AR070468A1 - Pirrolopirazinas inhibidores de quinasa - Google Patents

Pirrolopirazinas inhibidores de quinasa

Info

Publication number
AR070468A1
AR070468A1 ARP090100621A ARP090100621A AR070468A1 AR 070468 A1 AR070468 A1 AR 070468A1 AR P090100621 A ARP090100621 A AR P090100621A AR P090100621 A ARP090100621 A AR P090100621A AR 070468 A1 AR070468 A1 AR 070468A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
heterocycloalkyl
phenyl
heteroaryl
cycloalkyl
Prior art date
Application number
ARP090100621A
Other languages
English (en)
Inventor
Joe Timothy Bamberg
Mark Bartlett
Remy Lemoine
Timothy D Owens
Bois Daisy Joe Du
Yan Lou
David Bernard Smith
Rama K Kondru
Robert Than Hendricks
Michael Soth
Todd Richard Elworthy
Johannes Cornelius Hermann
Jaehyeon Park
Calvin Wesley Yee
Hanbiao Yang
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR070468A1 publication Critical patent/AR070468A1/es

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Inhiben la JAK y la SYK y son utiles para el tratamiento de enfermedades autoinmunes e inflamatorias. Reivindicacion 1: Un compuesto de la formula (1) en la que: R es R1, R2, R3 o R4; R1 es alquilo inferior, alcoxi inferior, fenilo, bencilo, heteroarilo, cicloalquilo, heterocicloalquilo o cicloalquilalquilo, opcionalmente sustituido por uno o más R1a; R1a es R1b o R1c; R1b es halogeno, oxo, hidroxi o -CN; R1c es -C(=O)O(R1f), -C(=O)(CH2)m(R1e), -S(R1f), -S(O)2(R1f) o -S(=O)(R1f), alquilo inferior, alcoxi inferior, amino, amido, haloalquilo inferior, fenilo, heteroarilo, cicloalquilo, heterocicloalquilo, cicloalquiloxi o heterocicloalquiloxi opcionalmente sustituido por uno o más R1d; R1d es H, halogeno, hidroxi, alquilo inferior, alcoxi inferior o haloalquilo inferior; R1e es H, alquilo inferior, alcoxi inferior, -CN, haloalquilo inferior, fenilo, heteroarilo, cicloalquilo o heterocicloalquilo; R1f es H, alquilo inferior, haloalquilo inferior, fenilo, heteroarilo, cicloalquilo o heterocicloalquilo; R2 es N(R2a)2; cada R2a es con independencia H o R2b; cada R2b es con independencia alquilo inferior, fenilo, heteroarilo, cicloalquilo, heterocicloalquilo o heterocicloalquil-alquileno, opcionalmente sustituido por uno o más R2c; R2c es R2d o R2e; R2d es halogeno, oxo o hidroxi; R2e es -N(R2g)2, -C(=O)(R2g), -C(=O)O(R2g), -C(=O)N(R2g)2, -N(R2g)C(=O)(R2g), -S(=O)2(R2g), -S(O)2N(R2g)2, alquilo inferior, alcoxi inferior, haloalquilo inferior, fenilo, heteroarilo, heteroariloxi, cicloalquilo o heterocicloalquilo, opcionalmente sustituido por uno o más R2f; cada R2f es con independencia H, halogeno, alquilo inferior, alcoxi inferior, haloalquilo inferior; cada R2g es con independencia H, alquilo inferior, alcoxi inferior, haloalquilo inferior o fenilo; R3 es -C(=O)R3a; R3a es alquilo inferior, alcoxi inferior, fenilo o N(R3b)2; cada R3b es con independencia H o alquilo inferior; R4 es -O(R4a); R4a es H o R4b; R4b es alquilo inferior, fenilo, bencilo, haloalquilo inferior, cicloalquilo, heterocicloalquilo, heteroarilo, opcionalmente sustituido por uno o más R4c; R4c es halogeno, hidroxi, alquilo inferior, haloalquilo inferior o alcoxi inferior; Q2 es cicloalquilo, cicloalquenilo, heterocicloalquilo o heteroarilo, opcionalmente sustituido por uno o más Q2a; Q2a es Q2b o Q2c; Q2b es halogeno, oxo, hidroxi, -CN, -SCH3, -S(O)2CH3 o -S(=O)CH3; Q2c es Q2d o Q2e; o dos Q2a forman juntos un sistema de anillo bicíclico, opcionalmente sustituido por uno o más Q2b o Q2c; Q2d es -O(Q2e), -S(=O)2(Q2e), -C(=O)N(Q2e)2, -S(O)2(Q2e), -C(=O)(Q2e), -C(=O)O(Q2e), -N(Q2e)2; -N(Q2e)C(=O)(Q2e), -N(Q2e)C(=O)O(Q2e) o -N(Q2e)C(=O)N(Q2e)2; cada Q2e es con independencia H o Q2e'; cada Q2e' es con independencia alquilo inferior, fenilo, bencilo, haloalquilo inferior, cicloalquilo, cicloalquenilo, heterocicloalquilo o heteroarilo, opcionalmente sustituido por uno o más Q2f; Q2f es Q2g o Q2h; Q2g es halogeno, hidroxi, ciano, oxo o -C(=O)(Q2h); Q2h es alquilo inferir, haloalquilo inferior, alcoxi inferior, amino, fenilo, bencilo, cicloalquilo, heterocicloalquilo o heteroarilo, opcionalmente sustituido por uno o más Q2i; y Q2i es halogeno, hidroxi, ciano, alquilo inferior, haloalquilo inferior o alcoxi inferior; o una sal farmacéuticamente aceptable del mismo.
ARP090100621A 2008-02-25 2009-02-23 Pirrolopirazinas inhibidores de quinasa AR070468A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US3103508P 2008-02-25 2008-02-25
US20572409P 2009-01-22 2009-01-22

