JP5899202B2 - 11β−HSD1の阻害剤としての3,3−二置換−(8−アザ−ビシクロ[3.2.1]オクタ−8−イル)−[5−(1H−ピラゾール−4−イル)−チオフェン−3−イル]−メタノン類 - Google Patents
11β−HSD1の阻害剤としての3,3−二置換−(8−アザ−ビシクロ[3.2.1]オクタ−8−イル)−[5−(1H−ピラゾール−4−イル)−チオフェン−3−イル]−メタノン類 Download PDFInfo
- Publication number
- JP5899202B2 JP5899202B2 JP2013506723A JP2013506723A JP5899202B2 JP 5899202 B2 JP5899202 B2 JP 5899202B2 JP 2013506723 A JP2013506723 A JP 2013506723A JP 2013506723 A JP2013506723 A JP 2013506723A JP 5899202 B2 JP5899202 B2 JP 5899202B2
- Authority
- JP
- Japan
- Prior art keywords
- independently
- compound
- compound according
- disease
- aza
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- 0 CCC1=CC2CC(*)(*)CC1C2 Chemical compound CCC1=CC2CC(*)(*)CC1C2 0.000 description 4
- GYCPLYCTMDTEPU-UHFFFAOYSA-N Brc1cncnc1 Chemical compound Brc1cncnc1 GYCPLYCTMDTEPU-UHFFFAOYSA-N 0.000 description 1
- RYPDHAPFMLDFJC-UHFFFAOYSA-N CC(C)(C)OC(N(C(CC1)C2)C1CC2(c1c[s]cn1)O)=O Chemical compound CC(C)(C)OC(N(C(CC1)C2)C1CC2(c1c[s]cn1)O)=O RYPDHAPFMLDFJC-UHFFFAOYSA-N 0.000 description 1
- RWIFKGSDSNLXBL-UHFFFAOYSA-N CCC1C(C#[O])N(Cc2ccccc2)C1CC Chemical compound CCC1C(C#[O])N(Cc2ccccc2)C1CC RWIFKGSDSNLXBL-UHFFFAOYSA-N 0.000 description 1
- BWNHMMBCCJAAEI-UHFFFAOYSA-N C[I]1C(C(C2)(CC34C2NC3CC4)O)=NC=CC1 Chemical compound C[I]1C(C(C2)(CC34C2NC3CC4)O)=NC=CC1 BWNHMMBCCJAAEI-UHFFFAOYSA-N 0.000 description 1
- MMZFGTAMARVHAF-UHFFFAOYSA-N OC(CC1CC2)(CC2N1C(c1c[s]c(-c2c[nH]nc2)c1)=O)c1ncccn1 Chemical compound OC(CC1CC2)(CC2N1C(c1c[s]c(-c2c[nH]nc2)c1)=O)c1ncccn1 MMZFGTAMARVHAF-UHFFFAOYSA-N 0.000 description 1
- OIDIBOYMWXTAOH-UHFFFAOYSA-N OC(c1c[s]c(-c2c[nH]nc2)c1)=O Chemical compound OC(c1c[s]c(-c2c[nH]nc2)c1)=O OIDIBOYMWXTAOH-UHFFFAOYSA-N 0.000 description 1
- XZPLVTJMQSTSRV-UHFFFAOYSA-N OC1(CC(CC2)N(Cc3ccccc3)C2C1)c(ncnc1)c1Br Chemical compound OC1(CC(CC2)N(Cc3ccccc3)C2C1)c(ncnc1)c1Br XZPLVTJMQSTSRV-UHFFFAOYSA-N 0.000 description 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N c1c[nH]c2ccccc12 Chemical compound c1c[nH]c2ccccc12 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 description 1
- PBMFSQRYOILNGV-UHFFFAOYSA-N c1ccnnc1 Chemical compound c1ccnnc1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 description 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N c1cncnc1 Chemical compound c1cncnc1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 description 1
- JYEUMXHLPRZUAT-UHFFFAOYSA-N c1cnnnc1 Chemical compound c1cnnnc1 JYEUMXHLPRZUAT-UHFFFAOYSA-N 0.000 description 1
- KYQCOXFCLRTKLS-UHFFFAOYSA-N c1nccnc1 Chemical compound c1nccnc1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 description 1
- JIHQDMXYYFUGFV-UHFFFAOYSA-N c1ncncn1 Chemical compound c1ncncn1 JIHQDMXYYFUGFV-UHFFFAOYSA-N 0.000 description 1
- FYADHXFMURLYQI-UHFFFAOYSA-N c1ncnnc1 Chemical compound c1ncnnc1 FYADHXFMURLYQI-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
- C07D451/06—Oxygen 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
- A61K31/41—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
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
-
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
