CA2887203A1 - 2,3-(hetero)aryl substituted pyridinyl compounds and their use as gdf-8 inhibitors - Google Patents

2,3-(hetero)aryl substituted pyridinyl compounds and their use as gdf-8 inhibitors Download PDF

Info

Publication number
CA2887203A1
CA2887203A1 CA2887203A CA2887203A CA2887203A1 CA 2887203 A1 CA2887203 A1 CA 2887203A1 CA 2887203 A CA2887203 A CA 2887203A CA 2887203 A CA2887203 A CA 2887203A CA 2887203 A1 CA2887203 A1 CA 2887203A1
Authority
CA
Canada
Prior art keywords
pyridin
fluoro
methylphenyl
pyridine
imidazo
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
CA2887203A
Other languages
English (en)
French (fr)
Inventor
Somasekhar Bhamidipati
Marina Gelman
Pingyu Ding
Rajinder Singh
Jeffrey Clough
Todd Kinsella
Donald Payan
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.)
Rigel Pharmaceuticals Inc
Original Assignee
Rigel Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=49474701&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2887203(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Rigel Pharmaceuticals Inc filed Critical Rigel Pharmaceuticals Inc
Publication of CA2887203A1 publication Critical patent/CA2887203A1/en
Pending legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/02Nutrients, e.g. vitamins, minerals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/18Drugs for disorders of the endocrine system of the parathyroid hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26Androgens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/44Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/26Radicals substituted by halogen atoms or nitro radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503Five-membered rings
    • C07F9/65031Five-membered rings having the nitrogen atoms in the positions 1 and 2
    • C07F9/65038Five-membered rings having the nitrogen atoms in the positions 1 and 2 condensed with carbocyclic rings or carbocyclic ring systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Nutrition Science (AREA)
  • Neurology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Emergency Medicine (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Epidemiology (AREA)
CA2887203A 2012-10-05 2013-10-04 2,3-(hetero)aryl substituted pyridinyl compounds and their use as gdf-8 inhibitors Pending CA2887203A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261710449P 2012-10-05 2012-10-05
US61/710,449 2012-10-05
PCT/US2013/063585 WO2014055955A1 (en) 2012-10-05 2013-10-04 Gdf-8 inhibitors

Publications (1)

Publication Number Publication Date
CA2887203A1 true CA2887203A1 (en) 2014-04-10

Family

ID=49474701

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2887203A Pending CA2887203A1 (en) 2012-10-05 2013-10-04 2,3-(hetero)aryl substituted pyridinyl compounds and their use as gdf-8 inhibitors

Country Status (20)

Country Link
US (3) US9145433B2 (cg-RX-API-DMAC7.html)
EP (1) EP2903978B1 (cg-RX-API-DMAC7.html)
JP (2) JP6457942B2 (cg-RX-API-DMAC7.html)
KR (1) KR20150072412A (cg-RX-API-DMAC7.html)
CN (1) CN104837832B (cg-RX-API-DMAC7.html)
AU (1) AU2013326867B2 (cg-RX-API-DMAC7.html)
BR (1) BR112015007182A2 (cg-RX-API-DMAC7.html)
CA (1) CA2887203A1 (cg-RX-API-DMAC7.html)
CL (1) CL2015000851A1 (cg-RX-API-DMAC7.html)
EA (1) EA201590693A1 (cg-RX-API-DMAC7.html)
IL (1) IL238031A0 (cg-RX-API-DMAC7.html)
MA (1) MA38050B1 (cg-RX-API-DMAC7.html)
MX (1) MX2015004151A (cg-RX-API-DMAC7.html)
PE (1) PE20150767A1 (cg-RX-API-DMAC7.html)
PH (1) PH12015500719A1 (cg-RX-API-DMAC7.html)
SA (1) SA515360229B1 (cg-RX-API-DMAC7.html)
SG (1) SG11201502527UA (cg-RX-API-DMAC7.html)
TN (1) TN2015000121A1 (cg-RX-API-DMAC7.html)
WO (1) WO2014055955A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA201503041B (cg-RX-API-DMAC7.html)

