MX2009006228A - Inhibidores de aspartil proteasa. - Google Patents
Inhibidores de aspartil proteasa.Info
- Publication number
- MX2009006228A MX2009006228A MX2009006228A MX2009006228A MX2009006228A MX 2009006228 A MX2009006228 A MX 2009006228A MX 2009006228 A MX2009006228 A MX 2009006228A MX 2009006228 A MX2009006228 A MX 2009006228A MX 2009006228 A MX2009006228 A MX 2009006228A
- Authority
- MX
- Mexico
- Prior art keywords
- sup
- formula
- disclosed
- aspartyl protease
- protease inhibitors
- Prior art date
Links
- 239000003696 aspartic proteinase inhibitor Substances 0.000 title 1
- 208000010877 cognitive disease Diseases 0.000 abstract 2
- 230000001149 cognitive effect Effects 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 230000004770 neurodegeneration Effects 0.000 abstract 2
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 2
- 102000004580 Aspartic Acid Proteases Human genes 0.000 abstract 1
- 108010017640 Aspartic Acid Proteases Proteins 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 229940122041 Cholinesterase inhibitor Drugs 0.000 abstract 1
- 239000000544 cholinesterase inhibitor Substances 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000000359 muscarinic M1 receptor agonist Substances 0.000 abstract 1
- 239000003683 muscarinic M2 receptor antagonist Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
Classifications
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/14—Ortho-condensed systems
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
-
- 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
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/06—Antimalarials
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic 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
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Neurology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Virology (AREA)
- Neurosurgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- AIDS & HIV (AREA)
- Molecular Biology (AREA)
- Psychiatry (AREA)
- Ophthalmology & Optometry (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Enzymes And Modification Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se describen compuestos de la fórmula I: (ver fórmula (I)) o un estereoisómero, tautómero, o un solvato o una sal aceptable farmacéuticamente de dichos compuestos, donde: R1, R2, R3, R4, R14, V, W, X, Y, Z, p y el anillo A se definen conforme a lo descrito en la especificación; además se describen el método para la inhibición de aspartil proteasa, y en particular, los métodos de tratamiento de enfermedades cardiovasculares, enfermedades cognitivas y neurodegenerativas; asimismo, se describen métodos para el tratamiento de enfermedades cognitivas o neurodegenerativas usando los compuestos de la fórmula I en combinación con un inhibidor de colinesterasa o un antagonista m2, o agonista m1 muscarínico.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87441906P | 2006-12-12 | 2006-12-12 | |
| PCT/US2007/025220 WO2008073365A1 (en) | 2006-12-12 | 2007-12-10 | Aspartyl protease inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2009006228A true MX2009006228A (es) | 2009-06-22 |
Family
ID=39356038
