HUP0105432A2 - Integrin-antagonista hatású új bifenil és bifenil-analóg vegyületek, eljárás előállításukra és ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents
Integrin-antagonista hatású új bifenil és bifenil-analóg vegyületek, eljárás előállításukra és ezeket tartalmazó gyógyszerkészítmények és alkalmazásukInfo
- Publication number
- HUP0105432A2 HUP0105432A2 HU0105432A HUP0105432A HUP0105432A2 HU P0105432 A2 HUP0105432 A2 HU P0105432A2 HU 0105432 A HU0105432 A HU 0105432A HU P0105432 A HUP0105432 A HU P0105432A HU P0105432 A2 HUP0105432 A2 HU P0105432A2
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- HU
- Hungary
- Prior art keywords
- biphenyl
- group
- cycloalkyl
- aryl
- alkyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 title 2
- 239000005557 antagonist Substances 0.000 title 1
- 235000010290 biphenyl Nutrition 0.000 title 1
- 239000004305 biphenyl Substances 0.000 title 1
- 102000006495 integrins Human genes 0.000 title 1
- 108010044426 integrins Proteins 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000002947 alkylene group Chemical group 0.000 abstract 3
- 150000003973 alkyl amines Chemical group 0.000 abstract 2
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 2
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 abstract 2
- 101150047265 COR2 gene Proteins 0.000 abstract 1
- 125000000520 N-substituted aminocarbonyl group Chemical group [*]NC(=O)* 0.000 abstract 1
- 101100467189 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) QCR2 gene Proteins 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000005556 thienylene group Chemical group 0.000 abstract 1
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- 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
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- C07D213/40—Acylated substituent nitrogen atom
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- C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
- C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
- C07C311/19—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
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- C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
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Abstract
A találmány tárgyát az (1) általános képletű vegyületek,gyógyászatilag elfogadható sóik és sztereoizomerjeik képezik, ahol aképletben R1 jelentése hidrogénatom, alkil-, cikloalkil-, aril- vagyheterociklusos csoport, melyek szubsztituáltak lehetnek; R2 jelentésehidrogénatom, alkil-, cikloalkil-, aril-, alkenil-, alkinil- vagyheterociklusos csoport, továbbá -NR2'SO2R2<, -NR2'COOR2', -NR2'COR2',-NR2'CONR2'2 vagy -NR2'CSNR2'2; U jelentése kötés vagy alkiléncsoport;V jelentése alkiléncsoport, -NR2'CO- vagy -NR2'SO2-; A és B jelentésefeniléncsoport vagy tieniléncsoport; W jelentése kötés vagyalkiléncsoport, ahol U, V, A, B és W jelentésében a csoportokszubsztituáltak lehetnek; C jelentése (b) vagy (c) általános képletűcsoport; R3 jelentése hidrogénatom, alkil-, cikloalkil-, aril-,alkilamin-, alkilamid- vagy heterociklusos csoport, vagy R3 lehetheterociklusos gyűrű része; R4 jelentése hidrogénatom, alkil-,cikloalkil-, aril-, alkilamin-, alkilamid- vagy heterociklusoscsoport, vagy R4 lehet heterociklusos gyűrűrendszer része; azzal akikötéssel, hogy ha A jelentése feniléncsoport és V jelentése -NR2'CO-vagy -NR2'SO2-, akkor C jelentése közvetlen kötéstől eltérő és Xjelentése nitrogénatomtól eltérő. A találmány tárgyát képezi továbbá afenti vegyületeket tartalmazó gyógyászati készítmények illetve avegyületek gyógyászati készítmények előállítására való alkalmazása. Ó
Applications Claiming Priority (1)
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US21338198A | 1998-12-16 | 1998-12-16 |
