HUP9800634A2 - p-Amidino-benzil-amid-származék trombin-inhibitorok, intermedierjeik és alkalmazásuk - Google Patents
p-Amidino-benzil-amid-származék trombin-inhibitorok, intermedierjeik és alkalmazásukInfo
- Publication number
- HUP9800634A2 HUP9800634A2 HU9800634A HUP9800634A HUP9800634A2 HU P9800634 A2 HUP9800634 A2 HU P9800634A2 HU 9800634 A HU9800634 A HU 9800634A HU P9800634 A HUP9800634 A HU P9800634A HU P9800634 A2 HUP9800634 A2 HU P9800634A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- general formula
- intermediates
- tube
- divalent
- Prior art date
Links
- 239000000543 intermediate Substances 0.000 title abstract 2
- 229940122388 Thrombin inhibitor Drugs 0.000 title 1
- 239000003868 thrombin inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 235000008206 alpha-amino acids Nutrition 0.000 abstract 2
- 239000000843 powder Substances 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 1
- 150000007513 acids Chemical class 0.000 abstract 1
- 150000001370 alpha-amino acid derivatives Chemical class 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000003943 azolyl group Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000006165 cyclic alkyl group Chemical group 0.000 abstract 1
- -1 cyclic α-amino acid Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000547 substituted alkyl group Chemical group 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
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/55—Protease inhibitors
-
- 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
-
- 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
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
-
- 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
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
-
- 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
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/0606—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
-
- 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
-
- 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
- C07K5/06104—Dipeptides with the first amino acid being acidic
- C07K5/06113—Asp- or Asn-amino acid
-
- 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
- C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Mutual Connection Of Rods And Tubes (AREA)
Abstract
A cím szerinti vegyületek (I) általánős képletében R1 hidrőxilcsőpőrt,adőtt esetben szűbsztitűált alkilcsőpőrt, ciklőalkil-, aril-,heterőarilcsőpőrt; A kétértékű a-aminősavcsőpőrt; B kétértékű,ciklűsős a-aminősav-csőpőrt; D adőtt esetben gyűrűben és/vagymetiléncsőpőrtőn szűbsztitűált benzil-, azőlil- vagy azinilcsőpőrt. Atalálmány tárgykörébe tartőznak a fenti vegyületek sztereőizőmerjei ésfiziőlógiailag elviselhető savakkal alkőtőtt sói, amelyekben azamidinfűnkció lehet egyszeresen vagy kétszeresen védett főrmában. Atalálmány tárgyát képezik tővábbá a (VII), (VIII), (IX) és (X)általánős képletű intermedierek, valamint a (XI) általánős képletűszerkezeti részletet tartalmazó vegyületek. ŕ
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE1995104504 DE19504504A1 (de) | 1995-02-10 | 1995-02-10 | Heterocyclische Thrombininhibitoren |
DE1995106610 DE19506610A1 (de) | 1995-02-24 | 1995-02-24 | Thrombininhibitoren |
Publications (2)
Publication Number | Publication Date |
---|---|
HUP9800634A2 true HUP9800634A2 (hu) | 1999-06-28 |
HUP9800634A3 HUP9800634A3 (en) | 2000-04-28 |
Family
ID=26012343
