CN106535890A - 5‑取代的吲唑‑3‑羧酰胺及其制备和应用 - Google Patents

5‑取代的吲唑‑3‑羧酰胺及其制备和应用 Download PDF

Info

Publication number
CN106535890A
CN106535890A CN201580026082.XA CN201580026082A CN106535890A CN 106535890 A CN106535890 A CN 106535890A CN 201580026082 A CN201580026082 A CN 201580026082A CN 106535890 A CN106535890 A CN 106535890A
Authority
CN
China
Prior art keywords
pyridin
carboxylic acid
acid amides
bases
methyl
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN201580026082.XA
Other languages
English (en)
Chinese (zh)
Inventor
J·胡德
S·K·克西
D·M·华莱士
G·K·米塔帕里
B·J·霍菲勒纳
C·C·马克
V·博露
B·伊斯特曼
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
WINTHERIX LLC
Original Assignee
WINTHERIX 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
Application filed by WINTHERIX LLC filed Critical WINTHERIX LLC
Publication of CN106535890A publication Critical patent/CN106535890A/zh
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • 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
    • A61P1/16—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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Psychology (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Reproductive Health (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
CN201580026082.XA 2014-03-20 2015-03-20 5‑取代的吲唑‑3‑羧酰胺及其制备和应用 Pending CN106535890A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461968350P 2014-03-20 2014-03-20
US61/968,350 2014-03-20
PCT/US2015/021847 WO2015143380A1 (en) 2014-03-20 2015-03-20 5-substituted indazole-3-carboxamides and preparation and use thereof

Publications (1)

Publication Number Publication Date
CN106535890A true CN106535890A (zh) 2017-03-22

Family

ID=54141450

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580026082.XA Pending CN106535890A (zh) 2014-03-20 2015-03-20 5‑取代的吲唑‑3‑羧酰胺及其制备和应用

Country Status (16)

Country Link
US (2) US9745271B2 (enExample)
EP (1) EP3119393A4 (enExample)
JP (1) JP6586104B2 (enExample)
KR (1) KR20160135283A (enExample)
CN (1) CN106535890A (enExample)
BR (1) BR112016021626A2 (enExample)
CA (1) CA2942687A1 (enExample)
CL (1) CL2016002364A1 (enExample)
IL (1) IL247713A0 (enExample)
MA (1) MA39763A (enExample)
MX (1) MX2016012208A (enExample)
PE (1) PE20170127A1 (enExample)
PH (1) PH12016501835A1 (enExample)
RU (1) RU2016141088A (enExample)
SG (2) SG11201607816UA (enExample)
WO (1) WO2015143380A1 (enExample)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112020501A (zh) * 2018-02-23 2020-12-01 萨穆梅德有限公司 5-杂芳基取代的吲唑-3-基甲酰胺类及其制备和用途
CN112135821A (zh) * 2018-05-07 2020-12-25 方济各安吉利克化学联合股份有限公司 作为糖原合酶激酶3β抑制剂的1H-吲唑-3-甲酰胺化合物
CN113735798A (zh) * 2021-09-27 2021-12-03 安徽美致诚药业有限公司 一种盐酸罗沙替丁醋酸酯的制备方法
WO2022052861A1 (zh) * 2020-09-09 2022-03-17 成都奥睿药业有限公司 5-取代吲哚3-酰胺衍生物及其制备方法和用途
CN114867718A (zh) * 2019-12-16 2022-08-05 韩国化学研究院 新型吲唑衍生物及其用途
CN115353512A (zh) * 2021-07-30 2022-11-18 上海翊石医药科技有限公司 一种杂环脲类化合物及其制备方法和用途
WO2023098699A1 (en) * 2021-12-01 2023-06-08 Nanjing Immunophage Biotech Co., Ltd Compounds and their uses as cd38 inhibitors

