ZA200108774B - Carboxylic acid derivatives that inhibit the binding of integrins to their receptors. - Google Patents
Carboxylic acid derivatives that inhibit the binding of integrins to their receptors. Download PDFInfo
- Publication number
- ZA200108774B ZA200108774B ZA200108774A ZA200108774A ZA200108774B ZA 200108774 B ZA200108774 B ZA 200108774B ZA 200108774 A ZA200108774 A ZA 200108774A ZA 200108774 A ZA200108774 A ZA 200108774A ZA 200108774 B ZA200108774 B ZA 200108774B
- Authority
- ZA
- South Africa
- Prior art keywords
- amino
- alkyl
- methyl
- dihydro
- propanoic acid
- Prior art date
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- 108010044426 integrins Proteins 0.000 title claims description 20
- 102000006495 integrins Human genes 0.000 title claims description 20
- 102000005962 receptors Human genes 0.000 title abstract description 4
- 108020003175 receptors Proteins 0.000 title abstract description 4
- 150000001732 carboxylic acid derivatives Chemical class 0.000 title description 3
- 150000001875 compounds Chemical class 0.000 claims abstract description 98
- 239000000203 mixture Substances 0.000 claims abstract description 71
- 238000000034 method Methods 0.000 claims abstract description 46
- -1 nitro, amino Chemical group 0.000 claims description 178
- 125000000217 alkyl group Chemical group 0.000 claims description 119
- 229910052799 carbon Inorganic materials 0.000 claims description 112
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 78
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 55
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims description 51
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 51
- 229910052739 hydrogen Inorganic materials 0.000 claims description 36
- 125000003118 aryl group Chemical group 0.000 claims description 30
- 239000001257 hydrogen Substances 0.000 claims description 27
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims description 24
- 235000019260 propionic acid Nutrition 0.000 claims description 24
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 22
- 125000000623 heterocyclic group Chemical group 0.000 claims description 22
- DUWWHGPELOTTOE-UHFFFAOYSA-N n-(5-chloro-2,4-dimethoxyphenyl)-3-oxobutanamide Chemical compound COC1=CC(OC)=C(NC(=O)CC(C)=O)C=C1Cl DUWWHGPELOTTOE-UHFFFAOYSA-N 0.000 claims description 22
- 229910052760 oxygen Inorganic materials 0.000 claims description 22
- 150000003839 salts Chemical class 0.000 claims description 20
- 125000003342 alkenyl group Chemical group 0.000 claims description 18
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 17
- 125000000304 alkynyl group Chemical group 0.000 claims description 16
- 125000003545 alkoxy group Chemical group 0.000 claims description 15
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 15
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 15
- 150000002431 hydrogen Chemical class 0.000 claims description 15
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 15
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 14
- 125000002877 alkyl aryl group Chemical group 0.000 claims description 13
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 13
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- 125000005083 alkoxyalkoxy group Chemical group 0.000 claims description 12
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- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 claims 2
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- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
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- 125000003774 valeryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
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Classifications
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- 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
- C07D213/60—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 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
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—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
- C07D405/02—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
- 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Emergency Medicine (AREA)
- Transplantation (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Oncology (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Dermatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13297199P | 1999-05-07 | 1999-05-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200108774B true ZA200108774B (en) | 2003-01-24 |
