IL193951A - A compound with central pyrrolidine units, an intermediate compound for the preparation of the mediated compound, a process for the production of the mediated compound, the use of a mediated compound for the manufacture of a drug, a pharmaceutical preparation, a method for the preparation of a pharmaceutical preparation, and a method for making conventional pharmaceutical salt of a non-salts compound. - Google Patents

A compound with central pyrrolidine units, an intermediate compound for the preparation of the mediated compound, a process for the production of the mediated compound, the use of a mediated compound for the manufacture of a drug, a pharmaceutical preparation, a method for the preparation of a pharmaceutical preparation, and a method for making conventional pharmaceutical salt of a non-salts compound.

Info

Publication number
IL193951A
IL193951A IL193951A IL19395108A IL193951A IL 193951 A IL193951 A IL 193951A IL 193951 A IL193951 A IL 193951A IL 19395108 A IL19395108 A IL 19395108A IL 193951 A IL193951 A IL 193951A
Authority
IL
Israel
Prior art keywords
compound
bridged
preparation
pharmaceutical composition
bridged compound
Prior art date
Application number
IL193951A
Other languages
English (en)
Hebrew (he)
Original Assignee
Pharmascience Inc
Aegera Therapeutics Inc
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.)
Filing date
Publication date
Application filed by Pharmascience Inc, Aegera Therapeutics Inc filed Critical Pharmascience Inc
Publication of IL193951A publication Critical patent/IL193951A/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/4025Heterocyclic 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 not condensed and containing further heterocyclic rings, e.g. cromakalim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08Peptides having 5 to 11 amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/1703Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • A61K38/1709Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • A61K38/1761Apoptosis related proteins, e.g. Apoptotic protease-activating factor-1 (APAF-1), Bax, Bax-inhibitory protein(s)(BI; bax-I), Myeloid cell leukemia associated protein (MCL-1), Inhibitor of apoptosis [IAP] or Bcl-2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/14Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/081Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids

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)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oncology (AREA)
  • Zoology (AREA)
  • Marine Sciences & Fisheries (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
IL193951A 2006-03-16 2008-09-07 A compound with central pyrrolidine units, an intermediate compound for the preparation of the mediated compound, a process for the production of the mediated compound, the use of a mediated compound for the manufacture of a drug, a pharmaceutical preparation, a method for the preparation of a pharmaceutical preparation, and a method for making conventional pharmaceutical salt of a non-salts compound. IL193951A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US78252306P 2006-03-16 2006-03-16
US87699406P 2006-12-26 2006-12-26
PCT/CA2007/000428 WO2007104162A1 (en) 2006-03-16 2007-03-16 Iap bir domain binding compounds

Publications (1)

Publication Number Publication Date
IL193951A true IL193951A (en) 2015-09-24

Family

ID=38509005

Family Applications (1)

Application Number Title Priority Date Filing Date
IL193951A IL193951A (en) 2006-03-16 2008-09-07 A compound with central pyrrolidine units, an intermediate compound for the preparation of the mediated compound, a process for the production of the mediated compound, the use of a mediated compound for the manufacture of a drug, a pharmaceutical preparation, a method for the preparation of a pharmaceutical preparation, and a method for making conventional pharmaceutical salt of a non-salts compound.

Country Status (15)

