HUP9701714A2 - Indole derivatives neuropeptide y receptor antagonists, use thereof and pharmaceutical compositions containing these compounds - Google Patents
Indole derivatives neuropeptide y receptor antagonists, use thereof and pharmaceutical compositions containing these compoundsInfo
- Publication number
- HUP9701714A2 HUP9701714A2 HU9701714A HUP9701714A HUP9701714A2 HU P9701714 A2 HUP9701714 A2 HU P9701714A2 HU 9701714 A HU9701714 A HU 9701714A HU P9701714 A HUP9701714 A HU P9701714A HU P9701714 A2 HUP9701714 A2 HU P9701714A2
- Authority
- HU
- Hungary
- Prior art keywords
- alkyl
- powder
- atom
- pipe
- hydrogen
- Prior art date
Links
- 229940054051 antipsychotic indole derivative Drugs 0.000 title abstract 2
- 150000002475 indoles Chemical class 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 title 1
- 239000002660 neuropeptide Y receptor antagonist Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 239000000843 powder Substances 0.000 abstract 10
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 8
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- -1 piperidinyl - Chemical class 0.000 abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 239000000126 substance Substances 0.000 abstract 3
- 125000001589 carboacyl group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000001624 naphthyl group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 2
- 125000004621 quinuclidinyl group Chemical group N12C(CC(CC1)CC2)* 0.000 abstract 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 abstract 1
- 125000004450 alkenylene group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 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
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000005046 dihydronaphthyl group Chemical group 0.000 abstract 1
- 125000002541 furyl group Chemical group 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000002636 imidazolinyl group Chemical group 0.000 abstract 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 1
- 125000002098 pyridazinyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 abstract 1
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 abstract 1
- 125000003831 tetrazolyl group Chemical group 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D209/12—Radicals substituted by oxygen atoms
-
- 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
- C07D209/10—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
- C07D209/16—Tryptamines
-
- 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
- C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D209/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an alkyl or cycloalkyl radical attached to the ring nitrogen atom
-
- 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
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- C07D403/06—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 carbon chain containing only aliphatic carbon 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
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Abstract
