DK2563780T3 - 3,3-DISUBSTITUEREDE- (8-aza-bicyclo [3.2.1] oct-8-yl) - [5- (1H-pyrazol-4-yl) -thiophene-3-yl] -METHANONER as inhibitors of 11 ( BETA) -HSD1 - Google Patents

3,3-DISUBSTITUEREDE- (8-aza-bicyclo [3.2.1] oct-8-yl) - [5- (1H-pyrazol-4-yl) -thiophene-3-yl] -METHANONER as inhibitors of 11 ( BETA) -HSD1 Download PDF

Info

Publication number
DK2563780T3
DK2563780T3 DK11709770.9T DK11709770T DK2563780T3 DK 2563780 T3 DK2563780 T3 DK 2563780T3 DK 11709770 T DK11709770 T DK 11709770T DK 2563780 T3 DK2563780 T3 DK 2563780T3
Authority
DK
Denmark
Prior art keywords
independently
compound according
disease
compound
aza
Prior art date
Application number
DK11709770.9T
Other languages
Danish (da)
English (en)
Inventor
Scott Peter Webster
Jonathan Robert Seckl
Brian Robert Walker
Peter Ward
Thomas David Pallin
Trevor Robert Perrior
Hazel Joan Dyke
Original Assignee
Univ Edinburgh
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 Univ Edinburgh filed Critical Univ Edinburgh
Application granted granted Critical
Publication of DK2563780T3 publication Critical patent/DK2563780T3/en

Links

Classifications

    • 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
    • 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
    • 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)
DK11709770.9T 2010-04-29 2011-03-10 3,3-DISUBSTITUEREDE- (8-aza-bicyclo [3.2.1] oct-8-yl) - [5- (1H-pyrazol-4-yl) -thiophene-3-yl] -METHANONER as inhibitors of 11 ( BETA) -HSD1 DK2563780T3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US32945310P 2010-04-29 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 (1)

Publication Number Publication Date
DK2563780T3 true DK2563780T3 (en) 2015-07-27

Family

ID=43880967

Family Applications (1)

Application Number Title Priority Date Filing Date
DK11709770.9T DK2563780T3 (en) 2010-04-29 2011-03-10 3,3-DISUBSTITUEREDE- (8-aza-bicyclo [3.2.1] oct-8-yl) - [5- (1H-pyrazol-4-yl) -thiophene-3-yl] -METHANONER as inhibitors of 11 ( BETA) -HSD1

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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

Also Published As

Publication number Publication date
JP5899202B2 (ja) 2016-04-06
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
CA2796297A1 (en) 2011-11-03

Similar Documents

Publication Publication Date Title
DK2563780T3 (en) 3,3-DISUBSTITUEREDE- (8-aza-bicyclo [3.2.1] oct-8-yl) - [5- (1H-pyrazol-4-yl) -thiophene-3-yl] -METHANONER as inhibitors of 11 ( BETA) -HSD1
DK2477983T3 (en) (4-phenyl-piperidin-1-yl) - [5-1H-pyrazol-4-yl) -thiophene-3-yl] -METHANONFORBINDELSER AND THEIR USE
US8614209B2 (en) Amido-thiophene compounds and their use
EP2229374A1 (en) Amido-thiophene compounds and their use as 11-beta-hsd1 inhibitors
US20120095046A1 (en) Amido-Isothiazole Compounds and Their Use as Inhibitors of 11Beta-HSD1 for the Treatment of Metabolic Syndrome and Related Disorders