BR112015007182A2 - inibidores de gdf-8 - Google Patents

inibidores de gdf-8

Info

Publication number
BR112015007182A2
BR112015007182A2 BR112015007182A BR112015007182A BR112015007182A2 BR 112015007182 A2 BR112015007182 A2 BR 112015007182A2 BR 112015007182 A BR112015007182 A BR 112015007182A BR 112015007182 A BR112015007182 A BR 112015007182A BR 112015007182 A2 BR112015007182 A2 BR 112015007182A2
Authority
BR
Brazil
Prior art keywords
inhibitors
methods
gdf
abstract
patient
Prior art date
Application number
BR112015007182A
Other languages
English (en)
Inventor
Payan Donald
Clough Jeffrey
Gelman Marina
Ding Pingyu
Singh Rajinder
Bhamidipati Somasekhar
Kinsella Todd
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=BR112015007182(A2) "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 BR112015007182A2 publication Critical patent/BR112015007182A2/pt

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
    • C07D401/02Heterocyclic 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
    • 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
    • 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)
  • Epidemiology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)

Abstract

abstract of the disclosure described are gcf-8 inhibitors of theformula (i), (i) and pharmaceutically acceptable salts thereof, wherein n, r1, r2, r5, r6, x and z are defined herein. also provided are pharmaceutical compositions comprising the same. such compounds and compositions are useful in methods for inhibiting gdf-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue. tradução do resumo resumo patente de invenção: “inibidores de gdf-8”. a presente invenção se refere a inibidores de gcf-8 da fórmula (i), (i) e sais farmaceuticamente aceitáveis dos mesmos, em que n, r1, r2, r5, r6, x e z são definidos aqui, neste requerimento de patente. a presente invenção também se refere a composições farmacêuticas compreendendo os mesmos. os compostos referidos e as composições referidas são úteis em métodos para inibir gdf-8 em uma célula e em métodos para tratar um paciente sofrendo de uma doença ou de um distúrbio, em que o paciente iria se beneficiar terapeuticamente de um aumento na massa ou na força do tecido muscular.
BR112015007182A 2012-10-05 2013-10-04 inibidores de gdf-8 BR112015007182A2 (pt)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
BR112015007182A2 true BR112015007182A2 (pt) 2017-07-04

Family

ID=49474701

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112015007182A BR112015007182A2 (pt) 2012-10-05 2013-10-04 inibidores de gdf-8

Country Status (20)

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

Families Citing this family (48)

* 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).
CR20160395A (es) 2014-02-13 2016-12-20 Incyte Corp Ciclopropilaminas como inhibidores de lsd1
KR102421235B1 (ko) 2014-02-13 2022-07-15 인사이트 코포레이션 Lsd1 저해제로서 사이클로프로필아민
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
US10233170B2 (en) * 2014-04-08 2019-03-19 Rigel Pharmaceuticals, Inc. 2,3-disubstituted pyridine compounds as TGF-beta inhibitors and methods of use
SG11201608658SA (en) 2014-04-22 2016-11-29 Univ Basel Novel manufacturing process for triazine, pyrimidine and pyridine derivatives
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
CA2953177C (en) 2014-06-23 2019-07-23 Dr. Reddy's Laboratories Ltd. Substituted imidazo[1,2-a]pyridine compounds useful for the treatment of pain
US9695167B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp 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
EP3259264B1 (en) * 2015-02-20 2022-07-27 Rigel Pharmaceuticals, Inc. Gdf-8 inhibitors
US9884868B2 (en) 2015-03-02 2018-02-06 Rigel Pharmaceuticals, Inc. TGF-beta inhibitors
MY191796A (en) 2015-04-03 2022-07-15 Incyte Corp Heterocyclic compounds as lsd1 inhibitors
HUE057041T2 (hu) 2015-07-06 2022-04-28 Alkermes Inc Hiszton deacetiláz hetero-halogén gátlói
US10421756B2 (en) 2015-07-06 2019-09-24 Rodin Therapeutics, Inc. Heterobicyclic N-aminophenyl-amides as inhibitors of histone deacetylase
CN110402244B (zh) 2015-08-12 2023-02-03 因赛特公司 Lsd1抑制剂的盐
WO2017035354A1 (en) 2015-08-26 2017-03-02 Blueprint Medicines Corporation Compounds and compositions useful for treating disorders related to ntrk
MX2018006195A (es) 2015-11-19 2018-09-05 Blueprint Medicines Corp Compuestos y composiciones utiles para el tratamiento de trastornos relacionados con ntrk.
WO2017091661A1 (en) * 2015-11-25 2017-06-01 Strovel Jeffrey William Bicyclic bet bromodomain inhibitors and uses thereof
WO2018013430A2 (en) 2016-07-12 2018-01-18 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus infection
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
EP3492461A4 (en) * 2016-07-29 2020-02-12 Shanghai Yingli Pharmaceutical Co. Ltd. NITROGEN HETEROCYCLIC AROMATIC COMPOUND, PREPARATION METHOD THEREOF, PHARMACEUTICAL COMPOSITION THEREOF AND APPLICATION THEREOF
US20180072741A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyrimidine compounds and uses thereof
WO2018049214A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer
WO2018049191A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridone derivatives as hpk1 modulators and uses thereof for the treatment of cancer
CN115819417A (zh) 2016-09-09 2023-03-21 因赛特公司 作为hpk1调节剂的吡唑并吡啶衍生物及其用于治疗癌症的用途
US11491025B2 (en) 2016-10-25 2022-11-08 Elevation Spine, Inc. Intervertebral implant and method of use
WO2018132279A1 (en) 2017-01-05 2018-07-19 Bristol-Myers Squibb Company Tgf beta receptor antagonists
PL3570834T3 (pl) 2017-01-11 2022-05-23 Alkermes, Inc. Bicykliczne inhibitory deacetylazy histonowej
US20180228786A1 (en) 2017-02-15 2018-08-16 Incyte Corporation Pyrazolopyridine compounds and uses thereof
US10631999B2 (en) 2017-06-30 2020-04-28 Elevation Spine, Inc. Systems and methods for inserting an interbody spacer and bone plate assembly
RS63343B1 (sr) 2017-08-07 2022-07-29 Alkermes Inc Biciklični inhibitori histonske deacetilaze
US10722495B2 (en) 2017-09-08 2020-07-28 Incyte Corporation Cyanoindazole compounds and uses thereof
US10745388B2 (en) 2018-02-20 2020-08-18 Incyte Corporation Indazole compounds and uses thereof
WO2019164847A1 (en) 2018-02-20 2019-08-29 Incyte Corporation Indazole compounds and uses thereof
PL3755703T3 (pl) 2018-02-20 2022-11-07 Incyte Corporation Pochodne n-(fenylo)-2-(fenylo)pirymidyno-4-karboksyamidu i związki pokrewne jako inhibitory hpk1 do leczenia nowotworu
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
EP3856348B1 (en) 2018-09-25 2024-01-03 Incyte Corporation Pyrazolo[4,3-d]pyrimidine compounds as alk2 and/or fgfr modulators
AU2020326703A1 (en) 2019-08-06 2022-02-17 Incyte Corporation Solid forms of an HPK1 inhibitor
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
WO2023131868A1 (en) * 2022-01-07 2023-07-13 Horizon Therapeutics Ireland Dac Heterocyclic inhibitors of glut9 for treatment of disease

