PE20110365A1 - Diazacarbazoles como inhibidores de checkpoint quinasa 1 (chk1) - Google Patents

Diazacarbazoles como inhibidores de checkpoint quinasa 1 (chk1)

Info

Publication number
PE20110365A1
PE20110365A1 PE2010001127A PE2010001127A PE20110365A1 PE 20110365 A1 PE20110365 A1 PE 20110365A1 PE 2010001127 A PE2010001127 A PE 2010001127A PE 2010001127 A PE2010001127 A PE 2010001127A PE 20110365 A1 PE20110365 A1 PE 20110365A1
Authority
PE
Peru
Prior art keywords
halo
dipyrido
pyrrol
chk1
inhibitors
Prior art date
Application number
PE2010001127A
Other languages
English (en)
Inventor
Hazel Joan Dyke
Charles Ellwood
Emanuela Gancia
Lewis J Gazzard
Simon Charles Goodacre
Samuel S Kintz
Joseph P Lyssikatos
Calum Macleod
Karen Williams
Huifen Chen
Original Assignee
Genentech Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41066724&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20110365(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Genentech Inc filed Critical Genentech Inc
Publication of PE20110365A1 publication Critical patent/PE20110365A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • 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
    • A61K31/435—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
    • A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and 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
    • A61K31/505—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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic 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
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • 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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (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 Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE 1,7-DIAZACARBAZOL DE FORMULAS (I), (I-a) Y (I-b) DONDE X ES CR2 O N, DONDE R2 ES H, HALO, CN, ENTRE OTROS; Y ES CR4 O N, DONDE R4 ES H, HALO, CF3, ENTRE OTROS; Z ES CR8 O N, DONDE R8 ES H, CN, NO2, ENTRE OTROS; R3 ES H, CN, HALO, ENTRE OTROS; R5 ES H, HALO, OCF3, OH, ENTRE OTROS; R6 ES H, CN, ALQUILO, ENTRE OTROS; R7 ES H, OH, O(ALQUILO C1-C3), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 3-[4-(1-METIL-PIPERIDIN-4-IL)-FENIL]-9H-DIPIRIDO[2,3-b;4',3'-d]PIRROL-6-CARBONITRILO; 3-(4-PIRROLIDIN-1-IL-FENIL)-9H-DIPIRIDO[2,3-b;4',3'-d]PIRROL-6-CARBONITRILO; N-{2-[4-(6-CIANO-9H-DIPIRIDO[2,3-b;4',3'-d]PIRROL-3-IL)-FENOXI]-ETIL}-METANSULFONAMIDA; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA CON UN SEGUNDO COMPUESTO ACTIVO QUE ES UN AGENTE QUE DANA EL ADN. DICHOS COMPUESTOS SON INHIBIDORES DE CHECKPOINT QUINASA 1 (CHK1) SIENDO UTILES EN EL TRATAMIENTO DE CANCER DE MAMA, CANCER DE PULMON DE CELULAS NO PEQUENAS, SARCOMA, MELANOMA
PE2010001127A 2008-06-11 2009-06-10 Diazacarbazoles como inhibidores de checkpoint quinasa 1 (chk1) PE20110365A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US6074608P 2008-06-11 2008-06-11
US14800109P 2009-01-28 2009-01-28

Publications (1)

Publication Number Publication Date
PE20110365A1 true PE20110365A1 (es) 2011-07-11

Family

ID=41066724

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2013002559A PE20140609A1 (es) 2008-06-11 2009-06-10 Diazacarbazoles y metodos de uso
PE2010001127A PE20110365A1 (es) 2008-06-11 2009-06-10 Diazacarbazoles como inhibidores de checkpoint quinasa 1 (chk1)

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2013002559A PE20140609A1 (es) 2008-06-11 2009-06-10 Diazacarbazoles y metodos de uso

Country Status (21)

