AR043038A1 - Compuestos de pirazolotriazina y usos de los mismos - Google Patents
Compuestos de pirazolotriazina y usos de los mismosInfo
- Publication number
- AR043038A1 AR043038A1 ARP040100365A ARP040100365A AR043038A1 AR 043038 A1 AR043038 A1 AR 043038A1 AR P040100365 A ARP040100365 A AR P040100365A AR P040100365 A ARP040100365 A AR P040100365A AR 043038 A1 AR043038 A1 AR 043038A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- members
- partially
- fully saturated
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 abstract 11
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 9
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 125000001424 substituent group Chemical group 0.000 abstract 9
- 125000001072 heteroaryl group Chemical group 0.000 abstract 8
- 125000003118 aryl group Chemical group 0.000 abstract 7
- -1 cyano, hydroxy, amino Chemical group 0.000 abstract 7
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 7
- 239000000126 substance Substances 0.000 abstract 7
- 125000002252 acyl group Chemical group 0.000 abstract 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 125000004442 acylamino group Chemical group 0.000 abstract 5
- 125000004423 acyloxy group Chemical group 0.000 abstract 5
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 5
- 125000002837 carbocyclic group Chemical group 0.000 abstract 5
- 150000003951 lactams Chemical group 0.000 abstract 5
- 150000002596 lactones Chemical group 0.000 abstract 5
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 4
- 239000005977 Ethylene Substances 0.000 abstract 4
- 125000006594 (C1-C3) alkylsulfony group Chemical group 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 102000018208 Cannabinoid Receptor Human genes 0.000 abstract 2
- 108050007331 Cannabinoid receptor Proteins 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 229940002612 prodrug Drugs 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 125000003107 substituted aryl group Chemical group 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 abstract 1
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 abstract 1
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 abstract 1
- 241001465754 Metazoa Species 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- HQABUPZFAYXKJW-UHFFFAOYSA-N butan-1-amine Chemical group CCCCN HQABUPZFAYXKJW-UHFFFAOYSA-N 0.000 abstract 1
- HPNMFZURTQLUMO-UHFFFAOYSA-N diethylamine Chemical group CCNCC HPNMFZURTQLUMO-UHFFFAOYSA-N 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 239000003446 ligand Substances 0.000 abstract 1
- 125000000040 m-tolyl group Chemical group [H]C1=C([H])C(*)=C([H])C(=C1[H])C([H])([H])[H] 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 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
- 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
- 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
-
- 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
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- 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
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- 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
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- 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
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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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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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
- A61P25/20—Hypnotics; Sedatives
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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
- A61P25/22—Anxiolytics
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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
- A61P25/24—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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
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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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/34—Tobacco-abuse
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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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