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2009006228A MX2009006228A (es) | 2006-12-12 | 2007-12-10 | Inhibidores de aspartil proteasa. |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8093254B2 (es) |
| EP (1) | EP2064191B1 (es) |
| JP (1) | JP2010512389A (es) |
| KR (1) | KR20090087487A (es) |
| CN (1) | CN101668751A (es) |
| AR (1) | AR064287A1 (es) |
| AU (1) | AU2007332754A1 (es) |
| CA (1) | CA2672293A1 (es) |
| MX (1) | MX2009006228A (es) |
| TW (1) | TW200831512A (es) |
| WO (1) | WO2008073365A1 (es) |
Families Citing this family (40)
| 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 |
| AU2006259675A1 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Aspartyl protease inhibitors |
| WO2006138265A2 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Heterocyclic aspartyl protease inhibitors, preparation and use thereof |
| PE20070135A1 (es) * | 2005-06-14 | 2007-03-09 | Schering Corp | Compuestos heterociclicos como inhibidores de aspartil proteasas |
| CA2628074C (en) | 2005-10-25 | 2014-01-14 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
| PE20080155A1 (es) | 2006-06-12 | 2008-03-10 | Schering Corp | Compuestos heterociclicos como inhibidores de aspartil-proteasa |
| JP5383484B2 (ja) | 2007-04-24 | 2014-01-08 | 塩野義製薬株式会社 | 環式基で置換されたアミノジヒドロチアジン誘導体 |
| US8653067B2 (en) | 2007-04-24 | 2014-02-18 | Shionogi & Co., Ltd. | Pharmaceutical composition for treating Alzheimer's disease |
| MX2010005028A (es) | 2007-11-05 | 2010-05-27 | Schering Corp | Moduladores de gamma secretasa. |
| KR101324426B1 (ko) | 2008-06-13 | 2013-10-31 | 시오노기세야쿠 가부시키가이샤 | β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체 |
| CN102186841A (zh) | 2008-10-22 | 2011-09-14 | 盐野义制药株式会社 | 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物 |
| GB0912777D0 (en) * | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
| GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
| EP2485590B1 (en) | 2009-10-08 | 2015-01-07 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
| WO2011044187A1 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| EP2485920B1 (en) | 2009-10-08 | 2016-04-27 | Merck Sharp & Dohme Corp. | 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 | |
| JPWO2011071109A1 (ja) * | 2009-12-11 | 2013-04-22 | 塩野義製薬株式会社 | アミノ基を有する縮合ヘテロ環化合物 |
| MX2012006491A (es) | 2009-12-11 | 2012-07-03 | Shionogi & Co | Derivados de oxazina. |
| EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
| JP5816630B2 (ja) | 2010-10-29 | 2015-11-18 | 塩野義製薬株式会社 | ナフチリジン誘導体 |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| ES2624288T3 (es) | 2011-01-21 | 2017-07-13 | Eisai R&D Management Co., Ltd. | Métodos y compuestos útiles en la síntesis de derivados de aminodihidrotiazina condensados |
| GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| EP2694489B1 (en) | 2011-04-07 | 2017-09-06 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| EP2694521B1 (en) | 2011-04-07 | 2015-11-25 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| US8883779B2 (en) | 2011-04-26 | 2014-11-11 | Shinogi & Co., Ltd. | Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them |
| CN103874496A (zh) | 2011-08-22 | 2014-06-18 | 默沙东公司 | 作为bace抑制剂的2-螺-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其用途 |
