HUP0402150A2 - A CB1 jelzésű kannabinoid receptorra nézve agonista, parciális agonista vagy antagonista hatású 1H-imidazol-származékok, eljárás az előállításukra, azokat tartalmazó gyógyszerkészítmények és alkalmazásuk gyógyszerkészítmények előállítására - Google Patents
A CB1 jelzésű kannabinoid receptorra nézve agonista, parciális agonista vagy antagonista hatású 1H-imidazol-származékok, eljárás az előállításukra, azokat tartalmazó gyógyszerkészítmények és alkalmazásuk gyógyszerkészítmények előállításáraInfo
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- HUP0402150A2 HUP0402150A2 HU0402150A HUP0402150A HUP0402150A2 HU P0402150 A2 HUP0402150 A2 HU P0402150A2 HU 0402150 A HU0402150 A HU 0402150A HU P0402150 A HUP0402150 A HU P0402150A HU P0402150 A2 HUP0402150 A2 HU P0402150A2
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- 238000004519 manufacturing process Methods 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 3
- 238000002360 preparation method Methods 0.000 title abstract 2
- 230000001270 agonistic effect Effects 0.000 title 2
- 239000008194 pharmaceutical composition Substances 0.000 title 2
- RAXXELZNTBOGNW-MQIHXRCWSA-N 1h-imidazole Chemical class C1=C[15NH]C=[15N]1 RAXXELZNTBOGNW-MQIHXRCWSA-N 0.000 title 1
- 230000000694 effects Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 4
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 4
- 125000004434 sulfur atom Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 125000004076 pyridyl group Chemical group 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 2
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 2
- -1 fluoroacetyl group Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000001624 naphthyl group Chemical group 0.000 abstract 2
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 2
- 125000002098 pyridazinyl group Chemical group 0.000 abstract 2
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000004306 triazinyl group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 abstract 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 238000000889 atomisation Methods 0.000 abstract 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 abstract 1
- 150000001602 bicycloalkyls Chemical group 0.000 abstract 1
- 229930003827 cannabinoid Natural products 0.000 abstract 1
- 239000003557 cannabinoid Substances 0.000 abstract 1
- 229940065144 cannabinoids Drugs 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 abstract 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 abstract 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 abstract 1
- 125000000286 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
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
- 230000018405 transmission of nerve impulse Effects 0.000 abstract 1
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
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- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
- C07D295/28—Nitrogen atoms
- C07D295/30—Nitrogen atoms non-acylated
-
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- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
- C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
- C07C257/18—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
Abstract