Publications (1)

Publication Number Publication Date
AR070468A1 true AR070468A1 (es) 2010-04-07

Family

ID=40514094

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090100621A AR070468A1 (es) 2008-02-25 2009-02-23 Pirrolopirazinas inhibidores de quinasa

Country Status (20)

Country Link
US (1) US7939531B2 (es)
EP (1) EP2247592B1 (es)
JP (1) JP5368485B2 (es)
KR (1) KR101261514B1 (es)
CN (1) CN101939324B (es)
AR (1) AR070468A1 (es)
AT (1) ATE522535T1 (es)
AU (1) AU2009218607B2 (es)
BR (1) BRPI0908494A2 (es)
CA (1) CA2713710A1 (es)
CL (1) CL2009000406A1 (es)
DK (1) DK2247592T3 (es)
IL (1) IL206358A0 (es)
MX (1) MX2010008198A (es)
PE (1) PE20091493A1 (es)
PL (1) PL2247592T3 (es)
PT (1) PT2247592E (es)
RU (1) RU2503676C2 (es)
TW (1) TWI380987B (es)
WO (1) WO2009106442A1 (es)

Families Citing this family (97)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2250172B1 (en) * 2008-02-25 2011-08-31 F. Hoffmann-La Roche AG Pyrrolopyrazine kinase inhibitors
BRPI0907928A2 (pt) * 2008-02-25 2015-07-28 Hoffmann La Roche Inibidores de pirrolopirazina quinase.
ES2372908T3 (es) * 2008-02-25 2012-01-27 F. Hoffmann-La Roche Ag Inhibidores de la pirrolopirazina quinasa.
WO2009106445A1 (en) * 2008-02-25 2009-09-03 F. Hoffmann-La Roche Ag Pyrrolopyrazine kinase inhibitors
WO2009152133A1 (en) * 2008-06-10 2009-12-17 Abbott Laboratories Novel tricyclic compounds
RU2011123647A (ru) 2008-11-10 2012-12-20 Вертекс Фармасьютикалз Инкорпорейтед Соединения, полезные в качестве ингибиторов atr киназы
JP5930278B2 (ja) 2008-11-25 2016-06-08 ユニバーシティー オブ ロチェスター Ｍｌｋ阻害剤および使用方法
PT3354650T (pt) 2008-12-19 2022-06-20 Vertex Pharma Compostos úteis como inibidores da cinase atr
PE20120508A1 (es) 2009-06-17 2012-05-09 Vertex Pharma Inhibidores de la replicacion de los virus de la gripe
KR101481872B1 (ko) * 2009-09-10 2015-01-12 에프. 호프만-라 로슈 아게 Ｊａｋ의 억제제
AR079234A1 (es) 2009-12-01 2012-01-04 Abbott Lab Derivados heterociclicos condensados nitrogenados, composiciones farmaceuticas que los contienen y uso de los mismos para tratar afecciones oncologicas, del sistema nervioso y/o del sistema inmune.
NZ599938A (en) 2009-12-01 2014-08-29 Abbvie Inc Novel tricyclic compounds
EP2338888A1 (en) * 2009-12-24 2011-06-29 Almirall, S.A. Imidazopyridine derivatives as JAK inhibitors
SG182662A1 (en) 2010-01-28 2012-08-30 Harvard College Compositions and methods for enhancing proteasome activity
UY33213A (es) 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
US8518945B2 (en) 2010-03-22 2013-08-27 Hoffmann-La Roche Inc. Pyrrolopyrazine kinase inhibitors
US8481541B2 (en) * 2010-03-22 2013-07-09 Hoffmann-La Roche Inc. Pyrrolopyrazine kinase inhibitors
EP2568984A1 (en) 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
MX2012013081A (es) 2010-05-12 2013-05-09 Vertex Pharma Compuestos utiles como inhibidores de cinasa atr.
EP2569286B1 (en) 2010-05-12 2014-08-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
CN102947272A (zh) 2010-05-12 2013-02-27 沃泰克斯药物股份有限公司 用作atr激酶抑制剂的2-氨基吡啶衍生物
EP2569289A1 (en) 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Pyrazines useful as inhibitors of atr kinase
JP2013526540A (ja) 2010-05-12 2013-06-24 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 Ａｔｒキナーゼ阻害剤として有用な化合物
KR20130083386A (ko) * 2010-05-20 2013-07-22 에프. 호프만-라 로슈 아게 피롤로[2,3-ｂ]피라진-7-카복스아마이드 유도체 및 ＪＡＫ 및 ＳＹＫ 억제제로서의 그의 용도
EP2571881A1 (en) 2010-05-20 2013-03-27 F.Hoffmann-La Roche Ag Pyrrolopyrazine derivatives as syk and jak inhibitors
CN103153994B (zh) * 2010-05-24 2016-02-10 罗切斯特大学 双环杂芳基激酶抑制剂及使用方法
US8623869B2 (en) 2010-06-23 2014-01-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2463289A1 (en) 2010-11-26 2012-06-13 Almirall, S.A. Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
DE102011009961A1 (de) * 2011-02-01 2012-08-02 Merck Patent Gmbh 7-Azaindolderivate
