SI9200105B - Imidazo(2,1-b)(3)benzazepine derivatives, compositions and method of use - Google Patents
Imidazo(2,1-b)(3)benzazepine derivatives, compositions and method of use Download PDFInfo
- Publication number
- SI9200105B SI9200105B SI9200105A SI9200105A SI9200105B SI 9200105 B SI9200105 B SI 9200105B SI 9200105 A SI9200105 A SI 9200105A SI 9200105 A SI9200105 A SI 9200105A SI 9200105 B SI9200105 B SI 9200105B
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- Prior art keywords
- alkyl
- halo
- represents hydrogen
- substituted
- hydroxycarbonyl
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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
-
- 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
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- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Immunology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Detergent Compositions (AREA)
- Paper (AREA)
Claims (7)
1 PATENTNI ZAHTEVKI 1. Spojina s formulo Rl R2 (I)
njena farmacevtsko sprejemljiva adicijska sol ali stereokemično izomema oblika, kjer vsaka od črtkanih črt neodvisno predstavlja fakultativno vez; R1 predstavja vodik, halo, C^-alkil ali C,_4-alkiloksi; Λ R predstavlja vodik, halo, C^-alkil ali C1_4-alkiloksi; R predstavlja vodik, CM-alkil, etenil, substituiran s hidroksikarbonilom ali C1.4-alkiloksikarbonilom, C,_4-alkil, substitutuiran s hidroksikarbonilom ali C,_4-alkiloksikarbonilom, hidroksi C!_4-alkil, formil ali hidroksikarbonil; R4 predstavlja vodik, CM-alkil, hidroksi C^-alkil, fenil ali halo; R5 predstavlja vodik, C^-alkil ali halo; L predstavlja C^-alkil; Cj.g-alkil, substituiran z enim substituentom, izbranim iz skupine, v kateri so hidroksi, halo, C|_4-alkiloksi, hidroksikarbonil, C1.4-alkiloksikarbonil, C1.4-alkiloksikarbonil-C j _4-alkiloksi, hidroksikarbonilC j _4-alkiloksi, C i _4-alkiloksikarbonilamino, C i _4-alkilaminokarbonil, C ,_4-alkilaminokarbonilamino, C j _4-alkilaminotio-karbonilamino, aril, ariloksi in arilkarbonil; Cj.g-alkil, substituiran tako s hidroksi kot tudi z ariloksi; C3.6-alkenil; C3.6-alkenil, substituiran z arilom; kjer je vsak aril fenil ali fenil, substituiran s halo, ciano, hidroksi, C].4-alkilom, CM-alkiloksi, aminokarbonilom ali fenilom, substituiranim s C^-alkiloksikarbonilom ali hidroksikarbonilom; ali L predstavlja ostanek s formulo 2 -Alk-V-Het1 (a-1), -Alk-NH-CO-Het2 (a-2) ali -Alk-Y-Het3 (a-3), kjer Alk predstavlja Cj^-alkandiil; Y predstavlja O, S ali NH; Het , Het inHet vsakokrat predstavljajo furani 1, tienil, oksazolil, tiazolil ali imidazolil, vsakokrat v danem primeru substituiran z enim ali dvema C1.4-alkilnima substituentoma; pirolil ali pirazolil, v danem primeru substituiran s formilom, hidroksiC^-alki lom, hidroksikarbonilom, Ci_4-alkiloksikarbonilom ali z enim ali dvema CM-alkilnima substituentoma; tiadiazolil ali oksadiazolil, v danem primeru substituiran z amino ali C,_4-alkilom, piridinil, pirimidinil, pirazinil ali piridazinil, vsakokrat v danem primeru substituiran s CN4-alkilom, Ci_4-alkiloksi, amino, hidroksi ali halo; ali imidazo[4,5-c]piridin-2-il; in 2 Het lahko tudi predstavlja član, izbran iz skupine, v kateri so: (a) 4,5-dihidro-5-okso-lH-tetrazolil, substituiran s Cj.4-alkilom; (b) 2-okso-3-oksazolidinil; (c) 2,3-dihidro-2-okso-lH-benzimidazol-l-il; in (d) ostanek s formulo 3 3
or
(b-l) (b-2) kjer R6 predstavlja vodik ali C^-alkil; in A-Z predstavlja -S-CH=CH-, -S-CH2-CH2-, -S-CH2-CH2-CH2-, -CH=CH-CH=CH-, -CH2-CH2-CH2-CH2-, -N(CH3)-C(CH3)=CH- ali -CH=C (CH3)-0-.
