MA37450B1 - Inhibiteurs d'indazole du trajet de signal de wnt et leurs utilisations thérapeutiques - Google Patents

Inhibiteurs d'indazole du trajet de signal de wnt et leurs utilisations thérapeutiques

Info

Publication number
MA37450B1
MA37450B1 MA37450A MA37450A MA37450B1 MA 37450 B1 MA37450 B1 MA 37450B1 MA 37450 A MA37450 A MA 37450A MA 37450 A MA37450 A MA 37450A MA 37450 B1 MA37450 B1 MA 37450B1
Authority
MA
Morocco
Prior art keywords
wnt
indazole
therapeutic uses
wnt pathway
signal pathway
Prior art date
Application number
MA37450A
Other languages
English (en)
Other versions
MA37450A1 (fr
Inventor
John Hood
David Wallace
Sunil Kc
Original Assignee
Samumed Llc
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=49292798&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MA37450(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Samumed Llc filed Critical Samumed Llc
Publication of MA37450A1 publication Critical patent/MA37450A1/fr
Publication of MA37450B1 publication Critical patent/MA37450B1/fr

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
    • C07D471/02—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
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/535—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Neurology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Virology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Ophthalmology & Optometry (AREA)

Abstract

L'invention concerne des composés d'indazole pour traiter diverses maladies et pathologies. Plus particulièrement, la présente invention concerne l'utilisation d'un composé d'indazole ou d'analogues de celui-ci, dans le traitement de troubles caractérisés par l'activation d'une signalisation de trajet de wnt (par exemple, un cancer, une prolifération cellulaire anormale, une angiogenèse, la maladie d'alzheimer, une maladie pulmonaire et l'arthrose), la modulation d'évènements cellulaires arbitrés par la signalisation de trajet de wnt, ainsi que de maladies génétiques et d'états/troubles/maladies neurologiques dus à des mutations ou à un dérèglement du trajet de wnt et/ou d'un ou plusieurs des composants de signalisation de wnt. L'invention concerne également des procédés de traitement d'états de maladie associés au wnt. Un mode de réalisation décrit dans la présente invention comprend un composé ayant la structure de la formule i.
MA37450A 2012-04-04 2013-03-13 Inhibiteurs d'indazole du trajet de signal de wnt et leurs utilisations thérapeutiques MA37450B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261620107P 2012-04-04 2012-04-04
PCT/US2013/031055 WO2013151708A1 (fr) 2012-04-04 2013-03-13 Inhibiteurs d'indazole du trajet de signal de wnt et leurs utilisations thérapeutiques

Publications (2)

Publication Number Publication Date
MA37450A1 MA37450A1 (fr) 2016-07-29
MA37450B1 true MA37450B1 (fr) 2018-03-30

Family

ID=49292798

Family Applications (1)

Application Number Title Priority Date Filing Date
MA37450A MA37450B1 (fr) 2012-04-04 2013-03-13 Inhibiteurs d'indazole du trajet de signal de wnt et leurs utilisations thérapeutiques

Country Status (32)

Country Link
US (9) US8673936B2 (fr)
EP (3) EP2760285B1 (fr)
JP (3) JP6167169B2 (fr)
KR (1) KR102048107B1 (fr)
CN (2) CN106892916A (fr)
AU (2) AU2013243899B2 (fr)
BR (1) BR112014023639B1 (fr)
CA (1) CA2853703C (fr)
CL (1) CL2014002511A1 (fr)
CO (1) CO7230336A2 (fr)
CY (1) CY1119485T1 (fr)
DK (1) DK2760285T3 (fr)
ES (1) ES2635386T3 (fr)
HR (1) HRP20171322T1 (fr)
HU (1) HUE033829T2 (fr)
IL (2) IL234743A (fr)
LT (1) LT2760285T (fr)
MA (1) MA37450B1 (fr)
ME (1) ME02832B (fr)
MX (1) MX355435B (fr)
MY (1) MY174896A (fr)
NZ (3) NZ727358A (fr)
PE (1) PE20142216A1 (fr)
PH (3) PH12017500997A1 (fr)
PL (1) PL2760285T3 (fr)
PT (1) PT2760285T (fr)
RS (1) RS56292B1 (fr)
RU (2) RU2638932C2 (fr)
SG (2) SG10201610539RA (fr)
SI (1) SI2760285T1 (fr)
WO (1) WO2013151708A1 (fr)
ZA (3) ZA201406273B (fr)