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
JP2002534385A (ja) * 1999-01-08 2002-10-15 スミスクライン・ビーチャム・コーポレイション 新規化合物
CA2359242C (en) 1999-01-21 2009-12-08 Metamorphix, Inc. Growth differentiation factor inhibitors and uses therefor
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
WO2002014282A1 (fr) * 2000-08-11 2002-02-21 Eisai Co., Ltd. Composes 2-aminopyridine et leur utilisation comme medicaments
AU9502601A (en) * 2000-09-06 2002-03-22 Chiron Corp Inhibitors of glycogen synthase kinase 3
US7320789B2 (en) 2001-09-26 2008-01-22 Wyeth Antibody inhibitors of GDF-8 and uses thereof
JP4317752B2 (ja) * 2001-10-15 2009-08-19 イー・アイ・デュポン・ドウ・ヌムール・アンド・カンパニー 無脊椎害虫を防除するためのイミノベンゾオキサジン、イミノベンズチアジンおよびイミノキナゾリン
EP1492784A4 (en) * 2002-03-28 2006-03-29 Merck & Co Inc SUBSTITUTED 2,3-DIPHENYLPYRIDINES
FR2856684B1 (fr) 2003-06-26 2008-04-11 Sanofi Synthelabo Derives de diphenylpyridine, leur preparation et leur application en therapeutique
WO2005016862A1 (en) * 2003-08-14 2005-02-24 Asahi Kasei Pharma Corporation Substituted arylalkanoic acid derivative and use thereof
US7799772B2 (en) 2003-12-18 2010-09-21 Janssen Pharmaceutica N.V. Pyrido-and pyrimidopyrimidine derivatives as anti-profilerative agents
WO2005085227A1 (en) * 2004-03-02 2005-09-15 Smithkline Beecham Corporation Inhibitors of akt 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
WO2007076086A2 (en) * 2005-12-22 2007-07-05 Biogen Idec Ma Inc Tricyclic spiro compounds useful as transforming growth factor modulators
EP2044056B1 (en) * 2006-07-14 2012-08-22 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
AU2007315234A1 (en) * 2006-10-30 2008-05-08 Novartis Ag Heterocyclic compounds as antiinflammatory agents
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
KR101511074B1 (ko) * 2007-04-16 2015-04-13 애브비 인코포레이티드 7-치환된 인돌 Mcl-1 억제제
JP5090528B2 (ja) 2007-07-26 2012-12-05 ノバルティス アーゲー ALK4またはALK5が介在する疾患を処置するための2、3、7位置換イミダゾ[1,2−b]ピリダジン類
US8263595B2 (en) 2007-08-31 2012-09-11 Merck Serono Sa Triazolopyridine compounds and their use as ask inhibitors
WO2009032653A1 (en) * 2007-08-31 2009-03-12 Smith Kline Beecham Corporation Inhibitors of akt activity
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
JP5731399B2 (ja) * 2008-12-30 2015-06-10 チェイル インダストリーズ インコーポレイテッド 新規な有機光電素子用化合物およびこれを含む有機光電素子
WO2010094695A1 (en) 2009-02-17 2010-08-26 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
ES2667049T3 (es) * 2010-02-05 2018-05-09 Merck Patent Gmbh Derivados de heteroaril-[1,8]naftiridina
US8575203B2 (en) 2010-04-21 2013-11-05 Boehringer Ingelheim International Gmbh Chemical compounds
EA201300080A1 (ru) * 2010-07-05 2013-06-28 Мерк Патент Гмбх Дипиридильные производные, пригодные для лечения заболеваний, индуцированных киназами
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
US9878992B2 (en) 2018-01-30
CA2887203A1 (en) 2014-04-10
PE20150767A1 (es) 2015-05-15
AU2013326867A1 (en) 2015-05-21
US20140107073A1 (en) 2014-04-17
EP2903978A1 (en) 2015-08-12
ZA201503041B (en) 2017-11-29
EA201590693A1 (ru) 2015-08-31
CN104837832B (zh) 2019-04-26
US9145433B2 (en) 2015-09-29
IL238031A0 (en) 2015-05-31
KR20150072412A (ko) 2015-06-29
US9518040B2 (en) 2016-12-13
US20160052909A1 (en) 2016-02-25
SG11201502527UA (en) 2015-04-29
CN104837832A (zh) 2015-08-12
WO2014055955A1 (en) 2014-04-10
EP2903978B1 (en) 2022-12-07
JP2019048841A (ja) 2019-03-28
CL2015000851A1 (es) 2015-08-28
PH12015500719A1 (en) 2015-05-18
JP6457942B2 (ja) 2019-01-23
US20170342048A1 (en) 2017-11-30
MX2015004151A (es) 2015-07-06
JP2016500671A (ja) 2016-01-14
MA38050B1 (fr) 2017-01-31
AU2013326867B2 (en) 2018-03-08
SA515360229B1 (ar) 2015-11-25
MA38050A1 (fr) 2016-06-30
TN2015000121A1 (en) 2016-06-29

