HRP20170621T1 - Postupak za pripremanje derivata piperazinil i diazepanil benzamida - Google Patents
Postupak za pripremanje derivata piperazinil i diazepanil benzamida Download PDFInfo
- Publication number
- HRP20170621T1 HRP20170621T1 HRP20170621TT HRP20170621T HRP20170621T1 HR P20170621 T1 HRP20170621 T1 HR P20170621T1 HR P20170621T T HRP20170621T T HR P20170621TT HR P20170621 T HRP20170621 T HR P20170621T HR P20170621 T1 HRP20170621 T1 HR P20170621T1
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- HR
- Croatia
- Prior art keywords
- formula
- compound
- xia
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- organic
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims 5
- MCBOTNKJOSKNFJ-UHFFFAOYSA-N n-(diazepan-1-yl)benzamide Chemical class C=1C=CC=CC=1C(=O)NN1CCCCCN1 MCBOTNKJOSKNFJ-UHFFFAOYSA-N 0.000 title 1
- 125000004193 piperazinyl group Chemical group 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 24
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 6
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims 6
- 238000006243 chemical reaction Methods 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000002904 solvent Substances 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 239000003960 organic solvent Substances 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- 230000003213 activating effect Effects 0.000 claims 1
- 239000007822 coupling agent Substances 0.000 claims 1
- 150000007529 inorganic bases Chemical group 0.000 claims 1
- 150000007530 organic bases Chemical group 0.000 claims 1
- 238000005897 peptide coupling reaction Methods 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—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
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- 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
- C07D401/10—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 linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Claims (4)
1. Postupak za pripremanje spoja s formulom (Ia)
[image]
ili njegove farmaceutski prihvatljive soli, tautomera ili solvata; naznačen time da sadrži
[image]
reakciju spoja s formulom (Xa) sa spojem s formulom (XIa) ; u prisutnosti peptidnog sredstva za spajanje; u organskom otapalu ili smjesi organskih otapala; da se dobije odgovarajući spoj s formulom (Ia).
2. Postupak za pripremanje spoja s formulom (Ia)
[image]
ili njegove farmaceutski prihvatljive soli, tautomera ili solvata; naznačen time da sadrži
[image]
aktiviranje spoja s formulom (Xa), da se dobije odgovarajući spoj s formulom (XIIa), pri čemu L je izlazna skupina;
[image]
reakciju spoja s formulom (XIIa) sa spojem s formulom (XIa); u prisutnosti tercijarne organske ili anorganske baze; u otapalu ili smjesi otapala; da se dobije odgovarajući spoj s formulom (Ia).
3. Postupak prema zahtjevu 1 ili 2, naznačen time da se spoj s formulom (XIa) priprema
[image]
reakcijom prikladno supstituiranog spoja s formulom (XX), pri čemu X je vodik ili prikladno odabrana dušikova zaštitna skupina i pri čemu je Z odabran od prikladnih izlaznih skupina i pri čemu su oba Z supstituenta isti, sa spojem s formulom (XXIa), u organskom otapalu kao što je THF, toluen, DMF, 2-metil-THF i acetonitril; da se dobije odgovarajući spoj s formulom (XIa), ili, kada X je vodik, reakcijom spoja s formulom (XX) sa spojem s formulom (XXIa) kao njegovom odgovarajućom kiselom adicijskom soli u vodi; da se dobije odgovarajući spoj s formulom (XIa).
