PE20160521A1 - Inhibidores de autotaxina que comprenden un nucleo ciclico de anillo heteroaromatico-bencil-amida - Google Patents

Inhibidores de autotaxina que comprenden un nucleo ciclico de anillo heteroaromatico-bencil-amida

Info

Publication number
PE20160521A1
PE20160521A1 PE2016000080A PE2016000080A PE20160521A1 PE 20160521 A1 PE20160521 A1 PE 20160521A1 PE 2016000080 A PE2016000080 A PE 2016000080A PE 2016000080 A PE2016000080 A PE 2016000080A PE 20160521 A1 PE20160521 A1 PE 20160521A1
Authority
PE
Peru
Prior art keywords
methyl
cyclical
heteroaromatic
nucleus
benzyl
Prior art date
Application number
PE2016000080A
Other languages
English (en)
Inventor
Cristopher Thomson
Oliver Ross Steward
David Andrew Sandham
David William Pearce
David Beattie
Jeffrey Mckenna
Andrew Stuart Lister
Urs Baettig
Darren Mark Legrand
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20160521A1 publication Critical patent/PE20160521A1/es

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/45—Non condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/504—Pyridazines; Hydrogenated pyridazines forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • 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
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/10—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 linked by a carbon chain containing aromatic 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
    • C07D413/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/10—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 linked by a carbon chain containing aromatic rings
    • 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
    • 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

Abstract

Referida a un derivado heterociclico de formula I, donde A, B, R2, R3, R4, R5 e Y, son como se describe en la presente solicitud. Tambien esta referida a una composicion farmaceutica. Son compuestos preferidos: (S,E)-1-(2-(5-metil-1,3,4-oxadiazol-2-il)piperidin-1-il)-3-(2-((5-metil-2H-tetrazol-2-il)metil)-4-(trifluorometil)fenil)prop-2-en-1-ona, (E)-1-(4-(3-metil-1,2,4-oxadiazol-5-il)piperidin-1-il)-3-(2-((5-metil-2H-tetrazol-2-il)metil)-4-(trifluorometil)fenil)prop-2-en-1-ona, entre todos. Dichos compuestos son inhibidores de autotaxina tambien conocido como ectonucleotido pirofosfatasa / fosfodiesterasa (ENPP2)
PE2016000080A 2013-07-18 2014-07-16 Inhibidores de autotaxina que comprenden un nucleo ciclico de anillo heteroaromatico-bencil-amida PE20160521A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP13177061 2013-07-18

Publications (1)

Publication Number Publication Date
PE20160521A1 true PE20160521A1 (es) 2016-05-20

Family

ID=48793121

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016000080A PE20160521A1 (es) 2013-07-18 2014-07-16 Inhibidores de autotaxina que comprenden un nucleo ciclico de anillo heteroaromatico-bencil-amida

Country Status (25)

