AU2013326867B2 - GDF-8 inhibitors - Google Patents

GDF-8 inhibitors Download PDF

Info

Publication number
AU2013326867B2
AU2013326867B2 AU2013326867A AU2013326867A AU2013326867B2 AU 2013326867 B2 AU2013326867 B2 AU 2013326867B2 AU 2013326867 A AU2013326867 A AU 2013326867A AU 2013326867 A AU2013326867 A AU 2013326867A AU 2013326867 B2 AU2013326867 B2 AU 2013326867B2
Authority
AU
Australia
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.)
Ceased
Application number
AU2013326867A
Other languages
English (en)
Other versions
AU2013326867A1 (en
Inventor
Somasekhar Bhamidipati
Jeffrey Clough
Pingyu Ding
Marina Gelman
Todd Kinsella
Donald Payan
Rajinder Singh
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=AU2013326867(B2) "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 AU2013326867A1 publication Critical patent/AU2013326867A1/en
Application granted granted Critical
Publication of AU2013326867B2 publication Critical patent/AU2013326867B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/18—Drugs for disorders of the endocrine system of the parathyroid hormones
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26—Androgens
    • 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
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
    • 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
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • 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
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/24—Heterocyclic 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
    • C07D213/26—Radicals substituted by halogen atoms or nitro radicals
    • 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • 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
    • 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
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503—Five-membered rings
    • C07F9/65031—Five-membered rings having the nitrogen atoms in the positions 1 and 2
    • C07F9/65038—Five-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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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)
  • Neurology (AREA)
  • Nutrition Science (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Emergency Medicine (AREA)
  • Reproductive Health (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pulmonology (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)
AU2013326867A 2012-10-05 2013-10-04 GDF-8 inhibitors Ceased AU2013326867B2 (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 (2)

Publication Number Publication Date
AU2013326867A1 AU2013326867A1 (en) 2015-05-21
AU2013326867B2 true AU2013326867B2 (en) 2018-03-08

Family

ID=49474701

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2013326867A Ceased AU2013326867B2 (en) 2012-10-05 2013-10-04 GDF-8 inhibitors

Country Status (20)

