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

Info

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
Authority
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
Other languages
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

Links

Classifications

    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Zoology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Hematology (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 (61)

* 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
WO2006072828A2 (en) * 2005-01-07 2006-07-13 Pfizer Products Inc. Heteroaromatic quinoline compounds and their use as pde10 inhibitors
NL2000397C2 (nl) * 2006-01-05 2007-10-30 Pfizer Prod Inc Bicyclische heteroarylverbindingen als PDE10 inhibitoren.
MX2008010668A (es) * 2006-02-21 2008-10-01 Amgen Inc Derivados de cinolina como inhibidores de fosfodiesterasa 10.
WO2007100880A1 (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
CA2654394A1 (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
MEP8509A (en) 2006-09-07 2011-12-20 Combination treatment for diabetes mellitus
US7786139B2 (en) 2006-11-21 2010-08-31 Omeros Corporation PDE10 inhibitors and related compositions and methods
PT2152663E (pt) 2007-06-04 2014-06-03 Univ Ben Gurion Compostos de triarilo e composições que compreendem os mesmos
US20090054434A1 (en) * 2007-08-23 2009-02-26 Amgen Inc. Isoquinolone derivatives as phosphodiesterase 10 inhibitors
US7858620B2 (en) 2007-09-19 2010-12-28 H. Lundbeck A/S Cyanoisoquinoline
TW200918519A (en) * 2007-09-19 2009-05-01 Lundbeck & Co As H Cyanoisoquinoline
EP2225248A1 (en) 2007-11-30 2010-09-08 Wyeth LLC Aryl and heteroaryl fused imidazo[1,5-a]pyrazines as inhibitors of phosphodiesterase 10
US20090143392A1 (en) * 2007-11-30 2009-06-04 Elbion Gmbh Methods of Treating Obesity and Metabolic Disorders
KR20100121527A (ko) 2008-02-29 2010-11-17 콘서트 파마슈티컬즈, 인크. 치환된 잔틴 유도체
WO2010030027A1 (en) 2008-09-10 2010-03-18 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
EP2351748A4 (en) 2008-10-09 2012-03-21 Kyorin Seiyaku Kk ISOCHINOLINE DERIVATIVES AND THESE PDE INHIBITORS CONTAINING ACTIVE SUBSTANCE
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
BRPI1008498B8 (pt) 2009-02-05 2021-05-25 Takeda Pharmaceuticals Co compostos de piridazinona úteis como inibidores da fosfodiesterase 10a, composição farmacêutica, e, uso de um composto
US20110053961A1 (en) 2009-02-27 2011-03-03 Concert Pharmaceuticals, Inc. Substituted xanthine derivatives
TW201111383A (en) 2009-05-29 2011-04-01 Wyeth Llc Substituted imidazo[1,5-a]quinoxalines as inhibitors of phosphodiesterase 10
PT2443105E (pt) 2009-06-19 2015-01-14 Lundbeck & Co As H Novo derivado de fenilimidazole como inibidor da enzima pde10a
TW201200516A (en) 2009-12-17 2012-01-01 Lundbeck & Co As H Phenylimidazole derivatives comprising an ethynylene linker as PDE10A enzyme inhibitors
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
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
PH12012501643A1 (en) 2010-02-26 2017-07-19 Mitsubishi Tanabe Pharma Corp Pyrazolopyrimidine compounds and their use as pde 10 inhibitors
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
WO2012112946A1 (en) 2011-02-18 2012-08-23 Allergan, Inc. Substituted 6,7-dialkoxy-3-isoquinolinol derivatives as inhibitors of phosphodiesterase 10 (pde10a)
US9938269B2 (en) 2011-06-30 2018-04-10 Abbvie Inc. Inhibitor compounds of phosphodiesterase type 10A
US20140296263A1 (en) 2011-07-19 2014-10-02 Concert Pharmaceuticals, Inc. Substituted xanthine derivatives
CA2845578C (en) 2011-08-25 2016-02-16 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
HK1206728A1 (en) 2012-09-17 2016-01-15 AbbVie Deutschland GmbH & Co. KG Novel inhibitor compounds of phosphodiesterase type 10a
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
MX2015012008A (es) 2013-03-14 2016-04-15 Abbvie Deutschland Compuestos inhibidores novedosos de fosfodiesterasa tipo 10a.
WO2014200885A1 (en) 2013-06-11 2014-12-18 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
AU2014340351B2 (en) 2013-10-21 2020-01-30 Alevere Medical Corporation Fused heterocyclic organic compounds, pharmaceutical compositions, and medical uses thereof
EP3065723B1 (en) 2013-11-05 2020-09-23 Ben Gurion University of the Negev Research and Development Authority Compounds for the treatment of diabetes and disease complications arising from same
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
WO2015160913A1 (en) 2014-04-18 2015-10-22 Concert Pharmaceuticals, Inc. Methods of treating hyperglycemia
EP3177933B1 (en) * 2014-08-06 2020-02-19 Société des Produits Nestlé S.A. Biomarkers for predicting degree of weight loss
GB202110990D0 (en) * 2021-07-30 2021-09-15 Benevolentai Cambridge Ltd Organic compound and their uses
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
EP0339054B1 (de) * 1987-10-08 1994-07-06 Andor Bilas Stoffgemisch zur stabilisierung der stoffwechsel-lage
WO1999014239A1 (de) * 1997-09-12 1999-03-25 Wolf Georg Forssmann 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
EP1641457B1 (en) * 2003-06-30 2009-08-05 Nycomed GmbH Pyrrolo-dihydroisoquinoline derivatives as pde10 inhibitors
EP1651251A4 (en) * 2003-07-31 2008-06-18 Bayer Pharmaceuticals Corp METHOD FOR THE TREATMENT OF DIABETES AND RELATED DISEASES USING PDE 10A INHIBITORS

