IL124641A - תולדות -1(פיפרידיניל-2,1 - מותמר)--4 (אימידאזול דחוס)- פיפרידין, תכשירי רוקחות המכילים אותן והכנתן - Google Patents
תולדות -1(פיפרידיניל-2,1 - מותמר)--4 (אימידאזול דחוס)- פיפרידין, תכשירי רוקחות המכילים אותן והכנתןInfo
- Publication number
- IL124641A IL124641A IL12464196A IL12464196A IL124641A IL 124641 A IL124641 A IL 124641A IL 12464196 A IL12464196 A IL 12464196A IL 12464196 A IL12464196 A IL 12464196A IL 124641 A IL124641 A IL 124641A
- Authority
- IL
- Israel
- Prior art keywords
- formula
- alkyl
- halo
- radical
- hydrogen
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims description 8
- 238000002360 preparation method Methods 0.000 title description 13
- 150000002460 imidazoles Chemical class 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 100
- -1 halo C1-4 alkyl Chemical group 0.000 claims abstract description 44
- 239000001257 hydrogen Substances 0.000 claims abstract description 41
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 41
- 150000003839 salts Chemical class 0.000 claims abstract description 32
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract description 24
- 125000001424 substituent group Chemical group 0.000 claims abstract description 21
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract description 20
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims abstract description 15
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract description 14
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims abstract description 12
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims abstract description 11
- 125000002883 imidazolyl group Chemical group 0.000 claims abstract description 10
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims abstract description 8
- 229910052799 carbon Inorganic materials 0.000 claims abstract description 7
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract description 7
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims abstract description 6
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims abstract description 6
- 125000002541 furyl group Chemical group 0.000 claims abstract description 6
- 125000000842 isoxazolyl group Chemical group 0.000 claims abstract description 6
- 125000002950 monocyclic group Chemical group 0.000 claims abstract description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract description 6
- 125000003373 pyrazinyl group Chemical group 0.000 claims abstract description 6
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims abstract description 6
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims abstract description 6
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims abstract description 5
- 125000004604 benzisothiazolyl group Chemical group S1N=C(C2=C1C=CC=C2)* 0.000 claims abstract description 5
- 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 claims abstract description 5
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims abstract description 5
- 125000001786 isothiazolyl group Chemical group 0.000 claims abstract description 5
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- 125000002098 pyridazinyl group Chemical group 0.000 claims abstract description 5
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- 125000000168 pyrrolyl group Chemical group 0.000 claims abstract description 5
- 125000000335 thiazolyl group Chemical group 0.000 claims abstract description 5
- 125000001544 thienyl group Chemical group 0.000 claims abstract description 5
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- 125000001475 halogen functional group Chemical group 0.000 claims abstract 15
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 3
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- 238000000034 method Methods 0.000 claims description 18
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- 239000003814 drug Substances 0.000 claims description 8
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- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 6
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- 239000000543 intermediate Substances 0.000 description 60
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
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- Epidemiology (AREA)