Country Link
US (2) US9763957B2 (es)
EP (1) EP3022202B1 (es)
JP (1) JP6424219B2 (es)
KR (1) KR20160033726A (es)
CN (1) CN105555783B (es)
AP (1) AP2016009020A0 (es)
AU (1) AU2014291711B2 (es)
BR (1) BR112016000779A8 (es)
CA (1) CA2918284A1 (es)
CL (1) CL2016000117A1 (es)
CR (1) CR20160033A (es)
CU (1) CU24355B1 (es)
EA (1) EA035256B1 (es)
ES (1) ES2742077T3 (es)
HK (1) HK1219483A1 (es)
IL (1) IL243595A0 (es)
MA (1) MA38837B1 (es)
MX (1) MX368059B (es)
PE (1) PE20160521A1 (es)
PH (1) PH12016500094A1 (es)
PL (1) PL3022202T3 (es)
PT (1) PT3022202T (es)
SG (1) SG11201600241RA (es)
TN (1) TN2016000022A1 (es)
WO (1) WO2015008230A1 (es)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA201492223A1 (ru) 2012-06-13 2015-03-31 Ф. Хоффманн-Ля Рош Аг Новые диазаспироциклоалканы и азаспироциклоалканы
CN104684915B (zh) 2012-09-25 2017-10-31 霍夫曼-拉罗奇有限公司 新型双环衍生物
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
WO2015008230A1 (en) * 2013-07-18 2015-01-22 Novartis Ag Autotaxin inhibitors comprising a heteroaromatic ring-benzyl-amide-cycle core
PE20160845A1 (es) 2013-11-26 2016-09-10 Hoffmann La Roche Nuevo octahidro-ciclobuta[1,2-c;3,4-c']dipirrol-2-ilo
JP6554481B2 (ja) 2014-03-26 2019-07-31 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ オートタキシン（ａｔｘ）及びリゾホスファチジン酸（ｌｐａ）産生の阻害剤としての縮合［１，４］ジアゼピン化合物
DK3122750T3 (da) 2014-03-26 2019-11-04 Hoffmann La Roche Bicykliske forbindelser som autotaxin (ATX)- og lysofosfatidsyre (LPA)-produktionshæmmere
AU2015240519B2 (en) 2014-04-04 2019-08-15 X-Rx, Inc. Substituted spirocyclic inhibitors of autotaxin
KR20170103960A (ko) 2015-01-20 2017-09-13 노파르티스 아게 Pet 영상화제
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
EP3302465A1 (en) 2015-06-05 2018-04-11 Vertex Pharmaceuticals Incorporated Triazoles for the treatment of demyelinating diseases
KR20180043837A (ko) * 2015-09-04 2018-04-30 에프. 호프만-라 로슈 아게 페녹시메틸 유도체
RU2018114289A (ru) 2015-09-24 2019-10-24 Ф. Хоффманн-Ля Рош Аг Бициклические соединения в качестве ингибиторов аутотаксина (atx)
KR20180053408A (ko) 2015-09-24 2018-05-21 에프. 호프만-라 로슈 아게 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서의 신규한 이환형 화합물
CR20180057A (es) 2015-09-24 2018-04-02 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de atx/ca.
CN107922412B (zh) 2015-09-24 2021-02-23 豪夫迈·罗氏有限公司 作为atx抑制剂的二环化合物
GB201617758D0 (en) * 2016-10-20 2016-12-07 Almac Discovery Limited Pharmaceutical compounds
WO2018106646A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Aminotriazoles for the treatment of demyelinating diseases
WO2018106641A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Pyrazoles for the treatment of demyelinating diseases
WO2018106643A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Heterocyclic azoles for the treatment of demyelinating diseases
WO2018167001A1 (en) 2017-03-16 2018-09-20 F. Hoffmann-La Roche Ag Heterocyclic compounds useful as dual atx/ca inhibitors
WO2018167113A1 (en) 2017-03-16 2018-09-20 F. Hoffmann-La Roche Ag New bicyclic compounds as atx inhibitors

