ES2158859T3 - Estereoisomeros itraconazol y saperconazol. - Google Patents
Estereoisomeros itraconazol y saperconazol.Info
- Publication number
- ES2158859T3 ES2158859T3 ES93905338T ES93905338T ES2158859T3 ES 2158859 T3 ES2158859 T3 ES 2158859T3 ES 93905338 T ES93905338 T ES 93905338T ES 93905338 T ES93905338 T ES 93905338T ES 2158859 T3 ES2158859 T3 ES 2158859T3
- Authority
- ES
- Spain
- Prior art keywords
- saperconazol
- itraconazol
- stereoisomeros
- preparation
- complexes
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- HUADITLKOCMHSB-AVQIMAJZSA-N 2-butan-2-yl-4-[4-[4-[4-[[(2s,4r)-2-(2,4-difluorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one Chemical compound O=C1N(C(C)CC)N=CN1C1=CC=C(N2CCN(CC2)C=2C=CC(OC[C@H]3O[C@@](CN4N=CN=C4)(OC3)C=3C(=CC(F)=CC=3)F)=CC=2)C=C1 HUADITLKOCMHSB-AVQIMAJZSA-N 0.000 title abstract 2
- VHVPQPYKVGDNFY-ZPGVKDDISA-N itraconazole Chemical compound O=C1N(C(C)CC)N=CN1C1=CC=C(N2CCN(CC2)C=2C=CC(OC[C@@H]3O[C@](CN4N=CN=C4)(OC3)C=3C(=CC(Cl)=CC=3)Cl)=CC=2)C=C1 VHVPQPYKVGDNFY-ZPGVKDDISA-N 0.000 title abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—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
- C07D405/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B82—NANOTECHNOLOGY
- B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
- B82Y15/00—Nanotechnology for interacting, sensing or actuating, e.g. quantum dots as markers in protein assays or molecular motors
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- 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
- C07D233/56—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 only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nanotechnology (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Crystallography & Structural Chemistry (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- General Chemical & Material Sciences (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
LA PRESENTE INVENCION SE REFIERE A LAS FORMAS ESTEREOISOMERICAS DE ITRACONAZOL (X = CL) Y SAPERCONAZOL (X = F), QUE SE PUEDEN REPRESENTAR CON LA FORMULA (CIS-(I)) Y A LAS SALES DE ADICION ACIDAS FARMACEUTICAMENTE ACEPTABLES DE LAS MISMAS, A LOS PROCESOS PARA LA PREPARACION DE DICHAS FORMAS ESTEREOISOMERICAS, A LOS COMPLEJOS DE LAS MISMAS CON DERIVADOS DE CICLODEXTRINAS, A LAS COMPOSICIONES FARMACEUTICAS QUE CONTIENE DICHOS COMPLEJOS Y A LOS METODOS PARA LA PREPARACION DE DICHOS COMPLEJOS Y COMPOSICIONES FARMACEUTICAS.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US85364892A | 1992-03-18 | 1992-03-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2158859T3 true ES2158859T3 (es) | 2001-09-16 |
Family
ID=25316567
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES93905338T Expired - Lifetime ES2158859T3 (es) | 1992-03-18 | 1993-03-10 | Estereoisomeros itraconazol y saperconazol. |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US5998413A (es) |
| EP (1) | EP0631578B1 (es) |
| KR (1) | KR100243534B1 (es) |
| AT (1) | ATE201408T1 (es) |
| AU (1) | AU665988B2 (es) |
| CA (1) | CA2117651C (es) |
| CZ (1) | CZ286619B6 (es) |
| DE (1) | DE69330248T2 (es) |
| DK (1) | DK0631578T3 (es) |
| ES (1) | ES2158859T3 (es) |
| FI (1) | FI113175B (es) |
| GR (1) | GR3036368T3 (es) |
| HU (1) | HU221189B1 (es) |
| NO (1) | NO307786B1 (es) |
| NZ (1) | NZ249494A (es) |