Country Link
US (5) US7579320B2 (https=)
EP (1) EP2004600A4 (https=)
JP (1) JP5419468B2 (https=)
KR (1) KR101446907B1 (https=)
AU (1) AU2007224932B2 (https=)
BR (1) BRPI0709610A2 (https=)
CA (1) CA2581960C (https=)
IL (1) IL193951A (https=)
MX (1) MX2008011837A (https=)
NO (1) NO20083868L (https=)
NZ (1) NZ571577A (https=)
PH (1) PH12014502420B1 (https=)
SG (1) SG170739A1 (https=)
TW (2) TWI504597B (https=)
WO (1) WO2007104162A1 (https=)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2005274937B2 (en) 2004-07-15 2011-08-18 Medivir Ab IAP binding compounds
MX2007007195A (es) 2004-12-20 2007-10-08 Genentech Inc Inhibidores de pirrolidina de iap.
ES2456671T3 (es) 2005-02-25 2014-04-23 Tetralogic Pharmaceuticals Corporation Inhibidores diméricos de IAP
US7772177B2 (en) * 2005-05-18 2010-08-10 Aegera Therapeutics, Inc. BIR domain binding compounds
US20100256046A1 (en) * 2009-04-03 2010-10-07 Tetralogic Pharmaceuticals Corporation Treatment of proliferative disorders
WO2007048224A1 (en) 2005-10-25 2007-05-03 Aegera Therapeutics Inc. Iap bir domain binding compounds
WO2007106192A2 (en) 2005-12-19 2007-09-20 Genentech, Inc. Inhibitors of iap
TWI504597B (zh) 2006-03-16 2015-10-21 Pharmascience Inc 結合於細胞凋亡抑制蛋白(iap)之桿狀病毒iap重複序列(bir)區域之化合物
BRPI0708942A2 (pt) * 2006-03-21 2011-06-14 Joyant Pharmaceuticals Inc composto promotor de apoptose, uso e mÉtodo de produÇço do mesmo e composiÇço farmacÊutica
AU2007250443B2 (en) 2006-05-16 2013-06-13 Pharmascience Inc. IAP BIR domain binding compounds
WO2008014229A2 (en) * 2006-07-24 2008-01-31 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
KR20090041391A (ko) * 2006-07-24 2009-04-28 테트랄로직 파마슈티칼스 이량체성 iap 길항제
CL2007002166A1 (es) * 2006-07-24 2008-01-25 Tetralogic Pharm Corp Compuestos derivados de heterociclos de nitrogeno, antagonistas de los inhibidores de las proteinas de la apoptosis; sus composiciones farmaceuticas; y uso de dichos compuestos para el tratamiento del cancer.
JP5454943B2 (ja) * 2007-04-12 2014-03-26 ジョイアント ファーマスーティカルズ、インク. 抗癌剤として有用なsmac模倣二量体及び三量体
PE20130150A1 (es) * 2007-04-30 2013-02-27 Genentech Inc Inhibidores de las iap
JP2010528587A (ja) * 2007-05-07 2010-08-26 テトラロジック ファーマシューティカルズ コーポレーション アポトーシス阻害タンパク質のアンタゴニストに対する感受性のバイオマーカーとしてTNFα遺伝子の発現を用いる方法
WO2008144925A1 (en) * 2007-05-30 2008-12-04 Aegera Therapeutics Inc. Iap bir domain binding compounds
MX2010011288A (es) 2008-04-23 2010-11-09 Rigel Pharmaceuticals Inc Compuestos de carboxamida para el tratamiento de trastornos metabolicos.
WO2009136290A1 (en) * 2008-05-05 2009-11-12 Aegera Therapeutics, Inc. Functionalized pyrrolidines and use thereof as iap inhibitors