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3473099A1 (en) 2011-09-14 2019-04-24 Samumed, LLC Indazole-3-carboxamides and their use as wnt/b-catenin signaling pathway inhibitors
PH12017500997A1 (en) 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
WO2014110086A2 (en) 2013-01-08 2014-07-17 Samumed, Llc 3-(benzoimidazol-2-yl)-indazole inhibitors of the wnt signaling pathway and therapeutic uses thereof
EP3119393A4 (en) 2014-03-20 2018-02-28 Samumed, LLC 5-substituted indazole-3-carboxamides and preparation and use thereof
WO2016040180A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040181A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040193A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof
WO2016040185A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof
WO2016040184A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040190A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof
US10206909B2 (en) 2015-08-03 2019-02-19 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017023988A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017024003A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017023972A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017023993A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-indol-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017023975A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
WO2017023989A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017024015A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017023987A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]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
WO2017023996A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
WO2017024021A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
WO2017023980A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]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
US10604512B2 (en) 2015-08-03 2020-03-31 Samumed, Llc 3-(1H-indol-2-yl)-1H-indazoles and therapeutic uses thereof
WO2017024026A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
WO2017024010A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
NZ742200A (en) 2015-11-06 2023-01-27 Samumed Llc Treatment of osteoarthritis
TN2018000130A1 (en) * 2015-11-06 2019-10-04 Neurocrine Biosciences Inc N-[2-(1 -benzylpiperidin-4-yl)ethyl]-4-(pyrazin-2-yl)-piperazine-1 -carboxamide derivatives and related compounds as muscarinic receptor 4 (m4) antagonists for treating neurological diseases
EA039638B1 (ru) * 2016-01-06 2022-02-21 Нейрокрин Байосайенсиз, Инк. Антагонисты мускаринового рецептора 4 и способы их применения
KR20230020560A (ko) * 2016-04-15 2023-02-10 펠리시텍스 쎄라퓨틱스, 인코포레이티드 정지 세포 표적화 및 유사분열 억제제를 이용하는 신생물 치료를 위한 조합
MX2018012511A (es) 2016-04-15 2019-07-08 Felicitex Therapeutics Inc Combinaciones para el tratamiento de neoplasias usando localizacion de celulas quiescentes e inhibidores de egfr.
AR108326A1 (es) 2016-04-27 2018-08-08 Samumed Llc Isoquinolin-3-il carboxamidas y preparación y uso de las mismas
AR108325A1 (es) 2016-04-27 2018-08-08 Samumed Llc Isoquinolin-3-il carboxamidas y preparación y uso de las mismas
SI3464285T1 (sl) * 2016-06-01 2023-02-28 Biosplice Therapeutics, Inc. Postopek za pripravo N-(5-(3-(7-(3-fluorofenil)-3H-imidazo(4,5-C)piridin-2-il)-1H-indazol-5- il)piridin-3-il)-3-metilbutanamida
HUE057289T2 (hu) 2016-08-31 2022-05-28 Jiangsu Hengrui Medicine Co Oxopikolinamid-származék, annak elõállítási módszere és gyógyszerészeti felhasználása
EP3528808B1 (en) 2016-10-21 2021-10-06 BioSplice Therapeutics, Inc. Methods of using indazole-3-carboxamides and their use as wnt/b-catenin signaling pathway inhibitors
KR102558716B1 (ko) 2016-11-07 2023-07-21 사뮤메드, 엘엘씨 단일-투여량, 즉시-사용가능한 주사용 제제
KR102279347B1 (ko) * 2016-12-15 2021-07-21 한국생명공학연구원 피리딘계 화합물을 유효성분으로 함유하는 dyrk 관련 질환의 예방 또는 치료용 약학적 조성물
KR101924801B1 (ko) * 2017-08-16 2018-12-04 한국원자력의학원 트리아졸로피리딘계 유도체를 유효성분으로 함유하는 암 예방 또는 치료용 조성물
BR112020003292A2 (pt) 2017-08-16 2020-08-18 Vanderbilt University compostos indazol como potencializadores alostéricos de mglur4 e seus usos terapêuticos, bem como composição farmacêutica e método para fabricação de medicamento para potenciar a atividade do receptor mglur4
KR102179406B1 (ko) * 2017-10-17 2020-11-16 한국화학연구원 신규한 인다졸 유도체 및 이의 용도
US12172975B2 (en) 2018-09-13 2024-12-24 Bristol-Myers Squibb Company 1H-indazole carboxamides as receptor-interacting protein kinase 1 inhibitors (RIPK1)
WO2020150545A1 (en) * 2019-01-17 2020-07-23 Samumed, Llc Pyrazole derivatives as modulators of the wnt/b-catenin signaling pathway
WO2020150552A2 (en) * 2019-01-17 2020-07-23 Samumed, Llc Methods of treating cartilage disorders through inhibition of clk and dyrk
WO2021113478A1 (en) 2019-12-06 2021-06-10 Neurocrine Biosciences, Inc. Muscarinic receptor 4 antagonists and methods of use
CN116322663A (zh) * 2020-09-30 2023-06-23 比奥维拉迪维治疗股份有限公司 Ampk激活剂及其使用方法
WO2024073502A1 (en) * 2022-09-28 2024-04-04 Accutar Biotechnology Inc. Heterocyclic compounds as e3 ligase inhibitors

