HUP9801688A2 - Acetamidszármazékok, eljárás előállításukra és ilyen vegyületeket tartalmazó gyógyászati készítmények - Google Patents
Acetamidszármazékok, eljárás előállításukra és ilyen vegyületeket tartalmazó gyógyászati készítményekInfo
- Publication number
- HUP9801688A2 HUP9801688A2 HU9801688A HUP9801688A HUP9801688A2 HU P9801688 A2 HUP9801688 A2 HU P9801688A2 HU 9801688 A HU9801688 A HU 9801688A HU P9801688 A HUP9801688 A HU P9801688A HU P9801688 A2 HUP9801688 A2 HU P9801688A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- alkyl
- pipe powder
- powder
- pipe
- Prior art date
Links
- 150000003869 acetamides Chemical class 0.000 title abstract 2
- 239000000843 powder Substances 0.000 abstract 17
- 125000000217 alkyl group Chemical group 0.000 abstract 10
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 2
- -1 alkyl radical Chemical class 0.000 abstract 2
- 125000003277 amino group Chemical group 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000000126 substance Substances 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 201000004384 Alopecia Diseases 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000004442 acylamino group Chemical group 0.000 abstract 1
- 125000005041 acyloxyalkyl group Chemical group 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 125000006515 benzyloxy alkyl group Chemical group 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 208000015114 central nervous system disease Diseases 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 125000005265 dialkylamine group Chemical group 0.000 abstract 1
- 125000005117 dialkylcarbamoyl group Chemical group 0.000 abstract 1
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 206010015037 epilepsy Diseases 0.000 abstract 1
- 208000024963 hair loss Diseases 0.000 abstract 1
- 230000003676 hair loss Effects 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 150000002466 imines Chemical class 0.000 abstract 1
- LPAGFVYQRIESJQ-UHFFFAOYSA-N indoline Chemical group C1=CC=C2NCCC2=C1 LPAGFVYQRIESJQ-UHFFFAOYSA-N 0.000 abstract 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 1
- 125000003884 phenylalkyl group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/34—One oxygen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- 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
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/34—One oxygen atom
- C07D239/36—One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
-
- 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
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
- C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
-
- 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
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Immunology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicinal Preparation (AREA)
Abstract
A találmány (I) általánős képletű acetamid-származékőkra és ezekgyógyászatilag elfőgadható savaddíciós sóira vőnatkőzik. A képletben X jelentése őxigénatőm vagy -NR4- általánős képletű csőpőrt; R1 jelentése hidrőgénatőm, alkilcsőpőrt, alkenilcsőpőrt vagy ciklőalkil-alkilcsőpőrt; R2 jelentése alkilcsőpőrt, ciklőalkilcsőpőrt, adőtt esetben szűbsztitűáltfenilcsőpőrt vagy adőtt esetben szűbsztitűált fenil-alkilcsőpőrt, vagyR1 és R2 adőtt esetben (XVI) általánős képletű csőpőrtőt - ebben azáltalánős képletben A jelentése egyszeres kémiai kötés,metiléncsőpőrt, őxigénatőm vagy iminőcsőpőrt, Ra és Rb egymástólfüggetlenül hidrőgénatőmőt vagy alkilcsőpőrtőt jelent, vagy ha Ajelentése egyszeres kémiai kötés, tővábbá Ra és Rb a 2-, illetve 3-helyzetben kapcsőlódik, akkőr a 2- és 3-helyzetű szénatőmők, valamintRa és Rb együtt fenilgyűrűt alkőthatnak - képeznek azzal anitrőgénatőmmal, amelyhez kapcsőlódnak; R3 jelentése hidrőgénatőm, alkilcsőpőrt