WO2009155709A1 (en) * 2008-06-27 2009-12-30 Aegera Therapeutics Inc. Bridged secondary amines and use thereof as iap bir domain binding compounds
CN102171209A (zh) * 2008-08-02 2011-08-31 健泰科生物技术公司 Iap抑制剂
WO2010015090A1 (en) * 2008-08-07 2010-02-11 Aegera Therapeutics Inc. Functionalized pyrrolidines and use thereof as iap inhibitors
US20110177060A1 (en) * 2008-09-19 2011-07-21 Aegera Therapeutics, Inc. Iap bir domain binding compounds
US20100317593A1 (en) * 2009-06-12 2010-12-16 Astrazeneca Ab 2,3-dihydro-1h-indene compounds
US8283372B2 (en) 2009-07-02 2012-10-09 Tetralogic Pharmaceuticals Corp. 2-(1H-indol-3-ylmethyl)-pyrrolidine dimer as a SMAC mimetic
EP2784076A1 (en) * 2009-10-28 2014-10-01 Joyant Pharmaceuticals, Inc. Dimeric SMAC mimetics
WO2011098904A1 (en) 2010-02-12 2011-08-18 Aegera Therapeutics, Inc. Iap bir domain binding compounds
UY33236A (es) 2010-02-25 2011-09-30 Novartis Ag Inhibidores dimericos de las iap
WO2012052758A1 (en) * 2010-10-22 2012-04-26 Astrazeneca Ab Response biomarkers for iap antagonists in human cancers
UY33794A (es) 2010-12-13 2012-07-31 Novartis Ag Inhibidores diméricos de las iap
WO2015196091A1 (en) 2014-06-20 2015-12-23 Reform Biologics, Llc Viscosity-reducing excipient compounds for protein formulations
WO2020112855A1 (en) * 2018-11-29 2020-06-04 Reform Biologics, Llc Excipient compounds for protein processing
US10478498B2 (en) 2014-06-20 2019-11-19 Reform Biologics, Llc Excipient compounds for biopolymer formulations
US11357857B2 (en) 2014-06-20 2022-06-14 Comera Life Sciences, Inc. Excipient compounds for protein processing
CA2916970A1 (en) * 2016-01-08 2017-07-08 Pharmascience Inc. A smac mimetic compound for use in the treatment of proliferative diseases
AU2018308116A1 (en) * 2017-07-25 2020-02-13 Hepagene Therapeutics (HK) Limited Dimeric peptide inhibitors of apoptosis proteins
CN109407133B (zh) * 2017-08-18 2023-09-22 南京中硼联康医疗科技有限公司 生物剂量计及具有其的中子捕获治疗系统
JP2021523092A (ja) * 2018-03-21 2021-09-02 ピラマル・ファーマ・リミテッドPiramal Pharma Limited アルファ−(ジアリールメチル)アルキルアミンの改良された不斉合成
WO2020027225A1 (ja) 2018-07-31 2020-02-06 ファイメクス株式会社 複素環化合物
CN113677399B (zh) * 2019-04-05 2024-10-11 和博医药有限公司 凋亡蛋白抑制剂的二价拮抗剂
WO2020223403A1 (en) * 2019-04-29 2020-11-05 The Regents Of The University Of California Anticancer smac derivatives
WO2021020585A1 (ja) 2019-07-31 2021-02-04 ファイメクス株式会社 複素環化合物
JP2023510426A (ja) 2020-01-20 2023-03-13 アストラゼネカ・アクチエボラーグ 癌を治療するための上皮細胞増殖因子受容体チロシンキナーゼ阻害剤
US11814367B2 (en) 2021-03-15 2023-11-14 Maze Therapeutics, Inc. Inhibitors of glycogen synthase 1 (GYS1) and methods of use thereof
JP7260725B1 (ja) * 2021-12-27 2023-04-18 株式会社トクヤマ ペプチド製造方法、保護基の除去方法、及び除去剤
WO2023127331A1 (ja) * 2021-12-27 2023-07-06 株式会社トクヤマ ペプチド製造方法、保護基の除去方法、除去剤、及びベンジル化合物