- A61P5/08—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
-
- 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
-
- 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
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Psychiatry (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Ophthalmology & Optometry (AREA)
- Pulmonology (AREA)
- Emergency Medicine (AREA)
- Virology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Dermatology (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Communicable Diseases (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32945310P | 2010-04-29 | 2010-04-29 | |
| US61/329,453 | 2010-04-29 | ||
| PCT/GB2011/000345 WO2011135276A1 (en) | 2010-04-29 | 2011-03-10 | 3, 3 -disubstituted- ( 8 - aza - bicyclo [3.2.1] oct- 8 - yl) -[5- (1h - pyrazol - 4 -yl) -thiophen-3 -yl] methanones as inhibitors of 11 (beta) -hsd1 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013527162A JP2013527162A (ja) | 2013-06-27 |
| JP2013527162A5 JP2013527162A5 (https=) | 2014-03-27 |
| JP5899202B2 true JP5899202B2 (ja) | 2016-04-06 |
Family
ID=43880967
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013506723A Active JP5899202B2 (ja) | 2010-04-29 | 2011-03-10 | 11β−HSD1の阻害剤としての3,3−二置換−(8−アザ−ビシクロ[3.2.1]オクタ−8−イル)−[5−(1H−ピラゾール−4−イル)−チオフェン−3−イル]−メタノン類 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US9365564B2 (https=) |
| EP (1) | EP2563780B1 (https=) |
| JP (1) | JP5899202B2 (https=) |
| KR (1) | KR101714820B1 (https=) |
| CN (1) | CN102947295B (https=) |
| AU (1) | AU2011247116B2 (https=) |
| BR (1) | BR112012027640B1 (https=) |
| CA (1) | CA2796297C (https=) |
| DK (1) | DK2563780T3 (https=) |
| ES (1) | ES2543692T3 (https=) |
| IL (1) | IL222417A (https=) |
| MX (1) | MX344142B (https=) |
| RU (1) | RU2593753C2 (https=) |
| WO (1) | WO2011135276A1 (https=) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0724251D0 (en) | 2007-12-12 | 2008-02-06 | Univ Edinburgh | Therapeutic compounds and their use |
| GB0804685D0 (en) | 2008-03-13 | 2008-04-16 | Univ Edinburgh | Therapeutic compounds and their use |
| EP2477983B1 (en) | 2009-09-16 | 2015-04-15 | The University Of Edinburgh | (4-phenyl-piperidin-1-yl)-[5-1h-pyrazol-4yl)-thiophen-3-yl]-methanone compounds and their use |
| WO2011135276A1 (en) | 2010-04-29 | 2011-11-03 | The University Of Edinburgh | 3, 3 -disubstituted- ( 8 - aza - bicyclo [3.2.1] oct- 8 - yl) -[5- (1h - pyrazol - 4 -yl) -thiophen-3 -yl] methanones as inhibitors of 11 (beta) -hsd1 |
| FR2993563B1 (fr) * | 2012-07-20 | 2015-12-18 | Metabrain Res | Derives de thiophenes utiles dans le traitement du diabete |
| WO2015131773A1 (zh) * | 2014-03-06 | 2015-09-11 | 上海海雁医药科技有限公司 | 作为食欲素受体拮抗剂的哌啶衍生物 |
| FR3035326B1 (fr) * | 2015-04-21 | 2017-05-12 | Pf Medicament | Utilisation de la (4-hydroxy-2-methyl-1,1-dioxido-2h-benzo[e][1,2]thiazin-3-yl)(naphtalen-2-yl)methanone dans la prevention et/ou le traitement de la steatohepatite non-alcoolique |
| CN104961698A (zh) * | 2015-07-13 | 2015-10-07 | 佛山市赛维斯医药科技有限公司 | 末端硝基取代的三氮唑亚砜类化合物、其制备方法及其用途 |
| CN104974080A (zh) * | 2015-07-19 | 2015-10-14 | 佛山市赛维斯医药科技有限公司 | 二吡啶叔醇结构的11β-HSD1抑制剂、制备方法及其用途 |