vagy hidrőxi-alkilcsőpőrt; R4 jelentése hidrőgénatőm vagy alkilcsőpőrt; vagy R3 és R4 pirrőlidin, piperidin- vagy 2,3-dihidrő-1H-indőlgyűrűt alkőtazzal a szénatőmmal és nitrőgénatőmmal, amelyhez kapcsőlódnak; R5 jelentése hidrőgénatőm, alkilcsőpőrt, alkenilcsőpőrt, hidrőxi-alkilcsőpőrt, adőtt esetben szűbsztitűált benzil-őxi-alkilcsőpőrt,acil-őxi-alkilcsőpőrt, alkőxi-alkilcsőpőrt, diflűőr-metilcsőpőrt,halőgénatőm, aminőcsőpőrt, mőnő- vagy dialkil-aminőcsőpőrt, acil-aminőcsőpőrt, aminő-alkilcsőpőrt, nitrőcsőpőrt, karbamőilcsőpőrt,mőnő- vagy dialkil-karbamőilcsőpőrt, karbőxilcsőpőrt, védettkarbőxilcsőpőrt, karbőxi-alkilcsőpőrt vagy védett karbőxi-alkilcsőpőrt; R6 jelentése hidrőgénatőm, alkilcsőpőrt, triflűőr-metilcsőpőrt vagy adőttesetben szűbsztitűált fenilcsőpőrt; vagy R5 és R6 együtt -(CH2)n- általánős képletű csőpőrtőt - a képletben nértéke 3, 4, 5 vagy 6 - alkőt; R7 jelentése hidrőgénatőm, halőgénatőm, alkilcsőpőrt, alkőxicsőpőrt,triflűőr-metilcsőpőrt, hidrőxilcsőpőrt, aminőcsőpőrt, mőnő- vagydialkil-aminőcsőpőrt, cianőcsőpőrt vagy nitrőcsőpőrt; és R8 jelentése hidrőgén-, halőgénatőm, alkil-, vagy alkőxicsőpőrt. Az (I) általánős képletű vegyületek és gyógyászatilag elfőgadhatósavaddíciós sóik erős és szelektív affinitást műtatnak a BZw3receptőrőkhőz, így felhasználhatók közpőnti idegrendszerimegbetegedések, példáűl szőrőngással együtt járó megbetegedések,depresszió és epilepszia kezelésére. ŕ
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP11393795 | 1995-04-13 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP9801688A2 true HUP9801688A2 (hu) | 1999-03-29 |
| HUP9801688A3 HUP9801688A3 (en) | 2001-11-28 |
Family
ID=14624947
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU9801688A HUP9801688A3 (en) | 1995-04-13 | 1996-04-10 | Acetamide derivatives, process for producing the same, and medicinal composition containing the same |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US5972946A (hu) |
| EP (1) | EP0826673B1 (hu) |
| KR (1) | KR100433589B1 (hu) |
| CN (1) | CN1094929C (hu) |
| AR (1) | AR002289A1 (hu) |
| AT (1) | ATE228113T1 (hu) |
| AU (1) | AU694647B2 (hu) |
| BR (1) | BR9604894A (hu) |
| CA (1) | CA2218033A1 (hu) |
| CZ (1) | CZ289093B6 (hu) |
| DE (1) | DE69624916T2 (hu) |
| DK (1) | DK0826673T3 (hu) |
| ES (1) | ES2187644T3 (hu) |
| HU (1) | HUP9801688A3 (hu) |
| IL (1) | IL117659A (hu) |
| NO (1) | NO310619B1 (hu) |
| NZ (1) | NZ304982A (hu) |
| PL (1) | PL322819A1 (hu) |
| PT (1) | PT826673E (hu) |
| RO (1) | RO117532B1 (hu) |
| RU (1) | RU2160256C2 (hu) |
| SK (1) | SK281840B6 (hu) |
| TW (1) | TW450963B (hu) |
| WO (1) | WO1996032383A1 (hu) |
| ZA (1) | ZA962438B (hu) |
Families Citing this family (74)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU221855B1 (hu) * | 1994-09-09 | 2003-02-28 | Nippon Shinyaku Co., Ltd. | Szubsztituált piridin-, pirimidin- és triazinszármazékok és ilyen vegyületeket tartalmazó gyógyászati készítmények |
| EP1004573B1 (en) | 1997-08-04 | 2002-10-30 | Taisho Pharmaceutical Co., Ltd | Aryloxyaniline derivatives |
| CA2310664C (en) | 1997-11-21 | 2008-03-11 | Euro-Celtique S.A. | Substituted 2-aminoacetamides and the use thereof |
| ZA9810490B (en) | 1997-12-03 | 1999-05-20 | Dainippon Pharmaceutical Co | 2-Aryl-8-oxodihydropurine derivative process for the preparation thereof pharmaceutical composition containing the same and intermediate therefor |
| FR2778564B1 (fr) * | 1998-05-13 | 2001-07-13 | Sanofi Sa | Utilisation de composes reduisant l'apoptose |
| WO1999058117A1 (fr) * | 1998-05-13 | 1999-11-18 | Sanofi-Synthelabo | Utilisation de composes reduisant l'apoptose |
| JP2002241369A (ja) * | 1998-05-18 | 2002-08-28 | Dainippon Pharmaceut Co Ltd | ４−ピリミジニルアミノアセトアミド誘導体及びそれを含有する医薬組成物 |
