CA2568929A1 - Phosphodiesterase 10 inhibition as treatment for obesity-related and metabolic syndrome-related conditions - Google Patents

Phosphodiesterase 10 inhibition as treatment for obesity-related and metabolic syndrome-related conditions Download PDF

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Publication number
CA2568929A1
CA2568929A1 CA002568929A CA2568929A CA2568929A1 CA 2568929 A1 CA2568929 A1 CA 2568929A1 CA 002568929 A CA002568929 A CA 002568929A CA 2568929 A CA2568929 A CA 2568929A CA 2568929 A1 CA2568929 A1 CA 2568929A1
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CA
Canada
Prior art keywords
pde10
antagonist
dimethoxy
subject
quinazoline
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
CA002568929A
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English (en)
French (fr)
Inventor
Shawn Clive Black
Earl Michael Gibbs
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.)
Pfizer Products Inc
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2568929A1 publication Critical patent/CA2568929A1/en
Abandoned legal-status Critical Current

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    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/48—Ergoline derivatives, e.g. lysergic acid, ergotamine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/2264—Obesity-gene products, e.g. leptin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P3/08—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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Zoology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Genetics & Genomics (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
CA002568929A 2004-06-07 2005-05-30 Phosphodiesterase 10 inhibition as treatment for obesity-related and metabolic syndrome-related conditions Abandoned CA2568929A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US57753504P 2004-06-07 2004-06-07
US60/577,535 2004-06-07
PCT/IB2005/001755 WO2005120514A1 (en) 2004-06-07 2005-05-30 Phosphodiesterase 10 inhibition as treatment for obesity-related and metabolic syndrome-related conditions

Publications (1)

Publication Number Publication Date
CA2568929A1 true CA2568929A1 (en) 2005-12-22

Family

ID=34970641

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002568929A Abandoned CA2568929A1 (en) 2004-06-07 2005-05-30 Phosphodiesterase 10 inhibition as treatment for obesity-related and metabolic syndrome-related conditions

Country Status (8)

Country Link
US (1) US20090162286A1 (enExample)
EP (1) EP1755611A1 (enExample)
JP (1) JP2008501776A (enExample)
BR (1) BRPI0511854A (enExample)
CA (1) CA2568929A1 (enExample)
MX (1) MXPA06014236A (enExample)
TW (1) TW200612957A (enExample)
WO (1) WO2005120514A1 (enExample)

Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060183763A1 (en) * 2004-12-31 2006-08-17 Pfizer Inc Novel pyrrolidyl derivatives of heteroaromatic compounds
EA012211B1 (ru) * 2005-01-07 2009-08-28 Пфайзер Продактс Инк. Гетероароматические соединения хинолинов и их применение в качестве ингибиторов pde10
NL2000397C2 (nl) * 2006-01-05 2007-10-30 Pfizer Prod Inc Bicyclische heteroarylverbindingen als PDE10 inhibitoren.
WO2007098169A1 (en) * 2006-02-21 2007-08-30 Amgen Inc. Cinnoline derivatives as phosphodiesterase 10 inhibitors
AU2007221049A1 (en) * 2006-02-28 2007-09-07 Amgen Inc. Cinnoline and quinazoline derivates as phosphodiesterase 10 inhibitors
JP2009535394A (ja) * 2006-05-02 2009-10-01 ファイザー・プロダクツ・インク Ｐｄｅ１０阻害剤としての二環式ヘテロアリール化合物
WO2008001182A1 (en) * 2006-06-26 2008-01-03 Pfizer Products Inc. Tricyclic heteroaryl compounds as pde10 inhibitors
US20080090834A1 (en) * 2006-07-06 2008-04-17 Pfizer Inc Selective azole pde10a inhibitor compounds
WO2008020302A2 (en) * 2006-08-17 2008-02-21 Pfizer Products Inc. Heteroaromatic quinoline-based compounds as phosphodiesterase (pde) inhibitors
UA100497C2 (ru) 2006-09-07 2013-01-10 Никомед Гмбх Комбинированное лечение сахарного диабета
US7786139B2 (en) 2006-11-21 2010-08-31 Omeros Corporation PDE10 inhibitors and related compositions and methods
KR101560844B1 (ko) 2007-06-04 2015-10-15 벤-구리온 유니버시티 오브 더 네게브 리서치 앤드 디벨럽먼트 어쏘러티 트라이-아릴계 화합물 및 이를 포함하는 조성물
WO2009029214A1 (en) * 2007-08-23 2009-03-05 Amgen Inc. Isoquinolone derivatives as phosphodiesterase 10 inhibitors
TW200918519A (en) * 2007-09-19 2009-05-01 Lundbeck & Co As H Cyanoisoquinoline
US7858620B2 (en) 2007-09-19 2010-12-28 H. Lundbeck A/S Cyanoisoquinoline
WO2009068246A2 (en) * 2007-11-30 2009-06-04 Elbion Gmbh Methods of treating obesity and metabolic disorders
WO2009070584A1 (en) 2007-11-30 2009-06-04 Wyeth Aryl and heteroaryl fused imidazo[1,5-a]pyrazines as inhibitors of phosphodiesterase 10
KR20100121527A (ko) 2008-02-29 2010-11-17 콘서트 파마슈티컬즈, 인크. 치환된 잔틴 유도체
WO2010145668A1 (en) 2009-06-19 2010-12-23 H. Lundbeck A/S Novel phenylimidazole derivative as pde10a enzyme inhibitor
EP2342191B1 (en) 2008-09-10 2013-03-20 Mitsubishi Tanabe Pharma Corporation Aromatic nitrogen-containing 6-membered ring compounds and their use
EP2348018A4 (en) 2008-09-25 2012-04-25 Kyorin Seiyaku Kk HETEROCYCLIC BIARYL DERIVATIVE AND PDE INHIBITOR CONTAINING ACTIVE SUBSTANCE
US20110224250A1 (en) * 2008-10-09 2011-09-15 Yasushi Kohno Isoquinoline derivative, and pde inhibitor comprising same as active ingredient
TWI396689B (zh) * 2008-11-14 2013-05-21 Amgen Inc 作為磷酸二酯酶１０抑制劑之吡衍生物
MY170610A (en) 2009-02-05 2019-08-20 Takeda Pharmaceuticals Co Pyridazinone compounds
US20110053961A1 (en) 2009-02-27 2011-03-03 Concert Pharmaceuticals, Inc. Substituted xanthine derivatives
WO2010138833A1 (en) 2009-05-29 2010-12-02 Wyeth SUBSTITUTED IMIDAZO[1,5-a]QUINOXALINES AS INHIBITORS OF PHOSPHODIESTERASE 10
TW201200516A (en) 2009-12-17 2012-01-01 Lundbeck & Co As H Phenylimidazole derivatives comprising an ethynylene linker as PDE10A enzyme inhibitors
TWI485151B (zh) 2009-12-17 2015-05-21 Lundbeck & Co As H 作為ｐｄｅ１０ａ酵素抑制劑之雜芳香族苯基咪唑衍生物
TWI481607B (zh) 2009-12-17 2015-04-21 Lundbeck & Co As H 作為ｐｄｅ１０ａ酵素抑制劑的２－芳基咪唑衍生物
TWI487705B (zh) * 2009-12-17 2015-06-11 Lundbeck & Co As H 作為ｐｄｅ１０ａ酵素抑制劑之雜芳香族芳基三唑衍生物
TWI476200B (zh) 2010-02-26 2015-03-11 Mitsubishi Tanabe Pharma Corp 吡唑並嘧啶化合物及其充作ｐｄｅ１０抑制劑之用途
TW201215607A (en) 2010-07-02 2012-04-16 Lundbeck & Co As H Aryl-and heteroarylamid derivatives as PDE10A enzyme inhibitor
TW201206935A (en) 2010-07-16 2012-02-16 Lundbeck & Co As H Triazolo-and pyrazoloquinazoline derivatives as PDE10A enzyme inhibitor
JO3089B1 (ar) 2010-11-19 2017-03-15 H Lundbeck As مشتقات ايميدازول كمثبطات لانزيمات pde10a
MX2013009575A (es) 2011-02-18 2014-10-14 Exonhit Therapeutics Sa Derivados de 6, 7-dialcoxi-3-isoquinolinol sustituidos como inhibidores de fosfodiesterasa 10 (pdei0a).
US9938269B2 (en) 2011-06-30 2018-04-10 Abbvie Inc. Inhibitor compounds of phosphodiesterase type 10A
WO2013013052A1 (en) 2011-07-19 2013-01-24 Concert Pharmaceuticals, Inc. Substituted xanthine derivatives
WO2013028590A1 (en) 2011-08-25 2013-02-28 Merck Sharp & Dohme Corp. Pyrimidine pde10 inhibitors
WO2013045607A1 (en) 2011-09-30 2013-04-04 H. Lundbeck A/S Quinazoline linked heteroaromatic tricycle derivatives as pde10a enzyme inhibitors
WO2013050527A1 (en) 2011-10-05 2013-04-11 H. Lundbeck A/S Quinazoline derivatives as pde10a enzyme inhibitors
BR112014011173A2 (pt) 2011-11-09 2017-05-09 Abbvie Deutschland carboxamidas heterocíclicas úteis como inibidores de fosfodiesterase tipo 10a
US20130116241A1 (en) 2011-11-09 2013-05-09 Abbvie Inc. Novel inhibitor compounds of phosphodiesterase type 10a
TWI570124B (zh) 2011-12-21 2017-02-11 Ｈ 朗德貝克公司 作為ｐｄｅ１０ａ酵素抑制劑的喹啉衍生物
WO2013127817A1 (en) 2012-02-27 2013-09-06 H. Lundbeck A/S Imidazole derivatives as pde10a enzyme inhibitors
US9464085B2 (en) 2012-08-17 2016-10-11 AbbVie Deutschland GmbH & Co. KG Inhibitor compounds of phosphodiesterase type 10A
IN2015DN01900A (enExample) 2012-09-17 2015-08-07 Abbvie Deutschland
WO2014071044A1 (en) 2012-11-01 2014-05-08 Allergan, Inc. Substituted 6,7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde10a)
US9790203B2 (en) 2012-11-26 2017-10-17 Abbvie Inc. Inhibitor compounds of phosphodiesterase type 10A
US9200005B2 (en) 2013-03-13 2015-12-01 AbbVie Deutschland GmbH & Co. KG Inhibitor compounds of phosphodiesterase type 10A
WO2014140184A1 (en) 2013-03-14 2014-09-18 AbbVie Deutschland GmbH & Co. KG Novel inhibitor compounds of phosphodiesterase type 10a
US9249163B2 (en) 2013-06-11 2016-02-02 Janssen Pharmaceutica Nv. PDE10a inhibitors for the treatment of type II diabetes
WO2014200882A1 (en) 2013-06-11 2014-12-18 Janssen Pharmaceutica Nv PDE10a INHIBITORS FOR THE TREATMENT OF TYPE II DIABETES
US9453002B2 (en) 2013-08-16 2016-09-27 Janssen Pharmaceutica Nv Substituted imidazoles as N-type calcium channel blockers
WO2015061280A1 (en) 2013-10-21 2015-04-30 Alevere Medical Corporation Fused heterocyclic organic compounds, pharmaceutical compositions, and medical uses thereof
EA201690938A1 (ru) 2013-11-05 2016-11-30 Бен-Гурион Юниверсити Оф Дзе Негев Рисерч Энд Дивелопмент Оторити Соединения для лечения диабета и осложнений, возникающих из-за этого заболевания
US9200016B2 (en) 2013-12-05 2015-12-01 Allergan, Inc. Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE 10A)
JP6026706B2 (ja) * 2014-04-09 2016-11-16 ゴールドクレスト医薬研究所株式会社 皮膚症状の改善剤、育毛剤又はスリミング剤
US20170216296A1 (en) 2014-04-18 2017-08-03 Concert Pharmaceuticals, Inc. Methods of treating hyperglycemia
US20180038869A1 (en) * 2014-08-06 2018-02-08 Nestec S.A. Biomarkers for predicting degree of weight loss
WO2026068583A1 (en) * 2024-09-25 2026-04-02 Noema Pharma Ag Use of phosphodiesterase 10 inhibitor gemlapodect for weight loss