Country Link
US (3) US8501765B2 (es)
EP (2) EP2706059A1 (es)
JP (2) JP5599784B2 (es)
KR (1) KR101710732B1 (es)
CN (2) CN102119163A (es)
AR (1) AR072092A1 (es)
AU (1) AU2009258124C1 (es)
BR (1) BRPI0909954A2 (es)
CA (1) CA2725754C (es)
CL (1) CL2010001415A1 (es)
DK (1) DK2300475T3 (es)
ES (1) ES2529361T3 (es)
HK (1) HK1149933A1 (es)
IL (1) IL209754A0 (es)
MX (1) MX2010013627A (es)
PE (2) PE20140609A1 (es)
PH (1) PH12013502369A1 (es)
RU (2) RU2515972C2 (es)
TW (2) TWI466886B (es)
WO (1) WO2009151598A1 (es)
ZA (1) ZA201008483B (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL1896040T3 (pl) 2005-06-29 2012-12-31 Threshold Pharmaceuticals Inc Proleki alkilatora fosforoamidowego
EP2706059A1 (en) * 2008-06-11 2014-03-12 Genentech, Inc. Diazacarbazoles and methods of use
AR072084A1 (es) * 2008-06-12 2010-08-04 Sanofi Aventis Derivados de azacarbolinas, su preparacion y su utilizacion terapeutica como inhibidores de las quinasas pim
AR073431A1 (es) * 2009-03-24 2010-11-03 Sanofi Aventis Derivados de azacarbolinas 9h- pirrolo (2,3-b:5,4-c) dipiridina , su preparacion y si utilizacion terapeutica
FR2950891B1 (fr) * 2009-10-06 2012-11-09 Sanofi Aventis Derives d'azacarbolines 9h-pyrrolo[2,3-b:5,4-c']dipyridine, leur preparation et leur utilisation therapeutique
US20110183938A1 (en) * 2009-12-16 2011-07-28 Genentech, Inc. 1,7-diazacarbazoles and methods of use
BR112013011918A2 (pt) 2010-11-16 2020-08-25 Array Biopharma, Inc inibidor de chk1, composição farmacêutica e kit compreendendo o referido inibidor
CN102503959B (zh) * 2011-10-25 2015-04-08 南方医科大学 一种稠三环类化合物及其制备方法、以及含该类化合物的药物组合物及其应用
WO2013068755A1 (en) * 2011-11-09 2013-05-16 Cancer Research Technology Limited 5-(pyridin-2-yl-amino)-pyrazine-2-carbonitrile compounds and their therapeutic use
EP2793882A4 (en) 2011-12-22 2015-04-29 Threshold Pharmaceuticals Inc ADMINISTRATION OF HYPOXIA ACTIVATED DRUGS IN COMBINATION WITH CHK1 INHIBITORS FOR THE TREATMENT OF CANCER
CN104662018B (zh) 2012-04-20 2017-10-24 阿迪维纳斯治疗有限公司 取代的杂双环化合物、组合物及其医疗应用
EP2671881A1 (en) 2012-06-07 2013-12-11 Syngenta Participations AG. Pesticidally active pyridyl- and pyrimidyl- substituted thiazole derivatives
AU2014293011A1 (en) 2013-07-26 2016-03-17 Race Oncology Ltd. Compositions to improve the therapeutic benefit of bisantrene
WO2015069489A1 (en) 2013-11-06 2015-05-14 Merck Patent Gmbh Predictive biomarker for hypoxia-activated prodrug therapy
EP3125920B1 (en) 2014-04-04 2020-12-23 Del Mar Pharmaceuticals Dianhydrogalactitol, diacetyldianhydrogalactitol or dibromodulcitol to treat non-small-cell carcinoma of the lung and ovarian cancer
CN107118207B (zh) * 2017-05-22 2020-10-02 苏州东南药业股份有限公司 一类cdk抑制剂的制备方法
EP3860996A4 (en) 2018-10-02 2022-08-31 Northwestern University BETA-CARBOLINES AS POSITIVE ALLOSTERIC MODULATORS OF HUMAN SEROTONIN RECEPTOR 2C (5-HT2C)
CA3122183A1 (en) * 2018-12-13 2020-06-18 Intervet International B.V. Process for preparing 1-[(3r,4s)-4-cyanotetrahydropyran-3-yl]-3-[(2-fluoro-6-methoxy-4-pyridyl)amino]p yrazole-4-carboxamide

