AR012622A1 - Inhibidores de proteasas, procedimiento para su preparacion, composicion farmaceutica que los comprende y el uso de los mismos en la fabricacion de unmedicamento - Google Patents
Inhibidores de proteasas, procedimiento para su preparacion, composicion farmaceutica que los comprende y el uso de los mismos en la fabricacion de unmedicamentoInfo
- Publication number
- AR012622A1 AR012622A1 ARP980101999A ARP980101999A AR012622A1 AR 012622 A1 AR012622 A1 AR 012622A1 AR P980101999 A ARP980101999 A AR P980101999A AR P980101999 A ARP980101999 A AR P980101999A AR 012622 A1 AR012622 A1 AR 012622A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- 6alkyl
- het
- alkenyl
- independently
- Prior art date
Links
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 title 1
- 238000004519 manufacturing process Methods 0.000 title 1
- 229940126601 medicinal product Drugs 0.000 title 1
- 238000000034 method Methods 0.000 title 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000002950 monocyclic group Chemical group 0.000 abstract 2
- 125000001624 naphthyl group Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 102220024746 rs199473444 Human genes 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 108091005804 Peptidases Proteins 0.000 abstract 1
- 239000004365 Protease Substances 0.000 abstract 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
- C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Enzymes And Modification Thereof (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Compuesto que inhiben proteasas de formulas (I), en la que: L es alquilo de C2-6, Ar-alquilo de C0-6, Het-alquilo de C0-6, CH(R4)NR5R6, CH(R4)Ar,CH(R4)OAr o NR4R7; Ar es fenilo o naftilo; Ar es fenilo o naftilo; Het es un anillo heterocíclico monocíclico, estable, de 5 a 7 miembros, o un anilloheterocíclico bicíclico, estable, de 7 a 10 miembros, saturado o insaturado, y que consta de átomos de carbono y de uno a cuatro heteroátomos seleccionadosentre el grupo constituido por N, O y S, estando dicho anillo heterocíclico unido a cualquier heteroátomo o átomo de carbono que dé como resultado unaestructura estable, o cualquier grupo bicíclico en el que cualquiera de dichos anillos heterocíclicos monocíclicos esté fusionado con un anillo bencénico; Wes C(O), SO2; X, Y y Z son, independientemente, N, O, S o CR10 con tal que al menos dos de X, Y y Z sean heteroátomos y al menos uno de X, Y y Z sea N, oque uno de X, Y y Z sea C = N, C = C o N = N, y los otros dos sean CR10 o N,con tal que, además, al menos dos de X, Y y Z sean N; -- indica un enlacesencillo o doble en el heterociclo de cinco miembros; R, R1, R2, R5, R8, R9, R10 y R12 son, independientemente, H, alquilo de C1-6, alquenilo de C2-6-, Ar-alquilo de C0-6 o Het-alquilo de C0-6; R3 es alquilo de C3-6, Ar, Het, CH(R11) Ar, CH(R11)OAr, NR11R12, CH(R11)NR12R13; o formula (II); R4, R11 y R15 son,independientemente, H, alquilo de C1-6, alquenilo de C2-6, cicloalquilo de C3-6-alquilo de C0-6, Ar-alquilo de C0-6 o Het-alquilo de C0-6; R7 es alquilode C1-6, alquenilo de C1-6, cicloalquilo de C3-6-alquilo de C0-6, Ar-alquilo de C0-6, o Het-alquilo de C0-6; R6 y R13 son R14, R14C(O), R14C(S), R14OC(O), oR14OC(O)NR9CH(R15)(CO); y R14 es alquilo de C1-6, alquenilo de C2-6, Ar-alquilo de C0-6, o Het alquilo de C0-6; y sus sales, hidratos y solvatos
