DK2800748T3 - Cykliske amidderivater som inhibitorer af 11-beta-hydroxysteroid-dehydrogenase og anvendelser deraf - Google Patents
Cykliske amidderivater som inhibitorer af 11-beta-hydroxysteroid-dehydrogenase og anvendelser deraf Download PDFInfo
- Publication number
- DK2800748T3 DK2800748T3 DK12846788.3T DK12846788T DK2800748T3 DK 2800748 T3 DK2800748 T3 DK 2800748T3 DK 12846788 T DK12846788 T DK 12846788T DK 2800748 T3 DK2800748 T3 DK 2800748T3
- Authority
- DK
- Denmark
- Prior art keywords
- compound
- group
- optionally substituted
- synthesis
- nmr
- Prior art date
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
- C07D401/06—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 only aliphatic carbon atoms
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- 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
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- A61P5/48—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
-
- 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
- C07D401/08—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 alicyclic 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
- 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
- C07D403/06—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 only aliphatic carbon atoms
-
- 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
- C07D405/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
- C07D413/06—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 only aliphatic carbon atoms
-
- 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
- C07D417/06—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 only aliphatic carbon atoms
-
- 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
- C07D417/12—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 chain containing hetero atoms as chain links
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Obesity (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Endocrinology (AREA)
- Psychiatry (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Immunology (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
Claims (14)
- CYKLISKE AMIDDERIVATERSOM INHIBITORER AF 11-BETA-HYDROXYSTEROID-DEHYDROGENASE OG ANVENDELSER DERAF1. Forbindelse med formlen (I):hvor: hvert R1 og R1a uafhængigt af hinanden er valgt fra gruppen bestående af H, methyl, CONHC(CH3)3, OH, C02H, C02CH3, C02CH2CH3, phenyl, CH2OH, CN og OCH3. eller hvilke som helst to R1 på nabostillede carbonatomer kan forbindes til dannelse af en cyklisk del, eller hvilke som helst to R1 på det samme carbon tilsammen kan danne en gruppe med formlen =0 Ar er en valgfrit substitueret Ci-Cis-heteroarylgruppe, der er valgt fra gruppen bestående af:hvor hvert R7 uafhængigt af hinanden er valgt fra gruppen bestående af H, halogen, OH, NO2, CN, SH, NH2, CF3, OCF3, valgfrit substitueret Ci-Ci2-alkyl, valgfrit substitueret Ci-Ci2-halogenalkyl, valgfrit substitueret C2-Ci2-alkenyl, valgfrit substitueret C2-Ci2-alkynyl, valgfrit substitueret C2-Ci2-heteroalkyl, valgfrit substitueret C3-Ci2-cycloalkyl, valgfrit substitueret C3-Ci2-cycloalkenyl, valgfrit substitueret C2-Ci2-heterocycloalkyl, valgfrit substitueret C2-C12-heterocycloalkenyl, valgfrit substitueret C6-Cis-aryl, valgfrit substitueret C1-C18-heteroaryl, valgfrit substitueret Ci-Ci2-alkyloxy, valgfrit substitueret