2. Spojina po zahtevku 1, označena s tem, daje L CM-alkil ali C^-alkil, substituiran s hidroksikarbonilom ali C].4-alkiloksikarbonilom.
3. Spojina po zahtevku 1, označena s tem, da R predstavlja vodik, Ci_4-alkil, formil, hidroksi C^-alkil ali hidroksikarbonil; R4 predstavlja vodik, halo ali hidroksiC1.4-alkil; in L predstavlja C].4-alkil, haloC|_4-alkil, hidroksikarbonilC, _4-alkil, C14- alkiloksikarbonilC1.4-alkil, C)_4-alkiloksikarbonilaminoC,_4-alkil, arilC^-alkil, propenil, ali je L ostanek s formulo -Alk-Y-Het' (a-1), -Alk-NH-CO-Het2 (a-2) ali -Alk-Y-Het3 (a-3); kjer 12 3 Het, Het in Het vsakokrat predstavljajo furanil, oksazolil ali tiazolil, vsakokrat v danem primeru substituiran s Ci_4-alkilom; tiadiazolil, v danem primeru 4 substituiran z amino; piridinil; pirimidinil, v danem primem substituiran s hidroksi; ali imidazo[4,5-c]piridin-2-il; ali lahko Het tudi predstavlja ostanek s formulo (b-2);
o
4. Spojina po zahtevku 3, označena s tem, da R1 predstavlja vodik ali halo; R2 predstavlja vodik, halo ali C1.4-alkiloksi; in L predstavlja vodik, C^-alkil, haloC1.4-alkil, hidroksikarbonilC]_4-alkil, CM-alkiloksikarbonilC1.4-alkil ali ostanek s formulo (a-1), kjer Y predstavlja NH.
5. Spojina po zahtevku 1, označena s tem, dajo izberemo iz skupine, v kateri so 5,6-dihidro-11-(1 -metil-4-piperidiniliden)-11 H-imidazo [2,1 -b] [3 Jbenzazepin; 9-fluoro-6,11 -dihidro-11 -(1 -metil-4-piperidiniliden)-5H-imidazo[2,1 -b] [3 Jbenzazepin; 11 -(1 -metil-4-piperidiniliden)-11 H-imidazo [2,1 -b] [3 Jbenzazepin; 6.11 -dihidro-11 -(1 -metil-4-piperidiniliden)-5H-imidazo[2,1 -b] [3 Jbenzazepin-3-metanol; 8-fluoro-6,11 -dihidro-11-(1 -metil-4-piperidiniliden)-5H-imidazo[2,1 -b] [3 Jbenzazepin; 6.11 -dihidro-11-(1 -metil-4-piperidiniliden)-5H-imidazo[2,1 -bj [3]benzazepin-3-karboksaldehid; 6.11 -dihidro-11 -(1 -metil-4-piperidiniliden)-5H-imidazo[2,1 -b] [3 Jbenzazepin-3-karboksilna kislina; 7-fluoro-6,11 -dihidro-11-(1 -metil-4-piperidiniliden)-5H-imidazo-[2, lbj [3 Jbenzazepin; in dihidrat 4-(8-fluoro-5,6-dihidro-l 1 H-imidazo [2,1-bJ [3 Jbenzazepin-11 -iliden)-1 -piperidin-propanojske kisline. 5
6. Farmacevtski sestavek, označen s tem, da kot aktivno sestavino vsebuje terapevtsko učinkovito količino spojine, definirane po kateremkoli od zahtevkov 1 do 5, in farmacevtsko sprejemljiv nosilec.
