(12) Patent Application Publication (10) Pub. No.: US 2010/0331307 A1 Salituro Et Al

Total Page:16

File Type:pdf, Size:1020Kb

(12) Patent Application Publication (10) Pub. No.: US 2010/0331307 A1 Salituro Et Al US 2010O3.31307A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2010/0331307 A1 Salituro et al. (43) Pub. Date: Dec. 30, 2010 (54) THERAPEUTIC COMPOUNDS AND Publication Classification COMPOSITIONS (51) Int. Cl. (76) Inventors: Francesco G. Salituro, A 6LX 3/553 (2006.01) Marlborough, MA (US); Jeffrey O. A6IP35/00 (2006.01) Saunders, Concord, MA (US); A 6LX 3L/2197 (2006.01) Shunqi Yan, Irvine, CA (US) C07D 40/12 (2006.01) C07D 417/4 (2006.01) Correspondence Address: C07D 405/4 (2006.01) LANDO & ANASTASI, LLP C07D 40/4 (2006.01) ONE MAINSTREET, SUITE 1100 CAMBRIDGE, MA 02142 (US) (52) U.S. Cl. ............... 514/210.21; 514/218: 514/253.06; (21) Appl. No.: 12/826,630 540/575:544/363 Filed: Jun. 29, 2010 (22) (57) ABSTRACT Related U.S. Application Data Compounds and compositions comprising compounds that (60) Provisional application No. 61/221,430, filed on Jun. modulate pyruvate kinase M2 (PKM2) are described herein. 29, 2009, provisional application No. 61/292,360, Also described herein are methods of using the compounds filed on Jan. 5, 2010. that modulate PKM2 in the treatment of cancer. Patent Application Publication Dec. 30, 2010 Sheet 1 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 2 of 70 US 2010/0331307 A1 Figure 1 Compound ACso MeO a. N ) C CSS B O F N S CC F C O MeO Ol s 9 OMe N C C5.S. B O C a OMe N^ S N O B O Cl OWe O s 9 OEt N CO S B O C OMe N1 RéaS -4. O A N 3. O O al av N 6S O C O OMe s N^N O OS C F O st C.C.N O or C O C 2N Sa l 9 OMe N OCN Of C O Patent Application Publication Dec. 30, 2010 Sheet 3 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 4 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 5 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 6 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 7 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 8 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 9 of 70 US 2010/0331307 A1 Figure 1 Compound ACso N H A O O Ns O N H A O O NS O S N H O O NS 4J, N H G.O.5.O O NS B O &ON N H s A O oo O N NO H s A O Oo O s^ N H CO-O-O Ns A O O -S NO Hs A Or Ns O O v'ry at S. B Q--O;O Sa R A Patent Application Publication Dec. 30, 2010 Sheet 10 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 11 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 12 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 13 of 70 US 2010/0331307 A1 Figure 1 Compound ACso O O J. N Oriol,O O Ns A C O f N H Q-O,O Ns B N O 21 S.N C N s: A O N 4 O CF N N s N N A O N 4 O 2 F aN ! C N s: A O N 4 C O Patent Application Publication Dec. 30, 2010 Sheet 14 of 70 US 2010/0331307 A1 Figure 1 Compound ACso F O N C N s: E O N 2 O 2N N N-N-N- OS2O A CF. O N N4 O N 1NCluj N s A O N N4 O N e YN Os O F N Nu N S. A O N 4 O e SaOl-C N s: A F O N 4 O 2 SaO-C N s A C O N 4 O 2 N Osao NS N- A OCHO N 4 OCH O e SaOl-C N s. A O N 4 Patent Application Publication Dec. 30, 2010 Sheet 15 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 16 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 17 of 70 US 2010/0331307 A1 Figure 1 Compound ACso O N O. O O-os-O SS D O N 4 O os-N “C,OS2O B 4 O N Osao o'- B C O N 4 O N O O os-N- SS Oor? HN D 4 O N OS2O O N orror 4 C O 2 N Osao SN Nu NCS B O H N a O e 1N O. O. Sa N- ‘s. C O H N 4 O N?Sa N-1N “C. OS 2O D O H N 4 Patent Application Publication Dec. 30, 2010 Sheet 18 of 70 US 2010/0331307 A1 Figure 1 Compound ACso O 1N OO SCO F HNS C 2 Patent Application Publication Dec. 30, 2010 Sheet 19 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 20 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Q OCH3 