Families Citing this family (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2987487T3 (da) 2009-08-10 2020-12-07 Samumed Llc Indazolinhibitorer af wnt-signalvejen og terapeutiske anvendelser deraf
CA2986631C (fr) 2009-12-21 2020-06-02 Samumed, Llc 1h-pyrazolo[3,4-b]pyridines et leurs utilisations therapeutiques
BR112014006127A2 (pt) 2011-09-14 2017-04-04 Samumed Llc indazol-3-carboxamidas e sua utilização como inibidores da via de sinalização wnt/b-catenina
PH12017500997A1 (en) 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
CN104271133B (zh) 2012-05-04 2017-10-13 萨穆梅德有限公司 1H‑吡唑并[3,4‑b]吡啶及其治疗应用
EP2943198B1 (fr) 2013-01-08 2019-07-17 Samumed, LLC Inhibiteurs de 3-(benzoimidazol-2-yl)-indazole de la voie de signalisation par wnt et leurs utilisations thérapeutiques
GB201322334D0 (en) * 2013-12-17 2014-01-29 Agency Science Tech & Res Maleimide derivatives as modulators of WNT pathway
GB201322333D0 (en) * 2013-12-17 2014-01-29 Agency Science Tech & Res WNT pathway modulators
WO2015143380A1 (fr) 2014-03-20 2015-09-24 Samumed, Llc Indazole-3-carboxamides 5-substitués, et préparation et utilisation de ceux-ci
JP6434989B2 (ja) * 2014-03-27 2018-12-05 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ ピリジルピペリジン
CN106488775A (zh) 2014-07-11 2017-03-08 基因泰克公司 Notch途径抑制
WO2016040181A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 3-1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine et ses utilisations thérapeutiques
WO2016040193A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine et ses utilisations thérapeutiques
WO2016040184A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 3-3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine et ses utilisations thérapeutiques
WO2016040188A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 3-3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine et ses utilisations thérapeutiques
WO2016040182A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 2-(1h-indazol-3-yl)-1h-imidazo[4,5-c]pyridine et ses utilisations thérapeutiques
WO2016040190A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine et ses utilisations thérapeutiques
WO2016040180A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 3-1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine et ses utilisations thérapeutiques
WO2016040185A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 2-1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine et ses utilisations thérapeutiques
BR112017027227B1 (pt) 2015-06-16 2023-12-12 Eisai R&D Management Co., Ltd Agente anti-câncer
RU2723551C2 (ru) 2015-06-23 2020-06-16 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Кристалл (6S,9aS)-N-бензил-8-({ 6-[3-(4-этилпиперазин-1-ил)азетидин-1-ил]пиридин-2-ил} метил)-6-(2-фтор-4-гидроксибензил)-4,7-диоксо-2-(проп-2-ен-1-ил)гексагидро-2H-пиразино[2,1-c][1,2,4]триазин-1(6H)-карбоксамида
WO2017024015A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines et leurs utilisations thérapeutiques
US10285983B2 (en) 2015-08-03 2019-05-14 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-B] pyridines and therapeutic uses thereof
US10206908B2 (en) 2015-08-03 2019-02-19 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
US10383861B2 (en) 2015-08-03 2019-08-20 Sammumed, LLC 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
US10285982B2 (en) 2015-08-03 2019-05-14 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
US10350199B2 (en) 2015-08-03 2019-07-16 Samumed, Llc 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
US10226448B2 (en) 2015-08-03 2019-03-12 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-yl)-1H-pyrazolo[3,4-B]pyridines and therapeutic uses thereof
US10519169B2 (en) 2015-08-03 2019-12-31 Samumed, Llc 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017023993A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-indol-2-yl)-1h-pyrazolo[4,3-b]pyridines et leurs utilisations thérapeutiques
WO2017023989A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[4,3-b]pyridines et leurs utilisations thérapeutiques
US10166218B2 (en) 2015-08-03 2019-01-01 Samumed, Llc 3-(1H-indol-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
US10231956B2 (en) 2015-08-03 2019-03-19 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
US10195185B2 (en) 2015-08-03 2019-02-05 Samumed, Llc 3-(1H-imidazo[4,5-C]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017024004A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines et leurs utilisations thérapeutiques
WO2017023988A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines et leurs utilisations thérapeutiques
US10463651B2 (en) 2015-08-03 2019-11-05 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-indazoles and therapeutic uses thereof
WO2017023986A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-2-yl)-1h-indazoles et leurs utilisations thérapeutiques
CN105254613A (zh) * 2015-10-08 2016-01-20 苏州云轩医药科技有限公司 具有Wnt信号通路抑制活性的杂环化合物及其应用
WO2017062688A1 (fr) * 2015-10-08 2017-04-13 Suzhou Yunxuan Yiyao Keji Youxian Gongsi Inhibiteurs de la voie de signalisation wnt et leurs applications thérapeutiques
US10450300B2 (en) 2015-10-08 2019-10-22 Suzhou Yunxuan Yiyao Keji Youxian Gongsi Wnt signaling pathway inhibitors and therapeutic applications thereof
CA3001542C (fr) 2015-11-03 2021-02-16 Theravance Biopharma R&D Ip, Llc Composes inhibiteurs de kinase jak pour le traitement de maladies respiratoires
WO2017079759A1 (fr) * 2015-11-06 2017-05-11 Samumed, Llc 2-(3h-indazol-3-yl)-1h-imidazo[4,5-c]pyridines et leurs utilisations anti-inflammatoires
CN109476660B (zh) * 2016-06-01 2023-04-04 拜斯丽治疗有限公司 N-(5-(3-(7-(3-氟苯基)-3h-咪唑并[4,5-c]吡啶-2-基)-1h-吲唑-5-基)吡啶-3-基)-3-甲基丁酰胺的制备方法
CA3041291A1 (fr) 2016-10-21 2018-04-26 Samumed, Llc Procedes d'utilisation d'indazole-3-carboxamides et leur utilisation en tant qu'inhibiteurs de la voie de signalisation wnt/s-catenine
US10758523B2 (en) 2016-11-07 2020-09-01 Samumed, Llc Single-dose, ready-to-use injectable formulations
RU2764979C2 (ru) 2017-05-01 2022-01-24 ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи Способы лечения с использованием соединения-ингибитора jak
CN108314721B (zh) * 2018-01-25 2021-06-22 首都医科大学 人Wnt5a-NL核酸重组体及其制备方法与应用
BR112020017087A2 (pt) 2018-02-23 2020-12-22 Samumed, Llc Indazol-3-carboxamidas substituídas 5-heteroarila e preparação e uso das mesmas
US10759799B2 (en) 2018-06-15 2020-09-01 Samumed, Llc Indazole containing macrocycles and therapeutic uses thereof
WO2020150552A2 (fr) 2019-01-17 2020-07-23 Samumed, Llc Procédés de traitement de troubles du cartilage par inhibition de clk et dyrk
WO2021121420A1 (fr) * 2019-12-20 2021-06-24 江苏凯迪恩医药科技有限公司 Composé benzopyrazole et intermédiaire, procédé de préparation correspondant et utilisation associée
WO2022012058A1 (fr) * 2020-07-16 2022-01-20 江苏凯迪恩医药科技有限公司 Composé à cycles fusionnés, et intermédiaire de celui-ci, procédé de préparation associé et application
MX2023004205A (es) 2020-10-13 2023-07-06 Teva Czech Ind S R O Formas en estado solido de lorecivivint.
EP4346811A1 (fr) * 2021-06-01 2024-04-10 University of Maryland, Baltimore Inhibiteurs de la double voie de signalisation wnt et activateurs d'ampk destinés aux traitements de maladie
CN114259565A (zh) * 2021-12-28 2022-04-01 广州市妇女儿童医疗中心 Wnt4在制备治疗纤维化药物中的应用