| PL (1) | PL172358B1 (es) |
| PT (1) | PT631578E (es) |
| RU (1) | RU2127733C1 (es) |
| SK (1) | SK283118B6 (es) |
| WO (1) | WO1993019061A1 (es) |
| ZA (1) | ZA931906B (es) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH08509464A (ja) * | 1993-01-27 | 1996-10-08 | セプラコア,インコーポレイテッド | (2r,4s)イトラコナゾールを使用する方法および組成物 |
| PH31594A (en) * | 1993-09-30 | 1998-11-03 | Janssen Pharmaceutica Nv | Oral formulations on an antifungal. |
| TW438601B (en) * | 1994-05-18 | 2001-06-07 | Janssen Pharmaceutica Nv | New mucoadhesive emulsion compositions and a process for the preparation thereof |
| US5486625A (en) * | 1994-07-08 | 1996-01-23 | Schering Corporation | Process for the preparation of chiral intermediates useful for the synthesis of antifungal agents |
| ES2112151B1 (es) * | 1995-03-17 | 1999-09-16 | Menarini Lab | Nuevos compuestos homoquirales para la preparacion de ketoconazol, terconazol y antifungicos relacionados, procedimiento para su fabricacion y utilizacion de los mismos. |
| DE69733664T3 (de) | 1996-04-19 | 2011-04-14 | Grifols Inc. (n.d. Ges.d.Staates Delaware), Los Angeles | Verfahren zur INaktivierung von Viren und Lyophilisierung von Blutproteinen |
| ATE255883T1 (de) * | 1996-05-20 | 2003-12-15 | Janssen Pharmaceutica Nv | Fungizide mittel mit verbesserter bioverfügbarkeit |
| EP0942725A1 (en) * | 1996-11-12 | 1999-09-22 | Sepracor, Inc. | Use of cis-hydroxyitraconazole in order to avoid side-effects of itraconazole and hydroxyintraconazole |
| JP2001504121A (ja) * | 1996-11-12 | 2001-03-27 | セプラコール,インク. | 2r,4s,r,s―および2s,4r,r,s―ヒドロキシイトラコナゾール―およびヒドロキシサパーコナゾール誘導体 |
| CN1237174A (zh) * | 1996-11-12 | 1999-12-01 | 塞普拉科公司 | 2r,4s,s,r-和2s,4r,s,r-羟基伊曲康唑 |
| WO1998021204A1 (en) | 1996-11-12 | 1998-05-22 | Sepracor, Inc. | 2r,4s,s,s- and 2s,4r,s,s-hydroxyitraconazole |
| AU5251398A (en) * | 1996-11-12 | 1998-06-03 | Sepracor, Inc. | (2r,4s,r,r-) and (2s,4r,r,r-)hydroxyitraconazole |
| WO1998034934A1 (en) | 1997-02-11 | 1998-08-13 | Janssen Pharmaceutica N.V. | Amino acid ester containing azole antifungals |
| US6683100B2 (en) | 1999-01-19 | 2004-01-27 | Novartis Ag | Organic compounds |
| US6194181B1 (en) | 1998-02-19 | 2001-02-27 | Novartis Ag | Fermentative preparation process for and crystal forms of cytostatics |
| EP0957101A1 (en) * | 1998-05-14 | 1999-11-17 | Janssen Pharmaceutica N.V. | Water soluble azoles as broad-spectrum antifungals |
| ES2251985T3 (es) | 1999-03-24 | 2006-05-16 | R.P. Scherer Technologies, Inc. | Particula granulada para mejorar la solubilidad acuosa de farmacos, y su procedimiento de preparacion. |
| KR100331529B1 (ko) * | 1999-06-16 | 2002-04-06 | 민경윤 | 난용성 항진균제의 경구투여용 조성물 및 그의 제조 방법 |
| US6932861B2 (en) | 2000-11-28 | 2005-08-23 | Fmc Corporation | Edible PGA coating composition |
| KR100438485B1 (ko) * | 2001-08-13 | 2004-07-09 | 한국디디에스제약 주식회사 | 아졸류 항진균제의 약제학적 조성물 |
| US7790905B2 (en) | 2002-02-15 | 2010-09-07 | Mcneil-Ppc, Inc. | Pharmaceutical propylene glycol solvate compositions |
| US7927613B2 (en) | 2002-02-15 | 2011-04-19 | University Of South Florida | Pharmaceutical co-crystal compositions |
| US7446107B2 (en) * | 2002-02-15 | 2008-11-04 | Transform Pharmaceuticals, Inc. | Crystalline forms of conazoles and methods of making and using the same |
