PE20071031A1 - Derivados de tiadiazolidinona como inhibidores de ptpasas - Google Patents

Derivados de tiadiazolidinona como inhibidores de ptpasas

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Publication number
PE20071031A1
PE20071031A1 PE2006001571A PE2006001571A PE20071031A1 PE 20071031 A1 PE20071031 A1 PE 20071031A1 PE 2006001571 A PE2006001571 A PE 2006001571A PE 2006001571 A PE2006001571 A PE 2006001571A PE 20071031 A1 PE20071031 A1 PE 20071031A1
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PE
Peru
Prior art keywords
ona
naphthalen
dioxo
hydrogen
tiadiazolidinone
Prior art date
Application number
PE2006001571A
Other languages
English (en)
Inventor
David Barnes
Gregory Raymond Bebernitz
Gary Mark Coppola
Katsumasa Nakajima
Travis Stams
Sidney Wolf Topiol
Thalaththani Ralalage Vedananda
James Richard Wareing
Original Assignee
Novartis Ag
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37950917&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20071031(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20071031A1 publication Critical patent/PE20071031A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/101,2,5-Thiadiazoles; Hydrogenated 1,2,5-thiadiazoles
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/433Thidiazoles
    • 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
    • A61P1/04Drugs 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
    • 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
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • 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
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    • 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
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61P35/00Antineoplastic agents
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    • 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
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    • 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/10Heterocyclic 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 two hetero rings linked by a carbon chain containing aromatic rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

REFERIDA A UN COMPUESTO DERIVADO DE TIADIAZOLIDINONA DE FORMULA (I), DONDE Q COMBINADO JUNTO CON LOS ATOMOS DE CARBONO CON LOS QUE ESTA UNIDO, FORMA UN ANILLO CARBOCICLICO O HETEROCICLICO DE 5 A 8 MIEMBROS, AROMATICO, O NO AROMATICO PARCIAL O COMPLETAMENTE SATURADO; R1 ES HIDROGENO, C(O)R6, C(O)NR7R8 O -C(O)OR9; R6 Y R7 SON HIDROGENO, CICLOALQUILO, ARILO, ARALQUILO, ENTRE OTROS; R8 Y R9 SON CICLOALQUILO, ARILO, ARALQUILO, ENTRE OTROS; R2, R3, R4 Y R5 SON HIDROGENO, HIDROXILO, HALOGENO, CIANO, NITRO, ALCOXILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 5-(3,6-DIHIDROXI-NAFTALEN-2-IL)-1,1-DIOXO-1,2,5-TIADIAZOLIDIN-3-ONA, SAL POTASICA DE 5-(3,7-DIHIDROXI-NAFTALEN-2-IL)-1,1-DIOXO-1,2,5-TIADIAZOLIDIN-3-ONA, 5-(7-BROMO-3-HIDROXI-NAFTALEN-2-IL)-1,1-DIOXO-1,2,5-TIADIAZOLIDIN-3-ONA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE LAS FOSFATASAS DE PROTEINA TIROSINA (PTPASAS) Y SON UTILES EN EL TRATAMIENTO DE LA RESISTENCIA A LA INSULINA ASOCIADA CON OBESIDAD, DIABETES MELLITUS, HIPERTENSION, HIPERTRIGLICERIDEMIA, ENTRE OTRAS
PE2006001571A 2005-12-08 2006-12-06 Derivados de tiadiazolidinona como inhibidores de ptpasas PE20071031A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US74857305P 2005-12-08 2005-12-08

Publications (1)

Publication Number Publication Date
PE20071031A1 true PE20071031A1 (es) 2007-11-15

Family

ID=37950917

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2010000531A PE20100733A1 (es) 2005-12-08 2006-12-06 Derivados de tiadiazolidinona como inhibidores de ptpasas
PE2006001571A PE20071031A1 (es) 2005-12-08 2006-12-06 Derivados de tiadiazolidinona como inhibidores de ptpasas

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2010000531A PE20100733A1 (es) 2005-12-08 2006-12-06 Derivados de tiadiazolidinona como inhibidores de ptpasas

Country Status (26)