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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
- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Gynecology & Obstetrics (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Emergency Medicine (AREA)
- Anesthesiology (AREA)
- Rheumatology (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Child & Adolescent Psychology (AREA)
- Pregnancy & Childbirth (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se describen compuestos que actúan como ligandos de receptor de cannabinoides y sus usos en el tratamiento d enfermedades ligadas a la mediación de los receptores de cannabinoides en animales. También se presentan sus composiciones farmacéuticas y procesos para su preparación. Reivindicación 1: Un compuesto de fórmula (1) caracterizado porque R1 es un arilo opcionalmente sustituido o un heteroarilo opcionalmente sustituido; R2 es un arilo opcionalmente sustituido o un heteroarilo opcionalmente sustituido; R3 es H, alquilo C1-4, alquilo C1-4 sustituido con halo o alcoxi C1-4; R4 es (i) un grupo que tiene la fórmula (2) o fórmula (3) en las que R4a es H o alquilo C1-3; cada R4b y R4b´ es independientemente H, ciano, hidroxi, amino, H2NC(O)-, o un resto químico seleccionado del grupo constituido por alquilo C1-6, alcoxi C1-6, aciloxi, acilo,. Alquil C1-3-O-C(O)-, alquil C1-4-NH-C(O)-, (alquil C1-4)2N-C(O)-, alquil C1-4-amino-, (alquil C1-4)2amino, cicloalquil C3-5amino, acilamino, arilalquil C1-4amino-,heteroarilalquil C1-4amino-, arilo, heteroarilo, un heterociclo parcial o totalmente saturado de 3 a 6 miembros y un anillo carbocíclico parcial o totalmente saturado de 3 a 6 miembros, estando opcionalmente sustituido el resto con uno o más sustituyentes, o R4b o R4b´ tomado conjuntamente con R4e, R4e´ , R4f o R4f´ forma un enlace, un puente metileno o un puente etileno; X es un enlace, -CH2CH2- o -C(R4c)(R4c´)-, siendo cara R3c y R4c´ independientemente H, ciano, hidroxi, amino, H2NC(O)- o un resto químico seleccionado del grupo constituido por alquilo C1-6, alcoxi C1-6, aciloxi, acilo, alquil C1-3-O-C(O)-, alquil C1-4-NH-C(O)-, (alquil C1-4)2N-C(O)-, alquil C1-6aminio-, dialquil C1-4amino-, cicloalquil C23-6amino, acilamino-, arilalquil C1-4amino-, heteroarilalquil C1-4amino-, arilo, heteroarilo, un heterociclo parcial o totalmente saturado de 3 a 6 miembros y un anillo carbocíclico parcial o totalmente saturado de 3 a 6 miembros, estando opcionalmente sustituido dicho resto con uno o más sustituyentes, o R4c o R4c´ tomado conjuntamente con R4e, R4e´, R4f o R4f´ forma un enlace, un puente metileno o un puente etileno; Y es O, S, -C(O)-o -C(R4d)(R4d´), siendo cada R4d y R4d´ independientemente H, ciano, hidroxi, amino, H2NC(O)-, o un resto químico seleccionado del grupo constituido por alquilo C1-6, alcoxi C1-6, aciloxi, acilo, alquil C1-3-O-C(O)-, alquil C1-4-NH-C(O)-, (alquil C1-4)2N-C(O)-, alquil C1-6-amino-, dialquil C1-4-amino-, cicloalquil C3-6amino-, acilamino-, arilalquil C1-4amino-, heteroarilalquil C1-4amino-, arilo, heteroarilo, un heterociclo parcial o totalmente saturado de 3 a 6 miembros y un anillo carbocíclico parcial o totalmente saturado de 3 a 6 miembros, estando opcionalmente sustituido dicho resto con uno o más sustituyentes, o R4d y R4d´ tomados conjuntamente forman un anillo heterocíclico parcial o totalmente saturado de 3 a 6 miembros, un anillo lactona de 5 o 6 miembros o u anillo lactama de 4 a 6 miembros, estando opcionalmente sustituido dicho anillo heterocíclico, dicho anillo lactona y dicho anillo lactama con uno o más sustituyentes, y conteniendo opcionalmente dicho anillo lactona y dicho anillo lactama un heteroátomo adicional seleccionado de O, N o S, o Y es -NR4"-, siendo R4" un H o un resto químico seleccionado del grupo constituido por alquilo C1-6, cicloalquilo C3-6, alquil C1-3sulfonilo-, alquil C1-3aminosulfonilo-, dialquil C1-3aminosulfonilo-, acilo, alquil C1-6-O-C(O)-, arilo y heteroarilo, estando opcionalmente sustituido dicho resto con uno o más sustituyentes; Z es un enlace, -CH2CH2- o -C(R4e)(R4e´)-, siendo cada R4e y R4e´ independientemente H, ciano, amino, H2NC(O)- o un resto químico seleccionado del grupo constituido por alquilo C1-6, alcoxi C1-6, aciloxi, acilo, alquil C1-3-O-C(O)-, alquil C1-4-NH-C(O)-, (alquil C1-4)2N-C(O)-, alquil C1-6amino-, dialquil C1-4amino-, cicloalquil