| CN104270945B (zh) | 2012-03-19 | 2017-03-29 | 巴克老龄化研究所 | App特异性bace抑制剂(asbi)及其用途 |
| US9422277B2 (en) | 2012-10-17 | 2016-08-23 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use |
| EP2908824B1 (en) | 2012-10-17 | 2018-05-02 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| US9303035B2 (en) | 2012-12-19 | 2016-04-05 | Novartis Ag | Substituted pyrazino[1′,2′:1,2]pyrrolo[3,4-d]pyrimidines, pyrimido[4′,5′:3,4]pyrrolo[2,1-c][1,4]oxazines and pyrimido[4′,5′:3,4]pyrrolo[1,2-d][1,4]oxazepines for inhibiting the CFTR channel |
| PE20151055A1 (es) | 2012-12-19 | 2015-08-05 | Novartis Ag | Compuestos triciclicos para inhibir el canal cftr |
| CA2899938C (en) | 2013-02-12 | 2021-10-19 | Buck Institute For Research On Aging | Hydantoins that modulate bace-mediated app processing |
| CN104761557B (zh) * | 2015-04-08 | 2017-02-22 | 河南师范大学 | 六氢‑1H‑吡咯并[3,4‑d]嘧啶类化合物及其制备方法 |
| CN108299169B (zh) * | 2018-02-02 | 2021-04-30 | 南京杰运医药科技有限公司 | 6-氯-3,4-二氢-2h-1-萘酮的合成方法 |
Family Cites Families (88)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US1077204A (en) | 1912-11-20 | 1913-10-28 | John Bonner Semple | Tracer for projectiles. |
| ZA87563B (en) | 1986-02-03 | 1987-09-30 | Squibb & Sons Inc | N-heterocyclic alcohol renin inhibitors |
| DE3643890A1 (de) | 1986-12-22 | 1988-06-30 | Basf Ag | Neue polyalkylpiperidinderivate mit alkylenbruecken, ihre verwendung als stabilisator und zwischenprodukte |
| JPH03500772A (ja) | 1987-10-21 | 1991-02-21 | ジ・アップジョン・カンパニー | (1‐アミノ‐2‐ヒドロキシ‐2‐ヘテロサイクリック)エチル基を含有するレニン抑制物質類 |
| EP0361341A3 (en) | 1988-09-28 | 1991-07-03 | Miles Inc. | Therapeutics for aids based on inhibitors of hiv protease |
| IL92011A0 (en) | 1988-10-19 | 1990-07-12 | Abbott Lab | Heterocyclic peptide renin inhibitors |
| US5534520A (en) | 1990-04-10 | 1996-07-09 | Fisher; Abraham | Spiro compounds containing five-membered rings |
| US5852029A (en) | 1990-04-10 | 1998-12-22 | Israel Institute For Biological Research | Aza spiro compounds acting on the cholinergic system with muscarinic agonist activity |
| AU2436792A (en) | 1991-08-16 | 1993-03-16 | Merck & Co., Inc. | Quinazoline derivatives as inhibitors of hiv reverse transcriptase |
| WO1993013064A1 (fr) | 1991-12-26 | 1993-07-08 | Nippon Soda Co., Ltd. | Procede de production d'un derive d'azetidinone substitue en position 4 |
| US5731431A (en) | 1991-12-26 | 1998-03-24 | Nippon Soda Co., Ltd. | Process for preparing 4-substituted azetidinone derivatives |
| US5536727A (en) | 1992-05-20 | 1996-07-16 | Merck & Co., Inc. | 17-Ethers and thioethers of 4-aza-steroids |
| JPH07508039A (ja) | 1992-05-20 | 1995-09-07 | メルク エンド カンパニー インコーポレーテッド | 4−アザステロイドのエステル誘導体 |
| DE4233715A1 (de) | 1992-10-07 | 1994-04-14 | Bayer Ag | Substituierte Carbamoylpyrazoline |
| US5338740A (en) | 1993-07-13 | 1994-08-16 | Pfizer Inc. | Angiotensin II receptor antagonists |
| US5502222A (en) | 1994-06-01 | 1996-03-26 | Schering Corporation | Process for preparing delta 9,11 and 21-chloro corticosteroids |
| US5889006A (en) | 1995-02-23 | 1999-03-30 | Schering Corporation | Muscarinic antagonists |
| IL117149A0 (en) | 1995-02-23 | 1996-06-18 | Schering Corp | Muscarinic antagonists |
