CA2568163A1 - Bicyclic, nitrogen-containing heterocycles as aromatase inhibitors - Google Patents

Bicyclic, nitrogen-containing heterocycles as aromatase inhibitors Download PDF

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Publication number
CA2568163A1
CA2568163A1 CA002568163A CA2568163A CA2568163A1 CA 2568163 A1 CA2568163 A1 CA 2568163A1 CA 002568163 A CA002568163 A CA 002568163A CA 2568163 A CA2568163 A CA 2568163A CA 2568163 A1 CA2568163 A1 CA 2568163A1
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CA
Canada
Prior art keywords
alkyl
aryl
compound
halogen
acid
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.)
Abandoned
Application number
CA002568163A
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English (en)
French (fr)
Inventor
Peter Herold
Robert Mah
Vincenzo Tschinke
Christoph Schumacher
Michael Quirmbach
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Speedel Experimenta AG
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Individual
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Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of CA2568163A1 publication Critical patent/CA2568163A1/en
Abandoned legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04Ortho- or peri-condensed ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/12Drugs for disorders of the metabolism for electrolyte homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/42Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of mineralocorticosteroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/74Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
CA002568163A 2004-05-28 2005-05-27 Bicyclic, nitrogen-containing heterocycles as aromatase inhibitors Abandoned CA2568163A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CH9152004 2004-05-28
CH915/04 2004-05-28
PCT/EP2005/052416 WO2005118540A2 (en) 2004-05-28 2005-05-27 Bicyclic, nitrogen-containing heterocycles as aromatase inhibitors

Publications (1)

Publication Number Publication Date
CA2568163A1 true CA2568163A1 (en) 2005-12-15

Family

ID=34968588

Family Applications (2)

Application Number Title Priority Date Filing Date
CA002568163A Abandoned CA2568163A1 (en) 2004-05-28 2005-05-27 Bicyclic, nitrogen-containing heterocycles as aromatase inhibitors
CA002568159A Abandoned CA2568159A1 (en) 2004-05-28 2005-05-27 Tetrahydro-imidazo [1,5-a] pyridin derivatives as aldosterone synthase inhibitors

Family Applications After (1)

Application Number Title Priority Date Filing Date
CA002568159A Abandoned CA2568159A1 (en) 2004-05-28 2005-05-27 Tetrahydro-imidazo [1,5-a] pyridin derivatives as aldosterone synthase inhibitors

Country Status (10)

Country Link
US (2) US8680079B2 (https=)
EP (2) EP1749005A1 (https=)
JP (2) JP5179174B2 (https=)
CN (2) CN1968930A (https=)
AR (2) AR049125A1 (https=)
BR (2) BRPI0511621A (https=)
CA (2) CA2568163A1 (https=)
IL (2) IL179406A0 (https=)
TW (2) TW200616623A (https=)
WO (2) WO2005118540A2 (https=)

