DK0752987T3 - Pyrimidinylderivater som interleukininhibitorer - Google Patents

Pyrimidinylderivater som interleukininhibitorer

Info

Publication number: DK0752987T3
Authority: DK; Denmark
Prior art keywords: beta; compounds; aspartic acid; protease activity; pyrimidinyl
Prior art date: 1994-03-31

Application number

DK95915448T

Other languages

English (en)

Inventor

Roland E Dolle

Catherine P Prouty

Prasad V Chaturvedula

Stanley J Schmidt

Original Assignee

Vertex Pharma

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

1994-03-31

Filing date

1995-03-29

Publication date

2004-03-15

1995-03-29 Application filed by Vertex Pharma filed Critical Vertex Pharma

2004-03-15 Application granted granted Critical

2004-03-15 Publication of DK0752987T3 publication Critical patent/DK0752987T3/da

Links

229940046732 interleukin inhibitors Drugs 0.000 title 1
125000000714 pyrimidinyl group Chemical group 0.000 title 1
150000001875 compounds Chemical class 0.000 abstract 3
108091005804 Peptidases Proteins 0.000 abstract 2
239000004365 Protease Substances 0.000 abstract 2
102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 abstract 2
230000000694 effects Effects 0.000 abstract 2
TVZJDRYAFYBTRU-YFKPBYRVSA-N (2s)-2-(pyrimidin-2-ylamino)butanedioic acid Chemical compound OC(=O)C[C@@H](C(O)=O)NC1=NC=CC=N1 TVZJDRYAFYBTRU-YFKPBYRVSA-N 0.000 abstract 1
LOGFVTREOLYCPF-KXNHARMFSA-N (2s,3r)-2-[[(2r)-1-[(2s)-2,6-diaminohexanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoic acid Chemical compound C[C@@H](O)[C@@H](C(O)=O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](N)CCCCN LOGFVTREOLYCPF-KXNHARMFSA-N 0.000 abstract 1
CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical class CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 abstract 1
102000004190 Enzymes Human genes 0.000 abstract 1
108090000790 Enzymes Proteins 0.000 abstract 1
102000003777 Interleukin-1 beta Human genes 0.000 abstract 1
108090000193 Interleukin-1 beta Proteins 0.000 abstract 1
241000124008 Mammalia Species 0.000 abstract 1
235000003704 aspartic acid Nutrition 0.000 abstract 1
-1 aspartic acid aldehydes Chemical class 0.000 abstract 1
OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 abstract 1
201000010099 disease Diseases 0.000 abstract 1
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
239000003112 inhibitor Substances 0.000 abstract 1
230000002401 inhibitory effect Effects 0.000 abstract 1
230000005764 inhibitory process Effects 0.000 abstract 1
238000000034 method Methods 0.000 abstract 1
239000000203 mixture Substances 0.000 abstract 1
230000000144 pharmacologic effect Effects 0.000 abstract 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
- A—HUMAN NECESSITIES
- 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]
- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
- C07F9/6509—Six-membered rings
- C07F9/6512—Six-membered rings having the nitrogen atoms in positions 1 and 3
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Molecular Biology (AREA)
Biochemistry (AREA)
Proteomics, Peptides & Aminoacids (AREA)
Genetics & Genomics (AREA)
Biophysics (AREA)
Public Health (AREA)
Animal Behavior & Ethology (AREA)
Pharmacology & Pharmacy (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Veterinary Medicine (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Crystallography & Structural Chemistry (AREA)
Immunology (AREA)
Pain & Pain Management (AREA)
Rheumatology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Enzymes And Modification Thereof (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

DK95915448T 1994-03-31 1995-03-29 Pyrimidinylderivater som interleukininhibitorer DK0752987T3 (da)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US22171294A	1994-03-31	1994-03-31
PCT/US1995/003909 WO1995026958A1 (en)	1994-03-31	1995-03-29	Pyrimidinyl derivatives as interleukin inhibitors

