NO20084832L - Pyrimidinderivater som P13K-inhibitorer - Google Patents

Pyrimidinderivater som P13K-inhibitorer

Info

Publication number
NO20084832L
NO20084832L NO20084832A NO20084832A NO20084832L NO 20084832 L NO20084832 L NO 20084832L NO 20084832 A NO20084832 A NO 20084832A NO 20084832 A NO20084832 A NO 20084832A NO 20084832 L NO20084832 L NO 20084832L
Authority
NO
Norway
Prior art keywords
group
alk
unsubstituted
alkyl
substituted
Prior art date
Application number
NO20084832A
Other languages
English (en)
Inventor
Stephen Price
Timothy Hancox
Stewart J Baker
Sukhjit Sohal
Paul John Goldsmith
Neil Anthony Pegg
Stephen Joseph Shuttleworth
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
Priority claimed from GB0608264A external-priority patent/GB0608264D0/en
Priority claimed from GB0608397A external-priority patent/GB0608397D0/en
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of NO20084832L publication Critical patent/NO20084832L/no

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/08—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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • 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
    • 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
    • A61P9/10—Drugs 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Emergency Medicine (AREA)
  • Virology (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Dermatology (AREA)

Abstract

Tienopyrimidiner med formel (Ia) eller (Ib): hvori R1 er en gruppe med formel: R2 er H, halo eller C1-C6 alkyl; R3 er en indolgruppe som er usubstituert eller substituert; R4 og R5 danner, sammen med N-atomet som de er bundet til, en gruppe valgt fra piperazin, piperidin og pyrrolidin, hvis gruppe er usubstituert eller substituert med en eller flere grupper valgt fra C1-C6 alkyl, -S(O)2 R10 , -S(O)2-(alk)q-NR11R12, okso (=O), -alk-OR10 , -(alk)q-Het, en heterosyklylgruppe og -NR13R14; eller en av R4 og R5 er C1-C6 alkyl og den andre er en piperazin-, piperidin- eller pyrrolidingruppe, hvis gruppe er usubstituert eller substituert; R10 er H eller C1-C6 alkyl som er usubstituert; R11 og R12 er hver uavhengig valgt fra H og C1-C6 alkyl som er usubstituert, eller R11 og R12 danner, sammen med N-atomet som de er bundet til, en 5- eller 6-leddet mettet heterosyklisk gruppe; R13 og R14 er hver uavhengig valgt fra C1-C6 alkyl, -S(O)2 R10, alk-OR10, -(alk)q-Ph og -(alk)q-Het; Ph er fenyl; q er 0 eller 1; Het er en tiazol-, imidazol-, pyrrol-, pyridin- eller pyrimidingruppe, hvis gruppe er usubstituert eller substituert; og alk er C1-C6 alkylen; og de farmasøytisk akseptable saltene derav har aktivitet som inhibitorer av PI3K og kan således bli brukt for å behandle sykdommer og forstyrrelser som kommer som et resultat av abnorm cellevekst, -funksjon eller -oppførsel assosiert med PI3 kinase, spesielt p110 delta subtypen, sånn som immunforstyrrelser, kardiovaskulær sykdom, viral infeksjon, inflammasjon, metabolske/endokrine forstyrrelser og neurologiske forstyrrelser. Prosesser for å syntetisere forbindelsene er også beskrevet.
NO20084832A 2006-04-26 2008-11-18 Pyrimidinderivater som P13K-inhibitorer NO20084832L (no)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0608264A GB0608264D0 (en) 2006-04-26 2006-04-26 Pharmaceutical compounds
GB0608397A GB0608397D0 (en) 2006-04-27 2006-04-27 Pharmaceutical compounds
PCT/GB2007/001504 WO2007122410A1 (en) 2006-04-26 2007-04-25 Pyrimidine derivatives as pi3k inhibitors

Publications (1)

Publication Number Publication Date
NO20084832L true NO20084832L (no) 2008-11-18

Family

ID=38110021

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20084832A NO20084832L (no) 2006-04-26 2008-11-18 Pyrimidinderivater som P13K-inhibitorer

Country Status (15)

Country Link
US (2) US8252792B2 (no)
EP (1) EP2032582A1 (no)
JP (1) JP5302186B2 (no)
KR (1) KR20090021155A (no)
AU (1) AU2007242594A1 (no)
BR (1) BRPI0710866A2 (no)
CA (1) CA2650196A1 (no)
CR (1) CR10369A (no)
EC (1) ECSP088867A (no)
IL (1) IL194755A0 (no)
MA (1) MA30360B1 (no)
MX (1) MX2008013582A (no)
NO (1) NO20084832L (no)
RU (1) RU2008141356A (no)
WO (1) WO2007122410A1 (no)

Families Citing this family (43)