7. Spojina s formulo R1 R2 (VID
njena kislinska adicijska sol ali stereokemično izomema oblika, kjer vsaka od črtkanih črt neodvisno predstavlja fakultativno vez, in kjer R1 predstavlja vodik, halo, C^-alkil ali CM-alkiloksi; R2 predstavlja vodik, halo, C|_4-alkil ali C^-alkiloksi; R3 predstavlja vodik, C].4-alkil, etenil, substituiran s hidroksikarbonilom ali Ci_4-alkiloksikarbonilom, CM-alkil, substituiran s hidroksikarbonilom ali C14-alkiloksikarbonilom, hidroksid _4-alkil, formil ali hidroksikarbonil; R4 predstavlja vodik, C^-alkil, hidroksiC].4-alkil, fenil ali halo; R5 predstavlja vodik, C1_4-alkil ali halo; in Q predstavlja feniloksikarbonil ali Cj.6-alkil, substituiran s članom, izbranim iz skupine, v kateri so halo, ciano, amino, izotiocianato, (4-amino-3-piridiniljaminotiokarbonilamino, (CH30)2CH-CH2-NH-C(=NCH3)-NH- in metilsulfoniloksi.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US71448691A | 1991-06-13 | 1991-06-13 | |
| US85363192A | 1992-03-18 | 1992-03-18 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| SI9200105A SI9200105A (en) | 1992-12-31 |
| SI9200105B true SI9200105B (en) | 2001-10-31 |
Family
ID=27109168
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SI9200105A SI9200105B (en) | 1991-06-13 | 1992-06-12 | Imidazo(2,1-b)(3)benzazepine derivatives, compositions and method of use |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US5468743A (sl) |
| EP (2) | EP0588858B1 (sl) |
| JP (1) | JP2845407B2 (sl) |
| KR (1) | KR0184017B1 (sl) |
| CN (2) | CN1033586C (sl) |
| AT (1) | ATE250061T1 (sl) |
| AU (1) | AU652840B2 (sl) |
| CA (1) | CA2103242C (sl) |
| DE (1) | DE69233205T2 (sl) |
| DK (1) | DK0588858T3 (sl) |
| DZ (1) | DZ1582A1 (sl) |
| ES (1) | ES2207632T3 (sl) |
| FI (1) | FI104175B (sl) |
| HR (1) | HRP920155A2 (sl) |
| HU (2) | HU221016B1 (sl) |
| IE (1) | IE921918A1 (sl) |
| IL (1) | IL101850A (sl) |
| MA (1) | MA22553A1 (sl) |
| MX (1) | MX9202856A (sl) |
| NO (2) | NO934492D0 (sl) |
| NZ (1) | NZ242774A (sl) |
| PT (1) | PT588858E (sl) |
| SG (1) | SG47823A1 (sl) |
| SI (1) | SI9200105B (sl) |
| TN (1) | TNSN92048A1 (sl) |
| TW (1) | TW218381B (sl) |
| WO (1) | WO1992022551A1 (sl) |
| YU (1) | YU61192A (sl) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL101851A (en) * | 1991-06-13 | 1996-05-14 | Janssen Pharmaceutica Nv | History 01 -) 4 - Pipridinyl - and Pipridinylidene (- Imidazo] A-1,2 [Pirolo, Thiano or Purano (] 3,2 [Azpin, their preparation and pharmaceutical preparations containing them and composition |
| GR1001393B (el) * | 1992-10-12 | 1993-10-29 | Janssen Pharmaceutica Nv | Παράγωγα ιμιδαζο[2,1-Β] 3] βενζαζεπίνης, συν?έσεις και μέ?οδος χρήσεως. |
| WO1994013671A1 (en) * | 1992-12-04 | 1994-06-23 | Janssen Pharmaceutica N.V. | Antiallergic triazolobenzazepine derivatives |
| ES2155092T3 (es) * | 1993-07-13 | 2001-05-01 | Janssen Pharmaceutica Nv | Imidazoazepinas antialergicas. |
| TW382017B (en) * | 1995-12-27 | 2000-02-11 | Janssen Pharmaceutica Nv | 1-(1,2-disubstituted piperidinyl)-4-(fused imidazole)-piperidine derivatives |
| TW527186B (en) | 1996-03-19 | 2003-04-11 | Janssen Pharmaceutica Nv | Fused imidazole derivatives as multidrug resistance modulators |
| JP3775780B2 (ja) | 1997-09-18 | 2006-05-17 | 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 | 薬剤の経口的バイオアベイラビリテイを向上させるための縮合イミダゾール誘導体 |