Family Cites Families (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US93428A (en) * 1869-08-10 Improvement in spurs for excelsior-machines
US180828A (en) * 1876-08-08 Improvement in horse-powers
US207525A (en) * 1878-08-27 Improvement in car-coupling draw-bars
US89896A (en) * 1869-05-11 Improvement in bee-hive
US194741A (en) * 1877-08-28 Improvement in circular looms
US219140A (en) * 1879-09-02 Improvement in the art of ornamenting metallic foils
US69812A (en) * 1867-10-15 Improved refrigerator
US93429A (en) * 1869-08-10 Improvement in flasks for vulcanizing rubber plates for setting teeth
US25347A (en) * 1859-09-06 Improvement
US258581A (en) * 1882-05-30 husset
US211627A (en) * 1879-01-28 Improvement in perforating-stamps
US32437A (en) * 1861-05-28 Improvement in steam-plows
JPH0680077B2 (ja) 1985-02-08 1994-10-12 サントリー株式会社 プロリンエンドペプチダ−ゼインヒビタ−活性を有する新規ペプチド化合物
JPH04208299A (ja) 1990-11-30 1992-07-29 Ajinomoto Co Inc プロリルエンドペプチターゼ阻害ペプチド
US5817667A (en) * 1991-04-17 1998-10-06 University Of Georgia Research Foudation Compounds and methods for the treatment of cancer
US5595756A (en) * 1993-12-22 1997-01-21 Inex Pharmaceuticals Corporation Liposomal compositions for enhanced retention of bioactive agents
AUPN727595A0 (en) * 1995-12-22 1996-01-18 Walter And Eliza Hall Institute Of Medical Research, The Therapeutic compositions
JP4208299B2 (ja) 1998-08-19 2009-01-14 東レ株式会社 金属板貼合わせ成形加工用ポリエステルフィルム
US6110691A (en) 2000-01-06 2000-08-29 Board Of Regents, The University Of Texas System Activators of caspases
US6608026B1 (en) 2000-08-23 2003-08-19 Board Of Regents, The University Of Texas System Apoptotic compounds
US6992063B2 (en) 2000-09-29 2006-01-31 The Trustees Of Princeton University Compositions and method for regulating apoptosis
AU2001293189A1 (en) 2000-09-29 2002-04-08 Trustees Of Princeton University Compositions and methods for regulating apoptosis
WO2002030959A2 (en) 2000-10-13 2002-04-18 Abbott Laboratories Peptides derived from smac (diablo) and methods of use therefor
EP1392317A4 (en) * 2001-05-16 2005-10-19 Antexpharma Inc SUBSTITUTED 1-BENZAZEPINE AND DERIVATIVES THEREOF
CA2449168A1 (en) 2001-05-31 2002-12-05 The Trustees Of Princeton University Iap binding peptides and assays for identifying compounds that bind iap
ES2278928T3 (es) * 2001-06-19 2007-08-16 Altana Pharma Ag Inhibidores de triptasa.
US20060258581A1 (en) 2001-11-21 2006-11-16 Reed John C Methods and composition for derepressions of IAP-inhibited caspase
EP1495124A2 (en) 2002-04-17 2005-01-12 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts Smac-peptides as therapeutics against cancer and autoimmune diseases
WO2004005248A1 (en) * 2002-07-02 2004-01-15 Novartis Ag Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap)
ATE415413T1 (de) 2002-07-15 2008-12-15 Univ Princeton Iap-bindende verbindungen
FR2844271A1 (fr) * 2002-09-09 2004-03-12 Oreal Derives bis-paraphenylenediamine a groupement pyrrolidinyle et utilisation de ces derives pour la coloration de fibres keratiniques
US7229617B2 (en) 2002-11-27 2007-06-12 Irm Llc Methods and compositions for inducing apoptosis in cancer cells
WO2004066958A2 (en) 2003-01-30 2004-08-12 The Trustees Of Princeton University Caspase-9:bir3 domain of xiap complexes and methods of use
WO2005049853A2 (en) * 2003-11-13 2005-06-02 Genentech, Inc. Compositions and methods for screening pro-apoptotic compounds
CA2553871A1 (en) 2004-01-16 2005-08-04 The Regents Of The University Of Michigan Smac peptidomimetics and the uses thereof
KR20060126548A (ko) 2004-02-05 2006-12-07 노파르티스 아게 (a) DNA 토포이소머라제 억제제 및 (b) IAP 억제제조합물
CN1926118A (zh) * 2004-03-01 2007-03-07 德克萨斯大学董事会 二聚的小分子细胞凋亡增强剂
WO2005094818A1 (en) 2004-03-23 2005-10-13 Genentech, Inc. Azabicyclo-octane inhibitors of iap
RS52545B (sr) 2004-04-07 2013-04-30 Novartis Ag Inhibitori protein apoptoze (iap)
BRPI0511350A (pt) 2004-07-02 2007-12-04 Genentech Inc composto, métodos de indução da apoptose em uma célula, de sensibilização de uma célula à um sinal apoptótico, de inibição da ligação de uma proteìna iap e de tratamento de uma doença e cáncer e usos de um composto
