ECSP12012042A - Derivados de pirazol como inhibidores de jak - Google Patents

Derivados de pirazol como inhibidores de jak

Info

Publication number
ECSP12012042A
ECSP12012042A ECSP12012042A ECSP12012042A EC SP12012042 A ECSP12012042 A EC SP12012042A EC SP12012042 A ECSP12012042 A EC SP12012042A EC SP12012042 A ECSP12012042 A EC SP12012042A
Authority
EC
Ecuador
Prior art keywords
jak inhibitors
derivatives
pirazol derivatives
pirazol
jak
Prior art date
Application number
Other languages
English (en)
Inventor
Paul Robert Eastwood
Moll Joan Taltavull
Matassa Victor Giulio
TAÑA Jordi BACH
Santacama Luis Miquel Pages
Rodrigues Jacob Gonzalez
Original Assignee
Almirall Sa
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=43706312&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ECSP12012042(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from EP10382039A external-priority patent/EP2360158A1/en
Application filed by Almirall Sa filed Critical Almirall Sa
Publication of ECSP12012042A publication Critical patent/ECSP12012042A/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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P17/06—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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material 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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Otolaryngology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Se describen nuevos derivados de pirazol que tienen la estructura química de fórmula (I); así como un procedimiento para su preparación, composiciones farmacéuticas que los comprenden y su uso en terapira como inhibidores de quinasas janus (JAK).
ECSP12012042 2010-02-18 2012-07-13 Derivados de pirazol como inhibidores de jak ECSP12012042A (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP10382039A EP2360158A1 (en) 2010-02-18 2010-02-18 Pyrazole derivatives as jak inhibitors
US30605110P 2010-02-19 2010-02-19
US37108110P 2010-08-05 2010-08-05
EP10382217 2010-08-05

Publications (1)

Publication Number Publication Date
ECSP12012042A true ECSP12012042A (es) 2013-05-31

Family

ID=43706312

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSP12012042 ECSP12012042A (es) 2010-02-18 2012-07-13 Derivados de pirazol como inhibidores de jak

Country Status (22)