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PL2041139T3 (pl) 2006-04-26 2012-05-31 Hoffmann La Roche Związki farmaceutyczne
CA2671845C (en) 2006-12-07 2015-03-24 Genentech, Inc. Phosphoinositide 3-kinase inhibitor compounds and methods of use
PE20081679A1 (es) 2006-12-07 2008-12-18 Hoffmann La Roche Compuestos del inhibidor de fosfoinositida 3-cinasa y metodos de uso
ATE510841T1 (de) 2007-06-12 2011-06-15 Hoffmann La Roche Thiazoliopyrimidine und ihre verwendung als hemmer der phosphatidylinositol-3 kinase
BRPI0816769A2 (pt) 2007-09-12 2016-11-29 Hoffmann La Roche combinações de compostos inibidores de fosfoinositida 3-cinase e agentes quimioterapêuticos, e métodos de uso
CN101932587A (zh) 2007-09-24 2010-12-29 吉宁特有限公司 噻唑并嘧啶pi3k抑制剂化合物及使用方法
WO2009055730A1 (en) 2007-10-25 2009-04-30 Genentech, Inc. Process for making thienopyrimidine compounds
GB0721095D0 (en) * 2007-10-26 2007-12-05 Piramed Ltd Pharmaceutical compounds
US8163763B2 (en) 2008-07-31 2012-04-24 Genentech, Inc. Pyrimidine compounds, compositions and methods of use
CA2738868C (en) 2008-10-01 2017-01-17 Novartis Ag Smoothened antagonism for the treatment of hedgehog pathway-related disorders
TWI378933B (en) 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
PT2385832E (pt) 2009-01-08 2015-11-02 Curis Inc Inibidores de fosfoinoritide 3-quinase com uma fração de ligação ao zinco
MX2011012520A (es) 2009-05-27 2011-12-12 Hoffmann La Roche Compuestos inhibidores de pi3k de pirimidina biciclicos selectivos para p110 delta y metodos de uso de los mismos.
SG182247A1 (en) * 2009-05-27 2012-08-30 Hoffmann La Roche Bicyclic indole-pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use
GEP20207129B (en) 2009-06-17 2020-07-10 Vertex Pharma Inhibitors of influenza viruses replication
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ES2567168T3 (es) 2009-11-12 2016-04-20 F. Hoffmann-La Roche Ag Compuestos purina y pirazolopirimidina N7-sustituidos, composiciones y métodos de utilización
EA026134B1 (ru) 2010-12-16 2017-03-31 Ф. Хоффманн-Ля Рош Аг Трициклические ингибиторы pi3k и способы их применения
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CN104350144B (zh) 2012-05-23 2017-08-04 弗·哈夫曼-拉罗切有限公司 获得和使用内胚层和肝细胞的组合物和方法
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US9676765B2 (en) 2012-11-07 2017-06-13 Karus Therapeutics Limited Histone deacetylase inhibitors and their use in therapy
SI2994465T1 (sl) 2013-05-10 2018-10-30 Karus Therapeutics Limited Novi inhibitorji histon deacetilaze
US9296727B2 (en) 2013-10-07 2016-03-29 Vertex Pharmaceuticals Incorporated Methods of regioselective synthesis of 2,4-disubstituted pyrimidines
HUE038820T2 (hu) 2013-11-13 2018-11-28 Vertex Pharma Eljárás influenzavírusok replikációjának inhibitorai elõállítására
PT3068776T (pt) 2013-11-13 2019-08-26 Vertex Pharma Inibidores da replicação de vírus da gripe
GB201402431D0 (en) 2014-02-12 2014-03-26 Karus Therapeutics Ltd Compounds
GB201419264D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
GB201419228D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
CN107074873B (zh) * 2014-12-11 2022-01-07 纳科法尔马有限公司 作为抗癌药的7-(吗啉基)-2-(N-哌嗪基)甲基噻吩并[2,3-c]吡啶衍生物
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CN114656378A (zh) * 2016-05-16 2022-06-24 得克萨斯州大学系统董事会 阳离子磺酰胺氨基脂质和两亲性两性离子氨基脂质
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WO2004017950A2 (en) 2002-08-22 2004-03-04 Piramed Limited Phosphadidylinositol 3,5-biphosphate inhibitors as anti-viral agents
GB0423653D0 (en) * 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
PL2041139T3 (pl) 2006-04-26 2012-05-31 Hoffmann La Roche Związki farmaceutyczne

Also Published As

Publication number Publication date
JP5302186B2 (ja) 2013-10-02
US20120283257A1 (en) 2012-11-08
US8252792B2 (en) 2012-08-28
JP2009534453A (ja) 2009-09-24
CR10369A (es) 2009-01-09
EP2032582A1 (en) 2009-03-11
IL194755A0 (en) 2009-08-03
WO2007122410A1 (en) 2007-11-01
KR20090021155A (ko) 2009-02-27
ECSP088867A (es) 2008-12-30
BRPI0710866A2 (pt) 2012-08-14
US8697693B2 (en) 2014-04-15
MX2008013582A (es) 2009-01-19
MA30360B1 (fr) 2009-04-01
US20100016306A1 (en) 2010-01-21
CA2650196A1 (en) 2007-11-01
RU2008141356A (ru) 2010-06-10
AU2007242594A1 (en) 2007-11-01

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