C2-C12-alkenyloxy, valgfrit substitueret C2-Ci2-alkynyloxy, valgfrit substitueret C2-C10-heteroalkyloxy, valgfrit substitueret C3-Ci2-cycloalkyloxy, valgfrit substitueret C3-Ci2-cycloalkenyloxy, valgfrit substitueret C2-Ci2-heterocycloalkyloxy, valgfrit substitueret C2-Ci2-heterocycloalkenyloxy, valgfrit substitueret C6-Ci8-aryloxy, valgfrit substitueret Ci-Cis-heteroaryloxy, valgfrit substitueret Ci-Ci2-alkylamino, SR9, SO3H, S02NR9R1°, SO2R9, SONR9R10SOR9, COR9, COOH, COOR9, CONR9R10, NR9COR10, NR9COOR10, NR9S02R1°, NR9CONR9R10, NR9R10 og acyl; hvor R8 er er valgt fra gruppen bestående af H, valgfrit substitueret Ci-Ci2-alkyl, valgfrit substitueret C2-Ci2-alkenyl, valgfrit substitueret C2-Ci2-alkynyl, valgfrit substitueret C2-Ci2-heteroalkyl, valgfrit substitueret C3-Ci2-cycloalkyl, valgfrit substitueret C2-Ci2-heterocycloalkyl, valgfrit substitueret C6-Cis-aryl, valgfrit substitueret Ci-Cie-heteroaryl, S03H, S02NR9R1°, SO2R9, SONR9R10, SOR9, COR9, COOH, COOR9 og CONR9R10; hvor hvert R9 og R10 uafhængigt af hinanden er valgt fra gruppen bestående af H, valgfrit substitueret Ci-Ci2-alkyl, valgfrit substitueret C2-Cio-heteroalkyl, valgfrit substitueret Ci-Ci2-halogenalkyl, valgfrit substitueret C3-Ci2-cycloalkyl, valgfrit substitueret C6-Ci8-aryl og valgfrit substitueret Ci-Ci8-heteroaryl; e er et helt tal, der er valgt fra gruppen bestående af 0, 1,2,3 og 4; f er et helt tal, der er valgt fra gruppen bestående af 0,1,2 og 3; A er -CRaRb-; B er en gruppe med formlen -(CRcRd)n-; hvor hvert Ra, Rb, Rc og Rd uafhængigt af hinanden er valgt fra gruppen bestående af H, halogen, OH, NO2, CN, SH, NH2, CF3, OCF3, Ci-Ci2-alkyl, C2-Cio-heteroalkyl Ci-Ci2-halogenalkyl, C3-Ci2-cycloalkyl, C6-Ci8-aryl, C1-C18-heteroaryl; SR2, S03H, S02NR2R3, SO2R2, SONR2R3, SOR2, COR2, COOH, COOR2, CONR2R3, NR2COR3, NR2COOR3, NR2S02R3, NR2CONR2R2, NR2R3 og acyl, hvor hvert R2 og R3 uafhængigt af hinanden er valgt fra gruppen bestående af H, Ci-Ci2-alkyl, C2-Cio-heteroalkyl, Ci-Ci2-halogenalkyl, C3-Ci2-cycloalkyl, Ce-Cie-aryl og Ci-Ci8-heteroaryl; W1 og W2 er er valgt således, at det ene er N, og det andet er (CR12), bindingen fra carbonylcarbon er forbundet med enten W1 eller W2, som er N, Der O eller (CR12), n er et helt tal, der er valgt fra gruppen bestående af 0, 1 og 2; a er et helt tal, der er valgt fra gruppen bestående af 0, 1 og 2, 3; b er et helt tal, der er valgt fra gruppen bestående af 0, 1, 2, 3, 4, 5, 6, 7 og 8, c er 1; eller et farmaceutisk acceptabelt salt deraf.
- 2. Forbindelse ifølge krav 1, hvor D er (CR12).
- 3. Forbindelse ifølge krav 1 eller 2, hvor B er CH2.
- 4. Forbindelse ifølge et hvilket som helst af kravene 1 til 3, hvor Ra og Rb er forskellige.
- 5. Forbindelse ifølge krav 1 med formlen:hvor Ar, Ra, Rb, R1, R1a, a og b er som defineret i krav 1.
- 6. Forbindelse ifølge krav 5, hvor ét af Ra og Rb er H, og det andet er valgfrit substitueret alkyl.
- 7. Forbindelse ifølge krav 1, hvor R7-substituenten er lokaliseret i 4- eller 5-positionen af den seksleddede ring.
- 8. Forbindelse ifølge krav 1, hvor R7 er valgt fra gruppen bestående af CH3, CH2CH3, CH2CH2CH3, CH(CH3)2, (CH2)3CH3, Cl, Br, F, I, OH, NO2, NH2, CN, S03H, OCH3, OCH2CH2CH3, CF3 og OCF3.
- 9. Forbindelse ifølge krav 1, der er valgt fra gruppen bestående af:eller et farmaceutisk acceptabelt salt deraf.