MX2013011450A (es) 2011-04-05 2014-02-03 Vertex Pharma Compuestos de aminopirazina utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr).
WO2012154967A1 (en) 2011-05-12 2012-11-15 Proteostasis Therapeutics, Inc. Proteostasis regulators
CN103502249A (zh) * 2011-05-17 2014-01-08 普林斯匹亚生物制药公司 作为酪氨酸激酶抑制剂的氮杂吲哚衍生物
WO2012178125A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2723745A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
JP2014522818A (ja) * 2011-06-22 2014-09-08 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 Ａｔｒキナーゼ阻害剤として有用な化合物
DK3141548T3 (da) * 2011-07-05 2020-07-06 Vertex Pharma Fremgangsmåder og mellemprodukter til fremstilling af azaindoler
EP2554544A1 (en) 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
CN104024258B (zh) * 2011-09-01 2017-02-15 霍夫曼-拉罗奇有限公司 吡咯并吡嗪激酶抑制剂
BR112014004569A2 (pt) 2011-09-01 2017-06-13 F. Hoffmann-La Roche Ag composto da fórmula i, métodos para tratar condição inflamatória, artrite reumatoide, asma e distúrbio imune, composição farmacêutica e uso do composto
CA2850566C (en) 2011-09-30 2022-05-03 Vertex Pharmaceuticals Incorporated Process for making 4-[chloro-n-hydroxycarbonimidoyl]phenyl derivative
WO2013049719A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
MX2014003796A (es) 2011-09-30 2015-01-16 Vertex Pharma Compuestos utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr).
IN2014CN02501A (es) 2011-09-30 2015-06-26 Vertex Pharma
US8853217B2 (en) 2011-09-30 2014-10-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2013064445A1 (en) 2011-11-01 2013-05-10 F. Hoffmann-La Roche Ag Imidazopyridazine compounds
WO2013071094A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8841449B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
US8846917B2 (en) 2011-11-09 2014-09-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2013071090A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2776420A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
CN104159891B (zh) 2012-01-10 2016-09-07 霍夫曼-拉罗奇有限公司 哒嗪酰胺化合物和它们作为syk 抑制剂的用途
JP2015515478A (ja) 2012-04-05 2015-05-28 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 Ａｔｒキナーゼの阻害剤として有用な化合物及びそれらの併用療法
KR20150043323A (ko) * 2012-08-21 2015-04-22 에프. 호프만-라 로슈 아게 비장 티로신 키나제 억제제로서 피롤로[2,3-b]피라진
PT2892900T (pt) 2012-09-10 2017-11-06 Principia Biopharma Inc Compostos de pirazolopirimidina como inibidores de cinase
EP2904406B1 (en) 2012-10-04 2018-03-21 Vertex Pharmaceuticals Incorporated Method for measuring atr inhibition mediated increases in dna damage
EP2909202A1 (en) 2012-10-16 2015-08-26 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2922538B1 (en) 2012-11-20 2016-10-19 Principia Biopharma Inc. Azaindole derivatives as jak3 inhibitors
CN104884059B (zh) 2012-11-30 2018-08-10 罗切斯特大学 用于hiv/aids治疗的混合谱系激酶抑制剂
PL3808749T3 (pl) 2012-12-07 2023-07-10 Vertex Pharmaceuticals Incorporated Pirazolo[1,5-a]pirymidyny użyteczne jako inhibitory kinazy atr do leczenia chorób nowotworowych
WO2014116228A1 (en) 2013-01-25 2014-07-31 President And Fellows Of Harvard College Usp14 inhibitors for treating or preventing viral infections
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
US9403780B2 (en) 2013-05-14 2016-08-02 3M Innovative Properties Company Pyridine- or pyrazine-containing compounds
US9296727B2 (en) 2013-10-07 2016-03-29 Vertex Pharmaceuticals Incorporated Methods of regioselective synthesis of 2,4-disubstituted pyrimidines
WO2015073528A1 (en) 2013-11-12 2015-05-21 Proteostasis Therapeutics, Inc. Proteasome activity enhancing compounds
SG10201804021TA (en) 2013-11-13 2018-07-30 Vertex Pharma Methods of preparing inhibitors of influenza viruses replication
US20160376375A1 (en) 2013-11-27 2016-12-29 Baylor College Of Medicine CSGP4 - Specific Chimeric Antigen Receptor for Cancer