US7674787B2 (en) 2004-07-09 2010-03-09 The Regents Of The University Of Michigan Conformationally constrained Smac mimetics and the uses thereof
EP1773348A4 (en) 2004-07-12 2009-05-20 Idun Pharmaceuticals Inc TETRA PEPTIDE ANALOGS
AU2005274937B2 (en) 2004-07-15 2011-08-18 Medivir Ab IAP binding compounds
MX2007007195A (es) 2004-12-20 2007-10-08 Genentech Inc Inhibidores de pirrolidina de iap.
ES2456671T3 (es) 2005-02-25 2014-04-23 Tetralogic Pharmaceuticals Corporation Inhibidores diméricos de IAP
US20070003535A1 (en) 2005-03-17 2007-01-04 Reed John C Methods and compositions for derepression of IAP-inhibited caspase
DE102005017116A1 (de) 2005-04-13 2006-10-26 Novartis Ag Hemmstoffe für Inhibitoren von Apoptose Proteinen (IAP)
US7772177B2 (en) 2005-05-18 2010-08-10 Aegera Therapeutics, Inc. BIR domain binding compounds
EP1888619B1 (en) 2005-05-25 2013-04-17 2cureX ApS Compounds modifying apoptosis
JP2008545780A (ja) 2005-06-08 2008-12-18 ノバルティス アクチエンゲゼルシャフト 有機化合物
WO2007021825A2 (en) * 2005-08-09 2007-02-22 Tetralogic Pharmaceuticals Corporation Treatment of proliferative disorders
WO2007048224A1 (en) 2005-10-25 2007-05-03 Aegera Therapeutics Inc. Iap bir domain binding compounds
WO2007106192A2 (en) 2005-12-19 2007-09-20 Genentech, Inc. Inhibitors of iap
WO2007075525A2 (en) 2005-12-20 2007-07-05 Novartis Ag Combination of an iap-inhibitor and a taxane7
WO2007101347A1 (en) 2006-03-07 2007-09-13 Aegera Therapeutics Inc. Bir domain binding compounds
TWI504597B (zh) 2006-03-16 2015-10-21 Pharmascience Inc 結合於細胞凋亡抑制蛋白(iap)之桿狀病毒iap重複序列(bir)區域之化合物
BRPI0708942A2 (pt) 2006-03-21 2011-06-14 Joyant Pharmaceuticals Inc composto promotor de apoptose, uso e mÉtodo de produÇço do mesmo e composiÇço farmacÊutica
JP5230610B2 (ja) 2006-05-05 2013-07-10 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン 二価smac模倣物およびその使用
AU2007250443B2 (en) 2006-05-16 2013-06-13 Pharmascience Inc. IAP BIR domain binding compounds
KR20090041391A (ko) 2006-07-24 2009-04-28 테트랄로직 파마슈티칼스 이량체성 iap 길항제
WO2008014229A2 (en) 2006-07-24 2008-01-31 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
US20100056495A1 (en) 2006-07-24 2010-03-04 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
WO2008014238A2 (en) 2006-07-24 2008-01-31 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
CL2007002166A1 (es) 2006-07-24 2008-01-25 Tetralogic Pharm Corp Compuestos derivados de heterociclos de nitrogeno, antagonistas de los inhibidores de las proteinas de la apoptosis; sus composiciones farmaceuticas; y uso de dichos compuestos para el tratamiento del cancer.
WO2008014240A2 (en) 2006-07-24 2008-01-31 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
PE20110220A1 (es) 2006-08-02 2011-04-11 Novartis Ag DERIVADOS DE 2-OXO-ETIL-AMINO-PROPIONAMIDA-PIRROLIDIN-2-IL-SUSTITUIDOS COMO INHIBIDORES DEL ENLACE DE LA PROTEINA Smac AL INHIBIDOR DE LA PROTEINA DE APOPTOSIS
US8044209B2 (en) 2006-10-12 2011-10-25 Novartis Ag Pyrrolydine derivatives as IAP inhibitors
KR20090082221A (ko) 2006-10-19 2009-07-29 노파르티스 아게 유기 화합물
CN101541325A (zh) 2006-11-28 2009-09-23 诺瓦提斯公司 Iap抑制剂用于治疗急性髓性白血病的用途
KR20090087094A (ko) 2006-11-28 2009-08-14 노파르티스 아게 Iap 억제제 및 flt3 억제제의 조합물
ATE542798T1 (de) 2006-12-07 2012-02-15 Novartis Ag Organische verbindungen
US8063218B2 (en) 2006-12-19 2011-11-22 Genentech, Inc. Imidazopyridine inhibitors of IAP
JP5454943B2 (ja) 2007-04-12 2014-03-26 ジョイアント ファーマスーティカルズ、インク. 抗癌剤として有用なsmac模倣二量体及び三量体
WO2008128171A2 (en) 2007-04-13 2008-10-23 The Regents Of The University Of Michigan Diazo bicyclic smac mimetics and the uses thereof
PE20130150A1 (es) 2007-04-30 2013-02-27 Genentech Inc Inhibidores de las iap
WO2008144925A1 (en) 2007-05-30 2008-12-04 Aegera Therapeutics Inc. Iap bir domain binding compounds
EP2058312A1 (en) 2007-11-09 2009-05-13 Universita' degli Studi di Milano SMAC mimetic compounds as apoptosis inducers