A találmány tárgyát képezik (I) általános képletű vegyületek, ezekprodrugjai, sztereoizomerjei és sói, az ezeket tartalmazógyógyszerkészítmények, eljárás az (I) és (II) általános képletűvegyületek, valamint az (I) általános képletű vegyületeket tartalmazógyógyszerkészítmények előállítására, eljárás az (I) általános képletűvegyületek alkalmazására a kannabinoidok közreműködésével lejátszódóidegi ingerületátvitellel kapcsolatos rendellenességek kezeléséreszolgáló gyógyszerkészítmények előállításánál, továbbá a találmánytárgyát képezik a (IX) és (X) általános képletű vegyületek is; ahol az(I) és (II) általános képletben R jelentése adott esetbenhelyettesített fenilcsoport, tienilcsoport, piridilcsoport,pirimidinilcsoport, pirazinilcsoport, piridazinilcsoport,triazinilcsoport vagy naftilcsoport, R1 jelentése adott esetbenhelyettesített fenilcsoport, piridilcsoport, pirimidinilcsoport,pirazinilcsoport, piridazinilcsoport, triazinilcsoport, naftilcsoport,vagy adott esetben helyettesített, öttagú, 1 vagy 2 nitrogénatomot,oxigénatomot és/vagy kénatomot tartalmazó aromás heterociklusoscsoport, R2 jelentése hidrogénatom, adott esetben egy kénatomot,oxigénatomot vagy nitrogénatomot tartalmazó alkilcsoport,cikloalkilcsoport, alkenilcsoport vagy cikloalkenilcsoport, R3jelentése adott esetben egy vagy több oxigénatomot, nitrogénatomotés/vagy kénatomot tartalmazó és adott esetben helyettesítettalkilcsoport, alkoxicsoport, cikloalkoxicsoport, cikloalkilcsoport,bicikloalkilcsoport, tricikloalkilcsoport, alkenilcsoport vagycikloalkenilcsoport, vagy adott esetben helyettesített benzilcsoport,fenil-etil-csoport, fenilcsoport vagy piridilcsoport, vagy NR5R6általános képletű csoport, vagy R2 és R3 együtt, továbbá azzal anitrogénatommal együtt, amelyhez kapcsolódnak, egy telített vagytelítetlen, a gyűrűben 4-10 atomot tartalmazó, adott esetbenhelyettesített és adott esetben egy vagy két nitrogénatomot,oxigénatomot és/vagy kénatomot tartalmazó heterociklusos csoportotképez, és R4 jelentése hidrogénatom, halogénatom, cianocsoport,karbamoilcsoport, formilcsoport, acetilcsoport, trifluor-acetil-csoport, fluor-acetil-csoport, propionilcsoport, szulfamoilcsoport,metánszulfonilcsoport, metil-szulfanil-csoport vagy adott esetbenhelyettesített alkilcsoport; R7 alkil vagy benzilcsoport ; R, R1 és R4jelentése az 1. igénypontban megadott, és R9 jelentésehidroxilcsoport, egyenes vagy elágazó szénláncú 1-4 szénatomosalkoxicsoport, benziloxicsoport vagy klóratom; és a (X) általánosképletben R jelentése 4-klór-fenil-csoport, 4-bróm-fenil-csoport vagy4-(trifluor--metil)-fenil-csoport. Ó
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01203851 | 2001-09-21 | ||
| PCT/EP2002/010434 WO2003027076A2 (en) | 2001-09-21 | 2002-09-17 | 1h-imidazole derivatives having cb1 agonistic, cb1 partial agonistic or cb1- antagonistic activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0402150A2 true HUP0402150A2 (hu) | 2005-02-28 |
| HUP0402150A3 HUP0402150A3 (en) | 2005-08-29 |
Family
ID=8181044
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0402150A HUP0402150A3 (en) | 2001-09-21 | 2002-09-17 | 1h-imidazole derivatives having cb1 agonistic, cb1 partial agonistic or cb1-antagonistic activity, process for the preparation, pharmaceutical compositions containing them and their use for production of pharmaceutical compositions |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US20040235854A1 (hu) |
| EP (1) | EP1438296B1 (hu) |
| JP (1) | JP4393869B2 (hu) |
| KR (1) | KR100950431B1 (hu) |