- 10. Farmaceutisk sammensætning, som indbefatter en forbindelse ifølge et hvilket som helst af kravene 1 til 9 og en farmaceutisk acceptabel diluent, excipiens eller bærer.
- 11. Forbindelse ifølge krav 1 til anvendelse som et medikament.
- 12. Forbindelse ifølge et hvilket som helst af kravene 1 til 9 til anvendelse ved behandling af en lidelse, der er valgt fra gruppen bestående af diabetes, hyperglykæmi, lav glucosetolerance, hyperinsulinæmi, hyperlipidæmi, hypertriglyceridæmi, hypercholesterolæmi, dyslipidæmi, adipositas, abdominal adipositas, glaukom, hypertension, aterosklerose og følgevirkningerne deraf, retinopati, nefropati, neuropati, osteoporose, osteoarthritis, demens, depression, neurodegenerativ sygdom, psykiatriske lidelser, Cushings sygdom, Cushings syndrom, virussygdomme og inflammatoriske sygdomme.
- 13. Forbindelse til anvendelse ifølge krav 12, hvor lidelsen er diabetes.
- 14. Forbindelse til anvendelse ifølge krav 13, hvor lidelsen er type ll-diabetes.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IN4527CH2011 | 2011-12-22 | ||
PCT/IN2012/000841 WO2013128465A1 (en) | 2011-12-22 | 2012-12-21 | Cyclic amide derivatives as inhibitors of 11 - beta - hydroxysteroid dehydrogenase and uses thereof |
Publications (1)
Publication Number | Publication Date |
---|---|
DK2800748T3 true DK2800748T3 (da) | 2017-07-17 |
Family
ID=54258979
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK12846788.3T DK2800748T3 (da) | 2011-12-22 | 2012-12-21 | Cykliske amidderivater som inhibitorer af 11-beta-hydroxysteroid-dehydrogenase og anvendelser deraf |
Country Status (21)
Country | Link |
---|---|
US (1) | US9453014B2 (da) |
EP (1) | EP2800748B1 (da) |
JP (1) | JP6118340B2 (da) |
KR (1) | KR102083040B1 (da) |
CN (1) | CN104125956B (da) |
AU (1) | AU2012372019B2 (da) |
BR (1) | BR112014015301A8 (da) |
CA (1) | CA2860187C (da) |
CL (1) | CL2014001704A1 (da) |
CO (1) | CO7160013A2 (da) |
DK (1) | DK2800748T3 (da) |
ES (1) | ES2630309T3 (da) |
IL (1) | IL233270A0 (da) |
MA (1) | MA35874B1 (da) |
MX (1) | MX354361B (da) |
MY (1) | MY173696A (da) |
PH (1) | PH12014501442B1 (da) |
RU (1) | RU2669695C2 (da) |
SG (1) | SG11201403268QA (da) |
WO (1) | WO2013128465A1 (da) |
ZA (1) | ZA201405263B (da) |
Families Citing this family (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN105418582A (zh) | 2011-09-26 | 2016-03-23 | 日东电工株式会社 | 用于提高的日光采集效率的高荧光且光稳定性生色团 |
JP2013084952A (ja) | 2011-10-05 | 2013-05-09 | Nitto Denko Corp | 太陽光捕集効率を向上させるための、感圧接着剤層を含む波長変換膜 |
AR089284A1 (es) | 2011-12-22 | 2014-08-13 | Galapagos Nv | Dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de trastornos inflamatorios |
HUE041509T2 (hu) | 2011-12-22 | 2019-05-28 | Janssen Biopharma Inc | Szubsztituált nukleozidok, nukleotidok és ezek analógjai |
US9441007B2 (en) | 2012-03-21 | 2016-09-13 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
USRE48171E1 (en) | 2012-03-21 | 2020-08-25 | Janssen Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