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001068648A1 (en) 2000-03-15 2001-09-20 Aventis Pharma Deutschland Gmbh Substituted beta-carbolines with ikb-kinase inhibiting activity
BR0109161A (pt) * 2000-03-15 2002-11-26 Aventis Pharma Gmbh Beta-carbolinas substituìdas com atividade de inibição de ikb-quinase
GB0116966D0 (en) * 2001-07-11 2001-09-05 Pharma Mar Sa Anittumoral compounds
GB0121941D0 (en) * 2001-09-11 2001-10-31 Astrazeneca Ab Chemical compounds
DE60217532T8 (de) * 2001-11-07 2008-02-07 Millennium Pharmaceuticals, Inc., Cambridge Carboline derivate als ikb-inhibitoren zur behandlung des m ultiplen myelomas
MXPA05008688A (es) * 2003-02-17 2005-10-05 Pharmacia Italia Spa Derivados tetraciclicos de pirazol como inhibidores de la cinasa, procedimiento para su preparacion y composiciones farmaceuticas que los comprenden.
SE0401655D0 (sv) 2004-06-24 2004-06-24 Astrazeneca Ab New compounds
JP2008542433A (ja) * 2005-06-09 2008-11-27 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ＣＤＫ−１インヒビターとしてのα−カルボリン
US8119655B2 (en) * 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
WO2008054956A2 (en) 2006-10-09 2008-05-08 Takeda San Diego, Inc. Kinase inhibitors
EP2081930A2 (en) 2006-10-09 2009-07-29 Takeda San Diego, Inc. Kinase inhibitors
US8618121B2 (en) 2007-07-02 2013-12-31 Cancer Research Technology Limited 9H-pyrimido[4,5-B]indoles, 9H-pyrido[4',3':4,5]pyrrolo[2,3-D]pyridines, and 9H 1,3,6,9 tetraaza-fluorenes as CHK1 kinase function inhibitors
US8133506B2 (en) 2008-03-12 2012-03-13 Aptalis Pharmatech, Inc. Drug delivery systems comprising weakly basic drugs and organic acids
US20090312288A1 (en) 2008-04-16 2009-12-17 Takeda Pharmaceutical Company Limited Kinase inhibitors
EP2706059A1 (en) * 2008-06-11 2014-03-12 Genentech, Inc. Diazacarbazoles and methods of use
AR072084A1 (es) * 2008-06-12 2010-08-04 Sanofi Aventis Derivados de azacarbolinas, su preparacion y su utilizacion terapeutica como inhibidores de las quinasas pim
WO2010015589A1 (en) 2008-08-05 2010-02-11 Nycomed Gmbh Benzyl-substituted tetracyclic heterocyclic compounds as pde5 inhibitors
AR073431A1 (es) * 2009-03-24 2010-11-03 Sanofi Aventis Derivados de azacarbolinas 9h- pirrolo (2,3-b:5,4-c) dipiridina , su preparacion y si utilizacion terapeutica