| CN (2) | CN101538244A (hu) |
| AR (1) | AR036597A1 (hu) |
| AT (1) | ATE415391T1 (hu) |
| AU (1) | AU2002337106B2 (hu) |
| BR (1) | BR0212481A (hu) |
| CA (1) | CA2457444C (hu) |
| DE (1) | DE60230054D1 (hu) |
| DK (1) | DK1438296T3 (hu) |
| ES (1) | ES2318045T3 (hu) |
| HR (1) | HRP20040185A2 (hu) |
| HU (1) | HUP0402150A3 (hu) |
| IL (2) | IL160522A0 (hu) |
| MX (1) | MXPA04002669A (hu) |
| NO (1) | NO20041171L (hu) |
| PL (1) | PL367998A1 (hu) |
| PT (1) | PT1438296E (hu) |
| RU (1) | RU2299200C2 (hu) |
| SI (1) | SI1438296T1 (hu) |
| TW (1) | TWI231757B (hu) |
| UA (1) | UA77440C2 (hu) |
| WO (1) | WO2003027076A2 (hu) |
| ZA (1) | ZA200402188B (hu) |
Families Citing this family (113)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2002319627A1 (en) | 2001-07-20 | 2003-03-03 | Merck And Co., Inc. | Substituted imidazoles as cannabinoid receptor modulators |
| US7109216B2 (en) | 2001-09-21 | 2006-09-19 | Solvay Pharmaceuticals B.V. | 1H-imidazole derivatives having CB1 agonistic, CB1 partial agonistic or CB1-antagonistic activity |
| AR036608A1 (es) | 2001-09-24 | 2004-09-22 | Bayer Corp | Derivados de imidazol, composiciones farmaceuticas y el uso de dichos derivados para la fabricacion de un medicamento para el tratamiento de la obesidad |
| EP1430032A2 (en) * | 2001-09-24 | 2004-06-23 | Elan Pharmaceuticals, Inc. | Substituted amides for the treatment of neurological disorders |
| CA2478183C (en) | 2002-03-12 | 2010-02-16 | Merck & Co. Inc. | Substituted amides |
| AU2003275242B2 (en) | 2002-09-27 | 2010-03-04 | Merck Sharp & Dohme Corp. | Substituted pyrimidines |
| 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 |
| PL378206A1 (pl) * | 2003-01-02 | 2006-03-20 | F. Hoffmann-La Roche Ag | Nowi odwrotni agoniści receptora CB1 |
| EP1586068B1 (en) * | 2003-01-23 | 2008-07-30 | U.S. Genomics, Inc. | Methods for analyzing polymer populations |
| US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
| ATE478859T1 (de) | 2003-02-07 | 2010-09-15 | Daiichi Sankyo Co Ltd | Pyrazolderivat |
| US7176210B2 (en) | 2003-02-10 | 2007-02-13 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
| PL378841A1 (pl) * | 2003-04-21 | 2006-05-29 | Daiichi Pharmaceutical Co., Ltd. | Pochodna pięcioczłonowego układu heterocyklicznego |
| US7141669B2 (en) | 2003-04-23 | 2006-11-28 | Pfizer Inc. | Cannabiniod 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 |
| US20040224963A1 (en) * | 2003-05-09 | 2004-11-11 | Pfizer Inc | Pharmaceutical composition for the prevention and treatment of nicotine addiction in a mammal |
| US20040224962A1 (en) * | 2003-05-09 | 2004-11-11 | Pfizer Inc | Pharmaceutical composition for the treatment of obesity or to facilitate or promote weight loss |
| SE0301446D0 (sv) | 2003-05-16 | 2003-05-16 | Astrazeneca Ab | New Compounds |
| US7232823B2 (en) | 2003-06-09 | 2007-06-19 | Pfizer, Inc. | Cannabinoid receptor ligands and uses thereof |
| SE0301701D0 (sv) | 2003-06-10 | 2003-06-10 | Astrazeneca Ab | Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof |
| SE0301699D0 (sv) | 2003-06-10 | 2003-06-10 | Astrazeneca Ab | Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof |
| SE0301698D0 (sv) * | 2003-06-10 | 2003-06-10 | Astrazeneca Ab | Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof |
| US20040259887A1 (en) * | 2003-06-18 | 2004-12-23 | Pfizer Inc | Cannabinoid receptor ligands and uses thereof |