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HU0105432A HUP0105432A3 (en) | 1998-12-16 | 1999-12-13 | New biphenyl and biphenyl-analogous compounds as integrin antagonists, process for their preparation and pharmaceutical compositions containing them and their use |
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EP (1) | EP1140809B1 (hu) |
JP (1) | JP2002532465A (hu) |
KR (1) | KR20010086112A (hu) |
CN (1) | CN1334801A (hu) |
AT (1) | ATE303359T1 (hu) |
AU (1) | AU761407B2 (hu) |
BG (1) | BG105574A (hu) |
BR (1) | BR9916367A (hu) |
CA (1) | CA2355161A1 (hu) |
CZ (1) | CZ20012185A3 (hu) |
DE (1) | DE69927050T2 (hu) |
EE (1) | EE200100317A (hu) |
ES (1) | ES2249059T3 (hu) |
HR (1) | HRP20010531A2 (hu) |
HU (1) | HUP0105432A3 (hu) |
ID (1) | ID30235A (hu) |
IL (1) | IL143484A0 (hu) |
MA (1) | MA25331A1 (hu) |
NO (1) | NO20012975L (hu) |
NZ (1) | NZ512339A (hu) |
PL (1) | PL348260A1 (hu) |
SK (1) | SK8432001A3 (hu) |
WO (1) | WO2000035864A1 (hu) |
ZA (1) | ZA200114432B (hu) |
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MY149050A (en) * | 2001-04-16 | 2013-07-15 | Merck Sharp & Dohme | 3,4 di-substituted cyclobutene-1,2-diones as cxc-chemokine receptor ligands |
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WO2003080053A1 (en) | 2002-03-18 | 2003-10-02 | Schering Corporation | Combination treatments for chemokine-mediated diseases |
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CN1720240B (zh) | 2002-10-09 | 2010-10-27 | 先灵公司 | 作为cxc-和cc-趋化因子受体配体的噻二唑二氧化物和噻二唑氧化物 |
FR2847251B1 (fr) * | 2002-11-19 | 2006-11-17 | NOUVEAUX COMPOSES BI-AROMATIQUES ACTIVEURS DES RECEPTEURS DE TYPE PPARy ET LEUR UTILISATION DANS DES COMPOSITIONS COSMETIQUES OU PHARMACEUTIQUES | |
JP4206382B2 (ja) | 2002-11-19 | 2009-01-07 | アキリオン ファーマシューティカルズ,インコーポレーテッド | 置換されたアリールチオウレアおよび関連化合物;ウイルス複製のインヒビター |
MXPA05005171A (es) * | 2002-11-19 | 2005-10-26 | Galderma Res & Dev | Compuestos bi-aromaticos activadores de los receptores de tipo ppar-gama y su uso en composiciones cosmeticas o farmaceuticas. |
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PA8591801A1 (es) | 2002-12-31 | 2004-07-26 | Pfizer Prod Inc | Inhibidores benzamidicos del receptor p2x7. |
ES2396565T3 (es) | 2003-05-12 | 2013-02-22 | Pah Usa 15 Llc | Inhibidores benzamida del receptor P2X7 |
US7208601B2 (en) | 2003-08-08 | 2007-04-24 | Mjalli Adnan M M | Aryl and heteroaryl compounds, compositions, and methods of use |
US7501538B2 (en) | 2003-08-08 | 2009-03-10 | Transtech Pharma, Inc. | Aryl and heteroaryl compounds, compositions and methods of use |
JP2007501844A (ja) | 2003-08-08 | 2007-02-01 | トランス テック ファーマ,インコーポレイテッド | アリール及びヘテロアリール化合物、組成物並びに使用方法 |
US7504401B2 (en) | 2003-08-29 | 2009-03-17 | Locus Pharmaceuticals, Inc. | Anti-cancer agents and uses thereof |
CN1918138B (zh) | 2003-12-19 | 2011-05-04 | 先灵公司 | 作为cxc-和cc-趋化因子受体配体的噻二唑化合物 |
MXPA06007205A (es) | 2003-12-22 | 2006-08-31 | Schering Corp | Dioxidos de isotiazol como ligandos del receptor cxc y cc-quimiocina. |
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DE602004021404D1 (de) | 2004-12-23 | 2009-07-16 | Gpc Biotech Ag | Quadratsäurederivate mit antiproliferativer Wirkung |
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JP2009500334A (ja) | 2005-06-29 | 2009-01-08 | シェーリング コーポレイション | Cxc−ケモカインレセプターリガンドとしてのジ置換オキサジアゾール |
CN101583352A (zh) * | 2005-07-29 | 2009-11-18 | 拜尔健康护理有限责任公司 | 治疗肥胖症的联苯氨基酸衍生物的制备和用途 |
ES2684821T3 (es) | 2005-12-29 | 2018-10-04 | Lexicon Pharmaceuticals, Inc. | Derivados de aminoácidos multicíclicos y métodos de su uso |
AR060901A1 (es) * | 2006-05-12 | 2008-07-23 | Jerini Ag | Compuestos heterociclicos para la inhibicion de integrinas y uso de estos |
US8450348B2 (en) | 2007-02-21 | 2013-05-28 | Forma Tm, Llc | Derivatives of squaric acid with anti-proliferative activity |
AU2008268409B2 (en) * | 2007-06-26 | 2013-12-05 | Lexicon Pharmaceuticals, Inc. | Compositions comprising tryptophan hydroxylase inhibitors |