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102595900A (zh) * 2009-08-10 2012-07-18 埃皮瑟瑞克斯有限公司 Wnt信号传导途径的吲唑抑制剂及其治疗用途
CN102821607A (zh) * 2009-12-21 2012-12-12 萨穆梅德有限公司 1H-吡唑并[3,4-b]吡啶及其治疗应用
US20130079329A1 (en) * 2011-09-14 2013-03-28 John Hood INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/Beta-CATENIN SIGNALING PATHWAY INHIBITORS
WO2013151708A1 (en) * 2012-04-04 2013-10-10 Samumed, Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof

Family Cites Families (35)

* 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
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
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
US6967023B1 (en) 2000-01-10 2005-11-22 Foamix, Ltd. Pharmaceutical and cosmetic carrier or composition for topical application
US6648873B2 (en) 2001-09-21 2003-11-18 Durect Corp. Aural catheter system including anchor balloon and balloon inflation device
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
CN1656079A (zh) 2002-05-31 2005-08-17 卫材株式会社 吡唑化合物和含有该化合物的药物组合物
GB0218625D0 (en) 2002-08-10 2002-09-18 Astex Technology Ltd Pharmaceutical compounds
PL210065B1 (pl) 2002-09-25 2011-11-30 Memory Pharm Corp Związki indazole, benzotiazole i benzoizotiazole, kompozycje farmaceutyczne je zawierające oraz zastosowanie związków
FR2845382A1 (fr) 2002-10-02 2004-04-09 Sanofi Synthelabo Derives d'indazolecarboxamides, leur preparation et leur utilisation en therapeutique
US20040197264A1 (en) 2003-04-04 2004-10-07 Alexander Schwarz Microspheres comprising therapeutic and diagnostic radioactive isotopes
WO2005014554A1 (en) 2003-08-08 2005-02-17 Astex Therapeutics Limited 1h-indazole-3-carboxamide compounds as mapkap kinase modulators
EP1532980A1 (en) 2003-11-24 2005-05-25 Novo Nordisk A/S N-heteroaryl indole carboxamides and analogues thereof, for use as glucokinase activators in the treatment of diabetes
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
CA2560741C (en) 2004-03-25 2013-08-06 Memory Pharmaceuticals Corporation Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, and preparation and uses thereof
CN101102767A (zh) 2004-11-23 2008-01-09 细胞基因公司 用jnk抑制剂治疗和控制中枢神经系统损伤的方法和组合物
EP1861161A4 (en) 2005-01-24 2012-05-16 Neurosystec Corp APPARATUS AND METHOD FOR DISPENSING THERAPEUTIC AND / OR OTHER AGENTS IN THE INTERNAL EAR AND OTHER FABRICS
CN101312968A (zh) 2005-09-23 2008-11-26 记忆药物公司 吲唑、苯并噻唑、苯并异噻唑、苯并异噁唑、吡唑并吡啶、异噻唑并吡啶及其制备和用途
AR057987A1 (es) 2005-11-24 2008-01-09 Astrazeneca Ab Compuestos agonistas de cb1 (receptor cannabinoide)
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
