TW201204732A - Novel homopiperazine derivatives as protein tyrosine kinase inhibitors and pharmaceutical use thereof - Google Patents

Novel homopiperazine derivatives as protein tyrosine kinase inhibitors and pharmaceutical use thereof

Info

Publication number
TW201204732A
TW201204732A TW100124316A TW100124316A TW201204732A TW 201204732 A TW201204732 A TW 201204732A TW 100124316 A TW100124316 A TW 100124316A TW 100124316 A TW100124316 A TW 100124316A TW 201204732 A TW201204732 A TW 201204732A
Authority
TW
Taiwan
Prior art keywords
tyrosine kinase
protein tyrosine
kinase inhibitors
novel
pharmaceutical use
Prior art date
Application number
TW100124316A
Other languages
English (en)
Chinese (zh)
Inventor
Simon Feldbaek Nielsen
Daniel Rodriguez Greve
Gunnar Grue-Sorensen
Carsten Ryttersgaard
Soren Christian Schou
Anette Graven Sams
Original Assignee
Leo Pharma As
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 Leo Pharma As filed Critical Leo Pharma As
Publication of TW201204732A publication Critical patent/TW201204732A/zh

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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/08—Antiseborrheics
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P17/16—Emollients or protectives, e.g. against radiation
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Toxicology (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
TW100124316A 2010-07-09 2011-07-08 Novel homopiperazine derivatives as protein tyrosine kinase inhibitors and pharmaceutical use thereof TW201204732A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US36309510P 2010-07-09 2010-07-09

Publications (1)

Publication Number Publication Date
TW201204732A true TW201204732A (en) 2012-02-01

Family

ID=44513700

Family Applications (1)

Application Number Title Priority Date Filing Date
TW100124316A TW201204732A (en) 2010-07-09 2011-07-08 Novel homopiperazine derivatives as protein tyrosine kinase inhibitors and pharmaceutical use thereof

Country Status (7)

Country Link
US (1) US9586961B2 (OSRAM)
EP (1) EP2590981B1 (OSRAM)
JP (1) JP2013533868A (OSRAM)
CN (1) CN102985425A (OSRAM)
RU (1) RU2013105450A (OSRAM)
TW (1) TW201204732A (OSRAM)
WO (1) WO2012003829A1 (OSRAM)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104072499A (zh) * 2013-03-29 2014-10-01 黄传满 哌嗪取代嘧啶类化合物及其用途
CN103242321A (zh) * 2013-05-21 2013-08-14 苏州科捷生物医药有限公司 苄基哌嗪类化合物及其抗肿瘤用途
CN103396414B (zh) * 2013-07-16 2015-06-03 浙江医药高等专科学校 咪唑取代的噻唑并环己烷类化合物、及其抗肿瘤用途
MD4649C1 (ro) * 2013-12-05 2020-04-30 Pfizer Inc. Pirol[2,3-d]pirimidinil, pirol[2,3-b]pirazinil şi pirol[2,3-d]piridinil acrilamide
AR101214A1 (es) * 2014-07-22 2016-11-30 Bayer Cropscience Ag Ciano-cicloalquilpenta-2,4-dienos, ciano-cicloalquilpent-2-en-4-inas, ciano-heterociclilpenta-2,4-dienos y ciano-heterociclilpent-2-en-4-inas sustituidos como principios activos contra el estrés abiótico de plantas
CN105712998B (zh) * 2014-12-05 2019-12-13 上海润诺生物科技有限公司 氮杂吲哚类衍生物、其制备方法及其在医药上的应用
SI3512857T1 (sl) * 2016-09-14 2021-07-30 Janssen Pharmaceutica Nv Spiro biciklični zaviralci interakcije menin-MLL
JP7101685B2 (ja) * 2017-01-20 2022-07-15 レオ ファーマ アクティーゼルスカブ 新規ｊａｋキナーゼ阻害剤としての二環式アミン
EP3576743B1 (en) * 2017-02-03 2023-01-18 LEO Pharma A/S 5-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-5-azaspiro[2 5]octane-8-carboxylic acid derivatives as jak kinase inhibitors
CN108069986B (zh) * 2017-12-08 2018-10-02 牡丹江医学院 一种治疗角膜炎的活性药物及其制备方法
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
EP4025219A4 (en) 2019-09-05 2023-08-30 Incyte Corporation RUXOLITINIB FORMULATION TO REDUCE ITCHING IN ATOPIC DERMATITIS
US11992490B2 (en) 2019-10-16 2024-05-28 Incyte Corporation Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP)
IL293965A (en) 2019-12-19 2022-08-01 Janssen Pharmaceutica Nv History of Spiro straight chain transformed