Country Link
US (1) US7700633B2 (es)
EP (1) EP1963292B1 (es)
JP (1) JP2009519248A (es)
KR (1) KR20080074969A (es)
CN (1) CN101326173A (es)
AR (1) AR056838A1 (es)
AT (1) ATE546440T1 (es)
AU (1) AU2006321905B2 (es)
BR (1) BRPI0619600A2 (es)
CA (1) CA2629857A1 (es)
CR (1) CR10049A (es)
EC (1) ECSP088506A (es)
ES (1) ES2381280T3 (es)
IL (1) IL191549A0 (es)
MA (1) MA30202B1 (es)
NO (1) NO20083031L (es)
NZ (1) NZ568243A (es)
PE (2) PE20100733A1 (es)
PL (1) PL1963292T3 (es)
PT (1) PT1963292E (es)
RU (1) RU2008127254A (es)
TN (1) TNSN08249A1 (es)
TW (1) TW200732315A (es)
UA (1) UA94724C2 (es)
WO (1) WO2007067615A2 (es)
ZA (1) ZA200804074B (es)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA94921C2 (en) * 2005-12-08 2011-06-25 Новартис Аг 1-orthofluorophenyl substituted 1, 2, 5-thiazolidinedione derivatives as ptp-as inhibitors
JP2009518421A (ja) * 2005-12-08 2009-05-07 ノバルティス アクチエンゲゼルシャフト 1,1,3−トリオキソ−1,2,5−チアジアゾリジンおよびPTPase阻害剤としてのそれらの使用
EP1963294B1 (en) * 2005-12-08 2012-10-10 Novartis AG 1,2,5-thiazolidine derivatives useful for treating conditions mediated by protein tyrosine phosphatases (ptpase)
WO2008067527A1 (en) * 2006-12-01 2008-06-05 Novartis Ag Inhibitors of protein tyrosine phosphatase for the treatment of muscle atrophy and related disorders
AR066820A1 (es) * 2007-06-04 2009-09-16 Novartis Ag Compuestos de tiadiazolidin-3 ona
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
JP5809157B2 (ja) 2010-10-08 2015-11-10 持田製薬株式会社 環状アミド誘導体
AU2012248627A1 (en) 2011-04-28 2013-11-14 Mochida Pharmaceutical Co., Ltd. Cyclic amide derivative
WO2020127924A1 (en) * 2018-12-21 2020-06-25 Bionice, S.L.U. Process and intermediates for the preparation of voxelotor
CN114025844B (zh) * 2019-03-14 2022-07-26 卡里科生命科学有限责任公司 蛋白酪氨酸磷酸酶抑制剂及其使用方法
GB201915094D0 (en) * 2019-10-18 2019-12-04 Balticgruppen Bio Ab New formulations
WO2021127586A1 (en) * 2019-12-20 2021-06-24 Calico Life Sciences Llc Protein tyrosine phosphatase degraders and methods of use thereof
WO2022192598A1 (en) * 2021-03-11 2022-09-15 Kumquat Biosciences Inc. Heterocycles and uses thereof
CA3236854A1 (en) * 2021-11-11 2023-05-19 Andrew Bogdan Protein tyrosine phosphatase inhibitors and methods of use thereof
WO2023150150A1 (en) * 2022-02-02 2023-08-10 Nerio Therapeutics, Inc. Protein tyrosine phosphatase inhibitors and uses thereof
WO2023150523A1 (en) * 2022-02-02 2023-08-10 Nerio Therapeutics, Inc. Protein tyrosine phosphatase inhibitors and uses thereof
TW202337459A (zh) * 2022-02-02 2023-10-01 美商耐瑞歐醫療公司 蛋白酪胺酸磷酸酶抑制劑及其用途
WO2024059041A1 (en) * 2022-09-13 2024-03-21 Kumquat Biosciences, Inc. Benzo-fused n-heterocycles and uses thereof
WO2024067802A1 (zh) * 2022-09-30 2024-04-04 深圳众格生物科技有限公司 蛋白酪氨酸磷酸酶抑制剂及其制备方法和医药用途
CN117343052B (zh) * 2023-12-04 2024-02-06 英矽智能科技(上海)有限公司 蛋白酪氨酸磷酸酶抑制剂及其应用

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1492780B1 (en) 2002-04-03 2011-11-23 Novartis AG 5-substituted 1,1-dioxo-¬1,2,5 thiazolidine-3-one derivatives as ptpase 1b inhibitors
GB0225986D0 (en) * 2002-11-07 2002-12-11 Astrazeneca Ab Chemical compounds
GB0227813D0 (en) * 2002-11-29 2003-01-08 Astrazeneca Ab Chemical compounds
EP1594497B1 (en) * 2002-12-30 2009-05-27 Vertex Pharmaceuticals Incorporated Sulfhydantoins as phosphate isosteres for use as phosphatase inhibitors in the treatment of cancer and autoimmune disorders
US7141596B2 (en) * 2003-10-08 2006-11-28 Incyte Corporation Inhibitors of proteins that bind phosphorylated molecules
JP2009518421A (ja) 2005-12-08 2009-05-07 ノバルティス アクチエンゲゼルシャフト 1,1,3−トリオキソ−1,2,5−チアジアゾリジンおよびPTPase阻害剤としてのそれらの使用
EP1963294B1 (en) 2005-12-08 2012-10-10 Novartis AG 1,2,5-thiazolidine derivatives useful for treating conditions mediated by protein tyrosine phosphatases (ptpase)
EP2038267A2 (en) 2006-03-31 2009-03-25 Novartis AG Thiadiazolidinone inhibitors of ptpase

Also Published As

Publication number Publication date
JP2009519248A (ja) 2009-05-14
AU2006321905A1 (en) 2007-06-14
MA30202B1 (fr) 2009-02-02
ZA200804074B (en) 2009-03-25
US7700633B2 (en) 2010-04-20
TW200732315A (en) 2007-09-01
IL191549A0 (en) 2008-12-29
PL1963292T3 (pl) 2012-07-31
NO20083031L (no) 2008-08-28
ECSP088506A (es) 2008-07-30
AR056838A1 (es) 2007-10-24
CN101326173A (zh) 2008-12-17
EP1963292A2 (en) 2008-09-03
TNSN08249A1 (en) 2009-10-30
NZ568243A (en) 2011-07-29
CA2629857A1 (en) 2007-06-14
WO2007067615A2 (en) 2007-06-14
WO2007067615A3 (en) 2007-11-15
KR20080074969A (ko) 2008-08-13
AU2006321905B2 (en) 2011-08-11
ES2381280T3 (es) 2012-05-24
RU2008127254A (ru) 2010-01-20
CR10049A (es) 2008-08-25
US20080262050A1 (en) 2008-10-23
ATE546440T1 (de) 2012-03-15
EP1963292B1 (en) 2012-02-22
PT1963292E (pt) 2012-05-10
BRPI0619600A2 (pt) 2011-10-11
PE20100733A1 (es) 2010-10-29
UA94724C2 (en) 2011-06-10

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