HUP0100336A2 - Vla-4 antagonists, pharmaceutical compositions comprising them and process for preparing them - Google Patents
Vla-4 antagonists, pharmaceutical compositions comprising them and process for preparing themInfo
- Publication number
- HUP0100336A2 HUP0100336A2 HU0100336A HUP0100336A HUP0100336A2 HU P0100336 A2 HUP0100336 A2 HU P0100336A2 HU 0100336 A HU0100336 A HU 0100336A HU P0100336 A HUP0100336 A HU P0100336A HU P0100336 A2 HUP0100336 A2 HU P0100336A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- alkenyl
- optionally substituted
- cycloalkenyl
- alkynyl
- Prior art date
Links
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 239000005557 antagonist Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 6
- 125000000304 alkynyl group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- -1 sulfo- Chemical group 0.000 abstract 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 2
- 101100244083 Arabidopsis thaliana PKL gene Proteins 0.000 abstract 1
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 108010008212 Integrin alpha4beta1 Proteins 0.000 abstract 1
- 229910018830 PO3H Inorganic materials 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000004945 acylaminoalkyl group Chemical group 0.000 abstract 1
- 125000006323 alkenyl amino group Chemical group 0.000 abstract 1
- 125000003302 alkenyloxy group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000006319 alkynyl amino group Chemical group 0.000 abstract 1
- 125000005133 alkynyloxy group Chemical group 0.000 abstract 1
- 125000003275 alpha amino acid group Chemical group 0.000 abstract 1
- 125000003368 amide group Chemical group 0.000 abstract 1
- 230000003042 antagnostic effect Effects 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000001769 aryl amino group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 125000005841 biaryl group Chemical group 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 125000001841 imino group Chemical group [H]N=* 0.000 abstract 1
- 208000026278 immune system disease Diseases 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
- C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C275/42—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
- C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
-
- 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
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
-
- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Immunology (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
A találmány tárgya VLA-4 antagonista hatású vegyületek, előállításukés felhasználásuk. A vegyületek (I) általános képletében R1 adottesetben szubsztituált alkil-, alkenil-, alkinil-, adott esetben aromásgyűrűvel kondenzált cikloalkil-, cikloalkenil-, aril-, biaril-,alkoxi-, alkenil-oxi-, alkinil-oxi-, aralkoxi-, alkil-amino-, alkenil-amino-, alkinil-amino-, aril-oxi-, aril-amino- vagy heterociklusoscsoport; R2(CH2)q-V-(CH2)q-Vr-R8 általános képletű csoport; R3hidrogénatom, alkil-, alkenil-, aril- vagy heteroarilcsoport; R4hidrogénatom, adott esetben szubsztituált aril-, alkil-, cikloalkil-,alkenil-, cikloalkenil-, alkinil-, heterociklusos csoport,heterociklusos-karbonil-, amino-karbonil-, amido- vagy acilcsoport; R5adott esetben szubsztituált alkil-, alkenil-, alkinil-, cikloalkil-,cikloalkenilcsoport; R6 adott esetben szubsztituált alkil-, alkenil-,alkinil-, cikloalkil-, cikloalkenil-, aralkil-, acil-amino-alkil-csoport vagy egy aminosav oldallánc; R7 és R8 hidrogénatom, adottesetben szubsztituált alkil-, alkenil-, aril-, heteroarilcsoport; vagyR2 és R6 egy heterogyűrűt képez; V