエンザウイルス複製の阻害剤
WO2011000566A2 (en) 2009-06-30 2011-01-06 Savira Pharmaceuticals Gmbh Compounds and pharmaceutical compositions for the treatment of negative-sense ssrna virus infections
US8435980B2 (en) 2009-07-15 2013-05-07 Abbvie Inc. Pyrrolopyridine inhibitors of kinases
US8563530B2 (en) 2010-03-31 2013-10-22 Gilead Pharmassel LLC Purine nucleoside phosphoramidate
JP2013523836A (ja) 2010-04-07 2013-06-17 バーテックス ファーマシューティカルズ インコーポレイテッド 3−(6−(1−(2,2−ジフルオロベンゾ[d][1,3]ジオキソール−5−イル)シクロプロパンカルボキサミド)−3−メチルピリジン−2−イル)安息香酸の固体形態
JP2013523884A (ja) 2010-04-14 2013-06-17 アレイ バイオファーマ、インコーポレイテッド JAKキナーゼの阻害剤としての5,7置換イミダゾ[1,2−c]ピリミジン
US20130040933A1 (en) 2010-04-27 2013-02-14 Brandon Cash Azaindoles as janus kinase inhibitors
RU2013132717A (ru) 2010-12-16 2015-01-27 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы репликации вирусов гриппа
WO2012083117A1 (en) 2010-12-16 2012-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
CN103562205A (zh) 2010-12-16 2014-02-05 沃泰克斯药物股份有限公司 流感病毒复制的抑制剂
KR20140058547A (ko) 2011-07-05 2014-05-14 버텍스 파마슈티칼스 인코포레이티드 아자인돌을 제조하기 위한 방법 및 중간체
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
MX2014005565A (es) 2011-11-07 2014-05-30 Vertex Pharma Metodos para tratar enfermedades inflamatorias y composiciones farmaceuticas utiles para los mismos.
WO2013184985A1 (en) 2012-06-08 2013-12-12 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
WO2014201332A1 (en) 2013-06-14 2014-12-18 Vertex Pharmaceuticals Incorporated Pharmaceutical combinations useful for treating rheumatoid arthritis
RU2016110094A (ru) 2013-08-22 2017-09-27 Вертекс Фармасьютикалз Инкорпорейтед Изотопно-обогащенные азаиндолы
EP3030566B1 (en) 2013-09-12 2020-07-08 Janssen BioPharma, Inc. 7,8-dihydro-3h-pyrazino[1,2-b]pyridazine-3,5(6h)-dione compounds and uses thereof
US9296727B2 (en) 2013-10-07 2016-03-29 Vertex Pharmaceuticals Incorporated Methods of regioselective synthesis of 2,4-disubstituted pyrimidines
KR102338461B1 (ko) 2013-11-13 2021-12-13 버텍스 파마슈티칼스 인코포레이티드 인플루엔자 바이러스 복제 억제제의 제조 방법
CN110156779A (zh) 2013-11-13 2019-08-23 沃泰克斯药物股份有限公司 流感病毒复制抑制剂
KR20160084465A (ko) 2013-11-13 2016-07-13 버텍스 파마슈티칼스 인코포레이티드 아자인돌 화합물의 제형
MX381488B (es) 2014-08-08 2025-03-12 Janssen Sciences Ireland Uc Indoles para su uso en la infección por el virus de la gripe.
US9932346B2 (en) 2014-09-08 2018-04-03 Janssen Sciences Ireland Uc Pyrrolopyrimidines for use in influenza virus infection
MA40773A (fr) 2014-10-02 2017-08-08 Vertex Pharma Variants du virus influenza a
MA40772A (fr) 2014-10-02 2017-08-08 Vertex Pharma Variants du virus de la grippe a
WO2016183116A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
EP3294735B8 (en) 2015-05-13 2022-01-05 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
KR20180087290A (ko) 2015-11-27 2018-08-01 얀센 사이언시즈 아일랜드 유씨 인플루엔자 바이러스 감염에서 사용하기 위한 복소환식 인돌
MA43583A (fr) 2016-01-07 2021-05-19 Janssen Sciences Ireland Unlimited Co Dérivés d'acide pentanoïque substitués par pyrrolo-[2,3-b]pyrimidne-pyridines pour traiter des infections par le virus de la grippe
CN108473477B (zh) 2016-01-20 2021-10-22 爱尔兰詹森科学公司 用于在流感病毒感染中使用的芳基取代的嘧啶
WO2017223231A1 (en) 2016-06-21 2017-12-28 Alios Biopharma, Inc. (s)-8-(benzhydryl )-6-isopropyl-3,5-dioxo- 5, 6,7,8,-tetrahydro-3h-pyrazino-[1,2-b]pyridazin-yl-isobutyrate antiviral agent for use in treating influenza
WO2018191475A1 (en) 2017-04-12 2018-10-18 Vertex Pharmaceuticals Incorporated Combination therapies for treating influenza virus infection

