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Last Updated: March 28, 2024

Claims for Patent: 9,828,399


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Summary for Patent: 9,828,399
Title:TC-PTP inhibitors as APC activators for immunotherapy
Abstract: The invention encompasses the novel class of compounds represented by the Formula (I) below, which are inhibitors of the TC-PTP enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown above and methods of treating or preventing TC-PTP mediated diseases, including cancer, via their use in the activation of antigen-presenting cells, like dendritic cells, for applications in the immunotherapeutic treatment of diseases. ##STR00001##
Inventor(s): Tremblay; Michel L. (Montreal, CA), Penafuerte; Claudia (Montreal, CA), Feldhammer; Matthew (Montreal, CA), Zogopoulos; George (Montreal, CA), Black; Cameron (Baie d\'Urfe, CA), Kennedy; Brian (Kirkland, CA)
Assignee: The Royal Institution For The Advancement Of Learning/McGill University (Montreal, CA)
Application Number:15/122,031
Patent Claims:1. A compound of structural Formula Ib, or a pharmaceutically acceptable salts thereof, and stereoisomers thereof: ##STR00031## wherein: R.sup.1 is selected from the group consisting of (a) C.sub.1-3 alkyl optionally substituted with 1-5 halogens and optionally with one group selected from --OH, --OC.sub.1-3 alkyl optionally substituted with 1-3 halogens, and --CN; (b) --(C.dbd.O)R.sup.4; (c) --CN; (d) --(C.dbd.O)OR.sup.4; (e) --(C.dbd.O)NHR.sup.4; and (f) --(C.dbd.O)NR.sup.5R.sup.6; R.sup.4 is selected from the group consisting of (a) H; and (b) C.sub.1-3 alkyl optionally substituted with 1-5 halogens and; R.sup.5 and R.sup.6 are independently selected from the group consisting of C.sub.1-3 alkyl optionally substituted with 1-5 halogens and optionally with one group selected from --OH, and --OC.sub.1-3 alkyl optionally substituted with 1-3 halogens.

2. The compound of Formula Ib as defined in claim 1, or a pharmaceutically acceptable salt thereof, selected from the following compounds: ##STR00032##

3. A pharmaceutical composition comprising a compound of claim 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

4. A pharmaceutical composition according to claim 3, further comprising one or more additional compounds selected from the group consisting of: (a) a cytotoxic agent; (b) an antimetabolite; (c) an alkylating agent; (d) an anthracycline; (e) an antibiotic; (f) an anti-mitotic agent; (g) an hormone therapy; (h) a signal transduction inhibitor; (i) a gene expression modulator; (j) an apoptosis inducer; (k) an angiogenesis inhibitor; and (l) an immunotherapy agent.

5. The pharmaceutical composition of claim 4, wherein said cytotoxic agent is taxol, cytochalasin B, gramicidin D, ethidium bromide, emetine, mitomycin, etoposide, tenoposide, vincristine, vinblastine, colchicin, doxorubicin, daunorubicin, dihydroxy anthracin dione, mitoxantrone, mithramycin, actinomycin D, 1-dehydrotestosterone, glucocorticoids, procaine, tetracaine, lidocaine, propranolol, puromycin, analogs or homologs thereof, or a combination thereof; wherein said antimetabolites is methotrexate, 6-mercaptopurine, 6-thioguanine, cytarabine, 5-fluorouracil decarbazine, or a combination thereof; wherein said alkylating agent is mechlorethamine, thioepa chlorambucil, melphalan, carmustine (BSNU), lomustine (CCNU), cyclothosphamide, busulfan, dibromomannitol, streptozotocin, mitomycin C, cis-dichlorodiamine platinum (II) (DDP) cisplatin, or a combination thereof; wherein said anthracycline is daunorubicin, doxorubicin, or a combination thereof; wherein said antibiotic is dactinomycin, bleomycin, mithramycin, anthramycin (AMC), or a combination thereof; wherein said anti-mitotic agent is vincristine, vinblastine, or a combination thereof; wherein said signal transduction inhibitor is imatinib, trastuzumab, or a combination thereof; wherein said gene expression modulator is a siRNA, a shRNA, an antisense oligonucleotide, an HDAC inhibitor, or a combination thereof; wherein said immunotherapy agent is a monoclonal antibody, a chimeric antigen receptors (CARs) -T-Cell, or a combination thereof; wherein said hormone therapy is an luteinizing hormone-releasing hormone (LHRH) antagonist; wherein said apoptosis inducers is a recombinant human TNF-related apoptosis-inducing ligand (TRAIL); wherein said angiogenesis inhibitors is sorafenib, sunitinib, pazopanib, everolimus or a combination thereof.

6. The pharmaceutical composition of claim 5, wherein said monoclonal antibody is anti-CTLA4, anti-PD1 or a combination thereof.

Details for Patent 9,828,399

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 09/25/1998 ⤷  Try a Trial 2034-02-28
Genentech, Inc. HERCEPTIN trastuzumab For Injection 103792 02/10/2017 ⤷  Try a Trial 2034-02-28
Genentech, Inc. HERCEPTIN HYLECTA trastuzumab and hyaluronidase-oysk Injection 761106 02/28/2019 ⤷  Try a Trial 2034-02-28
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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