oxigénatom, iminocsoport, kénatom,szulfinil- vagy szulfonil csoport; X szulfo-, karboxil-, PO3H, OPO3H,CO2R5, SO2R5 vagy CON(R4)2 általános képletű csoport; W CH csoportvagy nitrogénatom; Y karbonil-, szulfonil- vagy PO2 csoport; Z(CH2)n', CHR6 vagy NR7 általános képletű csoport; n és n' 0-4; m és p1-4; q és q' 1-5; és r nulla vagy 1. Az (I) általános képletűvegyületeket tartalmazó gyógyszerkészítmények gyulladásos, immun- ésautoimmun betegségek kezelésére használhatók. ÓThe subject of the invention is VLA-4 antagonistic compounds, their production and use. In the general formula of the compounds (I), R1 optionally substituted alkyl-, alkenyl-, alkynyl-, optionally condensed with an aromatic ring, cycloalkyl-, cycloalkenyl-, aryl-, biaryl-, alkoxy-, alkenyloxy-, alkynyloxy-, aralkyloxy- , alkylamino, alkenylamino, alkynylamino, aryloxy, arylamino or heterocyclic; a group of formula R2(CH2)q-V-(CH2)q-Vr-R8; R3 is hydrogen, alkyl, alkenyl, aryl or heteroaryl; R4 is a hydrogen atom, an optionally substituted aryl, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, heterocyclic group, heterocyclic carbonyl, aminocarbonyl, amido or acyl group; R5 optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl; R6 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aralkyl, acylaminoalkyl or an amino acid side chain; R7 and R8 are a hydrogen atom, an optionally substituted alkyl, alkenyl, aryl, heteroaryl group; orR 2 and R 6 form a heteroring; V is an oxygen atom, imino group, sulfur atom, sulfinyl or sulfonyl group; X is a sulfo-, carboxyl-, PO3H, OPO3H, CO2R5, SO2R5 or CON(R4)2 group; W CH group or nitrogen atom; Y is a carbonyl, sulfonyl or PO2 group; a group of formula Z(CH2)n', CHR6 or NR7; n and n' are 0-4; m and p1-4; q and q' 1-5; and r is zero or 1. Pharmaceutical preparations containing compounds of the general formula (I) can be used for the treatment of inflammatory, immune and autoimmune diseases. HE
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US1233698A | 1998-01-23 | 1998-01-23 | |
| US11072398P | 1998-12-03 | 1998-12-03 | |
| PCT/EP1999/000384 WO1999037605A1 (en) | 1998-01-23 | 1999-01-21 | Vla-4 antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0100336A2 true HUP0100336A2 (en) | 2001-07-30 |
| HUP0100336A3 HUP0100336A3 (en) | 2002-11-28 |
Family
ID=26683440
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0100336A HUP0100336A3 (en) | 1998-01-23 | 1999-01-21 | Vla-4 antagonists, pharmaceutical compositions comprising them and process for preparing them |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP1049665A1 (en) |
| JP (1) | JP4564654B2 (en) |
| KR (1) | KR20010034317A (en) |
| CN (1) | CN1294576A (en) |
| AU (1) | AU746174B2 (en) |
| BR (1) | BR9907733A (en) |
| CA (1) | CA2318639A1 (en) |
| EE (1) | EE200000428A (en) |
| HU (1) | HUP0100336A3 (en) |
| ID (1) | ID26665A (en) |
| IL (1) | IL137329A0 (en) |
| NO (1) | NO20003694L (en) |
| WO (1) | WO1999037605A1 (en) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUP0201213A3 (en) | 1999-01-22 | 2003-02-28 | Wyeth Corp | Pirimidinyl, pirazinyl and thiadiazolyl phenylalanin derivatives which treat vla-4 related disorders and pharaceutical compositions containing them |
| WO2000043372A1 (en) * | 1999-01-22 | 2000-07-27 | Elan Pharmaceuticals, Inc. | Acyl derivatives which treat vla-4 related disorders |
| US6436904B1 (en) | 1999-01-25 | 2002-08-20 | Elan Pharmaceuticals, Inc. | Compounds which inhibit leukocyte adhesion mediated by VLA-4 |
| EP1161416B1 (en) | 1999-03-01 | 2004-04-14 | Elan Pharmaceuticals, Inc. | Alpha-aminoacetic acid derivatives useful as alpha 4 beta 7 - receptor antagonists |