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

Families Citing this family (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6457942B2 (ja) * 2012-10-05 2019-01-23 ライジェル ファーマシューティカルズ, インコーポレイテッド Gdf−8阻害剤
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
LT3105218T (lt) 2014-02-13 2019-12-10 Incyte Corp Ciklopropilaminai kaip lsd1 inhibitoriai
WO2015123424A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
JP6767875B2 (ja) * 2014-04-08 2020-10-14 ライジェル ファーマシューティカルズ, インコーポレイテッド Tgf−ベータ阻害剤としての2,3−二置換ピリジン化合物および使用方法
BR112016023811B8 (pt) 2014-04-22 2023-01-10 Piqur Therapeutics Ag Método para fabricação para derivados de triazina, pirimidina e piridina, seus intermediários e seus métodos de fabricação
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
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
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
WO2015200341A1 (en) * 2014-06-23 2015-12-30 Dr. Reddy's Laboratories Ltd. Substituted imidazo[1,2-a]pyridine compounds useful for the treatment of pain
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
WO2016007736A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyrazines as lsd1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines 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
EP3259264B1 (en) 2015-02-20 2022-07-27 Rigel Pharmaceuticals, Inc. Gdf-8 inhibitors
JP6836998B2 (ja) * 2015-03-02 2021-03-03 ライジェル ファーマシューティカルズ, インコーポレイテッド TGF−β阻害剤
EA201792205A1 (ru) 2015-04-03 2018-02-28 Инсайт Корпорейшн Гетероциклические соединения как ингибиторы lsd1
HUE057041T2 (hu) 2015-07-06 2022-04-28 Alkermes Inc Hiszton deacetiláz hetero-halogén gátlói
WO2017007755A1 (en) 2015-07-06 2017-01-12 Rodin Therapeutics, Inc. Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase
DK3334709T3 (da) 2015-08-12 2025-02-03 Incyte Holdings Corp Salte af en lsd1-hæmmer
WO2017035354A1 (en) 2015-08-26 2017-03-02 Blueprint Medicines Corporation Compounds and compositions useful for treating disorders related to ntrk
SG10201912607SA (en) * 2015-11-19 2020-02-27 Blueprint Medicines Corp Compounds and compositions useful for treating disorders related to ntrk
EP3380469B1 (en) * 2015-11-25 2022-03-16 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
AU2017296040C1 (en) 2016-07-15 2023-06-22 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
US10280164B2 (en) 2016-09-09 2019-05-07 Incyte Corporation Pyrazolopyridone compounds and uses thereof
US20180072741A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyrimidine compounds and uses thereof
US20180072718A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine compounds and uses thereof
AR109596A1 (es) 2016-09-09 2018-12-26 Incyte Corp Compuestos pirazolopiridina y sus usos
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
HRP20220223T1 (hr) 2017-01-11 2022-04-29 Alkermes, Inc. Biciklički inhibitori histon deacetilaze
WO2018152220A1 (en) 2017-02-15 2018-08-23 Incyte Corporation Pyrazolopyridine compounds and uses thereof
US10758370B2 (en) 2017-06-30 2020-09-01 Elevation Spine, Inc. Interbody spacer and bone plate assembly
EP3651762B1 (en) 2017-07-12 2024-07-03 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
US11225475B2 (en) 2017-08-07 2022-01-18 Alkermes, Inc. Substituted pyridines as inhibitors of histone deacetylase
US10722495B2 (en) 2017-09-08 2020-07-28 Incyte Corporation Cyanoindazole compounds and uses thereof
JP7270989B2 (ja) 2017-10-20 2023-05-11 ヴァンダービルト ユニバーシティー ムスカリン性アセチルコリン受容体m4のアンタゴニスト
US10752635B2 (en) 2018-02-20 2020-08-25 Incyte Corporation Indazole compounds and uses thereof
US10745388B2 (en) 2018-02-20 2020-08-18 Incyte Corporation Indazole compounds and uses thereof
DK3755703T3 (da) 2018-02-20 2022-06-27 Incyte Corp N-(phenyl)-2-(phenyl)pyrimidin-4-carboxamidderivater og relaterede forbindelser som hpk1-inhibitorer til behandling af kræft
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
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
WO2020068729A1 (en) 2018-09-25 2020-04-02 Incyte Corporation Pyrazolo[4,3-d]pyrimidine compounds as alk2 abd/or fgfr modulators
US12419865B2 (en) 2018-12-06 2025-09-23 Arisan Therapeutics Inc. Compounds for the treatment of arenavirus infection
JP7574215B2 (ja) 2019-04-29 2024-10-28 ソレント セラピューティクス,エルエルシー MRGX2の阻害薬である3-アミノ-4H-ベンゾ[e][1,2,4]チアジアジン1,1-ジオキシド誘導体
KR20220059480A (ko) 2019-08-06 2022-05-10 인사이트 코포레이션 고체 형태의 hpk1 억제제
US20230174620A1 (en) 2020-04-28 2023-06-08 Acceleron Pharma Inc. Actrii proteins and use in treating post-capillary pulmonary hypertension
EP4196473B1 (en) 2020-08-13 2024-10-02 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
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
US11912680B2 (en) 2021-12-28 2024-02-27 Empathbio, Inc. Nitric oxide releasing prodrugs of MDA and MDMA
MX2024008528A (es) * 2022-01-07 2024-07-19 Horizon Therapeutics Ireland Dac Inhibidores heterociclicos de glut9 para el tratamiento de enfermedades.
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

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000040243A1 (en) * 1999-01-08 2000-07-13 Smithkline Beecham Corporation Novel compounds
WO2001057040A1 (en) * 2000-02-03 2001-08-09 Abbott Laboratories 6,7-disubstituted-4-aminopyrido[2,3-d]pyrimidine compounds
EP1308441A1 (en) * 2000-08-11 2003-05-07 Eisai Co., Ltd. 2-aminopyridine compounds and use thereof as drugs
WO2003082191A2 (en) * 2002-03-28 2003-10-09 Merck & Co., Inc. Substituted 2,3-diphenyl pyridines
WO2005000817A2 (fr) * 2003-06-26 2005-01-06 Sanofi-Aventis Derives de diphenylpyridine, leur preparation et leur application en therapeutique
WO2005100353A1 (en) * 2004-04-15 2005-10-27 Almirall Prodesfarma, Sa Condensed pyridine derivatives useful as a28 adenosine receptor antagonists
WO2008080461A1 (en) * 2006-12-29 2008-07-10 Laboratorios Almirall, S.A. 5-phenyl-6-pyridin-4-yl-1,3-dihydro-2h-imidazo[4,5-b]pyridin-2-one derivatives useful as a2b adenosine receptor antagonists
WO2009032653A1 (en) * 2007-08-31 2009-03-12 Smith Kline Beecham Corporation Inhibitors of akt activity
WO2009115665A1 (fr) * 2008-02-07 2009-09-24 Sanofi-Aventis Dérivés de 5.6-bisaryl-2-pyr1dine-carboxamide, leur préparatio leur application en thérapeutique comme antagonistes des recepteurs a l'urotensine ii