FR2921657A1 (fr) * | 2007-09-28 | 2009-04-03 | Sanofi Aventis Sa | Derives de nicotinamide, leur preparation et leur application en therapeutique |
AU2009264273B2 (en) | 2008-06-24 | 2015-01-22 | Onxeo Dk, Branch Of Onxeo S.A., France | Squaric acid derivatives as inhibitors of the nicotinamide |
CN102702135B (zh) * | 2012-06-15 | 2014-05-28 | 中国农业大学 | 一种含苯并噻唑结构的苯甲酰基硫脲类化合物及其制备方法和应用 |
DK2953948T3 (en) * | 2013-02-07 | 2017-12-18 | Scifluor Life Sciences Inc | FLUORINATED INTEGRIN ANTAGONISTS |
JP7475635B2 (ja) * | 2020-01-30 | 2024-04-30 | 公立大学法人大阪 | 含窒素化合物およびその製造方法、ならびに該含窒素化合物を含む光機能性材料 |
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DE19548709A1 (de) * | 1995-12-23 | 1997-07-03 | Merck Patent Gmbh | Tyrosinderivate |
ATE212978T1 (de) * | 1996-03-29 | 2002-02-15 | Searle & Co | Para-substituierte phenylpropansäure derivate als integrin-antagonisten |
EP0907637A1 (de) * | 1996-06-28 | 1999-04-14 | MERCK PATENT GmbH | Phenylalanin-derivate als integrin-inhibitoren |
MY153569A (en) * | 1998-01-20 | 2015-02-27 | Mitsubishi Tanabe Pharma Corp | Inhibitors of ?4 mediated cell adhesion |
-
1999
- 1999-12-13 AU AU24312/00A patent/AU761407B2/en not_active Ceased
- 1999-12-13 DE DE69927050T patent/DE69927050T2/de not_active Expired - Fee Related
- 1999-12-13 ES ES99967934T patent/ES2249059T3/es not_active Expired - Lifetime
- 1999-12-13 ID IDW00200101362A patent/ID30235A/id unknown
- 1999-12-13 KR KR1020017007518A patent/KR20010086112A/ko not_active Application Discontinuation
- 1999-12-13 AT AT99967934T patent/ATE303359T1/de not_active IP Right Cessation
- 1999-12-13 IL IL14348499A patent/IL143484A0/xx unknown
- 1999-12-13 HU HU0105432A patent/HUP0105432A3/hu unknown
- 1999-12-13 EP EP99967934A patent/EP1140809B1/en not_active Expired - Lifetime
- 1999-12-13 SK SK843-2001A patent/SK8432001A3/sk unknown
- 1999-12-13 BR BR9916367-5A patent/BR9916367A/pt not_active IP Right Cessation
- 1999-12-13 CN CN99816127A patent/CN1334801A/zh active Pending
- 1999-12-13 CZ CZ20012185A patent/CZ20012185A3/cs unknown
- 1999-12-13 PL PL99348260A patent/PL348260A1/xx not_active Application Discontinuation
- 1999-12-13 WO PCT/EP1999/009843 patent/WO2000035864A1/en active IP Right Grant
- 1999-12-13 EE EEP200100317A patent/EE200100317A/xx unknown
- 1999-12-13 JP JP2000588126A patent/JP2002532465A/ja active Pending
- 1999-12-13 CA CA002355161A patent/CA2355161A1/en not_active Abandoned
- 1999-12-13 NZ NZ512339A patent/NZ512339A/xx unknown
-
2001
- 2001-05-30 ZA ZA200114432A patent/ZA200114432B/xx unknown
- 2001-06-07 BG BG105574A patent/BG105574A/xx unknown
- 2001-06-13 MA MA26235A patent/MA25331A1/fr unknown
- 2001-06-15 NO NO20012975A patent/NO20012975L/no not_active Application Discontinuation
- 2001-07-16 HR HR20010531A patent/HRP20010531A2/hr not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
CN1334801A (zh) | 2002-02-06 |
SK8432001A3 (en) | 2001-12-03 |
ID30235A (id) | 2001-11-15 |
CZ20012185A3 (cs) | 2001-10-17 |
CA2355161A1 (en) | 2000-06-22 |
JP2002532465A (ja) | 2002-10-02 |
KR20010086112A (ko) | 2001-09-07 |
PL348260A1 (en) | 2002-05-20 |
AU2431200A (en) | 2000-07-03 |
NO20012975D0 (no) | 2001-06-15 |
MA25331A1 (fr) | 2001-12-31 |
AU761407B2 (en) | 2003-06-05 |
EP1140809A1 (en) | 2001-10-10 |
WO2000035864A1 (en) | 2000-06-22 |
HRP20010531A2 (en) | 2002-08-31 |
NZ512339A (en) | 2003-03-28 |
ZA200114432B (en) | 2002-05-30 |
EE200100317A (et) | 2002-08-15 |
ATE303359T1 (de) | 2005-09-15 |
EP1140809B1 (en) | 2005-08-31 |
HUP0105432A3 (en) | 2002-12-28 |
BG105574A (en) | 2002-01-31 |
NO20012975L (no) | 2001-08-13 |
DE69927050D1 (de) | 2005-10-06 |
IL143484A0 (en) | 2002-04-21 |
DE69927050T2 (de) | 2006-06-29 |
BR9916367A (pt) | 2001-10-30 |
ES2249059T3 (es) | 2006-03-16 |
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