MA33032B1 - Pyrimidines condensees - Google Patents

Pyrimidines condensees

Info

Publication number
MA33032B1
MA33032B1 MA34073A MA34073A MA33032B1 MA 33032 B1 MA33032 B1 MA 33032B1 MA 34073 A MA34073 A MA 34073A MA 34073 A MA34073 A MA 34073A MA 33032 B1 MA33032 B1 MA 33032B1
Authority
MA
Morocco
Prior art keywords
compounds
primidines
intensive
tautomer
stereoisomer
Prior art date
Application number
MA34073A
Other languages
Arabic (ar)
English (en)
Inventor
Matthias Vennemann
Thomas Bär
Thomas Maier
Swen HÖLDER
Gerrit Beneke
Florian Dehmel
Armin Zülch
Andreas Strub
Thomas Beckers
Stuart Ince
Hartmut Rehwinkel
Ningshu Liu
Ulf Bömer
Original Assignee
Bayer Schering Pharma Ag
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 Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of MA33032B1 publication Critical patent/MA33032B1/fr

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
    • A61K31/33—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
    • 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
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Abstract

La présente invention concerne des composés de formule (I) ou un N-oxyde, un sel, un tautomère ou un stéréo-isomère desdits composés, ou un sel dudit N-oxyde, tautomère ou stéréo-isomère desdits composés, où le cycle B et la pyrimidine avec laquelle il est condensé, R4, R5, R6, R7, m et n ont les significations telles que données dans la description et les revendications, qui sont des inhibiteurs efficaces de la voie Pi3K/Akt, des procédés pour leur production et leur utilisation en tant qu'agents pharmaceutiques.
MA34073A 2009-02-13 2010-02-02 Pyrimidines condensees MA33032B1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09075072 2009-02-13
EP09152914 2009-02-16
PCT/EP2010/000620 WO2010091808A1 (fr) 2009-02-13 2010-02-02 Pyrimidines condensées

Publications (1)

Publication Number Publication Date
MA33032B1 true MA33032B1 (fr) 2012-02-01

Family

ID=42115325

Family Applications (1)

Application Number Title Priority Date Filing Date
MA34073A MA33032B1 (fr) 2009-02-13 2010-02-02 Pyrimidines condensees

Country Status (29)

Country Link
US (1) US8957064B2 (fr)
EP (1) EP2396330B1 (fr)
JP (1) JP5777526B2 (fr)
KR (1) KR20110114663A (fr)
CN (1) CN102317291B (fr)
AR (1) AR075253A1 (fr)
AU (1) AU2010213192A1 (fr)
BR (1) BRPI1008782A2 (fr)
CA (1) CA2752105C (fr)
CL (1) CL2011001972A1 (fr)
CO (1) CO6410298A2 (fr)
CR (1) CR20110432A (fr)
CU (1) CU20110159A7 (fr)
DO (1) DOP2011000260A (fr)
EA (1) EA201101186A1 (fr)
EC (1) ECSP11011258A (fr)
ES (1) ES2580779T3 (fr)
HK (1) HK1165423A1 (fr)
IL (1) IL213953A0 (fr)
MA (1) MA33032B1 (fr)
MX (1) MX2011008583A (fr)
PE (1) PE20120534A1 (fr)
SG (1) SG172898A1 (fr)
SV (1) SV2011003997A (fr)
TN (1) TN2011000404A1 (fr)
TW (1) TW201036978A (fr)
UY (1) UY32432A (fr)
WO (1) WO2010091808A1 (fr)
ZA (1) ZA201106663B (fr)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2010001746A (es) * 2007-08-14 2010-03-10 Bayer Schering Pharma Ag Pirimidinas biciclicas fusionadas.
CA2806655A1 (fr) 2010-07-28 2012-02-02 Bayer Intellectual Property Gmbh Imidazo[1,2-b]pyridazines substituees
US8987286B2 (en) * 2010-12-16 2015-03-24 Bayer Intellectual Property Gmbh Substituted pyrimido[1,2-b]indazoles and their use as modulators of the Pi3K/Akt pathway
EA024890B1 (ru) * 2011-04-07 2016-10-31 Байер Интеллектчуал Проперти Гмбх Имидазопиридазины в качестве ингибиторов akt киназы
JP6077642B2 (ja) 2012-04-10 2017-02-08 シャンハイ インリ ファーマシューティカル カンパニー リミティド 縮合ピリミジン化合物、その調製法、中間体、組成物、及び使用
MX361136B (es) 2013-01-23 2018-11-28 Astrazeneca Ab Compuestos quimicos.
JP6441910B2 (ja) 2013-09-30 2018-12-19 シャンハイ インリ ファーマシューティカル カンパニー リミティド 縮合ピリミジン化合物、中間体、その調製方法、組成物及び使用
JP6139789B2 (ja) 2013-10-16 2017-05-31 シャンハイ インリ ファーマシューティカル カンパニー リミティド 縮合複素環化合物、その調製方法、医薬組成物及びその使用
EA037361B1 (ru) * 2016-06-16 2021-03-18 Янссен Фармацевтика Нв Производные бициклического пиридина, пиразина и пиримидина в качестве ингибиторов pi3k бета
EP3548035A4 (fr) 2016-11-30 2020-07-22 Case Western Reserve University Combinaisons d'inhibiteurs de 15-pgdh avec des corcostéroïdes et/ou des inhibiteurs du tnf et leurs utilisations
US11718589B2 (en) 2017-02-06 2023-08-08 Case Western Reserve University Compositions and methods of modulating short-chain dehydrogenase
WO2018175906A1 (fr) 2017-03-24 2018-09-27 Nanosyn, Inc. Composés de triazolo-pyrimidine fusionnés ayant une application pharmaceutique utile
JP7053654B2 (ja) 2017-03-29 2022-04-12 ヤンセン ファーマシューティカ エヌ．ベー． ＰＩ３Ｋβ阻害剤としてのキノキサリン及びピリドピラジン誘導体
WO2020159942A1 (fr) * 2019-01-29 2020-08-06 Tosk, Inc. Modulateurs de pyrazolopyrimidine de ras gtpase
WO2020227491A1 (fr) * 2019-05-07 2020-11-12 The Trustees Of The University Of Pennsylvania Triazolopyrimidines deutérés
CN112921405B (zh) * 2019-12-05 2023-06-27 成都先导药物开发股份有限公司 一种合成On-DNA吡唑并[1，5-a]嘧啶化合物的方法
CN111333655B (zh) * 2020-04-13 2021-07-13 武汉工程大学 一种***并嘧啶类化合物及其制备方法和应用
CN114874221A (zh) * 2022-05-12 2022-08-09 广州佳途科技股份有限公司 一种rip2激酶抑制剂中间体及其合成方法