Country Link
US (2) US9206183B2 (es)
EP (1) EP2536728A1 (es)
JP (1) JP5820400B2 (es)
KR (1) KR20130002371A (es)
CN (1) CN102762570B (es)
AR (1) AR080187A1 (es)
AU (1) AU2011217489B2 (es)
CA (1) CA2790155A1 (es)
CL (1) CL2012002265A1 (es)
CO (1) CO6541658A2 (es)
CR (1) CR20120427A (es)
EA (1) EA201201143A1 (es)
EC (1) ECSP12012042A (es)
GT (1) GT201200243A (es)
MX (1) MX2012009430A (es)
NZ (2) NZ600881A (es)
PE (1) PE20130012A1 (es)
PH (1) PH12012501408A1 (es)
SG (2) SG182713A1 (es)
UY (1) UY33213A (es)
WO (1) WO2011101161A1 (es)
ZA (1) ZA201204959B (es)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY33213A (es) 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
WO2012030918A1 (en) * 2010-09-01 2012-03-08 Ambit Biosciences Corporation Adenosine a3 receptor modulating compounds and methods of use thereof
EP2463289A1 (en) 2010-11-26 2012-06-13 Almirall, S.A. Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
DK2734205T3 (en) 2011-07-21 2018-06-14 Tolero Pharmaceuticals Inc Heterocyclic Protein Kinase Inhibitors
EP2554544A1 (en) 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
SG11201406584TA (en) 2012-04-24 2014-11-27 Vertex Pharma Dna-pk inhibitors
US9013997B2 (en) 2012-06-01 2015-04-21 Broadcom Corporation System for performing distributed data cut-through
PH12015501130B1 (en) * 2012-11-21 2023-01-27 Ptc Therapeutics Inc Substituted reverse pyrimidine bmi-1 inhibitors
EP2938610A2 (en) * 2012-12-28 2015-11-04 The U.S.A. as represented by the Secretary, Department of Health and Human Services Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof
MX2015008829A (es) 2013-01-09 2016-04-25 Concert Pharmaceuticals Inc Momelotinib deuterado.
RS62649B1 (sr) 2013-03-12 2021-12-31 Vertex Pharma Inhibitori dnk-pk
MX370588B (es) 2013-08-30 2019-12-16 Ptc Therapeutics Inc Inhibidores de la bmi-1 de pirimidina sustituida.
KR102411227B1 (ko) 2013-10-17 2022-06-21 버텍스 파마슈티칼스 인코포레이티드 Dna-pk 억제제로서 (s)-n-메틸-8-(1-((2'-메틸-[4,5'-비피리미딘]-6-일)아미노)프로판-2-일)퀴놀린-4-카복스아미드 및 이의 듀테로화된 유도체의 공결정
US10584115B2 (en) 2013-11-21 2020-03-10 Ptc Therapeutics, Inc. Substituted pyridine and pyrazine BMI-1 inhibitors
LT3077395T (lt) 2013-12-05 2018-02-12 Pfizer Inc. Pirolo[2,3-d]pirimidinilo, pirolo[2,3-b]pirazinilo ir pirolo[2,3-d]piridinilo akrilamidai
US9868722B2 (en) 2013-12-10 2018-01-16 Cleave Biosciences, Inc. Monocyclic pyrimidine/pyridine compounds as inhibitors of P97 complex
TW201605811A (zh) * 2013-12-11 2016-02-16 阿爾米雷爾有限公司 作為jak抑制劑之吡唑并嘧啶-2基衍生物
US9828363B2 (en) 2014-01-20 2017-11-28 Cleave Biosciences, Inc. Fused pyrimidines as inhibitors of P97 complex
WO2015138273A1 (en) * 2014-03-13 2015-09-17 Merck Sharp & Dohme Corp. 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors
TWI679205B (zh) 2014-09-02 2019-12-11 日商日本新藥股份有限公司 吡唑并噻唑化合物及醫藥
KR20170090476A (ko) 2014-12-05 2017-08-07 어레이 바이오파마 인크. 야누스 키나제 저해제로서의 4,6-치환된-피라졸로[1,5-a]피라진
TW201705961A (zh) * 2015-06-11 2017-02-16 阿爾米雷爾有限公司 作為jak抑制劑的2-(吡唑并吡啶-3-基)嘧啶衍生物
WO2017013270A1 (en) 2015-07-23 2017-01-26 Universite De Strasbourg Use of leptin signaling inhibitor for protecting kidneys from patients having ciliopathy
MX383747B (es) 2016-02-24 2025-03-14 Pfizer Derivados de pirazolo[1,5-a]pirazin-4-ilo como inhibidores de quinasas janus (jak)
TWI712604B (zh) 2016-03-01 2020-12-11 日商日本新藥股份有限公司 具jak抑制作用之化合物之結晶
MX394860B (es) 2016-09-27 2025-03-24 Vertex Pharma Metodo para tratar cancer usando una combinacion de agentes que dañan adn e inhibidores de proteina cinasa dependiente de adn (adn-pk).
WO2019034973A1 (en) 2017-08-14 2019-02-21 Pfizer Inc. PYRAZOLO [1,5-A] PYRAZIN-4-YL AND RELATED DERIVATIVES
MX2020010556A (es) 2018-04-13 2021-03-02 Sumitomo Pharma Oncology Inc Inhibidores de cinasa de insercion proviral en linfomas murinos (pim) para el tratamiento de neoplasias mieloproliferativas y fibrosis asociadas con cancer.
JP2021535198A (ja) 2018-08-17 2021-12-16 ピーティーシー セラピューティクス, インコーポレイテッド 膵臓癌を治療する方法
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
HUE072069T2 (hu) 2019-02-12 2025-10-28 Sumitomo Pharma America Inc 2-((1R,4R)-4-((3-(3-(trifluormetil)fenil)imidazo[1,2- b]piridazin-6-il)amino)ciklohexil)propán-2-ol sósavas sójának kristályos formája
PL3954689T3 (pl) * 2019-04-12 2024-08-05 Primegene (Beijing) Co., Ltd. Związki pochodne pirazolopirazyny, kompozycja farmaceutyczna i ich zastosowanie
CA3156007A1 (en) 2019-09-27 2021-04-01 Disc Medicine, Inc. METHODS OF TREATING MYELOFIBROSE AND ASSOCIATED CONDITIONS
AU2021273014A1 (en) 2020-05-13 2022-11-17 AbbVie Deutschland GmbH & Co. KG Anti-hemojuvelin (HJV) antibodies for treating anemia of chronic disease
ES3075793T3 (en) 2020-05-13 2026-08-07 Disc Medicine Inc Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis
AU2023372386A1 (en) 2022-10-31 2025-05-08 Sumitomo Pharma America, Inc. Pim1 inhibitor for treating myeloproliferative neoplasms
WO2026139841A1 (en) * 2024-12-24 2026-07-02 Novartis Ag Aromatic carboxamide compounds and methods of using thereof

