DE60228053D1 - Benzamidinderivate mit entzündungshemmender und immunsuppressiver wirkung - Google Patents
Benzamidinderivate mit entzündungshemmender und immunsuppressiver wirkungInfo
- Publication number
- DE60228053D1 DE60228053D1 DE60228053T DE60228053T DE60228053D1 DE 60228053 D1 DE60228053 D1 DE 60228053D1 DE 60228053 T DE60228053 T DE 60228053T DE 60228053 T DE60228053 T DE 60228053T DE 60228053 D1 DE60228053 D1 DE 60228053D1
- Authority
- DE
- Germany
- Prior art keywords
- group
- carbon atoms
- hydrogen
- methyl
- selected independently
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 230000000947 anti-immunosuppressive effect Effects 0.000 title 1
- 230000003110 anti-inflammatory effect Effects 0.000 title 1
- PXXJHWLDUBFPOL-UHFFFAOYSA-N benzamidine Chemical class NC(=N)C1=CC=CC=C1 PXXJHWLDUBFPOL-UHFFFAOYSA-N 0.000 title 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- -1 methoxy, ethoxy, propoxy group Chemical group 0.000 abstract 2
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 abstract 1
- 125000000320 amidine group Chemical group 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000005392 carboxamide group Chemical group NC(=O)* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- CYEBJEDOHLIWNP-UHFFFAOYSA-N methanethioamide Chemical group NC=S CYEBJEDOHLIWNP-UHFFFAOYSA-N 0.000 abstract 1
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/36—Radicals substituted by singly-bound nitrogen atoms
- C07D213/40—Acylated substituent nitrogen atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
- C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
- C07C257/14—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to acyclic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
- C07C279/18—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to carbon atoms of six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
- C07C279/30—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to nitro or nitroso groups
- C07C279/32—N-nitroguanidines
- C07C279/36—Substituted N-nitroguanidines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C335/00—Thioureas, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
- C07C335/04—Derivatives of thiourea
- C07C335/16—Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C335/20—Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/40—Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
-
- 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
- C07D277/44—Acylated amino or imino radicals
- C07D277/48—Acylated amino or imino radicals by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof, e.g. carbonylguanidines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/14—The ring being saturated
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2603/00—Systems containing at least three condensed rings
- C07C2603/56—Ring systems containing bridged rings
- C07C2603/58—Ring systems containing bridged rings containing three rings
- C07C2603/70—Ring systems containing bridged rings containing three rings containing only six-membered rings
- C07C2603/74—Adamantanes
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT2001TO000110A ITTO20010110A1 (it) | 2001-02-08 | 2001-02-08 | Nuovi derivati benzamidinici dotati di attivita' anti-infiammatoria ed immunosoppressiva. |
| PCT/EP2002/001201 WO2002070468A2 (en) | 2001-02-08 | 2002-02-06 | Novel benzamidine derivatives having anti-inflammatory and immunosuppressive activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DE60228053D1 true DE60228053D1 (de) | 2008-09-18 |
Family
ID=11458519
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60228053T Expired - Lifetime DE60228053D1 (de) | 2001-02-08 | 2002-02-06 | Benzamidinderivate mit entzündungshemmender und immunsuppressiver wirkung |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US7202277B2 (de) |
| EP (1) | EP1363875B1 (de) |
| JP (1) | JP4104984B2 (de) |
| AT (1) | ATE403645T1 (de) |
| AU (1) | AU2002249183B2 (de) |
| CA (1) | CA2437109C (de) |
| DE (1) | DE60228053D1 (de) |
| DK (1) | DK1363875T3 (de) |
| ES (1) | ES2311600T3 (de) |
| IT (1) | ITTO20010110A1 (de) |
| PT (1) | PT1363875E (de) |
| WO (1) | WO2002070468A2 (de) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ITTO20010110A1 (it) * | 2001-02-08 | 2002-08-08 | Rotta Research Lab | Nuovi derivati benzamidinici dotati di attivita' anti-infiammatoria ed immunosoppressiva. |
| US8450302B2 (en) * | 2002-08-02 | 2013-05-28 | Ab Science | 2-(3-aminoaryl) amino-4-aryl-thiazoles and their use as c-kit inhibitors |
| ES2294344T3 (es) * | 2002-08-02 | 2008-04-01 | Ab Science | 2-(3-aminoaril)amino-4-aril-tiazoles y su utilizacion como inhibidores de c-kit. |
| US7208491B2 (en) * | 2003-02-07 | 2007-04-24 | Hoffmann-La Roche Inc. | N-monoacylated o-phenylenediamines |
| SE0301446D0 (sv) | 2003-05-16 | 2003-05-16 | Astrazeneca Ab | New Compounds |
