BRPI0517461A - compostos farmacêuticos - Google Patents
compostos farmacêuticosInfo
- Publication number
- BRPI0517461A BRPI0517461A BRPI0517461-9A BRPI0517461A BRPI0517461A BR PI0517461 A BRPI0517461 A BR PI0517461A BR PI0517461 A BRPI0517461 A BR PI0517461A BR PI0517461 A BRPI0517461 A BR PI0517461A
- Authority
- BR
- Brazil
- Prior art keywords
- substituted
- unsubstituted
- formula
- disorders
- alkyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 229920006395 saturated elastomer Polymers 0.000 abstract 3
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 abstract 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 abstract 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 abstract 2
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 208000017701 Endocrine disease Diseases 0.000 abstract 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical group C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 239000012828 PI3K inhibitor Substances 0.000 abstract 1
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 abstract 1
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 abstract 1
- 208000036142 Viral infection Diseases 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 239000000470 constituent Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 208000026278 immune system disease Diseases 0.000 abstract 1
- 125000001041 indolyl group Chemical group 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 208000030159 metabolic disease Diseases 0.000 abstract 1
- 230000002503 metabolic effect Effects 0.000 abstract 1
- AQNQGBUEVCAVML-UHFFFAOYSA-N oxazepane Chemical compound C1CCNOCC1 AQNQGBUEVCAVML-UHFFFAOYSA-N 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 abstract 1
- 150000003230 pyrimidines Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000002194 synthesizing effect Effects 0.000 abstract 1
- PGAZQSBUJDVGIX-UHFFFAOYSA-N thiazepane Chemical group C1CCNSCC1 PGAZQSBUJDVGIX-UHFFFAOYSA-N 0.000 abstract 1
- -1 thiomorloline Chemical compound 0.000 abstract 1
- 229930192474 thiophene Natural products 0.000 abstract 1
- 230000009385 viral infection Effects 0.000 abstract 1
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
- 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
- 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
- A61P3/04—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
- 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
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Virology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
COMPOSTOS FARMACêUTICOS. Pirimidinas fundidas de fórmula (I) em que A representa um anel tiofeno ou furano; n é 1 ou 2; R é um grupo de fórmula (1) em que m é O ou 1; R¬ 30¬ é H ou C~ 1~-C~ 6~ alquila; R¬ 4¬ e R¬ 5¬ formam, juntamente com o átomo de N ao qual eles estão ligados, um grupo heterocíclico que contém N saturado de 5- ou 6- elémentos que inclui O ou 1 heteroátomos adicionais selecionados entre N, S e O, que podem estar fundidos a um anel de benzeno e que é não substituído ou substituido ou um de R¬ 4¬ e R¬ 5¬ é alquila e o outro é um grupo heterocíclico que contém N saturado de 5- ou 6- e- lementos como definido acima ou um grupo alquila que é substituído por um grupo heterocíclico que contém N saturado de 5- ou 6- elementos como definido acima; R é selecionado entre: a fórmula (a) em que R¬ 6¬ e R¬ 7¬ formam, juntamente com o átomo de nitrogênio ao qual eles estão ligados, um grupo morfolina, tiomorlolina, piperidina, piperazina, oxazepano ou tiazepano que não é substituído ou é substituído e fórmula (b) em que Y é uma cadeia C~ 2~- C~ 4~ alquileno que contém, entre átomos de carbono constituintes da cadeia e/ou em uma ou ambas as extremidades da cadeia, 1 ou 2 heteroátomos selecionados entre O, N e S e que não é substituido ou é substituido; e R¬ 3¬ é um grupo indol que não é substituído ou é substituído e o sal farmaceuticamente aceitável do mesmo tem atividade como inibidores de PI3K e podem assim ser usados para tratar doenças ou distúrbios que surgem do crescimento anormal, da função ou do comportamento da célula associados com a PI3 quinase tais como câncer, distúrbios imunológ icos, doença card iovascular, infecção viral, inflamação, distúrbios do metabolismo/endócrinos e distúrbios neurológicos. Também são descritos processos para a síntese dos compostos.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0423653.5A GB0423653D0 (en) | 2004-10-25 | 2004-10-25 | Pharmaceutical compounds |
| PCT/GB2005/004137 WO2006046035A1 (en) | 2004-10-25 | 2005-10-25 | Pharmaceutical compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0517461A true BRPI0517461A (pt) | 2008-10-07 |
Family
ID=33485146
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0517019-2A BRPI0517019A (pt) | 2004-10-25 | 2005-10-25 | compostos farmacêuticos |
| BRPI0517461-9A BRPI0517461A (pt) | 2004-10-25 | 2005-10-25 | compostos farmacêuticos |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0517019-2A BRPI0517019A (pt) | 2004-10-25 | 2005-10-25 | compostos farmacêuticos |
Country Status (17)
| Country | Link |
|---|---|
| US (8) | US7776856B2 (pt) |
| EP (3) | EP1812444B1 (pt) |
| JP (3) | JP5077946B2 (pt) |
| KR (3) | KR20070084474A (pt) |
| CN (2) | CN101087794B (pt) |
| AU (2) | AU2005298404B2 (pt) |
| BR (2) | BRPI0517019A (pt) |
| CA (2) | CA2585089C (pt) |
| ES (3) | ES2558867T3 (pt) |
| GB (1) | GB0423653D0 (pt) |
| IL (2) | IL182614A (pt) |
| MX (2) | MX2007004868A (pt) |
| NO (2) | NO20072115L (pt) |
| NZ (2) | NZ554586A (pt) |
| RU (2) | RU2422449C2 (pt) |
| WO (3) | WO2006046031A1 (pt) |
| ZA (2) | ZA200703311B (pt) |
Families Citing this family (145)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2264819C (en) * | 1996-09-04 | 2010-03-23 | Intertrust Technologies Corp. | Trusted infrastructure support systems, methods and techniques for secure electronic commerce, electronic transactions, commerce process control and automation, distributed computing, and rights management |
| GB0423653D0 (en) | 2004-10-25 | 2004-11-24 | Piramed Ltd | Pharmaceutical compounds |
| KR20090021155A (ko) * | 2006-04-26 | 2009-02-27 | 에프. 호프만-라 로슈 아게 | Pi3k 억제제로서의 피리미딘 유도체 |
| WO2007129161A2 (en) | 2006-04-26 | 2007-11-15 | F. Hoffmann-La Roche Ag | Thieno [3, 2-d] pyrimidine derivative useful as pi3k inhibitor |
| EP2246354A1 (en) * | 2006-04-26 | 2010-11-03 | F. Hoffmann-La Roche AG | Thieno[3,2-d]pyrimidine derivative useful as PI3K inhibitor |
| TWI498332B (zh) | 2006-04-26 | 2015-09-01 | Hoffmann La Roche | 作為pi3k抑制劑之嘧啶衍生物及相關製備方法、醫藥組合物、用途、套組及產物 |
| TW200801012A (en) * | 2006-04-26 | 2008-01-01 | Piramed Ltd | Phosphoinositide 3-kinase inhibitor compounds and methods of use |
| GB0608820D0 (en) | 2006-05-04 | 2006-06-14 | Piramed Ltd | Pharmaceutical compounds |