Family Cites Families (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1016489B (it) 1974-03-18 1977-05-30 Isf Spa Inalatore
GB2041363B (en) 1979-01-19 1982-10-06 Pfizer Ltd N-benzyl-imidazoles
US6536427B2 (en) 1990-03-02 2003-03-25 Glaxo Group Limited Inhalation device
US6596260B1 (en) 1993-08-27 2003-07-22 Novartis Corporation Aerosol container and a method for storage and administration of a predetermined amount of a pharmaceutically active aerosol
US6051397A (en) 1993-11-16 2000-04-18 Max Planck Gesellschaft Zur Forderung Der Wissenschaften DNA encoding MCK-10, a novel receptor tyrosine kinase
ES2216418T3 (es) 1995-12-07 2004-10-16 Jago Research Ag Boquilla para un inhalador para la administracion de varias dosis de un polvo seco farmacologico.
BR9612410A (pt) 1996-01-03 1999-07-13 Glaxo Group Ltd Aparelho para inalação
DK0883415T3 (da) 1996-02-21 2002-08-19 Schering Corp Inhalator til pulverformigt medikament
US6207665B1 (en) 1997-06-12 2001-03-27 Schering Aktiengesellschaft Piperazine derivatives and their use as anti-inflammatory agents
ZA987383B (en) 1997-08-19 2000-02-17 Lilly Co Eli Treatment of congestive heart failure with growth hormone secretagogues.
ZA987385B (en) 1997-08-19 2000-04-18 Lilly Co Eli Growth hormone secretagogues.
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
SE9902765D0 (sv) 1999-07-21 1999-07-21 Astra Pharma Prod Novel compounds
US7069929B2 (en) 2000-02-01 2006-07-04 Quadrant Technologies Limited Dry powder inhaler
JP2005509616A (ja) 2001-10-16 2005-04-14 センジェント・セラピューティクス・インク チロシンホスファターゼに対する有機硫黄阻害剤
ES2201907B1 (es) 2002-05-29 2005-06-01 Almirall Prodesfarma, S.A. Nuevos derivados de indolilpiperidina como potentes agentes antihistaminicos y antialergicos.
CN1668614A (zh) * 2002-07-18 2005-09-14 辉瑞产品公司 用作ccr1趋化因子受体拮抗剂双环哌啶衍生物
WO2004009533A1 (en) * 2002-07-24 2004-01-29 Ptc Therapeutics, Inc. Acetylamino benzoic acid compounds and their use for nonsense suppression and the treatment of disease
JP2006096662A (ja) 2002-09-18 2006-04-13 Sumitomo Pharmaceut Co Ltd 新規６−置換ウラシル誘導体及びアレルギー性疾患の治療剤
JP2004107299A (ja) 2002-09-20 2004-04-08 Japan Energy Corp 新規１−置換ウラシル誘導体及びアレルギー性疾患の治療剤
GB0224917D0 (en) * 2002-10-25 2002-12-04 Novartis Ag Organic compounds
TW200418806A (en) * 2003-01-13 2004-10-01 Fujisawa Pharmaceutical Co HDAC inhibitor
PE20040950A1 (es) 2003-02-14 2005-01-01 Theravance Inc DERIVADOS DE BIFENILO COMO AGONISTAS DE LOS RECEPTORES ADRENERGICOS ß2 Y COMO ANTAGONISTAS DE LOS RECEPTORES MUSCARINICOS
US20040167188A1 (en) 2003-02-14 2004-08-26 Zhili Xin Protein-tyrosine phosphatase inhibitors and uses thereof
US7169797B2 (en) * 2003-02-14 2007-01-30 Abbott Laboratories Protein-tyrosine phosphatase inhibitors and uses thereof
JP2007524596A (ja) 2003-02-28 2007-08-30 トランスフォーム・ファーマシューティカルズ・インコーポレイテッド 共結晶医薬組成物
US7135575B2 (en) * 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
AU2004220225B2 (en) 2003-03-14 2010-06-17 Ono Pharmaceutical Co., Ltd. Nitrogen-containing heterocyclic derivatives and drugs containing the same as the active ingredient
JP2007503397A (ja) 2003-08-22 2007-02-22 シエーリング アクチエンゲゼルシャフト ケモカインを阻害するピペラジン誘導体、及び、この誘導体の心筋炎治療のための使用
GB2407042B (en) 2003-10-17 2007-10-24 Vectura Ltd Inhaler
JP2007521339A (ja) 2004-02-06 2007-08-02 バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト ケモカイン阻害性ピペラジン誘導体、及び多発性骨髄腫を治療するためのそれらの使用
CN101090723A (zh) 2004-02-24 2007-12-19 舍林股份公司 用于治疗子宫内膜异位症的哌嗪脲衍生物
NZ549589A (en) 2004-02-24 2009-10-30 Microdose Therapeutx Inc Synthetic jet based medicament delivery method and apparatus
GB0409236D0 (en) 2004-04-26 2004-05-26 Novartis Ag Organic compounds
GB0410712D0 (en) 2004-05-13 2004-06-16 Novartis Ag Organic compounds
GB0413960D0 (en) 2004-06-22 2004-07-28 Novartis Ag Organic compounds
JP5315611B2 (ja) 2004-06-23 2013-10-16 小野薬品工業株式会社 Ｓ１ｐ受容体結合能を有する化合物およびその用途
GT200500375A (es) 2004-12-20 2006-11-28 Derivados de piperidina y su uso como agentes antiinflamatorios
WO2006078941A2 (en) 2005-01-20 2006-07-27 Sirtris Pharmaceuticals, Inc. Novel sirtuin activating compounds and methods of use thereof
WO2006104280A1 (ja) 2005-03-31 2006-10-05 Takeda Pharmaceutical Company Limited 糖尿病の予防・治療剤
US7576106B2 (en) 2005-10-11 2009-08-18 Chemocentryx, Inc. Piperidine derivatives and methods of use
NZ576637A (en) 2006-10-25 2012-05-25 Novartis Ag Powder dispersion apparatus with and mediciment receptacles that are cut open using an elliptical arc shaped knife blade oriented to yaw between 4 and 12 degrees
US8614233B2 (en) 2007-05-29 2013-12-24 Universite De Montreal Cinnamoyl inhibitors of transglutaminase
DE102007047738A1 (de) * 2007-10-05 2009-04-09 Merck Patent Gmbh Imidazolderivate
WO2009117112A2 (en) 2008-03-21 2009-09-24 Novartis Ag Powder dispersion apparatus, method of making and using the apparatus, components that can be used on the apparatus and other devices, and various active agents
BRPI1009800A2 (pt) 2009-04-02 2016-03-15 Merck Patent Gmbh compostos heterocíclicos como inibidores de autotaxina
ES2775000T3 (es) 2009-04-02 2020-07-23 Merck Patent Gmbh Derivados de piperidina y piperazina como inhibidores de autotaxina
JP5934212B2 (ja) 2010-08-20 2016-06-15 アラーガン、インコーポレイテッドＡｌｌｅｒｇａｎ，Ｉｎｃｏｒｐｏｒａｔｅｄ 複数のプロスタグランジン受容体に作用し、一般的な抗炎症反応を生じる化合物
WO2012088438A1 (en) 2010-12-22 2012-06-28 Eutropics Pharmaceuticals, Inc. Compositions and methods useful for treating diseases
CN103619837A (zh) 2011-04-22 2014-03-05 阿勒根公司 用于治疗疼痛的脂肪酸酰胺水解酶抑制剂
BR112014001933A2 (pt) 2011-07-29 2017-02-21 Karyopharm Therapeutics Inc moduladores de transporte nuclear e usos dos mesmos
WO2015008229A1 (en) 2013-07-18 2015-01-22 Novartis Ag Autotaxin inhibitors
WO2015008230A1 (en) * 2013-07-18 2015-01-22 Novartis Ag Autotaxin inhibitors comprising a heteroaromatic ring-benzyl-amide-cycle core

