BR0009674A - Composto, droga, e, uso de composto - Google Patents
Composto, droga, e, uso de compostoInfo
- Publication number
- BR0009674A BR0009674A BR0009674-1A BR0009674A BR0009674A BR 0009674 A BR0009674 A BR 0009674A BR 0009674 A BR0009674 A BR 0009674A BR 0009674 A BR0009674 A BR 0009674A
- Authority
- BR
- Brazil
- Prior art keywords
- compound
- compounds
- drug
- prodrugs
- application
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 7
- 229940079593 drug Drugs 0.000 title abstract 3
- 239000003814 drug Substances 0.000 title abstract 3
- 108060005987 Kallikrein Proteins 0.000 abstract 2
- 102000001399 Kallikrein Human genes 0.000 abstract 2
- 229940002612 prodrug Drugs 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 108090000190 Thrombin Proteins 0.000 abstract 1
- 229940122388 Thrombin inhibitor Drugs 0.000 abstract 1
- 229940121363 anti-inflammatory agent Drugs 0.000 abstract 1
- 239000002260 anti-inflammatory agent Substances 0.000 abstract 1
- 239000003146 anticoagulant agent Substances 0.000 abstract 1
- 229940127219 anticoagulant drug Drugs 0.000 abstract 1
- 230000002860 competitive effect Effects 0.000 abstract 1
- -1 heterocyclic amidines Chemical class 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 229960004072 thrombin Drugs 0.000 abstract 1
- 239000003868 thrombin inhibitor Substances 0.000 abstract 1
- 108010036927 trypsin-like serine protease Proteins 0.000 abstract 1
Classifications
-
- 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
-
- 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
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- A61P9/06—Antiarrhythmics
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B43/00—Formation or introduction of functional groups containing nitrogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/022—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2
- C07K5/0222—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2 with the first amino acid being heterocyclic, e.g. Pro, Trp
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Oncology (AREA)
- Urology & Nephrology (AREA)
- Psychiatry (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)
- Peptides Or Proteins (AREA)
Abstract
"COMPOSTO, DROGA, E, USO DE COMPOSTO". A invenção refere-se a pró-drogas de amidinas heterocíclicas de cinco membros, farmacologicamente ativas, a partir das quais são obtidos compostos in vivo, que são inibidores competitivos de proteases de serina tipo tripsina, em especial trombina e quininogenases como calicreína, sua produção e sua aplicação como medicamentos. A invenção refere-se também a composições farmacêuticas, que contêm as pró-drogas dos compostos ativos como componentes, assim como à aplicação dos compostos como inibidores de trombina, anticoagulantes e como agentes antiinflamatórios.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19915930 | 1999-04-09 | ||
| DE19934123 | 1999-07-23 | ||
| DE19947920 | 1999-10-06 | ||
| PCT/EP2000/003009 WO2000061609A2 (de) | 1999-04-09 | 2000-04-05 | Prodrugs von thrombininhibitoren |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR0009674A true BR0009674A (pt) | 2002-01-15 |
Family
ID=27219075
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0009674-1A BR0009674A (pt) | 1999-04-09 | 2000-04-05 | Composto, droga, e, uso de composto |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US7144902B1 (pt) |
| EP (1) | EP1165601A2 (pt) |
| JP (1) | JP2002542165A (pt) |
| KR (1) | KR20010108481A (pt) |
| CN (1) | CN1355810A (pt) |
| AU (1) | AU765244B2 (pt) |
| BG (1) | BG105986A (pt) |
| BR (1) | BR0009674A (pt) |
| CA (1) | CA2370267A1 (pt) |
| HK (1) | HK1046289A1 (pt) |
| HU (1) | HUP0202401A3 (pt) |
| IL (1) | IL145772A0 (pt) |
| NO (1) | NO20014875L (pt) |
| NZ (1) | NZ515026A (pt) |
| PL (1) | PL352824A1 (pt) |
| SK (1) | SK14222001A3 (pt) |
| TR (1) | TR200102912T2 (pt) |
| WO (1) | WO2000061609A2 (pt) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10064797A1 (de) * | 2000-12-22 | 2002-06-27 | Knoll Ag | Orale und parenterale pharmazeutische Formulierung, umfassend eine niedermolekulare Thrombininhibitor-Pro-Pharmakon |
| WO2004002985A1 (en) * | 2002-06-27 | 2004-01-08 | Lg Life Sciences Ltd. | Peptidic thrombin inhibitor compound |
| KR101154246B1 (ko) | 2003-05-16 | 2012-06-13 | 내셔날 인스티튜트 포 바이올로지칼 스탠다즈 앤 컨트롤 (엔아이비에스씨) | 활성화 혼합물 |
| US7939629B2 (en) | 2004-10-19 | 2011-05-10 | Lonza Ag | Method for solid phase peptide synthesis |
| CA2607020C (en) * | 2005-05-05 | 2015-01-13 | Chroma Therapeutics Ltd. | Alpha amino acid ester-drug conjugates hydrolysable by carboxylesterases |
| SG195607A1 (en) | 2005-05-10 | 2013-12-30 | Incyte Corp | Modulators of indoleamine 2,3-dioxygenase and methods of using the same |
| JP5294874B2 (ja) | 2005-12-20 | 2013-09-18 | インサイト・コーポレイション | インドールアミン２，３−ジオキシゲナーゼのモジュレーターとしてのｎ−ヒドロキシアミジノヘテロ環 |
| CA2663057C (en) * | 2006-09-19 | 2015-12-08 | Incyte Corporation | N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase |
| CL2007002650A1 (es) | 2006-09-19 | 2008-02-08 | Incyte Corp | Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras. |
| EP3360873A1 (en) | 2008-07-08 | 2018-08-15 | Incyte Holdings Corporation | 1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase |
| JP2013515000A (ja) | 2009-12-18 | 2013-05-02 | アクティベサイト ファーマシューティカルズ インコーポレイティッド | 血漿カリクレインの阻害薬のプロドラッグ |
| US9206123B2 (en) | 2009-12-18 | 2015-12-08 | Activesite Pharmaceuticals, Inc. | Prodrugs of inhibitors of plasma kallikrein |
| WO2012142308A1 (en) | 2011-04-13 | 2012-10-18 | Activesite Pharmaceuticals, Inc. | Prodrugs of inhibitors of plasma kallikrein |
| TWI696618B (zh) | 2013-11-08 | 2020-06-21 | 美商英塞特控股公司 | 用於合成吲哚胺2,3-雙加氧酶抑制劑之方法 |
| JP6556146B2 (ja) * | 2014-08-26 | 2019-08-07 | 武田薬品工業株式会社 | 複素環化合物 |
| CN106674190B (zh) * | 2016-12-13 | 2019-05-10 | 台州市创源工业技术有限公司 | 一种2-噻吩甲胺的合成方法 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA951617B (en) * | 1994-03-04 | 1997-02-27 | Lilly Co Eli | Antithrombotic agents. |
| TW541316B (en) | 1995-12-21 | 2003-07-11 | Astrazeneca Ab | Prodrugs of thrombin inhibitors |
| TW523513B (en) | 1996-03-01 | 2003-03-11 | Akzo Nobel Nv | Serine protease inhibitors |
| DE19632773A1 (de) | 1996-08-14 | 1998-02-19 | Basf Ag | Neue Thrombininhibitoren |
| CN1289341A (zh) * | 1998-01-26 | 2001-03-28 | Basf公司 | 凝血酶抑制剂 |
| EP1049673A1 (de) | 1998-01-26 | 2000-11-08 | Basf Aktiengesellschaft | Heterocyclische amidine als kallikrein protease inhibitoren |
| KR20000047461A (ko) * | 1998-12-29 | 2000-07-25 | 성재갑 | 트롬빈 억제제 |
| HUP0203167A3 (en) * | 1999-04-09 | 2003-09-29 | Basf Ag | Peptidic substances, their preparations and their use as complement protease inhibitors |
-
2000
- 2000-04-05 BR BR0009674-1A patent/BR0009674A/pt not_active IP Right Cessation
- 2000-04-05 WO PCT/EP2000/003009 patent/WO2000061609A2/de not_active Application Discontinuation
- 2000-04-05 US US09/958,349 patent/US7144902B1/en not_active Expired - Fee Related
- 2000-04-05 TR TR2001/02912T patent/TR200102912T2/xx unknown
- 2000-04-05 SK SK1422-2001A patent/SK14222001A3/sk not_active Application Discontinuation
- 2000-04-05 JP JP2000611551A patent/JP2002542165A/ja active Pending
- 2000-04-05 CN CN00807958A patent/CN1355810A/zh active Pending
- 2000-04-05 HK HK02107849.6A patent/HK1046289A1/zh unknown
- 2000-04-05 PL PL00352824A patent/PL352824A1/xx unknown
- 2000-04-05 IL IL14577200A patent/IL145772A0/xx unknown
- 2000-04-05 CA CA002370267A patent/CA2370267A1/en not_active Abandoned
- 2000-04-05 KR KR1020017012870A patent/KR20010108481A/ko not_active Ceased
- 2000-04-05 AU AU41156/00A patent/AU765244B2/en not_active Ceased
- 2000-04-05 HU HU0202401A patent/HUP0202401A3/hu unknown
- 2000-04-05 NZ NZ515026A patent/NZ515026A/en unknown
- 2000-04-05 EP EP00920661A patent/EP1165601A2/de not_active Withdrawn
-
2001
- 2001-10-05 BG BG105986A patent/BG105986A/bg unknown
- 2001-10-08 NO NO20014875A patent/NO20014875L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| WO2000061609B1 (de) | 2001-04-26 |
| NO20014875D0 (no) | 2001-10-08 |
| TR200102912T2 (tr) | 2002-03-21 |
| WO2000061609A2 (de) | 2000-10-19 |
| AU765244B2 (en) | 2003-09-11 |
| PL352824A1 (en) | 2003-09-08 |
| AU4115600A (en) | 2000-11-14 |
| WO2000061609A3 (de) | 2001-03-15 |
| KR20010108481A (ko) | 2001-12-07 |
| NO20014875L (no) | 2001-11-13 |
| CN1355810A (zh) | 2002-06-26 |
| US7144902B1 (en) | 2006-12-05 |
| HUP0202401A2 (en) | 2002-10-28 |
| CA2370267A1 (en) | 2000-10-19 |
| SK14222001A3 (sk) | 2002-07-02 |
| HUP0202401A3 (en) | 2003-11-28 |
| HK1046289A1 (zh) | 2003-01-03 |
| NZ515026A (en) | 2003-10-31 |
| JP2002542165A (ja) | 2002-12-10 |
| IL145772A0 (en) | 2002-07-25 |
| BG105986A (bg) | 2002-06-28 |
| EP1165601A2 (de) | 2002-01-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B25A | Requested transfer of rights approved |
Free format text: ABBOTT GMBH & CO. KG (DE) |
|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 7A,8A E 9A ANUIDADES. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 NA RPI2003 DE 26/05/2009. |