Family
ID=22456441
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200108774A ZA200108774B (en) | 1999-05-07 | 2001-10-24 | Carboxylic acid derivatives that inhibit the binding of integrins to their receptors. |
Country Status (24)
| Country | Link |
|---|---|
| EP (1) | EP1176956B1 (fr) |
| JP (1) | JP5132855B2 (fr) |
| AT (1) | ATE383153T1 (fr) |
| AU (1) | AU5267900A (fr) |
| CA (1) | CA2373360C (fr) |
| CY (1) | CY1107438T1 (fr) |
| CZ (1) | CZ303312B6 (fr) |
| DE (1) | DE60037726T2 (fr) |
| DK (1) | DK1176956T3 (fr) |
| ES (1) | ES2296625T3 (fr) |
| HK (1) | HK1045805A1 (fr) |
| IL (2) | IL146311A0 (fr) |
| IN (1) | IN2001KN01110A (fr) |
| MX (1) | MXPA01011340A (fr) |
| NO (1) | NO324421B1 (fr) |
| NZ (1) | NZ515248A (fr) |
| PL (1) | PL205322B1 (fr) |
| RO (1) | RO122246B1 (fr) |
| RU (1) | RU2263109C2 (fr) |
| SI (1) | SI20744B (fr) |
| SK (1) | SK286696B6 (fr) |
| TR (2) | TR200103178T2 (fr) |
| WO (1) | WO2000067746A1 (fr) |
| ZA (1) | ZA200108774B (fr) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6972296B2 (en) | 1999-05-07 | 2005-12-06 | Encysive Pharmaceuticals Inc. | Carboxylic acid derivatives that inhibit the binding of integrins to their receptors |
| US6723711B2 (en) * | 1999-05-07 | 2004-04-20 | Texas Biotechnology Corporation | Propanoic acid derivatives that inhibit the binding of integrins to their receptors |
| AR026748A1 (es) | 1999-12-08 | 2003-02-26 | Vertex Pharma | Un compuesto inhibidor de caspasas, una composicion farmaceutica que lo comprende, un metodo para la sintesis del mismo y un compuesto intermediario paradicha sintesis |
| ES2200617B1 (es) | 2001-01-19 | 2005-05-01 | Almirall Prodesfarma, S.A. | Derivados de urea como antagonistas de integrinas alfa 4. |
| SI21096B (sl) * | 2001-10-09 | 2012-05-31 | Encysive Pharmaceuticals Inc | Derivati karboksilne kisline ki inhibirajo vezavo integrinov na njihove receptorje |
| OA12771A (en) * | 2002-02-14 | 2006-07-04 | Pharmacia Corp | Substituted pyridinones as modulators of P38 map kinase. |
| AU2003248758A1 (en) | 2002-06-28 | 2004-01-19 | Vertex Pharmaceuticals Incorporated | Caspase inhibitors and uses thereof |
| AU2003265398A1 (en) | 2002-08-09 | 2004-02-25 | Transtech Pharma, Inc. | Aryl and heteroaryl compounds and methods to modulate coagulation |
| CA2513493A1 (fr) * | 2002-11-08 | 2004-05-27 | Schering Corporation | Produits de combinaison comprenant des derives d'acide carboxylique inhibant la liaison des integrines a leurs recepteurs et autres composes therapeutiques |
| TW200500343A (en) | 2002-12-20 | 2005-01-01 | Vertex Pharma | Caspase inhibitors and uses thereof |
| PE20050159A1 (es) | 2003-05-27 | 2005-04-19 | Vertex Pharma | Derivados de acido 3-[2-(3-amino-2-oxo-2h-piridin-1-il)-acetilamino]-4-oxo-pentanoico como inhibidores de caspasa |
| CN1832920A (zh) | 2003-08-08 | 2006-09-13 | 特兰斯泰克制药公司 | 芳基和杂芳基化合物,组合物及其使用方法 |
| 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 |
| EP1917244A2 (fr) | 2005-08-24 | 2008-05-07 | Abbott GmbH & Co. KG | Composes guanidine a substitution hetaryl et utilisation en tant que partenaires de liaison pour des recepteurs de 5-ht5 |
| WO2008109991A1 (fr) * | 2007-03-09 | 2008-09-18 | University Health Network | Inhibiteur de carnitine palmitoyltransférase et traitement du cancer |
| US8680282B2 (en) | 2007-08-01 | 2014-03-25 | University Health Network | Cyclic inhibitors of carnitine palmitoyltransferase and treating cancer |
| MX2011011326A (es) * | 2009-04-27 | 2012-02-13 | Elan Pharm Inc | Antagonistas de piridinona de las integrinas alfa-4. |
| EP2475654B1 (fr) | 2009-09-09 | 2016-12-28 | E. I. du Pont de Nemours and Company | Dérivés herbicides de pyrimidone |
| WO2012033548A2 (fr) * | 2010-09-07 | 2012-03-15 | E. I. Du Pont De Nemours And Company | Oxo-hétérocycles et sulfono-hétérocycles bis-azotés herbicides |
| HUE031624T2 (en) * | 2012-01-31 | 2017-07-28 | Daiichi Sankyo Co Ltd | Pyridone derivative |
| AU2014321397C1 (en) | 2013-09-20 | 2019-08-01 | Biomarin Pharmaceutical Inc. | Glucosylceramide synthase inhibitors for the treatment of diseases |
| WO2015136468A1 (fr) | 2014-03-13 | 2015-09-17 | Prothena Biosciences Limited | Polythérapie pour la sclérose en plaques |
| KR102373700B1 (ko) * | 2014-04-02 | 2022-03-11 | 인터뮨, 인크. | 항섬유성 피리디논 |
| US10246451B2 (en) * | 2017-04-26 | 2019-04-02 | Aviara Pharmaceuticals, Inc. | Propionic acid derivatives and methods of use thereof |
