AR078351A1 - Inhibidores de la hsl para el tratamiento de la diabetes - Google Patents

Inhibidores de la hsl para el tratamiento de la diabetes

Info

Publication number
AR078351A1
AR078351A1 ARP100103302A ARP100103302A AR078351A1 AR 078351 A1 AR078351 A1 AR 078351A1 AR P100103302 A ARP100103302 A AR P100103302A AR P100103302 A ARP100103302 A AR P100103302A AR 078351 A1 AR078351 A1 AR 078351A1
Authority
AR
Argentina
Prior art keywords
piperidine
phenyl
methoxy
benzenesulfonyl
carboxylic acid
Prior art date
Application number
ARP100103302A
Other languages
English (en)
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR078351A1 publication Critical patent/AR078351A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/96Sulfur atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Proceso de obtencion, composiciones farmacéuticas y usos. Reivindicacion 1: Compuesto de la formula (1) en la que R1 es dimetilpropilo, dimetilbutilo, ciclopropilalquilo, pirazolilo, metil-trifluorometil-1H-pirazolilo, morfolinilo, fenilo, 2-clorofenilo, 4-metilfenilo o 4-metoxifenilo; R2 es hidrogeno, alquilo, hidroxialquilo o alcoxialquilo; R3 es hidrogeno, alquilo, hidroxialquilo o alcoxialquilo; R4 es hidrogeno, halogeno, alquilo, hidroxialquilo o alcoxialquilo; R5 es hidrogeno o alquilo; R6 es 2,3-dihidro-benzofuranilo, alquilpiridin-3-ilo, haloalcoxipiridin-3-ilo, piridazinilo, alcoxipiridazinilo, alquil-trifluorometil-1H-pirazolilo, fenilo o fenilo sustituido, dicho fenilo sustituido es un fenilo sustituido en la posicion 4 por un sustituyente elegido entre cloro, isopropilo, hidroxialquilo, isopropoxi, cicloalquilalcoxi, haloalcoxi, haloalcoxialquilo, alcoxicarbonilalcoxi, carboxialcoxi, hidroxialcoxi, alcoxihaloalcoxi e hidroxihaloalcoxi y, dicho fenilo sustituido en la posicion 4 está además opcionalmente sustituido por un sustituyente elegido con independencia entre fluor, trifluormetoxi, alcoxicarbonilalcoxi e hidroxialcoxicarbonilo, pero en el caso, en el que R6 sea fenilo o fenilo sustituido en la posicion 4 por cloro, entonces A2 es G; A1 es carbonilo o -S(O)2-; A2 es un enlace sencillo, -CH2CH2- o G; G es un resto de formula (2); n es el numero cero, 1, 2, 3, 4 o 5; y sus sales farmacéuticamente aceptables; con la condicion de que se excluyan la (4-trifluorometoxi-fenil)-amida del ácido 1-(tolueno-4-sulfonil)-piperidina-4-carboxílico; [2-(4-difluorometoxi-fenil)-etil]-amida del ácido 1-(tolueno-4-sulfonil)-piperidina-4-carboxílico; (4-iso-propil-fenil)-amida del ácido 1-bencenosulfonil-piperidina-4-carboxílico; (4-isopropil-fenil)-amida del ácido 1-(tolueno-4-sulfonil)-piperidina-4-carboxílico (4-trifluorometoxi-fenil)-amida del ácido 1-(4-metoxi-bencenosulfonil)-piperidina-4-carboxílico; (4-trifluorometoxi-fenil]-amida del ácido 1-bencenosulfonil-piperidina-4-carboxílico; (4-difluoro-metoxi-fenil)-amida del ácido 1-(4-metoxi-bencenosulfonil)-piperidina-4-carboxílico; (4-isopropil-fenil)-amida del ácido 1-(4-metoxi-bencenosulfonil)-piperidina-4-carboxílico; (4-cloro-2-fluor-fenil)-amida del ácido 1-(4-metoxi-benceno-sulfonil)-piperidina-4-carboxílico; (4-isopropil-fenil)-amida del ácido 1-benzoil-piperidina-4-carboxílico; (4-isopropil-fenil)-amida del ácido 1-(2-cloro-benzoil)-piperidina-4-carboxílico; (1-fenil-ciclopropilmetil)-amida del ácido 1-bencenosulfonil-piperidina-4-carboxílico y (1-fenil-ciclo-pentilmetil)-amida del ácido 1-(tolueno-4-sulfonil)-piperidina-4-carboxílico.
ARP100103302A 2009-09-11 2010-09-09 Inhibidores de la hsl para el tratamiento de la diabetes AR078351A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09170071 2009-09-11

Publications (1)

Publication Number Publication Date
AR078351A1 true AR078351A1 (es) 2011-11-02

Family

ID=42983383

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100103302A AR078351A1 (es) 2009-09-11 2010-09-09 Inhibidores de la hsl para el tratamiento de la diabetes