| WO2001042192A2 (en) * | 1999-12-07 | 2001-06-14 | Novartis Ag | Vla-4 integrin antagonists |
| JP2003519697A (en) | 1999-12-28 | 2003-06-24 | ファイザー・プロダクツ・インク | Non-peptide VLA-4-dependent cell binding inhibitors useful for the treatment of inflammatory diseases, autoimmune diseases and respiratory diseases |
| DE10019755A1 (en) * | 2000-04-20 | 2001-11-08 | Bayer Ag | New cyclic carboxylic acids are integrin antagonists, useful for treating inflammatory diseases, autoimmune and immune disorders, e.g. atherosclerosis, asthma and diabetes |
| GB2369357A (en) * | 2000-10-09 | 2002-05-29 | Bayer Ag | Aliphatic, cyclic amino carboxylic acids as integrin antagonists |
| GB2367816A (en) | 2000-10-09 | 2002-04-17 | Bayer Ag | Urea- and thiourea-containing derivatives of beta-amino acids |
| GB2377933A (en) | 2001-07-06 | 2003-01-29 | Bayer Ag | Succinic acid derivatives useful as integrin antagonists |
| TWI281470B (en) | 2002-05-24 | 2007-05-21 | Elan Pharm Inc | Heterocyclic compounds which inhibit leukocyte adhesion mediated by alpha4 integrins |
| TW200307671A (en) | 2002-05-24 | 2003-12-16 | Elan Pharm Inc | Heteroaryl compounds which inhibit leukocyte adhesion mediated by α 4 integrins |
| TW200610754A (en) * | 2004-06-14 | 2006-04-01 | Daiichi Seiyaku Co | Vla-4 inhibitor |
| GB0523576D0 (en) * | 2005-11-18 | 2005-12-28 | Theradeas Ltd | Drug composition and its use in therapy |
| EP2124996A4 (en) | 2007-02-20 | 2010-03-24 | Merrimack Pharmaceuticals Inc | Methods of treating multiple sclerosis by administration of alpha-fetoprotein in combination with an integrin antagonist |
| CA2721093A1 (en) | 2008-04-11 | 2009-10-15 | Merrimack Pharmaceuticals, Inc. | Human serum albumin linkers and conjugates thereof |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6306840B1 (en) * | 1995-01-23 | 2001-10-23 | Biogen, Inc. | Cell adhesion inhibitors |
| EP1042279B1 (en) * | 1997-12-23 | 2005-03-02 | Aventis Pharma Limited | Substituted beta-alanines |
-
1999
- 1999-01-21 EE EEP200000428A patent/EE200000428A/en unknown
- 1999-01-21 CA CA002318639A patent/CA2318639A1/en not_active Abandoned
- 1999-01-21 BR BR9907733-7A patent/BR9907733A/en not_active IP Right Cessation
- 1999-01-21 ID IDW20001404A patent/ID26665A/en unknown
- 1999-01-21 AU AU28292/99A patent/AU746174B2/en not_active Ceased
- 1999-01-21 CN CN99803780A patent/CN1294576A/en active Pending
- 1999-01-21 JP JP2000528529A patent/JP4564654B2/en not_active Expired - Fee Related
- 1999-01-21 WO PCT/EP1999/000384 patent/WO1999037605A1/en not_active Application Discontinuation
- 1999-01-21 IL IL13732999A patent/IL137329A0/en unknown
- 1999-01-21 HU HU0100336A patent/HUP0100336A3/en unknown
- 1999-01-21 EP EP99908811A patent/EP1049665A1/en not_active Withdrawn
- 1999-01-21 KR KR1020007008039A patent/KR20010034317A/en not_active Application Discontinuation
-
2000
- 2000-07-19 NO NO20003694A patent/NO20003694L/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| WO1999037605A1 (en) | 1999-07-29 |
| JP2002501039A (en) | 2002-01-15 |
| NO20003694L (en) | 2000-09-20 |
| EE200000428A (en) | 2001-12-17 |
| HUP0100336A3 (en) | 2002-11-28 |
| NO20003694D0 (en) | 2000-07-19 |
| ID26665A (en) | 2001-01-25 |
| AU746174B2 (en) | 2002-04-18 |
| JP4564654B2 (en) | 2010-10-20 |
| AU2829299A (en) | 1999-08-09 |
| EP1049665A1 (en) | 2000-11-08 |
| IL137329A0 (en) | 2001-07-24 |
| BR9907733A (en) | 2000-10-17 |
| CN1294576A (en) | 2001-05-09 |
| KR20010034317A (en) | 2001-04-25 |
| CA2318639A1 (en) | 1999-07-29 |
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