PE20121439A1 - Derivados de pirazol que modulan la estearoil-coa-desaturasa - Google Patents

Derivados de pirazol que modulan la estearoil-coa-desaturasa

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Publication number
PE20121439A1
PE20121439A1 PE2012000427A PE2012000427A PE20121439A1 PE 20121439 A1 PE20121439 A1 PE 20121439A1 PE 2012000427 A PE2012000427 A PE 2012000427A PE 2012000427 A PE2012000427 A PE 2012000427A PE 20121439 A1 PE20121439 A1 PE 20121439A1
Authority
PE
Peru
Prior art keywords
alkyl
benzyl
pirazole
desaturase
coa
Prior art date
Application number
PE2012000427A
Other languages
English (en)
Inventor
Natalie Dales
Jianmin Fu
Qi Jia
Natalia Pokrovskaia
Shaoyi Sun
Zaihui Zhang
Original Assignee
Novartis Ag
Xenon Pharmaceuticals Inc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43066810&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20121439(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag, Xenon Pharmaceuticals Inc filed Critical Novartis Ag
Publication of PE20121439A1 publication Critical patent/PE20121439A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/10—Anti-acne agents
    • 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
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric 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
    • 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
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • 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
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Nutrition Science (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A UN COMPUESTO DERIVADO DE PIRAZOL DE FORMULA (I) DONDE: Q SE SELECCIONA ENTRE (A) Y( B); W ES -N(R8)C(O)-, -C(O)N(R8)-, ALQUILENO C1-6, ENTRE OTROS; V ES ALQUILENO C1-6; R1 ES H, ALQUILO C1-7 OPCIONALMENTE SUSTITUIDO, ALQUENILO C2-6, ALQUINILO C2-6, ALCOXILO C1-7, ENTRE OTROS; R2 ES ALQUILO C3-7, ALQUENILO C2-6, HIDROXILO, HIDROXI-ALQUILO C1-4, ENTRE OTROS; R3 ES H, ALQUILO C1-6, ALCOXILO C1-6, CICLOALQUILO C3-7, ENTRE OTROS; R8 ES H, ALQUILO C1-7, HIDROXI-ALQUILO C1-4, CICLOALQUILO C3-7; ENTRE OTROS; R5 Y R5a SON INDEPENDIENTEMENTE H, ALQUILO C1-6, HALO-ALQUILO C1-4, ENTRE OTROS O JUNTOS FORMAN UN GRUPO OXO O UN GRUPO CICLOALQUILO C3-7. R6 ES ALQUILO C1-6, ARILO C6-10, CICLOAQUILO C3-7, ENTRE OTROS; R7 ES H, ALQUILO C1-7, HALO-ALQUILO C1-4, ENTRE OTROS; n ES UN ENTERO DE 1 A 3; p ES UN ENTERO DE 0 A 6. SON COMPUESTOS PREFERIDOS: N-(3,4-DIFLUORO-BENCIL)-3-(1-(4-FLUORO-BENCIL)-5-OXO-1H-1,2,4-TRIAZOL-4(5H)-IL)-1H-PIRAZOL-5-CARBOXAMIDA; 3-(3-(4-FLUORO-BENCIL)-2-OXO-IMIDAZOLIN-1-IL)-N-((5-METIL-ISOXAZOL-3-IL)-METIL)-1H-PIRAZOL-5-CARBOXAMIDA; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES INHIBIDOR DE LA ENZIMA ESTEAROIL-COA-DESATURASA (SCD), SIENDO UTIL EN EL TRATAMIENTO DE DIABETES, OBESIDAD, ENFERMEDAD CARDIOVASCULAR, TRASTORNOS DERMATOLOGICOS
PE2012000427A 2009-10-01 2010-10-01 Derivados de pirazol que modulan la estearoil-coa-desaturasa PE20121439A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US24763409P 2009-10-01 2009-10-01

Publications (1)

Publication Number Publication Date
PE20121439A1 true PE20121439A1 (es) 2012-11-06

Family

ID=43066810

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2012000427A PE20121439A1 (es) 2009-10-01 2010-10-01 Derivados de pirazol que modulan la estearoil-coa-desaturasa

Country Status (22)