Also Published As

Publication number Publication date
EA201690246A1 (ru) 2016-06-30
CU24355B1 (es) 2018-08-06
CU20160007A7 (es) 2016-07-29
US20160184318A1 (en) 2016-06-30
JP2016528212A (ja) 2016-09-15
SG11201600241RA (en) 2016-02-26
JP6424219B2 (ja) 2018-11-14
PT3022202T (pt) 2019-09-03
EP3022202B1 (en) 2019-05-15
IL243595A0 (en) 2016-02-29
WO2015008230A1 (en) 2015-01-22
BR112016000779A2 (pt) 2017-07-25
MX368059B (es) 2019-09-18
CN105555783A (zh) 2016-05-04
MA38837A1 (fr) 2018-03-30
MA38837B1 (fr) 2018-10-31
AP2016009020A0 (en) 2016-02-29
PL3022202T3 (pl) 2019-10-31
US10183025B2 (en) 2019-01-22
ES2742077T3 (es) 2020-02-13
EA035256B1 (ru) 2020-05-21
HK1219483A1 (zh) 2017-04-07
CA2918284A1 (en) 2015-01-22
CR20160033A (es) 2016-04-01
EP3022202A1 (en) 2016-05-25
US9763957B2 (en) 2017-09-19
CL2016000117A1 (es) 2016-07-22
US20180021345A1 (en) 2018-01-25
AU2014291711B2 (en) 2017-02-02
TN2016000022A1 (en) 2017-07-05
PH12016500094A1 (en) 2016-04-18
BR112016000779A8 (pt) 2020-01-07
CN105555783B (zh) 2017-12-01
MX2016000735A (es) 2016-10-21
AU2014291711A1 (en) 2016-02-11
KR20160033726A (ko) 2016-03-28