Also Published As

Publication number Publication date
DK3141252T3 (en) 2018-11-19
SG10201405826RA (en) 2014-12-30
IL216980A0 (en) 2012-02-29
EA201500266A1 (ru) 2015-10-30
PT2442809T (pt) 2016-12-06
CN110540538A (zh) 2019-12-06
EA201500871A8 (ru) 2019-02-28
US9808459B2 (en) 2017-11-07
US20140296201A1 (en) 2014-10-02
AR077130A1 (es) 2011-08-03
EA030188B1 (ru) 2018-07-31
ZA201109127B (en) 2015-07-29
JP6030619B2 (ja) 2016-11-24
RS55341B1 (sr) 2017-03-31
CN104940202A (zh) 2015-09-30
TW201925196A (zh) 2019-07-01
RS57869B1 (sr) 2018-12-31
JP2016204390A (ja) 2016-12-08
ES2692396T3 (es) 2018-12-03
GEP20207129B (en) 2020-07-10
US8829007B2 (en) 2014-09-09
CL2011003192A1 (es) 2013-01-04
US10874673B2 (en) 2020-12-29
CN102458408A (zh) 2012-05-16
US20160152614A1 (en) 2016-06-02
ME02558B (me) 2017-02-20
HK1215530A1 (zh) 2016-09-02
PL2442809T3 (pl) 2017-02-28
EP2442809A1 (en) 2012-04-25
LT3141252T (lt) 2018-11-12
EP3141252A1 (en) 2017-03-15
US9518056B2 (en) 2016-12-13
AU2010262905A1 (en) 2012-01-12
EA201500871A1 (ru) 2016-11-30
US20190151314A1 (en) 2019-05-23
US20140142119A1 (en) 2014-05-22
US20180078553A1 (en) 2018-03-22
LT2442809T (lt) 2016-12-12
CN104940202B (zh) 2018-10-16
CY1118246T1 (el) 2017-06-28
EA037529B1 (ru) 2021-04-08
JP2020011990A (ja) 2020-01-23
TW201520211A (zh) 2015-06-01
WO2010148197A1 (en) 2010-12-23
JP2015034177A (ja) 2015-02-19
JP2015038146A (ja) 2015-02-26
HK1215675A1 (zh) 2016-09-09
CA2764177A1 (en) 2010-12-23
EP3141252B1 (en) 2018-07-25
EP3427738A1 (en) 2019-01-16
HUE031048T2 (en) 2017-06-28
ECSP12011610A (es) 2012-02-29
NZ597059A (en) 2014-01-31
CO6491048A2 (es) 2012-07-31
TWI574963B (zh) 2017-03-21
UY32717A (es) 2011-01-31
KR20120097471A (ko) 2012-09-04
PH12015501678A1 (en) 2020-06-22
US10039762B2 (en) 2018-08-07
KR20180108856A (ko) 2018-10-04
SG10201405827PA (en) 2014-11-27
JP2012530713A (ja) 2012-12-06
CN102458408B (zh) 2015-06-03
MX348066B (es) 2017-05-26
TWI483941B (zh) 2015-05-11
EA025276B1 (ru) 2016-12-30
NZ619259A (en) 2015-07-31
BRPI1011993A2 (pt) 2021-07-06
EP2442809B1 (en) 2016-08-31
AU2010262905B2 (en) 2015-04-16
US20170100400A1 (en) 2017-04-13
EA201270032A1 (ru) 2012-07-30
HK1204322A1 (en) 2015-11-13
ES2604667T3 (es) 2017-03-08
AP2012006067A0 (en) 2012-02-29
AP3631A (en) 2016-03-08
PL3141252T3 (pl) 2019-01-31
ZA201500820B (en) 2016-05-25
KR102050712B1 (ko) 2019-12-02
CN104151312A (zh) 2014-11-19
SI2442809T1 (sl) 2017-01-31
MX2011013475A (es) 2012-03-14
CN104922128A (zh) 2015-09-23
HRP20161577T1 (hr) 2017-01-27
PE20160127A1 (es) 2016-02-24
KR20170015551A (ko) 2017-02-08
EP3427738B1 (en) 2021-12-01
JP5721706B2 (ja) 2015-05-20
US9345708B2 (en) 2016-05-24
MX375432B (es) 2025-03-06
IL262734B (en) 2020-11-30
GEP20156325B (en) 2015-07-10
DK2442809T3 (en) 2016-12-19
TR201815272T4 (tr) 2018-11-21
JP6348939B2 (ja) 2018-06-27
CN104922128B (zh) 2019-12-20
HRP20181715T1 (hr) 2019-04-05
JP2018002747A (ja) 2018-01-11
IL216980B (en) 2018-11-29
KR101702609B1 (ko) 2017-02-03
HK1169326A1 (en) 2013-01-25
GEP20227397B (en) 2022-07-25
PT3141252T (pt) 2018-11-14
CY1120778T1 (el) 2019-12-11
TW201728584A (zh) 2017-08-16
TW201103935A (en) 2011-02-01
KR101903354B1 (ko) 2018-10-04
CN104151312B (zh) 2016-06-15
TWI639596B (zh) 2018-11-01
SG176722A1 (en) 2012-01-30
US20120171245A1 (en) 2012-07-05
CA2764177C (en) 2018-06-05
PH12015501678B1 (en) 2022-07-06
SI3141252T1 (sl) 2018-12-31
TWI666209B (zh) 2019-07-21
JP6620135B2 (ja) 2019-12-11
IL262734A (en) 2018-12-31
EP3141252B8 (en) 2019-03-13