C3-6amino-, acilamino-, arilalquil C1-4amino-, heteroarilalquil C1-4amino-, arilo, heteroarilo, un heterociclo parcial o totalmente saturado de 3 a 6 miembros y un anillo carbocíclico parcial o totalmente saturado de 3 a 6 miembros, estando opcionalmente sustituido dicho resto con uno o más sustituyentes, o R4e y R4e´ tomado conjuntamente con R4b, R4b´, R4c o R4c´ forman un enlace, un puente metileno o un puente etileno; y cada R4f y R4f´ es independientemente H, ciano, hidroxi, amino, H2NC(O)- o un resto químico seleccionado del grupo constituido por alquilo C1-6, alcoxi C1-6, aciloxi, acilo, alquil C1-3-O-C(O)-, alquil C1-4-NH-C(O)-, (alquil C1-4)2N-C(O)-, alquil C1-6amino-, dialquil C1-4amino-, cicloalquil C3-6amino-, acilamino-, arilalquil C1-4amino-, heteroarilalquil C1-4amino-, arilo, heteroarilo, un heterociclo parcial o totalmente saturado de 3 a 6 miembros y un anillo carbocíclico parcial o totalmente saturado de 3 a 6 miembros, estando opcionalmente sustituido dicho resto con uno o más sustituyentes, o R4f o R4f´ tomados conjuntamente con Rb, R4b´, R4c o R4c´ forma un enlace, un puente metileno o un puente etileno; (ii) un grupo que tiene la fórmula (4) en la que cada R5 y R6 es independientemente H o alquilo C1-4, y R7 es un alquilo C1-4 opcionalmente sustituido, o un anillo heterocíclico parcial o totalmente saturado de 4 a 6 miembros opcionalmente sustituido que contiene de 1 a 2 heteroátomos independientemente seleccionados de O, S o N, o R5 y R6 o R5 y R7 tomados conjuntamente forman una lactona de 5 o 6 miembros, una lactama de 4 a 6 miembros o un heterociclo parcial o totalmente saturado de 4 a 6 miembros que contiene de 1 a 2 heteroátomos independientemente seleccionados de O, S, o N, estando opcionalmente sustituidos dicha lactona, dicha lactama y dicho heterociclo con uno o más sustituyentes; o (iii) un grupo amino que tiene unido al mismo al menos un resto químico seleccionado del grupo constituido por alquilo C1-8, arilalquilo C1-4, un cicloalquilo C3-8 parcial o totalmente saturado, hidroxialquilo C1-6, alcoxi C1-3-alquilo C1-6, heteroarilalquilo C1-3, arilo, heteroarilo y un heterociclo total o parcialmente saturado, estando dicho resto opcionalmente sustituido con uno o más sustituyentes y a condición de que R4 no es n-butilamina o dietilamina cuando R1 sea fenilo, ?-tolilo o p-metoxifenilo, y R2 sea fenilo o m-tolilo; una sal farmacéuticamente aceptable del mismo, un profármaco de dicho compuesto o dicha sal, o un solvato o hidrato de dicho compuesto, dicha sal o dicho profármaco.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US44572803P | 2003-02-06 | 2003-02-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR043038A1 true AR043038A1 (es) | 2005-07-13 |
Family
ID=32851000
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040100365A AR043038A1 (es) | 2003-02-06 | 2004-02-05 | Compuestos de pirazolotriazina y usos de los mismos |
Country Status (29)
| Country | Link |
|---|---|
| US (1) | US7329658B2 (es) |
| EP (1) | EP1592691A1 (es) |
| JP (1) | JP4018736B2 (es) |
| KR (1) | KR20050099531A (es) |
| CN (1) | CN1768061A (es) |
| AP (1) | AP2005003368A0 (es) |
| AR (1) | AR043038A1 (es) |
| AU (1) | AU2004209447A1 (es) |
| BR (1) | BRPI0406957A (es) |
| CA (1) | CA2513409A1 (es) |
| CL (1) | CL2004000182A1 (es) |
| CR (1) | CR7932A (es) |
| EA (1) | EA200501253A1 (es) |
| EC (1) | ECSP055945A (es) |
| GT (1) | GT200400013A (es) |
| HR (1) | HRP20050659A2 (es) |
| IS (1) | IS7936A (es) |
| MA (1) | MA27652A1 (es) |
| MX (1) | MXPA05007562A (es) |
| NL (1) | NL1025404C2 (es) |
| NO (1) | NO20054082L (es) |
| OA (1) | OA12980A (es) |
| PE (1) | PE20040946A1 (es) |
| PL (1) | PL379009A1 (es) |
| TN (1) | TNSN05190A1 (es) |
| TW (1) | TWI260223B (es) |
| UY (1) | UY28178A1 (es) |
| WO (1) | WO2004069837A1 (es) |
| ZA (1) | ZA200506255B (es) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE375349T1 (de) * | 2002-08-02 | 2007-10-15 | Merck & Co Inc | Substituierte furo(2,3-b)pyridin derivate |
| US7176210B2 (en) | 2003-02-10 | 2007-02-13 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
| US7268133B2 (en) | 2003-04-23 | 2007-09-11 | Pfizer, Inc. Patent Department | Cannabinoid receptor ligands and uses thereof |
| US7145012B2 (en) | 2003-04-23 | 2006-12-05 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