Family Cites Families (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS54128591A (en) 1978-03-25 1979-10-05 Kyowa Hakko Kogyo Co Ltd Cephalosporin analog
PL182198B1 (en) 1995-06-21 2001-11-30 Asta Medica Ag Pharmaceutic powder holding container with integrated measuring device and powdered
GB9919778D0 (en) * 1999-08-21 1999-10-27 Zeneca Ltd Chemical compounds
GB0020556D0 (en) * 2000-08-22 2000-10-11 Glaxo Group Ltd Fused pyrazole derivatives
PE20020506A1 (es) 2000-08-22 2002-07-09 Glaxo Group Ltd Derivados de pirazol fusionados como inhibidores de la proteina cinasa
EP2048142A3 (en) 2001-04-26 2009-04-22 Eisai R&D Management Co., Ltd. Nitrogen-containing condensed cyclic compound having a pyrazolyl group as a substituent group and pharmaceutical composition thereof
DE10129703A1 (de) 2001-06-22 2003-01-02 Sofotec Gmbh & Co Kg Zerstäubungssystem für eine Pulvermischung und Verfahren für Trockenpulverinhalatoren
CA2450555A1 (en) 2001-06-25 2003-01-03 Merck & Co., Inc. (pyrimidyl)(phenyl)substituted fused heteroaryl p38 inhibiting and pkg kinase inhibiting compounds
US7125888B2 (en) 2002-05-02 2006-10-24 Merck & Co., Inc. Tyrosine kinase inhibitors
ES2195785B1 (es) 2002-05-16 2005-03-16 Almirall Prodesfarma, S.A. Nuevos derivados de piridazin-3(2h)-ona.
CA2487679A1 (en) * 2002-05-30 2003-12-11 Vertex Pharmaceuticals Incorporated Inhibitors of jak and cdk2 protein kinases
ES2211344B1 (es) 2002-12-26 2005-10-01 Almirall Prodesfarma, S.A. Nuevos derivados de piridazin-3(2h)-ona.
ES2232306B1 (es) 2003-11-10 2006-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de piridazin-3(2h)-ona.
ES2364340T3 (es) * 2004-03-30 2011-08-31 Vertex Pharmaceuticals Incorporated Azaindoles útiles como inhibidores de jak y otras proteína quinasas.
ES2251866B1 (es) 2004-06-18 2007-06-16 Laboratorios Almirall S.A. Nuevos derivados de piridazin-3(2h)-ona.
ES2251867B1 (es) 2004-06-21 2007-06-16 Laboratorios Almirall S.A. Nuevos derivados de piridazin-3(2h)-ona.
WO2006008207A1 (de) 2004-07-17 2006-01-26 Robert Bosch Gmbh Sigma-delta-modulator
WO2006038001A1 (en) 2004-10-06 2006-04-13 Celltech R & D Limited Aminopyrimidine derivatives as jnk inhibitors
WO2006068826A2 (en) * 2004-12-21 2006-06-29 Smithkline Beecham Corporation 2-pyrimidinyl pyrazolopyridine erbb kinase inhibitors
DK2383268T3 (en) 2005-02-04 2015-09-14 Astrazeneca Ab PYRAZOLYLAMINOPYRIDINDERIVATER useful as kinase inhibitors
ES2265276B1 (es) 2005-05-20 2008-02-01 Laboratorios Almirall S.A. Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor beta2 adrenergico.
ES2296516B1 (es) 2006-04-27 2009-04-01 Laboratorios Almirall S.A. Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor beta2 adrenergico.
JP5352452B2 (ja) * 2006-06-06 2013-11-27 メディシノバ, インコーポレイテッド 置換ピラゾロ[1,5−a]ピリジン化合物およびその使用方法
TW200831104A (en) 2006-10-04 2008-08-01 Pharmacopeia Inc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
