ZA200104672B - Procollagen C-porteinase inhibitors. - Google Patents

Procollagen C-porteinase inhibitors. Download PDF

Info

Publication number: ZA200104672B
Authority: ZA; South Africa
Prior art keywords: compound; alkyl; aralkyl; heteroaralkyl; resin
Prior art date: 1998-12-10

Application number

ZA200104672A

Other languages

English (en)

Inventor

Sharon Marie Dankwardt

Keith Adrian Murray Walker

Harold Edgar Van Wart

Original Assignee

Hoffmann La Roche

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.)

1998-12-10

Filing date

2001-06-07

Publication date

2002-09-09

2001-06-07 Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche

2002-09-09 Publication of ZA200104672B publication Critical patent/ZA200104672B/en

Links

239000003112 inhibitor Substances 0.000 title claims description 4
108010050808 Procollagen Proteins 0.000 title description 5
150000001875 compounds Chemical class 0.000 claims description 200
-1 aralkenyl Chemical group 0.000 claims description 143
125000000217 alkyl group Chemical group 0.000 claims description 103
229910052739 hydrogen Inorganic materials 0.000 claims description 76
239000001257 hydrogen Substances 0.000 claims description 75
125000004475 heteroaralkyl group Chemical group 0.000 claims description 65
125000003710 aryl alkyl group Chemical group 0.000 claims description 57
125000003118 aryl group Chemical group 0.000 claims description 57
125000000753 cycloalkyl group Chemical group 0.000 claims description 57
125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 55
125000001072 heteroaryl group Chemical group 0.000 claims description 53
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102100028728 Bone morphogenetic protein 1 Human genes 0.000 claims description 39
125000002947 alkylene group Chemical group 0.000 claims description 31
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 25
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 24
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125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 21
238000000034 method Methods 0.000 claims description 21
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125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 11
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235000012424 soybean oil Nutrition 0.000 description 1
230000003595 spectral effect Effects 0.000 description 1
239000007921 spray Substances 0.000 description 1
238000010561 standard procedure Methods 0.000 description 1
239000008107 starch Substances 0.000 description 1
235000019698 starch Nutrition 0.000 description 1
239000008117 stearic acid Substances 0.000 description 1
150000003431 steroids Chemical class 0.000 description 1
238000003860 storage Methods 0.000 description 1
238000007920 subcutaneous administration Methods 0.000 description 1
239000005720 sucrose Substances 0.000 description 1
125000006296 sulfonyl amino group Chemical group [H]N(*)S(*)(=O)=O 0.000 description 1
230000000153 supplemental effect Effects 0.000 description 1
239000000829 suppository Substances 0.000 description 1
239000000725 suspension Substances 0.000 description 1
238000010189 synthetic method Methods 0.000 description 1
239000003826 tablet Substances 0.000 description 1
239000000454 talc Substances 0.000 description 1
229910052623 talc Inorganic materials 0.000 description 1
239000011975 tartaric acid Substances 0.000 description 1
235000002906 tartaric acid Nutrition 0.000 description 1
125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
WHRNULOCNSKMGB-UHFFFAOYSA-N tetrahydrofuran thf Chemical compound C1CCOC1.C1CCOC1 WHRNULOCNSKMGB-UHFFFAOYSA-N 0.000 description 1
125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
WROMPOXWARCANT-UHFFFAOYSA-N tfa trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.OC(=O)C(F)(F)F WROMPOXWARCANT-UHFFFAOYSA-N 0.000 description 1
125000001113 thiadiazolyl group Chemical group 0.000 description 1
BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 description 1
125000005505 thiomorpholino group Chemical group 0.000 description 1
DZLNHFMRPBPULJ-UHFFFAOYSA-N thioproline Chemical compound OC(=O)C1CSCN1 DZLNHFMRPBPULJ-UHFFFAOYSA-N 0.000 description 1
FGMPLJWBKKVCDB-UHFFFAOYSA-N trans-L-hydroxy-proline Natural products ON1CCCC1C(O)=O FGMPLJWBKKVCDB-UHFFFAOYSA-N 0.000 description 1
238000001890 transfection Methods 0.000 description 1
230000009466 transformation Effects 0.000 description 1
238000000844 transformation Methods 0.000 description 1
238000013519 translation Methods 0.000 description 1
230000014621 translational initiation Effects 0.000 description 1
150000003852 triazoles Chemical class 0.000 description 1
125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 description 1
LEIMLDGFXIOXMT-UHFFFAOYSA-N trimethylsilyl cyanide Chemical compound C[Si](C)(C)C#N LEIMLDGFXIOXMT-UHFFFAOYSA-N 0.000 description 1
125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
229960000281 trometamol Drugs 0.000 description 1
238000000108 ultra-filtration Methods 0.000 description 1
210000004325 uterine smooth muscle cell Anatomy 0.000 description 1
235000013311 vegetables Nutrition 0.000 description 1
239000003981 vehicle Substances 0.000 description 1
125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
JPZXHKDZASGCLU-LBPRGKRZSA-N β-(2-naphthyl)-alanine Chemical compound C1=CC=CC2=CC(C[C@H](N)C(O)=O)=CC=C21 JPZXHKDZASGCLU-LBPRGKRZSA-N 0.000 description 1
ORQXBVXKBGUSBA-QMMMGPOBSA-N β-cyclohexyl-alanine Chemical compound OC(=O)[C@@H](N)CC1CCCCC1 ORQXBVXKBGUSBA-QMMMGPOBSA-N 0.000 description 1

