AR049092A1 - Derivados de tetrahidronaftiridina como ligandos del receptor h3 de histamina - Google Patents
Derivados de tetrahidronaftiridina como ligandos del receptor h3 de histaminaInfo
- Publication number
- AR049092A1 AR049092A1 ARP050101916A ARP050101916A AR049092A1 AR 049092 A1 AR049092 A1 AR 049092A1 AR P050101916 A ARP050101916 A AR P050101916A AR P050101916 A ARP050101916 A AR P050101916A AR 049092 A1 AR049092 A1 AR 049092A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- nr2r3
- alkoxy
- halogen
- Prior art date
Links
- 239000003446 ligand Substances 0.000 title abstract 2
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 title 2
- 229960001340 histamine Drugs 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 7
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 2
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- ZCZVGQCBSJLDDS-UHFFFAOYSA-N 1,2,3,4-tetrahydro-1,8-naphthyridine Chemical class C1=CC=C2CCCNC2=N1 ZCZVGQCBSJLDDS-UHFFFAOYSA-N 0.000 abstract 1
- 102000004384 Histamine H3 receptors Human genes 0.000 abstract 1
- 108090000981 Histamine H3 receptors Proteins 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- -1 hydroxy C1-4 alkyl Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
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- 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
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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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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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
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- 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
- A61P11/06—Antiasthmatics
-
- 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
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
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- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- 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
- A61P27/16—Otologicals
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- 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]
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
- A61P37/08—Antiallergic agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Child & Adolescent Psychology (AREA)
- Otolaryngology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Anesthesiology (AREA)
- Obesity (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pyridine Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
Derivados de tetrahidronaftiridina como ligandos del receptor H3 de histamina, composiciones farmacéuticas que los contienen, usos y procedimientos de preparacion. Reivindicacion 1: Un compuesto que tiene la formula (1), o de formula (2) o una sal o solvato farmacéuticamente aceptable del mismo, en las que: R1 es het1, opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre: halogeno; alquilo C1-4, opcionalmente sustituido con halogeno; alcoxi C1-4, opcionalmente sustituido con halogeno; CN; morfolino; -NR2R3; -(CH2)nC(O)NR2R3; -(CH2)nC(O)O-R4; -(CH2)n-NR5-C(O)-R4; -(CH2)n-NR5-C(O)-NR2R3; -SO2-NR2R3; -SO2-alquilo C1-4; -R6; -O-R6, en los que independientemente para cada sustituyente: n es un numero seleccionado entre 0, 1, 2 y 3; R2 y R3, están independientemente de cada otro seleccionados entre H y alquilo C1-4 o R2 y R3 tomados juntos con el átomo de N al que están unidos forman un heterociclo saturado de 4, 5, 6, o 7 miembros; R4 y R5 están independientemente de cada otro seleccionados entre H y alquilo C1-4; R6 es fenilo, opcionalmente sustituido con halogeno, alquilo C1-4, o alcoxi C1-4; A es (i) un grupo de formula (3) en la que m es un numero entero entre 2 y 6; R7 y R8 están cada uno de ellos seleccionados independientemente entre H, alquilo C1-6, cicloalquilo C3-7 e hidroxialquilo C1-6 o R7 y R8 tomados juntos con el átomo de N al que están unidos forman un heterociclo saturado de 4-, 5-, 6- o 7- miembros, en el que un átomo de C está opcionalmente reemplazado por N, O, S, SO o SO2 y en el que dicho heterociclo saturado está opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre alquilo C1-4, alcoxi C1-4, alcoxi C1-4-alquilo C1- 4, hidroxialquilo C1-4, hidroxi, C(O)Oalquilo C1-4, -C(O)-alquilo C1-4-NH2, -C(O)NH2, halo, amino, alquil C1-4amino y di[alquil C1-4]amino; o (ii) un grupo de formula (4) en la que p es un numero entero seleccionado entre 0, 1 y 2; Q representa un heterociclo saturado de 4, 5 o 6 miembros opcionalmente sustituido con H, alquilo C1-6, cicloalquilo C3-7, hidroxialquilo C1-6, -alquil C1-4-COOH y -alquil C1-4-O-alquil C1-4-COOH; en la que het1 se selecciona entre grupos heteroaromáticos monocíclicos o bicíclicos que tienen 5 a 10 miembros en el anillo, que contienen 1, 2, 3 o 4 heteroátomo(s) seleccionado(s) entre N, O y S.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04291222A EP1595881A1 (en) | 2004-05-12 | 2004-05-12 | Tetrahydronaphthyridine derivates useful as histamine H3 receptor ligands |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR049092A1 true AR049092A1 (es) | 2006-06-28 |