Country Link
US (1) US20130011361A1 (es)
EP (1) EP2483264A1 (es)
JP (1) JP2013506638A (es)
KR (1) KR20120080226A (es)
CN (1) CN102574841A (es)
AU (1) AU2010302577A1 (es)
BR (1) BR112012007509A2 (es)
CA (1) CA2776294A1 (es)
CL (1) CL2012000797A1 (es)
CO (1) CO6761294A2 (es)
CR (1) CR20120134A (es)
EA (1) EA201200545A1 (es)
EC (1) ECSP12011837A (es)
IL (1) IL218294A0 (es)
IN (1) IN2012DN01913A (es)
MA (1) MA33693B1 (es)
MX (1) MX2012003938A (es)
PE (1) PE20121439A1 (es)
SG (1) SG178869A1 (es)
TN (1) TN2012000085A1 (es)
WO (1) WO2011039358A1 (es)
ZA (1) ZA201201390B (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013056148A2 (en) 2011-10-15 2013-04-18 Genentech, Inc. Methods of using scd1 antagonists
US11970486B2 (en) 2016-10-24 2024-04-30 Janssen Pharmaceutica Nv Compounds and uses thereof
EP3566055A4 (en) 2017-01-06 2020-12-02 Yumanity Therapeutics, Inc. TREATMENT METHODS FOR NEUROLOGICAL DISORDERS
EP3700934A4 (en) 2017-10-24 2021-10-27 Yumanity Therapeutics, Inc. COMPOUNDS AND USES OF THESE COMPOUNDS
CA3094527A1 (en) * 2018-03-23 2019-09-26 Yumanity Therapeutics, Inc. Compounds and uses thereof
GB202012969D0 (en) * 2020-08-19 2020-09-30 Univ Of Oxford Inhibitor compounds

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60012721T4 (de) 1999-03-29 2010-09-09 Uutech Ltd., Coleraine Analoge des magensaft inhibierenden peptides und ihre verwendung für die behandlung von diabetes
WO2001023420A2 (en) 1999-09-28 2001-04-05 Bayer Corporation Pituitary adenylate cyclase activating peptide (pacap) receptor 3 (r3) agonists and their pharmacological methods of use
ATE475718T1 (de) 2000-02-24 2010-08-15 Xenon Pharmaceuticals Inc Stearoyl-coa-desaturase zur identifizierung von triglyceridreduktionstherapeutika
CA2430987A1 (en) 2000-09-26 2002-04-04 Xenon Genetics, Inc. Methods and compositions employing a novel stearoyl-coa desaturase-hscd5
EP2289510A1 (en) * 2004-09-20 2011-03-02 Xenon Pharmaceuticals Inc. Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-coa desaturase enzymes
EP1807085B1 (en) * 2004-09-20 2013-08-21 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
WO2007046867A2 (en) * 2005-05-19 2007-04-26 Xenon Pharmaceuticals Inc. Piperidine derivatives and their uses as therapeutic agents
ES2597453T3 (es) * 2006-08-15 2017-01-18 Xenon Pharmaceuticals Inc. Compuestos heterocíclicos adecuados para el tratamiento de enfermedades relacionadas con un elevado nivel de lípidos
CN101506203B (zh) * 2006-08-24 2013-10-16 诺瓦提斯公司 治疗代谢病、心血管病和其他病症的作为硬脂酰辅酶a脱饱和酶(scd)抑制剂的2-(吡嗪-2-基)-噻唑和2-(1h-吡唑-3-基)-噻唑衍生物及相关化合物
BRPI0718509A2 (pt) * 2006-09-22 2015-09-29 Novartis Ag compostos orgânicos heterocíclicos
US8068738B2 (en) * 2007-02-21 2011-11-29 Tte Technology, Inc. System and method for decoding infra-red (IR) signals
BRPI0907826A2 (pt) * 2008-02-20 2019-12-10 Novartis Ag inibidores heterocíclicos de estearoil-coa desaturase

Also Published As

Publication number Publication date
IN2012DN01913A (es) 2015-07-24
MA33693B1 (fr) 2012-10-01
SG178869A1 (en) 2012-04-27
TN2012000085A1 (en) 2013-09-19
CL2012000797A1 (es) 2013-08-09
BR112012007509A2 (pt) 2016-11-22
CO6761294A2 (es) 2013-09-30
KR20120080226A (ko) 2012-07-16
IL218294A0 (en) 2012-04-30
US20130011361A1 (en) 2013-01-10
WO2011039358A1 (en) 2011-04-07
EP2483264A1 (en) 2012-08-08
CA2776294A1 (en) 2011-04-07
ECSP12011837A (es) 2012-06-29
MX2012003938A (es) 2012-08-03
JP2013506638A (ja) 2013-02-28
ZA201201390B (en) 2012-10-31
CR20120134A (es) 2012-05-17
CN102574841A (zh) 2012-07-11
EA201200545A1 (ru) 2012-12-28
AU2010302577A1 (en) 2012-03-15

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