Publications (1)

Publication Number	Publication Date
DK0752987T3 true DK0752987T3 (da)	2004-03-15

Family

ID=22829018

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
DK95915448T DK0752987T3 (da)	1994-03-31	1995-03-29	Pyrimidinylderivater som interleukininhibitorer

Country Status (18)

Country	Link
US (3)	US5670494A (da)
EP (1)	EP0752987B1 (da)
JP (1)	JP3703836B2 (da)
CN (2)	CN1118458C (da)
AT (1)	ATE254111T1 (da)
AU (1)	AU703451B2 (da)
CA (1)	CA2186511C (da)
DE (1)	DE69532113T2 (da)
DK (1)	DK0752987T3 (da)
ES (1)	ES2210289T3 (da)
FI (1)	FI112943B (da)
HK (1)	HK1012623A1 (da)
HU (1)	HU224731B1 (da)
MX (1)	MX9604420A (da)
NO (1)	NO308603B1 (da)
NZ (1)	NZ283876A (da)
PT (1)	PT752987E (da)
WO (1)	WO1995026958A1 (da)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US5874424A (en) *	1995-12-20	1999-02-23	Vertex Pharmaceuticals Incorporated	Inhibitors of interleukin-1β converting enzyme
US6204261B1 (en) *	1995-12-20	2001-03-20	Vertex Pharmaceuticals Incorporated	Inhibitors of interleukin-1β Converting enzyme inhibitors
US6008217A (en) *	1995-12-20	1999-12-28	Vertex Pharmaceuticals Incorporated	Inhibitors of interleukin-1β converting enzyme
US5714484A (en) *	1993-12-08	1998-02-03	Prototek, Inc.	α-(1,3-dicarbonylenol ether) methyl ketones as cysteine protease inhibitors
HU224731B1 (en)	1994-03-31	2006-01-30	Vertex Pharma	Pyrimidinyl derivatives as interleukin inhibitors and pharmaceutical compositions containing them
US5756466A (en) *	1994-06-17	1998-05-26	Vertex Pharmaceuticals, Inc.	Inhibitors of interleukin-1β converting enzyme
US6420522B1 (en)	1995-06-05	2002-07-16	Vertex Pharmaceuticals Incorporated	Inhibitors of interleukin-1β converting enzyme
US5847135A (en) *	1994-06-17	1998-12-08	Vertex Pharmaceuticals, Incorporated	Inhibitors of interleukin-1β converting enzyme
US5716929A (en) *	1994-06-17	1998-02-10	Vertex Pharmaceuticals, Inc.	Inhibitors of interleukin-1β converting enzyme
US6001814A (en) *	1994-11-21	1999-12-14	Cortech Inc.	Serine protease inhibitors
US6011158A (en) *	1994-12-13	2000-01-04	Corvas International, Inc.	Aromatic heterocyclic derivatives as enzyme inhibitors
BR9509994A (pt) *	1994-12-13	1997-12-30	Corvas Int Inc	Derivados heterocíclicos aromáticos como inibidores de enzimas
CA2215211A1 (en) *	1995-03-31	1996-10-03	Takeda Chemical Industries, Ltd.	Cysteine protease inhibitor
US5948785A (en) *	1995-04-27	1999-09-07	The Green Cross Corporation	Heterocyclic amide compounds and pharmaceutical use of the same
US5843904A (en) *	1995-12-20	1998-12-01	Vertex Pharmaceuticals, Inc.	Inhibitors of interleukin-1βconverting enzyme
US6136834A (en)	1995-12-27	2000-10-24	Ono Pharmaceutical Co., Ltd.	Tetrazole compounds and pharmaceutical agents containing such derivative
KR20000049050A (ko) *	1996-10-11	2000-07-25	로즈 암스트롱, 크리스틴 에이. 트러트웨인	술폰아미드 치환된 아스파르트산 인터루킨-1β 전환 효소 억제제
DK0946502T3 (da)	1996-10-11	2003-04-07	Abbott Gmbh & Co Kg	Sulfonamidinhibitorer for det interleukin-1beta-omdannende enzym
US5919790A (en) *	1996-10-11	1999-07-06	Warner-Lambert Company	Hydroxamate inhibitors of interleukin-1β converting enzyme
JP2002509153A (ja) *	1998-01-20	2002-03-26	ワーナー−ランバート・カンパニー	インターロイキン−１β変換酵素（ＩＣＥ）のインビボ阻害剤としてのＮ−［２−（５−ベンジルオキシカルボニル−アミノ−６−オキソ−２−（４−フルオロフェニル）−１，６−ジヒドロ−１−ピリミジニル）アセトキシル］−Ｌ−アスパラギン酸アルデヒド