Similar Documents

Publication Publication Date Title
BR112015007182A2 (pt) inibidores de gdf-8
BR112014018990A8 (pt) Derivados de ácido benzotiazol-6-il acético e seu uso para tratamento de uma infecção
EA201490300A1 (ru) 4-имидазопиридазин-1-ил-бензамиды и 4-имидазотриазин-1-ил-бензамиды в качестве btk-ингибиторов
BR112015003188A2 (pt) Composto, composição farmacêutica, uso do composto e método para tratar uma doença ou condição mediada por rorgammat em um paciente
BR112013028430A2 (pt) composto, composição farmacêutica, método para tratar uma doença ou condição mediada por tirosina quinase do baço (syk), e, uso de uma quantidade terapeuticamente eficiente do composto
BR112012027034A2 (pt) inibidores da arginase e suas aplicações terapêuticas
BR112013006344A2 (pt) lactamas substituídas por piperdinila como moduladores de gpr119, composição farmacêutica as compreendendo, uso e processso para preparação das mesmas
EA201692506A2 (ru) Ингибиторы репликации вирусов гриппа
EA201370166A1 (ru) Содержащие диарилацетиленгидразид ингибиторы тирозинкиназы
EA201491060A1 (ru) Новые производные трифторметилоксадиазола и их применение для лечения заболевания
EA201490228A1 (ru) Новые производные трифторметилоксадиазола и их применение для лечения заболевания
UA109010C2 (en) MORPHOLINOPYRIMIDINES AND THEIR APPLICATIONS IN THERAPY
EA201591727A1 (ru) Соединения биариламида в качестве ингибиторов киназы
BR112014028954A2 (pt) amidas de n-piridinila substituídas no anel como inibidores da quinase
BR112015022197A8 (pt) uso de um composto para fabricação de um medicamento ou composição farmacêutica para o tratamento de cataplexia
MD4602B1 (ro) Inhibitori ai virusului hepatic C
UY32174A (es) Nuevos heterociclos sustituidos, composiciones farmaceuticas conteniendolos, procedimientos de preparacion y aplicaciones
EA201100030A1 (ru) Пиразольные соединения 436
UA98373C2 (ru) Конденсированные гетероциклические производные и их применение как c-met ингибиторов
BR112014007163A2 (pt) composições farmacêuticas de n-metil-2 [3 ((e)-2 piridin-2 il-vinil)-1h-indazol-6 ilsulfanil]-benzamida
EA201270492A1 (ru) Соединения для лечения дислипидемии и связанных с ней заболеваний
EA201591195A1 (ru) Новые хинолоновые производные
EA201070327A1 (ru) Катехоламиновые производные и их пролекарства
EA201490471A1 (ru) Пиридазиноновые соединения и их применение в качестве ингибиторов daao
EA201390984A1 (ru) Гетероциклические соединения, подходящие для лечения дислипидемии

Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]
B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]