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- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP95203652 | 1995-12-27 | ||
| PCT/EP1996/005885 WO1997024356A1 (en) | 1995-12-27 | 1996-12-20 | 1-(1,2-disubstituted piperidinyl)-4-(fused imidazole)-piperidine derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL124641A0 IL124641A0 (en) | 1998-12-06 |
| IL124641A true IL124641A (he) | 2001-11-25 |
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| Application Number | Title | Priority Date | Filing Date |
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| IL12464296A IL124642A (he) | 1995-12-27 | 1996-12-20 | H - אציל 2, 4 - פיפרידינים או הקסאמתילנאימינים מותמרים, תהליך להכנתם ותכשירי רוקחות המכילים אותם |
| IL12464196A IL124641A (he) | 1995-12-27 | 1996-12-20 | תולדות -1(פיפרידיניל-2,1 - מותמר)--4 (אימידאזול דחוס)- פיפרידין, תכשירי רוקחות המכילים אותן והכנתן |
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| IL12464296A IL124642A (he) | 1995-12-27 | 1996-12-20 | H - אציל 2, 4 - פיפרידינים או הקסאמתילנאימינים מותמרים, תהליך להכנתם ותכשירי רוקחות המכילים אותם |
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|---|---|
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| EP (1) | EP0843679B1 (he) |
| JP (1) | JP4097043B2 (he) |
| KR (1) | KR100485147B1 (he) |
| CN (1) | CN1066733C (he) |
| AR (2) | AR005278A1 (he) |
| AT (1) | ATE208392T1 (he) |
| AU (1) | AU716071B2 (he) |
| BR (1) | BR9612307A (he) |
| CA (1) | CA2238817C (he) |
| CY (1) | CY2271B1 (he) |
| CZ (1) | CZ295861B6 (he) |
| DE (1) | DE69616802T2 (he) |
| DK (1) | DK0843679T3 (he) |
| EA (1) | EA001374B1 (he) |
| ES (1) | ES2167619T3 (he) |
| HU (1) | HU229766B1 (he) |
| IL (2) | IL124642A (he) |
| MY (1) | MY117680A (he) |
| NO (1) | NO310916B1 (he) |
| NZ (1) | NZ325845A (he) |
| PL (1) | PL183767B1 (he) |
| PT (1) | PT843679E (he) |
| SI (1) | SI0843679T1 (he) |
| SK (1) | SK283540B6 (he) |
| TR (1) | TR199801210T2 (he) |
| TW (1) | TW382017B (he) |
| WO (1) | WO1997024356A1 (he) |
| ZA (1) | ZA9610889B (he) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
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| TW527186B (en) * | 1996-03-19 | 2003-04-11 | Janssen Pharmaceutica Nv | Fused imidazole derivatives as multidrug resistance modulators |
| AU1146099A (en) * | 1997-09-18 | 1999-04-05 | Janssen Pharmaceutica N.V. | Fused imidazole derivatives for improving oral bioavailability of pharmaceuticalagents |
| BR9916371A (pt) * | 1998-12-19 | 2001-09-18 | Janssen Pharmaceutica Nv | Composto de espiro anti-histamìnico |
| AU7788500A (en) * | 1999-10-25 | 2001-05-08 | Janssen Pharmaceutica N.V. | Use of substance p antagonists for influencing the circadian timing system |
| WO2002100862A2 (en) | 2001-06-12 | 2002-12-19 | Janssen Pharmaceutica N.V. | Novel substituted tetracyclic imidazole derivatives, processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine |
| US20030083345A1 (en) * | 2001-07-10 | 2003-05-01 | Torsten Hoffmann | Method of treatment and/or prevention of brain, spinal or nerve injury |
| WO2003044023A1 (en) * | 2001-11-23 | 2003-05-30 | Janssen Pharmaceutica N.V. | The use of anti-histaminics for acute reduction of elevated intracranial pressure |
| EP1457493A4 (en) | 2001-12-10 | 2005-11-30 | Kyorin Seiyaku Kk | CONDENSED, BICYCLIC PYRIDINE DERIVATIVES AS TACHYKININ RECEPTOR ANTAGONISTS |
| ES2242940T3 (es) * | 2002-01-16 | 2005-11-16 | Janssen Pharmaceutica N.V. | Prucaloprida n-oxido. |
| KR100887471B1 (ko) * | 2002-01-18 | 2009-03-10 | 교린 세이야꾸 가부시키 가이샤 | 축합 바이사이클릭 피리미딘 유도체 |
| US7026309B2 (en) | 2002-03-26 | 2006-04-11 | Kyorin Pharmaceutical Co., Ltd. | Fused bicyclic pyridine derivative as tachykinin receptor antagonist |
| JP4677235B2 (ja) * | 2002-12-23 | 2011-04-27 | 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 | 置換４−（４−ピペリジン−４−イル−ピペラジン−１−イル）−アゼパン誘導体およびそれらのニューロキニン拮抗薬としての使用 |
| JO2696B1 (en) | 2002-12-23 | 2013-03-03 | شركة جانسين فارماسوتيكا ان. في | Derivatives of 1-piperdine-4-yl-4-biprolidine-3-yl-piperazine substituted and used as quinine antagonists |
| JO2676B1 (en) | 2004-04-06 | 2012-06-17 | جانسين فارماسوتيكا ان. في | Derivatives of second-aza-spiro- (5,4) -dikan and their use as antihistamines |
