BR112012006531A2 - derivados de imidazopirimidina ou imidazopiridina como inibidores da fosfodiesterase 10a. - Google Patents

derivados de imidazopirimidina ou imidazopiridina como inibidores da fosfodiesterase 10a.

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Publication number
BR112012006531A2
BR112012006531A2 BR112012006531A BR112012006531A BR112012006531A2 BR 112012006531 A2 BR112012006531 A2 BR 112012006531A2 BR 112012006531 A BR112012006531 A BR 112012006531A BR 112012006531 A BR112012006531 A BR 112012006531A BR 112012006531 A2 BR112012006531 A2 BR 112012006531A2
Authority
BR
Brazil
Prior art keywords
imidazopyrimidine
imidazopyridine derivatives
phosphodiesterase inhibitors
derivatives
imidazopyridine
Prior art date
Application number
BR112012006531A
Other languages
English (en)
Inventor
Alexander Flohr
Bernd Kuhn
Daniela Alberati
Jens-Uwe Peters
Katrin Groebke Zbinden
Konrad Bleicher
Markus Rudolph
Matthias Koerner
Rubén Alvarez Sanchéz
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
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BR112012006531A2 publication Critical patent/BR112012006531A2/pt

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    • 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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/535—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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Addiction (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

derivados de imidazopirimidina ou imidazopiridina como inibidores da fosfodiesterase 10a. a presente invenção refere-se a novos derivados de imidazopiridina de fórmula (i) em que r1, r2, r3, r4, r5 e a são como definidos no relatório descritivo e nas reivindicações, bem como sais fisiologicamente aceitáveis e ésteres dos mesmos. estes compostos inibem pde10a e podem ser utilizados como medicamentos.
BR112012006531A 2009-09-24 2010-09-21 derivados de imidazopirimidina ou imidazopiridina como inibidores da fosfodiesterase 10a. BR112012006531A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09171253 2009-09-24
PCT/EP2010/063830 WO2011036127A1 (en) 2009-09-24 2010-09-21 Imidazopyridine or imidazopyrimidine derivatives as phosphodiesterase 10a inhibitors

Publications (1)

Publication Number Publication Date
BR112012006531A2 true BR112012006531A2 (pt) 2016-11-22

Family

ID=43416552

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012006531A BR112012006531A2 (pt) 2009-09-24 2010-09-21 derivados de imidazopirimidina ou imidazopiridina como inibidores da fosfodiesterase 10a.

Country Status (22)

Country Link
US (2) US8017604B2 (pt)
EP (1) EP2480546B1 (pt)
JP (1) JP5629322B2 (pt)
KR (1) KR101426624B1 (pt)
CN (1) CN102548991B (pt)
AR (1) AR078437A1 (pt)
BR (1) BR112012006531A2 (pt)
CA (1) CA2770087C (pt)
CL (1) CL2012000708A1 (pt)
CY (1) CY1116120T1 (pt)
DK (1) DK2480546T3 (pt)
ES (1) ES2530884T3 (pt)
HR (1) HRP20150345T1 (pt)
IL (1) IL218032A (pt)
MX (1) MX2012003469A (pt)
PE (1) PE20121438A1 (pt)
PL (1) PL2480546T3 (pt)
PT (1) PT2480546E (pt)
RU (1) RU2502737C2 (pt)
SI (1) SI2480546T1 (pt)
TW (1) TWI402268B (pt)
WO (1) WO2011036127A1 (pt)

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US8470820B2 (en) * 2010-01-22 2013-06-25 Hoffman-La Roche Inc. Nitrogen-containing heteroaryl derivatives
CN103298468A (zh) * 2011-02-01 2013-09-11 协和发酵麒麟株式会社 稠环杂环衍生物
CN103476757A (zh) 2011-02-18 2013-12-25 阿勒根公司 作为磷酸二酯酶10(pde10a)的抑制剂的取代的6,7-二烷氧基-3-异喹啉醇衍生物
US8975276B2 (en) * 2011-06-29 2015-03-10 Bristol-Myers Squibb Company Inhibitors of PDE10
EP2574607A1 (en) 2011-09-06 2013-04-03 F. Hoffmann-La Roche AG PDE10 modulators
WO2013041472A1 (en) * 2011-09-19 2013-03-28 F. Hoffmann-La Roche Ag Triazolopyridine compounds as pde10a inhibitors
WO2014071044A1 (en) 2012-11-01 2014-05-08 Allergan, Inc. Substituted 6,7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde10a)
MX2015009377A (es) * 2013-01-31 2015-10-09 Hoffmann La Roche Compuestos radiomarcados.
CN105189493B (zh) 2013-02-27 2017-04-12 持田制药株式会社 新型吡唑衍生物
KR20160003173A (ko) 2013-04-29 2016-01-08 에프. 호프만-라 로슈 아게 2-페닐 또는 2-헤트아릴 이미다졸[1,2-a]피리딘 유도체
SG11201508924XA (en) * 2013-04-30 2015-11-27 Hoffmann La Roche Pd-CATALYZED COUPLING OF PYRAZOLE AMIDES
US10039764B2 (en) 2013-07-12 2018-08-07 University Of South Alabama Treatment and diagnosis of cancer and precancerous conditions using PDE10A inhibitors and methods to measure PDE10A expression
KR101770532B1 (ko) 2013-09-26 2017-08-22 에프. 호프만-라 로슈 아게 이미징 수단으로서의 이미다조[1,2-a]피리딘-7-아민
US9200016B2 (en) 2013-12-05 2015-12-01 Allergan, Inc. Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE 10A)
JP7050759B2 (ja) 2016-09-02 2022-04-08 サイクレリオン・セラピューティクス，インコーポレーテッド 縮合二環式ｓｇｃ刺激剤
CN113698406A (zh) * 2021-08-30 2021-11-26 成都药明康德新药开发有限公司 6-甲基吡唑并[1,5-a]嘧啶-3-胺的合成方法

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CA2566184A1 (en) * 2004-05-10 2005-11-17 Banyu Pharmaceutical Co., Ltd. Imidazopyridine compound
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IL218032A0 (en) 2012-04-30
RU2502737C2 (ru) 2013-12-27
US8017604B2 (en) 2011-09-13
TWI402268B (zh) 2013-07-21
DK2480546T3 (en) 2015-02-02
PT2480546E (pt) 2015-02-09
AU2010299927A1 (en) 2012-03-15
CN102548991B (zh) 2015-03-25
PL2480546T3 (pl) 2015-05-29
JP2013505911A (ja) 2013-02-21
EP2480546B1 (en) 2014-12-31
KR20120068943A (ko) 2012-06-27
ES2530884T3 (es) 2015-03-06
IL218032A (en) 2014-06-30
HRP20150345T1 (hr) 2015-05-08
US20110071128A1 (en) 2011-03-24
SI2480546T1 (sl) 2015-03-31
CL2012000708A1 (es) 2012-09-07
US20110294779A1 (en) 2011-12-01
PE20121438A1 (es) 2012-10-26
CN102548991A (zh) 2012-07-04
JP5629322B2 (ja) 2014-11-19
CA2770087A1 (en) 2011-03-31
KR101426624B1 (ko) 2014-08-05
EP2480546A1 (en) 2012-08-01
WO2011036127A1 (en) 2011-03-31
US8263584B2 (en) 2012-09-11
CY1116120T1 (el) 2017-02-08
MX2012003469A (es) 2012-04-19
AR078437A1 (es) 2011-11-09
TW201116530A (en) 2011-05-16
RU2012113128A (ru) 2013-11-10
CA2770087C (en) 2014-09-09

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