| SI1144411T1 (sl) * | 1998-12-19 | 2005-10-31 | Janssen Pharmaceutica N.V. | Antihistaminske spiro spojine |
| CN100491378C (zh) | 2001-06-12 | 2009-05-27 | 詹森药业有限公司 | 新的取代四环咪唑衍生物,其制备方法,包含它们的药物组合物及它们作为药物的用途 |
| CN1160557C (zh) | 2001-09-03 | 2004-08-04 | 北京埃索特核电子机械有限公司 | 钴60γ射线源-碘化铯或钨酸镉阵列探测器集装箱检测设备 |
| EP1858896B1 (en) | 2005-03-08 | 2010-08-18 | Janssen Pharmaceutica NV | Diaza-spiro-[4.4]-nonane derivatives as neurokinin (nk1) antagonists |
| US20070077302A1 (en) * | 2005-09-30 | 2007-04-05 | Azaam Alli | Methods for stabilizing ophthalmic compositions |
| US20070077303A1 (en) * | 2005-09-30 | 2007-04-05 | Azaam Alli | Methods for providing oxidatively stable ophthalmic compositions |
| EA016221B1 (ru) * | 2006-03-31 | 2012-03-30 | ВИСТЭКОН ФАРМАСЬЮТИКАЛС, ЭлЭлСи | Офтальмические композиции и способ лечения аллергических заболеваний глаз |
| US20080139531A1 (en) * | 2006-12-04 | 2008-06-12 | Alcon Manufacturing Ltd. | Use of connective tissue mast cell stabilizers to facilitate ocular surface re-epithelization and wound repair |
| US20090182035A1 (en) * | 2007-04-11 | 2009-07-16 | Alcon Research, Ltd. | Use of a combination of olopatadine and cilomilast to treat non-infectious rhinitis and allergic conjunctivitis |
| CA2682730A1 (en) * | 2007-04-11 | 2008-10-23 | Alcon Research, Ltd. | Use of an inhibitor of tnf.alpha. plus an antihistamine to treat allergic rhinitis and allergic conjunctivitis |
| BR112012007091A2 (pt) * | 2009-10-01 | 2016-04-19 | Alcon Res Ltd | composições de olopatadina e seus usos |
| AR079170A1 (es) * | 2009-12-10 | 2011-12-28 | Lilly Co Eli | Compuesto de ciclopropil-benzamida-imidazo-benzazepina inhibidor de diacil-glicerol aciltransferasa, sal del mismo, composicion farmaceutica que lo comprende, su uso para preparar un medicamento util para el tratamiento de obesidad o para mejorar la sensibilidad a insulina y compuesto intermedio par |
| AU2012275113A1 (en) * | 2011-06-29 | 2014-01-30 | Allergan, Inc. | Alcaftadine for use in the treatment of urticaria |
| WO2014080259A1 (en) * | 2012-11-21 | 2014-05-30 | Enaltec Labs Pvt. Ltd. | Novel polymorphic forms of alcaftadine |
| WO2014083571A1 (en) * | 2012-11-29 | 2014-06-05 | Neuland Laboratories Limited | A process for the preparation of alcaftadine |
| US9255105B2 (en) | 2012-12-06 | 2016-02-09 | Enaltec Labs Private Limited | Process of preparing alcaftadine |
| US9682984B2 (en) | 2013-03-25 | 2017-06-20 | Crystal Pharma S.A.U. | Methods for the preparation of alcaftadine |
| CN103408549B (zh) * | 2013-06-14 | 2016-01-20 | 苏州汇和药业有限公司 | 一种阿卡他定中间体的制备方法 |
| MX2017002610A (es) | 2014-08-29 | 2017-10-11 | Tes Pharma S R L | INHIBIDORES DE ACIDO A-AMINO-ß-CARBOXIMUCONICO SEMIALDEHIDO DESCARBOXILASA. |
| CN104710427A (zh) * | 2014-12-20 | 2015-06-17 | 威海法莫斯特医药技术开发有限公司 | 一种阿卡他定新晶型 |
| CN104860920B (zh) * | 2015-04-15 | 2017-08-25 | 武汉武药科技有限公司 | 一种阿卡他定中间体的制备方法 |
| CN105130993B (zh) * | 2015-07-28 | 2018-01-12 | 武汉武药科技有限公司 | 一种合成阿卡他定的新氧化方法 |
| CN104987337B (zh) * | 2015-07-28 | 2018-01-12 | 武汉武药科技有限公司 | 一种制备阿卡他定的氧化方法 |
| WO2018031973A1 (en) | 2016-08-12 | 2018-02-15 | Silk Technologies, Ltd. | Silk-derived protein for treating inflammation |
