PE20070078A1 - Compuestos heterociclicos macrociclicos como inhibidores de aspartil proteasa - Google Patents
Compuestos heterociclicos macrociclicos como inhibidores de aspartil proteasaInfo
- Publication number
- PE20070078A1 PE20070078A1 PE2006000654A PE2006000654A PE20070078A1 PE 20070078 A1 PE20070078 A1 PE 20070078A1 PE 2006000654 A PE2006000654 A PE 2006000654A PE 2006000654 A PE2006000654 A PE 2006000654A PE 20070078 A1 PE20070078 A1 PE 20070078A1
- Authority
- PE
- Peru
- Prior art keywords
- aspartile
- macrociclic
- protease inhibitors
- heterocyclic compounds
- alkenyl
- Prior art date
Links
Classifications
-
- 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
- C07D487/08—Bridged systems
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
-
- 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
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (AREA)
- Virology (AREA)
- Hospice & Palliative Care (AREA)
- AIDS & HIV (AREA)
- Molecular Biology (AREA)
- Psychiatry (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
REFERIDA A UN COMPUESTO DE FORMULA (I), DONDE W ES UN ENLACE, -C(=S)(C(R3)(R4))a-, -(C(R3)(R4))aC(=S)-,ENTRE OTROS; U ES UN ENLACE, -S(O)1-2-, O, ENTRE OTROS; b ES UN ENTERO DE 0 A 2; R1 Y R5 SON H, ALQUILO, ALQUENILO, ENTRE OTROS; R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 Y R18 SON H, ALQUILO, ALQUENILO, ENTRE OTROS; c, d, e, f, g Y h SON UN ENTERO DE 0 A 4; X, Y y Z SON O, N(R5),C(O), ENTRE OTROS; L Y M SON CICLOALQUILENO, HETEROCICLOALQUILENO, ALQUENILENO, ENTRE OTROS; s Y t SON 1 O 2. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE ASPARTIL PROTEASA Y SON UTILES PARA EL TRATAMIENTO DE ENFERMEDADES CARDIOVASCULARES, ENFERMEDADES COGNITIVAS, ENTRE OTRAS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US69054205P | 2005-06-14 | 2005-06-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20070078A1 true PE20070078A1 (es) | 2007-03-08 |
Family
ID=37309231
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2006000654A PE20070078A1 (es) | 2005-06-14 | 2006-06-12 | Compuestos heterociclicos macrociclicos como inhibidores de aspartil proteasa |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US7812013B2 (es) |
| EP (1) | EP1902057B1 (es) |
| JP (1) | JP2008543841A (es) |
| CN (1) | CN101193892A (es) |
| AR (1) | AR053902A1 (es) |
| CA (1) | CA2609562A1 (es) |
| MX (1) | MX2007016185A (es) |
| PE (1) | PE20070078A1 (es) |
| TW (1) | TW200716645A (es) |
| WO (1) | WO2006138195A1 (es) |
Families Citing this family (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| JP2008516945A (ja) * | 2004-10-15 | 2008-05-22 | アストラゼネカ・アクチエボラーグ | 置換されたアミノ化合物およびそれらの使用 |
| CN101084198A (zh) * | 2004-10-15 | 2007-12-05 | 阿斯利康(瑞典)有限公司 | 取代的氨基-嘧啶酮及其用途 |
| JP2008523139A (ja) * | 2004-12-14 | 2008-07-03 | アストラゼネカ・アクチエボラーグ | 置換アミノピリジン類及びその使用 |
| EP1896032B1 (en) * | 2005-06-14 | 2012-10-31 | Merck Sharp & Dohme Corp. | The preparation and use of compounds as protease inhibitors |
| AR053902A1 (es) * | 2005-06-14 | 2007-05-23 | Schering Corp | Inhibidores de aspartil proteasa heterociclicos macrociclicos |
| AR054620A1 (es) * | 2005-06-14 | 2007-07-04 | Schering Corp | Inhibidores de aspartil proteasas |
| EP1896478B1 (en) | 2005-06-14 | 2014-05-21 | Merck Sharp & Dohme Corp. | Aspartyl protease inhibitors |