Family Cites Families (175)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4164559A (en) 1977-09-21 1979-08-14 Cornell Research Foundation, Inc. Collagen drug delivery device
ES8401486A1 (es) 1981-11-10 1983-12-01 Wellcome Found Un procedimiento para la preparacion de nuevos derivados de imidazo (4,5-c)piridina.
US4474752A (en) 1983-05-16 1984-10-02 Merck & Co., Inc. Drug delivery system utilizing thermosetting gels
US4783443A (en) 1986-03-03 1988-11-08 The University Of Chicago Amino acyl cephalosporin derivatives
EP0410509A1 (fr) 1989-07-25 1991-01-30 Duphar International Research B.V Indazole-1H-carboxamides-3 substitués
GB9414139D0 (en) 1994-07-13 1994-08-31 Smithkline Beecham Plc Novel compounds
US6440102B1 (en) 1998-07-23 2002-08-27 Durect Corporation Fluid transfer and diagnostic system for treating the inner ear
DE19853299C2 (de) 1998-11-19 2003-04-03 Thomas Lenarz Katheter zur Applikation von Medikamenten in Flüssigkeitsräumen des menschlichen Innenohrs
US6120484A (en) 1999-02-17 2000-09-19 Silverstein; Herbert Otological implant for delivery of medicament and method of using same
BR0010482A (pt) 1999-05-21 2002-04-23 Bristol Myers Squibb Co Inibidores pirrolotriazìnicos de cinases
NZ516348A (en) 1999-06-23 2003-06-30 Aventis Pharma Gmbh Substituted benzimidazole
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
TWI262914B (en) 1999-07-02 2006-10-01 Agouron Pharma Compounds and pharmaceutical compositions for inhibiting protein kinases
US6844367B1 (en) 1999-09-17 2005-01-18 Millennium Pharmaceuticals, Inc. Benzamides and related inhibitors of factor Xa
US6967023B1 (en) 2000-01-10 2005-11-22 Foamix, Ltd. Pharmaceutical and cosmetic carrier or composition for topical application
YU54202A (sh) 2000-01-18 2006-01-16 Agouron Pharmaceuticals Inc. Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije
US6897231B2 (en) 2000-07-31 2005-05-24 Signal Pharmaceuticals, Inc. Indazole derivatives as JNK inhibitors and compositions and methods related thereto
US20050009876A1 (en) 2000-07-31 2005-01-13 Bhagwat Shripad S. Indazole compounds, compositions thereof and methods of treatment therewith
MXPA03002294A (es) 2000-09-15 2005-09-08 Vertex Pharma Compuestos de pirazol utiles como inhibidores de proteina cinasa.
WO2002050073A1 (fr) 2000-12-19 2002-06-27 Smithkline Beecham P.L.C. Pyrazolo[3,4-c]pyridine en tant qu'inhibiteurs de gsk-3
US20050192262A1 (en) 2001-03-13 2005-09-01 Tomas Hagstrom Treatment of tumours
EP1435957B1 (fr) 2001-04-30 2009-06-17 Vertex Pharmaceuticals Incorporated Inhibiteurs de gsk-3 et structures cristallines de la proteine gsk-3beta et de complexes proteiques
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
US7642278B2 (en) 2001-07-03 2010-01-05 Novartis Vaccines And Diagnostics, Inc. Indazole benzimidazole compounds
EP1401831A1 (fr) 2001-07-03 2004-03-31 Chiron Corporation Composes d'indazole benzimidazole utilises comme inhibiteurs de tyrosine et de serine/threonine kinase
US20030199516A1 (en) 2001-09-13 2003-10-23 Genesoft, Inc. Methods of treating infection by drug resistant bacteria
US7101884B2 (en) 2001-09-14 2006-09-05 Merck & Co., Inc. Tyrosine kinase inhibitors
US6648873B2 (en) 2001-09-21 2003-11-18 Durect Corp. Aural catheter system including anchor balloon and balloon inflation device
US6897208B2 (en) 2001-10-26 2005-05-24 Aventis Pharmaceuticals Inc. Benzimidazoles
WO2003035005A2 (fr) 2001-10-26 2003-05-01 University Of Connecticut Heteroindanes: nouvelle classe de ligands cannabimimetiques efficaces
IL161576A0 (en) 2001-10-26 2004-09-27 Aventis Pharma Inc Benzimidazoles and analogues and their use as protein kinases inhibitors
FR2831536A1 (fr) 2001-10-26 2003-05-02 Aventis Pharma Sa Nouveaux derives de benzimidazoles, leur procede de preparation, leur application a titre de medicament, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de kdr
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
US20040127492A1 (en) 2002-02-19 2004-07-01 Pharmacia Corporation Cyclic pyrazoles for the inhibition of mitogen activated protein kinase-activated protein kinase-2
EP1476431A1 (fr) 2002-02-19 2004-11-17 Pharmacia Corporation Derives de pyrazole tricycliques utilises dans le traitement des inflammations
EP1506176B1 (fr) 2002-05-17 2013-04-24 Pfizer Italia S.r.l. Derives d'aminoindazole agissant comme inhibiteurs de kinase, methode d'obtention et compositions pharmaceutiques les renfermant
