ATE428698T1 - Die aktivität von gamma-secretase blockierende malonamidderivate - Google Patents
Die aktivität von gamma-secretase blockierende malonamidderivateInfo
- Publication number
- ATE428698T1 ATE428698T1 AT04764665T AT04764665T ATE428698T1 AT E428698 T1 ATE428698 T1 AT E428698T1 AT 04764665 T AT04764665 T AT 04764665T AT 04764665 T AT04764665 T AT 04764665T AT E428698 T1 ATE428698 T1 AT E428698T1
- Authority
- AT
- Austria
- Prior art keywords
- secretase
- gamma
- activity
- malonamide derivatives
- blocking
- Prior art date
Links
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 title 1
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 title 1
- 230000000903 blocking effect Effects 0.000 title 1
- 230000000694 effects Effects 0.000 title 1
- WRIRWRKPLXCTFD-UHFFFAOYSA-N malonamide Chemical class NC(=O)CC(N)=O WRIRWRKPLXCTFD-UHFFFAOYSA-N 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
- C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D223/16—Benzazepines; Hydrogenated benzazepines
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
-
- 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
- A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
- A61K31/558—Eicosanoids, e.g. leukotrienes or prostaglandins having heterocyclic rings containing oxygen as the only ring hetero atom, e.g. thromboxanes
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
- C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D223/18—Dibenzazepines; Hydrogenated dibenzazepines
- C07D223/20—Dibenz [b, e] azepines; Hydrogenated dibenz [b, e] azepines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
- C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
- C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
- C07D243/24—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D313/00—Heterocyclic compounds containing rings of more than six members having one oxygen atom as the only ring hetero atom
- C07D313/02—Seven-membered rings
- C07D313/06—Seven-membered rings condensed with carbocyclic rings or ring systems
- C07D313/10—Seven-membered rings condensed with carbocyclic rings or ring systems condensed with two six-membered rings
- C07D313/14—[b,f]-condensed
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Pyrane Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP03019683 | 2003-09-09 | ||
| PCT/EP2004/009700 WO2005023772A1 (en) | 2003-09-09 | 2004-08-31 | Malonamide derivatives blocking the activity of gama-secretase |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE428698T1 true ATE428698T1 (de) | 2009-05-15 |
Family
ID=34224068
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT04764665T ATE428698T1 (de) | 2003-09-09 | 2004-08-31 | Die aktivität von gamma-secretase blockierende malonamidderivate |
Country Status (34)
| Country | Link |
|---|---|
| US (1) | US7160875B2 (de) |
| EP (1) | EP1711470B1 (de) |
| JP (2) | JP4571639B2 (de) |
| KR (3) | KR100834177B1 (de) |
| CN (1) | CN100593539C (de) |
| AR (1) | AR045609A1 (de) |
| AT (1) | ATE428698T1 (de) |
| AU (1) | AU2004270361B2 (de) |
| BR (1) | BRPI0413533A (de) |
| CA (1) | CA2537440C (de) |
| CO (1) | CO5660268A2 (de) |
| CR (1) | CR8264A (de) |