Also Published As

Publication number Publication date
CA2581960A1 (en) 2007-09-16
EP2004600A1 (en) 2008-12-24
NZ571577A (en) 2011-09-30
RU2008140935A (ru) 2010-04-27
MX2008011837A (es) 2009-02-10
TW201538520A (zh) 2015-10-16
US20080207525A1 (en) 2008-08-28
US8765681B2 (en) 2014-07-01
US20100221261A1 (en) 2010-09-02
JP2009529544A (ja) 2009-08-20
EP2004600A4 (en) 2012-05-02
KR101446907B1 (ko) 2014-10-06
SG170739A1 (en) 2011-05-30
NO20083868L (no) 2008-11-06
US7645741B2 (en) 2010-01-12
US20130071411A1 (en) 2013-03-21
US7579320B2 (en) 2009-08-25
TWI504597B (zh) 2015-10-21
US20140336134A1 (en) 2014-11-13
PH12014502420A1 (en) 2015-11-16
TWI543988B (zh) 2016-08-01
JP5419468B2 (ja) 2014-02-19
US9365614B2 (en) 2016-06-14
BRPI0709610A2 (pt) 2011-07-19
WO2007104162A1 (en) 2007-09-20
TW200800961A (en) 2008-01-01
CA2581960C (en) 2015-11-24
AU2007224932B2 (en) 2013-05-23
AU2007224932A1 (en) 2007-09-20
KR20080112304A (ko) 2008-12-24
PH12014502420B1 (en) 2017-11-08
US20080069812A1 (en) 2008-03-20

Similar Documents

Publication Publication Date Title
IL193951A (en) A compound with central pyrrolidine units, an intermediate compound for the preparation of the mediated compound, a process for the production of the mediated compound, the use of a mediated compound for the manufacture of a drug, a pharmaceutical preparation, a method for the preparation of a pharmaceutical preparation, and a method for making conventional pharmaceutical salt of a non-salts compound.
IL210577A (en) Compound 1,2,3,4-tetrahydrocyclopenta [b] indole-3-yl acetic acid, salt, hydrate and solvent, pharmaceutical, compound, salt, hydrate, solvent or pharmaceutical for use as a medicine or treatment Salt, hydrate, solvent or pharmaceutical preparation in the manufacture of a drug and process for the preparation
EP2054416B8 (en) Substituted pyrazolopyrimidines, a process for their preparation and their use as medicine
IL206500A0 (en) Process for the preparation of sitagliptin and pharmaceutically acceptable salts thereof
IL250439A0 (en) Use of fingolimod, or a phosphate derivative thereof or a pharmaceutical acceptable salt thereof for the preparation of a drug for the treatment of multiple sclerosis
SI2086945T1 (sl) Novi postopek za pripravo statinov in njihovih farmacevtsko sprejemljivih soli
IL195788A (en) Vegf Antagonist Vascular Endothelial Growth Factor, a method of preparation and an appropriate intravenous injection containing them
ZA201001015B (en) (Carboxylalkylene-phenyl)-phenyl-oxalamides, method for the production thereof, and use of same as a medicament
ZA201001014B (en) (Cyclopropyl-phenyl)-phenyl-oxalamides, method for the production thereof, and use of same as a medicament
PT2364983E (pt) Novo derivado tricíclico ou seus sais farmaceuticamente aceitáveis, seu método de preparação, e composição farmacêutica que o contém
IL188643A (en) Derivatives – n (troaryl) –1 – troarylalkyl – 1h – indole – 2– carboxamide, process for the production of derivatives, drug, pharmaceutical composition and use of derivatives for drug production.
IL176913A0 (en) 7-phenylamino-4-quinolone-3-carboxylic acid derivatives, methods for production and use thereof as medicaments
WO2007144169A3 (en) Entacapone-derivatives
EP2133060A4 (en) METHOD FOR PRODUCING PREPARATION FOR ORAL ADMINISTRATION
WO2008006795A3 (en) Indole compounds
IL188069A0 (en) Process for preparing new tiotropium salts, new tiotropium salts as such and pharmaceutical compositions thereof
WO2010070677A3 (en) A process for the preparation of prasugrel and its pharmaceutically acceptable salts thereof
WO2010012459A3 (en) A process for the preparation of solifenacin salts and their inclusion into pharmaceutical dosage forms
ATE500226T1 (de) Aripiprazolhemifumarat und verfahren zu dessen herstellung
WO2011131370A8 (en) Melt-granulated fingolimod
WO2008117305A3 (en) A novel process for preparing pregabalin and its acid addition salts
WO2008034912A3 (en) Process for the synthesis of clopidogrel and new forms of pharmaceutically acceptable salts thereof
WO2009125975A3 (ko) 미티글리나이드 및 메트포르민 복합제제 및 그의 제조방법
PL2291374T3 (pl) Sposób wytwarzania solifenacyny i/lub jej farmaceutycznie dopuszczalnych soli o wysokiej czystości farmaceutycznej
WO2009080745A3 (de) Perhydrochinoxalin-derivate als analgetika

Legal Events

Date Code Title Description
FF Patent granted
KB Patent renewed
KB Patent renewed
MM9K Patent not in force due to non-payment of renewal fees