Also Published As

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

Similar Documents

Publication Publication Date Title
US20090162286A1 (en) Phosphodiesterase 10 Inhibition as Treatment for Obesity-Related and Metabolic Syndrome-Related Conditions
US8927545B2 (en) Inhibiting Eph B-3 kinase
AU2007252506B2 (en) Antitumor agent for thyroid cancer
US9555033B2 (en) Identification of LKB1 mutation as a predictive biomarker for sensitivity to TOR kinase inhibitors
JP2018524382A (ja) キラルジアリール大環状分子及びその使用
KR20070084191A (ko) 키나제 억제제로서의 １,４ 치환된 피라졸로피리미딘
JP2017105852A (ja) 運動障害を処置するためのｐｄｅ７インヒビターの使用
CN107976546A (zh) 对TOR激酶抑制活性标记PRAS40、GSK3-β或 P70S6K1的磷酸化抑制
US6417208B1 (en) Method of identification of inhibitors of PDE1C
CN118159534A (zh) 抑制PI3K同工型α的化合物和用于治疗癌症的方法
Gopalakrishnan et al. Potassium channel subtypes as molecular targets for overactive bladder and other urological disorders
Stec et al. The imidazo [1, 2-a] pyridine ring system as a scaffold for potent dual phosphoinositide-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitors
CN102947302A (zh) 三唑并[4，5-b]吡啶衍生物
CA2419623A1 (en) Method for treatment of migraine using pde5 inhibitors
CN101189241A (zh) 噻吩并吡啶衍生物、喹啉衍生物和具有c-Met自体磷酸化抑制活性的喹唑啉衍生物
CN118338905A (zh) Wee1激酶抑制剂在治疗癌症中的应用
RU2736123C1 (ru) Производные 2-аминохиназолина в качестве ингибиторов p70s6 киназы
EP1917965A1 (en) Inhibitors of the mutant form of KIT
Sayyah et al. Jak2 inhibitors: rationale and role as therapeutic agents in hematologic malignancies
KR20220130190A (ko) 암 치료를 위한 표피성장인자 수용체 티로신 키나제 억제제
Wu et al. Inhibition of proinflammatory tumor necrosis factor-α-induced inducible nitric-oxide synthase by xanthine-based 7-[2-[4-(2-chlorobenzene) piperazinyl] ethyl]-1, 3-dimethylxanthine (KMUP-1) and 7-[2-[4-(4-nitrobenzene) piperazinyl] ethyl]-1, 3-dimethylxanthine (KMUP-3) in rat trachea: the involvement of soluble guanylate cyclase and protein kinase G
JP2007513967A (ja) 変異レセプターチロシンキナーゼが駆動する細胞増殖性疾患の処置において使用するための組成物
EP1572208A2 (en) Method for counteracting a pathologic change in the beta-adrenergic pathway
EP1173254A2 (en) Novel treatment of neurotraumatic conditions with a raf inhibitor
JP2008533181A (ja) 三環式アゾール誘導体、それらの製造及び医薬品としての使用

Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued