HUP0300544A2 - Integrin expresszálás inhibitorokat tartalmazó gyógyszerkészítmények - Google Patents
Integrin expresszálás inhibitorokat tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0300544A2 HUP0300544A2 HU0300544A HUP0300544A HUP0300544A2 HU P0300544 A2 HUP0300544 A2 HU P0300544A2 HU 0300544 A HU0300544 A HU 0300544A HU P0300544 A HUP0300544 A HU P0300544A HU P0300544 A2 HUP0300544 A2 HU P0300544A2
- Authority
- HU
- Hungary
- Prior art keywords
- ring
- integrin expression
- formula
- group
- substituent
- Prior art date
Links
- 102000006495 integrins Human genes 0.000 title abstract 4
- 108010044426 integrins Proteins 0.000 title abstract 4
- 239000003112 inhibitor Substances 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 201000011510 cancer Diseases 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 206010003210 Arteriosclerosis Diseases 0.000 abstract 1
- 206010012689 Diabetic retinopathy Diseases 0.000 abstract 1
- 206010027476 Metastases Diseases 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 239000013543 active substance Substances 0.000 abstract 1
- 230000010100 anticoagulation Effects 0.000 abstract 1
- 208000011775 arteriosclerosis disease Diseases 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000009401 metastasis Effects 0.000 abstract 1
- 230000004263 retinal angiogenesis Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229940124530 sulfonamide Drugs 0.000 abstract 1
- -1 sulfonamide compound Chemical class 0.000 abstract 1
Classifications
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- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/18—Sulfonamides
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
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- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
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- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- A—HUMAN NECESSITIES
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- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- 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
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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- 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]
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- 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
- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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- 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
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- 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
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- 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
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- 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
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- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
- C07D215/38—Nitrogen atoms
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- C07D217/24—Oxygen atoms
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- C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
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- 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
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- 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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- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
Abstract
A találmány tárgya integrin expresszálás inhibitor, hatóanyag artériasclerosis, psoriasis, rák, retina angiogenezis, diabetikus retinopathavagy gyulladásos betegségek kezelésére, egy véralvadásgátló vagy rákáttétel elnyomó hatóanyag integrin gátló hatás alapján. Nevezetesen, atalálmány tárgya olyan integrin expresszálás inhibitor, amelyhatóanyagként az (I) általános képletű szulfonamid-vegyületet, annakgyógyászatilag elfogadható sóját vagy hidrátját tartalmazza. Aképletben B jelentése 6-10 szénatomos arilgyűrű vagy 6-10-tagúheteroarilgyűrű, amely szubsztituenst tartalmazhat, és amelyben agyűrű egy részlete lehet telített, K jelentése egy egyszeres kötés,CH=CH- vagy -(CR4bR5b)mb csoport (ahol a képletben R4b és R5b azonosakvagy különbözőek egymástól, és jelentésük egyaránt hidrogénatom vagy1-4 szénatomos alkilcsoport, és mb jelentése 1 vagy 2 értékű egészszám), R1 jelentése hidrogénatom vagy 1-6 szénatomos alkilcsoport, Zjelentése egyszeres kötés vagy -CO-NH-csoport, és R jelentése 6-10szénatomos arilgyűrű vagy 6-10-tagú heteroarilgyűrű, amelyszubsztituenst tartalmazhat, és amelyben a gyűrű egy részlete lehettelített. Ó
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2000026080 | 2000-02-03 | ||
JP2000402084 | 2000-12-28 | ||
PCT/JP2001/000713 WO2001056607A1 (fr) | 2000-02-03 | 2001-02-01 | Inhibiteurs de l'expression de l'integrine |
Publications (2)
Publication Number | Publication Date |
---|---|
HUP0300544A2 true HUP0300544A2 (hu) | 2003-07-28 |
HUP0300544A3 HUP0300544A3 (en) | 2005-03-29 |
Family
ID=26584780
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0300544A HUP0300544A3 (en) | 2000-02-03 | 2001-02-01 | Pharmaceutical compositions containing integrin expression inhibitors |
Country Status (16)
Country | Link |
---|---|
US (3) | US20040018192A1 (hu) |
EP (1) | EP1258252B1 (hu) |
JP (1) | JP4039856B2 (hu) |
KR (1) | KR100767000B1 (hu) |
CN (1) | CN100356979C (hu) |
AT (1) | ATE464892T1 (hu) |
AU (1) | AU781506B2 (hu) |
CA (1) | CA2399001C (hu) |
DE (1) | DE60141889D1 (hu) |
ES (1) | ES2341843T3 (hu) |
HU (1) | HUP0300544A3 (hu) |
MX (1) | MXPA02007249A (hu) |
NO (1) | NO329158B1 (hu) |
NZ (1) | NZ520299A (hu) |
RU (1) | RU2240826C2 (hu) |
WO (1) | WO2001056607A1 (hu) |
Families Citing this family (63)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2000247949A (ja) | 1999-02-26 | 2000-09-12 | Eisai Co Ltd | スルホンアミド含有インドール化合物 |
CA2395772C (en) | 1999-12-28 | 2010-09-28 | Eisai Co., Ltd. | Sulfonamide-containing heterocyclic compounds |
ES2280502T3 (es) * | 2001-02-21 | 2007-09-16 | EISAI R&D MANAGEMENT CO., LTD. | Metodo para evaluar el efecto de un inhibidor de la angiogenesis a traves de la inhibicion de la expresion de integrinas. |
WO2002070478A1 (en) * | 2001-03-06 | 2002-09-12 | Astrazeneca Ab | Indolone derivatives having vascular-damaging activity |
JPWO2003022271A1 (ja) * | 2001-09-05 | 2004-12-24 | エーザイ株式会社 | リンパ球活性化抑制剤および自己免疫疾患治療剤 |
EP1481678A4 (en) * | 2002-03-05 | 2009-12-30 | Eisai R&D Man Co Ltd | ANTITUMORAL AGENT CONTAINING A SULFONAMIDE-CONTAINING HETEROCYCLIC COMPOUND AND AN ANGIOGENESIS INHIBITOR |
CA2784937A1 (en) | 2002-05-24 | 2003-12-04 | Millennium Pharmaceuticals, Inc. | Ccr9 inhibitors and methods of use thereof |
GB0215650D0 (en) * | 2002-07-05 | 2002-08-14 | Cyclacel Ltd | Bisarylsufonamide compounds |
JP4845380B2 (ja) * | 2002-09-19 | 2011-12-28 | シェーリング コーポレイション | サイクリン依存性キナーゼインヒビターとしてのピラゾロピリミジン |
MY133311A (en) | 2002-09-19 | 2007-11-30 | Schering Corp | Novel imidazopyridines as cyclin dependent kinase inhibitors |
US7227035B2 (en) | 2002-11-18 | 2007-06-05 | Chemocentryx | Bis-aryl sulfonamides |
CA2500492C (en) | 2002-11-18 | 2010-03-16 | Solomon Ungashe | Aryl sulfonamides |
US7741519B2 (en) | 2007-04-23 | 2010-06-22 | Chemocentryx, Inc. | Bis-aryl sulfonamides |
US7420055B2 (en) | 2002-11-18 | 2008-09-02 | Chemocentryx, Inc. | Aryl sulfonamides |
CN101165049A (zh) * | 2003-09-10 | 2008-04-23 | 卫材R&D管理有限公司 | 含磺酰胺的吲哚化合物结晶 |
US20070104716A1 (en) * | 2003-11-22 | 2007-05-10 | Sloan-Kettering Institute For Cancer Research | Methods for controlling pathological angiogenesis by inhibition of a6b4 integrin |
WO2005090297A1 (en) * | 2004-03-19 | 2005-09-29 | Biotie Therapies Corporation | Sulphonamide derivatives |
EP2394662B1 (en) | 2004-04-02 | 2018-03-21 | The Regents of The University of California | Methods and compositions for treating and preventing disease associated with alpha v beta 5 integrin |
JP5094394B2 (ja) * | 2005-04-20 | 2012-12-12 | 武田薬品工業株式会社 | 縮合複素環化合物 |
JP2008540539A (ja) * | 2005-05-10 | 2008-11-20 | バーテックス ファーマシューティカルズ インコーポレイテッド | イオンチャンネルの調節因子としての二環系誘導体 |
WO2007008926A1 (en) | 2005-07-11 | 2007-01-18 | Aerie Pharmaceuticals, Inc. | Isoquinoline compounds |
US20070135499A1 (en) * | 2005-07-11 | 2007-06-14 | Aerie Pharmaceuticals, Inc. | Hydrazide compounds |
EP1932837A4 (en) * | 2005-08-17 | 2011-05-25 | Daiichi Sankyo Co Ltd | HETEROCYCLIC BICYCLOUS BINDING WITH ANTIPILY EFFECT |
FI20055496A0 (fi) * | 2005-09-16 | 2005-09-16 | Biotie Therapies Corp | Kollageenireseptorien alfa-l-domeeniin sitoutuvat modulaattorit |
FI20055498A0 (fi) * | 2005-09-16 | 2005-09-16 | Biotie Therapies Corp | Sulfonamidijohdannaisia |
EP2068878B1 (en) | 2006-09-20 | 2019-04-10 | Aerie Pharmaceuticals, Inc. | Rho kinase inhibitors |
US7943728B2 (en) * | 2006-12-26 | 2011-05-17 | National Cheng Kung University | Disintegrin variants and their use in treating osteoporosis-induced bone loss and angiogenesis-related diseases |
US8455513B2 (en) | 2007-01-10 | 2013-06-04 | Aerie Pharmaceuticals, Inc. | 6-aminoisoquinoline compounds |
DK2178870T3 (en) * | 2007-08-17 | 2018-10-22 | Lg Chemical Ltd | INDOLE AND INDAZOLIC COMPOUNDS AS AN INHIBITOR OF CELLULAR NECROSE |