WO2016004305A2 (en) | 2014-07-02 | 2016-01-07 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
CN106397377B (zh) * | 2016-09-05 | 2019-04-05 | 中南大学 | 一种富电子五元杂环酸及其衍生物脱羧上氟的方法 |
IL268345B (en) | 2017-02-24 | 2022-08-01 | Univ California | Preparations and methods for promoting hair growth with mpc1 inhibitors |
IL271443B2 (en) * | 2017-06-30 | 2024-01-01 | Univ California | Preparations and methods for regulating hair growth |
US11351149B2 (en) | 2020-09-03 | 2022-06-07 | Pfizer Inc. | Nitrile-containing antiviral compounds |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE2961415D1 (en) * | 1978-05-20 | 1982-01-28 | Bayer Ag | Heteroaryloxy-acetamides, process for their preparation and their use as herbicides |
DE2903966A1 (de) * | 1979-02-02 | 1980-08-07 | Bayer Ag | Substituierte carbonsaeureamide, verfahren zu ihrer herstellung und ihre verwendung als herbizide |
JPH03503650A (ja) * | 1988-04-05 | 1991-08-15 | アボツト・ラボラトリーズ | Cckアンタゴニストとしてのトリプトファン誘導体 |
FR2703679B1 (fr) * | 1993-04-05 | 1995-06-23 | Rhone Poulenc Rorer Sa | Nouveaux derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent. |
FR2777566B1 (fr) * | 1998-04-15 | 2003-02-21 | Synthelabo | Derives d'azacycloalcanes, leur preparation et leur application en therapeutique |
US7022725B2 (en) * | 2000-11-17 | 2006-04-04 | Takeda Pharmaceutical Company Limited | Isoxazole derivatives |
WO2004089470A2 (en) * | 2003-04-11 | 2004-10-21 | Novo Nordisk A/S | New amide derivatives and pharmaceutical use thereof |
DE102004005172A1 (de) * | 2004-02-02 | 2005-08-18 | Aventis Pharma Deutschland Gmbh | Indazolderivate als Inhibitoren der Hormon Sensitiven Lipase |
US20050239853A1 (en) | 2004-02-04 | 2005-10-27 | Tjeerd Barf | New compounds |
WO2006012504A2 (en) * | 2004-07-23 | 2006-02-02 | Daiamed, Inc. | Compounds and methods for treatment of thrombosis |
WO2009126675A1 (en) * | 2008-04-09 | 2009-10-15 | Boehringer Ingelheim International Gmbh | 2-sulfonylamino-4-heteroaryl butyramide antagonists of ccr10 |
ES2350077B1 (es) * | 2009-06-04 | 2011-11-04 | Laboratorios Salvat, S.A. | Compuestos inhibidores de 11beta-hidroxiesteroide deshidrogenasa de tipo 1. |
-
2012
- 2012-12-21 AU AU2012372019A patent/AU2012372019B2/en not_active Ceased
- 2012-12-21 MX MX2014007719A patent/MX354361B/es active IP Right Grant
- 2012-12-21 ES ES12846788T patent/ES2630309T3/es active Active
- 2012-12-21 CA CA2860187A patent/CA2860187C/en not_active Expired - Fee Related
- 2012-12-21 US US14/367,614 patent/US9453014B2/en active Active
- 2012-12-21 DK DK12846788.3T patent/DK2800748T3/da active
- 2012-12-21 SG SG11201403268QA patent/SG11201403268QA/en unknown
- 2012-12-21 RU RU2014126646A patent/RU2669695C2/ru active
- 2012-12-21 KR KR1020147020455A patent/KR102083040B1/ko active IP Right Grant
- 2012-12-21 CN CN201280070441.8A patent/CN104125956B/zh not_active Expired - Fee Related
- 2012-12-21 JP JP2014548339A patent/JP6118340B2/ja not_active Expired - Fee Related