IL164209A0 (en) 2002-05-31 2005-12-18 Eisai Co Ltd Pyrazole derivatives and pharmaceutical compositions containing the same
US7449488B2 (en) 2002-06-04 2008-11-11 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
MXPA04012245A (es) 2002-06-04 2005-09-30 Neogenesis Pharmaceuticals Inc Compuestos de pirazolo[1,5a]pirimidina como agentes antivirales.
US20050282733A1 (en) 2002-06-27 2005-12-22 Prins Johannes B Differentiation modulating agents and uses therefor
GB0218625D0 (en) 2002-08-10 2002-09-18 Astex Technology Ltd Pharmaceutical compounds
FR2845382A1 (fr) 2002-10-02 2004-04-09 Sanofi Synthelabo Derives d'indazolecarboxamides, leur preparation et leur utilisation en therapeutique
DE602004029145D1 (de) 2003-02-27 2010-10-28 Palau Pharma Sa Pyrazolopyridin-derivate
US7135575B2 (en) 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
EP1644371B1 (fr) 2003-07-03 2008-02-13 Aventis Pharmaceuticals Inc. Derives de pyrazoloisoquinoline utiles comme inhibiteurs de kinase
KR101204247B1 (ko) 2003-07-22 2012-11-22 아스텍스 테라퓨틱스 리미티드 3,4-이치환된 1ｈ-피라졸 화합물 및 그의 시클린 의존성키나제 (ｃｄｋ) 및 글리코겐 합성효소 키나제-3(ｇｓｋ-3) 조정제로서 용도
US7008953B2 (en) 2003-07-30 2006-03-07 Agouron Pharmaceuticals, Inc. 3, 5 Disubstituted indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
CN1829713A (zh) 2003-07-30 2006-09-06 辉瑞大药厂 3,5二取代的吲唑化合物、药物组合物和介导或抑制细胞增殖的方法
US20050090529A1 (en) 2003-07-31 2005-04-28 Pfizer Inc 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
WO2005014554A1 (fr) 2003-08-08 2005-02-17 Astex Therapeutics Limited Composes 1h-indazole-3-carboxamide utilises comme modulateurs de la mapkap kinase
DK1692113T3 (en) 2003-11-14 2018-01-08 Lorus Therapeutics Inc ARYLIMIDAZOLES AND USE THEREOF AS ANTICANCES
EP1532980A1 (fr) 2003-11-24 2005-05-25 Novo Nordisk A/S Carboxamides d'indole n-heteroarylé et leurs analogues, utiles comme des activateurs de glucokinase pour le traitement de diabetes
FR2864084B1 (fr) 2003-12-17 2006-02-10 Aventis Pharma Sa Nouveaux derives organophosphores des indazoles et leur utilisation comme medicaments
FR2867778B1 (fr) 2004-03-16 2006-06-09 Sanofi Synthelabo Utilisation de derives d'indazolecarboxamides pour la preparation d'un medicament destine au traitement et a la prevention du paludisme
EP1735306A2 (fr) 2004-03-25 2006-12-27 Memory Pharmaceuticals Corporation Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, et leur preparation et leurs utilisations
DE602005024677D1 (de) 2004-04-22 2010-12-23 Memory Pharm Corp Indole, 1h-indazole, 1,2-benzisoxazole, 1,2-benzoisothiazole, deren herstellung und verwendungen
EP1753428A4 (fr) 2004-05-14 2010-09-15 Abbott Lab Inhibiteurs de kinases en tant qu'agents therapeutiques
WO2006003440A1 (fr) 2004-07-05 2006-01-12 Astex Therapeutics Limited Pyrazoles 3,4-disubstitutes servant d'inhibiteurs de kinases cyclines dependantes (cdk), ou de kinases aurora ou de glycogene syntases 3 (gsk-3)
WO2006015124A2 (fr) 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Modulateurs heterocycliques a cycles fusionnes pour les kinases
US7626021B2 (en) 2004-07-27 2009-12-01 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
AR050188A1 (es) 2004-08-03 2006-10-04 Uriach Y Compania S A J Compuestos heterociclicos condensados utiles en terapia como inhibidores de quinasas p38 y composiciones farmaceuticas que los contienen
WO2006024945A1 (fr) 2004-09-03 2006-03-09 Pfizer Inc. Compositions pharmaceutiques contenant un inhibiteur des cdk
US7652043B2 (en) 2004-09-29 2010-01-26 The Johns Hopkins University WNT pathway antagonists
WO2006054143A1 (fr) 2004-11-17 2006-05-26 Pfizer Inc. Formes polymorphes de {5-[3-(4,6-difluoro-1h-benzimidazol-2-yl)-1h-indazol-5-yl]-4-methyl-pyridin-3-ylmethyl}-ethyl-amine
US20060116519A1 (en) 2004-11-17 2006-06-01 Agouron Pharmaceuticals, Inc. Synthesis of 5-bromo-4-methyl-pyridin-3-ylmethyl)-ethyl-carbamic acid tert-butyl ester
WO2006063302A2 (fr) 2004-12-10 2006-06-15 Wyeth Variants de la glycogene syntase kinase 3 et ses utilisations
US20060142247A1 (en) 2004-12-17 2006-06-29 Guy Georges Tricyclic heterocycles
AU2005321091B2 (en) 2004-12-30 2012-04-12 Astex Therapeutics Limited Pyrazole compounds that modulate the activity of CDK, GSK and Aurora kinases
CA2594963A1 (fr) 2005-01-24 2006-07-27 Neurosystec Corporation Appareil et methode permettant de distribuer des agents therapeutiques et/ou autres a l'oreille interne et a d'autres tissus