JP2011016723A (ja) * | 2007-11-02 | 2011-01-27 | Katayama Kagaku Kogyo Kk | 骨及び軟骨形成タンパク質を含有する医薬品及び医療器具 |
US8455514B2 (en) | 2008-01-17 | 2013-06-04 | Aerie Pharmaceuticals, Inc. | 6-and 7-amino isoquinoline compounds and methods for making and using the same |
US8450344B2 (en) | 2008-07-25 | 2013-05-28 | Aerie Pharmaceuticals, Inc. | Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds |
CA2929545C (en) | 2009-05-01 | 2019-04-09 | Aerie Pharmaceuticals, Inc. | Dual mechanism inhibitors for the treatment of disease |
CA2767409C (en) | 2009-07-24 | 2018-10-30 | The Regents Of The University Of California | Methods and compositions for treating and preventing disease associated with .alpha.v.beta.5 integrin |
US20120196854A1 (en) | 2009-10-06 | 2012-08-02 | Kyowa Hakko Kirin Co., Ltd. | Pharmaceutical composition comprising aromatic heterocyclic compound |
TWI410408B (zh) * | 2010-03-16 | 2013-10-01 | Purzer Pharmaceutical Co Ltd | 苯磺醯胺衍生物及其醫藥組合物 |
CN102199148A (zh) * | 2010-03-25 | 2011-09-28 | 瑞安大药厂股份有限公司 | 苯磺酰胺衍生物及其医药组合物 |
FR2984316B1 (fr) * | 2011-12-16 | 2017-08-11 | Oreal | Coupleur de structure 7-amino-indole, composition tinctoriale en comprenant, procedes et utilisations. |
WO2013126608A1 (en) | 2012-02-22 | 2013-08-29 | Sanford-Burnham Medical Research Institute | Sulfonamide compounds and uses as tnap inhibitors |
US9415043B2 (en) | 2013-03-15 | 2016-08-16 | Aerie Pharmaceuticals, Inc. | Combination therapy |
CN104163798A (zh) * | 2014-07-29 | 2014-11-26 | 苏州康润医药有限公司 | 3-氨基-8-三氟甲基喹啉的合成方法 |
CN104098498A (zh) * | 2014-07-30 | 2014-10-15 | 天津市斯芬克司药物研发有限公司 | 一种吲唑类化合物及其制备方法 |
WO2016087593A1 (en) * | 2014-12-05 | 2016-06-09 | Syngenta Participations Ag | Novel fungicidal quinolinylamidines |
KR102579582B1 (ko) | 2015-11-17 | 2023-09-15 | 에어리 파마슈티컬즈, 인코포레이티드 | 키나아제 억제제 및 이의 중간체의 제조 방법 |
US9643927B1 (en) | 2015-11-17 | 2017-05-09 | Aerie Pharmaceuticals, Inc. | Process for the preparation of kinase inhibitors and intermediates thereof |
AU2017319520A1 (en) | 2016-08-31 | 2019-03-07 | Aerie Pharmaceuticals, Inc. | Ophthalmic compositions |
JP2020508436A (ja) | 2016-12-07 | 2020-03-19 | プロジェニティ, インコーポレイテッド | 胃腸管の検出方法、装置およびシステム |
JP7150723B2 (ja) | 2016-12-14 | 2022-10-11 | ビオラ・セラピューティクス・インコーポレイテッド | 消化管疾病のインテグリン阻害薬による治療 |
AU2018243687C1 (en) | 2017-03-31 | 2020-12-24 | Aerie Pharmaceuticals, Inc. | Aryl cyclopropyl-amino-isoquinolinyl amide compounds |
CA3083228A1 (en) * | 2017-12-14 | 2019-06-20 | Dana-Farber Cancer Institute, Inc. | Small molecule degraders that recruit dcaft15 |
SG11202004260YA (en) | 2017-12-15 | 2020-06-29 | Bayer Animal Health Gmbh | Process for preparing antihelmintic 4-amino-quinoline-3-carboxamide derivatives |
AU2019211383A1 (en) | 2018-01-25 | 2020-06-11 | Dana-Farber Cancer Institute, Inc. | Sulfonamide derivatives for protein degradation |
US20230033021A1 (en) | 2018-06-20 | 2023-02-02 | Progenity, Inc. | Treatment of a disease of the gastrointestinal tract with an integrin inhibitor |
AU2019337703B2 (en) | 2018-09-14 | 2023-02-02 | Aerie Pharmaceuticals, Inc. | Aryl cyclopropyl-amino-isoquinolinyl amide compounds |