| US7141669B2 (en) * | 2003-04-23 | 2006-11-28 | Pfizer Inc. | Cannabiniod receptor ligands and uses thereof |
| US20040214856A1 (en) * | 2003-04-23 | 2004-10-28 | Pfizer Inc | Cannabinoid receptor ligands and uses thereof |
| CA2524397A1 (en) * | 2003-05-07 | 2004-11-18 | Pfizer Products Inc. | Cannabinoid receptor ligands and uses thereof |
| US20040224962A1 (en) * | 2003-05-09 | 2004-11-11 | Pfizer Inc | Pharmaceutical composition for the treatment of obesity or to facilitate or promote weight loss |
| US7232823B2 (en) * | 2003-06-09 | 2007-06-19 | Pfizer, Inc. | Cannabinoid receptor ligands and uses thereof |
| US20050026983A1 (en) * | 2003-07-30 | 2005-02-03 | Pfizer Inc | Imidazole compounds and uses thereof |
| US20050043327A1 (en) * | 2003-08-21 | 2005-02-24 | Pfizer Inc | Pharmaceutical composition for the prevention and treatment of addiction in a mammal |
| US7151097B2 (en) * | 2003-11-07 | 2006-12-19 | Pfizer Inc. | Bicyclic pyrazolyl and imidazolyl compounds and uses thereof |
| WO2005049615A1 (en) * | 2003-11-21 | 2005-06-02 | Pfizer Products Inc. | Pyrazolo`1,5-a!`1,3,5! triazin -4-one derivatives as cb1 receptor antagonists |
| US7649002B2 (en) | 2004-02-04 | 2010-01-19 | Pfizer Inc | (3,5-dimethylpiperidin-1yl)(4-phenylpyrrolidin-3-yl)methanone derivatives as MCR4 agonists |
| US7262318B2 (en) * | 2004-03-10 | 2007-08-28 | Pfizer, Inc. | Substituted heteroaryl- and phenylsulfamoyl compounds |
| US20050288340A1 (en) * | 2004-06-29 | 2005-12-29 | Pfizer Inc | Substituted heteroaryl- and phenylsulfamoyl compounds |
| PA8660701A1 (es) | 2005-02-04 | 2006-09-22 | Pfizer Prod Inc | Agonistas de pyy y sus usos |
| CA2609783A1 (en) * | 2005-05-27 | 2006-12-07 | Pfizer Products Inc. | Combination of a cannabinoid-1- receptor-antagonist and a microsomal triglyceride transfer protein inhibitor for treating obesity or mainataining weight loss |
| US7923465B2 (en) | 2005-06-02 | 2011-04-12 | Glenmark Pharmaceuticals S.A. | Cannabinoid receptor ligands, pharmaceutical compositions containing them, and process for their preparation |
| AU2006253842A1 (en) | 2005-06-02 | 2006-12-07 | Glenmark Pharmaceuticals S.A. | Novel cannabinoid receptor ligands, pharmaceutical compositions containing them, and process for their preparation |
| WO2006131807A1 (en) * | 2005-06-06 | 2006-12-14 | Pfizer Products Inc. | Preparation of 3-amino-4,5-disubstituted-pyrazole derivatives |
| BRPI0613505A2 (pt) | 2005-06-30 | 2011-01-11 | Prosidion Ltd | agonistas de gpcr |
| US7741317B2 (en) | 2005-10-21 | 2010-06-22 | Bristol-Myers Squibb Company | LXR modulators |
| JP4847275B2 (ja) * | 2005-10-21 | 2011-12-28 | 田辺三菱製薬株式会社 | ピラゾロ［１，５−ａ］ピリミジン化合物 |
| US7888376B2 (en) | 2005-11-23 | 2011-02-15 | Bristol-Myers Squibb Company | Heterocyclic CETP inhibitors |
| SG185849A1 (en) | 2006-02-23 | 2012-12-28 | Pfizer Ltd | Melanocortin type 4 receptor agonist piperidinoylpyrrolidines |
| TWI419889B (zh) * | 2006-07-05 | 2013-12-21 | Mitsubishi Tanabe Pharma Corp | 吡唑并〔１，５-ａ〕嘧啶化合物 |
| JP2010509392A (ja) | 2006-11-13 | 2010-03-25 | ファイザー・プロダクツ・インク | ジアリール、ジピリジニルおよびアリール−ピリジニル誘導体ならびにその使用 |
| KR100808241B1 (ko) * | 2006-11-21 | 2008-03-03 | 윤성화 | Ｃｂ1에 길항 활성을 갖는 1ｈ-파이라졸-3-옥심카바메이트화합물 유도체 |
| ES2382009T3 (es) | 2006-12-01 | 2012-06-04 | Bristol-Myers Squibb Company | Derivados de N-((3-bencil)-2,2-(bis-fenil-)-propan-1-amina como inhibidores de CETP para el tratamiento de aterosclerosis y enfermedades cardiovasculares |
| GB0700122D0 (en) | 2007-01-04 | 2007-02-14 | Prosidion Ltd | GPCR agonists |
| US20100048632A1 (en) | 2007-01-04 | 2010-02-25 | Matthew Colin Thor Fyfe | Piperidine GPCR Agonists |
| WO2008081208A1 (en) | 2007-01-04 | 2008-07-10 | Prosidion Limited | Piperidine gpcr agonists |
| AR064735A1 (es) | 2007-01-04 | 2009-04-22 | Prosidion Ltd | Agonistas de gpcr y composicion farmaceutica en base al compuesto |
| CL2008000017A1 (es) | 2007-01-04 | 2008-08-01 | Prosidion Ltd | Compuestos derivados de heterociclos de nitrogeno y oxigeno, agonistas de gpcr; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de la obesidad, diabetes, sindrome metabolico, hiperlipidemia, toleranci |
| PE20090142A1 (es) * | 2007-04-11 | 2009-02-19 | Merck & Co Inc | Derivados de furo[2,3-b] piridina sustituidos como moduladores del receptor canabinoide-1 |