| CN108727384A (zh) * | 2018-07-07 | 2018-11-02 | 张正光 | 一种阿卡他定中间体的制备方法 |
| WO2021255622A1 (en) | 2020-06-15 | 2021-12-23 | Alkem Laboratories Limited | Combination of alcaftadine and a corticosteroid |
| JP2024512121A (ja) | 2021-04-01 | 2024-03-18 | アルケム・ラボラトリーズ・リミテッド | アルカフタジンを含む鼻用組成物 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4148903A (en) * | 1977-07-28 | 1979-04-10 | Merck & Co., Inc. | Antipsychotic, antiserotonin and antihistaminic pyrrolo[2,1-b][3]benzazepines |
| GB8900380D0 (en) * | 1989-01-09 | 1989-03-08 | Janssen Pharmaceutica Nv | 2-aminopyrimidinone derivatives |
| CA2093797C (en) * | 1990-10-10 | 1998-09-22 | Richard J. Friary | Substituted imidazobenzazepines and imidazopyridoazepines |
| IL101851A (en) * | 1991-06-13 | 1996-05-14 | Janssen Pharmaceutica Nv | History 01 -) 4 - Pipridinyl - and Pipridinylidene (- Imidazo] A-1,2 [Pirolo, Thiano or Purano (] 3,2 [Azpin, their preparation and pharmaceutical preparations containing them and composition |
-
1992
- 1992-05-13 IL IL10185092A patent/IL101850A/en not_active IP Right Cessation
- 1992-05-15 NZ NZ242774A patent/NZ242774A/en not_active IP Right Cessation
- 1992-05-16 CN CN92105040A patent/CN1033586C/zh not_active Expired - Lifetime
- 1992-05-18 DZ DZ920051A patent/DZ1582A1/fr active
- 1992-05-21 TW TW081103954A patent/TW218381B/zh not_active IP Right Cessation
- 1992-06-09 DE DE69233205T patent/DE69233205T2/de not_active Expired - Lifetime
- 1992-06-09 EP EP92911635A patent/EP0588858B1/en not_active Expired - Lifetime
- 1992-06-09 KR KR1019930703788A patent/KR0184017B1/ko not_active IP Right Cessation
- 1992-06-09 ES ES92911635T patent/ES2207632T3/es not_active Expired - Lifetime
- 1992-06-09 SG SG1996004579A patent/SG47823A1/en unknown
- 1992-06-09 US US08/142,474 patent/US5468743A/en not_active Expired - Lifetime
- 1992-06-09 DK DK92911635T patent/DK0588858T3/da active
- 1992-06-09 AU AU19001/92A patent/AU652840B2/en not_active Expired
- 1992-06-09 JP JP4510733A patent/JP2845407B2/ja not_active Expired - Lifetime
- 1992-06-09 PT PT92911635T patent/PT588858E/pt unknown
- 1992-06-09 HU HU9303553A patent/HU221016B1/hu unknown
- 1992-06-09 AT AT92911635T patent/ATE250061T1/de active
- 1992-06-09 WO PCT/EP1992/001330 patent/WO1992022551A1/en active IP Right Grant
- 1992-06-09 CA CA002103242A patent/CA2103242C/en not_active Expired - Lifetime
- 1992-06-09 EP EP92201666A patent/EP0518435A1/en active Pending
- 1992-06-10 HR HR920155A patent/HRP920155A2/hr not_active Application Discontinuation
- 1992-06-11 MA MA22843A patent/MA22553A1/fr unknown
- 1992-06-12 YU YU61192A patent/YU61192A/sh unknown
- 1992-06-12 SI SI9200105A patent/SI9200105B/sl unknown
- 1992-06-12 MX MX9202856A patent/MX9202856A/es unknown
- 1992-06-15 TN TNTNSN92048A patent/TNSN92048A1/fr unknown
- 1992-07-01 IE IE191892A patent/IE921918A1/en not_active Application Discontinuation
-
1993
- 1993-12-09 NO NO934492D patent/NO934492D0/no unknown
- 1993-12-09 NO NO934492A patent/NO300636B1/no not_active IP Right Cessation
- 1993-12-10 FI FI935556A patent/FI104175B/fi not_active IP Right Cessation
-
1995
- 1995-06-06 HU HU95P/P00164P patent/HU211289A9/hu unknown
-
1996
- 1996-04-24 CN CN96106116A patent/CN1070368C/zh not_active Expired - Lifetime
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