WO1999046248A1 (en)	1998-03-09	1999-09-16	Vertex Pharmaceuticals Incorporated	1,2-diazepane derivatives as interleukin-1beta converting enzyme inhibitors
PT1064298E (pt)	1998-03-19	2009-01-02	Vertex Pharma	Inibidores de caspasas
JP2003520185A (ja) *	1998-06-03	2003-07-02	コーテックインコーポレーテッド	セリンプロテアーゼ阻害剤としてのα−ケトオキサジアゾール類
EP1098902A4 (en)	1998-07-23	2002-07-24	Yeda Res & Dev	TREATMENT OF AUTOIMMUNE DISEASES BY COPOLYMER 1 AND SIMILAR COPOLYMERS AND PEPTIDES
ES2527760T3 (es) *	1998-07-23	2015-01-29	Yeda Research And Development Co., Ltd.	Tratamiento de enfermedad de Crohn con copolímero 1 y polipéptidos
US6800287B2 (en) *	1998-09-25	2004-10-05	Yeda Research And Development Co., Ltd.	Copolymer 1 related polypeptides for use as molecular weight markers and for therapeutic use
US6972296B2 (en)	1999-05-07	2005-12-06	Encysive Pharmaceuticals Inc.	Carboxylic acid derivatives that inhibit the binding of integrins to their receptors
US7022663B2 (en) *	2000-02-18	2006-04-04	Yeda Research And Development Co., Ltd.	Oral, nasal and pulmonary dosage formulations of copolymer 1
WO2001087328A2 (en)	2000-05-12	2001-11-22	Immunex Corporation	Interleukin-1 inhibitors in the treatment of diseases
PE20011350A1 (es)	2000-05-19	2002-01-15	Vertex Pharma	PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE)
US20020077278A1 (en)	2000-06-05	2002-06-20	Yong V. Wee	Use of glatiramer acetate (copolymer 1) in the treatment of central nervous system disorders
WO2002076503A1 (en) *	2000-06-20	2002-10-03	Mayo Foundation For Medical Education And Research	Treatment of central nervous system diseases by antibodies against glatiramer acetate
US6943173B2 (en)	2000-07-18	2005-09-13	Neurogen Corporation	5-substituted 2-aryl-4-pyrimidinones
ES2349033T3 (es) *	2001-12-04	2010-12-22	Teva Pharmaceutical Industries, Ltd.	Procedimientos para la medida de la actividad del acetato de glatiramer.
WO2003068242A1 (en) *	2002-02-11	2003-08-21	Vertex Pharmaceuticals Incorporated	Phospholipids as caspase inhibitor prodrugs
US7001899B2 (en) *	2002-06-10	2006-02-21	The Procter & Gamble Company	Interleukin converting enzyme inhibitors
EP1553090A4 (en) *	2002-06-14	2006-07-05	Ajinomoto Kk	PROCESS FOR PREPARING A PYRIMIDINE COMPOUND
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
CA2566362C (en) *	2004-05-15	2013-09-10	Vertex Pharmaceuticals Incorporated	Treating seizures using ice inhibitors
CN1980658A (zh)	2004-05-27	2007-06-13	沃泰克斯药物股份有限公司	治疗自身炎性疾病的ice抑制剂
WO2006057961A1 (en)	2004-11-24	2006-06-01	Vertex Pharmaceuticals Incorporated	3-[2-(3-acylamino-2-oxo-2h-pyridin-1-yl)-acetylamino]-4-oxo-pentanoic acid derivatives and their use as caspase inhibitors
CN101772577A (zh) *	2007-08-03	2010-07-07	塞诺菲-安万特股份有限公司	半胱天冬蛋白酶成像探针
EP2262783A2 (en) *	2008-02-21	2010-12-22	Sanofi-Aventis	Covalently binding imaging probes
WO2012061786A1 (en)	2010-11-05	2012-05-10	Brandeis University	Ice cleaved alpha-synuclein a biomarker
US9956260B1 (en)	2011-07-22	2018-05-01	The J. David Gladstone Institutes	Treatment of HIV-1 infection and AIDS
EP2848696A1 (en)	2013-09-13	2015-03-18	Sanofi-Aventis Deutschland GmbH	Caspase-1 imaging probes