| JP4837701B2 (ja) * | 2007-04-20 | 2011-12-14 | 田辺三菱製薬株式会社 | 医薬組成物 |
| GB0720390D0 (en) | 2007-10-18 | 2007-11-28 | Prosidion Ltd | G-Protein coupled receptor agonists |
| GB0720389D0 (en) | 2007-10-18 | 2008-11-12 | Prosidion Ltd | G-Protein Coupled Receptor Agonists |
| SG157299A1 (en) * | 2008-05-09 | 2009-12-29 | Agency Science Tech & Res | Diagnosis and treatment of kawasaki disease |
| DK2326638T5 (da) | 2008-08-06 | 2014-01-13 | Pfizer Ltd | Diazepin- og diazocan-forbindelser som mc4-agonister |
| WO2012138945A1 (en) * | 2011-04-08 | 2012-10-11 | Aestus Therapeutics, Inc. | Methods of treating schizophrenia with pyrazole derivative inhibitors of tgf - beta |
| US8871754B2 (en) | 2012-11-19 | 2014-10-28 | Irm Llc | Compounds and compositions for the treatment of parasitic diseases |
| RS56720B1 (sr) | 2012-11-19 | 2018-03-30 | Novartis Ag | Jedinjenja i kompozicije za lečenje parazitskih oboljenja |
| EP3750891A4 (en) * | 2018-02-06 | 2021-08-11 | Jiangsu Hengrui Medicine Co., Ltd. | PYRAZOLO [1,5-A] [1,3,5] TRIAZINE-2-AMINE DERIVATIVE, METHOD OF PREPARATION AND MEDICAL USE |
| CN110551133A (zh) * | 2019-07-23 | 2019-12-10 | 上海合全药业股份有限公司 | 叔丁基-5-(羟甲基)-7-氧杂-2-氮杂螺[3.5]壬烷-2-甲酸基酯的制法 |
| CN112592346B (zh) * | 2019-07-30 | 2022-04-26 | 厦门宝太生物科技股份有限公司 | 一种a2a和/或a2b抑制剂中间体的制备方法 |
| SI4106876T1 (sl) | 2020-02-18 | 2025-11-28 | Gilead Sciences, Inc. | Protivirusne spojine |
| TWI775313B (zh) | 2020-02-18 | 2022-08-21 | 美商基利科學股份有限公司 | 抗病毒化合物 |
| TWI883391B (zh) | 2020-02-18 | 2025-05-11 | 美商基利科學股份有限公司 | 抗病毒化合物 |
| JP7688152B2 (ja) | 2021-04-16 | 2025-06-03 | ギリアード サイエンシーズ， インコーポレイテッド | アミドを使用してカルバヌクレオシドを調製する方法 |
| EP4387977A1 (en) | 2021-08-18 | 2024-06-26 | Gilead Sciences, Inc. | Phospholipid compounds and methods of making and using the same |
Family Cites Families (98)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US574491A (en) * | 1897-01-05 | Brake-beam | ||
| US3865824A (en) | 1972-03-07 | 1975-02-11 | Icn Pharmaceuticals | 2-Aryl-7-substituted pyrazolo {8 1,5{i a{b {9 1,3,5-triazines |
| US3910907A (en) | 1973-07-09 | 1975-10-07 | Icn Pharmaceuticals | Pyrazolo(1,5-a)-1,3,5-triazines |
| US3995039A (en) | 1975-05-27 | 1976-11-30 | Merck & Co., Inc. | Pyrazolo [1,5-a] [1,3,5] triazines |
| CH635587A5 (fr) | 1978-01-09 | 1983-04-15 | Aron Sa | Derives amines de pyrazolo (1,5-a) s.triazine, therapeutiquement actifs et leurs procedes de preparation. |
| US4734414A (en) | 1985-06-06 | 1988-03-29 | Biomeasure, Inc. | Anti-inflammatory and anti-arthritic pyrazolo-[1,5-a]-1,3,5-triazine derivatives, compositions, and method of use therefor |
| US4767858A (en) | 1985-06-06 | 1988-08-30 | Biomeasure, Incorporated | Anti-arthritic pyrazolo-triazine derivatives |
| GB8613591D0 (en) | 1986-06-04 | 1986-07-09 | Roussel Lab Ltd | Chemical compounds |
| DE3775527D1 (de) | 1986-10-22 | 1992-02-06 | Ciba Geigy Ag | 1,5-diphenylpyrazol-3-carbonsaeurederivate zum schuetzen von kulturpflanzen. |
| US4824834A (en) | 1986-10-31 | 1989-04-25 | Otsuka Pharmaceutical Company, Limited | Pyrazolotriazine compounds |
| US5051518A (en) | 1987-05-29 | 1991-09-24 | Ortho Pharmaceutical Corporation | Pharmacologically active 2- and 3-substituted (1',5'-diaryl-3-pyrazolyl)-N-hydroxypropanamides |
| AU611437B2 (en) | 1987-05-29 | 1991-06-13 | Ortho Pharmaceutical Corporation | Pharmacologically active 2- and 3-substituted (1',5'-diaryl-3-pyrazolyl)-n-hydroxypropanamides and method for synthesizing the same |
| US5055479A (en) | 1988-06-16 | 1991-10-08 | Sankyo Company, Limited | Method of treating cachexia |
| CA1330079C (en) | 1988-10-13 | 1994-06-07 | Michihiko Tsujitani | Pyrrolo (3,2-e)pyrazolo(1,5-a)pyrimidine derivative and medicine comprising the same |
| JP2691317B2 (ja) | 1989-08-25 | 1997-12-17 | 株式会社大塚製薬工場 | ４―ヒドロキシ―８―（３―低級アルコキシ―４―フェニルスルフィニルフェニル）ピラゾロ〔１，５―ａ〕―１，３，５―トリアジン光学活性体の塩類及びその製造方法 |
| PH27357A (en) | 1989-09-22 | 1993-06-21 | Fujisawa Pharmaceutical Co | Pyrazole derivatives and pharmaceutical compositions comprising the same |
| US5356894A (en) | 1990-05-29 | 1994-10-18 | Rodney Peter W | Morpholinyl substituted [1,2,4]-triazolo[1,5-a]triazine as antagonist |
| EP0459702A1 (en) | 1990-05-29 | 1991-12-04 | Zeneca Limited | Azole Derivatives |