| EP1644370A4 (en) | 2003-07-11 | 2008-06-04 | Bristol Myers Squibb Co | TETRAHYDROCHINOLINE DERIVATIVES AS CANNABINOID RECEPTOR MODULATORS |
| US20050026983A1 (en) * | 2003-07-30 | 2005-02-03 | Pfizer Inc | Imidazole compounds and uses thereof |
| US7326706B2 (en) | 2003-08-15 | 2008-02-05 | Bristol-Myers Squibb Company | Pyrazine modulators of cannabinoid receptors |
| US20050239859A2 (en) * | 2003-09-03 | 2005-10-27 | Solvay Pharmaceuticals Gmbh | Novel medical uses of 4,5-dihydro-1h-pyrazole derivatives having cb1- antagonistic activity |
| AR046182A1 (es) * | 2003-10-20 | 2005-11-30 | Solvay Pharm Bv | Derivados de 1h- imidazol como moduladores del receptor canabinoide. composiciones farmaceuticas que los contienen. |
| KR20060117952A (ko) * | 2003-10-20 | 2006-11-17 | 솔베이 파마슈티칼스 비. 브이 | 카나비노이드 수용체 조절제로서 1ｈ-이미다졸 유도체 |
| MXPA06004434A (es) * | 2003-10-24 | 2006-06-20 | Solvay Pharm Gmbh | Usos medicos novedosos de compuestos que muestran actividad antagonista cb1 y tratamiento de combinacion que involucra tales compuestos. |
| US20050143441A1 (en) * | 2003-10-27 | 2005-06-30 | Jochen Antel | Novel medical combination treatment of obesity involving 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity |
| US20050124660A1 (en) * | 2003-10-27 | 2005-06-09 | Jochen Antel | Novel medical uses of compounds showing CB1-antagonistic activity and combination treatment involving said compounds |
| RU2367659C2 (ru) | 2003-11-05 | 2009-09-20 | Ф.Хоффманн-Ля Рош Аг | Гетероарильные производные в качестве активаторов рецепторов, активируемых пролифераторами пероксисом (ppar) |
| TW200522944A (en) * | 2003-12-23 | 2005-07-16 | Lilly Co Eli | CB1 modulator compounds |
| FR2866340B1 (fr) | 2004-02-13 | 2006-11-24 | Sanofi Synthelabo | Derives d'oxazole, leur preparation et leur utilisation en therapeutique. |
| TWI335321B (en) * | 2004-02-19 | 2011-01-01 | Solvay Pharm Bv | Imidazoline derivatives having cb1-antagonistic activity |
| US7173044B2 (en) * | 2004-02-19 | 2007-02-06 | Solvay Pharmaceuticals B.V. | Imidazoline derivatives having CB1-antagonistic activity |
| PT1725536E (pt) * | 2004-02-19 | 2009-01-22 | Solvay Pharm Bv | Derivados de imidazolina apresentando actividade antagonista cb1 |
| GB0404105D0 (en) * | 2004-02-24 | 2004-03-31 | Glaxo Group Ltd | Novel compounds |
| JP2007527917A (ja) * | 2004-03-08 | 2007-10-04 | ワイス | イオンチャンネルモジュレーター |
| WO2005097127A2 (en) | 2004-04-02 | 2005-10-20 | Merck & Co., Inc. | Method of treating men with metabolic and anthropometric disorders |
| BRPI0509515A (pt) * | 2004-04-03 | 2007-09-11 | Astrazeneca Ab | composto, formulação farmacêutica, uso de um composto método para tratamento de doenças, e, processo para a preparação de um composto |
| EP1749002B1 (en) | 2004-05-10 | 2009-05-27 | F.Hoffmann-La Roche Ag | Pyrrole or imidazole amides for treating obesity |
| DK1756066T3 (da) * | 2004-05-28 | 2008-12-15 | Solvay Pharm Bv | Tetrasubstituerede imidazolderivater som canabinoid-CB1-receptormodulatorer med höj CB1/CB2-receptorundertypeselektivitet |
| US7524867B2 (en) | 2004-05-28 | 2009-04-28 | Solvay Pharmaceuticals, B.V. | Tetrasubstituted imidazole derivatives as cannabinoid CB1 receptor modulators with a high CB1/CB2 receptor subtype selectivity |