EP2086973B1 (en) 2006-10-11 2012-01-25 Amgen Inc., Imidazo- and triazolo-pyridine compounds and methods of use therof
ES2302447B1 (es) 2006-10-20 2009-06-12 Laboratorios Almirall S.A. Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor beta2 adrenergico.
JP5442449B2 (ja) * 2006-12-22 2014-03-12 アステックス、セラピューティックス、リミテッド 新規化合物
ES2319596B1 (es) 2006-12-22 2010-02-08 Laboratorios Almirall S.A. Nuevos derivados de los acidos amino-nicotinico y amino-isonicotinico.
US7977336B2 (en) 2006-12-28 2011-07-12 Banyu Pharmaceutical Co. Ltd Aminopyrimidine derivatives as PLK1 inhibitors
ES2306595B1 (es) 2007-02-09 2009-09-11 Laboratorios Almirall S.A. Sal de napadisilato de 5-(2-((6-(2,2-difluoro-2-feniletoxi)hexil)amino)-1-hidroxietil)-8-hidroxiquinolin-2(1h)-ona como agonista del receptor adrenergico beta2.
WO2008118823A2 (en) 2007-03-26 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
CN101790526A (zh) * 2007-06-08 2010-07-28 雅培制药有限公司 用作激酶抑制剂的5-杂芳基取代的吲唑化合物
UY31272A1 (es) 2007-08-10 2009-01-30 Almirall Lab Nuevos derivados de ácido azabifenilaminobenzoico
CA2695251C (en) 2007-08-14 2016-06-21 Bayer Schering Pharma Aktiengesellschaft Fused imidazoles for cancer treatment
CA2696631A1 (en) 2007-08-17 2009-02-26 Icagen, Inc. Heterocycles as potassium channel modulators
EA201000615A1 (ru) 2007-10-17 2010-12-30 Новартис Аг Производные имидазо[1,2-а]пиридина, применимые в качестве ингибиторов апк (активиноподобной киназы)
JP2011500806A (ja) * 2007-10-25 2011-01-06 メルク・シャープ・エンド・ドーム・コーポレイション 治療用化合物
RU2010129928A (ru) 2007-12-19 2012-01-27 Вертекс Фармасьютикалз Инкорпорейтед (Us) Пиразоло[1, 5-а]пиримидины, используемые в качестве ингибиторов jak2
WO2009086123A1 (en) 2007-12-21 2009-07-09 Wyeth Imidazo [1,2-a] pyridine compounds
RU2503676C2 (ru) 2008-02-25 2014-01-10 Ф.Хоффманн-Ля Рош Аг Пирролопиразиновые ингибиторы киназы
JP5576370B2 (ja) 2008-08-06 2014-08-20 ファイザー・インク Chk−1阻害剤としての6置換2−ヘテロシクリルアミノピラジン化合物
TW201022262A (en) 2008-10-29 2010-06-16 Astrazeneca Ab Novel compounds 515
AR074870A1 (es) * 2008-12-24 2011-02-16 Palau Pharma Sa Derivados de pirazolo (1,5-a ) piridina
JP5759471B2 (ja) * 2009-10-29 2015-08-05 ヴェクチュラ リミテッド Jak3キナーゼ阻害剤としての窒素含有ヘテロアリール誘導体
EP2338888A1 (en) 2009-12-24 2011-06-29 Almirall, S.A. Imidazopyridine derivatives as JAK inhibitors
UY33213A (es) 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
EP2397482A1 (en) 2010-06-15 2011-12-21 Almirall, S.A. Heteroaryl imidazolone derivatives as jak inhibitors
EP2463289A1 (en) 2010-11-26 2012-06-13 Almirall, S.A. Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
EP2527344A1 (en) 2011-05-25 2012-11-28 Almirall, S.A. Pyridin-2(1H)-one derivatives useful as medicaments for the treatment of myeloproliferative disorders, transplant rejection, immune-mediated and inflammatory diseases
EP2554544A1 (en) 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors

Also Published As

Publication number Publication date
CO6541658A2 (es) 2012-10-16
AU2011217489A1 (en) 2012-08-30
PE20130012A1 (es) 2013-01-28
UY33213A (es) 2011-09-30
CA2790155A1 (en) 2011-08-25
US20130209400A1 (en) 2013-08-15
NZ701440A (en) 2015-05-29
ZA201204959B (en) 2013-03-27
CR20120427A (es) 2013-01-30
SG10201500735VA (en) 2015-04-29
US20150118186A1 (en) 2015-04-30
NZ600881A (en) 2014-12-24
JP2013519696A (ja) 2013-05-30
US20140086870A9 (en) 2014-03-27
KR20130002371A (ko) 2013-01-08
CN102762570B (zh) 2015-11-25
PH12012501408A1 (en) 2012-10-29
EA201201143A1 (ru) 2013-03-29
CL2012002265A1 (es) 2013-02-15
WO2011101161A1 (en) 2011-08-25
GT201200243A (es) 2015-06-02
CN102762570A (zh) 2012-10-31
US9206183B2 (en) 2015-12-08
AU2011217489B2 (en) 2015-09-03
EP2536728A1 (en) 2012-12-26
MX2012009430A (es) 2012-09-07
SG182713A1 (en) 2012-09-27
AR080187A1 (es) 2012-03-21
JP5820400B2 (ja) 2015-11-24

Similar Documents

Publication Publication Date Title
CR20120427A (es) Derivados de pirazol como inhibidores de jak
CR20120634A (es) Derivados de heteroaril imidazolona como inhibidores de jak
GT201200207A (es) Derivados de imidazopiridina como inhibidores de jak
CR20140031A (es) Derivados de piridin-2(1h)-ona como inhibidores de jak
GT201300266A (es) Derivados de pirrolotriazinona como inhibidores de pi3k
UY32239A (es) Nuevos derivados de (3-oxo)piridazin-4-ilurea
CO6781467A2 (es) Derivados de imidazo[1,2-b]piridazina e imidazo[4,5-b]piridina como inhibidores de jak
UY35086A (es) Derivados de pirrolotriazinona como inhibidores de pi3k
UY33440A (es) ?compuestos pirimidinílicos para uso como inhibidores de atr?.
CL2017003107A1 (es) Derivados de 2-(pirazolopiridin-3-il)pirimidina como inhibidores de jak
ECSP109917A (es) Nuevos derivados de ácido azabifenilaminobenzoico
UY31918A (es) Compuestos de pirazol inhibidores de fgfr, composiciones farmaceuticas que los comprenden, procesos para su preparacion y su uso como medicamento
UY35087A (es) Derivados de pirrolotriazinona como inhibidores de pi3k
UY35332A (es) Derivados de pirrolotriazina como inhibidores de pi3k
UY35876A (es) Derivados de pirazolopirimidin-2-ilo como inhibidores de jak
ECSP13012372A (es) Nuevos derivados 1,4-diazepanos, inhibidores de pde-5.
UY30982A1 (es) Nuevos derivados de pirimidina, procesos de preparacion, composiciones farmacéuticas conteniéndolos y aplicaciones.
ECSP15015088A (es) Derivados de pirrolotriazinona como inhibidores de pi3k
CU20100087A7 (es) Algunos derivados de 2-pirazinona y su uso como inhibidores de elastasa de los neutrófilos
CU20100005A7 (es) Derivados de pirimidina trisustituida para el tratamiento de enfermedades proliferativas
CU20100250A7 (es) Compuestos pirazólicos 436
UY34430A (es) 18-metil-6,7-metilen-3-oxo-17-pregn-4-en-21,17bcarbolactona, preparados farmacéuticos que contienen los compuestos mencionados y su uso en la terapia de la endometriosis.