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US5441960A (en) *	1992-04-16	1995-08-15	Zeneca Limited	1-pyrimidinylacetamide human leukocyte elastate inhibitors
HU224731B1 (en) *	1994-03-31	2006-01-30	Vertex Pharma	Pyrimidinyl derivatives as interleukin inhibitors and pharmaceutical compositions containing them

1995
- 1995-03-29 HU HU9602664A patent/HU224731B1/hu not_active IP Right Cessation
- 1995-03-29 JP JP52582195A patent/JP3703836B2/ja not_active Expired - Fee Related
- 1995-03-29 NZ NZ283876A patent/NZ283876A/en not_active IP Right Cessation
- 1995-03-29 AU AU22323/95A patent/AU703451B2/en not_active Ceased
- 1995-03-29 CA CA002186511A patent/CA2186511C/en not_active Expired - Fee Related
- 1995-03-29 EP EP95915448A patent/EP0752987B1/en not_active Expired - Lifetime
- 1995-03-29 MX MX9604420A patent/MX9604420A/es active IP Right Grant
- 1995-03-29 PT PT95915448T patent/PT752987E/pt unknown
- 1995-03-29 CN CN95193258A patent/CN1118458C/zh not_active Expired - Fee Related
- 1995-03-29 DK DK95915448T patent/DK0752987T3/da active
- 1995-03-29 ES ES95915448T patent/ES2210289T3/es not_active Expired - Lifetime
- 1995-03-29 CN CNA031452183A patent/CN1504462A/zh active Pending
- 1995-03-29 DE DE69532113T patent/DE69532113T2/de not_active Expired - Lifetime
- 1995-03-29 AT AT95915448T patent/ATE254111T1/de not_active IP Right Cessation
- 1995-03-29 WO PCT/US1995/003909 patent/WO1995026958A1/en active IP Right Grant
- 1995-11-20 US US08/559,870 patent/US5670494A/en not_active Expired - Lifetime
1996
- 1996-09-26 NO NO964058A patent/NO308603B1/no unknown
- 1996-09-27 FI FI963897A patent/FI112943B/fi not_active IP Right Cessation
1997
- 1997-06-17 US US08/877,380 patent/US6162800A/en not_active Expired - Lifetime
1998
- 1998-12-16 HK HK98113788A patent/HK1012623A1/xx not_active IP Right Cessation
2000
- 2000-12-19 US US09/740,623 patent/US6407080B2/en not_active Expired - Fee Related