| FR2665898B1 (fr) | 1990-08-20 | 1994-03-11 | Sanofi | Derives d'amido-3 pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| EP0503099A4 (en) | 1990-10-09 | 1993-12-01 | Otsuka Pharmaceutical Co., Ltd. | Pyrimidine derivative, production thereof, and androgen inhibitor |
| GB9111130D0 (en) | 1991-05-23 | 1991-07-17 | Ici Plc | Azole derivatives |
| GB9111131D0 (en) | 1991-05-23 | 1991-07-17 | Ici Plc | Heterocyclic compounds |
| GB9125002D0 (en) | 1991-11-25 | 1992-01-22 | Ici Plc | Azole derivatives |
| FR2692575B1 (fr) | 1992-06-23 | 1995-06-30 | Sanofi Elf | Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| US5571813A (en) | 1993-06-10 | 1996-11-05 | Beiersdorf-Lilly Gmbh | Fused pyrimidine compounds and their use as pharmaceuticals |
| FR2714057B1 (fr) | 1993-12-17 | 1996-03-08 | Sanofi Elf | Nouveaux dérivés du 3-pyrazolecarboxamide, procédé pour leur préparation et compositions pharmaceutiques les contenant. |
| US5596106A (en) | 1994-07-15 | 1997-01-21 | Eli Lilly And Company | Cannabinoid receptor antagonists |
| FR2741621B1 (fr) | 1995-11-23 | 1998-02-13 | Sanofi Sa | Nouveaux derives de pyrazole, procede pour leur preparation et compositions pharmaceutiques en contenant |
| FR2742148B1 (fr) | 1995-12-08 | 1999-10-22 | Sanofi Sa | Nouveaux derives du pyrazole-3-carboxamide, procede pour leur preparation et compositions pharmaceutiques les contenant |
| RO121272B1 (ro) | 1996-07-24 | 2007-02-28 | The Du Pont Merck Pharmaceutical Company | Azolotriazine şi pirimidine |
| US6313124B1 (en) | 1997-07-23 | 2001-11-06 | Dupont Pharmaceuticals Company | Tetrazine bicyclic compounds |
| US6191131B1 (en) | 1997-07-23 | 2001-02-20 | Dupont Pharmaceuticals Company | Azolo triazines and pyrimidines |
| US6124289A (en) | 1996-07-24 | 2000-09-26 | Dupont Pharmaceuticals Co. | Azolo triazines and pyrimidines |
| US6060478A (en) | 1996-07-24 | 2000-05-09 | Dupont Pharmaceuticals | Azolo triazines and pyrimidines |
| EP0971588B1 (en) | 1997-01-21 | 2004-03-17 | Smithkline Beecham Corporation | Novel cannabinoid receptor modulators |
| FR2758723B1 (fr) | 1997-01-28 | 1999-04-23 | Sanofi Sa | Utilisation des antagonistes des recepteurs aux cannabinoides centraux pour la preparation de medicaments |
| FR2761266B1 (fr) | 1997-03-28 | 1999-07-02 | Sanofi Sa | Composition pharmaceutique formee par granulation humide pour l'administration orale d'un derive du n-piperidino-3- pyrazolecarboxamide, de ses sels et de leurs solvates |
| IL137019A (en) | 1998-01-28 | 2010-11-30 | Du Pont Pharm Co | 2,7 - dimethyl - 4 - (substituted amino) - 8 - arylpyrazolo [1,5-a] triazine derivatives and pharmaceutical compositions containing them |
| US6194410B1 (en) | 1998-03-11 | 2001-02-27 | Hoffman-La Roche Inc. | Pyrazolopyrimidine and pyrazolines and process for preparation thereof |
| US6509338B1 (en) | 1998-06-22 | 2003-01-21 | Bristol-Myers Squibb Company | Pyrazolo[1,5-A]triazine corticotropin releasing factor antagonists |
| FR2783246B1 (fr) | 1998-09-11 | 2000-11-17 | Aventis Pharma Sa | Derives d'azetidine, leur preparation et les medicaments les contenant |
| IL141769A0 (en) | 1998-09-11 | 2002-03-10 | Aventis Pharma Sa | Azetidine derivatives, preparation and medicines containing them |
| FR2789079B3 (fr) | 1999-02-01 | 2001-03-02 | Sanofi Synthelabo | Derive d'acide pyrazolecarboxylique, sa preparation, les compositions pharmaceutiques en contenant |
| OA12049A (en) | 1999-09-30 | 2006-05-02 | Neurogen Corp | Amino substituted pyrazoloÄ1,5,-aÜ-1,5-pyrimidinesand pyrazoloÄ1,5,-aÜ-1,3,5-triazines. |
| EP1218379A2 (en) | 1999-09-30 | 2002-07-03 | Neurogen Corporation | CERTAIN ALKYLENE DIAMINE-SUBSTITUTED PYRAZOLO 1,5,-a]-1,5-PYRIMIDINES AND PYRAZOLO 1,5-a]-1,3,5-TRIAZINES |
| FR2799124B1 (fr) | 1999-10-01 | 2004-08-13 | Sanofi Synthelabo | Utilisation des antagonistes des recepteurs aux cannabinoides centraux pour la preparation de medicaments |
| EP1223929B1 (en) | 1999-10-18 | 2006-08-23 | The University Of Connecticut | Cannabimimetic indole derivatives |
| MXPA02005100A (es) | 1999-10-18 | 2003-09-25 | Alexipharma Inc | Derivados de pirazol antagonistas de receptor de canabinoide. |
| FR2800372B1 (fr) | 1999-11-03 | 2001-12-07 | Sanofi Synthelabo | Derives tricycliques d'acide 1-benzylpyrazole-3- carboxylique, leur preparation, les medicaments en contenant |