| US10875875B2 (en) * | 2017-04-26 | 2020-12-29 | Aviara Pharmaceuticals, Inc. | Propionic acid derivatives and methods of use thereof |
| KR20200018407A (ko) | 2017-04-28 | 2020-02-19 | 텍사스 칠드런스 하스피탈 | 표적화 나노입자 |
| CA3090270A1 (fr) * | 2018-02-02 | 2019-08-08 | Genentech, Inc. | Compose pharmaceutique, sels de celui-ci, formulations de celui-ci, et procedes de fabrication et d'utilisation de celui-ci |
| WO2020092394A1 (fr) | 2018-10-30 | 2020-05-07 | Gilead Sciences, Inc. | Dérivés d'imidazopyridine utilisés en tant qu'inhibiteurs de l'intégrine alpha4bêta7 |
| KR20240015737A (ko) | 2018-10-30 | 2024-02-05 | 길리애드 사이언시즈, 인코포레이티드 | 알파4베타7 인테그린 억제제로서의 퀴놀린 유도체 |
| AU2019373245C1 (en) | 2018-10-30 | 2022-10-27 | Gilead Sciences, Inc. | Compounds for inhibition of alpha 4β7 integrin |
| CA3115820A1 (fr) | 2018-10-30 | 2020-05-07 | Gilead Sciences, Inc. | Composes pour l'inhibition de l'integrine .alpha.4.beta.7 |
| US11578069B2 (en) | 2019-08-14 | 2023-02-14 | Gilead Sciences, Inc. | Compounds for inhibition of α4 β7 integrin |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2614189A1 (de) * | 1976-04-02 | 1977-10-20 | Hoechst Ag | Therapeutisch wirksame ureido- und semicarbazido-derivate des tiazols und verfahren zu ihrer herstellung |
| US5220017A (en) * | 1991-04-10 | 1993-06-15 | Merck & Co., Inc. | Cholecystokinin antagonists |
| EP0691953B1 (fr) * | 1993-03-31 | 2000-08-02 | G.D. Searle & Co. | Amidinophenyl-1-pyrrolidones /piperidinones inhibitrices de l'agregation plaquettaire |
| US5770573A (en) * | 1993-12-06 | 1998-06-23 | Cytel Corporation | CS-1 peptidomimetics, compositions and methods of using the same |
| JPH07304755A (ja) * | 1994-05-12 | 1995-11-21 | Yamanouchi Pharmaceut Co Ltd | 縮合ジアゼピン誘導体 |
| US5610296A (en) * | 1994-12-05 | 1997-03-11 | G. D. Searle & Co. | Process for the preparation of amidino phenyl pyrrolidine beta-alanine urea analogs |
| US6306840B1 (en) * | 1995-01-23 | 2001-10-23 | Biogen, Inc. | Cell adhesion inhibitors |
| ATE208505T1 (de) * | 1996-05-15 | 2001-11-15 | Searle & Co | Verfahren und reagenz zur überwachung des blutspiegels von antiplättchen-verbindungen |
| JP2001500875A (ja) * | 1996-09-18 | 2001-01-23 | メルク エンド カンパニー インコーポレーテッド | 心臓血管系疾患関連の危険性を減らす併用治療法 |
| US6025358A (en) * | 1998-06-11 | 2000-02-15 | G. D. Searle & Co. | Double prodrugs of potent GP IIb/IIIa antagonists |
| EP1115724A1 (fr) * | 1998-09-21 | 2001-07-18 | Shire Biochem Inc. | Quinolizinones inhibiteurs de l'integrine |
-
2000
- 2000-05-05 DK DK00937527T patent/DK1176956T3/da active
- 2000-05-05 AU AU52679/00A patent/AU5267900A/en not_active Abandoned
- 2000-05-05 NZ NZ515248A patent/NZ515248A/xx not_active IP Right Cessation
- 2000-05-05 MX MXPA01011340A patent/MXPA01011340A/es active IP Right Grant
- 2000-05-05 ES ES00937527T patent/ES2296625T3/es not_active Expired - Lifetime
- 2000-05-05 TR TR2001/03178T patent/TR200103178T2/xx unknown
- 2000-05-05 CZ CZ20013963A patent/CZ303312B6/cs not_active IP Right Cessation
- 2000-05-05 CA CA2373360A patent/CA2373360C/fr not_active Expired - Lifetime
- 2000-05-05 JP JP2000616772A patent/JP5132855B2/ja not_active Expired - Fee Related
- 2000-05-05 SI SI200020021A patent/SI20744B/sl not_active IP Right Cessation
- 2000-05-05 AT AT00937527T patent/ATE383153T1/de active
- 2000-05-05 WO PCT/US2000/012303 patent/WO2000067746A1/fr active IP Right Grant
- 2000-05-05 PL PL351396A patent/PL205322B1/pl unknown
- 2000-05-05 EP EP00937527A patent/EP1176956B1/fr not_active Expired - Lifetime
- 2000-05-05 IL IL14631100A patent/IL146311A0/xx active IP Right Grant
- 2000-05-05 TR TR2002/01920T patent/TR200201920T2/xx unknown
- 2000-05-05 RO ROA200101210A patent/RO122246B1/ro unknown
- 2000-05-05 SK SK1608-2001A patent/SK286696B6/sk not_active IP Right Cessation
- 2000-05-05 RU RU2001133360/04A patent/RU2263109C2/ru not_active IP Right Cessation
- 2000-05-05 DE DE60037726T patent/DE60037726T2/de not_active Expired - Lifetime
- 2000-11-16 IN IN1110KON2001 patent/IN2001KN01110A/en unknown
-
2001
- 2001-10-24 ZA ZA200108774A patent/ZA200108774B/en unknown
- 2001-11-01 IL IL146311A patent/IL146311A/en not_active IP Right Cessation
- 2001-11-06 NO NO20015418A patent/NO324421B1/no not_active IP Right Cessation
-
2002
- 2002-07-31 HK HK02105650A patent/HK1045805A1/xx not_active IP Right Cessation
-
2008
- 2008-03-05 CY CY20081100253T patent/CY1107438T1/el unknown
Also Published As
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