KR101714820B1 - 11(베타)-ｈｓｄ1의 억제제로서 3,3-이치환된-(8-아자-비시클로[3.2.1]옥트-8-일)-[5-(1h-피라졸-4-일)-티오펜-3-일]-메탄온 - Google Patents

11(베타)-ｈｓｄ1의 억제제로서 3,3-이치환된-(8-아자-비시클로[3.2.1]옥트-8-일)-[5-(1h-피라졸-4-일)-티오펜-3-일]-메탄온 Download PDF

Info

Publication number
KR101714820B1
KR101714820B1 KR1020127028597A KR20127028597A KR101714820B1 KR 101714820 B1 KR101714820 B1 KR 101714820B1 KR 1020127028597 A KR1020127028597 A KR 1020127028597A KR 20127028597 A KR20127028597 A KR 20127028597A KR 101714820 B1 KR101714820 B1 KR 101714820B1
Authority
KR
South Korea
Prior art keywords
independently
compound
compounds
delete delete
disease
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
Application number
KR1020127028597A
Other languages
English (en)
Korean (ko)
Other versions
KR20130079379A (ko
Inventor
스캇 피터 웹스터
조나단 로버트 섹클
브라이언 로버트 월컬
피터 월드
토마스 데이빗 펠린
헤이즐 조안 디케
트레볼 로버트 퍼리어
Original Assignee
더 유니버시티 오브 에든버러
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 더 유니버시티 오브 에든버러 filed Critical 더 유니버시티 오브 에든버러
Publication of KR20130079379A publication Critical patent/KR20130079379A/ko
Application granted granted Critical
Publication of KR101714820B1 publication Critical patent/KR101714820B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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)
KR1020127028597A 2010-04-29 2011-03-10 11(베타)-ｈｓｄ1의 억제제로서 3,3-이치환된-(8-아자-비시클로[3.2.1]옥트-8-일)-[5-(1h-피라졸-4-일)-티오펜-3-일]-메탄온 Active KR101714820B1 (ko)

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 (2)

Publication Number Publication Date
KR20130079379A KR20130079379A (ko) 2013-07-10
KR101714820B1 true KR101714820B1 (ko) 2017-03-09

Family

ID=43880967

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020127028597A Active KR101714820B1 (ko) 2010-04-29 2011-03-10 11(베타)-ｈｓｄ1의 억제제로서 3,3-이치환된-(8-아자-비시클로[3.2.1]옥트-8-일)-[5-(1h-피라졸-4-일)-티오펜-3-일]-메탄온

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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009074789A1 (en) 2007-12-12 2009-06-18 The University Of Edinburgh Amido-thiophene compounds and their use as 11-beta-hsd1 inhibitors
WO2009112845A1 (en) 2008-03-13 2009-09-17 The University Of Edinburgh Amido-thiophene compounds and their use
WO2010023161A1 (en) 2008-08-25 2010-03-04 Boehringer Ingelheim International Gmbh Aryl- and heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use

Family Cites Families (23)

* 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
US20100022590A1 (en) 2008-01-17 2010-01-28 Biovitrum Ab (Publ.) Novel compounds
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009074789A1 (en) 2007-12-12 2009-06-18 The University Of Edinburgh Amido-thiophene compounds and their use as 11-beta-hsd1 inhibitors
WO2009112845A1 (en) 2008-03-13 2009-09-17 The University Of Edinburgh Amido-thiophene compounds and their use
WO2010023161A1 (en) 2008-08-25 2010-03-04 Boehringer Ingelheim International Gmbh Aryl- and heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use

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
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
KR101714820B1 (ko) 11(베타)-ｈｓｄ1의 억제제로서 3,3-이치환된-(8-아자-비시클로[3.2.1]옥트-8-일)-[5-(1h-피라졸-4-일)-티오펜-3-일]-메탄온
KR101702159B1 (ko) （４―페닐―피페리딘―1―일）―［５―（1ｈ―피라졸―４―일）―티오펜―３―일］―메탄온 화합물 및 그의 용도
EP2283004B1 (en) Amido-thiophene compounds and their use
EP2229374A1 (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

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

PE0801 Dismissal of amendment

St.27 status event code: A-2-2-P10-P12-nap-PE0801

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

P22-X000 Classification modified

St.27 status event code: A-2-2-P10-P22-nap-X000

P22-X000 Classification modified

St.27 status event code: A-2-2-P10-P22-nap-X000

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

FPAY Annual fee payment

Payment date: 20191204

Year of fee payment: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 5

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 6

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 7

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 8

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 9

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 10

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-OTH-PR1001 (AS PROVIDED BY THE NATIONAL OFFICE)

Year of fee payment: 10