| FR2741342B1 (fr) | 1995-11-22 | 1998-02-06 | Roussel Uclaf | Nouvelles phenylimidazolidines fluorees ou hydroxylees, procede, intermediaires de preparation, application comme medicaments, nouvelle utilisation et compositions pharmaceutiques |
| GB9611046D0 (en) | 1996-05-25 | 1996-07-31 | Wivenhoe Techn Ltd | Pharmacological compounds |
| 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 |
| GB9615831D0 (en) | 1996-07-27 | 1996-09-11 | Agrevo Uk Ltd | Fungicides |
| US5977138A (en) | 1996-08-15 | 1999-11-02 | Schering Corporation | Ether muscarinic antagonists |
| US5981556A (en) | 1997-07-22 | 1999-11-09 | G.D. Searle & Co. | 1,3-diazolino and 1,3-diazolidino heterocycles as useful nitric oxide synthase inhibitors |
| JPH11335518A (ja) | 1998-03-25 | 1999-12-07 | Polyplastics Co | ポリアセタ―ル樹脂組成物およびその製造方法 |
| US6066636A (en) | 1998-06-30 | 2000-05-23 | Schering Corporation | Muscarinic antagonists |
| US6638937B2 (en) | 1998-07-06 | 2003-10-28 | Bristol-Myers Squibb Co. | Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists |
| US6492408B1 (en) | 1999-07-21 | 2002-12-10 | Boehringer Ingelheim Pharmaceuticals, Inc. | Small molecules useful in the treatment of inflammatory disease |
| US6294554B1 (en) | 1999-09-22 | 2001-09-25 | Schering Corporation | Muscarinic antagonists |
| ATE339417T1 (de) | 1999-12-15 | 2006-10-15 | Bristol Myers Squibb Co | Biphenyl - sulfonamide als duale angiotensin - endothelin - rezeptor - antagonisten |
| JP3927748B2 (ja) | 2000-01-19 | 2007-06-13 | ユニ・チャーム株式会社 | 繊維シートのヒートシール方法およびヒートシール装置 |
| US6713276B2 (en) | 2000-06-28 | 2004-03-30 | Scios, Inc. | Modulation of Aβ levels by β-secretase BACE2 |
| JP2004502664A (ja) | 2000-06-30 | 2004-01-29 | イーラン ファーマスーティカルズ、インコーポレイテッド | アルツハイマー病処置用化合物 |
| PE20020276A1 (es) | 2000-06-30 | 2002-04-06 | Elan Pharm Inc | COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER |
| US6846813B2 (en) | 2000-06-30 | 2005-01-25 | Pharmacia & Upjohn Company | Compounds to treat alzheimer's disease |
| US6344473B1 (en) | 2000-08-07 | 2002-02-05 | G.D. Searle & Co. | Imidazoles useful as nitric oxide synthase inhibitors |
| WO2002012243A2 (en) | 2000-08-09 | 2002-02-14 | Boehringer Ingelheim Pharmaceuticals, Inc. | SYNTHESIS OF (R)-3-(4-BROMOBENZYL)-1-(3,5-DICHLOROPHENYL)-5-IODO-3-METHYL-1-H-IMIDAZO[1,2-a]IMIDAZOL-2-ONE |
| ATE439344T1 (de) | 2000-12-22 | 2009-08-15 | Schering Corp | Muscarin-antagonisten |
| WO2002074719A2 (en) | 2001-03-15 | 2002-09-26 | The Johns Hopkins University | Inhibitors of plasmepsins |
| EP1389194A2 (en) | 2001-04-27 | 2004-02-18 | Vertex Pharmaceuticals Incorporated | Inhibitors of bace |
| JP2005506339A (ja) | 2001-10-10 | 2005-03-03 | シェーリング コーポレイション | ムスカリン性アンタゴニストとしてのピペリジン化合物 |
| US6673821B2 (en) | 2001-10-22 | 2004-01-06 | Enanta Pharmaceuticals, Inc. | Nitrogen heterocycle inhibitors of aspartyl protease |
| WO2003106405A1 (en) | 2002-06-01 | 2003-12-24 | Sunesis Pharmaceuticals, Inc. | Aspartyl protease inhibitors |
| WO2004058727A1 (en) | 2002-12-20 | 2004-07-15 | Bayer Pharmaceuticals Corporation | Substituted 3,5-dihydro-4h-imidazol-4-ones for the treatment of obesity |
| US7354933B2 (en) | 2003-01-31 | 2008-04-08 | Aventis Pharma Sa | Cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors |
| FR2850652B1 (fr) | 2003-01-31 | 2008-05-30 | Aventis Pharma Sa | Nouveaux derives d'uree cyclique, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases |
| DE10336035A1 (de) | 2003-08-01 | 2005-03-24 | Endress + Hauser Wetzer Gmbh + Co Kg | Verfahren zur automatischen Anpassung eines busfähigen Feldgerätes der Prozessautomatisierungstechnik an das auf dem Feldbus verwendete Busprotokoll |
| WO2005016876A2 (en) | 2003-08-08 | 2005-02-24 | Schering Corporation | Cyclic amine bace-1 inhibitors having a benzamide substituent |
| AR045219A1 (es) | 2003-08-08 | 2005-10-19 | Pharmacopeia Inc | Aminas ciclicas inhibidoras de base - 1 que poseen un sustiuyente heterociclico |
| US20050171112A1 (en) | 2003-11-03 | 2005-08-04 | Probiodrug Ag | Combinations useful for the treatment of neuronal disorders |
| US20060034848A1 (en) | 2003-11-07 | 2006-02-16 | Ayae Kinoshita | Methods and compositions for treating Alzheimer's disease |
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| EP2335701B1 (en) | 2003-12-15 | 2012-07-11 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| JP2007530696A (ja) | 2004-03-30 | 2007-11-01 | メルク エンド カムパニー インコーポレーテッド | アスパラギン酸プロテアーゼ阻害剤として有用な2−アミノチアゾール化合物 |
| CA2563639A1 (en) | 2004-04-20 | 2005-11-03 | Merck & Co., Inc. | 2, 4, 6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease |
| JP2007533743A (ja) | 2004-04-20 | 2007-11-22 | メルク エンド カムパニー インコーポレーテッド | アルツハイマー病治療のためのβ−セクレターゼ阻害薬として有用な1,3,5−置換フェニル誘導体化合物 |
| US7618978B2 (en) | 2004-04-22 | 2009-11-17 | Eli Lilly And Company | Amides as BACE inhibitors |
| EP1756040A4 (en) | 2004-05-13 | 2008-04-30 | Merck & Co Inc | ALS-SEKRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER DISEASE, PHENYL ACETIC ACID AMID COMPOUNDS SUITABLE |
| US7714021B2 (en) | 2004-06-15 | 2010-05-11 | Merck & Co., Inc. | Pyrrolidin-3-yl compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease |
| BRPI0512213A (pt) | 2004-06-16 | 2008-02-19 | Wyeth Corp | método para tratamento, prevenção ou melhora de uma doença ou distúrbio; composição farmacêutica; processo para a preparação de um composto; e uso de um composto |
| RU2006144075A (ru) | 2004-06-16 | 2008-07-27 | Вайет (Us) | ДИФЕНИЛИМИДАЗОПИРИМИДИН И -ИМИДАЗОЛАМИНЫ КАК ИНГИБИТОРЫ β-СЕКРЕТАЗЫ |
| CA2574218A1 (en) | 2004-07-22 | 2006-02-09 | Schering Corporation | Substituted amide beta secretase inhibitors |
| CA2575340A1 (en) | 2004-07-28 | 2006-02-09 | Schering Corporation | Macrocyclic beta-secretase inhibitors |
| EP1776350B1 (en) | 2004-08-06 | 2013-01-23 | Janssen Pharmaceutica NV | NOVEL 2-AMINO-QUINAZOLINE DERIVATIVES USEFUL AS INHIBITORS OF ß-SECRETASE ( BACE ) |
| US8436006B2 (en) | 2004-08-06 | 2013-05-07 | Jansssen Pharmaceutica N.V. | 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) |
| DE602005023887D1 (de) | 2004-08-06 | 2010-11-11 | Janssen Pharmaceutica Nv | Als b-sekretase (bace)-hemmer nützliche 2-amino-chinazolinderivate |
| US8114887B2 (en) | 2004-10-13 | 2012-02-14 | Merck, Sharp & Dohme Corp. | Spiropiperidine compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease |
| WO2006044492A2 (en) | 2004-10-14 | 2006-04-27 | Ingenious Targeting Laboratory, Inc. | Methods for generating rat embryo-derived cell lines and genetic modification of rat genome |