| JO2525B1 (en) * | 2004-04-08 | 2010-03-17 | شركة جانسين فارماسوتيكا ان. في | Derived 4-alkyl-and-4-canoelperidine derivatives and their use as anti-neroquin |
| ES2346147T3 (es) | 2005-03-03 | 2010-10-11 | Janssen Pharmaceutica Nv | Derivados de oxa-diaza-espiro-(5.5)-undecanona sustituidos y su uso como antagonistas de las neuroquininas. |
| NZ556628A (en) | 2005-03-08 | 2009-09-25 | Janssen Pharmaceutica Nv | Diaza-spiro-[4.4]-nonane derivatives as neurokinin (NK1) antagonists |
| KR20100055430A (ko) * | 2007-07-19 | 2010-05-26 | 애들레이드 리서치 앤드 이노베이션 피티와이 리미티드 | 두개내압 감소 방법 |
| UA105182C2 (ru) | 2008-07-03 | 2014-04-25 | Ньюрексон, Інк. | Бензоксазины, бензотиазины и родственные соединения, которые имеют ингибирующую nos активность |
| WO2013004766A1 (en) | 2011-07-04 | 2013-01-10 | Ferrari Giulio | Nk-1 receptor antagonists for treating corneal neovascularisation |
| RU2020131446A (ru) | 2018-02-26 | 2022-03-28 | Оспедале Сан Раффаэле С.Р.Л. | Антагонисты nk-1 для применения в лечении глазной боли |
| EP4117673A1 (en) | 2020-03-11 | 2023-01-18 | Ospedale San Raffaele S.r.l. | Treatment of stem cell deficiency |
Family Cites Families (7)
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|---|---|---|---|---|
| US4329353A (en) | 1980-10-22 | 1982-05-11 | Janssen Pharmaceutica, N.V. | 1-(4-Aryl-cyclohexyl)piperidine derivatives, method of use thereof and pharmaceutical compositions thereof |
| EP0552292B1 (en) * | 1990-10-10 | 1995-06-21 | Schering Corporation | Substituted imidazobenzazepines and imidazopyridoazepines |
| IL101851A (en) * | 1991-06-13 | 1996-05-14 | Janssen Pharmaceutica Nv | 10-(4-piperidinyl- and piperidinylidene)-imidazo [1,2-a] (pyrrolo thieno or furano) [2,3] azepine derivatives their preparation and pharmaceutical compositions containing them and certain novel intermediates therefor |
| IL101850A (en) * | 1991-06-13 | 1996-01-31 | Janssen Pharmaceutica Nv | 11-(4-Piperidinyl)-imidazo (2,1-b) (3) benzazepine derivatives their preparation and pharmaceutical compositions containing them |
| EP0708776B1 (en) * | 1993-07-13 | 2001-01-03 | Janssen Pharmaceutica N.V. | Antiallergic imidazoazepines |
| RU2156763C2 (ru) | 1994-07-15 | 2000-09-27 | Мейдзи Сейка Кабусики Кайся | Азотсодержащие гетероциклические производные, фармацевтическая композиция на их основе и способ лечения или профилактики тромботических заболеваний |
| NZ321575A (en) | 1995-10-30 | 1999-05-28 | Janssen Pharmaceutica Nv | 1-(1,2-disubstituted piperidinyl)-4- substituted piperazine derivatives |
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1996
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- 1996-12-20 SK SK830-98A patent/SK283540B6/sk unknown
- 1996-12-20 AT AT96944693T patent/ATE208392T1/de active
- 1996-12-20 ES ES96944693T patent/ES2167619T3/es not_active Expired - Lifetime
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- 1996-12-20 IL IL12464196A patent/IL124641A/he not_active IP Right Cessation
- 1996-12-20 KR KR10-1998-0704830A patent/KR100485147B1/ko not_active Expired - Fee Related
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- 1996-12-20 TR TR1998/01210T patent/TR199801210T2/xx unknown
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- 1996-12-20 JP JP52403397A patent/JP4097043B2/ja not_active Expired - Fee Related
- 1996-12-20 HU HU9903948 patent/HU229766B1/hu not_active IP Right Cessation
- 1996-12-20 NZ NZ325845A patent/NZ325845A/xx not_active IP Right Cessation
- 1996-12-20 WO PCT/EP1996/005885 patent/WO1997024356A1/en not_active Ceased
- 1996-12-20 SI SI9630419T patent/SI0843679T1/xx unknown
- 1996-12-20 PT PT96944693T patent/PT843679E/pt unknown
- 1996-12-20 CA CA002238817A patent/CA2238817C/en not_active Expired - Fee Related
- 1996-12-20 DK DK96944693T patent/DK0843679T3/da active
- 1996-12-20 BR BR9612307A patent/BR9612307A/pt not_active IP Right Cessation
- 1996-12-20 EP EP96944693A patent/EP0843679B1/en not_active Expired - Lifetime
- 1996-12-23 ZA ZA9610889A patent/ZA9610889B/xx unknown
- 1996-12-26 AR ARP960105895A patent/AR005278A1/es active IP Right Grant
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1998
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2002
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2005
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