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4506797P | 1997-04-29 | 1997-04-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR012622A1 true AR012622A1 (es) | 2000-11-08 |
Family
ID=21935831
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP980101999A AR012622A1 (es) | 1997-04-29 | 1998-04-29 | Inhibidores de proteasas, procedimiento para su preparacion, composicion farmaceutica que los comprende y el uso de los mismos en la fabricacion de unmedicamento |
Country Status (18)
| Country | Link |
|---|---|
| EP (1) | EP1019046A4 (es) |
| JP (1) | JP2002504097A (es) |
| KR (1) | KR20010020391A (es) |
| CN (1) | CN1261276A (es) |
| AR (1) | AR012622A1 (es) |
| AU (1) | AU7365198A (es) |
| BR (1) | BR9809333A (es) |
| CA (1) | CA2287989A1 (es) |
| CO (1) | CO4940477A1 (es) |
| HU (1) | HUP0001294A3 (es) |
| IL (1) | IL132629A0 (es) |
| MA (1) | MA26487A1 (es) |
| NO (1) | NO995268L (es) |
| PE (1) | PE69099A1 (es) |
| PL (1) | PL337725A1 (es) |
| TR (1) | TR199902703T2 (es) |
| WO (1) | WO1998048799A1 (es) |
| ZA (1) | ZA983522B (es) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2314980A1 (en) | 1997-12-19 | 1999-07-01 | Smithkline Beecham Corporation | Compounds of heteroaryl substituted imidazole, their pharmaceutical compositions and uses |
| US6100282A (en) * | 1998-01-02 | 2000-08-08 | Hoffman-La Roche Inc. | Thiazole derivatives |
| MA26618A1 (fr) * | 1998-04-09 | 2004-12-20 | Smithkline Beecham Corp | Composes et compositions pharmaceutiques pour le traitement du paludisme |
| US6858617B2 (en) | 1998-05-26 | 2005-02-22 | Smithkline Beecham Corporation | Substituted imidazole compounds |
| EP1126852B1 (en) | 1998-11-04 | 2004-01-21 | SmithKline Beecham Corporation | Pyridin-4-yl or pyrimidin-4-yl substituted pyrazines |
| CO5150165A1 (es) * | 1998-11-13 | 2002-04-29 | Smithkline Beecham Plc | Inhibidores de proteasa: tipo catepsina k |
| US20030144175A1 (en) | 1998-12-23 | 2003-07-31 | Smithkline Beecham Corporation | Protease inhibitors |
| AU1588901A (en) | 1999-11-10 | 2001-06-06 | Smithkline Beecham Corporation | Protease inhibitors |
| AU1474801A (en) | 1999-11-10 | 2001-06-06 | Smithkline Beecham Corporation | Protease inhibitors |
| EP1232154A4 (en) | 1999-11-10 | 2004-06-23 | Smithkline Beecham Corp | PROTEASE INHIBITORS |
| EP1233950B1 (en) | 1999-11-23 | 2005-10-05 | Smithkline Beecham Corporation | 3,4-DIHYDRO-(1H)QUINAZOLIN-2-ONE COMPOUNDS AS CSBP/P39 kINASE INHIBITORS |
| JP2003514900A (ja) | 1999-11-23 | 2003-04-22 | スミスクライン・ビーチャム・コーポレイション | CSBP/p38キナーゼ阻害剤としての3,4−ジヒドロ−(1H)−キナゾリン−2−オン化合物 |
| KR20020062312A (ko) * | 1999-12-03 | 2002-07-25 | 오노 야꾸힝 고교 가부시키가이샤 | 1,3,4-옥사디아졸린 유도체 및 이들을 유효 성분으로하는 약제 |
| US6797720B2 (en) | 1999-12-03 | 2004-09-28 | Ono Pharmaceutical Co., Ltd. | 1,3,4-oxadiazoline derivative and an agent comprising its derivative as active ingredient |
| US7235551B2 (en) | 2000-03-02 | 2007-06-26 | Smithkline Beecham Corporation | 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases |
| AU4344101A (en) | 2000-03-21 | 2001-10-03 | Smithkline Beecham Corp | Protease inhibitors |
| EP1465862A1 (en) | 2002-01-17 | 2004-10-13 | SmithKline Beecham Corporation | Cycloalkyl ketoamides derivatives useful as cathepsin k inhibitors |
| AU2002333956A1 (en) * | 2002-07-04 | 2004-02-02 | Aventis Pharma S.A. | Novel thiophene acyl hydrazino derivatives, method for preparing same, use thereof as medicines, pharmaceutical compositions and novel use |
| KR100962972B1 (ko) | 2002-07-26 | 2010-06-09 | 주식회사유한양행 | 1-페닐피페리딘-3-온 유도체 및 그의 제조방법 |
| WO2011015524A2 (en) * | 2009-08-03 | 2011-02-10 | Bayer Cropscience Ag | Fungicide heterocycles derivatives |
| JP6243908B2 (ja) * | 2012-08-23 | 2017-12-06 | アリオス バイオファーマ インク. | パラミクソウイルス感染症を治療するための化合物 |
| HK1225716A1 (zh) | 2013-08-21 | 2017-09-15 | Alios Biopharma, Inc. | 抗病毒化合物 |
| MA41614A (fr) | 2015-02-25 | 2018-01-02 | Alios Biopharma Inc | Composés antiviraux |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SK56798A3 (en) * | 1995-10-30 | 1998-12-02 | Smithkline Beecham Corp | Protease inhibitors, pharmaceutical composition containing them and their use |
-
1998
- 1998-04-24 MA MA25047A patent/MA26487A1/fr unknown
- 1998-04-27 PE PE1998000320A patent/PE69099A1/es not_active Application Discontinuation
- 1998-04-28 ZA ZA983522A patent/ZA983522B/xx unknown
- 1998-04-29 HU HU0001294A patent/HUP0001294A3/hu unknown
- 1998-04-29 IL IL13262998A patent/IL132629A0/xx unknown
- 1998-04-29 CO CO98023491A patent/CO4940477A1/es unknown
- 1998-04-29 WO PCT/US1998/008740 patent/WO1998048799A1/en not_active Ceased
- 1998-04-29 CA CA002287989A patent/CA2287989A1/en not_active Abandoned
- 1998-04-29 KR KR1019997010013A patent/KR20010020391A/ko not_active Withdrawn
- 1998-04-29 BR BR9809333-9A patent/BR9809333A/pt not_active IP Right Cessation
- 1998-04-29 AU AU73651/98A patent/AU7365198A/en not_active Abandoned
- 1998-04-29 PL PL98337725A patent/PL337725A1/xx unknown
- 1998-04-29 JP JP54738998A patent/JP2002504097A/ja active Pending
- 1998-04-29 EP EP98920926A patent/EP1019046A4/en not_active Withdrawn
- 1998-04-29 CN CN98806641A patent/CN1261276A/zh active Pending
- 1998-04-29 AR ARP980101999A patent/AR012622A1/es unknown
- 1998-04-29 TR TR1999/02703T patent/TR199902703T2/xx unknown
-
1999
- 1999-10-28 NO NO995268A patent/NO995268L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| EP1019046A4 (en) | 2002-11-27 |
| JP2002504097A (ja) | 2002-02-05 |
| AU7365198A (en) | 1998-11-24 |
| CA2287989A1 (en) | 1998-11-05 |
| PE69099A1 (es) | 1999-09-26 |
| WO1998048799A1 (en) | 1998-11-05 |
| ZA983522B (en) | 1998-10-29 |
| NO995268L (no) | 1999-11-15 |
| TR199902703T2 (xx) | 2000-02-21 |
| HUP0001294A2 (hu) | 2001-04-28 |
| PL337725A1 (en) | 2000-08-28 |
| MA26487A1 (fr) | 2004-12-20 |
| BR9809333A (pt) | 2000-07-04 |
| IL132629A0 (en) | 2001-03-19 |
| CN1261276A (zh) | 2000-07-26 |
| CO4940477A1 (es) | 2000-07-24 |
| EP1019046A1 (en) | 2000-07-19 |
| KR20010020391A (ko) | 2001-03-15 |
| HUP0001294A3 (en) | 2001-06-28 |
| NO995268D0 (no) | 1999-10-28 |
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