Az indőlszármazékők (I) általánős képletében Rb jelentése hidrőgén-,halőgénatőm, hidrőxil-, alkil-, alkőxi-, alkanőil- vagy triflűőr-metil-csőpőrt; R1 jelentése hidrőgénatőm, ak vagy -(CH2)vR1a általánősképletű csőpőrt, ahől v értéke 1-12 közötti szám és R1a jelentéseadőtt esetben szűbsztitűált fenil-, naftil-, hexametilén-iminil-,heptametilén-minil-, piperazinil-, imidazőlinil-, piperidinil-,triptőlinil-, pirrőlidinil-, kinűklidinil- vagy mőrfőlinilcsőpőrt; Ajelentése kémiai kötés, -(CH2)m- vagy -C(O)- csőpőrt; A1 jelentésekémiai kötés, -NRa-, -O-, -(CH2)m- vagy -S(O)n-csőpőrt, ahől m értéke0-6 közötti és n értéke 0, 1 vagy 2 egész szám, és Ra jelentésehidrőgénatőm, alkil- vagy alkanőilcsőpőrt; D jelentése kémiai kötés,alkeniléncsőpőrt vagy -C(X)(Y)- általánős képletű csőpőrt, ahől az Xés Y csőpőrtők egyikének jelentése hidrőxilcsőpőrt, a másikéhidrőgénatőm, vagy mindkettő hidrőgénatőm, vagy X és Y együtt =0 vagy=NORc csőpőrtőt alkőt, ahől Rc hidrőgénatőm, benzil-, acetil-,benzőil- vagy alkilcsőpőrt; R2 jelentése hidrőxil-, alkil-, alkőxi-,fenőxicsőpőrt, adőtt esetben szűbsztitűált aminőcsőpőrt vagy ennekkvaternerizált származéka vagy adőtt esetben szűbsztitűáltheterőciklűsős csőpőrt; R jelentése adőtt esetben szűbsztitűáltfenil-, naftil-, dihidrőnaftil-, tetrahidrőnaftil-, ciklőalkil-,alkil-, pirazinil-, tiazőlil-, fűril-, pirimidil-, piridinil-,kinőlinil-, izőkinőlinil-, őxazőlil-, piridazinil-, imidazőlil-,triazőlil-, tetrazőlil-, piperidinil-, pirrőlidinil-, kinűklidinil-,mőrfőlinil-, hexametilén-iminil- vagy heptametilén-iminil-csőpőrt; X1és Y1 közül az egyik jelentése hidrőgénatőm, a másiké hidrőxilcsőpőrt,X1 és Y1 együtt =O vagy NOR9 csőpőrtőt alkőt, ahől R9 jelentésehidrőgénatőm vagy alkilcsőpőrt. p, q és s értéke 0-6 közötti egészszám. ŕIn the general formula of the indole derivatives (I), Rb is hydrogen, halogen atom, hydroxyl, alkyl, alkyloxy, alkanoyl or trifluoromethyl; R1 is a hydrogen atom, ak or -(CH2)vR1a, where v is a number between 1-12 and R1a is optionally substituted phenyl, naphthyl, hexamethyleneiminyl, heptamethyleneminyl, piperazinyl, imidazolinyl, piperidinyl -, tryptolinyl, pyrrolidinyl, quinuclidinyl or mórpholinyl pipe powder; It means a chemical bond, -(CH2)m- or -C(O)- tube powder; A1 is a chemical bond, -NRa-, -O-, -(CH2)m- or -S(O)n-, where m is between 0-6 and n is an integer of 0, 1 or 2, and Ra is a hydrogen atom, alkyl - or alkanoyl tube powder; D is a chemical bond, an alkenylene pipe powder or a pipe powder with the general formula -C(X)(Y)-, where one of the pipe powders X and Y is a hydroxyl pipe powder, the other is a hydrogen atom, or both are hydrogen atoms, or X and Y together form =0 or =NORc pipe powder, from which Rc is a hydrogen, benzyl, acetyl, benzoyl or alkyl group; R2 means hydroxyl-, alkyl-, alkyl-, phenoxy-, or, where applicable, reduced-substituted amino-tube powder or its quaternized derivative, or, where applicable, reduced-substituted power-cyclic tube powder; R is optionally substituted phenyl, naphthyl, dihydronaphthyl, tetrahydronaphthyl, cycloalkyl, alkyl, pyrazinyl, thiazolyl, furyl, pyrimidyl, pyridinyl, quinolinyl, isoquinolinyl, oxazolyl, pyridazinyl, imidazolyl -triazolyl, tetrazolyl, piperidinyl, pyrrolidinyl, quinuclidinyl, mórpholinyl, hexamethyleneiminyl or heptamethyleneiminyl; One of X1 and Y1 represents a hydrogen atom, the other represents a hydroxyl atom, X1 and Y1 together form =O or NOR9 an atom, from which R9 represents a hydrogen atom or an alkyl atom. The values of p, q and s are integers between 0 and 6. ŕ
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US315095P | 1995-09-01 | 1995-09-01 | |
GBGB9523999.2A GB9523999D0 (en) | 1995-11-23 | 1995-11-23 | Indolyl neuropeptide y receptor antagonists |
US2163896P | 1996-07-12 | 1996-07-12 | |