Also Published As

Publication number	Publication date
US6162800A (en)	2000-12-19
EP0752987A4 (en)	1997-04-09
DE69532113T2 (de)	2004-07-29
NO964058D0 (no)	1996-09-26
HU9602664D0 (en)	1996-11-28
NZ283876A (en)	2001-03-30
ES2210289T3 (es)	2004-07-01
CN1118458C (zh)	2003-08-20
WO1995026958A1 (en)	1995-10-12
FI112943B (fi)	2004-02-13
CN1149292A (zh)	1997-05-07
PT752987E (pt)	2004-03-31
CN1504462A (zh)	2004-06-16
EP0752987B1 (en)	2003-11-12
AU703451B2 (en)	1999-03-25
DE69532113D1 (de)	2003-12-18
FI963897A (fi)	1996-09-27
ATE254111T1 (de)	2003-11-15
HK1012623A1 (en)	1999-08-06
HU224731B1 (en)	2006-01-30
EP0752987A1 (en)	1997-01-15
CA2186511A1 (en)	1995-10-12
JPH09511249A (ja)	1997-11-11
NO964058L (no)	1996-09-26
CA2186511C (en)	2009-02-10
MX9604420A (es)	1997-12-31
US5670494A (en)	1997-09-23
HUT75715A (en)	1997-05-28
AU2232395A (en)	1995-10-23
US6407080B2 (en)	2002-06-18
JP3703836B2 (ja)	2005-10-05
FI963897A0 (fi)	1996-09-27
US20010003750A1 (en)	2001-06-14
NO308603B1 (no)	2000-10-02

Publication	Publication Date	Title
DK0752987T3 (da)	2004-03-15	Pyrimidinylderivater som interleukininhibitorer
DE69232929D1 (de)	2003-04-03	Saccharinderivate als proteolytische Enzyminhibitoren
FI942423A (fi)	1994-11-26	Sakkariinijohdannisia proteolyyttisen entsyymin inhibiittoreina
MX9206008A (es)	1993-11-01	Inhibidores de enzima proteolitica, derivados de sacarina 2-substituida.
ATE252585T1 (de)	2003-11-15	Bicyclischer lactaminhibitor des interleukin-1- beta-konvertierenden enzyms
HUP0101146A2 (hu)	2001-08-28	Foszfolipáz enzim inhibitor hatású indolszármazékok, valamint a vegyületeket tartalmazó gyógyászati készítmények
NO20052864L (no)	2005-06-13	Nye hydroksyindoler, deres anvendelse som fosfordiesterase 4 inhibitorer samt fremstilling av forbindelser
ATE267168T1 (de)	2004-06-15	Beta-alanin-derivate als zell-adhäsions- inhibitoren
DE69413167D1 (de)	1998-10-15	Peptid-Phosphinyloxymethyl-Ketonen als Inhibitoren von Interleukin-1 beta-konvertierenden Enzymen
DK0559743T3 (da)	1995-07-03	Nye hydroxamsyre- og N-hydroxyurinstofderivater og deres anvendelse
YU89202A (sh)	2006-05-25	Faktor viia inhibitorni derivati (tio)uree, njihovo dobijanje i upotreba
NO20025510D0 (no)	2002-11-15	Tienodibenzoazulenforbindelser som tumor nekrose faktor inhibitorer
DK0765320T3 (da)	2001-11-26	Benzimidazolonderivater med central dopaminerg aktivitet
BR0315662A (pt)	2005-08-30	Derivados de 1-(4-benzil-piperazin-1-il)-3-fenil-propenona
FI970469A0 (fi)	1997-02-04	Bentsimidatsolijohdannaisia, joilla on dopaminerginen aktiivisuus
DK0652874T3 (da)	2004-03-22	2-heterocycliske-5-hydroxy-1,3-pyrimidiner der er nyttige som antiinflammatoriske midler
TR200103550T2 (tr)	2002-05-21	Faktör VIIa inhibitörler.
BR0010748A (pt)	2002-02-19	Compostos heterocìclicos contendo imidazo, suas composições e usos
NO970498L (no)	1997-02-04	Benzimidazolderivater med dopaminergisk aktivitet
TH56149B (th)	2003-04-11	สารประกอบที่ใช้เป็นสารต่อต้านการอักเสบ