F3C na 1N Os O SN Nu N'S B H 2 O OCH3 2N N 1s Nu NOsao B O N 4 O OCH3 N? N Sa Nu- B C O N 2 O OCH3 N2 N Sa Nu- Cls, O B F O N 4 O OCH3 N e Yn Os O C Sa N- N S A O N 4 O OCH 2N N Osao Sa N- B CF. O N a O OCH 2N N OS2O Sa N- B O N 4 O OCH C 2 N Osao SN N- B O N 2 Patent Application Publication Dec. 30, 2010 Sheet 21 of 70 US 2010/0331307 A1 Figure 1 Compound ACso O OCH3 N O. O. SaN N N S B O N 4 Patent Application Publication Dec. 30, 2010 Sheet 22 of 70 US 2010/0331307 A1 Figure 1 Compound ACso O OCH F N F N B O N 4 Patent Application Publication Dec. 30, 2010 Sheet 23 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 24 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 25 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 26 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 27 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 28 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 29 of 70 US 2010/0331307 A1 Figure 1 Compound ACso H Yo N O --O- R O CC o? So NS B O N SS Cl CC O Nsa A O O JCl N SS B -S N-N O O NS O F CC.". A O 1Ol i 'O. oo Ns A O FC 1Cl 'O oo Ns B O N SS OlOCF3 C.C. o Ns. A O H Y N OC co Ns- B O H *C. N 'O.C.". NS B O Patent Application Publication Dec. 30, 2010 Sheet 30 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 31 of 70 US 2010/0331307 A1 Figure 1 Compound ACso H N OC ...) A Patent Application Publication Dec. 30, 2010 Sheet 32 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 33 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 34 of 70 US 2010/0331307 A1 Figure 1 Compound ACso O 1n 1 O n O Patent Application Publication Dec. 30, 2010 Sheet 35 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Patent Application Publication Dec. 30, 2010 Sheet 36 of 70 US 2010/0331307 A1 Figure 1 Compound ACso N^ Yo CC N Ois NS B O CCON ~ d’oSS is B -O O H N1 N A C N-N NS F O CCC.C CC C., O O NS B O F CCCC'sN SC A O N ~ SS COC do N. B (b. O N ~ s S-C CC of O NS B -O O N w CrOC o Ns- A F O N SC COCO or B N SC O H S.o A N s FuO O Sr N S. Patent Application Publication Dec. 30, 2010 Sheet 37 of 70 US 2010/0331307 A1 Figure 1 Compound ACso Ns O N A O No H N1 N S A N-N of O N. O C H N1 N1 N Nss 2 co N A O C N S2 ON O NS A O C H N1 Ns A N-N do Ns.
Recommended publications
  • AHFS Pharmacologic-Therapeutic Classification System
    AHFS Pharmacologic-Therapeutic Classification System Abacavir 48:24 - Mucolytic Agents - 382638 8:18.08.20 - HIV Nucleoside and Nucleotide Reverse Acitretin 84:92 - Skin and Mucous Membrane Agents, Abaloparatide 68:24.08 - Parathyroid Agents - 317036 Aclidinium Abatacept 12:08.08 - Antimuscarinics/Antispasmodics - 313022 92:36 - Disease-modifying Antirheumatic Drugs - Acrivastine 92:20 - Immunomodulatory Agents - 306003 4:08 - Second Generation Antihistamines - 394040 Abciximab 48:04.08 - Second Generation Antihistamines - 394040 20:12.18 - Platelet-aggregation Inhibitors - 395014 Acyclovir Abemaciclib 8:18.32 - Nucleosides and Nucleotides - 381045 10:00 - Antineoplastic Agents - 317058 84:04.06 - Antivirals - 381036 Abiraterone Adalimumab; -adaz 10:00 - Antineoplastic Agents - 311027 92:36 - Disease-modifying Antirheumatic Drugs - AbobotulinumtoxinA 56:92 - GI Drugs, Miscellaneous - 302046 92:20 - Immunomodulatory Agents - 302046 92:92 - Other Miscellaneous Therapeutic Agents - 12:20.92 - Skeletal Muscle Relaxants, Miscellaneous - Adapalene 84:92 - Skin and Mucous Membrane Agents, Acalabrutinib 10:00 - Antineoplastic Agents - 317059 Adefovir Acamprosate 8:18.32 - Nucleosides and Nucleotides - 302036 28:92 - Central Nervous System Agents, Adenosine 24:04.04.24 - Class IV Antiarrhythmics - 304010 Acarbose Adenovirus Vaccine Live Oral 68:20.02 - alpha-Glucosidase Inhibitors - 396015 80:12 - Vaccines - 315016 Acebutolol Ado-Trastuzumab 24:24 - beta-Adrenergic Blocking Agents - 387003 10:00 - Antineoplastic Agents - 313041 12:16.08.08 - Selective