PCT/US1996/014163 WO1997009308A1 (en) | 1995-09-01 | 1996-08-30 | Indolyl neuropeptide y receptor antagonists |
Publications (2)
Publication Number | Publication Date |
---|---|
HUP9701714A2 true HUP9701714A2 (en) | 1999-06-28 |
HUP9701714A3 HUP9701714A3 (en) | 2000-03-28 |
Family
ID=27267993
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU9701714A HUP9701714A3 (en) | 1995-09-01 | 1996-08-30 | Indole derivatives neuropeptide y receptor antagonists, use thereof and pharmaceutical compositions containing these compounds |
Country Status (14)
Country | Link |
---|---|
EP (1) | EP0789688A4 (en) |
CN (1) | CN1173867A (en) |
AU (1) | AU717422B2 (en) |
BR (1) | BR9606619A (en) |
CA (1) | CA2203912A1 (en) |
CZ (1) | CZ132897A3 (en) |
HU (1) | HUP9701714A3 (en) |
IL (1) | IL120724A0 (en) |
MX (1) | MX9703186A (en) |
NO (1) | NO308296B1 (en) |
NZ (1) | NZ318228A (en) |
PL (1) | PL320010A1 (en) |
TR (1) | TR199700334T1 (en) |
WO (1) | WO1997009308A1 (en) |
Families Citing this family (58)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU729590B2 (en) * | 1996-10-23 | 2001-02-08 | Sanofi-Aventis | Cosmetic composition containing a neuropeptide Y receptor antagonist |
US6143931A (en) | 1997-04-16 | 2000-11-07 | Arqule, Inc. | Synthesis and use of α-ketoamide derivatives and arrays |
DE69808266D1 (en) * | 1997-04-16 | 2002-10-31 | Arqule Inc | PRODUCTION AND USE OF ALPHA KETOAMIDE DERIVATIVES AND ARRANGEMENTS |
US6337332B1 (en) | 1998-09-17 | 2002-01-08 | Pfizer Inc. | Neuropeptide Y receptor antagonists |
US6200990B1 (en) * | 1998-12-21 | 2001-03-13 | Alcon Laboratories, Inc. | Neuroprotective agents having antioxidant and NMDA antagonist activity |
AU3840000A (en) * | 1999-04-20 | 2000-11-02 | Meiji Seika Kaisha Ltd. | Tricyclic compounds |
US6469006B1 (en) * | 1999-06-15 | 2002-10-22 | Bristol-Myers Squibb Company | Antiviral indoleoxoacetyl piperazine derivatives |
MXPA00006605A (en) | 1999-07-02 | 2004-12-09 | Pfizer | Bicycliccarbonyl indole compounds as anti-inflammatory/analgesic agents. |
CA2399791A1 (en) | 2000-02-11 | 2001-08-16 | Bristol-Myers Squibb Company | Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases |
EP1265607A2 (en) * | 2000-03-09 | 2002-12-18 | Eli Lilly And Company | METHOD FOR THE TREATMENT OF RENAL DYSFUNCTION WITH sPLA 2 INHIBITORS |
US6900226B2 (en) | 2000-09-06 | 2005-05-31 | Hoffman-La Roche Inc. | Neuropeptide Y antagonists |
TWI224101B (en) | 2001-06-20 | 2004-11-21 | Wyeth Corp | Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1) |
WO2003000253A1 (en) | 2001-06-20 | 2003-01-03 | Wyeth | Substituted indole acid derivatives as inhibitors of plasminogen activator inhibitor-1 (pai-1) |
US6673829B2 (en) | 2001-09-14 | 2004-01-06 | Novo Nordisk A/S | Aminoazetidine,-pyrrolidine and -piperidine derivatives |
EP1430027B1 (en) | 2001-09-14 | 2010-09-01 | High Point Pharmaceuticals, LLC | Novel aminoazetidine, -pyrrolidine and -piperidine derivatives |
PT1501826E (en) | 2002-02-01 | 2007-01-31 | Hoffmann La Roche | Substituted indoles as alpha-1 agonists |
DE60324183D1 (en) | 2002-12-10 | 2008-11-27 | Wyeth Corp | Aryl-, aryloxy- und alkyloxysubstituierte 1h-indol-3-yl-glyoxylsäurederivateals inhibitoren des plasminogenaktivatorinhibitors-1 (pai-1) |
DE60306547T2 (en) | 2002-12-10 | 2007-06-28 | Wyeth | SUBSTITUTED 3-ALKYL AND 3-ARYL ALKYL-1H-INDOL-1-YL-ACETIC ACID DERIVATIVES AS PLASMINOGEN ACTIVATOR |