| CY (1) | CY1109225T1 (de) |
| DE (1) | DE602004020680D1 (de) |
| DK (1) | DK1711470T3 (de) |
| EA (1) | EA009940B1 (de) |
| EC (1) | ECSP066414A (de) |
| ES (1) | ES2322652T3 (de) |
| HR (1) | HRP20090266T1 (de) |
| IL (1) | IL173905A (de) |
| MA (1) | MA28034A1 (de) |
| MX (1) | MXPA06002562A (de) |
| MY (1) | MY141308A (de) |
| NO (1) | NO20061047L (de) |
| NZ (1) | NZ545538A (de) |
| PL (1) | PL1711470T3 (de) |
| PT (1) | PT1711470E (de) |
| RS (1) | RS20060146A (de) |
| SI (1) | SI1711470T1 (de) |
| TN (1) | TNSN06077A1 (de) |
| TW (1) | TW200519092A (de) |
| UA (1) | UA83501C2 (de) |
| WO (1) | WO2005023772A1 (de) |
| ZA (1) | ZA200601989B (de) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1592684B1 (de) * | 2003-02-04 | 2008-07-30 | F. Hoffmann-La Roche Ag | Malonamidderivate als gamma-secretaseinhibitoren |
| UA83501C2 (uk) * | 2003-09-09 | 2008-07-25 | Ф.Хоффманн-Ля Рош Аг | ПОХІДНІ МАЛОНАМІДУ, ЩО БЛОКУЮТЬ АКТИВНІСТЬ γ-СЕКРЕТАЗИ |
| RU2356895C2 (ru) * | 2003-10-06 | 2009-05-27 | Ф.Хоффманн-Ля Рош Аг | ПРОИЗВОДНЫЕ ЗАМЕЩЕННОГО ДИБЕНЗОАЗЕПИНА И БЕНЗОДИАЗЕПИНА, ПОЛЕЗНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ γ-СЕКРЕТАЗЫ |
| US7211573B2 (en) | 2004-12-08 | 2007-05-01 | Hoffmann-La Roche Inc. | Malonamide derivatives |
| CA2645756C (en) * | 2006-03-27 | 2013-12-31 | F. Hoffmann-La Roche Ag | Malonamide derivatives as gamma secretase inhibitors |
| CN101516859B (zh) * | 2006-09-20 | 2012-07-04 | 霍夫曼-拉罗奇有限公司 | 4-氧代-2,3,4,5-四氢-苯并[b][1,4]二氮杂*衍生物 |
| EP2109604A1 (de) * | 2007-02-02 | 2009-10-21 | F. Hoffmann-Roche AG | 6-oxo-6,7-dihydro-5h-dibenzo[b,d]azepin-7-ylderivate |
| CA2679985A1 (en) * | 2007-03-15 | 2008-09-18 | F. Hoffmann-La Roche Ag | Malonamides as orexin antagonists |
| US7579464B2 (en) * | 2007-05-25 | 2009-08-25 | Hoffmann-La Roche Inc. | Process for preparation of enantiomerically pure compounds |
| CN101909633B (zh) * | 2008-01-11 | 2012-05-30 | 霍夫曼-拉罗奇有限公司 | γ-分泌酶抑制剂用于治疗癌症的应用 |
| US8741889B2 (en) | 2008-01-11 | 2014-06-03 | Hoffmann-La Roche Inc | Method of treating non-small cell lung cancer and colon cancer with gamma-secretase inhibitor |
| US8309299B2 (en) | 2010-05-19 | 2012-11-13 | Hoffmann-La Roche Inc. | Combination therapy and method for assessing resistance to treatment |
| WO2012040444A2 (en) * | 2010-09-24 | 2012-03-29 | Bristol-Myers Squibb Company | Treatment of patients with incipient alzheimer's disease |
| WO2012050370A2 (ko) * | 2010-10-15 | 2012-04-19 | 성균관대학교산학협력단 | 감마-세크레타제 저해제를 유효성분으로 함유하는 류마티스성 관절염의 예방 또는 치료용 조성물 |
| KR101330184B1 (ko) | 2010-10-15 | 2013-11-15 | 성균관대학교산학협력단 | 감마-세크레타제 저해제를 유효성분으로 함유하는 류마티스성 관절염의 예방 또는 치료용 조성물 |
| US20120114638A1 (en) | 2010-11-08 | 2012-05-10 | John Boylan | Combination therapy |
| US20120184529A1 (en) | 2011-01-14 | 2012-07-19 | Demario Mark D | Combination therapy |
| US20120225860A1 (en) | 2011-03-02 | 2012-09-06 | John Frederick Boylan | Method for administration of a gamma secretase inhibitor |
| TWI530489B (zh) | 2011-03-22 | 2016-04-21 | 必治妥美雅史谷比公司 | 雙(氟烷基)-1,4-苯二氮呯酮化合物 |
| AR087107A1 (es) | 2011-07-27 | 2014-02-12 | Lilly Co Eli | Compuesto inhibidor de la señalizacion de la trayectoria notch |
