PE20080145A1 - Tetrahidro-pirimidoazepinas como moduladores de trpv1 - Google Patents
Tetrahidro-pirimidoazepinas como moduladores de trpv1Info
- Publication number
- PE20080145A1 PE20080145A1 PE2007000298A PE2007000298A PE20080145A1 PE 20080145 A1 PE20080145 A1 PE 20080145A1 PE 2007000298 A PE2007000298 A PE 2007000298A PE 2007000298 A PE2007000298 A PE 2007000298A PE 20080145 A1 PE20080145 A1 PE 20080145A1
- Authority
- PE
- Peru
- Prior art keywords
- tetrahydro
- phenyl
- alkyl
- pyrimidoazepine
- trpv1
- Prior art date
Links
- YPMZXYBOODEMMC-UHFFFAOYSA-N 2,3,4,5-tetrahydro-1h-pyrimido[5,4-b]azepine Chemical compound C1=CC=CNC2=C1NCNC2 YPMZXYBOODEMMC-UHFFFAOYSA-N 0.000 title abstract 2
- 102000003566 TRPV1 Human genes 0.000 title abstract 2
- 101150016206 Trpv1 gene Proteins 0.000 title abstract 2
- -1 PYRAZINYL Chemical class 0.000 abstract 3
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical group [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 2
- SLRMQYXOBQWXCR-UHFFFAOYSA-N 2154-56-5 Chemical group [CH2]C1=CC=CC=C1 SLRMQYXOBQWXCR-UHFFFAOYSA-N 0.000 abstract 1
- NZVMMYXAMNUWBZ-UHFFFAOYSA-N 3H-azepine-2,4-diamine Chemical compound N1=C(CC(=CC=C1)N)N NZVMMYXAMNUWBZ-UHFFFAOYSA-N 0.000 abstract 1
- 108091006146 Channels Proteins 0.000 abstract 1
- 102000034573 Channels Human genes 0.000 abstract 1
- 206010011224 Cough Diseases 0.000 abstract 1
- 229910003827 NRaRb Inorganic materials 0.000 abstract 1
- 102000011040 TRPV Cation Channels Human genes 0.000 abstract 1
- 108010062740 TRPV Cation Channels Proteins 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000001052 transient effect Effects 0.000 abstract 1
Classifications
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- 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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- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
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- A—HUMAN NECESSITIES
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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- A61P13/08—Drugs for disorders of the urinary system of the prostate
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Ophthalmology & Optometry (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Nutrition Science (AREA)
- Child & Adolescent Psychology (AREA)
- Gastroenterology & Hepatology (AREA)
- Psychology (AREA)
- Endocrinology (AREA)
- Toxicology (AREA)
Abstract
SE REFIERE A COMPUESTOS TETRAHIDRO-PIRIMIDOAZEPINA DE FORMULA (I), EN DONDE R1 ES H, -NRaRb, ALQUILO(C1-C6), -OALQUILO(C1-C6), -S-ALQUILO(C1-C6), CICLOALQUILO MONOCICLICO, ENTRE OTROS; R2 ES H, ALQUILO(C1-C6); R3 ES FENILO, BENCILO, PIRIDILO, PIRAZINILO, TIOFENILO, ENTRE OTROS, OPCIONALMENTE SUSTITUIDOS CON Rg; Ar ES FENILO, PIRIDILO, IMIDAZOLILO, PIRIMIDINILO O HETEROARILO FUSIONADO BICICLICO OPCIONALMENTE SUSTITUIDO CON Rk. SON SELECCIONADOS: (4-TER-BUTIL-FENIL)-[7-(3-TRIFLUOROMETIL-PIRIDIN-2-IL)-6,7,8,9-TETRAHIDRO-5H-PIRIMIDO[4,5-d]AZEPIN-4-IL]-AMINA, N-INDAN-2-IL-N,N-DIMETIL-7-(3-TRIFLUORMETIL-PIRIDIN-2-IL)-6,7,8,9-TETRAHIDRO-5H-PIRIMIDO[4,5-d]AZEPIN-2,4-DIAMINA, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y UN PROCEDIMIENTO DE PREPARACION. ESTOS COMPUESTOS SON MODULADORES DE TRPV1 (PROTEINAS DE CANAL POTENCIAL RECEPTOR TRANSITORIO VAINILLOIDE) Y SON UTILES EN EL TRATAMIENTO DE DOLOR, PRURITO, TOS, ASMA Y ENFERMEDAD INFLAMATORIA DEL INTESTINO
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US78541506P | 2006-03-21 | 2006-03-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20080145A1 true PE20080145A1 (es) | 2008-02-11 |
Family
ID=38353855