Family
ID=34931096
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050101916A AR049092A1 (es) | 2004-05-12 | 2005-05-11 | Derivados de tetrahidronaftiridina como ligandos del receptor h3 de histamina |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US7557121B2 (es) |
| EP (2) | EP1595881A1 (es) |
| JP (1) | JP4084410B2 (es) |
| KR (1) | KR100908155B1 (es) |
| CN (2) | CN101798305A (es) |
| AP (1) | AP2006003786A0 (es) |
| AR (1) | AR049092A1 (es) |
| AT (1) | ATE491707T1 (es) |
| AU (1) | AU2005243403B2 (es) |
| BR (1) | BRPI0510762A (es) |
| CA (1) | CA2564201C (es) |
| CR (1) | CR8747A (es) |
| DE (1) | DE602005025345D1 (es) |
| DK (1) | DK1756104T3 (es) |
| EA (1) | EA010487B1 (es) |
| EC (1) | ECSP066984A (es) |
| ES (1) | ES2355572T3 (es) |
| GE (1) | GEP20084552B (es) |
| GT (1) | GT200500112A (es) |
| IL (1) | IL178882A (es) |
| MA (1) | MA28579B1 (es) |
| MX (1) | MXPA06013113A (es) |
| NL (1) | NL1029016C2 (es) |
| NO (1) | NO20064577L (es) |
| PA (1) | PA8632801A1 (es) |
| PE (1) | PE20060312A1 (es) |
| SV (1) | SV2005002112A (es) |
| TN (1) | TNSN06369A1 (es) |
| TW (1) | TW200607506A (es) |
| UY (1) | UY28895A1 (es) |
| WO (1) | WO2005111036A1 (es) |
| ZA (1) | ZA200609111B (es) |
Families Citing this family (59)
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| JP2008543880A (ja) | 2005-06-17 | 2008-12-04 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | ナフチリジン化合物 |
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| MX2008016343A (es) | 2006-06-23 | 2009-01-19 | Abbott Lab | Derivados ciclopropil amina como moduladores del receptro de histamina h3. |
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| JP2011518127A (ja) * | 2008-03-31 | 2011-06-23 | エヴォテック・アクチエンゲゼルシャフト | ヒスタミンｈ３受容体アンタゴニストとしてのテトラヒドロナフチリジンおよびそれらのアザ誘導体 |
| WO2010026113A1 (en) * | 2008-09-03 | 2010-03-11 | Evotec Neurosciences Gmbh | Acyl- and sufonyl tetrahydronaphthyridines and aza derivatives thereof as histamine h3 receptor antagonists |
| WO2010052222A1 (en) * | 2008-11-07 | 2010-05-14 | Evotec Neurosciences Gmbh | (dihydro)naphthyridinone derivatives as histamine h3 receptor antagonists |
| EP2421863A1 (en) * | 2009-04-21 | 2012-02-29 | NeuroSearch AS | Substituted naphthyridine derivatives and their medical use |
| US9186353B2 (en) | 2009-04-27 | 2015-11-17 | Abbvie Inc. | Treatment of osteoarthritis pain |
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| KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| NZ331272A (en) | 1996-02-09 | 2000-01-28 | Black James Foundation | Histamine H3 receptor ligands |
| WO2000035298A1 (en) | 1996-11-27 | 2000-06-22 | Wm. Wrigley Jr. Company | Chewing gum containing medicament active agents |
| GB9711643D0 (en) | 1997-06-05 | 1997-07-30 | Janssen Pharmaceutica Nv | Glass thermoplastic systems |
| GB9803536D0 (en) | 1998-02-19 | 1998-04-15 | Black James Foundation | Histamine H,receptor ligands |
| EP0982300A3 (en) | 1998-07-29 | 2000-03-08 | Societe Civile Bioprojet | Non-imidazole alkylamines as histamine H3 - receptor ligands and their therapeutic applications |
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| KR100852362B1 (ko) | 2000-08-08 | 2008-08-14 | 오르토-맥네일 파마슈티칼, 인코퍼레이티드 | 비-이미다졸 아릴옥시피페리딘 |
| US7186732B2 (en) * | 2000-08-08 | 2007-03-06 | Ortho-Mcneil Pharmaceutical, Inc. | Non-imidazole aryloxyalkylamines |
| WO2002076925A2 (en) | 2001-03-23 | 2002-10-03 | Eli Lilly And Company | Non-imidazole aryl alkylamines compounds as histamine h3 receptor antagonists, preparation and therapeutic uses |
| GB0206033D0 (en) * | 2002-03-14 | 2002-04-24 | Pfizer Ltd | Compounds useful in therapy |
| ATE461178T1 (de) | 2003-07-29 | 2010-04-15 | High Point Pharmaceuticals Llc | Pyridazinyl-piperazine und deren verwendung als histamin-h3-rezeptorliganden |
| WO2007052124A1 (en) * | 2005-11-04 | 2007-05-10 | Pfizer Limited | Tetrahydronaphthyridine derivative |
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