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE108064T1 (de) * 1987-10-08 1994-07-15 Andor Bilas Stoffgemisch zur stabilisierung der stoffwechsel- lage.
ATE273996T1 (de) * 1997-09-12 2004-09-15 Pharis Biotec Gmbh Zusammensetzung zur therapie von diabetes mellitus und fettsucht
IL149106A0 (en) * 2001-04-20 2002-11-10 Pfizer Prod Inc Therapeutic use of selective pde10 inhibitors
US20030032579A1 (en) * 2001-04-20 2003-02-13 Pfizer Inc. Therapeutic use of selective PDE10 inhibitors
CA2530114A1 (en) * 2003-06-30 2005-01-13 Altana Pharma Ag Pyrrolo-dihydroisoquinoline derivatives as pde10 inhibitors
WO2005012485A2 (en) * 2003-07-31 2005-02-10 Bayer Pharmaceuticals Corporation Methods for treating diabetes and related disorders using pde10a inhibitors

Also Published As

Publication number Publication date
MXPA06014236A (es) 2007-02-14
BRPI0511854A (pt) 2008-01-15
TW200612957A (en) 2006-05-01
US20090162286A1 (en) 2009-06-25
EP1755611A1 (en) 2007-02-28
JP2008501776A (ja) 2008-01-24
WO2005120514A1 (en) 2005-12-22

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EEER Examination request
FZDE Discontinued