Family Cites Families (29)

* 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
JP2003517580A (ja) 1999-01-21 2003-05-27 メタモーフイクス・インコーポレーテツド 増殖分化因子インヒビター及びそれらの用途
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
WO2002020495A2 (en) * 2000-09-06 2002-03-14 Chiron Corporation Inhibitors of glycogen synthase kinase 3
US7320789B2 (en) 2001-09-26 2008-01-22 Wyeth Antibody inhibitors of GDF-8 and uses thereof
DE60230651D1 (de) * 2001-10-15 2009-02-12 Du Pont Iminobenzoxazine, iminobenzothiazine and iminoquinazoline zur bekämpfung von wirbellosen schädlingen
KR20060079190A (ko) * 2003-08-14 2006-07-05 아사히 가세이 파마 가부시키가이샤 치환 아릴알칸산 유도체 및 그의 용도
AU2004298448B2 (en) 2003-12-18 2010-09-09 Janssen Pharmaceutica N.V. Pyrido- and pyrimidopyrimidine derivatives as anti- proliferative agents
JP2007526324A (ja) * 2004-03-02 2007-09-13 スミスクライン・ビーチャム・コーポレイション Akt活性のある阻害剤
US7777035B2 (en) 2005-06-22 2010-08-17 Chemocentryx, Inc. Azaindazole compounds and methods of use
EP1973914A2 (en) * 2005-12-22 2008-10-01 Biogen Idec MA Inc. Transforming growth factor modulators
CA2657227A1 (en) 2006-07-14 2008-01-17 Novartis Ag Pyrimidine derivatives as alk-5 inhibitors
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.
EP2121669A2 (en) * 2007-01-30 2009-11-25 Biogen Idec MA, Inc. Furanone compounds and methods of making and using the same
KR101511074B1 (ko) * 2007-04-16 2015-04-13 애브비 인코포레이티드 7-치환된 인돌 Mcl-1 억제제
KR101150581B1 (ko) 2007-07-26 2012-06-11 노파르티스 아게 유기 화합물
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
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
EP2377907B1 (en) * 2008-12-30 2014-12-03 Cheil Industries Inc. Novel compounds for an organic photoelectric device, and organic photoelectric device comprising same
EP2398797B1 (en) 2009-02-17 2013-11-06 Boehringer Ingelheim International GmbH Pyrimido[5,4-d]pyrimidine derivatives for the inhibition of tyrosine kinases
CN102762568A (zh) * 2009-12-23 2012-10-31 伊兰药品公司 作为polo样激酶的抑制剂的蝶啶酮
WO2011096196A1 (en) * 2010-02-02 2011-08-11 Oncotherapy Science, Inc. Lsd1 for target genes of cancer therapy and diagnosis
EP2531500B1 (en) * 2010-02-05 2018-01-24 Merck Patent GmbH Hetaryl-[1,8]naphthyridine derivatives
US8575203B2 (en) 2010-04-21 2013-11-05 Boehringer Ingelheim International Gmbh Chemical compounds
SG186871A1 (en) * 2010-07-05 2013-02-28 Merck Patent Gmbh Bipyridyl derivatives useful for the treatment of kinase - induced diseases
JP6457942B2 (ja) * 2012-10-05 2019-01-23 ライジェル ファーマシューティカルズ, インコーポレイテッド Gdf−8阻害剤