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU9800634A HUP9800634A3 (en) | 1995-02-10 | 1996-02-06 | P-amidino-benzylamide derivatives as thrombin inhibitors, intermediates and use thereof |
Country Status (15)
Country | Link |
---|---|
US (1) | US5932567A (hu) |
EP (1) | EP0809651A1 (hu) |
JP (1) | JPH10513462A (hu) |
KR (1) | KR19980702112A (hu) |
CN (1) | CN1173872A (hu) |
AU (1) | AU706834B2 (hu) |
BR (1) | BR9607412A (hu) |
CA (1) | CA2210989A1 (hu) |
CZ (1) | CZ237697A3 (hu) |
EA (1) | EA002767B1 (hu) |
FI (1) | FI973282A0 (hu) |
HU (1) | HUP9800634A3 (hu) |
MX (1) | MX9705970A (hu) |
NO (1) | NO973657L (hu) |
WO (1) | WO1996024609A1 (hu) |
Families Citing this family (34)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SE9900043D0 (sv) * | 1999-01-11 | 1999-01-11 | Astra Ab | New use |
US5705487A (en) * | 1994-03-04 | 1998-01-06 | Eli Lilly And Company | Antithrombotic agents |
US5707966A (en) * | 1994-03-04 | 1998-01-13 | Eli Lilly And Company | Antithrombotic agents |
US5726159A (en) * | 1994-03-04 | 1998-03-10 | Eli Lilly And Company | Antithrombotic agents |
US5710130A (en) * | 1995-02-27 | 1998-01-20 | Eli Lilly And Company | Antithrombotic agents |
US5914319A (en) * | 1995-02-27 | 1999-06-22 | Eli Lilly And Company | Antithrombotic agents |
SE9602263D0 (sv) | 1996-06-07 | 1996-06-07 | Astra Ab | New amino acid derivatives |
US6200967B1 (en) | 1996-06-25 | 2001-03-13 | Eli Lilly And Company | Anticoagulant agents |
EP1110968B1 (en) * | 1996-06-25 | 2003-10-01 | Eli Lilly & Company | Intermediate for the preparation of Thrombininhibitors as anticoagulant agents |
US5863929A (en) * | 1996-06-25 | 1999-01-26 | Eli Lilly And Company | Anticoagulant agents |
US6369080B2 (en) | 1996-10-11 | 2002-04-09 | Cor Therapeutics, Inc. | Selective factor Xa inhibitors |
US6194435B1 (en) | 1996-10-11 | 2001-02-27 | Cor Therapeutics, Inc. | Lactams as selective factor Xa inhibitors |
US6063794A (en) | 1996-10-11 | 2000-05-16 | Cor Therapeutics Inc. | Selective factor Xa inhibitors |
US6262047B1 (en) | 1996-10-11 | 2001-07-17 | Cor Therapeutics, Inc. | Selective factor Xa inhibitors |
WO1998046626A1 (en) | 1997-04-14 | 1998-10-22 | Cor Therapeutics, Inc. | SELECTIVE FACTOR Xa INHIBITORS |
JP2001521524A (ja) * | 1997-04-14 | 2001-11-06 | シーオーアール セラピューティクス インコーポレイテッド | 選択的Xa因子阻害剤 |
CA2285659A1 (en) | 1997-04-14 | 1998-10-22 | Cor Therapeutics, Inc. | Selective factor xa inhibitors |
US7109326B2 (en) | 1997-04-15 | 2006-09-19 | Genentech, Inc. | Halo-alkoxycarbonyl prodrugs |
AR013084A1 (es) | 1997-06-19 | 2000-12-13 | Astrazeneca Ab | Derivados de amidino utiles como inhibidores de la trombina, composicion farmaceutica, utilizacion de dichos compuestos para la preparacion demedicamentos y proceso para la preparacion de los compuestos mencionados |
US6228854B1 (en) | 1997-08-11 | 2001-05-08 | Cor Therapeutics, Inc. | Selective factor Xa inhibitors |
US6218382B1 (en) | 1997-08-11 | 2001-04-17 | Cor Therapeutics, Inc | Selective factor Xa inhibitors |
US6333321B1 (en) | 1997-08-11 | 2001-12-25 | Cor Therapeutics, Inc. | Selective factor Xa inhibitors |
SE9704543D0 (sv) | 1997-12-05 | 1997-12-05 | Astra Ab | New compounds |
KR20000047461A (ko) * | 1998-12-29 | 2000-07-25 | 성재갑 | 트롬빈 억제제 |
US6486193B2 (en) | 1998-12-31 | 2002-11-26 | Aventis Pharmaceuticals Inc. | 3-substituted pyrrolidines useful as inhibitors of matrix metalloproteinases |
DE50008510D1 (de) * | 1999-04-09 | 2004-12-09 | Abbott Gmbh & Co Kg | Niedermolekulare inhibitoren von komplementproteasen |