SG182187A1 (en) 2007-06-08 2012-07-30 Abbott Gmbh & Co Kg 5-heteroaryl substituted indazoles as kinase inhibitors
MX2010009462A (es) * 2008-02-29 2010-09-24 Pfizer Derivados de indazol.
WO2011050245A1 (en) 2009-10-23 2011-04-28 Yangbo Feng Bicyclic heteroaryls as kinase inhibitors
AR081626A1 (es) * 2010-04-23 2012-10-10 Cytokinetics Inc Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos
IT1402028B1 (it) 2010-10-14 2013-08-28 Gsi Geosyntec Invest B V Metodo e dispositivo per il drenaggio di acqua infiltrata in strutture idrauliche.
DE102011087651A1 (de) 2011-12-02 2013-06-06 Siemens Aktiengesellschaft Schaltgeräteauslöseeinrichtung
WO2013124158A1 (en) 2012-02-21 2013-08-29 Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. 1h-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors
PE20170186A1 (es) 2014-03-20 2017-04-01 Bayer Pharma AG Nuevos compuestos
CR20160432A (es) 2014-03-20 2017-07-21 Bayer Pharma AG Inhibidores de las vías de señalización de wnt
KR20160127042A (ko) 2014-03-20 2016-11-02 인플라알엑스 게엠베하 바이러스성 폐렴의 치료를 위한 c5a의 억제제
EP3119393A4 (en) 2014-03-20 2018-02-28 Samumed, LLC 5-substituted indazole-3-carboxamides and preparation and use thereof

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102595900A (zh) * 2009-08-10 2012-07-18 埃皮瑟瑞克斯有限公司 Wnt信号传导途径的吲唑抑制剂及其治疗用途
CN102821607A (zh) * 2009-12-21 2012-12-12 萨穆梅德有限公司 1H-吡唑并[3,4-b]吡啶及其治疗应用
US20130079329A1 (en) * 2011-09-14 2013-03-28 John Hood INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/Beta-CATENIN SIGNALING PATHWAY INHIBITORS
WO2013151708A1 (en) * 2012-04-04 2013-10-10 Samumed, Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112020501A (zh) * 2018-02-23 2020-12-01 萨穆梅德有限公司 5-杂芳基取代的吲唑-3-基甲酰胺类及其制备和用途
US11713320B2 (en) 2018-02-23 2023-08-01 Biosplice Therapeutics, Inc. 5-heteroaryl substituted indazole-3-carboxamides and preparation and use thereof
CN112135821A (zh) * 2018-05-07 2020-12-25 方济各安吉利克化学联合股份有限公司 作为糖原合酶激酶3β抑制剂的1H-吲唑-3-甲酰胺化合物
CN112135821B (zh) * 2018-05-07 2024-05-31 方济各安吉利克化学联合股份有限公司 作为糖原合酶激酶3β抑制剂的1H-吲唑-3-甲酰胺化合物
CN114867718A (zh) * 2019-12-16 2022-08-05 韩国化学研究院 新型吲唑衍生物及其用途
CN114867718B (zh) * 2019-12-16 2024-10-01 韩国化学研究院 新型吲唑衍生物及其用途
WO2022052861A1 (zh) * 2020-09-09 2022-03-17 成都奥睿药业有限公司 5-取代吲哚3-酰胺衍生物及其制备方法和用途
CN114230565A (zh) * 2020-09-09 2022-03-25 成都奥睿药业有限公司 5-取代吲哚3-酰胺衍生物及其制备方法和用途
CN114230565B (zh) * 2020-09-09 2023-10-27 成都奥睿药业有限公司 5-取代吲哚3-酰胺衍生物及其制备方法和用途
CN115353512A (zh) * 2021-07-30 2022-11-18 上海翊石医药科技有限公司 一种杂环脲类化合物及其制备方法和用途
CN113735798A (zh) * 2021-09-27 2021-12-03 安徽美致诚药业有限公司 一种盐酸罗沙替丁醋酸酯的制备方法
WO2023098699A1 (en) * 2021-12-01 2023-06-08 Nanjing Immunophage Biotech Co., Ltd Compounds and their uses as cd38 inhibitors