    [Show full text]
  • Solid Forms of Ortataxel Feste Formen Von Ortataxel Formes Solides D’Ortataxel
    (19) & (11) EP 2 080 764 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: C07D 493/04 (2006.01) A61K 31/357 (2006.01) 22.08.2012 Bulletin 2012/34 A61P 35/00 (2006.01) (21) Application number: 08000904.6 (22) Date of filing: 18.01.2008 (54) Solid forms of ortataxel Feste Formen von Ortataxel Formes solides d’ortataxel (84) Designated Contracting States: (74) Representative: Minoja, Fabrizio AT BE BG CH CY CZ DE DK EE ES FI FR GB GR Bianchetti Bracco Minoja S.r.l. HR HU IE IS IT LI LT LU LV MC MT NL NO PL PT Via Plinio, 63 RO SE SI SK TR 20129 Milano (IT) Designated Extension States: AL BA MK RS (56) References cited: WO-A-01/02407 WO-A-02/44161 (43) Date of publication of application: WO-A-2007/078050 US-A1- 2007 212 394 22.07.2009 Bulletin 2009/30 US-B1- 7 232 916 (73) Proprietor: INDENA S.p.A. • HENNENFENT K L ET AL: "NOVEL 20139 Milano (IT) FORMULATIONS OF TAXANES: A REVIEW. OLD WINE IN A NEW BOTTLE?" ANNALS OF (72) Inventors: ONCOLOGY,KLUWER, DORDRECHT, NL, vol. 17, • Ciceri, Daniele no. 5, 2006, pages 735-749, XP008065745 ISSN: 20139 Milano (IT) 0923-7534 • Sardone, Nicola • NICOLETTI MARIA INES ET AL: "IDN5109, a 20139 Milano (IT) taxane with oral bioavailability and potent • Gabetta, Bruno antitumor activity" CANCER RESEARCH, vol. 60, 20139 Milano (IT) no. 4, 15 February 2000 (2000-02-15), pages • Ricotti, Maurizio 842-846, XP002478136 ISSN: 0008-5472 20139 Milano (IT) Note: Within nine months of the publication of the mention of the grant of the European patent in the European Patent Bulletin, any person may give notice to the European Patent Office of opposition to that patent, in accordance with the Implementing Regulations.
    [Show full text]
  • Photodynamic Therapy with Methyl Aminolevulinate for Primary Nodular Basal Cell Carcinoma: Results of Two Randomized Studies
    Clinical trial Photodynamic therapy with methyl aminolevulinate for primary nodular basal cell carcinoma: results of two randomized studies Peter Foley, MBBS, BMedSc, MD, FACD, Michael Freeman, MBBS, FACD, Alan Menter, MB, FAAD, Gregory Siller, MBBS, FACD, Rokea A. El-Azhary, MD, PhD, FAAD, Kurt Gebauer, MBBS, FACD, Nicholas J. Lowe, MD, FAAD, Michael T. Jarratt, MD, FAAD, Dedee F. Murrell, BMBCh, MD, FAAD, Phoebe Rich, MD, FAAD, David M. Pariser, MD, FAAD, Allan R. Oseroff, MD, PhD, FAAD, Ross Barnetson, MD, FRACP, FACD, Christopher Anderson, MBBS, FACD, Steven Kossard, MBBS, FACD, Lawrence E. Gibson, MD, FAAD, and Whitney D. Tope, MPhIL, MD, FAAD From the Department of Medicine Abstract (Dermatology), The University of Background Data suggest that photodynamic therapy using topical methyl aminolevulinate Melbourne, St. Vincent’s Hospital (MAL PDT) may be a noninvasive alternative to excisional surgery for nodular basal cell Melbourne, Fitzroy, Vic., Suite 5 ACH carcinoma (BCC). In the studies described here, we investigated the histologic response, House, Benowa and Department of Dermatology, Princess Alexandra tolerability, and cosmetic outcome with MAL PDT for primary nodular BCC (£ 5 mm in depth). Hospital, Woolloongabba, Qld, Fremantle Methods Two multicenter, randomized, double-blind studies with similar design and Dermatology, Fremantle, WA, and procedures were conducted. After surface debridement and minor tumor debulking, MAL cream Department of Dermatology, St. George 160 mg/g (66 patients with 75 lesions) or placebo cream (65 patients with 75 lesions) was applied Hospital, University of New South Wales, for 3 h, followed by illumination with broad-spectrum red light (75 J/cm2, 570–670 nm).