US6586405B2 (en) | 2000-08-11 | 2003-07-01 | Corvas International, Inc. | Non-covalent inhibitors of urokinase and blood vessel formation |
IL149042A0 (en) * | 2000-08-11 | 2002-11-10 | Corvas Int Inc | Non-covalent inhibitors of urokinase and blood vessel formation |
DE10049937A1 (de) * | 2000-10-06 | 2002-04-11 | Knoll Ag | Niedermolekulare Inhibitoren von Serinproteasen mit Polyhydroxyalkyl- und Polyhydroxycycloalkylresten |
US6716869B2 (en) * | 2001-12-17 | 2004-04-06 | Pharmacia Corporation | Protease inhibitors of the coagulation cascade isolated from Dysidea sponges |
WO2003070229A2 (de) * | 2002-02-22 | 2003-08-28 | MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. | Verwendung von proteinaseinhibitoren zur behandlung von autoimmunerkrankungen |
DE102004022897A1 (de) * | 2004-05-10 | 2005-12-08 | Bayer Cropscience Ag | Azinyl-imidazoazine |
DE102008041214A1 (de) | 2008-08-13 | 2010-02-18 | Bayer Cropscience Ag | N-substituierte Azinylakyl-azincarboxamide und deren Analoge |
US10597863B2 (en) | 2018-01-19 | 2020-03-24 | Resource Fiber LLC | Laminated bamboo platform and concrete composite slab system |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU675981B2 (en) * | 1992-12-02 | 1997-02-27 | Bristol-Myers Squibb Company | Guanidinyl-substituted heterocyclic thrombin inhibitors |
SE9301916D0 (sv) * | 1993-06-03 | 1993-06-03 | Ab Astra | New peptides derivatives |
AU1025795A (en) * | 1994-01-27 | 1995-08-03 | Mitsubishi Chemical Corporation | Prolineamide derivatives |
IL112795A (en) * | 1994-03-04 | 2001-01-28 | Astrazeneca Ab | Derivatives of peptides as antithrombotic drugs, their preparation, and pharmaceutical preparations containing them |
-
1996
- 1996-02-06 KR KR1019970705507A patent/KR19980702112A/ko not_active Application Discontinuation
- 1996-02-06 EP EP96903987A patent/EP0809651A1/de not_active Withdrawn
- 1996-02-06 WO PCT/EP1996/000472 patent/WO1996024609A1/de not_active Application Discontinuation
- 1996-02-06 CN CN96191860A patent/CN1173872A/zh active Pending
- 1996-02-06 HU HU9800634A patent/HUP9800634A3/hu unknown
- 1996-02-06 AU AU47875/96A patent/AU706834B2/en not_active Ceased
- 1996-02-06 US US08/875,515 patent/US5932567A/en not_active Expired - Fee Related
- 1996-02-06 JP JP8523967A patent/JPH10513462A/ja not_active Abandoned
- 1996-02-06 CZ CZ972376A patent/CZ237697A3/cs unknown
- 1996-02-06 CA CA002210989A patent/CA2210989A1/en not_active Abandoned
- 1996-02-06 EA EA199700155A patent/EA002767B1/ru not_active IP Right Cessation
- 1996-02-06 MX MX9705970A patent/MX9705970A/es unknown
- 1996-02-06 BR BR9607412A patent/BR9607412A/pt not_active Application Discontinuation
-
1997
- 1997-08-08 NO NO973657A patent/NO973657L/no not_active Application Discontinuation
- 1997-08-08 FI FI973282A patent/FI973282A0/fi unknown
Also Published As
Publication number | Publication date |
---|---|
NO973657D0 (no) | 1997-08-08 |
BR9607412A (pt) | 1998-07-07 |
JPH10513462A (ja) | 1998-12-22 |
EA002767B1 (ru) | 2002-08-29 |
NO973657L (no) | 1997-10-03 |
EP0809651A1 (de) | 1997-12-03 |
FI973282A (fi) | 1997-08-08 |
CZ237697A3 (cs) | 1998-04-15 |
CN1173872A (zh) | 1998-02-18 |
HUP9800634A3 (en) | 2000-04-28 |
KR19980702112A (ko) | 1998-07-15 |
WO1996024609A1 (de) | 1996-08-15 |
US5932567A (en) | 1999-08-03 |
MX9705970A (es) | 1997-11-29 |
AU706834B2 (en) | 1999-06-24 |
FI973282A0 (fi) | 1997-08-08 |
CA2210989A1 (en) | 1996-08-15 |
AU4787596A (en) | 1996-08-27 |
EA199700155A1 (ru) | 1997-12-30 |
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