| CN104945315A (zh) * | 2015-07-19 | 2015-09-30 | 佛山市赛维斯医药科技有限公司 | 一类硝基二吡啶叔醇结构的11β-HSD1抑制剂及其用途 |
| CN104961677A (zh) * | 2015-07-19 | 2015-10-07 | 佛山市赛维斯医药科技有限公司 | 一类腈基二吡啶叔醇结构的11β-HSD1抑制剂及其用途 |
| EP3373920A4 (en) | 2015-11-13 | 2019-07-17 | Pietro Paolo Sanna | METHOD AND COMPOSITIONS FOR TREATING ALCOHOL CONSUMPTION MALFUNCTIONS |
| EA202092441A1 (ru) | 2016-06-07 | 2021-05-21 | Джакобио Фармасьютикалс Ко., Лтд. | Новые гетероциклические производные, применимые в качестве ингибиторов shp2 |
| KR20240026521A (ko) | 2017-03-23 | 2024-02-28 | 자코바이오 파마슈티칼스 컴퍼니 리미티드 | Shp2 억제제로서 유용한 신규한 헤테로환형 유도체 |
| CN112839935A (zh) | 2018-09-26 | 2021-05-25 | 北京加科思新药研发有限公司 | 可用作shp2抑制剂的新型杂环衍生物 |
| TW202523658A (zh) * | 2019-05-24 | 2025-06-16 | 美商賽吉醫療公司 | 化合物、組合物及使用方法 |
| MX2022003845A (es) * | 2019-09-30 | 2022-06-22 | Actinogen Medical Ltd | Tratamientos cognitivos medicinales. |
| WO2022051565A1 (en) * | 2020-09-04 | 2022-03-10 | Ikena Oncology, Inc. | Substituted 4-piperidinyl-quinazolines, 4-piperidinyl-pyrimidine-2-amines, and related compounds and their use in treating medical conditions |
| US12029718B2 (en) | 2021-11-09 | 2024-07-09 | Cct Sciences, Llc | Process for production of essentially pure delta-9-tetrahydrocannabinol |
| WO2022094668A1 (en) * | 2020-11-06 | 2022-05-12 | Actinogen Medical Limited | Process for preparing heterocyclic methanone compounds and aza-bicyclo intermediates thereof |
| JP2023550654A (ja) * | 2020-11-25 | 2023-12-04 | セージ セラピューティクス, インコーポレイテッド | 神経変性障害の治療のためのcyp46a1阻害剤としての4-フルオロ-(4-(4-ベンジル)ピペリジン-1-イル)(2-(ピリミジン-4-イル)ピリジン-3-イル)メタノン誘導体および類似化合物 |
| JP2025519558A (ja) * | 2022-06-10 | 2025-06-26 | アクチノゲン メディカル リミテッド | 抗うつ薬抵抗性対象の治療 |
| CN115073422A (zh) * | 2022-07-28 | 2022-09-20 | 成都普瑞熙药业有限公司 | 一种制备4-(1-甲基-1h-吡唑-5-基)哌啶及其盐的方法 |
| CN120153257A (zh) * | 2022-10-07 | 2025-06-13 | 射线质医疗有限公司 | 用于11β-HSD1抑制剂治疗的受试者选择 |
| CN120957989A (zh) * | 2023-03-02 | 2025-11-14 | 射线质医疗有限公司 | 用于制备氮杂双环杂芳基化合物的流动化学工艺 |
| WO2025073002A1 (en) * | 2023-10-03 | 2025-04-10 | Actinogen Medical Limited | Tablet formulation |
| GB202408335D0 (en) | 2024-06-11 | 2024-07-24 | Astrazeneca Ab | Therapies for wound treatment |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5087631A (en) | 1990-12-18 | 1992-02-11 | Glaxo Inc. | Oxathi(SIV)azol-5-one compounds |
| AR011913A1 (es) | 1997-03-06 | 2000-09-13 | Yamano Masaki | Derivados de 4,4-difluoro-2,3,4,5-tetrahidro-1h-1-benzoazepina y composiciones farmaceuticas de los mismos. |
| US6303593B1 (en) | 1999-03-02 | 2001-10-16 | Merck & Co., Inc. | 3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity |
| AU2002353716A1 (en) | 2001-11-22 | 2003-06-10 | Biovitrum Ab | Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1 |
| SE0202430D0 (sv) | 2002-08-14 | 2002-08-14 | Astrazeneca Ab | New Compounds |
| US7700583B2 (en) | 2003-04-11 | 2010-04-20 | High Point Pharmaceuticals, Llc | 11β-hydroxysteroid dehydrogenase type 1 active compounds |
| GB0325745D0 (en) | 2003-11-05 | 2003-12-10 | Astrazeneca Ab | Chemical compounds |
| GB0326029D0 (en) | 2003-11-07 | 2003-12-10 | Astrazeneca Ab | Chemical compounds |