CN103665803B (zh) * 2013-12-05 2015-07-01 湖南大学 一种基于金属环钯化合物的结晶聚乳酸及其制备方法和金属环钯化合物的应用
JP6543252B2 (ja) 2013-12-06 2019-07-10 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 ＡＴＲキナーゼ阻害剤として有用な２−アミノ−６−フルオロ−Ｎ−［５−フルオロ−ピリジン−３−イル］ピラゾロ［１，５−ａ］ピリミジン−３−カルボキサミド化合物、その調製、その異なる固体形態および放射性標識された誘導体
EP3107544B1 (en) 2014-02-21 2020-10-07 Principia Biopharma Inc. Salts and solid form of a btk inhibitor
MX2016015874A (es) 2014-06-05 2017-03-27 Vertex Pharma Derivados radiomarcadores de un compuesto de 2-amino-6-fluoro-n-[5 -fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida util como inhibidor de ataxia telangiectasia mutada y rad3 relacionado (atr) cinasa, preparacion de tal compuesto y diferentes formas solidas del mismo.
PT3157566T (pt) 2014-06-17 2019-07-11 Vertex Pharma Método para tratamento de cancro utilizando uma combinação de inibidores chk1 e atr
BR112016030730B1 (pt) 2014-07-03 2023-05-02 Board Of Regents, The University Of Texas System Composto
US20160002248A1 (en) * 2014-07-03 2016-01-07 Board Of Regents, The University Of Texas System Gls1 inhibitors for treating disease
CA2970723C (en) 2014-12-18 2023-09-05 Principia Biopharma Inc. Treatment of pemphigus
CA2984183C (en) 2015-05-01 2021-11-09 Pfizer Inc. Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl, pyrrolo[2,3-b]pyridinyl acrylamides and epoxides thereof
WO2016183116A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
JP6857617B2 (ja) 2015-05-13 2021-04-14 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の複製の阻害剤
TW201718572A (zh) 2015-06-24 2017-06-01 普林斯匹亞生物製藥公司 酪胺酸激酶抑制劑
US10125128B2 (en) 2015-06-30 2018-11-13 Board Of Regents, The University Of Texas System GLS1 inhibitors for treating disease
CA3000684A1 (en) 2015-09-30 2017-04-06 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of dna damaging agents and atr inhibitors
US20170100396A1 (en) 2015-10-07 2017-04-13 F. Hoffmann-La Roche Ag Pyrrolopyrazine derivatives for use in the treatment, amelioration or prevention of influenza
CN116270646A (zh) 2015-10-16 2023-06-23 艾伯维公司 制备咪唑并[1,2-a]吡咯并[2,3-e]吡嗪类化合物及其固态形式的方法
US11365198B2 (en) 2015-10-16 2022-06-21 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US10550126B2 (en) 2015-10-16 2020-02-04 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11512092B2 (en) 2015-10-16 2022-11-29 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11524964B2 (en) 2015-10-16 2022-12-13 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11773106B2 (en) 2015-10-16 2023-10-03 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
AU2016378746B2 (en) 2015-12-22 2021-05-20 Board Of Regents, The University Of Texas System Salt forms and polymorphs of (R)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl) acetamido) pyridazin-3-yl)-2-fluorobutyl)-N-methyl-1H-1,2,3-triazole-4-carboxamide
EP3478273A1 (en) 2016-06-29 2019-05-08 Principia Biopharma Inc. Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
WO2018177993A1 (de) 2017-03-31 2018-10-04 Bayer Cropscience Aktiengesellschaft Pyrazole zur bekämpfung von arthropoden
EP3697764A4 (en) 2017-10-18 2021-07-21 Board Of Regents, The University Of Texas System GLUTAMINASE INHIBITOR THERAPY
EP3720441A1 (en) * 2017-12-04 2020-10-14 H. Hoffnabb-La Roche Ag Pyrrolo[2,3-b]pyrazine compounds as cccdna inhibitors for the treatment of hepatitis b virus (hbv) infection
CA3086759A1 (en) * 2018-01-05 2019-07-11 Ac Immune Sa 1,3,4,5-tetrahydro-2h-pyrido[4,3-b]indole derivatives for the treatment, alleviation or prevention of disorders associated with tau aggregates like alzheimer's disease
AU2020300689A1 (en) * 2019-07-03 2022-02-24 Borah, Inc. Chemical compounds
EP4077316A1 (en) 2019-12-20 2022-10-26 Pfizer Inc. Benzimidazole derivatives
WO2023025109A1 (zh) * 2021-08-23 2023-03-02 上海维申医药有限公司 一类Toll样受体抑制剂及其制备和应用