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1087970E (pt) * 1998-06-19 2004-06-30 Pfizer Prod Inc Compostos pirrolo¬2,3-d|pirimidina
PA8474101A1 (es) * 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
JP5213229B2 (ja) 2004-04-23 2013-06-19 エグゼリクシス， インコーポレイテッド キナーゼ調節因子および使用方法
SI2049529T1 (sl) 2006-07-14 2010-11-30 Merck Sharp & Dohme Substituiran diazepan oreksin receptor antagonist
AU2008234822A1 (en) * 2007-04-02 2008-10-09 Palau Pharma, S. A. Pyrrolopyrimidine derivatives as JAK3 inhibitors
WO2009017838A2 (en) 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
ES2557931T3 (es) * 2007-08-08 2016-01-29 Lexicon Pharmaceuticals, Inc. (7H-Pirrolo[2,3-d]pirimidin-4-il)-piperazinas como inhibidores de cinasas para el tratamiento de cáncer e inflamación
CA2714177A1 (en) 2008-02-06 2009-08-13 Novartis Ag Pyrrolo [2,3-d] pyridines and use thereof as tyrosine kinase inhibitors
NZ588830A (en) 2008-04-22 2012-11-30 Portola Pharm Inc Inhibitors of protein kinases

Also Published As

Publication number Publication date
JP2013533868A (ja) 2013-08-29
EP2590981B1 (en) 2014-09-03
US9586961B2 (en) 2017-03-07
EP2590981A1 (en) 2013-05-15
US20130172325A1 (en) 2013-07-04
CN102985425A (zh) 2013-03-20
RU2013105450A (ru) 2014-08-20
WO2012003829A1 (en) 2012-01-12

Similar Documents

Publication Publication Date Title
TW201204732A (en) Novel homopiperazine derivatives as protein tyrosine kinase inhibitors and pharmaceutical use thereof
PH12019500521A1 (en) Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer
AU2012258977A8 (en) Inhibitors of LRRK2 kinase activity
NZ754827A (en) Substituted pyrazole compounds and methods of using them for treatment of hyperproliferative diseases
MX2013007792A (es) Nuevos derivados de sulfamida piperazina como inhibidores de proteina tirosina cinasa y uso farmaceutico de los mismos.
AU2012277802A8 (en) Novel inhibitor compounds of phosphodiesterase type 10A
TW201613593A (en) Molecules for administration to ROS1 mutant cancer cells
MX2013012983A (es) Composiciones y metodos para la produccion de compuestos de pirimidina con actividad inhibidora de tirosina cinasa de bruton.
WO2018102452A3 (en) Using substituted pyrazole compounds for treatment of hyperproliferative diseases
PH12018502028B1 (en) Allosteric modulators of nicotinic acetylcholine receptors
MY186126A (en) Quinazoline inhibitors of activating mutant forms of epidermal growth factor receptor
MY169142A (en) Macrocyclic derivatives for the treatment of proliferative diseases
TN2014000356A1 (en) Heterocyclyl compounds as mek inhibitors
NZ598137A (en) Oxazine derivatives and their use in the treatment of neurological disorders
PH12013502090A1 (en) 1,3 oxazines as bace1 and/or bace2 inhibitors
WO2014100071A3 (en) Substituted pyrrolopyrimidines as hdm2 inhibitors
ECSP13012852A (es) Derivados de 6-ciclobutil-1,5-dihidro-pirazolo [3,4-d]pirimidin-4-ona y su uso como inhibidores de pde9a.
MX2013007558A (es) 1,4-oxazinas como inhibidores de los genes enzima de segmentacion de la proteina precursora del sitio 1 y/o 2 (bace1 y/o bace2).
PH12013502262A1 (en) Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as bace1 and/or bace2 inhibitors
MX2013007957A (es) 1,4-oxazinas como inhibidores de los genes de enzima de segmentacion de la proteina precursora amiloide del sitio beta 1 y/o (bace1 y/o bace2).
MX357780B (es) Derivados policíclicos, proceso para su preparación y su uso farmacéutico.
MX336051B (es) Diarilacetileno hidracido que contiene inhibidores de tirosina quinasa.
WO2012048129A3 (en) Inhibitors of polo-like kinase
CY1120082T1 (el) Αμινογλυκοσιδες και χρησεις αυτων στη θεραπευτικη αγωγη γενετικων διαταραχων
EA201491321A1 (ru) Фторметил-5,6-дигидро-4н-[1,3]оксазины