Country Status (17)

Country Link
US (1) US8258158B2 (es)
EP (1) EP2475644B1 (es)
JP (1) JP5642793B2 (es)
KR (1) KR101369551B1 (es)
CN (1) CN102498099B (es)
AR (1) AR078351A1 (es)
AU (1) AU2010294326A1 (es)
BR (1) BR112012005140A2 (es)
CA (1) CA2771452A1 (es)
ES (1) ES2445166T3 (es)
HK (1) HK1169993A1 (es)
IL (1) IL217966A0 (es)
IN (1) IN2012DN01232A (es)
MX (1) MX2012002597A (es)
SG (1) SG179031A1 (es)
TW (1) TW201114744A (es)
WO (1) WO2011029808A1 (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5951650B2 (ja) 2011-03-18 2016-07-13 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH N−(3−カルバモイルフェニル)−1h−ピラゾール−5−カルボキサミド誘導体及び害虫を防除するためのそれらの使用
WO2014037327A1 (en) * 2012-09-10 2014-03-13 Boehringer Ingelheim International Gmbh N-cyclopropyl-n-piperidinyl-amides, pharmaceutical compositions containing them, and uses thereof
US10793522B2 (en) * 2016-12-09 2020-10-06 Boehringer Ingelheim International Gmbh Sulfonamides as inhibitors of the uptake of extracellular citrate
GB2560713A (en) * 2017-03-20 2018-09-26 Eternygen Gmbh Inhibitor of citrate transporter
CN110003177B (zh) * 2019-05-28 2021-11-19 沈阳药科大学 含有脲基的苯并咪唑类化合物及应用
CN110003176B (zh) * 2019-05-28 2021-12-21 沈阳药科大学 含有酰胺的苯并咪唑类化合物及其应用
GB201918410D0 (en) * 2019-12-13 2020-01-29 Z Factor Ltd Compounds and their use for the treatment of alpha1-antitrypsin deficiency
WO2022130352A1 (en) * 2020-12-19 2022-06-23 Cadila Healthcare Limited Novel compounds suitable for the treatment of dyslipidemia
GB202108523D0 (en) 2021-06-15 2021-07-28 Z Factor Ltd Compositions and their use for the treatment of alpha1-antitrypsin deficiency

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3779339B2 (ja) 1994-03-04 2006-05-24 三井化学株式会社 含フッ素カルボン酸エステル化合物、液晶材料、液晶組成物および液晶素子
EP1087937A1 (en) * 1998-06-17 2001-04-04 Du Pont Pharmaceuticals Company Cyclic hydroxamic acids as metalloproteinase inhibitors
US7071213B2 (en) 2001-11-14 2006-07-04 Schering Corporation Cannabinoid receptor ligands
MX2007010532A (es) * 2005-03-03 2007-10-12 Hoffmann La Roche Derivados de amida de acido 1-sulfonil-piperidina-3-carboxilico como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa para el tratamiento de diabetes mellitus tipo ii.
JP2009526761A (ja) * 2006-01-30 2009-07-23 アレイ バイオファーマ、インコーポレイテッド ヘテロ二環式チオフェン化合物および使用の方法
WO2007144394A2 (en) * 2006-06-16 2007-12-21 High Point Pharmaceuticals, Llc. Pharmaceutical use of substituted piperidine carboxamides
EP1958631A1 (en) 2007-02-14 2008-08-20 AEterna Zentaris GmbH Novel triazole derivatives as ligands of G-protein coupled receptors
US8324250B2 (en) 2009-03-19 2012-12-04 Hoffmann-La Roche Inc. Piperidine derivatives as NK3 receptor antagonists
US8329904B2 (en) * 2009-05-12 2012-12-11 Hoffmann-La Roche Inc. Azacyclic derivatives
US8399676B2 (en) * 2009-07-30 2013-03-19 Hoffman-La Roche Inc. Piperidine derivatives

Also Published As

Publication number Publication date
IN2012DN01232A (es) 2015-05-15
US20110065707A1 (en) 2011-03-17
HK1169993A1 (en) 2013-02-15
MX2012002597A (es) 2012-04-02
IL217966A0 (en) 2012-03-29
KR101369551B1 (ko) 2014-03-04
ES2445166T3 (es) 2014-02-28
JP2013504533A (ja) 2013-02-07
EP2475644A1 (en) 2012-07-18
CN102498099A (zh) 2012-06-13
TW201114744A (en) 2011-05-01
KR20120059617A (ko) 2012-06-08
CA2771452A1 (en) 2011-03-17
US8258158B2 (en) 2012-09-04
WO2011029808A1 (en) 2011-03-17
SG179031A1 (en) 2012-04-27
CN102498099B (zh) 2014-10-29
EP2475644B1 (en) 2014-01-08
AU2010294326A1 (en) 2012-03-08
JP5642793B2 (ja) 2014-12-17
BR112012005140A2 (pt) 2016-05-03

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