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JP5179174B2 (ja) * 2004-05-28 2013-04-10 ノバルティス ファーマ アーゲー アルドステロンシンターゼ阻害剤としてのテトラヒドロ−イミダゾ[1,5−a]ピリジン誘導体
TW200617010A (en) * 2004-07-09 2006-06-01 Speedel Experimenta Ag Organic compounds
TW200804378A (en) * 2005-12-09 2008-01-16 Speedel Experimenta Ag Organic compounds
AR060225A1 (es) * 2006-03-31 2008-06-04 Speedel Experimenta Ag Proceso para preparar 6,7- dihidro-5h-imidazo (1,5-a) piridin -8- ona
EP1842543A1 (en) 2006-04-05 2007-10-10 Speedel Pharma AG Pharmaceutical composition coprising an aldosterone synthase inhibitor and a mineralcorticoid receptor antagonist
TW200808812A (en) * 2006-04-12 2008-02-16 Speedel Experimenta Ag Imidazo compounds
TW200808813A (en) 2006-04-12 2008-02-16 Speedel Experimenta Ag Imidazo compounds
TW200813071A (en) 2006-04-12 2008-03-16 Speedel Experimenta Ag Spiro-imidazo compounds
JP4642922B2 (ja) * 2008-07-24 2011-03-02 明治製菓株式会社 ピリピロペンa生合成遺伝子
US9216221B2 (en) 2008-11-07 2015-12-22 University Of Sheffield Medicament and method of diagnosis for treating subclinical Cushing's syndrome
EP2426124B1 (en) 2009-05-13 2013-08-07 Meiji Seika Pharma Co., Ltd. Process for producing pyripyropene derivative
JP5466759B2 (ja) 2009-05-28 2014-04-09 ノバルティス アーゲー ネプリライシン阻害剤としての置換アミノ酪酸誘導体
SG176009A1 (en) 2009-05-28 2011-12-29 Novartis Ag Substituted aminopropionic derivatives as neprilysin inhibitors
US8519134B2 (en) * 2009-11-17 2013-08-27 Novartis Ag Aryl-pyridine derivatives as aldosterone synthase inhibitors
JO2967B1 (en) 2009-11-20 2016-03-15 نوفارتس ايه جي Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors
UA111151C2 (uk) 2010-03-01 2016-04-11 Мейдзі Сейка Фарма Ко., Лтд. Спосіб одержання похідних пірипіропену
US8877815B2 (en) 2010-11-16 2014-11-04 Novartis Ag Substituted carbamoylcycloalkyl acetic acid derivatives as NEP
US8673974B2 (en) 2010-11-16 2014-03-18 Novartis Ag Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors
SG10201605304VA (en) 2011-07-08 2016-08-30 Novartis Ag Method of treating atherosclerosis in high triglyceride subjects
CN103958478B (zh) * 2011-11-30 2017-08-01 霍夫曼-拉罗奇有限公司 双环二氢异喹啉‑1‑酮衍生物
UY35144A (es) 2012-11-20 2014-06-30 Novartis Ag Miméticos lineales sintéticos de apelina para el tratamiento de insuficiencia cardiaca
TR201808541T4 (tr) 2013-02-14 2018-07-23 Novartis Ag Nep (nötr endopeptidaz) inhibitörleri olarak ikame edilmiş bisfenil butanoik fosfonik asit türevleri.
HK1218252A1 (zh) 2013-07-25 2017-02-10 Novartis Ag 合成apelin多肽之生物结合物
KR20160031551A (ko) 2013-07-25 2016-03-22 노파르티스 아게 심부전의 치료를 위한 시클릭 폴리펩티드
CN105531263B (zh) * 2013-10-17 2019-08-23 豪夫迈·罗氏有限公司 作为醛固酮合酶抑制剂的苯基-二氢吡啶衍生物
CN105593212B (zh) * 2013-10-17 2019-06-04 豪夫迈·罗氏有限公司 作为醛固酮合酶抑制剂的苯基-二氢吡啶衍生物
JP6471153B2 (ja) * 2013-10-17 2019-02-13 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft アルドステロン合成酵素阻害剤としての新規フェニルジヒドロピリジン誘導体
MA41580A (fr) 2015-01-23 2017-11-29 Novartis Ag Conjugués d'acides gras de l'apeline synthétique présentant une demi-vie améliorée
JOP20190086A1 (ar) 2016-10-21 2019-04-18 Novartis Ag مشتقات نافثيريدينون جديدة واستخدامها في معالجة عدم انتظام ضربات القلب
WO2018165649A1 (en) 2017-03-10 2018-09-13 Embera Neurotherapeutics, Inc. Pharmaceutical compositions and uses thereof
UY38072A (es) 2018-02-07 2019-10-01 Novartis Ag Compuestos derivados de éster butanoico sustituido con bisfenilo como inhibidores de nep, composiciones y combinaciones de los mismos
JP7657151B2 (ja) 2018-11-27 2025-04-04 ノバルティス アーゲー 代謝性障害の処置のためのプロタンパク質コンバターゼスブチリシン/ケキシン9型(pcsk9)阻害剤としての環状ペプチド
JP2022507958A (ja) 2018-11-27 2022-01-18 ノバルティス アーゲー 代謝障害の治療用のプロタンパク質転換酵素サブチリシン/ケキシン9型(pcsk9)阻害薬としての環状四量体化合物
PY1998404A (es) 2018-11-27 2021-06-17 Novartis Ag Compuestos tetrámeros cíclicos como inhibidores de proproteína convertasa subtilisina/kexina tipo 9 (pcsk9) para el tratamiento de trastornos metabólicos
WO2023084449A1 (en) 2021-11-12 2023-05-19 Novartis Ag Diaminocyclopentylpyridine derivatives for the treatment of a disease or disorder
AR127698A1 (es) 2021-11-23 2024-02-21 Novartis Ag Derivados de naftiridinona para el tratamiento de una enfermedad o un trastorno
KR20260015867A (ko) 2023-05-24 2026-02-03 노파르티스 아게 질환 또는 장애 치료용 나프티리디논 유도체
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US7612088B2 (en) * 2004-05-28 2009-11-03 Speedel Experimenta Ag Heterocyclic compounds and their use as aldosterone synthase inhibitors
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TW200716634A (en) * 2005-05-31 2007-05-01 Speedel Experimenta Ag Heterocyclic spiro-compounds
TW200716105A (en) * 2005-05-31 2007-05-01 Speedel Experimenta Ag Imidazole compounds
TW200808812A (en) * 2006-04-12 2008-02-16 Speedel Experimenta Ag Imidazo compounds
TW200808813A (en) * 2006-04-12 2008-02-16 Speedel Experimenta Ag Imidazo compounds
TW200813071A (en) * 2006-04-12 2008-03-16 Speedel Experimenta Ag Spiro-imidazo compounds

Also Published As

Publication number Publication date
TW200616623A (en) 2006-06-01
WO2005118581A1 (en) 2005-12-15
TW200612947A (en) 2006-05-01
BRPI0510409A (pt) 2007-10-23
JP2008500997A (ja) 2008-01-17
EP1749005A1 (en) 2007-02-07
BRPI0511621A (pt) 2008-01-02
US8680079B2 (en) 2014-03-25
IL179408A0 (en) 2007-05-15
AR049126A1 (es) 2006-06-28
CN1968930A (zh) 2007-05-23
EP1765777A2 (en) 2007-03-28
US20070225232A1 (en) 2007-09-27
AR049125A1 (es) 2006-06-28
US20080076784A1 (en) 2008-03-27
IL179406A0 (en) 2007-05-15
JP2008501000A (ja) 2008-01-17
WO2005118540A2 (en) 2005-12-15
WO2005118540A3 (en) 2006-02-02
JP5179174B2 (ja) 2013-04-10
CN1960991A (zh) 2007-05-09
CA2568159A1 (en) 2005-12-15

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