US11179383B2 (en) | 2018-10-30 | 2021-11-23 | Gilead Sciences, Inc. | Compounds for inhibition of α4β7 integrin |
JP7214882B2 (ja) | 2018-10-30 | 2023-01-30 | ギリアード サイエンシーズ, インコーポレイテッド | アルファ4ベータ7インテグリン阻害剤としてのイミダゾピリジン誘導体 |
SG11202103484RA (en) | 2018-10-30 | 2021-05-28 | Gilead Sciences Inc | Quinoline derivatives as alpha4beta7 integrin inhibitors |
JP7189368B2 (ja) | 2018-10-30 | 2022-12-13 | ギリアード サイエンシーズ, インコーポレイテッド | アルファ4ベータ7インテグリンの阻害のための化合物 |
CN116726362A (zh) | 2018-11-19 | 2023-09-12 | 比奥拉治疗股份有限公司 | 用生物治疗剂治疗疾病的方法和装置 |
US11578069B2 (en) | 2019-08-14 | 2023-02-14 | Gilead Sciences, Inc. | Compounds for inhibition of α4 β7 integrin |
EP3870261B1 (en) | 2019-12-13 | 2024-01-31 | Biora Therapeutics, Inc. | Ingestible device for delivery of therapeutic agent to the gastrointestinal tract |
WO2022173805A1 (en) * | 2021-02-09 | 2022-08-18 | Triana Biomedicines, Inc. | Amide and ether substituted n-(1h-indol-7-yl)benzenesulfonamides and uses thereof |
WO2022173727A1 (en) * | 2021-02-09 | 2022-08-18 | Celgene Corporation | Sulfonamides and their use for treatment of helminthic infections and diseases |
Family Cites Families (22)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB9115160D0 (en) | 1991-07-12 | 1991-08-28 | Erba Carlo Spa | Methylen-oxindole derivatives and process for their preparation |
HU224069B1 (hu) * | 1993-09-10 | 2005-05-30 | Eisai Co. Ltd. | Heterobiciklusos szulfonamid-származékok, eljárás előállításukra, ezeket hatóanyagként tartalmazó gyógyászati készítmények, valamint alkalmazásuk gyógyászati készítmények előállítására |
JP3545461B2 (ja) | 1993-09-10 | 2004-07-21 | エーザイ株式会社 | 二環式ヘテロ環含有スルホンアミド誘導体 |
US5753230A (en) * | 1994-03-18 | 1998-05-19 | The Scripps Research Institute | Methods and compositions useful for inhibition of angiogenesis |
US5574018A (en) | 1994-07-29 | 1996-11-12 | Amgen Inc. | Conjugates of vitamin B12 and proteins |
JP3690831B2 (ja) * | 1995-02-27 | 2005-08-31 | エーザイ株式会社 | インドール含有スルホンアミド誘導体 |
US5760028A (en) * | 1995-12-22 | 1998-06-02 | The Dupont Merck Pharmaceutical Company | Integrin receptor antagonists |
DE69713582T2 (de) * | 1996-03-29 | 2003-01-09 | Searle & Co | Zimtsäurederivate und deren verwendung als integrin-antagonisten |
AU2323897A (en) * | 1996-03-29 | 1997-10-22 | G.D. Searle & Co. | Cyclopropyl alkanoic acid derivatives |
ATE204857T1 (de) * | 1996-03-29 | 2001-09-15 | Searle & Co | Meta-substituierte phenylenderivate und ihre verwendung als alphavbeta3 intergrin-antagonisten oder inhibitoren |
AU2420897A (en) * | 1996-03-29 | 1997-10-22 | G.D. Searle & Co. | Meta-substituted phenylene sulphonamide derivatives |
EP0891325B1 (en) * | 1996-03-29 | 2002-02-06 | G.D. Searle & Co. | Para-substituted phenylpropanoic acid derivatives as integrin antagonists |
AU6696698A (en) * | 1997-03-11 | 1998-09-29 | Allergan Sales, Inc. | Anti-angiogenic agents |
EP0973396A4 (en) * | 1997-04-07 | 2001-02-07 | Merck & Co Inc | METHOD FOR TREATING CANCER |
EP0991619B1 (en) * | 1997-06-23 | 2003-09-10 | Tanabe Seiyaku Co., Ltd. | Inhibitors of alpha 4-beta 1 mediated cell adhesion |