| ITTO20030668A1 (it) | 2003-09-02 | 2005-03-03 | Rotta Res Lab S P A O Ra Rottapharm | Derivati dell'adamantano dotati di attivita' neuroprotettiva, antidepressiva e anti-ischemica e procedimento per la loro preparazione. |
| FR2865133B1 (fr) * | 2004-01-19 | 2008-01-18 | Rytek | Compositions pour le traitement de pathologies digestives |
| EP1704860B1 (de) * | 2005-03-24 | 2010-10-27 | Rottapharm S.P.A. | Benzamidin Derivative zur Behandlung und Vorbeugung von Mucositis |
| UY30048A1 (es) | 2005-12-23 | 2007-07-31 | Astrazeneca Ab | Derivados sustituidos de la n,2-(1h-benzimidazol-1-il) acetamida, composiciones farmacéuticas conteniéndolos, procesos de preparación y aplicaciones |
| TWI433839B (zh) | 2006-08-11 | 2014-04-11 | Neomed Inst | 新穎的苯并咪唑衍生物290 |
| CA2808582A1 (en) | 2009-08-14 | 2011-02-17 | University Of Virginia Patent Foundation | Imidamide sphingosine kinase inhibitors |
| CN102344391B (zh) * | 2011-07-28 | 2013-12-25 | 山东新华制药股份有限公司 | N-(4-乙酰氨基苯基)-n′，n′-二甲基乙脒的合成方法 |
| WO2013083813A2 (en) * | 2011-12-07 | 2013-06-13 | Universität Zürich | Modulators of spermine/spermidine n'-acetyltransferase (ssat) and ssat associated proteins for use in prevention or treatment of rheumatoid arthritis |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE950637C (de) * | 1944-05-27 | 1956-10-11 | Hoechst Ag | Verfahren zur Herstellung von 4-Aminochinaldinverbindungen |
| US2559085A (en) * | 1948-10-22 | 1951-07-03 | Honorary Advisory Council Sci | Preparation of n-substituted-n'-nitroguanidines |
| GB1311432A (en) * | 1971-01-07 | 1973-03-28 | Ici Ltd | Guanidine derivatives their preparation and antiviral compositions containing them |
| FR2456731A1 (fr) | 1979-05-16 | 1980-12-12 | Choay Sa | Nouveaux derives substitues d'ary |
| US5028627A (en) | 1989-09-13 | 1991-07-02 | Cornell Research Foundation, Inc. | Method of using arginine derivatives to inhibit systemic hypotension associated with nitric oxide production or endothelial derived relaxing factor |
| US5240694A (en) * | 1991-09-23 | 1993-08-31 | University Of Virginia | Combined antiviral and antimediator treatment of common colds |
| GB9127376D0 (en) | 1991-12-24 | 1992-02-19 | Wellcome Found | Amidino derivatives |
| GB9312761D0 (en) | 1993-06-21 | 1993-08-04 | Wellcome Found | Amino acid derivatives |
| CZ293323B6 (cs) * | 1995-08-30 | 2004-04-14 | G. D. Searle & Co. | Meta-guanidinové, močovinové, thiomočovinové nebo azacyklické deriváty aminobenzoové kyseliny jako antagonisty integrinů |
| WO1997036859A1 (en) | 1996-03-29 | 1997-10-09 | G.D. Searle & Co. | Para-substituted phenylpropanoic acid derivatives as integrin antagonists |
| ATE204857T1 (de) * | 1996-03-29 | 2001-09-15 | Searle & Co | Meta-substituierte phenylenderivate und ihre verwendung als alphavbeta3 intergrin-antagonisten oder inhibitoren |
| US20020052343A1 (en) | 1999-12-15 | 2002-05-02 | Allen Darin Arthur | Salicylamides as serine protease inhibitors |
| ITTO20010110A1 (it) * | 2001-02-08 | 2002-08-08 | Rotta Research Lab | Nuovi derivati benzamidinici dotati di attivita' anti-infiammatoria ed immunosoppressiva. |
-
2001
- 2001-02-08 IT IT2001TO000110A patent/ITTO20010110A1/it unknown
-
2002
- 2002-02-06 JP JP2002569789A patent/JP4104984B2/ja not_active Expired - Fee Related
- 2002-02-06 DE DE60228053T patent/DE60228053D1/de not_active Expired - Lifetime
- 2002-02-06 CA CA2437109A patent/CA2437109C/en not_active Expired - Fee Related
- 2002-02-06 DK DK02718096T patent/DK1363875T3/da active
- 2002-02-06 PT PT02718096T patent/PT1363875E/pt unknown
- 2002-02-06 AU AU2002249183A patent/AU2002249183B2/en not_active Ceased
- 2002-02-06 AT AT02718096T patent/ATE403645T1/de active
- 2002-02-06 WO PCT/EP2002/001201 patent/WO2002070468A2/en active IP Right Grant
- 2002-02-06 ES ES02718096T patent/ES2311600T3/es not_active Expired - Lifetime
- 2002-02-06 EP EP02718096A patent/EP1363875B1/de not_active Expired - Lifetime
- 2002-02-06 US US10/467,624 patent/US7202277B2/en not_active Expired - Fee Related
-
2007
- 2007-01-12 US US11/652,675 patent/US20070135523A1/en not_active Abandoned
-
2008
- 2008-04-30 US US12/112,299 patent/US7560591B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| CA2437109C (en) | 2010-07-06 |
| EP1363875A2 (de) | 2003-11-26 |
| CA2437109A1 (en) | 2002-09-12 |
| PT1363875E (pt) | 2008-08-22 |
| WO2002070468A2 (en) | 2002-09-12 |
| JP4104984B2 (ja) | 2008-06-18 |
| DK1363875T3 (da) | 2008-11-24 |
| ITTO20010110A0 (it) | 2001-02-08 |
| AU2002249183B2 (en) | 2006-11-16 |
| US20080207764A1 (en) | 2008-08-28 |
| US20040110801A1 (en) | 2004-06-10 |
| ITTO20010110A1 (it) | 2002-08-08 |
| ATE403645T1 (de) | 2008-08-15 |
| US20070135523A1 (en) | 2007-06-14 |
| US7560591B2 (en) | 2009-07-14 |
| EP1363875B1 (de) | 2008-08-06 |
| US7202277B2 (en) | 2007-04-10 |
| JP2004531489A (ja) | 2004-10-14 |
| WO2002070468A3 (en) | 2003-09-04 |
| ES2311600T3 (es) | 2009-02-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8364 | No opposition during term of opposition |