| DE19853278A1 (de) | 1998-11-19 | 2000-05-25 | Aventis Pharma Gmbh | Substituierte 4-Amino-2-aryl-cyclopenta[d]pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
| EP1140106B1 (en) | 1998-12-18 | 2005-08-03 | Scios Inc. | Treatment of diseases involving cyst formation |
| US6342495B1 (en) | 1998-12-18 | 2002-01-29 | Scios, Inc. | Agonists and antagonists of peripheral-type benzodiazepine receptors |
| EP1607744A3 (en) * | 1998-12-18 | 2009-09-30 | Scios Inc. | Treatment of diseases involving cyst formation with combinations comprising a PTBR agonist |
| IL143929A0 (en) * | 1999-01-22 | 2002-04-21 | Elan Pharm Inc | Acyl derivatives which treat vla-4 related disorders |
| CA2357781A1 (en) | 1999-01-22 | 2000-07-27 | Elan Pharmaceuticals, Inc. | Multicyclic compounds which inhibit leukocyte adhesion mediated by vla-4 |
| AR035476A1 (es) * | 1999-01-22 | 2004-06-02 | Elan Pharm Inc | Compuestos heteroarilo y heterociclicos con anillo fusionado, los cuales inhiben la adhesion de leucocitos mediada por vla-4, composiciones farmaceuticas, el uso de las mismas para la manufactura de un medicamento y un metodo para fijar vla-4 en una muestra biologica |
| US6436904B1 (en) * | 1999-01-25 | 2002-08-20 | Elan Pharmaceuticals, Inc. | Compounds which inhibit leukocyte adhesion mediated by VLA-4 |
| DE19904710A1 (de) * | 1999-02-05 | 2000-08-10 | Aventis Pharma Gmbh | Substituierte 4-Amino-2-aryl-tetrahydrochinazoline, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
| AU3246600A (en) | 1999-03-01 | 2000-09-21 | Elan Pharmaceuticals, Inc. | Alpha-aminoacetic acid derivatives useful as alpha 4 beta 7 receptor antagonists |
| US7037916B2 (en) * | 1999-07-15 | 2006-05-02 | Pharmacopeia Drug Discovery, Inc. | Pyrimidine derivatives as IL-8 receptor antagonists |
| AU780048B2 (en) * | 1999-11-17 | 2005-02-24 | Dainippon Pharmaceutical Co. Ltd. | (5-chloro-6-phenyl-2-(4-trifluoromethylphenyl)-4- pyrimidinylamino)acetamide derivatives, process for producing the same, medicinal compositions containing the same and intermediate of these compounds |
| US20020072521A1 (en) * | 2000-03-16 | 2002-06-13 | Taeyoung Yoon | 5-substituted arylpyrimidines |
| JP2004504302A (ja) | 2000-07-18 | 2004-02-12 | ニューロジェン・コーポレーション | ５−置換２−アリール−４−ピリミジノン |
| EP1698627A1 (en) * | 2000-09-15 | 2006-09-06 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| CN1926132B (zh) * | 2000-09-15 | 2010-12-29 | 沃泰克斯药物股份有限公司 | 可用作蛋白激酶抑制剂的吡唑化合物 |
| US6660731B2 (en) * | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| CN100355750C (zh) * | 2000-09-15 | 2007-12-19 | 沃泰克斯药物股份有限公司 | 可用作蛋白激酶抑制剂的吡唑化合物 |
| US7473691B2 (en) * | 2000-09-15 | 2009-01-06 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| ATE326462T1 (de) * | 2000-12-21 | 2006-06-15 | Vertex Pharma | Pyrazolverbindungen als protein-kinase- inhibitoren |
| EP2198867A1 (en) * | 2001-12-07 | 2010-06-23 | Vertex Pharmaceuticals, Inc. | Pyrimidine-based compounds useful as GSK-3 inhibitors |
| SG159380A1 (en) * | 2002-02-06 | 2010-03-30 | Vertex Pharma | Heteroaryl compounds useful as inhibitors of gsk-3 |
| AU2003215379A1 (en) * | 2002-02-22 | 2003-09-09 | Pharmacia And Upjohn Company | Substituted pyrimidinones and pyrimidinthiones |
| AU2003218215A1 (en) * | 2002-03-15 | 2003-09-29 | Vertex Pharmaceuticals, Inc. | Azolylaminoazines as inhibitors of protein kinases |
| TW200307671A (en) | 2002-05-24 | 2003-12-16 | Elan Pharm Inc | Heteroaryl compounds which inhibit leukocyte adhesion mediated by α 4 integrins |
| TWI281470B (en) | 2002-05-24 | 2007-05-21 | Elan Pharm Inc | Heterocyclic compounds which inhibit leukocyte adhesion mediated by alpha4 integrins |
| MY141867A (en) | 2002-06-20 | 2010-07-16 | Vertex Pharma | Substituted pyrimidines useful as protein kinase inhibitors |
| NZ550883A (en) | 2002-08-02 | 2008-06-30 | Vertex Pharma | Pyrazole compositions useful as inhibitors of glycogen synthase kinase-3 (GSK-3) |
| NZ540612A (en) | 2003-01-14 | 2008-02-29 | Arena Pharm Inc | 1,2,3-Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia |
| WO2004072029A2 (en) * | 2003-02-06 | 2004-08-26 | Vertex Pharmaceuticals Incorporated | Pyrazolopyridazines useful as inhibitors of protein kinases |
| AR045047A1 (es) | 2003-07-11 | 2005-10-12 | Arena Pharm Inc | Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos |
| AU2004263515A1 (en) | 2003-08-05 | 2005-02-17 | Vertex Pharmaceuticals Incorporated | Condensed pyrimidine compounds as inhibitors of voltage-gated ion channels |
| US7378409B2 (en) * | 2003-08-21 | 2008-05-27 | Bristol-Myers Squibb Company | Substituted cycloalkylamine derivatives as modulators of chemokine receptor activity |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3631045A (en) * | 1969-11-04 | 1971-12-28 | American Home Prod | 4 5-diamino-7h-pyrrolo(2 3-d)pyrimidine derivatives |
| US3631036A (en) * | 1969-11-04 | 1971-12-28 | American Home Prod | 5-amino-2 6-substituted-7h-pyrrolo(2 3-d) pyrimidines and related compounds |
| FR2263750A1 (en) * | 1974-03-12 | 1975-10-10 | Delalande Sa | N-phenyl-N-(2-aryl-6-methyl-pyrimidin-4-yl)amino acid derivs. - useful e.g. as analeptics, hypotensives, analgesics, etc. |
| FR2525595A1 (fr) * | 1982-04-27 | 1983-10-28 | Pharmuka Lab | Nouveaux derives d'arene et d'heteroarenecarboxamides et leur utilisation comme medicaments |
| FR2582514B1 (fr) * | 1985-05-30 | 1988-02-19 | Rhone Poulenc Sante | Medicaments a base d'amides, nouveaux amides et leur preparation |
| DK273689A (da) * | 1988-06-06 | 1989-12-07 | Sanofi Sa | 4-amino-3-carboxyquinoliner og -naphthyridiner, fremgangsmaade til deres fremstilling og anvendelse deraf i laegemidler |
| JPH07165721A (ja) * | 1993-12-15 | 1995-06-27 | Sumitomo Chem Co Ltd | 放射性イソキノリンカルボキサミド誘導体 |
-
1996
- 1996-03-26 IL IL11765996A patent/IL117659A/xx not_active IP Right Cessation
- 1996-03-27 ZA ZA962438A patent/ZA962438B/xx unknown
- 1996-04-10 ES ES96909327T patent/ES2187644T3/es not_active Expired - Lifetime
- 1996-04-10 CZ CZ19973223A patent/CZ289093B6/cs not_active IP Right Cessation
- 1996-04-10 KR KR1019970707215A patent/KR100433589B1/ko not_active IP Right Cessation
- 1996-04-10 RO RO97-01858A patent/RO117532B1/ro unknown
- 1996-04-10 AT AT96909327T patent/ATE228113T1/de not_active IP Right Cessation
- 1996-04-10 RU RU97118591/04A patent/RU2160256C2/ru active
- 1996-04-10 DE DE69624916T patent/DE69624916T2/de not_active Expired - Fee Related
- 1996-04-10 WO PCT/JP1996/000977 patent/WO1996032383A1/ja active IP Right Grant
- 1996-04-10 AU AU52874/96A patent/AU694647B2/en not_active Ceased
- 1996-04-10 CN CN96194408A patent/CN1094929C/zh not_active Expired - Fee Related
- 1996-04-10 SK SK1374-97A patent/SK281840B6/sk unknown
- 1996-04-10 PT PT96909327T patent/PT826673E/pt unknown
- 1996-04-10 EP EP96909327A patent/EP0826673B1/en not_active Expired - Lifetime
- 1996-04-10 NZ NZ304982A patent/NZ304982A/xx unknown
- 1996-04-10 DK DK96909327T patent/DK0826673T3/da active
- 1996-04-10 HU HU9801688A patent/HUP9801688A3/hu unknown
- 1996-04-10 PL PL96322819A patent/PL322819A1/xx unknown
- 1996-04-10 CA CA002218033A patent/CA2218033A1/en not_active Abandoned
- 1996-04-10 US US08/930,604 patent/US5972946A/en not_active Expired - Fee Related
- 1996-04-10 BR BR9604894A patent/BR9604894A/pt not_active Application Discontinuation
- 1996-04-12 TW TW085104372A patent/TW450963B/zh not_active IP Right Cessation
- 1996-04-12 AR ARP960102179A patent/AR002289A1/es not_active Application Discontinuation
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1997
- 1997-10-10 NO NO19974685A patent/NO310619B1/no not_active IP Right Cessation
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