US6197794B1 (en) * | 1998-01-08 | 2001-03-06 | Celltech Therapeutics Limited | Phenylalanine derivatives |
EP1054871A2 (en) * | 1998-04-01 | 2000-11-29 | Du Pont Pharmaceuticals Company | Pyrimidines and triazines as integrin antagonists |
KR20010042704A (ko) * | 1998-04-16 | 2001-05-25 | 데이비드 비. 맥윌리암스 | 인테그린이 인테그린 수용체에 결합하는 것을 억제하는n,n-이치환된 아미드 |
GB9826174D0 (en) * | 1998-11-30 | 1999-01-20 | Celltech Therapeutics Ltd | Chemical compounds |
JP2002533387A (ja) * | 1998-12-23 | 2002-10-08 | ジー.ディー.サール & カンパニー | 腫瘍治療の複合療法としてインテグリン拮抗物質と一つ以上の抗腫瘍剤を使用する方法 |
US6291503B1 (en) * | 1999-01-15 | 2001-09-18 | Bayer Aktiengesellschaft | β-phenylalanine derivatives as integrin antagonists |
JP2000247949A (ja) * | 1999-02-26 | 2000-09-12 | Eisai Co Ltd | スルホンアミド含有インドール化合物 |
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2001
- 2001-02-01 JP JP2001556505A patent/JP4039856B2/ja not_active Expired - Fee Related
- 2001-02-01 AT AT01948941T patent/ATE464892T1/de not_active IP Right Cessation
- 2001-02-01 MX MXPA02007249A patent/MXPA02007249A/es active IP Right Grant
- 2001-02-01 ES ES01948941T patent/ES2341843T3/es not_active Expired - Lifetime
- 2001-02-01 WO PCT/JP2001/000713 patent/WO2001056607A1/ja active IP Right Grant
- 2001-02-01 AU AU28867/01A patent/AU781506B2/en not_active Ceased
- 2001-02-01 HU HU0300544A patent/HUP0300544A3/hu unknown
- 2001-02-01 NZ NZ520299A patent/NZ520299A/en not_active IP Right Cessation
- 2001-02-01 US US10/181,562 patent/US20040018192A1/en not_active Abandoned
- 2001-02-01 RU RU2002123580/15A patent/RU2240826C2/ru not_active IP Right Cessation
- 2001-02-01 CA CA2399001A patent/CA2399001C/en not_active Expired - Fee Related
- 2001-02-01 KR KR1020027009945A patent/KR100767000B1/ko not_active IP Right Cessation
- 2001-02-01 DE DE60141889T patent/DE60141889D1/de not_active Expired - Lifetime
- 2001-02-01 EP EP01948941A patent/EP1258252B1/en not_active Expired - Lifetime
- 2001-02-01 CN CNB018043887A patent/CN100356979C/zh not_active Expired - Fee Related
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US7834049B2 (en) | 2010-11-16 |
ES2341843T3 (es) | 2010-06-29 |
DE60141889D1 (de) | 2010-06-02 |
AU2886701A (en) | 2001-08-14 |
NZ520299A (en) | 2004-05-28 |
EP1258252A4 (en) | 2005-11-02 |
NO20023688L (no) | 2002-10-03 |
HUP0300544A3 (en) | 2005-03-29 |
MXPA02007249A (es) | 2002-12-09 |
CA2399001A1 (en) | 2001-08-09 |
NO329158B1 (no) | 2010-08-30 |
KR100767000B1 (ko) | 2007-10-15 |
US20040018192A1 (en) | 2004-01-29 |
RU2002123580A (ru) | 2004-03-20 |
US20050176712A1 (en) | 2005-08-11 |
EP1258252A1 (en) | 2002-11-20 |
AU781506B2 (en) | 2005-05-26 |
CN100356979C (zh) | 2007-12-26 |
WO2001056607A1 (fr) | 2001-08-09 |
CN1396833A (zh) | 2003-02-12 |
EP1258252B1 (en) | 2010-04-21 |
ATE464892T1 (de) | 2010-05-15 |
KR20020073575A (ko) | 2002-09-27 |
JP4039856B2 (ja) | 2008-01-30 |
NO20023688D0 (no) | 2002-08-02 |
US20100267754A1 (en) | 2010-10-21 |
RU2240826C2 (ru) | 2004-11-27 |
CA2399001C (en) | 2010-07-20 |
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