| JP2015529253A (ja) | 2012-09-21 | 2015-10-05 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | Notch阻害剤としてのフルオロアルキルおよびフルオロシクロアルキル1,4−ベンゾジアゼピノン化合物 |
| JP2015534553A (ja) | 2012-09-21 | 2015-12-03 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 置換1,5−ベンゾジアゼピノン化合物 |
| US9133126B2 (en) | 2012-09-21 | 2015-09-15 | Bristol-Myers Squibb Company | Fluoroalkyl dibenzoazepinone compounds |
| JP2015531792A (ja) | 2012-09-21 | 2015-11-05 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 1,4−ベンゾジアゼピノン化合物のプロドラッグ |
| TWI614238B (zh) | 2012-09-21 | 2018-02-11 | 必治妥美雅史谷比公司 | 雙(氟烷基)-1,4-苯并二氮呯酮化合物及其前藥 |
| CN104822677A (zh) | 2012-09-21 | 2015-08-05 | 百时美施贵宝公司 | 氟烷基-1,4-苯并二氮杂*酮化合物 |
| US9242941B2 (en) | 2012-09-21 | 2016-01-26 | Bristol-Myers Squibb Company | Alkyl, fluoroalkyl-1,4-benzodiazepinone compounds |
| EP2897946B1 (de) | 2012-09-21 | 2016-11-16 | Bristol-Myers Squibb Company | N-substituierte bis(fluoralkyl)-1,4-benzodiazepinonverbindungen |
| JP2015529251A (ja) | 2012-09-21 | 2015-10-05 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | Notch阻害剤としての三環系複素環式化合物 |
| CN105101968A (zh) | 2013-04-04 | 2015-11-25 | 百时美施贵宝公司 | 治疗增殖性疾病的组合疗法 |
| EP2932966A1 (de) | 2014-04-16 | 2015-10-21 | Novartis AG | Gammasekretasehemmer zur Behandlung von Atemwegserkrankungen |
| MX378973B (es) * | 2015-10-30 | 2025-03-10 | Pipeline Therapeutics Inc | Compuestos de dibenzo-azepina y su uso en el tratamiento de enfermedades y trastornos óticos. |
| IL267253B2 (en) * | 2016-12-16 | 2023-04-01 | Pipeline Therapeutics Inc | Methods for treating cochlear synaptopathy |
| EP3615055A1 (de) | 2017-04-28 | 2020-03-04 | Novartis AG | Zellen, die einen auf bcma abzielenden chimären antigenrezeptor exprimieren, und kombinationsbehandlung mit einem gamma-sekretase-inhibitor |
| EP3615068A1 (de) | 2017-04-28 | 2020-03-04 | Novartis AG | Auf bcma abzielender wirkstoff und kombinationstherapie mit einem gamma-sekretase-inhibitor |
| WO2019034532A1 (en) * | 2017-08-15 | 2019-02-21 | Bayer Aktiengesellschaft | 4-oxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-7-carboxamides |
| BR112020024351A2 (pt) | 2018-06-01 | 2021-02-23 | Novartis Ag | moléculas de ligação contra bcma e usos das mesmas |
| CA3144324A1 (en) | 2019-06-24 | 2020-12-30 | Novartis Ag | Dosing regimen and combination therapies for multispecific antibodies targeting b-cell maturation antigen |
| WO2022020658A1 (en) * | 2020-07-23 | 2022-01-27 | Purdue Research Foundation | Notch signaling inhibitors for treating obesity and metabolic disorders |
| CN117881667A (zh) * | 2021-08-31 | 2024-04-12 | 巴斯夫欧洲公司 | 含有稠环系的除草剂丙二酰胺 |
| CN119095890A (zh) | 2022-11-04 | 2024-12-06 | 株式会社Lg化学 | 全息图记录介质和包括其的光学元件 |
| CN116621721B (zh) * | 2023-04-12 | 2025-03-18 | 珠海市柏瑞医药科技有限公司 | 一种壬二酰胺的制备方法 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK0675886T3 (da) * | 1992-12-10 | 2000-09-18 | Pfizer | Aminomethylensubstituerede ikke-aromatiske heterocykler og deres anvendelse som substance P-antagonister |
| US5672598A (en) * | 1995-03-21 | 1997-09-30 | The Procter & Gamble Company | Lactam-containing hydroxamic acids |
| CA2404273A1 (en) * | 2000-04-11 | 2001-10-18 | Bristol-Myers Squibb Pharma Company | Substituted lactams as inhibitors of a.beta. protein production |