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2007000298A PE20080145A1 (es) | 2006-03-21 | 2007-03-19 | Tetrahidro-pirimidoazepinas como moduladores de trpv1 |
Country Status (30)
| Country | Link |
|---|---|
| US (3) | US8673895B2 (es) |
| EP (1) | EP2024368B1 (es) |
| JP (1) | JP5232768B2 (es) |
| KR (1) | KR101461376B1 (es) |
| CN (1) | CN101448835B (es) |
| AR (1) | AR059985A1 (es) |
| AU (1) | AU2007227203B2 (es) |
| BR (1) | BRPI0709034B1 (es) |
| CA (1) | CA2646977C (es) |
| CR (1) | CR10387A (es) |
| DK (1) | DK2024368T3 (es) |
| EA (1) | EA017069B1 (es) |
| EC (1) | ECSP088807A (es) |
| ES (1) | ES2474152T3 (es) |
| HR (1) | HRP20140664T1 (es) |
| MX (1) | MX2008012163A (es) |
| NI (1) | NI200800253A (es) |
| NO (1) | NO341676B1 (es) |
| NZ (1) | NZ571343A (es) |
| PE (1) | PE20080145A1 (es) |
| PL (1) | PL2024368T3 (es) |
| PT (1) | PT2024368E (es) |
| RS (1) | RS53436B (es) |
| SG (1) | SG177176A1 (es) |
| SI (1) | SI2024368T1 (es) |
| TW (1) | TWI440639B (es) |
| UA (1) | UA92636C2 (es) |
| UY (1) | UY30229A1 (es) |
| WO (1) | WO2007109355A2 (es) |
| ZA (1) | ZA200808975B (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1693804B1 (en) * | 1996-09-04 | 2009-11-11 | 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 |
| WO2008057300A2 (en) * | 2006-10-27 | 2008-05-15 | Redpoint Bio Corporation | Trpvi antagonists and uses thereof |
| AU2008231543B2 (en) * | 2007-03-23 | 2011-07-28 | Pfizer Limited | Pyrimido [4, 5-D] azepine derivatives as 5-HT2C agonists |
| US8288397B2 (en) * | 2007-12-17 | 2012-10-16 | Janssen Pharmaceutica Nv | Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of TRPV1 |
| US20090156598A1 (en) * | 2007-12-17 | 2009-06-18 | Lebsack Alec D | Imidazolopyrimidine modulators of TRPV1 |
| CA2729045A1 (en) * | 2008-07-31 | 2010-02-04 | Philippe Bergeron | Pyrimidine compounds, compositions and methods of use |
| CA2742897A1 (en) * | 2008-11-06 | 2010-05-14 | Astrazeneca Ab | Modulators of amyloid beta. |
| CN102480961A (zh) * | 2009-06-24 | 2012-05-30 | 健泰科生物技术公司 | 与含氧杂环稠合的嘧啶化合物、组合物和使用方法 |
| CN102711766B (zh) * | 2009-11-12 | 2014-06-04 | 霍夫曼-拉罗奇有限公司 | N-9-取代的嘌呤化合物、组合物和使用方法 |
| CA2780018C (en) * | 2009-11-12 | 2015-10-20 | F. Hoffmann-La Roche Ag | N-7 substituted purine and pyrazolopyrimidine compounds, compositions and methods of use |
| CN103037969B (zh) * | 2010-06-23 | 2015-07-29 | 约翰森·马瑟公开有限公司 | 络合物 |
| CN102154494B (zh) * | 2011-03-14 | 2013-01-02 | 中国人民解放军军事医学科学院基础医学研究所 | 一种用于儿童哮喘检测的标志物 |
| TWI582073B (zh) | 2013-02-20 | 2017-05-11 | Lg生命科學股份有限公司 | 鞘胺醇-1-磷酸酯受體促效劑、其製造方法及包含該促效劑作爲活性劑之醫藥組成物 |
| CN103641762A (zh) * | 2013-12-18 | 2014-03-19 | 中国药科大学 | 一类trpv1/cox-2双重抑制剂、其制备方法及其制备镇痛药物的用途 |
| AU2020232616A1 (en) * | 2019-03-01 | 2021-09-09 | Revolution Medicines, Inc. | Bicyclic heterocyclyl compounds and uses thereof |
| BR112022010761A2 (pt) | 2019-12-03 | 2022-08-23 | Lg Chemical Ltd | Agonista do receptor de esfingosina-1-fosfato, método de preparação do mesmo e composição farmacêutica contendo o mesmo como ingrediente ativo |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4160834A (en) | 1977-03-09 | 1979-07-10 | Eli Lilly And Company | 1-(Substituted benzoyl)-3-(substituted pyrazinyl)ureas |
| JPH03167178A (ja) | 1989-11-24 | 1991-07-19 | Taiji Nakayama | ピリミジン誘導体 |
| JPH03255077A (ja) | 1990-03-01 | 1991-11-13 | Taiji Nakayama | ピリミジン誘導体およびそれを有効成分とする血小板凝集阻止剤 |
| WO1993014080A1 (en) | 1992-01-15 | 1993-07-22 | E.I. Du Pont De Nemours And Company | Bridged heterocyclic fungicides |
| JPH06172355A (ja) | 1992-04-14 | 1994-06-21 | Mect Corp | ピリミジン誘導体およびそれを有効成分とする血小板凝集阻止剤 |
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