| RU2006146608A (ru) | 2004-06-09 | 2008-07-20 | Ф.Хоффманн-Ля Рош Аг (Ch) | ОКТАГИДРОПИРРОЛО[3,4-с]-ПРОИЗВОДНЫЕ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ПРОТИВОВИРУСНЫХ АГЕНТОВ |
| EP1894919B1 (en) | 2005-06-07 | 2012-03-28 | Shionogi & Co., Ltd. | Heterocyclic compound having type i 11 beta hydroxysteroid dehydrogenase inhibitory activity |
| CN101243074A (zh) * | 2005-06-08 | 2008-08-13 | 日本烟草产业株式会社 | 杂环化合物 |
| EP1889842A4 (en) | 2005-06-08 | 2009-07-29 | Japan Tobacco Inc | HETEROCYCLIC CONNECTION |
| US7803806B2 (en) | 2005-11-03 | 2010-09-28 | Sgx Pharmaceuticals, Inc. | Pyrimidinyl-thiophene kinase modulators |
| BRPI0710479A2 (pt) | 2006-01-18 | 2012-08-14 | Hoffmann La Roche | composto, processo para sua preparaÇço, composiÇço farmacÊutica, uso de um composto e mÉtodo de tratamento de doenÇa ou desosrdem metabàlica. |
| CN101484424B (zh) | 2006-02-28 | 2014-05-14 | 达特神经科学(开曼)有限公司 | 治疗化合物 |
| UA95480C2 (uk) | 2006-06-08 | 2011-08-10 | Елі Ліллі Енд Компані | Заміщені карбоксаміди |
| TW200811170A (en) * | 2006-06-27 | 2008-03-01 | Sanofi Aventis | Urea derivatives of tropane, their preparation and their therapeutic application |
| US7666888B2 (en) | 2006-07-20 | 2010-02-23 | Amgen Inc. | Substituted azole aromatic heterocycles as inhibitors of 11β-HSD-1 |
| JP5529743B2 (ja) * | 2007-11-05 | 2014-06-25 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | 選択的11−ベータ−ヒドロキシステロイドデヒドロゲナーゼ1型阻害剤としての7−アザインドール誘導体 |
| GB0724251D0 (en) * | 2007-12-12 | 2008-02-06 | Univ Edinburgh | Therapeutic compounds and their use |
| US20100022590A1 (en) | 2008-01-17 | 2010-01-28 | Biovitrum Ab (Publ.) | Novel compounds |
| GB0804685D0 (en) * | 2008-03-13 | 2008-04-16 | Univ Edinburgh | Therapeutic compounds and their use |
| CA2735204C (en) * | 2008-08-25 | 2017-06-20 | Boehringer Ingelheim International Gmbh | Aryl- and heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use |
| EP2443113A1 (en) | 2009-06-15 | 2012-04-25 | The University Of Edinburgh | Amido-isothiazole compounds and their use as inhibitors of 11beta-hsd1 for the treatment of metabolic syndrome and related disorders |
| EP2477983B1 (en) | 2009-09-16 | 2015-04-15 | The University Of Edinburgh | (4-phenyl-piperidin-1-yl)-[5-1h-pyrazol-4yl)-thiophen-3-yl]-methanone compounds and their use |
| WO2011135276A1 (en) | 2010-04-29 | 2011-11-03 | The University Of Edinburgh | 3, 3 -disubstituted- ( 8 - aza - bicyclo [3.2.1] oct- 8 - yl) -[5- (1h - pyrazol - 4 -yl) -thiophen-3 -yl] methanones as inhibitors of 11 (beta) -hsd1 |
-
2011
- 2011-03-10 WO PCT/GB2011/000345 patent/WO2011135276A1/en not_active Ceased
- 2011-03-10 MX MX2012012413A patent/MX344142B/es active IP Right Grant
- 2011-03-10 JP JP2013506723A patent/JP5899202B2/ja active Active
- 2011-03-10 BR BR112012027640-9A patent/BR112012027640B1/pt active IP Right Grant
- 2011-03-10 RU RU2012143502/04A patent/RU2593753C2/ru active
- 2011-03-10 DK DK11709770.9T patent/DK2563780T3/en active
- 2011-03-10 CN CN201180031564.6A patent/CN102947295B/zh active Active
- 2011-03-10 AU AU2011247116A patent/AU2011247116B2/en active Active