| WO2004000284A1 (en) | 2002-06-21 | 2003-12-31 | Transform Pharmaceuticals, Inc. | Pharmaceutical compositions with improved dissolution |
| CA2477923C (en) | 2002-03-01 | 2021-02-23 | University Of South Florida | Multiple-component solid phases containing at least one active pharmaceutical ingredient |
| EP1511490A4 (en) * | 2002-05-31 | 2009-03-11 | Transform Pharmaceuticals Inc | NOVEL CONAZOLE CRYSTALLINE FORMS AND RELATED METHODS, PHARMACEUTICAL COMPOSITIONS AND METHODS |
| US20070059356A1 (en) * | 2002-05-31 | 2007-03-15 | Almarsson Oern | Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen |
| KR100446256B1 (ko) * | 2002-07-11 | 2004-09-01 | 경동제약 주식회사 | 고 광학선택성을 가지는시스-2-(브로모메틸)-2-(2,4-디클로로페닐)-13-디옥소란-4-메틸알콜의 제조방법 |
| US8183290B2 (en) | 2002-12-30 | 2012-05-22 | Mcneil-Ppc, Inc. | Pharmaceutically acceptable propylene glycol solvate of naproxen |
| US8486456B2 (en) | 2005-08-08 | 2013-07-16 | Abbott Gmbh & Co., Kg | Itraconazole compositions with improved bioavailability |
| PL1912626T3 (pl) | 2005-08-08 | 2016-10-31 | Postaci użytkowe o polepszonej biodostępności | |
| US8653083B2 (en) | 2005-08-22 | 2014-02-18 | The Johns Hopkins University | Hedgehog pathway antagonists to treat disease |
| EP2753179A4 (en) * | 2011-09-09 | 2015-03-04 | Univ Leland Stanford Junior | TOPICAL ITRACONAZOLE FORMULATIONS AND THEIR USE |
| CN102379844A (zh) * | 2011-10-31 | 2012-03-21 | 广州维美投资有限公司 | 一种伊曲康唑异构体注射剂 |
| CN105061411A (zh) * | 2015-06-23 | 2015-11-18 | 扬州艾迪生物科技有限公司 | 一种光学异构体2s,4r,2’s-伊曲康唑晶型及制备方法与应用 |
| CN106146480B (zh) * | 2016-07-18 | 2019-08-06 | 山东罗欣药业集团恒欣药业有限公司 | 一种伊曲康唑的制备方法 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4267179A (en) * | 1978-06-23 | 1981-05-12 | Janssen Pharmaceutica, N.V. | Heterocyclic derivatives of (4-phenylpiperazin-1-yl-aryloxymethyl-1,3-dioxolan-2-yl)methyl-1H-imidazoles and 1H-1,2,4-triazoles |
| US4287195A (en) * | 1978-07-14 | 1981-09-01 | Janssen Pharmaceutica, N.V. | Heterocyclic derivatives of [4-(piperazin-1-yl-phenyloxymethyl)-1,3-dioxolan-2-ylmethyl]-1H-imidazoles and 1H-1,2,4-triazoles |
| US4490530A (en) * | 1981-01-14 | 1984-12-25 | Janssen Pharmaceutica N.V. | Heterocyclic derivatives of (4-phenylpiperazin-1-yl-aryloxymethyl-1,3-dioxolan-2-yl)-methyl-1H-imidazoles and 1H-1,2,4-triazoles |
| HU191101B (en) * | 1983-02-14 | 1987-01-28 | Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt,Hu | Process for preparing water-soluble cyclodextrin polymers substituted with ionic groups |
| DE3346123A1 (de) * | 1983-12-21 | 1985-06-27 | Janssen Pharmaceutica, N.V., Beerse | Pharmazeutische praeparate von in wasser schwerloeslichen oder instabilen arzneistoffen und verfahren zu ihrer herstellung |
| GB8506792D0 (en) * | 1985-03-15 | 1985-04-17 | Janssen Pharmaceutica Nv | Derivatives of y-cyclodextrin |
| US4916134A (en) * | 1987-03-25 | 1990-04-10 | Janssen Pharmacuetica N.V. | 4-[4-[4-[4-[[2-(2,4-difluorophenyl)-2-(1H-azolylmethyl)-1,3-dioxolan-4-yl]me]phenyl]-1-piperazinyl]phenyl]triazolones |
| FR2622198B1 (fr) * | 1987-10-21 | 1992-04-30 | Mero Rousselot Satia | Compositions granulees de polysaccharides a dissolution aqueuse instantanee, procede pour leur preparation et utilisation |
| US5002935A (en) * | 1987-12-30 | 1991-03-26 | University Of Florida | Improvements in redox systems for brain-targeted drug delivery |