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100415791B1 (ko) * 1998-06-19 2004-01-24 화이자 프로덕츠 인코포레이티드 피롤로[2,3-디]피리미딘 화합물
CA2699568C (en) * 1999-12-24 2013-03-12 Aventis Pharma Limited Azaindoles
GB0115109D0 (en) * 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
JP2005534618A (ja) 2002-03-28 2005-11-17 エーザイ株式会社 神経変性疾患用の、ｃ−ｊｕｎｎ−末端キナーゼ阻害剤としての７−アザインドール
US20070066641A1 (en) * 2003-12-19 2007-03-22 Prabha Ibrahim Compounds and methods for development of RET modulators
CA2550361C (en) * 2003-12-19 2014-04-29 Prabha Ibrahim Compounds and methods for development of ret modulators
AU2005269387A1 (en) * 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
US7626021B2 (en) * 2004-07-27 2009-12-01 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
EP1814883A1 (en) * 2004-11-22 2007-08-08 Vertex Pharmaceuticals Incorporated Bicyclic inhibitors or rho kinase
US7456289B2 (en) * 2004-12-31 2008-11-25 National Health Research Institutes Anti-tumor compounds
WO2007015866A2 (en) * 2005-07-20 2007-02-08 Kalypsys, Inc. Inhibitors of p38 kinase and methods of treating inflammatory disorders
CL2007002617A1 (es) 2006-09-11 2008-05-16 Sanofi Aventis Compuestos derivados de pirrolo[2,3-b]pirazin-6-ilo; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar inflamacion de las articulaciones, artritis reumatoide, tumores, linfoma de las celulas del manto.
WO2008063888A2 (en) * 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
PE20121126A1 (es) * 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa

Also Published As

Publication number Publication date
MX2010008198A (es) 2010-08-23
JP5368485B2 (ja) 2013-12-18
DK2247592T3 (da) 2011-09-26
CN101939324A (zh) 2011-01-05
CA2713710A1 (en) 2009-09-03
JP2011513262A (ja) 2011-04-28
TWI380987B (zh) 2013-01-01
KR101261514B1 (ko) 2013-05-07
IL206358A0 (en) 2010-12-30
RU2010139566A (ru) 2012-04-10
EP2247592A1 (en) 2010-11-10
AU2009218607B2 (en) 2014-02-13
AU2009218607A1 (en) 2009-09-03
PE20091493A1 (es) 2009-09-25
ATE522535T1 (de) 2011-09-15
EP2247592B1 (en) 2011-08-31
PL2247592T3 (pl) 2012-01-31
KR20100114094A (ko) 2010-10-22
PT2247592E (pt) 2011-11-03
US7939531B2 (en) 2011-05-10
RU2503676C2 (ru) 2014-01-10
US20090215750A1 (en) 2009-08-27
WO2009106442A1 (en) 2009-09-03
TW200938547A (en) 2009-09-16
BRPI0908494A2 (pt) 2015-08-11
CN101939324B (zh) 2014-10-15
CL2009000406A1 (es) 2010-09-21

Similar Documents

Publication Publication Date Title
AR070468A1 (es) Pirrolopirazinas inhibidores de quinasa
AR070467A1 (es) Inhibidores de quinasa de pirrolopirazina
AR081204A1 (es) Pirrolopirazinas como inhibidores de quinasas
AR080779A1 (es) Pirrolopirazina como inhibidores quinasa, composiciones farmaceuticas que los contienen y sus aplicaciones
AR080699A1 (es) Pirrolopirazinas como inhibidores de jak y syk
AR049652A1 (es) Sales cuaternarias antagonistas del receptor ccr2
PE20061164A1 (es) Piperazin-piperidinas sustituidas con pirazinilo con actividad antagonista de cxcr3
AR081203A1 (es) Pirrolopirazinas como inhibidores de quinasas
AR063979A1 (es) Antagonistas de receptor de orexina de diazepam sustituidos
AR036095A1 (es) Compuestos de pirazina que actuan como ligandos del receptor de 5-ht
PE20071001A1 (es) Derivados de 1-(azolin-2-il)-amino-1-fenil-2-hetaril-etano con actividad pesticida
CO5700755A2 (es) Derivados de ester y amida del acido 2-cianopropanoico y metodos de su uso
AR088535A1 (es) Derivados de amidas de aminoacidos sustituidos con n-urea como moduladores de receptor formil peptido del receptor del tipo 1 (fprl-1)
DOP2014000097A (es) Nuevos compuestos inhibidores de la fosfodiesterasa del tipo 10a
Weiss et al. Sulfonamides as selective NaV1. 7 inhibitors: optimizing potency and pharmacokinetics while mitigating metabolic liabilities
JP2013505948A5 (es)
PE20170327A1 (es) 2-AMINO-6-METIL-4,4a,5,6-TETRAHIDROPIRANO[3,4d] [1,3] TIAZIN-8a(8H)-IL-1,3-TIAZOL-4-ILAMIDAS
AR075597A1 (es) Derivados de indol como antagonistas de receptores crth2, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento del asma y otras enfermedades alergicas .
AR081390A1 (es) Compuestos de morfolina, composiciones farmaceuticas que los comprenden y su uso en el tratamiento de enfermedades mediadas por el antagonismo del receptor mineralocorticoide (mra)
WO2005068468A3 (en) Heterocyclic protein kinase inhibitors and uses thereof
CL2012000516A1 (es) Compuestos derivados de 3-[4-(4-(fenil/piridin/ pirimidin)- piperazin -1-il)-butil]-2, 3-dihidro-4h-croman-4-ona, moduladores del receptor de dopamina d3; proceso de preparacion; composicion farmaceutica; y su uso para el tratamiento de un desorden neurologico o psiquiatrico, disfuncion erectil o dependencia a drogas, entre otros.
PE20211246A1 (es) Compuestos biciclicos para su uso como inhibidores de rip1 quinasa
JP2018526419A5 (es)
PE20170083A1 (es) Nuevos compuestos
AR109076A1 (es) Derivados de heterociclos bicíclicos condensados como pesticidas

Legal Events

Date Code Title Description
FB Suspension of granting procedure