4. Postupak za pripremanje spoja s formulom (XIa) naznačen time da sadrži
[image]
reakciju prikladno supstituiranog spoja s formulom (XX), pri čemu X je vodik ili prikladno odabrana dušikova zaštitna skupina i pri čemu je Z odabran od prikladnih izlaznih skupina i pri čemu su oba Z supstituenta isti, sa spojem s formulom (XXIa), u organskom otapalu kao što je THF, toluen, DMF, 2-metil-THF i acetonitril; da se dobije odgovarajući spoj s formulom (XIa), ili kada X je vodik, da sadrži reakciju spoja s formulom (XX) sa spojem s formulom (XXIa) kao njegovom odgovarajućom kiselom adicijskom soli u vodi; da se dobije odgovarajući spoj s formulom (XIa).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87000306P | 2006-12-14 | 2006-12-14 | |
| EP07855037.3A EP2121636B1 (en) | 2006-12-14 | 2007-12-10 | Process for the preparation of piperazinyl and diazepanyl benzamide derivatives |
| PCT/US2007/086936 WO2008076685A2 (en) | 2006-12-14 | 2007-12-10 | Process for the preparation of piperazinyl and diazepanyl benzamide derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20170621T1 true HRP20170621T1 (hr) | 2017-07-28 |
Family
ID=39387172
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20170621TT HRP20170621T1 (hr) | 2006-12-14 | 2017-04-19 | Postupak za pripremanje derivata piperazinil i diazepanil benzamida |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US7893257B2 (hr) |
| EP (1) | EP2121636B1 (hr) |
| JP (2) | JP5385150B2 (hr) |
| KR (1) | KR101462891B1 (hr) |
| CN (1) | CN101605767A (hr) |
| AR (1) | AR064358A1 (hr) |
| BR (1) | BRPI0721088B8 (hr) |
| CA (2) | CA2672661C (hr) |
| CL (1) | CL2007003637A1 (hr) |
| CO (1) | CO6210827A2 (hr) |
| CR (1) | CR10928A (hr) |
| CY (1) | CY1118814T1 (hr) |
| DK (1) | DK2121636T3 (hr) |
| EA (1) | EA200970583A1 (hr) |
| EC (1) | ECSP099405A (hr) |
| ES (1) | ES2620818T3 (hr) |
| HR (1) | HRP20170621T1 (hr) |
| HU (1) | HUE032761T2 (hr) |
| IL (2) | IL199309A0 (hr) |
| LT (1) | LT2121636T (hr) |
| MX (1) | MX2009006472A (hr) |
| MY (1) | MY147320A (hr) |
| NO (1) | NO344305B1 (hr) |
| NZ (1) | NZ577603A (hr) |
| PH (1) | PH12012502236A1 (hr) |
| PL (1) | PL2121636T3 (hr) |
| PT (1) | PT2121636T (hr) |
| RS (1) | RS55866B1 (hr) |
| SG (1) | SG177207A1 (hr) |
| SI (1) | SI2121636T1 (hr) |
| TW (1) | TW200846004A (hr) |
| WO (1) | WO2008076685A2 (hr) |
| ZA (1) | ZA200904894B (hr) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0324159D0 (en) | 2003-10-15 | 2003-11-19 | Glaxo Group Ltd | Novel compounds |
| DK1976828T3 (en) | 2005-12-29 | 2017-03-06 | Celtaxsys Inc | DIAMINE DERIVATIVES AS INhibitors of Leukotriene A4 HYDROLASE |
| KR101462891B1 (ko) * | 2006-12-14 | 2014-11-19 | 얀센 파마슈티카 엔.브이. | 피페라지닐 및 디아제파닐 벤즈아미드 유도체의 제조 방법 |
| ES2384414T3 (es) | 2007-09-06 | 2012-07-04 | Glaxo Group Limited | Derivado de piperazina que tiene afinidad por el receptor H3 de histamina |
| ES2602331T3 (es) | 2007-12-10 | 2017-02-20 | Novartis Ag | Pirazin-carboxamidas de tipo amilorida como bloqueantes de ENaC |