| FR2800375B1 (fr) | 1999-11-03 | 2004-07-23 | Sanofi Synthelabo | Derives tricycliques d'acide pyrazolecarboxylique, leur preparation, les compositions pharmaceutiques en contenant |
| WO2001054695A1 (en) | 2000-01-31 | 2001-08-02 | The University Of Kentucky Research Foundation | Triazines as appetite suppressor |
| FR2804604B1 (fr) | 2000-02-09 | 2005-05-27 | Sanofi Synthelabo | Utilisation d'un antagoniste des recepteurs aux cannabinoides centraux pour la preparation de medicaments utiles pour faciliter l'arret de la consommation de tabac |
| JP2004502642A (ja) | 2000-02-11 | 2004-01-29 | ブリストル−マイヤーズ スクイブ カンパニー | カンナビノイドレセプターモジュレーター、それらの製造方法、および呼吸系および非呼吸系疾患の処置のためのカンナビノイドレセプターモジュレーターの使用 |
| US6479479B2 (en) | 2000-03-03 | 2002-11-12 | Aventis Pharma S.A. | Azetidine derivatives, their preparation and pharmaceutical compositions containing them |
| US6566356B2 (en) | 2000-03-03 | 2003-05-20 | Aventis Pharma S.A. | Pharmaceutical compositions containing 3-aminoazetidine derivatives, novel derivatives and their preparation |
| US6355631B1 (en) | 2000-03-03 | 2002-03-12 | Aventis Pharma S.A. | Pharmaceutical compositions containing azetidine derivatives, novel azetidine derivatives and their preparation |
| CN1205188C (zh) | 2000-03-23 | 2005-06-08 | 索尔瓦药物有限公司 | 具有cb1－拮抗活性的4,5－二氢－1h－吡唑衍生物 |
| FR2809621B1 (fr) | 2000-05-12 | 2002-09-06 | Sanofi Synthelabo | Utilisation d'un antagoniste des recepteurs aux cannabinoides centraux pour la preparation de medicaments utiles comme antidiarrheiques |
| US20020019421A1 (en) | 2000-07-05 | 2002-02-14 | Roni Biberman | Compositions and therapy for substance addiction |
| US20020091114A1 (en) | 2000-10-04 | 2002-07-11 | Odile Piot-Grosjean | Combination of a CB1 receptor antagonist and of sibutramine, the pharmaceutical compositions comprising them and their use in the treatment of obesity |
| FR2814678B1 (fr) * | 2000-10-04 | 2002-12-20 | Aventis Pharma Sa | Association d'un antagoniste du recepteur cb1 et de sibutramine, les compositions pharmaceutiques les contenant et leur utilisation pour la traitement de l'obesite |
| CA2432148C (en) | 2000-12-28 | 2011-01-18 | Ono Pharmaceutical Co., Ltd. | Tri-heterocyclic compounds and a pharmaceutical comprising them as an active ingredient |
| RS50863B (sr) | 2001-03-13 | 2010-08-31 | Bristol-Myers Squibb Pharma Company | 4-(2-butilamino)-2,7-dimetil-8-(2-metil-6-metoksipirid-3-il) pirazolo/1,5a/-1,3,5-triazin,njegovi enantiomeri i farmaceutski prihvatljive soli kao ligandi receptora za faktor koji oslobađa kortikotropin |
| AU2002256690B2 (en) | 2001-03-22 | 2006-05-18 | Solvay Pharmaceuticals B.V. | 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity |
| ITMI20011483A1 (it) | 2001-07-11 | 2003-01-11 | Res & Innovation Soc Coop A R | Uso di composti come antagonisti funzionali ai recettori centrali deicannabinoidi |
| WO2003007887A2 (en) | 2001-07-20 | 2003-01-30 | Merck & Co., Inc. | Substituted imidazoles as cannabinoid receptor modulators |
| FR2829028B1 (fr) | 2001-08-29 | 2004-12-17 | Aventis Pharma Sa | Association d'un antagoniste du recepteur cb1 et d'un produit qui active la neurotransmission dopaminergique dans le cerveau, les compositions pharmaceutiques les contenant et leur utilisation pour le traitement de la maladie de |
| FR2829027A1 (fr) | 2001-08-29 | 2003-03-07 | Aventis Pharma Sa | Association avec un antagoniste du recepteur cb1, les compositions pharmaceutiques les contenant et leur utilisation pour le traitement de la maladie de parkinson |
| JP2005507875A (ja) | 2001-08-31 | 2005-03-24 | ユニバーシティ オブ コネチカット | カンナビノイド受容体に作用する新規なピラゾール類似体 |
| TWI231757B (en) | 2001-09-21 | 2005-05-01 | Solvay Pharm Bv | 1H-Imidazole derivatives having CB1 agonistic, CB1 partial agonistic or CB1-antagonistic activity |
| US6974810B2 (en) | 2001-09-21 | 2005-12-13 | Solvay Pharmaceuticals B.V. | 4,5-Dihydro-1H-pyrazole derivatives having potent CB1-antagonistic activity |
| HUP0401567A3 (en) | 2001-09-21 | 2005-06-28 | Solvay Pharm Bv | Novel 4,5-dyhydro-1h-pyrazole derivatives having cb1-antagonistic activity, their use and pharmaceutical compositions containing them |
| US6509367B1 (en) | 2001-09-22 | 2003-01-21 | Virginia Commonwealth University | Pyrazole cannabinoid agonist and antagonists |
| JP2005532982A (ja) | 2001-09-24 | 2005-11-04 | バイエル・フアーマシユーチカルズ・コーポレーシヨン | 肥満の処置のためのピロール誘導体の製造及び使用 |