WO2006130673A1 (fr) 2005-05-31 2006-12-07 Janssen Pharmaceutica, N.V. 3-benzoimidazolyl-pyrazolopyridines utilisees pour traiter des troubles dont la mediation est assuree par des kinases
MX2008002588A (es) 2005-08-25 2008-03-18 Hoffmann La Roche Inhibidores de p38-map-cinasa y los metodos para utilizarlos.
US8106066B2 (en) 2005-09-23 2012-01-31 Memory Pharmaceuticals Corporation Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, pyrazolopyridines, isothiazolopyridines, and preparation and uses thereof
UY29825A1 (es) 2005-10-03 2007-05-31 Astrazeneca Ab Derivados sustituidos de 3h-imidazol-(4,5 b (beta))piridina-2-il benzoatos y benzamidas, composiciones farmacéuticas que los contienen y aplicaciones
AR057987A1 (es) 2005-11-24 2008-01-09 Astrazeneca Ab Compuestos agonistas de cb1 (receptor cannabinoide)
US8399442B2 (en) 2005-12-30 2013-03-19 Astex Therapeutics Limited Pharmaceutical compounds
GB0602178D0 (en) 2006-02-03 2006-03-15 Merck Sharp & Dohme Therapeutic treatment
JP2009530337A (ja) 2006-03-23 2009-08-27 エフ．ホフマン−ラ ロシュ アーゲー 置換インダゾール誘導体、その製造方法、及びその薬剤としての利用法
MX2008012482A (es) 2006-03-31 2008-10-10 Abbott Lab Compuestos de indazol.
DE602007004618D1 (de) 2006-06-22 2010-03-18 Biovitrum Ab Publ Pyridin- und pyrazinderivate als mnk-kinaseinhibitoren
EP2049106A2 (fr) 2006-07-14 2009-04-22 Astex Therapeutics Limited Combinaisons pharmaceutiques
WO2008048502A1 (fr) 2006-10-17 2008-04-24 Janssen Pharmaceutica N.V. Inhibiteurs de pyrazole kinase substitués
WO2008061109A2 (fr) 2006-11-15 2008-05-22 Forest Laboratories Holdings Limited Dérivés d'indazole utiles en tant que ligands des récepteurs de l'hormone concentrant la mélanine
EP1932834B1 (fr) 2006-12-11 2011-04-27 The Genetics Company, Inc. 1,4-DI-carboxylamides aromatiques et leur utilisation
EP1932830A1 (fr) 2006-12-11 2008-06-18 The Genetics Company, Inc. Sulfamides et leur utilisation en tant que médicament
UY30779A1 (es) 2006-12-14 2008-07-31 Bayer Schering Pharma Ag Derivados de dihidropiridina de utilidad como inhibidores de la proteina quinasa
MX2009010984A (es) 2007-04-10 2010-01-15 Sgx Pharmaceuticals Inc Moduladores de heterociclo cinasa de anillo fusionado.
JP2010526078A (ja) 2007-04-30 2010-07-29 ジェネンテック， インコーポレイテッド Ｗｎｔシグナル伝達のピラゾールインヒビター
CN101730531A (zh) 2007-05-10 2010-06-09 阿瓦隆药品公司 芴、蒽、呫吨、二苯并环庚酮和吖啶的衍生物及其用途
US20080287452A1 (en) 2007-05-16 2008-11-20 Wyeth Heteroaryl/aryl pyrimidine analogs and their use as agonists of the wnt-beta-catenin cellular messaging system
US8304408B2 (en) 2007-05-24 2012-11-06 The Regents Of The University Of California Wnt signaling inhibitors, and methods for making and using them
TW200908968A (en) 2007-05-29 2009-03-01 Sgx Pharmaceuticals Inc Substituted pyrrolopyridines and pyrazolopyridines as kinase modulators
WO2008150845A1 (fr) 2007-05-31 2008-12-11 Vanderbilt University Pyrvinium pour le traitement du cancer
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
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
EP2157859A4 (fr) 2007-06-19 2011-01-12 Takeda Pharmaceutical Composés d'indazole permettant d'activer la glucokinase
FR2917735B1 (fr) 2007-06-21 2009-09-04 Sanofi Aventis Sa Nouveaux indazoles substitutes, leur preparation et leur utilisation en therapeutique
WO2009011850A2 (fr) 2007-07-16 2009-01-22 Abbott Laboratories Nouveaux composés thérapeutiques
JP2010535169A (ja) 2007-08-02 2010-11-18 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ プロテインキナーゼ阻害薬と組み合わせられたモルホリニルアントラサイクリン誘導体
RU2350271C1 (ru) 2007-08-20 2009-03-27 Федеральное государственное учреждение "Российский научный центр "Восстановительная травматология и ортопедия" имени академика Г.А. Илизарова Федерального агентства по высокотехнологичной медицинской помощи", ФГУ "РНЦ "ВТО" им. акад. Г.А. Илизарова Росмедтехнологий" Способ лечения ранних стадий остеоартроза тазобедренного сустава
EP2185556A1 (fr) 2007-08-27 2010-05-19 Wyeth a Corporation of the State of Delaware Analogues de l'imidazopyridine et leur utilisation en tant qu'agonistes du système de messagerie cellulaire wnt-bêta-caténine
WO2009061345A2 (fr) 2007-11-07 2009-05-14 Cornell Research Foundation, Inc. Ciblage de cdk4 et cdk6 dans une thérapie contre le cancer
JP5710268B2 (ja) 2007-12-19 2015-04-30 ジェネンテック， インコーポレイテッド ８−アニリノイミダゾピリジン及びその抗ガン及び／又は抗炎症剤としての使用
AU2009260503B2 (en) * 2008-05-27 2014-03-27 The Board Of Regents Of The University Of Texas System Wnt protein signalling inhibitors