| US8383657B2 (en) | 2007-12-21 | 2013-02-26 | Abbott Laboratories | Thiazolylidine urea and amide derivatives and methods of use thereof |
| CA2905340C (en) | 2013-03-12 | 2022-05-31 | Celtaxsys, Inc. | Low dose oral formulations of acebilustat |
| EP2968264A4 (en) | 2013-03-14 | 2016-11-02 | Celtaxsys Inc | INHIBITORS OF LEUCOTRIENE A4 HYDROLASE |
| EP2970309A4 (en) | 2013-03-14 | 2016-11-09 | Celtaxsys Inc | INHIBITORS OF LEUCOTRIENE A4 HYDROLASE |
| KR20150131211A (ko) | 2013-03-14 | 2015-11-24 | 켈탁시스, 인코퍼레이티드 | 류코트라이엔 a4 가수분해효소의 저해제 |
| CN108341792B (zh) * | 2018-04-28 | 2021-09-17 | 苏州莱克施德药业有限公司 | 一种Volasertib中间体1-环丙基甲基哌嗪的制备方法 |
| CA3102077A1 (en) | 2018-05-31 | 2019-12-05 | Sanjeev AHUJA | Method of reducing pulmonary exacerbations in respiratory disease patients |
| CN113372245B (zh) * | 2021-06-17 | 2023-01-13 | 仪征市海帆化工有限公司 | 一种n-苯甲酰基-o,o-对甲苯磺酰基-二乙醇胺的合成方法 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2525223A (en) * | 1948-05-25 | 1950-10-10 | American Cyanamid Co | Preparation of n-substituted piperazines |
| DE818805C (de) | 1948-08-02 | 1951-10-29 | Rhone Poulenc Sa | Verfahren zur Herstellung von am Stickstoff durch eine Alkylgruppe monosubstituierten Piperazinen |
| US3342816A (en) * | 1965-06-01 | 1967-09-19 | Lilly Co Eli | Cyclopropylpiperazinoalkyl-phenothiazines |
| DE3542002A1 (de) * | 1985-11-28 | 1987-06-04 | Bayer Ag | 1-cyclopropyl-6-fluor-1,4-dihydro-4-oxo-7- (1-piperazinyl)-3-chinolincarbonsaeuren, verfahren zu ihrer herstellung sowie diese enthaltende antibakterielle mittel |
| DE3605005A1 (de) * | 1986-02-18 | 1987-08-20 | Basf Ag | Verfahren zur herstellung von n-methylpiperazin |
| US6011029A (en) | 1996-02-26 | 2000-01-04 | Bristol-Myers Squibb Company | Inhibitors of farnesyl protein transferase |
| CA2235642C (en) * | 1998-05-15 | 2007-11-13 | Torcan Chemical Ltd. | Processes for preparing sildenafil |
| WO2002020500A2 (en) | 2000-09-01 | 2002-03-14 | Icos Corporation | Materials and methods to potentiate cancer treatment |
| US6642226B2 (en) | 2001-02-06 | 2003-11-04 | Hoffman-La Roche Inc. | Substituted phenyl-piperidine methanone compounds |
| DE10201240A1 (de) * | 2002-01-15 | 2003-07-24 | Bayer Ag | Substituierte Alkyluracile und ihre Verwendung |
| EA009860B1 (ru) * | 2002-10-23 | 2008-04-28 | Янссен Фармацевтика, Н.В. | Пиперазинил- и диазапанилбензамиды и бензтиоамиды |
| WO2005035534A1 (ja) * | 2003-10-08 | 2005-04-21 | Ono Pharmaceutical Co., Ltd. | 複素ビシクロ環および複素トリシクロ環化合物およびその医薬 |
| GB0324159D0 (en) * | 2003-10-15 | 2003-11-19 | Glaxo Group Ltd | Novel compounds |
| WO2006042103A2 (en) | 2004-10-05 | 2006-04-20 | Axys Pharmaceuticals, Inc. | Reversible inhibitors of cathepsin b |
| CA2589748C (en) | 2004-12-24 | 2013-08-13 | Astrazeneca Ab | Heterocyclic compounds as ccr2b antagonists |
| FR2885616B1 (fr) * | 2005-05-12 | 2007-06-22 | Servier Lab | Nouveaux derives de phenylpyridinylpiperazine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| JP5185120B2 (ja) * | 2005-09-16 | 2013-04-17 | 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 | ヒスタミンｈ３受容体のモジュレーターとしてのシクロプロピルアミン |