| HN2002000266A (es) | 2001-09-24 | 2003-11-16 | Bayer Corp | Preparacion y uso de derivados de imidazol para el tratamiento de la obesidad. |
| WO2003027114A1 (en) | 2001-09-24 | 2003-04-03 | Bayer Pharmaceuticals Corporation | Preparation and use of 1,5,6,7-tetrahydropyrrolo[3,2-c]pyridine derivatives for treatment of obesity |
| SE0104332D0 (sv) | 2001-12-19 | 2001-12-19 | Astrazeneca Ab | Therapeutic agents |
| SE0104330D0 (sv) | 2001-12-19 | 2001-12-19 | Astrazeneca Ab | Therapeutic agents |
| US20030139386A1 (en) | 2001-12-21 | 2003-07-24 | Sophie Cote | Pharmaceutical compositions based on azetidine derivatives |
| US20050171161A1 (en) | 2002-03-06 | 2005-08-04 | Fong Tung M. | Method of treatment or prevention of obesity |
| AU2003217712A1 (en) | 2002-03-07 | 2003-09-22 | Smithkline Beecham Corporation | Pyrazolopyrimidine and pyrazolotriazine derivatives and pharmaceutical compositions containing them |
| EP1496838B1 (en) | 2002-03-12 | 2010-11-03 | Merck Sharp & Dohme Corp. | Substituted amides |
| AR038966A1 (es) | 2002-03-18 | 2005-02-02 | Solvay Pharm Bv | Derivados de tiazol que tienen actividad antagonista, agonista o agonista parcial de cb1 |
| WO2003082190A2 (en) | 2002-03-26 | 2003-10-09 | Merck & Co., Inc. | Spirocyclic amides as cannabinoid receptor modulators |
| ES2192494B1 (es) | 2002-03-27 | 2005-02-16 | Consejo Superior De Investigaciones Cientificas | Derivados de 1,2,4-triazol con propiedades cannabinoides. |
| AU2003225964B2 (en) | 2002-03-28 | 2008-11-20 | Merck Sharp & Dohme Corp. | Substituted 2,3-diphenyl pyridines |
| FR2837706A1 (fr) | 2002-03-28 | 2003-10-03 | Sanofi Synthelabo | Utilisation d'un antagoniste des recepteurs aux cannabinoides cb1 pour la preparation de medicaments utiles pour traiter les dysfonctionnements sexuels et/ou ameliorer les performances sexuelles |
| CA2480856A1 (en) | 2002-04-05 | 2003-10-23 | Merck & Co., Inc. | Substituted aryl amides |
| FR2838439B1 (fr) | 2002-04-11 | 2005-05-20 | Sanofi Synthelabo | Derives de terphenyle, leur preparation, les compositions pharmaceutqiues en contenant |
| JP4459629B2 (ja) | 2002-04-12 | 2010-04-28 | メルク エンド カムパニー インコーポレーテッド | 二環式アミド |
| US6825209B2 (en) | 2002-04-15 | 2004-11-30 | Research Triangle Institute | Compounds having unique CB1 receptor binding selectivity and methods for their production and use |
| ES2287476T3 (es) | 2002-05-10 | 2007-12-16 | Smithkline Beecham Corporation | Pirazolopirimidinas sustituidas. |
| CN100366207C (zh) | 2002-08-02 | 2008-02-06 | 华沙整形外科股份有限公司 | 用于照明手术空间的系统和技术 |
| UA80295C2 (en) | 2002-09-06 | 2007-09-10 | Biogen Inc | Pyrazolopyridines and using the same |
| EP1556373A1 (en) | 2002-10-18 | 2005-07-27 | Pfizer Products Inc. | Cannabinoid receptor ligands and uses thereof |
| US7129239B2 (en) | 2002-10-28 | 2006-10-31 | Pfizer Inc. | Purine compounds and uses thereof |
| US7247628B2 (en) | 2002-12-12 | 2007-07-24 | Pfizer, Inc. | Cannabinoid receptor ligands and uses thereof |
| TWI290500B (en) * | 2004-12-14 | 2007-12-01 | Arima Optoelectronics Corp | Laser dicing apparatus for a silicon wafer and dicing method thereof |
-
2004
- 2004-01-21 US US10/763,105 patent/US7329658B2/en not_active Expired - Fee Related
- 2004-01-26 AP AP2005003368A patent/AP2005003368A0/xx unknown
- 2004-01-26 WO PCT/IB2004/000269 patent/WO2004069837A1/en not_active Ceased
- 2004-01-26 EA EA200501253A patent/EA200501253A1/ru unknown
- 2004-01-26 CN CNA2004800091255A patent/CN1768061A/zh active Pending
- 2004-01-26 EP EP04705138A patent/EP1592691A1/en not_active Withdrawn
- 2004-01-26 PL PL379009A patent/PL379009A1/pl not_active Application Discontinuation
- 2004-01-26 CA CA002513409A patent/CA2513409A1/en not_active Abandoned
- 2004-01-26 HR HR20050659A patent/HRP20050659A2/hr not_active Application Discontinuation
- 2004-01-26 JP JP2006500314A patent/JP4018736B2/ja not_active Expired - Fee Related
- 2004-01-26 AU AU2004209447A patent/AU2004209447A1/en not_active Abandoned
- 2004-01-26 MX MXPA05007562A patent/MXPA05007562A/es unknown
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- 2004-01-26 KR KR1020057014432A patent/KR20050099531A/ko not_active Abandoned
- 2004-01-26 OA OA1200500215A patent/OA12980A/en unknown
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2005
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