KR101061599B1 (ko) 2008-12-05 2011-09-02 한국과학기술연구원 비정상 세포 성장 질환의 치료를 위한 단백질 키나아제 저해제인 신규 인다졸 유도체, 이의 약학적으로 허용가능한염 및 이를 유효성분으로 함유하는 약학적 조성물
CN101440092B (zh) 2008-12-25 2010-11-17 浙江大学 2-吲唑-4-氮杂吲哚-5-氨基衍生物及制备和应用
US8637507B2 (en) 2009-03-18 2014-01-28 Merck Sharp & Dohme Corp. Bicyclic compounds as inhibitors of diacylglycerol acyltransferase
EP2411001B1 (fr) 2009-03-23 2018-01-17 Merck Sharp & Dohme Corp. Antagonistes du récepteur p2x3 pour le traitement de la douleur
CA2761896A1 (fr) 2009-05-13 2010-11-18 The University Of North Carolina At Chapel Hill Inhibiteurs de kinases cycline-dependantes et leurs procedes d'utilisation
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
JP2013500267A (ja) 2009-07-23 2013-01-07 ヴァンダービルト ユニバーシティー ｍＧＬｕＲ４増強剤としての置換されたベンゾイミダゾールスルホンアミド類および置換されたインドールスルホンアミド類
DK2987487T3 (da) * 2009-08-10 2020-12-07 Samumed Llc Indazolinhibitorer af wnt-signalvejen og terapeutiske anvendelser deraf
JP2013501792A (ja) 2009-08-10 2013-01-17 サミュメッド リミテッド ライアビリティ カンパニー Ｗｎｔ／ｂ−カテニンシグナル伝達経路阻害剤としてのインダゾールおよびその治療的使用
WO2011050245A1 (fr) 2009-10-23 2011-04-28 Yangbo Feng Hétéroaryles bicycliques formant inhibiteurs de la kinase
SG181861A1 (en) 2009-12-21 2012-07-30 Array Biopharma Inc Substituted n-(1h-indazol-4-yl)imidazo[1, 2-a]pyridine-3- carboxamide compounds as cfms inhibitors
CA2986631C (fr) 2009-12-21 2020-06-02 Samumed, Llc 1h-pyrazolo[3,4-b]pyridines et leurs utilisations therapeutiques
KR101792895B1 (ko) 2010-04-06 2017-11-02 피터 맥칼룸 캔서 인스티튜트 방사선 보호 화합물 및 방법
DE102010043379A1 (de) 2010-11-04 2012-05-10 Bayer Schering Pharma Aktiengesellschaft Substituierte 6-Fluor-1H-Pyrazolo[4,3-b]pyridine und ihre Verwendung
US20130310379A1 (en) 2010-11-19 2013-11-21 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
PT2663561E (pt) 2011-01-13 2016-06-07 Novartis Ag Derivados heterocíclicos novos e sua utilização no tratamento de distúrbios neurológicos
US8889684B2 (en) 2011-02-02 2014-11-18 Boehringer Ingelheim International Gmbh Azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors
US9464065B2 (en) 2011-03-24 2016-10-11 The Scripps Research Institute Compounds and methods for inducing chondrogenesis
JP2014509660A (ja) 2011-04-01 2014-04-21 ユニバーシティ・オブ・ユタ・リサーチ・ファウンデイション ＰＤＫ１キナーゼの阻害剤としての置換３−（１Ｈ−ベンゾ｛ｄ｝イミダゾール−２−イル）−１Ｈ−インダゾール類似体
AU2012290116B2 (en) 2011-08-02 2016-11-03 Buck Institute For Research On Aging Tropinol esters and related compounds to promote normal processing of APP
WO2013024011A1 (fr) 2011-08-12 2013-02-21 F. Hoffmann-La Roche Ag Composés d'indazole, compositions et procédés d'utilisation
EP2742046A1 (fr) 2011-08-12 2014-06-18 F.Hoffmann-La Roche Ag Composés de pyrazolo[3,4-c]pyridine et procédés d'utilisation
MX359032B (es) 2011-09-01 2018-09-12 Hoffmann La Roche Inhibidores de pirrolopirazina cinasa.
BR112014006127A2 (pt) 2011-09-14 2017-04-04 Samumed Llc indazol-3-carboxamidas e sua utilização como inibidores da via de sinalização wnt/b-catenina
EP2810198B1 (fr) 2012-01-30 2023-07-12 Universiteit Gent Composés anti-invasifs
EP2827869A4 (fr) 2012-03-23 2015-09-23 Dennis Brown Compositions et procédés d'amélioration du bénéfice thérapeutique de l'indirubine et de ses analogues y compris du mésoindigo
PH12017500997A1 (en) 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
CN104271133B (zh) 2012-05-04 2017-10-13 萨穆梅德有限公司 1H‑吡唑并[3,4‑b]吡啶及其治疗应用
EP2844651A1 (fr) 2012-05-04 2015-03-11 Basf Se Composés contenant du pyrazole substitué et leur utilisation comme pesticides
US9056874B2 (en) 2012-05-04 2015-06-16 Novartis Ag Complement pathway modulators and uses thereof
EP2943198B1 (fr) 2013-01-08 2019-07-17 Samumed, LLC Inhibiteurs de 3-(benzoimidazol-2-yl)-indazole de la voie de signalisation par wnt et leurs utilisations thérapeutiques
TW201441227A (zh) 2013-01-16 2014-11-01 Signal Pharm Llc 經取代吡咯并嘧啶化合物、其組合物及其治療方法
US9327886B2 (en) 2013-03-13 2016-05-03 Bayer Healthcare Llc Vial container with collar cap
CN105143221B (zh) 2013-03-14 2017-06-09 加拉帕戈斯股份有限公司 用于治疗炎性障碍的化合物及其药物组合物
FR3011239A1 (fr) 2013-10-01 2015-04-03 Univ Claude Bernard Lyon Nouveaux derives comprenant un groupe pyrazole et un groupe indole, utiles en tant qu'inhibiteurs de la kinase gsk3
WO2015143380A1 (fr) 2014-03-20 2015-09-24 Samumed, Llc Indazole-3-carboxamides 5-substitués, et préparation et utilisation de ceux-ci
