AR059985A1 - Tetrahidro-pirimidoazepinas como moduladores de trpv1 - Google Patents
Tetrahidro-pirimidoazepinas como moduladores de trpv1Info
- Publication number
- AR059985A1 AR059985A1 ARP070101128A ARP070101128A AR059985A1 AR 059985 A1 AR059985 A1 AR 059985A1 AR P070101128 A ARP070101128 A AR P070101128A AR P070101128 A ARP070101128 A AR P070101128A AR 059985 A1 AR059985 A1 AR 059985A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- substituted
- independently
- halo
- saturated monocyclic
- Prior art date
Links
- 102000003566 TRPV1 Human genes 0.000 title abstract 2
- 101150016206 Trpv1 gene Proteins 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 21
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 7
- 125000001475 halogen functional group Chemical group 0.000 abstract 7
- 125000001424 substituent group Chemical group 0.000 abstract 7
- -1 -NReRf Chemical group 0.000 abstract 5
- 125000006578 monocyclic heterocycloalkyl group Chemical group 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 abstract 2
- 125000002098 pyridazinyl group Chemical group 0.000 abstract 2
- 125000004076 pyridyl group Chemical group 0.000 abstract 2
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 2
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 abstract 1
- 206010011224 Cough Diseases 0.000 abstract 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 abstract 1
- 229910003827 NRaRb Inorganic materials 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 208000003251 Pruritus Diseases 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 abstract 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 239000002207 metabolite Substances 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 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
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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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Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Ophthalmology & Optometry (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Endocrinology (AREA)
- Gastroenterology & Hepatology (AREA)
- Psychology (AREA)
- Emergency Medicine (AREA)
- Immunology (AREA)
- Psychiatry (AREA)
- Vascular Medicine (AREA)
Abstract
Dichos compuestos pueden ser usados en composiciones farmacéuticas y para tratar trastornos y afecciones médicas intermediadas por TRPV1 Por lo tanto, los compuestos pueden ser administrados por ejemplo en dolor, prurito, tos, asma y enfermedad inflamatoria del intestino. Reivindicacion 1: Un compuesto de formula (1): donde: R1 es -H; NRaRb; un grupo -alquilo C1-6, -alquiloO C1-6, -S-alquilo C1-6, o -SO2-alquilo C1-6 no sustituido o sustituido con un sustituyente -OH, -Oalquilo C1-4, - NReRf, o halo sustituido; o un grupo cicloalquilo monocíclico no sustituido o sustituido con un -alquilo C1-6, -OH, -Oalquilo C1-4, -NReRf, o halo; donde Ra y Rb cada uno independientemente es -H; -alquilo C1-6, un grupo -alquilo C2-3 sustituido con -OH, -Oalquilo C1-4, -NRcRd, o halo sustituido; o un cicloalquilo monocíclico saturado, -alquilo C1-(cicloalquilo monocíclico saturado), heterocicloalquilo monocíclico saturado, -alquilo C1-(heterocicloalquilo monocíclico saturado), fenilo, o un grupo bencilo no sustituido o sustituido con uno, dos o tres porciones independientemente seleccionadas del grupo que consiste en -alquilo C1-6, OH, -Oalquilo C1-4, -NRpRq, y halo sustituidos, o Ra y Rb tomados conjuntamente con su nitrogeno de union forman un grupo heterocicloalquilo monocíclico saturado no sustituido o sustituido con uno, dos o tres porciones independientemente seleccionadas del grupo que consiste en -alquilo C1-6, -OH, -Oalquilo C1-4, -NRpRq, halo, -CO2H, y sustituyentes bencilo; donde Rc y Rd son cada uno independientemente -H o -alquilo C1-6, o Rc y Rd tomados conjuntamente con su nitrogeno de union forman un heterocicloalquilo monocíclico saturado; donde Rp y Rq son cada uno independientemente -H o -alquilo C1-6 o Rp y Rq tomados conjuntamente con su nitrogeno de union forman un heterocicloalquilo monocíclico saturado; donde Re y Rf son cada uno independientemente -H o -alquilo C1-6, o Re y Rf tomados conjuntamente con su nitrogeno de union forman un heterocicloalquilo monocíclico saturado; R2 es -H o -alquilo C1-6, R3 es un grupo fenilo, bencilo, fenetilo, indanilo, tiazolilo, tiofenilo, piridilo, pirimidinilo, pirazinilo, piridazinilo, quinolinilo, o isoquinolinilo no sustituido o sustituido con uno, dos, o tres sustituyentes Rg; donde cada sustituyente Rg es -alquilo C1-6, -OH, -Oalquilo C1-6, fenoxi, -CN, -NO2, N(Rh)Ri, -C(O)N(Rh)Ri, -N(Rh)C(O)Ri, -N(Rh)SO2 alquilo C1-6, -C(O)alquilo C1-6, -S(O)0-2-alquilo C1-6, -SO2CF3, SO2N(Rh)Ri, -SCF3, halo, -CF3, -OCF3, -COOH, C(O)Oalquilo C1-6, -C(Rj)2-CN, o -C(Rj)2-OH; o dos sustituyentes Rg adyacentes tomados conjuntamente forman -Oalquilo C1-2O-; donde Rh y Ri son cada uno independientemente -H o -alquilo C1-6; donde cada Rj es independientemente -H o -alquilo C1-6; y Ar es un grupo fenilo, piridilo, imidazolilo, pirimidinilo, piridazinilo, o un grupo heteroarilo fusionado-bicíclico no sustituido o sustituido con uno, dos o tres sustituyentes Rk; donde cada sustituyente Rk es independientemente -alquilo C1-6, -OH, -Oalquilo C1-6, fenoxi, -CN, -NO2, N(Rl)Rm, -C(O)N(Rl)Rm, N(Rl)C(O)Rm, -N(Rl)SO2 alquilo C1-6, -N(Rl)SO2CF3, -C(O)alquilo C1-6, -S(O)0-2-alquilo C1-6, -SO2CF3, SO2N(Rl)Rm, -SCF3, halo, -CF3, - OCF3, -COOH, o -C(O)Oalquilo C1-6; o dos sustituyentes Rk adyacentes tomados conjuntamente forman -Oalquilo C1-2O-; donde Rl y Rm son cada uno independientemente -H, -alquilo C1-6, o -CF3; o una sal farmacéuticamente aceptable, un profármaco farmacéuticamente aceptable o un metabolito de dicho compuesto farmacéuticamente activo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US78541506P | 2006-03-21 | 2006-03-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR059985A1 true AR059985A1 (es) | 2008-05-14 |
Family
ID=38353855
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070101128A AR059985A1 (es) | 2006-03-21 | 2007-03-20 | 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) |
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