| WO2007058581A1 (en) * | 2005-11-15 | 2007-05-24 | Astrazeneca Ab | Novel 2-aminopyrimidine derivatives and their use |
| US20080318985A1 (en) * | 2005-11-15 | 2008-12-25 | Astrazeneca Ab | Novel 2-Aminopyrimidinone Or 2-Aminopyridinone Derivatives and Their Use |
| TW200804290A (en) * | 2005-11-15 | 2008-01-16 | Astrazeneca Ab | Compounds and uses thereof |
| EP1951680A4 (en) * | 2005-11-15 | 2011-08-10 | Astrazeneca Ab | NOVEL 2-AMINOPYRIMIDINONE DERIVATIVES AND THEIR USE |
| WO2007058601A1 (en) * | 2005-11-21 | 2007-05-24 | Astrazeneca Ab | Novel 2-amino-imidazole-4-one compounds and their use in the manufacture of a medicament to be used in the treatment of cognitive impairment, alzheimer’s disease, neurodegeneration and dementia |
| TW200734311A (en) * | 2005-11-21 | 2007-09-16 | Astrazeneca Ab | New compounds |
| AR058381A1 (es) * | 2005-12-19 | 2008-01-30 | Astrazeneca Ab | Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica |
| US20090099217A1 (en) * | 2006-04-05 | 2009-04-16 | Astex Therapeutics Ltd. | 2-Aminopyrimidin-4-Ones And Their Use For Treating Or Preventing Alpha Beta-Related Pathologies |
| AU2007258435A1 (en) | 2006-06-12 | 2007-12-21 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| TW200815447A (en) * | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds IV |
| US20080051420A1 (en) * | 2006-06-14 | 2008-02-28 | Astrazeneca Ab | New Compounds 317 |
| TW200815349A (en) * | 2006-06-22 | 2008-04-01 | Astrazeneca Ab | New compounds |
| AU2007332754A1 (en) | 2006-12-12 | 2008-06-19 | Schering Corporation | Aspartyl protease inhibitors |
| TW200831484A (en) * | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
| TW200902503A (en) * | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| TW200902499A (en) * | 2007-05-15 | 2009-01-16 | Astrazeneca Ab | New compounds |
| EP2200990A1 (en) | 2007-09-06 | 2010-06-30 | Schering Corporation | Gamma secretase modulators |
| EP2217604A1 (en) | 2007-11-05 | 2010-08-18 | Schering Corporation | Gamma secretase modulators |
| EP2227471A1 (en) | 2007-12-11 | 2010-09-15 | Schering Corporation | Gamma secretase modulators |
| AU2009239536C1 (en) | 2008-04-22 | 2012-12-13 | Merck Sharp & Dohme Corp. | Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use |
| CN102282145A (zh) | 2008-11-13 | 2011-12-14 | 先灵公司 | γ分泌酶调节剂 |
| TW201020244A (en) * | 2008-11-14 | 2010-06-01 | Astrazeneca Ab | New compounds |
| US20100125081A1 (en) * | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | New compounds 574 |
| US20100125087A1 (en) * | 2008-11-14 | 2010-05-20 | Astrazeneca Ab | New compounds 575 |
| EP2379563B1 (en) | 2008-12-22 | 2014-07-16 | Merck Sharp & Dohme Corp. | Gamma secretase modulators |
| CA2747750A1 (en) | 2008-12-22 | 2010-07-01 | Theodros Asberom | Gamma secretase modulators |
| WO2010147969A2 (en) | 2009-06-16 | 2010-12-23 | Schering Corporation | Gamma secretase modulators |
| EP2443119A1 (en) | 2009-06-16 | 2012-04-25 | Schering Corporation | Gamma secretase modulators |
| WO2010147973A1 (en) | 2009-06-16 | 2010-12-23 | Schering Corporation | Gamma secretase modulators |
| US8563543B2 (en) | 2009-10-08 | 2013-10-22 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| WO2011044185A2 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| WO2011044184A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| PH12013501368A1 (en) | 2011-02-08 | 2013-08-28 | Merck Patent Gmbh | Aminostatin derivatives for the treatment of arthrosis |