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2015004151A (es) * 2012-10-05 2015-07-06 Rigel Pharmaceuticals Inc Inhibidores del factor de diferenciacion de crecimiento-8 (gdf-8).
ME03654B (me) 2014-02-13 2020-07-20 Incyte Corp Ciklopropilamini kao lsd1 inhibitori
PE20161384A1 (es) 2014-02-13 2016-12-28 Incyte Corp Ciclopropilaminas como inhibidores de lsd 1
WO2015123437A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
ES2759240T3 (es) * 2014-04-08 2020-05-08 Rigel Pharmaceuticals Inc Compuestos de piridina 2,3-disustituidos como inhibidores de TGF-beta
JP6513105B2 (ja) 2014-04-22 2019-05-15 ウニヴェルズィテート バーゼル トリアジン、ピリミジン及びピリジン誘導体の新規製造方法
CN103965192B (zh) * 2014-05-20 2016-01-13 定陶县友帮化工有限公司 一种6-氯咪唑并[1,2-a]吡啶-3-甲酸的合成方法
CN103965191A (zh) * 2014-05-20 2014-08-06 定陶县友帮化工有限公司 一种6-溴咪唑并[1,2-a]吡啶-3-甲酸的合成方法
CN103965190A (zh) * 2014-05-20 2014-08-06 定陶县友帮化工有限公司 一种咪唑并[1,2-a]吡啶-3-甲酸的合成方法
US9394305B2 (en) * 2014-06-23 2016-07-19 Dr. Reddy's Laboratories Ltd. Substituted imidazo[1,2-a]pyridine compounds as tropomyosin receptor kinase a (TrkA) inhibitors
US9695168B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007736A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyrazines as lsd1 inhibitors
CN104402881B (zh) * 2014-11-05 2016-04-20 定陶县友帮化工有限公司 一种3-醛基-6-溴咪唑并[1,2-a]吡啶-8-甲酸乙酯的合成方法
CN107531666A (zh) * 2015-02-20 2018-01-02 里格尔药品股份有限公司 Gdf‑8抑制剂
US9884868B2 (en) 2015-03-02 2018-02-06 Rigel Pharmaceuticals, Inc. TGF-beta inhibitors
MX373154B (es) 2015-04-03 2020-04-22 Incyte Holdings Corp Compuestos heterocíclicos como inhibidores de demetilasa 1 específica de lisina (lsd1).
US10421756B2 (en) 2015-07-06 2019-09-24 Rodin Therapeutics, Inc. Heterobicyclic N-aminophenyl-amides as inhibitors of histone deacetylase
US20180194769A1 (en) 2015-07-06 2018-07-12 Rodin Therapeutics, Inc. Hetero-halo inhibitors of histone deacetylase
MX389824B (es) 2015-08-12 2025-03-20 Incyte Holdings Corp Sales de un inhibidor de dimetilasa 1 especifica para lisina (lsd1).
KR20180043810A (ko) 2015-08-26 2018-04-30 블루프린트 메디신즈 코포레이션 Ntrk에 관련된 장애 치료용으로 유용한 화합물 및 조성물
SG10201912607SA (en) 2015-11-19 2020-02-27 Blueprint Medicines Corp Compounds and compositions useful for treating disorders related to ntrk
ES3011058T3 (en) * 2015-11-25 2025-04-07 Convergene Llc Bicyclic bet bromodomain inhibitors and uses thereof
US11352328B2 (en) 2016-07-12 2022-06-07 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus
US10722558B2 (en) 2016-07-15 2020-07-28 Acceleron Pharma Inc. Compositions and methods for treating pulmonary hypertension
US20190292179A1 (en) 2016-07-21 2019-09-26 Bristol-Myers Squibb Company TGF Beta RECEPTOR ANTAGONISTS
US11466003B2 (en) * 2016-07-29 2022-10-11 Shanghai Yingli Pharmaceutical Co., Ltd Nitrogenous heterocyclic aromatic compound, preparation method therefor, pharmaceutical composition thereof, and application thereof
US20180072718A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine compounds and uses thereof