WO2016040184A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 3-3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine et ses utilisations thérapeutiques
WO2016040193A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine et ses utilisations thérapeutiques
WO2016040188A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 3-3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine et ses utilisations thérapeutiques
WO2016040190A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine et ses utilisations thérapeutiques
WO2016040181A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 3-1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine et ses utilisations thérapeutiques
WO2016040180A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 3-1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine et ses utilisations thérapeutiques
WO2016040182A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 2-(1h-indazol-3-yl)-1h-imidazo[4,5-c]pyridine et ses utilisations thérapeutiques
US9538272B2 (en) 2014-09-08 2017-01-03 Apple Inc. Acoustic mesh and methods of use for electronic devices
WO2016040185A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 2-1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine et ses utilisations thérapeutiques
US10206908B2 (en) 2015-08-03 2019-02-19 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
US10231956B2 (en) 2015-08-03 2019-03-19 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
US10463651B2 (en) 2015-08-03 2019-11-05 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-indazoles and therapeutic uses thereof
WO2017023973A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-indol-2-yl)-1h-pyrazolo[3,4-b]pyridines et leurs utilisations thérapeutiques
WO2017023986A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-2-yl)-1h-indazoles et leurs utilisations thérapeutiques
WO2017023993A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-indol-2-yl)-1h-pyrazolo[4,3-b]pyridines et leurs utilisations thérapeutiques
US10383861B2 (en) 2015-08-03 2019-08-20 Sammumed, LLC 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
US10285983B2 (en) 2015-08-03 2019-05-14 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-B] pyridines and therapeutic uses thereof
WO2017024004A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines et leurs utilisations thérapeutiques
WO2017023989A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[4,3-b]pyridines et leurs utilisations thérapeutiques
WO2017023988A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines et leurs utilisations thérapeutiques
US20180228780A1 (en) 2015-08-03 2018-08-16 Samumed, Llc 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
US10350199B2 (en) 2015-08-03 2019-07-16 Samumed, Llc 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
WO2017023981A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines et ses utilisations thérapeutiques
US10195185B2 (en) 2015-08-03 2019-02-05 Samumed, Llc 3-(1H-imidazo[4,5-C]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
US10285982B2 (en) 2015-08-03 2019-05-14 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
WO2017024015A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines et leurs utilisations thérapeutiques
US10166218B2 (en) 2015-08-03 2019-01-01 Samumed, Llc 3-(1H-indol-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
US10226448B2 (en) 2015-08-03 2019-03-12 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-yl)-1H-pyrazolo[3,4-B]pyridines and therapeutic uses thereof
WO2017079759A1 (fr) 2015-11-06 2017-05-11 Samumed, Llc 2-(3h-indazol-3-yl)-1h-imidazo[4,5-c]pyridines et leurs utilisations anti-inflammatoires
AR108325A1 (es) 2016-04-27 2018-08-08 Samumed Llc Isoquinolin-3-il carboxamidas y preparación y uso de las mismas
CN109476660B (zh) 2016-06-01 2023-04-04 拜斯丽治疗有限公司 N-(5-(3-(7-(3-氟苯基)-3h-咪唑并[4,5-c]吡啶-2-基)-1h-吲唑-5-基)吡啶-3-基)-3-甲基丁酰胺的制备方法
CA3041291A1 (fr) 2016-10-21 2018-04-26 Samumed, Llc Procedes d'utilisation d'indazole-3-carboxamides et leur utilisation en tant qu'inhibiteurs de la voie de signalisation wnt/s-catenine
US10758523B2 (en) 2016-11-07 2020-09-01 Samumed, Llc Single-dose, ready-to-use injectable formulations
EP3813826A4 (fr) 2018-06-26 2022-07-06 BioSplice Therapeutics, Inc. Méthodes de traitement du cancer à l'aide d'un inhibiteur de clk
WO2020150552A2 (fr) 2019-01-17 2020-07-23 Samumed, Llc Procédés de traitement de troubles du cartilage par inhibition de clk et dyrk