- 2012-12-21 WO PCT/IN2012/000841 patent/WO2013128465A1/en active Application Filing
- 2012-12-21 BR BR112014015301A patent/BR112014015301A8/pt not_active IP Right Cessation
- 2012-12-21 EP EP12846788.3A patent/EP2800748B1/en not_active Not-in-force
- 2012-12-21 MY MYPI2014001836A patent/MY173696A/en unknown
-
2014
- 2014-06-19 IL IL233270A patent/IL233270A0/en unknown
- 2014-06-20 PH PH12014501442A patent/PH12014501442B1/en unknown
- 2014-06-23 CL CL2014001704A patent/CL2014001704A1/es unknown
- 2014-07-18 ZA ZA2014/05263A patent/ZA201405263B/en unknown
- 2014-07-20 MA MA37227A patent/MA35874B1/fr unknown
- 2014-07-22 CO CO14158010A patent/CO7160013A2/es unknown
Also Published As
Publication number | Publication date |
---|---|
MX2014007719A (es) | 2015-03-19 |
IL233270A0 (en) | 2014-08-31 |
JP6118340B2 (ja) | 2017-04-19 |
MX354361B (es) | 2018-02-28 |
NZ626745A (en) | 2016-06-24 |
ES2630309T3 (es) | 2017-08-21 |
MY173696A (en) | 2020-02-17 |
JP2015521154A (ja) | 2015-07-27 |
CN104125956A (zh) | 2014-10-29 |
CN104125956B (zh) | 2019-08-16 |
CA2860187C (en) | 2020-11-10 |
ZA201405263B (en) | 2016-05-25 |
AU2012372019A1 (en) | 2014-07-24 |
EP2800748A1 (en) | 2014-11-12 |
AU2012372019B2 (en) | 2017-06-15 |
BR112014015301A2 (pt) | 2017-06-13 |
BR112014015301A8 (pt) | 2017-07-04 |
MA35874B1 (fr) | 2014-12-01 |
SG11201403268QA (en) | 2014-07-30 |
CO7160013A2 (es) | 2015-01-15 |
PH12014501442A1 (en) | 2014-10-08 |
KR102083040B1 (ko) | 2020-02-28 |
US20150158860A1 (en) | 2015-06-11 |
PH12014501442B1 (en) | 2014-10-08 |
RU2669695C2 (ru) | 2018-10-15 |
RU2014126646A (ru) | 2016-02-10 |
CA2860187A1 (en) | 2013-09-06 |
KR20140127226A (ko) | 2014-11-03 |
WO2013128465A1 (en) | 2013-09-06 |
EP2800748B1 (en) | 2017-03-29 |
CL2014001704A1 (es) | 2015-03-13 |
US9453014B2 (en) | 2016-09-27 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
DK2800748T3 (da) | Cykliske amidderivater som inhibitorer af 11-beta-hydroxysteroid-dehydrogenase og anvendelser deraf | |
AU2017263361B2 (en) | Cyclopropyl-amide compounds as dual LSD1/HDAC inhibitors | |
AU2012367780B2 (en) | Derivatives of aza adamantane and uses thereof | |
CA2730793C (en) | Azole compound | |
KR101919680B1 (ko) | 신규한 피롤리딘 화합물 및 멜라노코르틴 수용체 아고니스트로서의 용도 | |
TW201018661A (en) | Heterocyclic rinf having nitrogen atom derivatives and medicament containing the derivatives as active ingredient | |
SK17042001A3 (sk) | Derivát indolylpiperidínu ako antihistaminické a antialergické činidlo | |
KR20220141331A (ko) | P2x3 조정제 | |
US20160355475A1 (en) | Novel indole derivative compound and pharmaceutical composition comprising the same | |
JP2013536207A (ja) | ヒドロキサメート骨格のデアセチラーゼ類阻害剤 | |
RU2536688C2 (ru) | Новые бензамидные производные | |
WO2014000629A1 (zh) | 六氢并环戊二烯衍生物、其制备方法及其在医药上的应用 | |
KR20080065674A (ko) | 신규한 인돌 함유 베타 효능제, 이의 제조 방법 및약제로서의 이의 용도 | |
NZ626745B2 (en) | Cyclic amide derivatives as inhibitors of 11 - beta - hydroxysteroid dehydrogenase and uses thereof | |
TW201910325A (zh) | 吲哚衍生物及其用途 |