WO2018049191A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridone derivatives as hpk1 modulators and uses thereof for the treatment of cancer
AU2017322427B2 (en) 2016-09-09 2021-12-23 Incyte Corporation Pyrazolopyridine derivatives as HPK1 modulators and uses thereof for the treatment of cancer
WO2018049152A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyrimidine derivatives as hpk1 modulators and uses thereof for the treatment of cancer
US11491025B2 (en) 2016-10-25 2022-11-08 Elevation Spine, Inc. Intervertebral implant and method of use
US10961239B2 (en) 2017-01-05 2021-03-30 Bristol-Myers Squibb Company TGF beta receptor antagonists
HUE057849T2 (hu) 2017-01-11 2022-06-28 Alkermes Inc Hiszton deacetiláz biciklusos gátlói
WO2018152220A1 (en) 2017-02-15 2018-08-23 Incyte Corporation Pyrazolopyridine compounds and uses thereof
WO2019006476A1 (en) 2017-06-30 2019-01-03 Elevation Spine, Inc. INTERVERTEBRAL SPACER AND BONE PLATE ASSEMBLY, INSTRUMENTATION AND METHODS
HUE058799T2 (hu) 2017-08-07 2022-09-28 Alkermes Inc Hiszton-deacetiláz biciklusos inhibitorai
WO2019051199A1 (en) 2017-09-08 2019-03-14 Incyte Corporation 6-CYANO-INDAZOLE COMPOUNDS AS HEMATOPOIETIC PROGENITOR KINASE 1 (HPK1) MODULATORS
WO2019164847A1 (en) 2018-02-20 2019-08-29 Incyte Corporation Indazole compounds and uses thereof
US10745388B2 (en) 2018-02-20 2020-08-18 Incyte Corporation Indazole compounds and uses thereof
EP3755703B1 (en) 2018-02-20 2022-05-04 Incyte Corporation N-(phenyl)-2-(phenyl)pyrimidine-4-carboxamide derivatives and related compounds as hpk1 inhibitors for treating cancer
US11299473B2 (en) 2018-04-13 2022-04-12 Incyte Corporation Benzimidazole and indole compounds and uses thereof
US10899755B2 (en) 2018-08-08 2021-01-26 Incyte Corporation Benzothiazole compounds and uses thereof
WO2020047198A1 (en) 2018-08-31 2020-03-05 Incyte Corporation Salts of an lsd1 inhibitor and processes for preparing the same
TW202028207A (zh) 2018-09-25 2020-08-01 美商英塞特公司 吡唑并嘧啶化合物及其用途
US12419865B2 (en) 2018-12-06 2025-09-23 Arisan Therapeutics Inc. Compounds for the treatment of arenavirus infection
MA55804A (fr) 2019-04-29 2022-04-06 Solent Therapeutics Llc Dérivés de 1,1-dioxyde de 3-amino-4h-benzo[e][1,2,4]thiadiazine en tant qu'inhibiteurs de mrgx2
KR20220059480A (ko) 2019-08-06 2022-05-10 인사이트 코포레이션 고체 형태의 hpk1 억제제
CN112225736B (zh) * 2020-11-12 2022-04-15 山东省科学院菏泽分院 一种6-溴咪唑并[1.2-a]吡啶-3-甲醛的制备方法
US12492178B2 (en) 2021-09-01 2025-12-09 Empathbio, Inc. Stable polymorph of R-MDMA HCl
WO2023129958A2 (en) 2021-12-28 2023-07-06 ATAI Life Sciences AG Nitric oxide releasing prodrugs of mda and mdma
AU2023205378A1 (en) * 2022-01-07 2024-07-04 Horizon Therapeutics Ireland Dac Heterocyclic inhibitors of glut9 for treatment of disease
KR102879073B1 (ko) * 2022-09-02 2025-10-31 단국대학교 천안캠퍼스 산학협력단 트리플루오로메틸페닐 티아디아진계 화합물 및 이를 유효성분으로 포함하는 근감소증 예방 또는 치료용 조성물
CN117049961A (zh) * 2023-08-16 2023-11-14 苏州君叶生物医药科技有限公司 一种酵母脱氢酶抑制剂的衍生物及其合成方法