| GB0611152D0 (en) | 2006-06-06 | 2006-07-19 | Ucb Sa | Therapeutic agents |
| WO2007146284A2 (en) * | 2006-06-12 | 2007-12-21 | Vertex Pharmaceuticals Incorporated | Thienopyrimidines useful as modulators of ion channels |
| GB0612630D0 (en) | 2006-06-26 | 2006-08-02 | Novartis Ag | Organic compounds |
| KR20090087027A (ko) * | 2006-11-13 | 2009-08-14 | 일라이 릴리 앤드 캄파니 | 염증 질환 및 암의 치료를 위한 티에노피리미디논 |
| RU2470936C2 (ru) * | 2006-12-07 | 2012-12-27 | Дженентек, Инк. | Соединения-ингибиторы фосфоинозитид 3-киназы и способы применения |
| MX2009005950A (es) * | 2006-12-07 | 2009-10-12 | Genentech Inc | Compuestos inhibidores de fosfoinositido 3-quinasas y metodos de uso. |
| WO2008152394A1 (en) * | 2007-06-12 | 2008-12-18 | F.Hoffmann-La Roche Ag | Pharmaceutical compounds |
| US7893060B2 (en) * | 2007-06-12 | 2011-02-22 | F. Hoffmann-La Roche Ag | Thiazolopyrimidines and their use as inhibitors of phosphatidylinositol-3 kinase |
| EP2205242B1 (en) * | 2007-09-12 | 2015-04-15 | Genentech, Inc. | Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use |
| CA2704711C (en) | 2007-09-24 | 2016-07-05 | Genentech, Inc. | Thiazolopyrimidine p13k inhibitor compounds and methods of use |
| JP5348725B2 (ja) * | 2007-10-25 | 2013-11-20 | ジェネンテック, インコーポレイテッド | チエノピリミジン化合物の製造方法 |
| GB0721095D0 (en) * | 2007-10-26 | 2007-12-05 | Piramed Ltd | Pharmaceutical compounds |
| US20110230464A1 (en) * | 2007-10-26 | 2011-09-22 | Paul Goldsmith | Purine derivatives useful as p13 kinase inhibitors |
| AU2008343813B2 (en) | 2007-12-19 | 2012-04-12 | Amgen Inc. | Inhibitors of PI3 kinase |
| JP5421925B2 (ja) | 2007-12-19 | 2014-02-19 | ジェネンテック, インコーポレイテッド | 5−アニリノイミダゾピリジン及び使用の方法 |
| CA2708176A1 (en) | 2007-12-21 | 2009-07-02 | Genentech, Inc. | Azaindolizines and methods of use |
| US9029411B2 (en) | 2008-01-25 | 2015-05-12 | Millennium Pharmaceuticals, Inc. | Thiophenes and uses thereof |
| DK2644194T3 (en) | 2008-03-18 | 2017-07-03 | Genentech Inc | Combinations of an anti-HER2 antibody-drug conjugate and docetaxel |
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| CA2729045A1 (en) * | 2008-07-31 | 2010-02-04 | Philippe Bergeron | Pyrimidine compounds, compositions and methods of use |
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| EA024252B1 (ru) | 2009-01-08 | 2016-08-31 | Кьюрис, Инк. | Ингибиторы фосфоинозитид-3-киназ с цинксвязывающей группой |
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| RU2683325C2 (ru) | 2009-02-05 | 2019-03-28 | Иммьюноджен, Инк. | Новые производные бензодиазепина |
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| US20100331305A1 (en) * | 2009-06-24 | 2010-12-30 | Genentech, Inc. | Oxo-heterocycle fused pyrimidine compounds, compositions and methods of use |
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| SG178986A1 (en) | 2009-09-08 | 2012-04-27 | Hoffmann La Roche | 4-substituted pyridin-3-yl-carboxamide compounds and methods of use |
| US8263633B2 (en) | 2009-09-28 | 2012-09-11 | F. Hoffman-La Roche Ag | Benzoxepin PI3K inhibitor compounds and methods of use |
| CA2776944A1 (en) * | 2009-10-12 | 2011-05-12 | F. Hoffmann-La Roche Ag | Combinations of a pi3k inhibitor and a mek inhibitor |
| WO2011049625A1 (en) | 2009-10-20 | 2011-04-28 | Mansour Samadpour | Method for aflatoxin screening of products |
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