JP2006514637A (en) | 2002-12-10 | 2006-05-11 | ワイス | Substituted 3-carbonyl-1H-indol-1-ylacetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) |
ES2325071T3 (en) | 2002-12-10 | 2009-08-25 | Wyeth | DERIVATIVES OF INDOL-OXO-ACETILAMINOACETIC ACID REPLACED AS INHIBITORS OF THE PLASMINOGEN-1 ACTIVATOR INHIBITOR (PAI-1). |
UA80453C2 (en) | 2002-12-10 | 2007-09-25 | Derivatives of substituted dyhydropyranoindol-3,4-dion as inhibitors of plasminogen activator inhibitor-1 (pai-1) | |
US7589207B2 (en) | 2002-12-13 | 2009-09-15 | Smithkline Beecham Corporation | Cyclohexyl compounds as CCR5 antagonists |
ATE462432T1 (en) | 2003-05-05 | 2010-04-15 | Probiodrug Ag | GLUTAMINYL CYCLASE INHIBITORS |
US7317025B2 (en) | 2003-09-24 | 2008-01-08 | Johnson & Johnson Pharmaceutical Research & Development, Llc | Non-peptidic NPY Y2 receptor inhibitors |
US7582773B2 (en) | 2003-09-25 | 2009-09-01 | Wyeth | Substituted phenyl indoles |
US7332521B2 (en) | 2003-09-25 | 2008-02-19 | Wyeth | Substituted indoles |
US7446201B2 (en) | 2003-09-25 | 2008-11-04 | Wyeth | Substituted heteroaryl benzofuran acids |
US7351726B2 (en) | 2003-09-25 | 2008-04-01 | Wyeth | Substituted oxadiazolidinediones |
US7342039B2 (en) | 2003-09-25 | 2008-03-11 | Wyeth | Substituted indole oximes |
US7442805B2 (en) | 2003-09-25 | 2008-10-28 | Wyeth | Substituted sulfonamide-indoles |
US7411083B2 (en) | 2003-09-25 | 2008-08-12 | Wyeth | Substituted acetic acid derivatives |
US7420083B2 (en) | 2003-09-25 | 2008-09-02 | Wyeth | Substituted aryloximes |
US7163954B2 (en) | 2003-09-25 | 2007-01-16 | Wyeth | Substituted naphthyl benzothiophene acids |
US7141592B2 (en) | 2003-09-25 | 2006-11-28 | Wyeth | Substituted oxadiazolidinediones |
US7268159B2 (en) | 2003-09-25 | 2007-09-11 | Wyeth | Substituted indoles |
US7265148B2 (en) | 2003-09-25 | 2007-09-04 | Wyeth | Substituted pyrrole-indoles |
AU2004290499C1 (en) | 2003-11-03 | 2011-02-24 | Probiodrug Ag | Combinations useful for the treatment of neuronal disorders |
BRPI0507485A (en) | 2004-02-05 | 2007-07-10 | Probiodrug Ag | new glutaminyl cyclase inhibitors |
CA2577857A1 (en) | 2004-08-23 | 2006-03-02 | Wyeth | Oxazolo-naphthyl acids as plaminogen activator inhibtor type-1 (pai-1) modulators useful in the treatment of thrombosis and cardiovascular diseases |
WO2006081455A1 (en) | 2005-01-27 | 2006-08-03 | Wyeth | Processes and compounds for the preparation of substituted naphthylindole derivatives |
WO2007022321A2 (en) | 2005-08-17 | 2007-02-22 | Wyeth | Substituted indoles and use thereof |
WO2007046112A1 (en) * | 2005-10-19 | 2007-04-26 | Suven Life Sciences Inc. | Arylthioether tryptamine derivatives as functional 5-ht6 ligands |
EP2089383B1 (en) | 2006-11-09 | 2015-09-16 | Probiodrug AG | 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases |
JP5523107B2 (en) | 2006-11-30 | 2014-06-18 | プロビオドルグ エージー | Novel inhibitors of glutaminyl cyclase |
ZA200905537B (en) | 2007-03-01 | 2010-10-27 | Probiodrug Ag | New use of glutaminyl cyclase inhibitors |
ES2533484T3 (en) | 2007-04-18 | 2015-04-10 | Probiodrug Ag | Thiourea derivatives as glutaminyl cyclase inhibitors |
MY160771A (en) | 2008-06-19 | 2017-03-15 | Takeda Pharmaceuticals Co | Heterocyclic compound and use thereof |
DK2475428T3 (en) | 2009-09-11 | 2015-09-28 | Probiodrug Ag | Heterocyclic derivatives as glutaminylcyklaseinhibitorer |
WO2011107530A2 (en) | 2010-03-03 | 2011-09-09 | Probiodrug Ag | Novel inhibitors |