| US7795426B2 (en) * | 2005-10-31 | 2010-09-14 | Janssen Pharmaceutica Nv | Processes for the preparation of cyclopropyl-amide derivatives |
| CN101389617A (zh) * | 2005-10-31 | 2009-03-18 | 詹森药业有限公司 | 制备哌嗪基和二氮杂环庚烷基苯甲酰胺衍生物的新方法 |
| KR101462891B1 (ko) * | 2006-12-14 | 2014-11-19 | 얀센 파마슈티카 엔.브이. | 피페라지닐 및 디아제파닐 벤즈아미드 유도체의 제조 방법 |
-
2007
- 2007-12-10 KR KR1020097014605A patent/KR101462891B1/ko active IP Right Grant
- 2007-12-10 CA CA2672661A patent/CA2672661C/en active Active
- 2007-12-10 LT LTEP07855037.3T patent/LT2121636T/lt unknown
- 2007-12-10 HU HUE07855037A patent/HUE032761T2/en unknown
- 2007-12-10 CN CNA2007800512756A patent/CN101605767A/zh active Pending
- 2007-12-10 CA CA2880932A patent/CA2880932A1/en not_active Abandoned
- 2007-12-10 PT PT78550373T patent/PT2121636T/pt unknown
- 2007-12-10 SG SG2011092046A patent/SG177207A1/en unknown
- 2007-12-10 MX MX2009006472A patent/MX2009006472A/es active IP Right Grant
- 2007-12-10 MY MYPI20092444A patent/MY147320A/en unknown
- 2007-12-10 EP EP07855037.3A patent/EP2121636B1/en active Active
- 2007-12-10 JP JP2009541499A patent/JP5385150B2/ja not_active Expired - Fee Related
- 2007-12-10 BR BRPI0721088A patent/BRPI0721088B8/pt not_active IP Right Cessation
- 2007-12-10 US US11/953,262 patent/US7893257B2/en not_active Expired - Fee Related
- 2007-12-10 RS RS20170402A patent/RS55866B1/sr unknown
- 2007-12-10 SI SI200731919A patent/SI2121636T1/sl unknown
- 2007-12-10 WO PCT/US2007/086936 patent/WO2008076685A2/en active Application Filing
- 2007-12-10 EA EA200970583A patent/EA200970583A1/ru unknown
- 2007-12-10 NZ NZ577603A patent/NZ577603A/en not_active IP Right Cessation
- 2007-12-10 ES ES07855037.3T patent/ES2620818T3/es active Active
- 2007-12-10 DK DK07855037.3T patent/DK2121636T3/en active
- 2007-12-10 PL PL07855037T patent/PL2121636T3/pl unknown
- 2007-12-13 TW TW096147556A patent/TW200846004A/zh unknown
- 2007-12-14 AR ARP070105628A patent/AR064358A1/es active IP Right Grant
- 2007-12-14 CL CL200703637A patent/CL2007003637A1/es unknown
-
2009
- 2009-06-11 EC EC2009009405A patent/ECSP099405A/es unknown
- 2009-06-11 IL IL199309A patent/IL199309A0/en active IP Right Grant
- 2009-06-12 CO CO09061632A patent/CO6210827A2/es not_active Application Discontinuation
- 2009-07-10 NO NO20092634A patent/NO344305B1/no not_active IP Right Cessation
- 2009-07-13 ZA ZA200904894A patent/ZA200904894B/xx unknown
- 2009-07-14 CR CR10928A patent/CR10928A/es unknown
-
2011
- 2011-01-10 US US12/987,370 patent/US8680273B2/en active Active
-
2012
- 2012-11-13 PH PH12012502236A patent/PH12012502236A1/en unknown
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2013
- 2013-08-05 JP JP2013162225A patent/JP2013241453A/ja active Pending
-
2014
- 2014-09-30 IL IL234893A patent/IL234893A/en active IP Right Grant
-
2017
- 2017-04-07 CY CY20171100420T patent/CY1118814T1/el unknown
- 2017-04-19 HR HRP20170621TT patent/HRP20170621T1/hr unknown
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