| US5017566A (en) * | 1987-12-30 | 1991-05-21 | University Of Florida | Redox systems for brain-targeted drug delivery |
| HK1009335A1 (en) * | 1989-04-03 | 1999-05-28 | Janssen Pharmaceutica N.V. | Regioselective substitutions in cyclodextrins |
| GB8908250D0 (en) * | 1989-04-12 | 1989-05-24 | Fisons Plc | Formulations |
| US5214046A (en) * | 1989-07-27 | 1993-05-25 | Hoffmann-La Roche Inc. | Substituted aminoalkoxybenzene anti-fungicidal compositions and use |
| JPH08509464A (ja) * | 1993-01-27 | 1996-10-08 | セプラコア,インコーポレイテッド | (2r,4s)イトラコナゾールを使用する方法および組成物 |
-
1993
- 1993-03-10 CA CA002117651A patent/CA2117651C/en not_active Expired - Fee Related
- 1993-03-10 WO PCT/EP1993/000552 patent/WO1993019061A1/en not_active Ceased
- 1993-03-10 SK SK1106-94A patent/SK283118B6/sk unknown
- 1993-03-10 DE DE69330248T patent/DE69330248T2/de not_active Expired - Fee Related
- 1993-03-10 CZ CZ19942215A patent/CZ286619B6/cs not_active IP Right Cessation
- 1993-03-10 KR KR1019940702921A patent/KR100243534B1/ko not_active Expired - Fee Related
- 1993-03-10 PT PT93905338T patent/PT631578E/pt unknown
- 1993-03-10 DK DK93905338T patent/DK0631578T3/da active
- 1993-03-10 HU HU9402656A patent/HU221189B1/hu not_active IP Right Cessation
- 1993-03-10 AU AU36324/93A patent/AU665988B2/en not_active Ceased
- 1993-03-10 RU RU94045798A patent/RU2127733C1/ru not_active IP Right Cessation
- 1993-03-10 EP EP93905338A patent/EP0631578B1/en not_active Expired - Lifetime
- 1993-03-10 NZ NZ249494A patent/NZ249494A/en not_active IP Right Cessation
- 1993-03-10 ES ES93905338T patent/ES2158859T3/es not_active Expired - Lifetime
- 1993-03-10 PL PL93305223A patent/PL172358B1/pl not_active IP Right Cessation
- 1993-03-10 AT AT93905338T patent/ATE201408T1/de not_active IP Right Cessation
- 1993-03-17 ZA ZA931906A patent/ZA931906B/xx unknown
-
1994
- 1994-09-16 FI FI944311A patent/FI113175B/fi active
- 1994-09-16 NO NO943450A patent/NO307786B1/no unknown
-
1996
- 1996-07-09 US US08/676,531 patent/US5998413A/en not_active Expired - Fee Related
-
2001
- 2001-08-10 GR GR20010401224T patent/GR3036368T3/el not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| PL172358B1 (en) | 1997-09-30 |
| WO1993019061A1 (en) | 1993-09-30 |
| DE69330248T2 (de) | 2002-03-21 |
| NO943450D0 (no) | 1994-09-16 |
| SK110694A3 (en) | 1995-04-12 |
| HUT71835A (en) | 1996-02-28 |
| RU94045798A (ru) | 1996-07-20 |
| HK1010729A1 (en) | 1999-06-25 |
| NO943450L (no) | 1994-11-11 |
| GR3036368T3 (en) | 2001-11-30 |
| KR950700904A (ko) | 1995-02-20 |
| KR100243534B1 (ko) | 2000-03-02 |
| CZ286619B6 (cs) | 2000-05-17 |
| NZ249494A (en) | 1996-04-26 |
| HU221189B1 (en) | 2002-08-28 |
| FI944311A0 (fi) | 1994-09-16 |
| US5998413A (en) | 1999-12-07 |
| HU9402656D0 (en) | 1994-11-28 |
| CA2117651A1 (en) | 1993-09-30 |
| FI113175B (fi) | 2004-03-15 |
| NO307786B1 (no) | 2000-05-29 |
| ZA931906B (en) | 1994-09-17 |
| CZ221594A3 (en) | 1995-01-18 |
| DE69330248D1 (de) | 2001-06-28 |
| CA2117651C (en) | 2006-01-03 |
| PT631578E (pt) | 2001-11-30 |
| RU2127733C1 (ru) | 1999-03-20 |
| AU3632493A (en) | 1993-10-21 |
| DK0631578T3 (da) | 2001-08-27 |
| FI944311L (fi) | 1994-09-16 |
| SK283118B6 (sk) | 2003-02-04 |
| AU665988B2 (en) | 1996-01-25 |
| EP0631578A1 (en) | 1995-01-04 |
| ATE201408T1 (de) | 2001-06-15 |
| EP0631578B1 (en) | 2001-05-23 |
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