| TW200608968A (en) * | 2004-05-28 | 2006-03-16 | Solvay Pharm Bv | Tetrasubstituted imidazole derivatives as cannabinoid cb1 receptor modulators with a high cb1/cb2 receptor subtype selectivity |
| TW200602314A (en) | 2004-05-28 | 2006-01-16 | Tanabe Seiyaku Co | A novel pyrrolidine compound and a process for preparing the same |
| US8030345B2 (en) | 2004-07-12 | 2011-10-04 | Cadila Healthcare Limited | Tricyclic pyrazole derivatives as cannabinoid receptor modulators |
| US20060025448A1 (en) | 2004-07-22 | 2006-02-02 | Cadila Healthcare Limited | Hair growth stimulators |
| FR2874012B1 (fr) * | 2004-08-09 | 2008-08-22 | Sanofi Synthelabo | Derives de pyrrole, leur preparation et leur utlisation en therapeutique |
| RU2007119315A (ru) | 2004-10-25 | 2008-11-27 | Зольвай Фармасьютиклз Гмбх (De) | Фармацевтические композиции, содержащие антагонисты каннабиноидного рецептора св1 и открыватели калиевых каналов, предназначенные для лечения сахарного диабета типа i, ожирения и связанных с ними состояний |
| WO2006060202A2 (en) * | 2004-11-30 | 2006-06-08 | Bayer Pharmaceuticals Corporation | Imidazole derivatives for the treatment of psychiatric disorders |
| WO2006060190A2 (en) * | 2004-11-30 | 2006-06-08 | Bayer Pharmaceuticals Corporation | Imidazole derivatives |
| WO2006060203A2 (en) * | 2004-11-30 | 2006-06-08 | Bayer Pharmaceuticals Corporation | Imidazole derivatives for the treatment of dementia and related disorders |
| AU2005311930B9 (en) | 2004-12-03 | 2009-09-10 | Merck Sharp & Dohme Corp. | Substituted piperazines as CB1 antagonists |
| JP2008525401A (ja) * | 2004-12-23 | 2008-07-17 | アストラゼネカ アクチボラグ | 治療薬 |
| US8084451B2 (en) * | 2005-01-10 | 2011-12-27 | University Of Connecticut | Heteropyrrole analogs acting on cannabinoid receptors |
| CA2593156C (en) * | 2005-01-10 | 2015-05-05 | Exelixis, Inc. | Heterocyclic carboxamide compounds as steroid nuclear receptors ligands |
| US8937184B2 (en) | 2005-02-16 | 2015-01-20 | Abbvie B.V. | 1H-imidazole derivatives as cannabinoid CB2 receptor modulators |
| US7923465B2 (en) | 2005-06-02 | 2011-04-12 | Glenmark Pharmaceuticals S.A. | Cannabinoid receptor ligands, pharmaceutical compositions containing them, and process for their preparation |
| JP2008545739A (ja) | 2005-06-02 | 2008-12-18 | グレンマーク・ファーマシューティカルズ・エスエー | 新規なカンナビノイド受容体リガンド、それらを含む薬剤組成物、およびそれらの調製方法 |
| AU2006264649A1 (en) | 2005-06-30 | 2007-01-11 | Prosidion Limited | GPCR agonists |
| WO2007024744A2 (en) * | 2005-08-21 | 2007-03-01 | Exelixis, Inc. | Heterocyclic carboxamide compounds as steroid nuclear receptor ligands |
| GB0518819D0 (en) * | 2005-09-15 | 2005-10-26 | Astrazeneca Ab | Therapeutic agents |
| GB0518817D0 (en) * | 2005-09-15 | 2005-10-26 | Astrazeneca Ab | Therapeutic agents |
| KR100694181B1 (ko) * | 2005-11-25 | 2007-03-12 | 연세대학교 산학협력단 | 근원세포 또는 근섬유로부터 신경세포 분화를 유도하는화합물, 이를 포함하는 약학적 조성물, 신경세포 분화를유도하는 방법 및 신경세포 분화를 유도하는 화합물을검색하는 스크리닝 방법 |
| AR058705A1 (es) | 2005-12-23 | 2008-02-20 | Astrazeneca Ab | Compuestos de bencimidazol como inhibidores del receptor vaniloide 1 (vr1) |
| PE20071320A1 (es) * | 2006-01-18 | 2007-12-29 | Schering Corp | Moduladores de receptores cannabinoides |
| TWI433839B (zh) | 2006-08-11 | 2014-04-11 | Neomed Inst | 新穎的苯并咪唑衍生物290 |
| AR064736A1 (es) | 2007-01-04 | 2009-04-22 | Prosidion Ltd | Agonistas de gpcr |
| EP2114936A1 (en) | 2007-01-04 | 2009-11-11 | 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 |