Also Published As

Publication number Publication date
CO7230336A2 (es) 2015-03-31
MA37450A1 (fr) 2016-07-29
EP2760285A4 (fr) 2015-04-22
JP2018188479A (ja) 2018-11-29
KR20140143796A (ko) 2014-12-17
US9199991B2 (en) 2015-12-01
ZA201406273B (en) 2019-12-18
HRP20171322T1 (hr) 2017-10-20
ZA201906377B (en) 2023-04-26
US20240116927A1 (en) 2024-04-11
RU2638932C2 (ru) 2017-12-19
US20130267495A1 (en) 2013-10-10
US10407425B2 (en) 2019-09-10
PH12014502183A1 (en) 2014-12-10
US20140179696A1 (en) 2014-06-26
CN106892916A (zh) 2017-06-27
US20230013144A1 (en) 2023-01-19
SG10201610539RA (en) 2017-02-27
US20140005170A1 (en) 2014-01-02
EP3284744B1 (fr) 2021-05-05
WO2013151708A1 (fr) 2013-10-10
EP3915988A1 (fr) 2021-12-01
CN104202984A (zh) 2014-12-10
RS56292B1 (sr) 2017-12-29
LT2760285T (lt) 2017-10-10
PE20142216A1 (es) 2015-01-12
US9994563B2 (en) 2018-06-12
JP6167169B2 (ja) 2017-07-19
US8664241B2 (en) 2014-03-04
JP2015512443A (ja) 2015-04-27
US20200190082A1 (en) 2020-06-18
JP6401345B2 (ja) 2018-10-10
RU2682245C1 (ru) 2019-03-18
US11697649B2 (en) 2023-07-11
CA2853703C (fr) 2019-01-22
MX355435B (es) 2018-04-18
CN104202984B (zh) 2017-04-05
AU2016203274B2 (en) 2017-09-14
IL234743A (en) 2017-10-31
CA2853703A1 (fr) 2013-10-10
US10947228B2 (en) 2021-03-16
US20160297812A1 (en) 2016-10-13
MY174896A (en) 2020-05-20
BR112014023639B1 (pt) 2022-03-29
PT2760285T (pt) 2017-08-16
PL2760285T3 (pl) 2017-12-29
CL2014002511A1 (es) 2015-01-09
US8673936B2 (en) 2014-03-18
EP3284744A1 (fr) 2018-02-21
RU2014144309A (ru) 2016-05-27
EP2760285A1 (fr) 2014-08-06
BR112014023639A2 (fr) 2017-06-20
ZA201906378B (en) 2022-12-21
ES2635386T3 (es) 2017-10-03
ME02832B (fr) 2018-01-20
US20190071440A1 (en) 2019-03-07
SI2760285T1 (sl) 2017-11-30
EP2760285B1 (fr) 2017-06-21
AU2013243899A1 (en) 2014-04-24
DK2760285T3 (en) 2017-09-18
HUE033829T2 (en) 2018-01-29
KR102048107B1 (ko) 2019-11-22
AU2013243899B2 (en) 2016-02-25
SG11201406310RA (en) 2014-11-27
PH12014502183B1 (en) 2014-12-10
JP2017214393A (ja) 2017-12-07
US8987298B2 (en) 2015-03-24
PH12017501588A1 (en) 2018-07-02
US20150152105A1 (en) 2015-06-04
AU2016203274A1 (en) 2016-06-09
PH12017500997A1 (en) 2018-02-19
NZ727358A (en) 2018-10-26
NZ740938A (en) 2019-11-29
CY1119485T1 (el) 2018-03-07
NZ629323A (en) 2016-12-23
IL254935A0 (en) 2017-12-31
MX2014011996A (es) 2014-11-10

Similar Documents

Publication Publication Date Title
MA37450B1 (fr) Inhibiteurs d'indazole du trajet de signal de wnt et leurs utilisations thérapeutiques
MA43619B1 (fr) Isoquinolin-3-yl carboxamides et préparation et utilisation de ceux-ci
MA43605B1 (fr) Isoquinolin-3-yl carboxamides et préparation et utilisation de ceux-ci
MX370487B (es) Inhibidores de 3-(benzo-imidazol-2-il)-indazol de la senda de señalización de wnt y usos terapéuticos de los mismos.
IN2014CN02646A (fr)
MA39219B1 (fr) Nouveaux composés inhibiteurs de la kinase lrrk2 utilisés pour le traitement du parkinson, de l’alzheimer et de la sclérose latérale amyotrophique
EA201491592A1 (ru) Соединения индолов и индазолов, активирующие ampk
MA35576B1 (fr) Nouveaux composés
MA35342B1 (fr) Composés de-pipéridinyle utiles comme inhibiteurs de la tankyrase
TN2015000547A1 (fr) Composes heteroaromatiques et leur utilisation comme ligands de dopamine d1
MA32655B1 (fr) Composés modulant sélectivement le récepteur cb2
EA201290894A1 (ru) Азетидиновые производные пиперидин-4-ила как ингибиторы jak1
MA31506B1 (fr) Composes modulant les sirtuines
MA38349A1 (fr) Œstra-1,3,5(10),16-tétraéno-3-carboxamide pour inhiber la 17-bêta-hydroxystéroïde déshydrogénase (akr1c3)
MA38556A1 (fr) Inhibiteurs de bace1
MA32506B1 (fr) Nouveaux composes
MA33190B1 (fr) Composes pour le traitement de troubles metaboliques
MA38925B1 (fr) Dérivés de phénylalanine substitués
MA37763A1 (fr) Difluoro-hexahydro-cyclopentaoxazinyles et difluoro-hexahydro-benzooxazinyles en tant qu'inhibiteurs de bace1
MA31902B1 (fr) Oxazolidinones pour le traitement et/ou la prophylaxie de l'insuffisance cardiaque
EA201100187A1 (ru) Селективные ингибиторы ммр-12 и ммр-13 на основе гидроксамовой кислоты
MX2020005238A (es) Compuestos novedosos como inhibidores mpges-1.
MA31385B1 (fr) Utilisation d'inhibiteurs de hdac pour le traitement de la destruction osseuse
MA33938B1 (fr) 5-alcynyl-pyrimidines
EA200901656A1 (ru) СОЕДИНЕНИЯ И КОМПОЗИЦИИ КАК ИНГИБИТОРЫ ITPKb