Classifications

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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- 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
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- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
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- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
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- 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
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- C07K5/06104—Dipeptides with the first amino acid being acidic
- 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
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- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
- 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
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- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
- C07K5/06147—Dipeptides with the first amino acid being heterocyclic and His-amino acid; Derivatives thereof
- 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
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- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
- C07K5/06156—Dipeptides with the first amino acid being heterocyclic and Trp-amino acid; Derivatives thereof
- 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
- C07K5/06165—Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof
- 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
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
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Landscapes

Chemical & Material Sciences (AREA)
Health & Medical Sciences (AREA)
Organic Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Genetics & Genomics (AREA)
Biophysics (AREA)
Molecular Biology (AREA)
Biochemistry (AREA)
Proteomics, Peptides & Aminoacids (AREA)
Engineering & Computer Science (AREA)
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General Chemical & Material Sciences (AREA)
Pharmacology & Pharmacy (AREA)
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Animal Behavior & Ethology (AREA)
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Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Peptides Or Proteins (AREA)
Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

ZA200104672A 1998-12-10 2001-06-07 Procollagen C-porteinase inhibitors. ZA200104672B (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US11166198P	1998-12-10	1998-12-10

Publications (1)

Publication Number	Publication Date
ZA200104672B true ZA200104672B (en)	2002-09-09

Family

ID=22339762

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
ZA200104672A ZA200104672B (en)	1998-12-10	2001-06-07	Procollagen C-porteinase inhibitors.

Country Status (12)

Country	Link
US (2)	US6426402B1 (tr)
EP (1)	EP1137661A1 (tr)
JP (1)	JP2002531576A (tr)
KR (1)	KR20010080709A (tr)
CN (1)	CN1330661A (tr)
AR (1)	AR021596A1 (tr)
AU (1)	AU772575B2 (tr)
BR (1)	BR9916004A (tr)
CA (1)	CA2352740A1 (tr)
TR (1)	TR200101663T2 (tr)
WO (1)	WO2000034313A1 (tr)
ZA (1)	ZA200104672B (tr)