| JP2010514828A (ja) | 2007-01-04 | 2010-05-06 | プロシディオン・リミテッド | ピペリジンｇｐｃｒアゴニスト |
| GB0700122D0 (en) | 2007-01-04 | 2007-02-14 | Prosidion Ltd | GPCR agonists |
| WO2008130616A2 (en) * | 2007-04-19 | 2008-10-30 | Schering Corporation | Diaryl morpholines as cb1 modulators |
| CA2688161C (en) | 2007-06-04 | 2020-10-20 | Kunwar Shailubhai | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
| US8969514B2 (en) | 2007-06-04 | 2015-03-03 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases |
| NZ582249A (en) * | 2007-06-28 | 2012-06-29 | Intervet Int Bv | Substituted piperazines as cb1 antagonists |
| EP2170847A2 (en) * | 2007-06-28 | 2010-04-07 | Intervet International BV | Substituted piperazines as cb1 antagonists |
| GB0720389D0 (en) | 2007-10-18 | 2008-11-12 | Prosidion Ltd | G-Protein Coupled Receptor Agonists |
| GB0720390D0 (en) | 2007-10-18 | 2007-11-28 | Prosidion Ltd | G-Protein coupled receptor agonists |
| ES2716407T3 (es) | 2007-11-30 | 2019-06-12 | Zynerba Pharmaceuticals Inc | Profármacos de tetrahidrocannabinol, composiciones que comprenden profármacos de tetrahidrocannabinol y métodos para uso de los mismos |
| ES2522968T3 (es) | 2008-06-04 | 2014-11-19 | Synergy Pharmaceuticals Inc. | Agonistas de guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos |
| US9029408B2 (en) | 2008-06-16 | 2015-05-12 | Gtx, Inc. | Compounds for treatment of cancer |
| PT2959900T (pt) * | 2008-06-16 | 2017-06-22 | Univ Tennessee Res Found | Composto para tratamento do cancro |
| US9447049B2 (en) | 2010-03-01 | 2016-09-20 | University Of Tennessee Research Foundation | Compounds for treatment of cancer |
| US8822513B2 (en) | 2010-03-01 | 2014-09-02 | Gtx, Inc. | Compounds for treatment of cancer |
| ES2624828T3 (es) | 2008-07-16 | 2017-07-17 | Synergy Pharmaceuticals Inc. | Agonistas de la guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros |
| WO2010047982A1 (en) | 2008-10-22 | 2010-04-29 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| CA2741672A1 (en) | 2008-10-31 | 2010-05-06 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| WO2010079241A1 (es) | 2009-01-12 | 2010-07-15 | Fundacion Hospital Nacional De Paraplejicos Para La Investigacion Y La Integracion | Uso de antagonistas y/o agonistas inversos de los receptores cb1 para la preparación de medicamentos que incrementen la excitabilidad de las motoneuronas |
| WO2011106273A1 (en) | 2010-02-25 | 2011-09-01 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| MX2012010115A (es) | 2010-03-01 | 2013-02-26 | Gtx Inc | Compuestos para el tratamiento de cancer. |
| US9616097B2 (en) | 2010-09-15 | 2017-04-11 | Synergy Pharmaceuticals, Inc. | Formulations of guanylate cyclase C agonists and methods of use |
| EA025380B1 (ru) | 2011-02-25 | 2016-12-30 | Мерк Шарп Энд Домэ Корп. | Новые циклические производные азабензимидазола, используемые в качестве антидиабетических агентов |
| KR20150036245A (ko) | 2012-08-02 | 2015-04-07 | 머크 샤프 앤드 돔 코포레이션 | 항당뇨병 트리시클릭 화합물 |
| RU2015140066A (ru) | 2013-02-22 | 2017-03-30 | Мерк Шарп И Доум Корп. | Противодиабетические бициклические соединения |
| WO2014139388A1 (en) | 2013-03-14 | 2014-09-18 | Merck Sharp & Dohme Corp. | Novel indole derivatives useful as anti-diabetic agents |
| US9486494B2 (en) | 2013-03-15 | 2016-11-08 | Synergy Pharmaceuticals, Inc. | Compositions useful for the treatment of gastrointestinal disorders |