Similar Documents

Publication Publication Date Title
PE20120508A1 (es) Inhibidores de la replicacion de los virus de la gripe
CL2009001152A1 (es) Compuestos derivados de n-(4-(cicloalquilo nitrogenado-1-il)-1h-pirrolo[2,3-b]piridin-3-il)amida, inhibidores de cinasa; proceso de preparacion; composicion farmaceutica; y su uso para el tratamiento de una enfermedad proliferativa.
CO6470846A2 (es) Derivados aminobut´ricos sustituidos como inhibidores de neprilisina
ECSP11011560A (es) Derivados amino-propiónicos sustituidos como inhibidores de neprilisina
HN2012001037A (es) Derivados del acido carbamoil-metil-amino-acetico sustiituido como inhibidores de nep novedosos
CO6231028A2 (es) Compuestos y composiciones como inhibidores de la proteina quinasa
HRP20090459T1 (hr) Aminofenil derivati kao novi inhibitori histonskih deacetilaza
PE20130382A1 (es) Derivados de n-(imidazopirimidin-7-il)-heteroarilamida y su uso como inhibidores de pde10a
UY33731A (es) ?derivados de ácido amino-fenil-pentanoico sustituidos como inhibidores de nep?
AR079690A1 (es) Derivados heterociclicos de pirrol[2,3-b]piridina, composiciones farmaceuticas que los contienen, procedimiento para prepararlos y uso de los mismos como agentes anticancer.
PE20110835A1 (es) Piridiloxi-indoles inhibidores del vegf-r2 y uso de los mismos para el tratamiento de enfermedades
PE20061150A1 (es) Derivados de n-(n-sulfonilaminoarilmetil)ciclopropanocarboxamida sustituidos como antagonistas del receptor vainilloide tipo 1 (vdr1)
PE20140630A1 (es) Derivados de acido 3-fenilpropionico ramificados y su uso
AR078278A1 (es) Antagonistas de la tiazol y oxazol hepcidina, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de anemias y enfermedades asociadas a deficiencias de hierro.
TW200734322A (en) Indole derivatives exhibiting PGD2 receptor antagonism
UY31463A1 (es) Inhibidores de péptido desformilasa
AR082968A1 (es) Inhibidores biciclicos de notum pectinacetilesterasa y una composicion farmaceutica en base al compuesto
NO20083708L (no) 4-Fenyl-tiazol-5-karboksylsyre og 4-fenyl-tiazol-5-karboksylmider som PLK1-inhibitorer
UA107353C2 (en) Salts of bicyclo-substituted pyrazolon azo derivatives, preparation method and use thereof
PE20091455A1 (es) Triazolopiridazinas como inhibidores de par1, su preparacion y uso como medicamentos
PE20140629A1 (es) Derivados de fenil-isoxazol y procedimiento para la preparacion de los mismos
NZ600266A (en) Compound, certain novel forms thereof, pharmaceutical compositions thereof and methods for preparation and use
CL2009001146A1 (es) Compuestos derivados de 5-(5-(2-(3,5-bis(trifluorometil)fenil)-n,2-dimetilpropanoamida)-4-(4-fluoro-2-metilfenil)piridin-2-il)pirrolidin-2-carboxamida, antagonistas de los receptores nk-1; composicion farmaceutica; y uso del compuesto para el tratamiento de la depresion; ansiedad, trastornos del sueño o emesis.
PE20140239A1 (es) Derivados de 1,4-oxazepano
AR051315A1 (es) Pirimidinas 5-sustituidas inhibidoras del vih

Legal Events

Date Code Title Description
FG Grant, registration