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US7244853B2 (en)	2001-05-09	2007-07-17	President And Fellows Of Harvard College	Dioxanes and uses thereof
EP1469875A1 (en) *	2002-01-29	2004-10-27	Wyeth	Compositions and methods for modulating connexin hemichannels
FR2840897B1 (fr)	2002-06-14	2004-09-10	Fournier Lab Sa	Nouveaux derives d'arylsulfonamides et leur utilisation en therapeutique
US7652036B2 (en)	2003-02-25	2010-01-26	Topotarget Uk Limited	Carbamic acid compounds comprising a bicyclic heteroaryl group as HDAC inhibitors
US20040213758A1 (en) *	2003-04-23	2004-10-28	Rimon Therapeutics Ltd.	Hydroxyamate-containing materials for the inhibition of matrix metalloproteinases
US20070160655A1 (en) *	2003-04-23	2007-07-12	Sefton Michael V	Hydroxyamate-containing materials for the inhibition of matrix metalloproteinases
US7317019B2 (en)	2003-08-21	2008-01-08	Bristol Myers Squibb Co.	N-alkylated diaminopropane derivatives as modulators of chemokine receptor activity
KR100629712B1 (ko) *	2003-08-26	2006-09-29	(주)아모레퍼시픽	항노화 효과를 나타내는 히드록삼산 유도체 및 이의제조방법
WO2006102557A2 (en)	2005-03-22	2006-09-28	The President And Fellows Of Harvard College	Treatment of protein degradation disorders
CA2642288C (en)	2006-02-14	2014-10-07	Dana-Farber Cancer Institute, Inc.	Histone deacetylase inhibitors
JP5441416B2 (ja)	2006-02-14	2014-03-12	プレジデントアンドフェロウズオブハーバードカレッジ	二官能性ヒストンデアセチラーゼインヒビター
AU2007248656B2 (en)	2006-05-03	2013-04-04	Dana-Farber Cancer Institute, Inc.	Histone deacetylase and tubulin deacetylase inhibitors
WO2009097893A1 (en) *	2008-02-04	2009-08-13	Proyecto De Biomedicina Cima, S.L.	Methods for the treatment of cardiac disease associated to myocardial fibrosis using an inhibitor of pcp
EP2280601A4 (en) *	2008-02-21	2012-08-29	Sequoia Pharmaceuticals Inc	AMINO ACID HEMMER OF CYTOCHROM P450
US8440716B2 (en)	2008-07-23	2013-05-14	President And Fellows Of Harvard College	Deacetylase inhibitors and uses thereof
US8580859B2 (en)	2008-08-01	2013-11-12	Bioxiness Pharmaceuticals, Inc.	Methionine analogs and methods of using same
WO2011019393A2 (en)	2009-08-11	2011-02-17	President And Fellows Of Harvard College	Class- and isoform-specific hdac inhibitors and uses thereof
CR20160316A (es) *	2014-01-10	2016-09-19	Glaxosmithkline Intellectual Property (No 2) Ltd	Compuestos derivados de hidroxiformamida y usos del mismo
JP2018525353A (ja) *	2015-07-09	2018-09-06	グラクソスミスクライン、インテレクチュアル、プロパティー、（ナンバー２）、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅＩｎｔｅｌｌｅｃｔｕａｌＰｒｏｐｅｒｔｙ（Ｎｏ．２）Ｌｉｍｉｔｅｄ	Ｂｍｐ１、ｔｌｌ１および／またはｔｌｌ２の阻害剤としての使用するための、ｎ−ヒドロキシホルムアミド化合物およびそれらを含んでなる組成物
US9813673B2 (en)	2016-01-20	2017-11-07	Gerard Dirk Smits	Holographic video capture and telepresence system
CN115197102B (zh) *	2021-04-12	2023-10-20	山东大学	类肽异羟肟酸类恶性疟原虫氨肽酶抑制剂及其制备方法和应用

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1999
- 1999-12-06 AU AU25375/00A patent/AU772575B2/en not_active Ceased
- 1999-12-06 JP JP2000586755A patent/JP2002531576A/ja active Pending
- 1999-12-06 BR BR9916004-8A patent/BR9916004A/pt not_active IP Right Cessation
- 1999-12-06 CN CN99814311A patent/CN1330661A/zh active Pending
- 1999-12-06 WO PCT/EP1999/009519 patent/WO2000034313A1/en not_active Application Discontinuation
- 1999-12-06 KR KR1020017007101A patent/KR20010080709A/ko not_active Application Discontinuation
- 1999-12-06 TR TR2001/01663T patent/TR200101663T2/tr unknown
- 1999-12-06 CA CA002352740A patent/CA2352740A1/en not_active Abandoned
- 1999-12-06 EP EP99968338A patent/EP1137661A1/en not_active Withdrawn
- 1999-12-09 AR ARP990106263A patent/AR021596A1/es unknown
- 1999-12-10 US US09/459,201 patent/US6426402B1/en not_active Expired - Fee Related
2001
- 2001-06-07 ZA ZA200104672A patent/ZA200104672B/en unknown
2002
- 2002-02-07 US US10/072,730 patent/US6951918B2/en not_active Expired - Fee Related

Also Published As

Publication number	Publication date
US20020169133A1 (en)	2002-11-14
AU772575B2 (en)	2004-04-29
AU2537500A (en)	2000-06-26
CN1330661A (zh)	2002-01-09
BR9916004A (pt)	2001-10-02
CA2352740A1 (en)	2000-06-15
TR200101663T2 (tr)	2001-11-21
US6426402B1 (en)	2002-07-30
KR20010080709A (ko)	2001-08-22
JP2002531576A (ja)	2002-09-24
AR021596A1 (es)	2002-07-31
WO2000034313A1 (en)	2000-06-15
EP1137661A1 (en)	2001-10-04
US6951918B2 (en)	2005-10-04

Publication	Publication Date	Title
ZA200104672B (en)	2002-09-09	Procollagen C-porteinase inhibitors.
EP1112284B1 (en)	2006-04-19	Piperazine-4-phenyl derivatives as inhibitors of the interaction between mdm2 and p53
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