| EP2970384A1 (en) | 2013-03-15 | 2016-01-20 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase and their uses |
| JP6606491B2 (ja) | 2013-06-05 | 2019-11-13 | シナジー ファーマシューティカルズ インコーポレイテッド | グアニル酸シクラーゼｃの超高純度アゴニスト、その作成および使用方法 |
| WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| AU2015269247B2 (en) | 2014-06-06 | 2019-10-24 | Research Triangle Institute | Apelin receptor (APJ) agonists and uses thereof |
| US10100059B2 (en) | 2015-12-09 | 2018-10-16 | Research Triangle Institute | Apelin receptor (APJ) agonists and uses thereof |
| AU2017343638B2 (en) | 2016-10-12 | 2021-12-09 | Research Triangle Institute | Heterocyclic apelin receptor (APJ) agonists and uses thereof |
| US11072602B2 (en) | 2016-12-06 | 2021-07-27 | Merck Sharp & Dohme Corp. | Antidiabetic heterocyclic compounds |
| WO2019042267A1 (zh) * | 2017-08-28 | 2019-03-07 | 中国医学科学院药物研究所 | 吡咯-2-甲酰胺类化合物及其制备方法和用途 |
| CN113166068A (zh) * | 2018-11-20 | 2021-07-23 | 上海科技大学 | MmpL3抑制剂、组合物及其用途 |
| CN112558265B (zh) * | 2019-09-26 | 2022-04-19 | 张家港梓阳电子科技有限公司 | 一种用于气体准分子激光器镜头的锁定装置 |
| CA3125847A1 (en) | 2020-07-27 | 2022-01-27 | Makscientific, Llc | Process for making biologically active compounds and intermediates thereof |
| WO2024009283A1 (en) * | 2022-07-07 | 2024-01-11 | University Of Southern California | At2 antagonists for non-addictive pain relief |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DD140966A1 (de) * | 1978-12-28 | 1980-04-09 | Doerthe Creuzburg | Mittel zur regulierung des pflanzenwachstums |
| US4813998A (en) * | 1986-02-27 | 1989-03-21 | Janssen Pharmaceutica N.V. | Herbicidal 1H-imidazole-5-carboxylic acid derivatives |
| FR2692575B1 (fr) | 1992-06-23 | 1995-06-30 | Sanofi Elf | Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| US5616601A (en) * | 1994-07-28 | 1997-04-01 | Gd Searle & Co | 1,2-aryl and heteroaryl substituted imidazolyl compounds for the treatment of inflammation |
| FR2789079B3 (fr) * | 1999-02-01 | 2001-03-02 | Sanofi Synthelabo | Derive d'acide pyrazolecarboxylique, sa preparation, les compositions pharmaceutiques en contenant |
| CO5170501A1 (es) * | 1999-04-14 | 2002-06-27 | Novartis Ag | AZOLES SUSTITUIDOS UTILES PARA EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR TNFa eIL-1 Y ENFERMEDADES DEL METABOLISMO OSEO |
| US6492516B1 (en) | 1999-05-14 | 2002-12-10 | Merck & Co., Inc. | Compounds having cytokine inhibitory activity |
| 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 |
| RU2281941C2 (ru) | 2001-03-22 | 2006-08-20 | Солвей Фармасьютикалс Б.В. | Производные 4,5-дигидро-1h-пиразола, обладающие cb1-антагонистической активностью |
| US7109216B2 (en) * | 2001-09-21 | 2006-09-19 | Solvay Pharmaceuticals B.V. | 1H-imidazole derivatives having CB1 agonistic, CB1 partial agonistic or CB1-antagonistic activity |
| AR036608A1 (es) * | 2001-09-24 | 2004-09-22 | Bayer Corp | Derivados de imidazol, composiciones farmaceuticas y el uso de dichos derivados para la fabricacion de un medicamento para el tratamiento de la obesidad |
| WO2003063781A2 (en) | 2002-01-29 | 2003-08-07 | Merck & Co., Inc. | Substituted imidazoles as cannabinoid receptor modulators |
| US7524867B2 (en) * | 2004-05-28 | 2009-04-28 | Solvay Pharmaceuticals, B.V. | Tetrasubstituted imidazole derivatives as cannabinoid CB1 receptor modulators with a high CB1/CB2 receptor subtype selectivity |
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