Also Published As

Publication number Publication date
HK1149933A1 (en) 2011-10-21
BRPI0909954A2 (pt) 2015-11-03
WO2009151598A8 (en) 2010-05-06
US9216980B2 (en) 2015-12-22
DK2300475T3 (en) 2014-12-08
PE20140609A1 (es) 2014-05-22
CN102119163A (zh) 2011-07-06
RU2013156074A (ru) 2015-06-27
JP5599784B2 (ja) 2014-10-01
ZA201008483B (en) 2012-03-28
IL209754A0 (en) 2011-02-28
MX2010013627A (es) 2010-12-21
RU2010154105A (ru) 2012-07-20
ES2529361T3 (es) 2015-02-19
JP2011522889A (ja) 2011-08-04
US20130261104A1 (en) 2013-10-03
WO2009151598A1 (en) 2009-12-17
US20150087630A1 (en) 2015-03-26
PH12013502369A1 (en) 2015-09-21
CL2010001415A1 (es) 2011-05-06
JP2015028027A (ja) 2015-02-12
RU2515972C2 (ru) 2014-05-20
EP2300475A1 (en) 2011-03-30
AU2009258124B2 (en) 2015-01-29
US20110118230A1 (en) 2011-05-19
AU2009258124C1 (en) 2016-01-07
CN104059066A (zh) 2014-09-24
AU2009258124A2 (en) 2011-01-20
AR072092A1 (es) 2010-08-04
CA2725754C (en) 2017-05-23
US8501765B2 (en) 2013-08-06
KR101710732B1 (ko) 2017-02-27
EP2300475B1 (en) 2014-11-05
AU2009258124A1 (en) 2009-12-17
TW201011023A (en) 2010-03-16
EP2706059A1 (en) 2014-03-12
TWI466886B (zh) 2015-01-01
CA2725754A1 (en) 2009-12-17
KR20110015697A (ko) 2011-02-16
TW201512199A (zh) 2015-04-01

Similar Documents

Publication Publication Date Title
PE20110365A1 (es) Diazacarbazoles como inhibidores de checkpoint quinasa 1 (chk1)
PE20130038A1 (es) Derivados de piperidin-4-il azetidina como inhibidores de jak1
PE20090773A1 (es) Derivados de morfolina pirimidina
PE20190175A1 (es) Compuestos de pirrolotriazina como inhibidores de tam
PE20091842A1 (es) Pirrolidinonas como activadores de glucoquinasa
PE20090601A1 (es) Derivados de piridin-il-oxi-piridinas como inhibidores de alk5
PE20090772A1 (es) Derivados de bencimidazol
PE20140826A1 (es) Compuestos sustituidos fungicidas de 2-[2-halogenalquil-4-(fenoxi)-fenil]-1-[1,2,4]triazol-1-il-etanol
PE20091158A1 (es) 5-anilinoimidazopiridinas y metodos de uso
PE20121806A1 (es) Macrociclos como inhibidores del factor de coagulacion (fxia)
PE20081512A1 (es) Compuestos y composiciones como inhibidores de la actividad del receptor de canabinoide 1
PE20091816A1 (es) Inhibidores de bace
EA201070110A1 (ru) Стали для кислых сред
PE20091656A1 (es) Compuestos heterociclicos como inhibidores de la cinasa raf
PE20060215A1 (es) 4-fenilamino-quinazolin-6-il-amidas
PE20091623A1 (es) DERIVADOS DE 1H-PIRAZOLO[3,4-b]PIRIDINA COMO INHIBIDORES DE RAF QUINASA
PE20140913A1 (es) Inhibidores de nampt y rock
CO6210776A2 (es) Diaminopirimidinas como fungicidas
EA200800182A1 (ru) Циклические анилинопиридинотриазины в качестве ингибиторов gsk-3
PE20141059A1 (es) Indazoles
PE20121480A1 (es) Aminopirimidinas como inhibidores de syk
PE20100138A1 (es) Derivados de morfolino pirimidina usados en enfermedades relacionadas en mtor quinasa y/o pi3k
PE20121335A1 (es) Compuestos derivados de amida como inhibidores de raf cinasas
PE20090895A1 (es) Derivados de triazol como inhibidores de la jak quinasa
PE20140934A1 (es) Derivados de pirazol

Legal Events

Date Code Title Description
FG Grant, registration
FD Application declared void or lapsed