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GB1541615A (en) * 1975-06-26 1979-03-07 Philip Morris Inc Azetidine compounds and process for their production
GB1543308A (en) 1975-06-26 1979-04-04 Philip Morris Inc Azetidine compounds and process for their production
CN1085962C (zh) 1996-06-25 2002-06-05 W·L·戈尔有限公司 柔性防水防油复合材料
TW414846B (en) 1997-11-05 2000-12-11 Mitsubishi Heavy Ind Ltd Combustion apparatus
GB9821898D0 (en) 1998-10-08 1998-12-02 Pfizer Ltd Heterocycles
US7399764B2 (en) * 2002-10-30 2008-07-15 Merck & Co., Inc. Inhibitors of Akt activity
EP1622616B1 (fr) 2003-04-24 2011-06-15 Merck Sharp & Dohme Corp. Inhibiteurs de l'activite akt
AU2004233827B2 (en) * 2003-04-24 2009-05-28 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
ATE499364T1 (de) 2004-04-09 2011-03-15 Merck Sharp & Dohme Hemmer der akt aktivität
CN1942463A (zh) 2004-04-15 2007-04-04 安斯泰来制药株式会社 2－氨基嘧啶衍生物
BRPI0511571A (pt) * 2004-05-27 2008-01-02 Pfizer derivados de aminopiridina como agonistas de dopamina d3 seletivos
US7544677B2 (en) 2004-08-23 2009-06-09 Merck & Co., Inc. Inhibitors of Akt activity
EP1827436A4 (fr) 2004-12-15 2011-08-10 Merck Sharp & Dohme Inhibiteurs d'activite akt
CA2597456A1 (fr) 2005-02-14 2006-08-31 Merck & Co., Inc. Inhibiteurs d'activite d'akt
NZ563423A (en) 2005-06-10 2010-05-28 Merck Sharp & Dohme Inhibitors of AKT activity
EP1942900B1 (fr) 2005-10-06 2015-06-03 Merck Sharp & Dohme Corp. Utilisation de derives de pyrazolo [1,5-a] pyrimidine comme inhibiteurs de proteines kinases procedes d'inhibition de proteines kinases
ATE533770T1 (de) * 2005-10-06 2011-12-15 Schering Corp Pyrazolopyrimidine als proteinkinaseinhibitoren
EP2086965B1 (fr) 2006-11-02 2010-02-10 Vertex Pharmaceuticals, Inc. Aminopyridines et aminopyrimidines utiles en tant qu'inhibiteurs de protéines kinases
JP5572388B2 (ja) * 2006-11-22 2014-08-13 インサイト・コーポレイション キナーゼ阻害剤としてのイミダゾトリアジンおよびイミダゾピリミジン
MX2010001746A (es) 2007-08-14 2010-03-10 Bayer Schering Pharma Ag Pirimidinas biciclicas fusionadas.

Also Published As

Publication number Publication date
US8957064B2 (en) 2015-02-17
AR075253A1 (es) 2011-03-16
CA2752105A1 (fr) 2010-08-19
CR20110432A (es) 2011-10-24
TN2011000404A1 (en) 2013-03-27
EP2396330A1 (fr) 2011-12-21
IL213953A0 (en) 2011-08-31
TW201036978A (en) 2010-10-16
KR20110114663A (ko) 2011-10-19
CN102317291A (zh) 2012-01-11
ES2580779T3 (es) 2016-08-26
JP2012517963A (ja) 2012-08-09
PE20120534A1 (es) 2012-05-10
CU20110159A7 (es) 2012-02-15
DOP2011000260A (es) 2011-10-15
EA201101186A1 (ru) 2012-04-30
WO2010091808A8 (fr) 2011-07-21
CA2752105C (fr) 2017-10-31
CL2011001972A1 (es) 2012-03-23
CN102317291B (zh) 2015-02-11
MX2011008583A (es) 2011-12-12
BRPI1008782A2 (pt) 2019-09-24
US20130317002A1 (en) 2013-11-28
CO6410298A2 (es) 2012-03-30
ECSP11011258A (es) 2011-10-31
HK1165423A1 (en) 2012-10-05
UY32432A (es) 2010-09-30
JP5777526B2 (ja) 2015-09-09
SG172898A1 (en) 2011-08-29
AU2010213192A1 (en) 2011-08-04
EP2396330B1 (fr) 2016-04-06
ZA201106663B (en) 2013-03-27
SV2011003997A (es) 2012-01-06
WO2010091808A1 (fr) 2010-08-19

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