    [Show full text]
  • SPECTRUM PHARMACEUTICALS, INC. (Exact Name of Registrant As Specified in Its Charter)
    Table of Contents UNITED STATES SECURITIES AND EXCHANGE COMMISSION Washington, D.C. 20549 FORM 8-K CURRENT REPORT PURSUANT TO SECTION 13 OR 15(D) OF THE SECURITIES AND EXCHANGE ACT OF 1934 Date of Report: July 20, 2007 SPECTRUM PHARMACEUTICALS, INC. (Exact name of registrant as specified in its charter) Delaware 000-28782 93-0979187 (State or other Jurisdiction (Commission File Number) (IRS Employer of Incorporation) Identification Number) 157 Technology Drive Irvine, California 92618 (Address of principal (Zip Code) executive offices) (949) 788-6700 (Registrant’s telephone number, including area code) N/A (Former Name or Former Address, if Changed Since Last Report) Check the appropriate box below if the Form 8-K filing is intended to simultaneously satisfy the filing obligation of the registrant under any of the following provisions: o Written communications pursuant to Rule 425 under the Securities Act (17 CFR 230.425) o Soliciting material pursuant to Rule 14a-12 under the Exchange Act (17 CFR 240.14a-12) o Pre-commencement communications pursuant to Rule 14d-2(b) under the Exchange Act (17 CFR 240.14d-2(b)) o Pre-commencement communications pursuant to Rule 13e-4(c) under the Exchange Act (17 CFR 240.13e-4(c)) TABLE OF CONTENTS Item 1.01 Entry Into Material Definitive Agreement. Item 8.01 Other Events. Item 9.01 Financial Statements and Exhibits. SIGNATURES EXHIBIT INDEX EXHIBIT 99.1 EXHIBIT 99.2 Table of Contents Item 1.01 Entry Into Material Definitive Agreement. On July 20, 2007, Spectrum Pharmaceuticals, Inc. (the “Company”) entered into a world-wide license agreement (the “License Agreement”) with Indena S.p.A., a Italian company (“Indena”), for ortataxel, a third-generation taxane classified as a new chemical entity that has demonstrated clinical activity in taxane-refractory tumors, effective as of July 17, 2007.
    [Show full text]
  • Multicenter, Single Arm, Phase II Trial on the Efficacy of Ortataxel in Recurrent Glioblastoma (2019) Journal of Neuro-Oncology, 142 (3), Pp
    Documents Export Date: 21 Jan 2020 Search: AU-ID("Gaviani, Paola" 6506528764) 1) Silvani, A., De Simone, I., Fregoni, V., Biagioli, E., Marchioni, E., Caroli, M., Salmaggi, A., Pace, A., Torri, V., Gaviani, P., Quaquarini, E., Simonetti, G., Rulli, E., D’Incalci, M., Poli, D., Mariotti, E., Caramia, G., Gritti, A.P., Pacchetti, I., Zucchetti, M., Lanza, A., Basso, G., Bini, P., Berzero, G., Diamanti, L., Di Cristofori, A., Manzoni, A., Lanfranchi, G., Ardizzoia, A., Villani, V. Multicenter, single arm, phase II trial on the efficacy of ortataxel in recurrent glioblastoma (2019) Journal of Neuro-Oncology, 142 (3), pp. 455-462. 1) https://www.scopus.com/inward/record.uri?eid=2-s2.0-85061248819&doi=10.1007%2fs11060-019-03116-z&partnerID=40&md5=55ca05a12a766ded77ba791fd16b7b7c DOI: 10.1007/s11060-019-03116-z Document Type: Article Publication Stage: Final Source: Scopus 2) Simonetti, G., Sommariva, A., Lusignani, M., Anghileri, E., Ricci, C.B., Eoli, M., Fittipaldo, A.V., Gaviani, P., Moreschi, C., Togni, S., Tramacere, I., Silvani, A. Prospective observational study on the complications and tolerability of a peripherally inserted central catheter (PICC) in neuro-oncological patients (2019) Supportive Care in Cancer, . 2) https://www.scopus.com/inward/record.uri?eid=2-s2.0-85075206792&doi=10.1007%2fs00520-019-05128-x&partnerID=40&md5=5550a094872f579fb7bf84be2a261c33 DOI: 10.1007/s00520-019-05128-x Document Type: Article Publication Stage: Article in Press Source: Scopus 3) Simonetti, G., Terreni, M.R., DiMeco, F., Fariselli, L., Gaviani, P. Letter to the editor: lung metastasis in WHO grade I meningioma (2018) Neurological Sciences, 39 (10), pp.
    [Show full text]
  • Tanibirumab (CUI C3490677) Add to Cart
    5/17/2018 NCI Metathesaurus Contains Exact Match Begins With Name Code Property Relationship Source ALL Advanced Search NCIm Version: 201706 Version 2.8 (using LexEVS 6.5) Home | NCIt Hierarchy | Sources | Help Suggest changes to this concept Tanibirumab (CUI C3490677) Add to Cart Table of Contents Terms & Properties Synonym Details Relationships By Source Terms & Properties Concept Unique Identifier (CUI): C3490677 NCI Thesaurus Code: C102877 (see NCI Thesaurus info) Semantic Type: Immunologic Factor Semantic Type: Amino Acid, Peptide, or Protein Semantic Type: Pharmacologic Substance NCIt Definition: A fully human monoclonal antibody targeting the vascular endothelial growth factor receptor 2 (VEGFR2), with potential antiangiogenic activity. Upon administration, tanibirumab specifically binds to VEGFR2, thereby preventing the binding of its ligand VEGF. This may result in the inhibition of tumor angiogenesis and a decrease in tumor nutrient supply. VEGFR2 is a pro-angiogenic growth factor receptor tyrosine kinase expressed by endothelial cells, while VEGF is overexpressed in many tumors and is correlated to tumor progression. PDQ Definition: A fully human monoclonal antibody targeting the vascular endothelial growth factor receptor 2 (VEGFR2), with potential antiangiogenic activity. Upon administration, tanibirumab specifically binds to VEGFR2, thereby preventing the binding of its ligand VEGF. This may result in the inhibition of tumor angiogenesis and a decrease in tumor nutrient supply. VEGFR2 is a pro-angiogenic growth factor receptor
    [Show full text]
  • BC Cancer Benefit Drug List September 2021
    Page 1 of 65 BC Cancer Benefit Drug List September 2021 DEFINITIONS Class I Reimbursed for active cancer or approved treatment or approved indication only. Reimbursed for approved indications only. Completion of the BC Cancer Compassionate Access Program Application (formerly Undesignated Indication Form) is necessary to Restricted Funding (R) provide the appropriate clinical information for each patient. NOTES 1. BC Cancer will reimburse, to the Communities Oncology Network hospital pharmacy, the actual acquisition cost of a Benefit Drug, up to the maximum price as determined by BC Cancer, based on the current brand and contract price. Please contact the OSCAR Hotline at 1-888-355-0355 if more information is required. 2. Not Otherwise Specified (NOS) code only applicable to Class I drugs where indicated. 3. Intrahepatic use of chemotherapy drugs is not reimbursable unless specified. 4. For queries regarding other indications not specified, please contact the BC Cancer Compassionate Access Program Office at 604.877.6000 x 6277 or [email protected] DOSAGE TUMOUR PROTOCOL DRUG APPROVED INDICATIONS CLASS NOTES FORM SITE CODES Therapy for Metastatic Castration-Sensitive Prostate Cancer using abiraterone tablet Genitourinary UGUMCSPABI* R Abiraterone and Prednisone Palliative Therapy for Metastatic Castration Resistant Prostate Cancer abiraterone tablet Genitourinary UGUPABI R Using Abiraterone and prednisone acitretin capsule Lymphoma reversal of early dysplastic and neoplastic stem changes LYNOS I first-line treatment of epidermal
    [Show full text]
  • (12) United States Patent (10) Patent No.: US 8,580,267 B2 Pedretti Et Al