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW458977B (en) * 1997-04-16 2001-10-11 Abbott Lab 6,7-disubstituted-4-aminopyrido[2,3-D] pyrimidine compounds
AU2408300A (en) 1999-01-08 2000-07-24 Smithkline Beecham Corporation Novel compounds
DE60027135T2 (de) 1999-01-21 2007-01-11 Metamorphix, Inc. Inhibitoren für wachstumdifferenzierungsfaktor und ihre anwendungen
JP2001081087A (ja) * 1999-09-13 2001-03-27 Sankio Chemical Co Ltd 新規な2−(2−ピリジル)ピリミジン誘導体
WO2001057040A1 (en) 2000-02-03 2001-08-09 Abbott Laboratories 6,7-disubstituted-4-aminopyrido[2,3-d]pyrimidine compounds
MXPA03001136A (es) * 2000-08-11 2003-06-24 Eisai Co Ltd Compuesto de 2-aminopiridina y uso medico del mismo.
AU2001295026B2 (en) * 2000-09-06 2008-04-03 Novartis Vaccines And Diagnostics, Inc. Inhibitors of glycogen synthase kinase 3
US7320789B2 (en) 2001-09-26 2008-01-22 Wyeth Antibody inhibitors of GDF-8 and uses thereof
US7148217B2 (en) * 2001-10-15 2006-12-12 E. I. Du Pont De Nemours And Company Iminobenzoxazines, iminobenzthiazines and iminoquinazolines for controlling invertebrate pests
JP2005531520A (ja) * 2002-03-28 2005-10-20 メルク エンド カムパニー インコーポレーテッド 置換2,3−ジフェニルピリジン類
FR2856684B1 (fr) * 2003-06-26 2008-04-11 Sanofi Synthelabo Derives de diphenylpyridine, leur preparation et leur application en therapeutique
EP1660427A4 (en) * 2003-08-14 2006-12-20 Asahi Kasei Pharma Corp SUBSTITUTED ARYLALKANIC DERIVATIVE AND ITS USE
UA83881C2 (en) 2003-12-18 2008-08-26 Янссен Фармацевтика Н.В. Pyrido- and pyrimidopyrimidine derivatives as anti-proliferative agents
EP1720855A4 (en) * 2004-03-02 2008-12-17 Smithkline Beecham Corp HEMMER OF ACT ACTIVITY
ES2241496B1 (es) * 2004-04-15 2006-12-01 Almirall Prodesfarma, S.A. Nuevos derivados de piridina.
US7777035B2 (en) 2005-06-22 2010-08-17 Chemocentryx, Inc. Azaindazole compounds and methods of use
US20100166819A1 (en) * 2005-12-22 2010-07-01 Biogen Idec Ma Inc. A Corporation Transforming Growth Factor Modulators
AR061974A1 (es) 2006-07-14 2008-08-10 Novartis Ag Derivados de pirimidina como inhibidores de alk, composiciones farmaceuticas y procesos de obtencion
FR2904827B1 (fr) * 2006-08-11 2008-09-19 Sanofi Aventis Sa Derives de 5,6-bisaryl-2-pyridine-carboxamide, leur preparation et leur application en therapeutique comme antiganistes des recepteurs a l'urotensine ii
BRPI0718266A2 (pt) 2006-10-30 2014-01-07 Novartis Ag Compostos heterocíclicos como agentes anti-inflamatórios.
ES2303776B1 (es) * 2006-12-29 2009-08-07 Laboratorios Almirall S.A. Derivados de 5-fenil-6-piridin-4-il-1,3-dihidro-2h-imidazo(4,5-b)piridin-2-ona utiles como antagonistas del receptor de adenosina a2b.
EP2121669A2 (en) * 2007-01-30 2009-11-25 Biogen Idec MA, Inc. Furanone compounds and methods of making and using the same
JP5496877B2 (ja) * 2007-04-16 2014-05-21 アッヴィ・インコーポレイテッド 7−置換インドールMcl−1阻害薬
PE20090506A1 (es) 2007-07-26 2009-05-28 Novartis Ag DERIVADOS DE IMIDAZO-[1,2-b]-PIRIDAZIN COMO INHIBIDORES DE ALK5 Y/O ALK4
WO2009032653A1 (en) * 2007-08-31 2009-03-12 Smith Kline Beecham Corporation Inhibitors of akt activity
CA2691448A1 (en) 2007-08-31 2009-03-05 Dominique Swinnen Triazolopyridine compounds and their use as ask inhibitors
WO2009051705A1 (en) * 2007-10-18 2009-04-23 Merck & Co., Inc. Substituted 1,2,4-oxadiazoles and analogs thereof as cb2 receptor modulators, useful in the treatment of pain, respiratory and non-respiratory diseases
FR2927330B1 (fr) * 2008-02-07 2010-02-19 Sanofi Aventis Derives de 5,6-bisaryl-2-pyridine-carboxamide, leur preparation et leur application en therapeutique comme antagonistes des recepteurs a l'urotensine ii
KR101015858B1 (ko) * 2008-06-26 2011-02-23 제일모직주식회사 유기 화합물, 및 이를 포함하는 유기 광전 소자
US8501940B2 (en) * 2008-07-15 2013-08-06 Hoffmann-La Roche Inc. Tetrahydrocinnoline derivatives
CN102272262B (zh) * 2008-12-30 2014-09-10 第一毛织株式会社 有机光电装置用新化合物和包括该化合物的有机光电装置
EP2398797B1 (en) 2009-02-17 2013-11-06 Boehringer Ingelheim International GmbH Pyrimido[5,4-d]pyrimidine derivatives for the inhibition of tyrosine kinases
EP2516441B1 (en) * 2009-12-23 2015-01-21 Elan Pharmaceuticals Inc. Pteridinones as inhibitors of polo-like kinase
WO2011096196A1 (en) * 2010-02-02 2011-08-11 Oncotherapy Science, Inc. Lsd1 for target genes of cancer therapy and diagnosis
WO2011095196A1 (en) * 2010-02-05 2011-08-11 Merck Patent Gmbh Hetaryl-[1,8]naphthyridine derivatives
US8575203B2 (en) 2010-04-21 2013-11-05 Boehringer Ingelheim International Gmbh Chemical compounds
EP2590946B1 (en) * 2010-07-05 2015-02-18 Merck Patent GmbH Bipyridyl derivatives useful for the treatment of kinase-induced diseases
MX2015004151A (es) * 2012-10-05 2015-07-06 Rigel Pharmaceuticals Inc Inhibidores del factor de diferenciacion de crecimiento-8 (gdf-8).