CN102791704B (en) | 2010-03-10 | 2015-11-25 | 前体生物药物股份公司 | The heterocycle inhibitor of glutaminyl cyclase (QC, EC 2.3.2.5) |
JP5945532B2 (en) | 2010-04-21 | 2016-07-05 | プロビオドルグ エージー | Benzimidazole derivatives as inhibitors of glutaminyl cyclase |
ES2570167T3 (en) | 2011-03-16 | 2016-05-17 | Probiodrug Ag | Benzimidazole derivatives as glutaminyl cyclase inhibitors |
LT2707101T (en) | 2011-05-12 | 2019-05-27 | Proteostasis Therapeutics, Inc. | Proteostasis regulators |
WO2012168697A1 (en) | 2011-06-06 | 2012-12-13 | Imperial Innovations Limited | Methods to predict binding affinity of tspo imaging agents to tspo |
CN104829465B (en) | 2015-02-13 | 2018-04-27 | 普济生物科技(台州)有限公司 | A kind of preparation method of 4- isopropylaminos-n-butyl alcohol |
CN105949135A (en) * | 2016-05-10 | 2016-09-21 | 湖南欧亚生物有限公司 | Synthetic method of selexipag |
EP3461819B1 (en) | 2017-09-29 | 2020-05-27 | Probiodrug AG | Inhibitors of glutaminyl cyclase |
CN111377821A (en) * | 2018-12-28 | 2020-07-07 | 南京艾德凯腾生物医药有限责任公司 | Method for synthesizing 4-isopropylamino-1-butanol |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE2931323A1 (en) * | 1979-08-02 | 1981-02-26 | Kali Chemie Pharma Gmbh | NEW N-AMINOALKYLINDOL DERIVATIVES AND THEIR SALTS |
US5264420A (en) * | 1990-09-27 | 1993-11-23 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
US5206382A (en) * | 1991-06-27 | 1993-04-27 | Fidia Georgetown Institute For The Neurosciences | Indole derivatives, pharmaceutical compositions and methods of treating neurological and psychiatric disorders |
WO1993023374A1 (en) * | 1992-05-08 | 1993-11-25 | Otsuka Pharmaceutical Factory, Inc. | Indole derivative |
TW270114B (en) * | 1993-10-22 | 1996-02-11 | Hoffmann La Roche | |
WO1996012489A1 (en) * | 1994-10-20 | 1996-05-02 | Eli Lilly And Company | Bicyclic neuropeptide y receptor antagonists |
-
1996
- 1996-08-30 HU HU9701714A patent/HUP9701714A3/en unknown
- 1996-08-30 WO PCT/US1996/014163 patent/WO1997009308A1/en not_active Application Discontinuation
- 1996-08-30 BR BR9606619A patent/BR9606619A/en unknown
- 1996-08-30 EP EP96930691A patent/EP0789688A4/en not_active Withdrawn
- 1996-08-30 CN CN96191324A patent/CN1173867A/en active Pending
- 1996-08-30 MX MX9703186A patent/MX9703186A/en unknown
- 1996-08-30 IL IL12072496A patent/IL120724A0/en unknown
- 1996-08-30 NZ NZ318228A patent/NZ318228A/en unknown
- 1996-08-30 PL PL96320010A patent/PL320010A1/en unknown
- 1996-08-30 TR TR97/00334T patent/TR199700334T1/en unknown
- 1996-08-30 CZ CZ971328A patent/CZ132897A3/en unknown
- 1996-08-30 AU AU69650/96A patent/AU717422B2/en not_active Ceased
- 1996-08-30 CA CA002203912A patent/CA2203912A1/en not_active Abandoned
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1997
- 1997-04-30 NO NO972016A patent/NO308296B1/en not_active IP Right Cessation
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CA2203912A1 (en) | 1997-03-13 |
NZ318228A (en) | 1999-07-29 |
EP0789688A4 (en) | 1997-11-19 |
TR199700334T1 (en) | 1997-08-21 |
NO972016L (en) | 1997-06-17 |
NO308296B1 (en) | 2000-08-28 |
WO1997009308A1 (en) | 1997-03-13 |
CN1173867A (en) | 1998-02-18 |
EP0789688A1 (en) | 1997-08-20 |
PL320010A1 (en) | 1997-09-01 |
NO972016D0 (en) | 1997-04-30 |
AU717422B2 (en) | 2000-03-23 |
MX9703186A (en) | 1997-07-31 |
AU6965096A (en) | 1997-03-27 |
BR9606619A (en) | 1997-12-23 |
IL120724A0 (en) | 1997-08-14 |
HUP9701714A3 (en) | 2000-03-28 |
CZ132897A3 (en) | 1997-11-12 |
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