    US008580267B2 (12) United States Patent (10) Patent No.: US 8,580,267 B2 Pedretti et al. (45) Date of Patent: Nov. 12, 2013 (54) IMMUNOCYTOKINES FORTUMOUR (56) References Cited THERAPY WITH CHEMOTHERAPEUTIC AGENTS FOREIGN PATENT DOCUMENTS (75) Inventors: Marta Pedretti, Zurich (CH): Dario WO O2/O59264 8, 2002 WO O3,O93478 11, 2003 Neri, Buchs (CH) WO 2004/OO2528 1, 2004 WO 2006/026020 3, 2006 (73) Assignee: Philogen S.p.A., Siena (IT) WO 2006/050834 5, 2006 WO 2007/128563 11, 2007 (*) Notice: Subject to any disclaimer, the term of this OTHER PUBLICATIONS patent is extended or adjusted under 35 U.S.C. 154(b) by 0 days. Paul, William, Fundamental Immunology, 3rd Edition, Raven Press, New York, 1993, pp. 292-295.* (21) Appl. No.: 13/139,655 Vajdos et al., Comprehensive functional maps of the antigen-binding site of an anti-ErbB2 antibody obtained with shotgun scanning 1-1. mutagenesis. J. Mol. Biol. 320:415-428, 2002.* (22) PCT Filed: Dec. 14, 2009 Bartolomei, M., et al. “Combined treatment of glioblastomapatients with locoregional pre-targeted 90Y-biotin radioimmunotherapy and (86). PCT No.: PCT/EP2009/008920 temozolomide.” QJNuclMed Mol Imaging. Sep. 2004:48(3):220-8. S371 (c)(1) Marlind, J., et al. "Antibody-mediated delivery of interleukin-2 to the (2), (4) Date. Jun. 14, 2011 Stroma of breast cancer strongly enhances the potency of chemo s 9 therapy” Clin Cancer Res. Oct. 15, 2008;14(20):6515-24. Brack, S.S., et al. “Tumor-targeting properties of novel antibodies (87) PCT Pub. No.: WO2010/078916 specific to the large isoform oftenascin-C.” Clin Cancer Res.
    [Show full text]
  • NIH Public Access Author Manuscript CA Cancer J Clin
    NIH Public Access Author Manuscript CA Cancer J Clin. Author manuscript; available in PMC 2012 July 1. NIH-PA Author ManuscriptPublished NIH-PA Author Manuscript in final edited NIH-PA Author Manuscript form as: CA Cancer J Clin. 2011 ; 61(4): 250±281. doi:10.3322/caac.20114. PHOTODYNAMIC THERAPY OF CANCER: AN UPDATE Patrizia Agostinis1, Kristian Berg2, Keith A. Cengel3, Thomas H. Foster4, Albert W. Girotti5, Sandra O. Gollnick6, Stephen M. Hahn3, Michael R. Hamblin7,8,9, Asta Juzeniene2, David Kessel10, Mladen Korbelik11, Johan Moan2,12, Pawel Mroz7,8, Dominika Nowis13, Jacques Piette14, Brian C. Wilson15, and Jakub Golab13,16,* 1Department of Molecular Cell Biology, Cell Death Research & Therapy Laboratory, Catholic University of Leuven, B-3000 Leuven, Belgium, [email protected] 2Department of Radiation Biology, Institute for Cancer Research, The Norwegian Radium Hospital, Oslo University Hospital, Montebello, N-0310 Oslo, Norway, [email protected]; [email protected] 3Department of Radiation Oncology, University of Pennsylvania, Philadelphia, PA 19004, USA, [email protected]; [email protected] 4Department of Imaging Sciences, University of Rochester, Rochester, NY 14642, USA, [email protected] 5Department of Biochemistry, Medical College of Wisconsin, Milwaukee, WI, 53226-3548, USA, [email protected] 6Department of Cell Stress Biology, Roswell Park Cancer Institute, Elm and Carlton Sts, Buffalo, NY, 14263, USA, [email protected] 7Wellman Center for Photomedicine,
    [Show full text]
  • WO 2015/042414 Al 26 March 2015 (26.03.2015) P O P C T
    (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2015/042414 Al 26 March 2015 (26.03.2015) P O P C T (51) International Patent Classification: (74) Agents: ABELLEIRA, Susan, M. et al; Hamilton, Brook, C07D 401/14 (2006.01) C07D 417/12 (2006.01) Smith & Reynolds, P.C., 530 Virginia Rd, P.O. Box 9133, C07D 213/73 (2006.01) C07D 419/12 (2006.01) Concord, MA 01742-9133 (US). C07D 401/12 (2006.01) A61K 31/433 (2006.01) (81) Designated States (unless otherwise indicated, for every C07D 413/12 (2006.01) A61P 35/00 (2006.01) kind of national protection available): AE, AG, AL, AM, (21) International Application Number: AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, PCT/US2014/056580 BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (22) International Filing Date: HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, 19 September 2014 (19.09.2014) KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, (25) Filing Language: English MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, (26) Publication Language: English SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, (30) Priority Data: TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