Also Published As

Publication number Publication date
EP2903978B1 (en) 2022-12-07
WO2014055955A1 (en) 2014-04-10
CN104837832B (zh) 2019-04-26
US20170342048A1 (en) 2017-11-30
KR20150072412A (ko) 2015-06-29
ZA201503041B (en) 2017-11-29
EP2903978A1 (en) 2015-08-12
MA38050B1 (fr) 2017-01-31
US20140107073A1 (en) 2014-04-17
CN104837832A (zh) 2015-08-12
US9518040B2 (en) 2016-12-13
AU2013326867B2 (en) 2018-03-08
US9145433B2 (en) 2015-09-29
EA201590693A1 (ru) 2015-08-31
PH12015500719A1 (en) 2015-05-18
JP2019048841A (ja) 2019-03-28
US9878992B2 (en) 2018-01-30
TN2015000121A1 (en) 2016-06-29
AU2013326867A1 (en) 2015-05-21
IL238031A0 (en) 2015-05-31
MA38050A1 (fr) 2016-06-30
BR112015007182A2 (pt) 2017-07-04
MX2015004151A (es) 2015-07-06
JP6457942B2 (ja) 2019-01-23
JP2016500671A (ja) 2016-01-14
PE20150767A1 (es) 2015-05-15
SA515360229B1 (ar) 2015-11-25
SG11201502527UA (en) 2015-04-29
CL2015000851A1 (es) 2015-08-28
US20160052909A1 (en) 2016-02-25

Similar Documents

Publication Publication Date Title
US10858335B2 (en) 2,3-Disubstituted pyridine compounds as TGF-β inhibitors and methods of use
EP2903978B1 (en) Gdf-8 inhibitors
AU2010341573B2 (en) Isoindolinone inhibitors of phosphatidylinositol 3-kinase
CA2733533C (en) Hedgehog pathway modulators
EP3122344B1 (en) Trka kinase inhibitors, compositions and methods thereof
JP2024516317A (ja) Shp2リン酸化酵素阻害剤の調製と応用
AU2014241152A1 (en) Benzimidazolone derivatives as bromodomain inhibitors
AU2006311914A1 (en) Heterocyclic compounds as tyrosine kinase modulators
TW201127385A (en) N-containing heteroaryl derivatives as JAK3 kinase inhibitors
JP2018528193A (ja) インドール誘導体、その調製方法および医薬におけるその使用
WO2013148603A1 (en) Cinnoline derivatives as as btk inhibitors
CN115340559A (zh) Shp2磷酸酶杂环类抑制剂的制备及其应用
CN112912142B (zh) 作为腺苷受体拮抗剂的5-氮杂吲唑衍生物
AU2005295091A1 (en) Substituted biaryl quinolin-4-ylamine analogues
CN115340561A (zh) Shp2磷酸酶稠环类抑制剂的制备及其应用
WO2025113625A1 (zh) 作为pkmyt1抑制剂的杂芳环和杂双环化合物及其应用

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20181003

EEER Examination request

Effective date: 20181003

EEER Examination request

Effective date: 20181003

EEER Examination request

Effective date: 20181003

EEER Examination request

Effective date: 20181003

EEER Examination request

Effective date: 20181003