| WO2012138590A1 (en) | 2011-04-07 | 2012-10-11 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| US9221839B2 (en) | 2011-04-07 | 2015-12-29 | Merck Sharp & Dohme Corp. | C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
| RU2014111055A (ru) | 2011-08-22 | 2015-09-27 | Мерк Шарп И Доум Корп. | 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение |
| CA2867891C (en) | 2012-03-19 | 2021-09-14 | Buck Institute For Research On Aging | App specific bace inhibitors (asbis) and uses thereof |
| US9624264B2 (en) | 2012-07-24 | 2017-04-18 | Merck Patent Gmbh | Hydroxystatin derivatives for the treatment of arthrosis |
| WO2014062553A1 (en) | 2012-10-17 | 2014-04-24 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| WO2014062549A1 (en) | 2012-10-17 | 2014-04-24 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| ES2769578T3 (es) | 2013-02-12 | 2020-06-26 | Buck Inst Res Aging | Hidantoínas que modulan el procesamiento de APP mediado por BACE |
| JP6321685B2 (ja) | 2013-02-25 | 2018-05-09 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung | 2−アミノ−3,4−ジヒドロ−キナゾリン誘導体、およびそのカテプシンd阻害剤としての使用 |
| ES2759060T3 (es) | 2013-08-06 | 2020-05-07 | Merck Patent Gmbh | Administración intraarticular de pepstatina para la artrosis |
| EP3416647A4 (en) | 2016-02-18 | 2019-10-23 | Merck Sharp & Dohme Corp. | N3-SUBSTITUTED IMINOPYRIMIDINONE AS ANTIMALARIAMIDAL |
| US10958463B1 (en) * | 2018-03-26 | 2021-03-23 | Lynq Technologies, Inc. | Pairing multiple devices into a designated group for a communication session |
| EP4076659A1 (en) * | 2019-12-19 | 2022-10-26 | Latvian Institute Of Organic Synthesis | Macrocyclic amides acting as plasmepsin inhbitors for the treatment of malaria |
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| US3200123A (en) * | 1962-01-26 | 1965-08-10 | Richardson Merreil Inc | Imidazoquinolines |
| US3197476A (en) * | 1962-12-06 | 1965-07-27 | Air Prod & Chem | Method of synthesis of 1-acyl imidazoles |
| DE69016430T2 (de) | 1989-06-09 | 1995-06-01 | Upjohn Co | Heterozyklische amine mit zns-wirksamkeit. |
| FR2719843B1 (fr) | 1994-05-10 | 1996-06-07 | Synthelabo | Dérivés de 5,6-dihydro-4h-imidazo [2',1':2,3] imidazo-[4,5,1-ij] quinoléine et de 4,5-dihydroimidazo [1,2-a] pyrrolo-[1,2,3-cd] benzimidazole, leur préparation et leur application en thérapeutique. |
| IL117149A0 (en) * | 1995-02-23 | 1996-06-18 | Schering Corp | Muscarinic antagonists |
| US5889006A (en) * | 1995-02-23 | 1999-03-30 | Schering Corporation | Muscarinic antagonists |
| FR2741072B1 (fr) | 1995-11-09 | 1997-12-12 | Synthelabo | Derives d'oxazolidin-2-one, leur preparation et leur application en therapeutique |
| FR2741073B1 (fr) | 1995-11-09 | 1997-12-12 | Synthelabo | Derives de 4,5-dihydroimidazo(1,2-a)pyrrolo(1,2,3-cd) benzimidazole, leur preparation et leur application en therapeutique |
| BR9707086A (pt) * | 1996-01-26 | 1999-04-13 | Clarence Webster Andrews, Iii. | Inibidores de proteinase aspartila |
| FR2747678B1 (fr) | 1996-04-22 | 1998-05-22 | Synthelabo | Composes derives d'imidazobenzoxazine, leurs procedes de preparation et leurs utilisations en therapeutique |