    [Show full text]
  • Ep 2569287 B1
    (19) TZZ _T (11) EP 2 569 287 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: C07D 413/04 (2006.01) C07D 239/46 (2006.01) 09.07.2014 Bulletin 2014/28 (86) International application number: (21) Application number: 11731562.2 PCT/US2011/036245 (22) Date of filing: 12.05.2011 (87) International publication number: WO 2011/143425 (17.11.2011 Gazette 2011/46) (54) COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE VERBINDUNGEN ALS HEMMER DER ATR-KINASE COMPOSÉS UTILISABLES EN TANT QU’INHIBITEURS DE LA KINASE ATR (84) Designated Contracting States: • VIRANI, Aniza, Nizarali AL AT BE BG CH CY CZ DE DK EE ES FI FR GB Abingdon GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO Oxfordshire OX144RY (GB) PL PT RO RS SE SI SK SM TR • REAPER, Philip, Michael Abingdon (30) Priority: 12.05.2010 US 333869 P Oxfordshire OX144RY (GB) (43) Date of publication of application: (74) Representative: Coles, Andrea Birgit et al 20.03.2013 Bulletin 2013/12 Kilburn & Strode LLP 20 Red Lion Street (73) Proprietor: Vertex Pharmaceuticals Inc. London WC1R 4PJ (GB) Boston, MA 02210 (US) (56) References cited: (72) Inventors: WO-A1-2010/054398 WO-A1-2010/071837 • CHARRIER, Jean-Damien Abingdon • C. A. HALL-JACKSON: "ATR is a caffeine- Oxfordshire OX144RY (GB) sensitive, DNA-activated protein kinase with a • DURRANT, Steven, John substrate specificity distinct from DNA-PK", Abingdon ONCOGENE, vol. 18, 1999, pages 6707-6713, Oxfordshire OX144RY (GB) XP002665425, cited in the application • KNEGTEL, Ronald, Marcellus Alphonsus Abingdon Oxfordshire OX144RY (GB) Note: Within nine months of the publication of the mention of the grant of the European patent in the European Patent Bulletin, any person may give notice to the European Patent Office of opposition to that patent, in accordance with the Implementing Regulations.
    [Show full text]
  • Modifications to the Harmonized Tariff Schedule of the United States To
    U.S. International Trade Commission COMMISSIONERS Shara L. Aranoff, Chairman Daniel R. Pearson, Vice Chairman Deanna Tanner Okun Charlotte R. Lane Irving A. Williamson Dean A. Pinkert Address all communications to Secretary to the Commission United States International Trade Commission Washington, DC 20436 U.S. International Trade Commission Washington, DC 20436 www.usitc.gov Modifications to the Harmonized Tariff Schedule of the United States to Implement the Dominican Republic- Central America-United States Free Trade Agreement With Respect to Costa Rica Publication 4038 December 2008 (This page is intentionally blank) Pursuant to the letter of request from the United States Trade Representative of December 18, 2008, set forth in the Appendix hereto, and pursuant to section 1207(a) of the Omnibus Trade and Competitiveness Act, the Commission is publishing the following modifications to the Harmonized Tariff Schedule of the United States (HTS) to implement the Dominican Republic- Central America-United States Free Trade Agreement, as approved in the Dominican Republic-Central America- United States Free Trade Agreement Implementation Act, with respect to Costa Rica. (This page is intentionally blank) Annex I Effective with respect to goods that are entered, or withdrawn from warehouse for consumption, on or after January 1, 2009, the Harmonized Tariff Schedule of the United States (HTS) is modified as provided herein, with bracketed matter included to assist in the understanding of proclaimed modifications. The following supersedes matter now in the HTS. (1). General note 4 is modified as follows: (a). by deleting from subdivision (a) the following country from the enumeration of independent beneficiary developing countries: Costa Rica (b).
    [Show full text]