- 2011-03-10 KR KR1020127028597A patent/KR101714820B1/ko active Active
- 2011-03-10 EP EP11709770.9A patent/EP2563780B1/en active Active
- 2011-03-10 CA CA2796297A patent/CA2796297C/en active Active
- 2011-03-10 ES ES11709770.9T patent/ES2543692T3/es active Active
- 2011-03-10 US US13/642,963 patent/US9365564B2/en active Active
-
2012
- 2012-10-14 IL IL222417A patent/IL222417A/en active IP Right Grant
-
2016
- 2016-05-13 US US15/154,254 patent/US9834549B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| JP2013527162A (ja) | 2013-06-27 |
| CA2796297C (en) | 2017-09-05 |
| EP2563780A1 (en) | 2013-03-06 |
| WO2011135276A1 (en) | 2011-11-03 |
| US9365564B2 (en) | 2016-06-14 |
| EP2563780B1 (en) | 2015-05-06 |
| IL222417A0 (en) | 2012-12-31 |
| CN102947295B (zh) | 2016-01-20 |
| BR112012027640B1 (pt) | 2021-08-03 |
| RU2593753C2 (ru) | 2016-08-10 |
| IL222417A (en) | 2016-08-31 |
| ES2543692T3 (es) | 2015-08-21 |
| BR112012027640A2 (pt) | 2017-08-08 |
| MX2012012413A (es) | 2013-02-26 |
| MX344142B (es) | 2016-12-07 |
| US20130123268A1 (en) | 2013-05-16 |
| US20160251346A1 (en) | 2016-09-01 |
| AU2011247116B2 (en) | 2015-12-03 |
| KR101714820B1 (ko) | 2017-03-09 |
| RU2012143502A (ru) | 2014-06-10 |
| US9834549B2 (en) | 2017-12-05 |
| CN102947295A (zh) | 2013-02-27 |
| KR20130079379A (ko) | 2013-07-10 |
| AU2011247116A1 (en) | 2012-11-22 |
| DK2563780T3 (en) | 2015-07-27 |
| CA2796297A1 (en) | 2011-11-03 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP5899202B2 (ja) | 11β−HSD1の阻害剤としての3,3−二置換−(8−アザ−ビシクロ[3.2.1]オクタ−8−イル)−[5−(1H−ピラゾール−4−イル)−チオフェン−3−イル]−メタノン類 | |
| JP5779181B2 (ja) | (4−フェニル−ピペリジン−1−イル)−[5−(1h−ピラゾール−4−イル)−チオフェン−3−イル]−メタノン化合物及びそれらの使用 | |
| EP2283004B1 (en) | Amido-thiophene compounds and their use | |
| JP3793200B2 (ja) | Ccr5モジュレータとしてのトロパン誘導体 | |
| WO2009074789A1 (en) | Amido-thiophene compounds and their use as 11-beta-hsd1 inhibitors | |
| WO2010146338A1 (en) | Amido-isothiazole compounds and their use as inhibitors of 11beta-hsd1 for the treatment of metabolic syndrome and related disorders | |
| TW200800189A (en) | 3-monosubstituted tropane derivatives as nociceptin receptor ligands | |
| CN1880319B (zh) | 作为ccr5调节剂的托烷衍生物 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RD01 | Notification of change of attorney |
Free format text: JAPANESE INTERMEDIATE CODE: A7426 Effective date: 20130719 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A821 Effective date: 20130719 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20140203 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20140203 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20141211 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20141216 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20150316 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20150818 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20151027 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20160223 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20160307 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 5899202 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |