HUP0401403A2 - 2,4-diaminothiazole derivatives, their use and pharmaceutical compositions containing them - Google Patents
2,4-diaminothiazole derivatives, their use and pharmaceutical compositions containing themInfo
- Publication number
- HUP0401403A2 HUP0401403A2 HU0401403A HUP0401403A HUP0401403A2 HU P0401403 A2 HUP0401403 A2 HU P0401403A2 HU 0401403 A HU0401403 A HU 0401403A HU P0401403 A HUP0401403 A HU P0401403A HU P0401403 A2 HUP0401403 A2 HU P0401403A2
- Authority
- HU
- Hungary
- Prior art keywords
- meanings
- nitrogen atom
- compounds
- group
- diverse
- Prior art date
Links
- WKXCZMFWXZRMEZ-UHFFFAOYSA-N 1,3-thiazole-2,4-diamine Chemical class NC1=CSC(N)=N1 WKXCZMFWXZRMEZ-UHFFFAOYSA-N 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 3
- 238000002360 preparation method Methods 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- FHCSBLWRGCOVPT-UHFFFAOYSA-N AZD2858 Chemical compound C1CN(C)CCN1S(=O)(=O)C1=CC=C(C=2N=C(C(N)=NC=2)C(=O)NC=2C=NC=CC=2)C=C1 FHCSBLWRGCOVPT-UHFFFAOYSA-N 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 230000009286 beneficial effect Effects 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- -1 cyano- Chemical class 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000008103 glucose Substances 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 208000011580 syndromic disease Diseases 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/38—Nitrogen atoms
- C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Abstract
A találmány tárgyát új 2,4-diamino-tiazol származékok és ezekettartalmazó gyógyászati készítmények képezik. E vegyületek éskészítmények gátolják a GKS-3-t (glükogén-szintáz kináz-3) és ígyeredményesen alkalmazhatók olyan rendellenességek, szindrómák ésbetegségek, valamint állapotok kezelésére, ahol a GSK-3 gátlásaelőnyös, különösen az IGT (csökkent glükóz tolerancia), I- és II-típusú diabetes, elhízottság, valamint Alzheimer-betegség kezelésére.A találmány szerinti (I) általános képletű vegyületek képletében aszubsztituensek jelentése igen sokféle, így például A jelentésevegyértékkötés vagy alkiléncsoport, R1 és R2 a nitrogénatommal együtt,amelyhez kapcsolódnak 5-7 tagú gyűrűt képezhetnek, amelyben adottesetben egy kettős kötés és egy további nitrogénatom van jelen, amelygyűrű adott esetben 1-2 szubsztituenst hordozhat; R2 és R3 A-val, anitrogénatommal és a szénatommal együtt, amelyekhez kapcsolódnak, 5-7tagból álló gyűrűt képeznek, ami adott esetben szubsztituálva van,vagy R1 és R2 jelentése egymástól függetlenül -C(=O)OR, alkil-,cikloalkil-alkil-, heteroaril-alkil-csoport, ahol a R jelentése igensokféle lehet, B jelentése vegyértékkötés, -C(=O)-, -S(=O)- vagy -S(=O)2-; D jelentése is igen sokféle lehet, így példáulhidroxicsoport, halogénatom, ciano-, nitrocsoport, -NR22R23, ahol aR22 és R23 jelentése is igen sokféle lehet. A találmány tárgyáhoztartozik az új vegyületek alkalmazása is gyógyászati készítményekelőállítására. ÓThe subject of the invention is new 2,4-diaminothiazole derivatives and medicinal preparations containing them. These compounds and preparations inhibit GKS-3 (glucogen synthase kinase-3) and thus can be effectively used to treat disorders, syndromes and diseases, as well as conditions where GSK-3 inhibition is beneficial, especially IGT (reduced glucose tolerance), I- and For the treatment of type II diabetes, obesity and Alzheimer's disease. Substituents in the formula of the compounds of general formula (I) according to the invention have many different meanings, such as, for example, A means a valence bond or an alkylene group, R1 and R2 together with the nitrogen atom to which they are connected can form a 5-7 membered ring , in which a double bond and an additional nitrogen atom are optionally present, which ring may optionally carry 1-2 substituents; R2 and R3, together with A, a nitrogen atom and the carbon atom to which they are attached, form a 5-7-membered ring, which is optionally substituted, or R1 and R2 are independently -C(=O)OR, alkyl-, cycloalkyl-alkyl -, heteroarylalkyl group, where R can have many meanings, B means a valence bond, -C(=O)-, -S(=O)- or -S(=O)2-; The meanings of D can also be very diverse, such as, for example, hydroxy group, halogen atom, cyano-, nitro group, -NR22R23, where the meanings of R22 and R23 can be very diverse. The subject of the invention also includes the use of new compounds for the production of medicinal preparations. HE
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30995301P | 2001-08-03 | 2001-08-03 | |
| DKPA200101175 | 2001-08-03 | ||
| PCT/DK2002/000508 WO2003011843A1 (en) | 2001-08-03 | 2002-07-22 | Novel 2,4-diaminothiazole derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0401403A2 true HUP0401403A2 (en) | 2004-10-28 |
| HUP0401403A3 HUP0401403A3 (en) | 2005-11-28 |
Family
ID=26069057
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0401403A HUP0401403A3 (en) | 2001-08-03 | 2002-07-22 | 2,4-diaminothiazole derivatives, their use and pharmaceutical compositions containing them |
Country Status (6)
| Country | Link |
|---|---|
| EP (1) | EP1417188A1 (en) |
| JP (1) | JP2004538315A (en) |
| CA (1) | CA2455753A1 (en) |
| HU (1) | HUP0401403A3 (en) |
| MX (1) | MXPA04000906A (en) |
| WO (1) | WO2003011843A1 (en) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003072577A1 (en) * | 2002-02-28 | 2003-09-04 | F.Hoffmann-La Roche Ag | Thiazole derivatives as npy receptor antagonists |
| BR0313278A (en) | 2002-08-07 | 2005-07-05 | Hoffmann La Roche | Compounds, process for the preparation of a compound, pharmaceutical composition comprising the same and its use, method for treating and prophylaxis of diseases and obesity and use of the compounds |
| JP2007501824A (en) * | 2003-08-12 | 2007-02-01 | エフ．ホフマン−ラ ロシュ アーゲー | Thiazole derivatives as NPY antagonists |
| CA2562242A1 (en) * | 2004-04-13 | 2005-10-27 | Icagen, Inc. | Polycylic thiazoles as potassium ion channel modulators |
| US7423053B2 (en) * | 2004-07-15 | 2008-09-09 | Hoffmann-La Roche Inc. | 4-Aminothiazole derivatives |
| CN101084207A (en) | 2004-09-20 | 2007-12-05 | 泽农医药公司 | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
| EP2316458A1 (en) * | 2004-09-20 | 2011-05-04 | Xenon Pharmaceuticals Inc. | Pyridazine derivatives for inhibiting human stearoyl-coa-desaturase |
| US7592343B2 (en) | 2004-09-20 | 2009-09-22 | Xenon Pharmaceuticals Inc. | Pyridazine-piperazine compounds and their use as stearoyl-CoA desaturase inhibitors |
| CA2587601C (en) * | 2004-12-03 | 2017-11-07 | Rhode Island Hospital | Diagnosis and treatment of alzheimer's disease |
| US20080207594A1 (en) | 2005-05-04 | 2008-08-28 | Davelogen Aktiengesellschaft | Use of Gsk-3 Inhibitors for Preventing and Treating Pancreatic Autoimmune Disorders |
| EP1879591B8 (en) * | 2005-05-04 | 2012-04-04 | DeveloGen Aktiengesellschaft | Use of azapaullones for preventing and treating pancreatic autoimmune disorders |
| CN101208089A (en) | 2005-06-03 | 2008-06-25 | 泽农医药公司 | Aminothiazole derivatives as human stearoyl-CoA desaturase inhibitors |
| JP2009506069A (en) | 2005-08-26 | 2009-02-12 | ブレインセルス，インコーポレイティド | Neurogenesis through modulation of muscarinic receptors |
| EP2258359A3 (en) | 2005-08-26 | 2011-04-06 | Braincells, Inc. | Neurogenesis by muscarinic receptor modulation with sabcomelin |
| AU2006304787A1 (en) | 2005-10-21 | 2007-04-26 | Braincells, Inc. | Modulation of neurogenesis by PDE inhibition |
| CA2625210A1 (en) | 2005-10-31 | 2007-05-10 | Braincells, Inc. | Gaba receptor mediated modulation of neurogenesis |
| US20100216734A1 (en) | 2006-03-08 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis by nootropic agents |
| EP2377531A2 (en) | 2006-05-09 | 2011-10-19 | Braincells, Inc. | Neurogenesis by modulating angiotensin |
| KR100670974B1 (en) * | 2006-09-18 | 2007-02-28 | (주) 리드제넥스 | Molecular diversity technology of thiazole library based on combinatorial chemistry |
| US20100184806A1 (en) | 2006-09-19 | 2010-07-22 | Braincells, Inc. | Modulation of neurogenesis by ppar agents |
| US20100216805A1 (en) | 2009-02-25 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis using d-cycloserine combinations |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| YU22400A (en) * | 1997-10-27 | 2003-08-29 | Agouron Pharmaceuticals Inc. | Substituted 4-amino-thiazol-2-y compounds as cdks inhibitors |
| ATE284387T1 (en) * | 1998-10-08 | 2004-12-15 | Smithkline Beecham Plc | 3-(3-CHLORO-4-HYDROXYPHENYLAMINO)-4-(2-NITROPHENYL)-1H-PYRROL-2,5-DIONE AS A GLYCOGEN SYNTHASE KINASE-3 INHIBITOR (GSK-3) |
| US6214852B1 (en) * | 1998-10-21 | 2001-04-10 | Bristol-Myers Squibb Company | N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases |
| GB9918180D0 (en) * | 1999-08-02 | 1999-10-06 | Smithkline Beecham Plc | Novel compositions |
| AU2001230026A1 (en) * | 2000-02-04 | 2001-08-14 | Novo-Nordisk A/S | 2,4-diaminothiazole derivatives |
| GB0008264D0 (en) * | 2000-04-04 | 2000-05-24 | Smithkline Beecham Plc | Novel method and compounds |
-
2002
- 2002-07-22 EP EP02750845A patent/EP1417188A1/en not_active Withdrawn
- 2002-07-22 HU HU0401403A patent/HUP0401403A3/en unknown
- 2002-07-22 WO PCT/DK2002/000508 patent/WO2003011843A1/en not_active Application Discontinuation
- 2002-07-22 CA CA002455753A patent/CA2455753A1/en not_active Abandoned
- 2002-07-22 MX MXPA04000906A patent/MXPA04000906A/en unknown
- 2002-07-22 JP JP2003517035A patent/JP2004538315A/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| EP1417188A1 (en) | 2004-05-12 |
| HUP0401403A3 (en) | 2005-11-28 |
| JP2004538315A (en) | 2004-12-24 |
| MXPA04000906A (en) | 2004-11-22 |
| CA2455753A1 (en) | 2003-02-13 |
| WO2003011843A1 (en) | 2003-02-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD9A | Lapse of provisional protection due to non-payment of fees |