Similar Documents

Publication Publication Date Title
PE20160521A1 (es) Inhibidores de autotaxina que comprenden un nucleo ciclico de anillo heteroaromatico-bencil-amida
PE20141686A1 (es) Compuestos de piperazina alquilados como inhibidores de actividad btk
CO2017002714A2 (es) Ácido 4-(3-fluoro-3-(2-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)etil)pirrolidin-1-il)-3-(3-(2-metoxietoxi)fenil)butanoico, o una sal del mismo
PE20170695A1 (es) Compuestos de indol carboxamida utiles como inhibidores de cinasas
PE20170939A1 (es) Pirimidinonas como inhibidores del factor xia
UY35998A (es) 1-(3-(tert-BUTIL)1-(p-TOLIL)-1H-PIRAZOL-5-IL)-3-(4-((2-((6-ETILPIRAZIN-2-IL)AMINO)PIRIDIN-4-IL)METOXI)NAFTALEN-1-IL) UREA Y SUS SALES DERIVADAS FARMACÉUTICAMENTE ACEPTABLES, COMO INHIBIDORES DE P38 M AP QUINASA
PE20151001A1 (es) Alcoxipirazoles como activadores de guanilato ciclasa soluble
PE20141167A1 (es) Piridopirazinas sustituidas como inhibidores novedosos de ptk
AR072952A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso
PE20190395A1 (es) Pirimidin-2-ilamino-1h-pirazoles como inhibidores de lrrk2 para el uso en el tratamiento de trastornos neurodegenerativos
PE20170004A1 (es) Inhibidores de biaril cinasa
EA201691997A1 (ru) Производные 2,4-тиазолинидона в лечении расстройств центральной нервной системы
UA111725C2 (uk) Кристалічний (r)-(e)-2-(4-(2-(5-(1-(3,5-дихлорпіридин-4-іл)етоксі)-1h-індазол-3-іл)вініл)-1h-піразол-1-іл)етанол
CR20150045A (es) Inhibidores de hepatitis c
PE20161368A1 (es) Inhibidores de diacilglicerol aciltranferasa 2
PH12015501955A1 (en) Heterocyclic compounds and use thereof as modulators of type iii receptor tyrosine kinases
GEP201706778B (en) Pyridinyl and fused pyridinyl triazolone derivatives
NI201500134A (es) Derivados de 2-((4-amino-3-(3-flúor-5-hidroxifenil)-1h-pirazolo[3,4-d]pirimidin-1-il) metil)-3-(2-(trifluorometil)bencil)quinazolina-4(3h)-ona y su uso como inhibidores de fosfoinositida 3-quinasas
PE20170946A1 (es) 2-amino-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1
PE20160839A1 (es) Derivados de 4-azaindol
CL2016001172A1 (es) Nuevos inhibidores de dgat2.
PE20151535A1 (es) Derivado de dihidropiridazin-3,5-diona
EA201600436A1 (ru) Кристаллическая солевая форма (s)-(2-(6-хлор-7-метил-1h-бензо[d]имидазол-2-ил)-2-метилпирролидин-1-ил)(5-метокси-2-(2h-1,2,3-триазол-2-ил)фенил)метанона и ее применение в качестве антагонистов орексинового рецептора
PE20190204A1 (es) [8-(fenilsulfonil)-3,8-diazabiciclo[3.2.1]oct-3-il](1h-1,2,3-triazol-4-il)metanonas
PE20161557A1 (es) Derivados aminoester