| 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 |
| EP1802588A4 (en) | 2004-10-15 | 2010-02-17 | Astrazeneca Ab | SUBSTITUTED AMINOPYRIMIDONE AND APPLICATIONS THEREOF |
| CA2593515A1 (en) | 2005-01-14 | 2006-07-20 | Wyeth | Amino-imidazolones for the inhibition of beta-secretase |
| AU2006259675A1 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Aspartyl protease inhibitors |
| EP1896406A2 (en) | 2005-06-14 | 2008-03-12 | Shering Corporation | The preparation and use of compounds as protease inhibitors |
| ATE489370T1 (de) | 2005-06-14 | 2010-12-15 | Schering Corp | Herstellung und verwendung von verbindungen als aspartylproteasehemmer |
| KR20080025079A (ko) * | 2005-06-14 | 2008-03-19 | 쉐링 코포레이션 | 아스파르틸 프로테아제 억제제 |
| AR053902A1 (es) | 2005-06-14 | 2007-05-23 | Schering Corp | Inhibidores de aspartil proteasa heterociclicos macrociclicos |
| WO2006138265A2 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Heterocyclic aspartyl protease inhibitors, preparation and use thereof |
| PE20070135A1 (es) * | 2005-06-14 | 2007-03-09 | Schering Corp | Compuestos heterociclicos como inhibidores de aspartil proteasas |
| TW200738683A (en) | 2005-06-30 | 2007-10-16 | Wyeth Corp | Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation |
| AU2006266167A1 (en) | 2005-06-30 | 2007-01-11 | Wyeth | Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for beta-secretase modulation |
| TW200730523A (en) | 2005-07-29 | 2007-08-16 | Wyeth Corp | Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation |
| JP2009509957A (ja) | 2005-09-26 | 2009-03-12 | ワイス | β−セクレターゼ阻害剤としてのアミノ−5−[4−(ジフルオロメトキシ)フェニル]−5−フェニルイミダゾロン化合物 |
| CA2628074C (en) | 2005-10-25 | 2014-01-14 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivative |
| PE20080155A1 (es) | 2006-06-12 | 2008-03-10 | Schering Corp | Compuestos heterociclicos como inhibidores de aspartil-proteasa |
| TW200808796A (en) | 2006-06-14 | 2008-02-16 | Astrazeneca Ab | New compounds III |
-
2007
- 2007-12-10 JP JP2009541321A patent/JP2010512389A/ja not_active Withdrawn
- 2007-12-10 MX MX2009006228A patent/MX2009006228A/es unknown
- 2007-12-10 CA CA002672293A patent/CA2672293A1/en not_active Abandoned
- 2007-12-10 US US12/517,744 patent/US8093254B2/en active Active
- 2007-12-10 CN CN200780051123A patent/CN101668751A/zh active Pending
- 2007-12-10 AU AU2007332754A patent/AU2007332754A1/en not_active Abandoned
- 2007-12-10 EP EP07862708.0A patent/EP2064191B1/en active Active
- 2007-12-10 WO PCT/US2007/025220 patent/WO2008073365A1/en not_active Ceased
- 2007-12-10 KR KR1020097013474A patent/KR20090087487A/ko not_active Withdrawn
- 2007-12-11 TW TW096147267A patent/TW200831512A/zh unknown
- 2007-12-11 AR ARP070105546A patent/AR064287A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| KR20090087487A (ko) | 2009-08-17 |
| EP2064191A1 (en) | 2009-06-03 |
| US20100069406A1 (en) | 2010-03-18 |
| AR064287A1 (es) | 2009-03-25 |
| EP2064191B1 (en) | 2014-06-25 |
| JP2010512389A (ja) | 2010-04-22 |
| AU2007332754A1 (en) | 2008-06-19 |
| TW200831512A (en) | 2008-08-01 |
| US8093254B2 (en) | 2012-01-10 |
| CN101668751A (zh) | 2010-03-10 |
| WO2008073365A1 (en) | 2008-06-19 |
| CA2672293A1 (en) | 2008-06-19 |
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