| GB0012671D0 (en) * | 2000-05-24 | 2000-07-19 | Merck Sharp & Dohme | Therapeutic agents |
| EP1592684B1 (de) * | 2003-02-04 | 2008-07-30 | F. Hoffmann-La Roche Ag | Malonamidderivate als gamma-secretaseinhibitoren |
| UA83501C2 (uk) * | 2003-09-09 | 2008-07-25 | Ф.Хоффманн-Ля Рош Аг | ПОХІДНІ МАЛОНАМІДУ, ЩО БЛОКУЮТЬ АКТИВНІСТЬ γ-СЕКРЕТАЗИ |
-
2004
- 2004-08-31 UA UAA200602854A patent/UA83501C2/uk unknown
- 2004-08-31 KR KR1020067004763A patent/KR100834177B1/ko not_active Expired - Fee Related
- 2004-08-31 HR HR20090266T patent/HRP20090266T1/xx unknown
- 2004-08-31 KR KR1020077017458A patent/KR20070087233A/ko not_active Ceased
- 2004-08-31 ES ES04764665T patent/ES2322652T3/es not_active Expired - Lifetime
- 2004-08-31 KR KR1020077017457A patent/KR100838852B1/ko not_active Expired - Fee Related
- 2004-08-31 MX MXPA06002562A patent/MXPA06002562A/es active IP Right Grant
- 2004-08-31 DE DE602004020680T patent/DE602004020680D1/de not_active Expired - Lifetime
- 2004-08-31 WO PCT/EP2004/009700 patent/WO2005023772A1/en not_active Ceased
- 2004-08-31 EP EP04764665A patent/EP1711470B1/de not_active Expired - Lifetime
- 2004-08-31 AU AU2004270361A patent/AU2004270361B2/en not_active Ceased
- 2004-08-31 EA EA200600503A patent/EA009940B1/ru not_active IP Right Cessation
- 2004-08-31 JP JP2006525701A patent/JP4571639B2/ja not_active Expired - Lifetime
- 2004-08-31 CA CA2537440A patent/CA2537440C/en not_active Expired - Fee Related
- 2004-08-31 RS YUP-2006/0146A patent/RS20060146A/sr unknown
- 2004-08-31 PT PT04764665T patent/PT1711470E/pt unknown
- 2004-08-31 AT AT04764665T patent/ATE428698T1/de active
- 2004-08-31 CN CN200480032641A patent/CN100593539C/zh not_active Expired - Lifetime
- 2004-08-31 DK DK04764665T patent/DK1711470T3/da active
- 2004-08-31 SI SI200431116T patent/SI1711470T1/sl unknown
- 2004-08-31 BR BRPI0413533-4A patent/BRPI0413533A/pt not_active Application Discontinuation
- 2004-08-31 NZ NZ545538A patent/NZ545538A/en not_active IP Right Cessation
- 2004-08-31 PL PL04764665T patent/PL1711470T3/pl unknown
- 2004-09-02 US US10/933,177 patent/US7160875B2/en not_active Expired - Lifetime
- 2004-09-06 MY MYPI20043603A patent/MY141308A/en unknown
- 2004-09-06 TW TW093126876A patent/TW200519092A/zh unknown
- 2004-09-08 AR ARP040103214A patent/AR045609A1/es not_active Application Discontinuation
-
2006
- 2006-02-23 IL IL173905A patent/IL173905A/en active IP Right Grant
- 2006-02-23 CO CO06018272A patent/CO5660268A2/es not_active Application Discontinuation
- 2006-03-01 CR CR8264A patent/CR8264A/es not_active Application Discontinuation
- 2006-03-03 NO NO20061047A patent/NO20061047L/no not_active Application Discontinuation
- 2006-03-07 EC EC2006006414A patent/ECSP066414A/es unknown
- 2006-03-07 TN TNP2006000077A patent/TNSN06077A1/fr unknown
- 2006-03-08 ZA ZA200601989A patent/ZA200601989B/en unknown
- 2006-03-10 MA MA28867A patent/MA28034A1/fr unknown
-
2009
- 2009-07-10 CY CY20091100729T patent/CY1109225T1/el unknown
-
2010
- 2010-06-18 JP JP2010138970A patent/JP2010229153A/ja active Pending
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