Also Published As

Publication number Publication date
RU2016141088A (ru) 2018-04-25
IL247713A0 (en) 2016-11-30
BR112016021626A2 (pt) 2018-05-15
JP6586104B2 (ja) 2019-10-02
EP3119393A4 (en) 2018-02-28
US20150266825A1 (en) 2015-09-24
US10669240B2 (en) 2020-06-02
WO2015143380A1 (en) 2015-09-24
JP2017508763A (ja) 2017-03-30
MA39763A (fr) 2017-01-25
US9745271B2 (en) 2017-08-29
EP3119393A1 (en) 2017-01-25
PE20170127A1 (es) 2017-03-30
PH12016501835A1 (en) 2017-01-09
CA2942687A1 (en) 2015-09-24
KR20160135283A (ko) 2016-11-25
RU2016141088A3 (enExample) 2018-11-20
MX2016012208A (es) 2017-01-26
CL2016002364A1 (es) 2017-06-23
SG10201914111XA (en) 2020-03-30
US20180127377A1 (en) 2018-05-10
SG11201607816UA (en) 2016-10-28

Similar Documents

Publication Publication Date Title
JP6586104B2 (ja) ５−置換インダゾール−３−カルボキサミドならびにその調製および使用の方法
KR102374844B1 (ko) 이소퀴놀린-3-일 카르복스아마이드 및 이의 제제와 용도
US10081631B2 (en) 2-(1H-indazol-3-yl)-1H-imidazo[4,5-C]pyridine and therapeutic uses thereof
US10350199B2 (en) 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
US10604512B2 (en) 3-(1H-indol-2-yl)-1H-indazoles and therapeutic uses thereof
US10392383B2 (en) 3-(1H-benzo[d]imidazol-2-yl)-1H-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
CN109705097B (zh) 吲唑-3-羧酰胺及其作为WNT/β-CATENIN信号传导通路抑制剂的用途
US10463651B2 (en) 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-indazoles and therapeutic uses thereof
JP6355648B2 (ja) Ｗｎｔシグナル伝達経路の３−（ベンゾイミダゾール−２−イル）−インダゾール阻害剤およびそれらの治療的使用
WO2016040180A1 (en) 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2017024013A1 (en) 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
WO2017024026A1 (en) 3-(1h-indol-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
CN120712252A (zh) 包含sos1抑制剂和抗癌药物的用于治疗癌症的药物组合物
WO2020150545A1 (en) Pyrazole derivatives as modulators of the wnt/b-catenin signaling pathway
CN112020501A (zh) 5-杂芳基取代的吲唑-3-基甲酰胺类及其制备和用途
CN108349956A (zh) 吡啶酮衍生物及其作为激酶抑制剂的用途
RU2775505C2 (ru) Изохинолин-3-иловые карбоксамиды и их получение и применение
HK40005209A (en) Isoquinolin-3-yl carboxamides and preparation and use thereof
HK40005209B (en) Isoquinolin-3-yl carboxamides and preparation and use thereof

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
RJ01 Rejection of invention patent application after publication
RJ01 Rejection of invention patent application after publication

Application publication date: 20170322