| US5935958A (en) * | 1996-07-01 | 1999-08-10 | Schering Corporation | Muscarinic antagonists |
| US5952349A (en) * | 1996-07-10 | 1999-09-14 | Schering Corporation | Muscarinic antagonists for treating memory loss |
| US5977138A (en) * | 1996-08-15 | 1999-11-02 | Schering Corporation | Ether muscarinic antagonists |
| US6066636A (en) * | 1998-06-30 | 2000-05-23 | Schering Corporation | Muscarinic antagonists |
| ECSP003637A (es) | 1999-08-31 | 2002-03-25 | Agouron Pharma | Inhibidores triciclicos de poli (adp-ribosa) polimerasas |
| US6294554B1 (en) * | 1999-09-22 | 2001-09-25 | Schering Corporation | Muscarinic antagonists |
| JP4012068B2 (ja) * | 2000-12-22 | 2007-11-21 | シェーリング コーポレイション | ムスカリンアンタゴニスト |
| AU2002306734A1 (en) | 2001-03-15 | 2002-10-03 | The Johns Hopkins University | Inhibitors of plasmepsins |
| US6706885B2 (en) | 2001-06-06 | 2004-03-16 | Merck & Co., Inc. | Process for preparing integrin antagonist intermediates |
| CN1301972C (zh) | 2001-10-10 | 2007-02-28 | 先灵公司 | 作为毒覃碱拮抗剂的哌啶化合物 |
| GB0315654D0 (en) * | 2003-07-03 | 2003-08-13 | Novartis Ag | Organic compounds |
| GB0323204D0 (en) * | 2003-10-03 | 2003-11-05 | Novartis Ag | Organic compounds |
| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| CA2548388A1 (en) | 2003-12-15 | 2005-06-30 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| WO2006022698A1 (en) * | 2004-08-10 | 2006-03-02 | Thomson Licensing | Method and apparatus for controlling a display function |
| TWI370820B (en) | 2005-04-27 | 2012-08-21 | Takeda Pharmaceutical | Fused heterocyclic compounds |
| AR053902A1 (es) | 2005-06-14 | 2007-05-23 | Schering Corp | Inhibidores de aspartil proteasa heterociclicos macrociclicos |
| WO2007092839A2 (en) | 2006-02-06 | 2007-08-16 | Janssen Pharmaceutica N.V. | Macrocycle derivatives useful as inhibitors of beta-secretase (bace) |
-
2006
- 2006-06-12 AR ARP060102460A patent/AR053902A1/es not_active Application Discontinuation
- 2006-06-12 CA CA002609562A patent/CA2609562A1/en not_active Abandoned
- 2006-06-12 MX MX2007016185A patent/MX2007016185A/es active IP Right Grant
- 2006-06-12 PE PE2006000654A patent/PE20070078A1/es not_active Application Discontinuation
- 2006-06-12 CN CNA2006800209345A patent/CN101193892A/zh active Pending
- 2006-06-12 JP JP2008516964A patent/JP2008543841A/ja not_active Ceased
- 2006-06-12 US US11/451,064 patent/US7812013B2/en active Active
- 2006-06-12 EP EP06772846.9A patent/EP1902057B1/en active Active
- 2006-06-12 WO PCT/US2006/022701 patent/WO2006138195A1/en not_active Ceased
- 2006-06-13 TW TW095121027A patent/TW200716645A/zh unknown
-
2009
- 2009-11-17 US US12/620,291 patent/US8557798B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| JP2008543841A (ja) | 2008-12-04 |
| EP1902057A1 (en) | 2008-03-26 |
| EP1902057B1 (en) | 2013-10-23 |
| CN101193892A (zh) | 2008-06-04 |
| TW200716645A (en) | 2007-05-01 |
| US20060281729A1 (en) | 2006-12-14 |
| US8557798B2 (en) | 2013-10-15 |
| MX2007016185A (es) | 2008-03-07 |
| AR053902A1 (es) | 2007-05-23 |
| WO2006138195A1 (en) | 2006-12-28 |
| US20100063121A1 (en) | 2010-03-11 |
| CA2609562A1 (en) | 2006-12-28 |
| US7812013B2 (en) | 2010-10-12 |
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Legal Events
| Date | Code | Title | Description |
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| FC | Refusal |