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000040243A1 (en) * 1999-01-08 2000-07-13 Smithkline Beecham Corporation Novel compounds
WO2001057040A1 (en) * 2000-02-03 2001-08-09 Abbott Laboratories 6,7-disubstituted-4-aminopyrido[2,3-d]pyrimidine compounds
EP1308441A1 (en) * 2000-08-11 2003-05-07 Eisai Co., Ltd. 2-aminopyridine compounds and use thereof as drugs
WO2003082191A2 (en) * 2002-03-28 2003-10-09 Merck & Co., Inc. Substituted 2,3-diphenyl pyridines
WO2005000817A2 (fr) * 2003-06-26 2005-01-06 Sanofi-Aventis Derives de diphenylpyridine, leur preparation et leur application en therapeutique
WO2005100353A1 (en) * 2004-04-15 2005-10-27 Almirall Prodesfarma, Sa Condensed pyridine derivatives useful as a28 adenosine receptor antagonists
WO2008080461A1 (en) * 2006-12-29 2008-07-10 Laboratorios Almirall, S.A. 5-phenyl-6-pyridin-4-yl-1,3-dihydro-2h-imidazo[4,5-b]pyridin-2-one derivatives useful as a2b adenosine receptor antagonists
WO2009032653A1 (en) * 2007-08-31 2009-03-12 Smith Kline Beecham Corporation Inhibitors of akt activity
WO2009115665A1 (fr) * 2008-02-07 2009-09-24 Sanofi-Aventis Dérivés de 5.6-bisaryl-2-pyr1dine-carboxamide, leur préparatio leur application en thérapeutique comme antagonistes des recepteurs a l'urotensine ii

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
DOMBROSKI, M. A. et al., BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2003), Vol. 14, No. 4, Pages 919-923 *
LIN, H. et al., BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2010), Vol. 20, No. 2, Pages 673- 678 *

Also Published As

Publication number Publication date
US9518040B2 (en) 2016-12-13
WO2014055955A1 (en) 2014-04-10
SA515360229B1 (ar) 2015-11-25
ZA201503041B (en) 2017-11-29
JP2016500671A (ja) 2016-01-14
CN104837832A (zh) 2015-08-12
JP6457942B2 (ja) 2019-01-23
EP2903978A1 (en) 2015-08-12
MA38050B1 (fr) 2017-01-31
US20140107073A1 (en) 2014-04-17
US9878992B2 (en) 2018-01-30
TN2015000121A1 (en) 2016-06-29
EA201590693A1 (ru) 2015-08-31
IL238031A0 (en) 2015-05-31
AU2013326867A1 (en) 2015-05-21
PE20150767A1 (es) 2015-05-15
CL2015000851A1 (es) 2015-08-28
KR20150072412A (ko) 2015-06-29
US20160052909A1 (en) 2016-02-25
US20170342048A1 (en) 2017-11-30
PH12015500719A1 (en) 2015-05-18
MX2015004151A (es) 2015-07-06
BR112015007182A2 (pt) 2017-07-04
MA38050A1 (fr) 2016-06-30
SG11201502527UA (en) 2015-04-29
US9145433B2 (en) 2015-09-29
CN104837832B (zh) 2019-04-26
JP2019048841A (ja) 2019-03-28
EP2903978B1 (en) 2022-12-07
CA2887203A1 (en) 2014-04-10

Similar Documents

Publication Publication Date Title
US9878992B2 (en) GDF-8 inhibitors
US10858335B2 (en) 2,3-Disubstituted pyridine compounds as TGF-β inhibitors and methods of use
AU2010336524B2 (en) Compounds and methods for kinase modulation, and indications therefor
JP4324338B2 (ja) 縮合イミダゾール化合物及び糖尿病治療薬
EP3122344B1 (en) Trka kinase inhibitors, compositions and methods thereof
DK2452940T3 (en) Azabicycloforbindelse and salt thereof
CA3142340A1 (en) Heterobicyclic inhibitors of mat2a and methods of use for treating cancer
AU2014241152A1 (en) Benzimidazolone derivatives as bromodomain inhibitors
CA3067765A1 (en) Imidazo[1,2-a]pyrazine modulators of the adenosine a2a receptor
BR112012007747B1 (pt) compostos heterocíclicos úteis como inibidores de pdk1, sua composição farmacêutica e seus usos
EP2516417A1 (en) Isoindolinone inhibitors of phosphatidylinositol 3-kinase
AU2014249003A1 (en) Novel compounds and compositions for inhibition of FASN
CA3185649A1 (en) Indole compounds as androgen receptor modulators
AU2005295091A1 (en) Substituted biaryl quinolin-4-ylamine analogues
WO2014141118A1 (en) Imidazo[4,5-c]quinoline derivatives and uses thereof

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired