Claims for Patent: 9,278,925

Summary for Patent: 9,278,925

Title:	Substituted 3-(biphenyl-3-yl)-4-hydroxy-8-methoxy-1-azaspiro[4.5]dec-3-en-2-one
Abstract:	The invention relates to substituted 3-(biphenyl-3-yl)-4-hydroxy-8-methoxy-1-azaspiro[4.5]dec-3-en-2-ones, in particular for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of neoplastic disorders.
Inventor(s):	Liu; Ningshu (Berlin, DE), Thede; Kai (Berlin, DE), Monning; Ursula (Woltersdorf, DE), Scholz; Arne (Berlin, DE), Hilger; Christoph-Stephan (Berlin, DE), Bomer; Ulf (Glienicke, DE), Fischer; Reiner (Moheim, DE)
Assignee:	BAYER INTELLECTUAL PROPERTY GMBH (Monheim, DE)
Application Number:	14/236,279
Patent Claims:	1. A compound of formula (I) ##STR00085## in which R.sup.1 represents a trifluoromethyl or methoxymethyl group and R.sup.2 represents hydrogen or fluorine, or a salt thereof. 2. A compound selected from (5r,8r)-3-(4'-chloro-3'-fluoro-4-methylbiphenyl-3-yl)-4-hydroxy-8-methoxy- -8-(methoxymethyl)-1-azaspiro[4.5]dec-3-en-2-one; (5r,8r)-3-(4'-chloro-4-methylbiphenyl-3-yl)-4-hydroxy-8-methoxy-8-(methox- ymethyl)-1-azaspiro[4.5]dec-3-en-2-one; (5r,8r)-3-(4'-chloro-3'-fluoro-4-methylbiphenyl-3-yl)-4-hydroxy-8-methoxy- -8-(trifluoromethyl)-1-azaspiro[4.5]dec-3-en-2-one; and (5r,8r)-3-(4'-chloro-4-methylbiphenyl-3-yl)-4-hydroxy-8-methoxy-8-(triflu- oromethyl)-1-azaspiro[4.5]dec-3-en-2-one. 3. A pharmaceutical formulation comprising a compound according to claim 1 in combination with a further active compound, wherein the further active compound includes at least one of afinitor, aldesleukin, alendronic acid, alfaferone, alitretinoin, allopurinol, aloprim, aloxi, altretamine, aminoglutethimide, amifostine, amrubicin, amsacrine, anastrozole, anzmet, aranesp, arglabin, arsenic trioxide, aromasin, 5-azacytidine, azathioprine, BCG or tice-BCG, bestatin, betamethasone acetate, betamethasone sodium phosphate, bexarotene, bleomycin sulphate, broxuridine, bortezomib, busulfan, calcitonin, campath, capecitabine, carboplatin, casodex, cefesone, celmoleukin, cerubidin, chlorambucil, cisplatin, cladribin, clodronic acid, cyclophosphamide, cytarabine, dacarbazine, dactinomycin, daunoxome, decadron, decadron phosphate, delestrogen, denileukin diftitox, depomedrol, deslorelin, dexrazoxane, diethylstilbestrol, diflucan, docetaxel, doxifluridine, doxorubicin, dronabinol, DW-166HC, eligard, elitek, ellence, emend, epirubicin, epoetin-alfa, epogen, eptaplatin, ergamisol, estrace, estradiol, estramustine sodium phosphate, ethinylestradiol, ethyol, etidronic acid, etopophos, etoposide, fadrozole, farstone, filgrastim, finasteride, fligrastim, floxuridine, fluconazole, fludarabin, 5-fluorodeoxyuridine monophosphate, 5-fluorouracil (5-FU), fluoxymesterone, flutamide, formestane, fosteabine, fotemustine, fulvestrant, gammagard, gemcitabine, gemtuzumab, gleevec, gliadel, goserelin, granisetron hydrochloride, histrelin, hycamtin, hydrocortone, erythro-hydroxynonyladenine, hydroxyurea, ibritumomab tiuxetan, idarubicin, ifosfamide, interferon-alpha, interferon-alpha-2, interferon-alpha-2.alpha., interferon-alpha-2.beta., interferon-alpha-n1, interferon-alpha-n3, interferon-beta, interferon-gamma-1.alpha., interleukin-2, intron A, iressa, irinotecan, kytril, lapatinib, lentinan sulphate, letrozole, leucovorin, leuprolide, leuprolide acetate, levamisole, levofolic acid calcium salt, levothroid, levoxyl, lomustine, lonidamine, marinol, mechlorethamine, mecobalamin, medroxyprogesterone acetate, megestrol acetate, melphalan, menest, 6-mercaptopurine, mesna, methotrexate, metvix, miltefosine, minocycline, mitomycin C, mitotane, mitoxantrone, modrenal, myocet, nedaplatin, neulasta, neumega, neupogen, nilutamide, nolvadex, NSC-631570, OCT-43, octreotide, ondansetron hydrochloride, orapred, oxaliplatin, paclitaxel, pediapred, pegaspargase, pegasys, pentostatin, picibanil, pilocarpine hydrochloride, pirarubicin, plicamycin, porfimer sodium, prednimustine, prednisolone, prednisone, premarin, procarbazine, procrit, raltitrexed, RDEA119, rebif, rhenium-186 etidronate, rituximab, roferon-A, romurtide, salagen, sandostatin, sargramostim, semustine, sizofiran, sobuzoxane, solu-medrol, streptozocin, strontium-89 chloride, synthroid, tamoxifen, tamsulosin, tasonermin, tastolactone, taxoter, teceleukin, temozolomide, teniposide, testosterone propionate, testred, thioguanine, thiotepa, thyrotropin, tiludronic acid, topotecan, toremifen, tositumomab, tastuzumab, teosulfan, tretinoin, trexall, trimethylmelamine, trimetrexate, triptorelin acetate, triptorelin pamoate, UFT, uridine, valrubicin, vesnarinone, vinblastine, vincristine, vindesine, vinorelbine, virulizin, zinecard, zinostatin-stimalamer, zofran; ABI-007, acolbifen, actimmune, affinitak, aminopterin, arzoxifen, asoprisnil, atamestane, atrasentan, BAY 43-9006 (sorafenib), avastin, CCI-779, CDC-501, celebrex, cetuximab, crisnatol, cyproterone acetate, decitabine, DN-101, doxorubicin-MTC, dSLIM, dutasteride, edotecarin, eflornithine, exatecan, fenretinide, histamine dihydrochloride, histrelin hydrogel implant, holmium-166 DOTMP, ibandronic acid, interferon-gamma, intron-PEG, ixabepilone, keyhole limpet hemocyanine, L-651582, lanreotide, lasofoxifen, libra, lonafarnib, miproxifen, minodronate, MS-209, liposomal MTP-PE, MX-6, nafarelin, nemorubicin, neovastat, nolatrexed, oblimersen, onko-TCS, osidem, paclitaxel polyglutamate, pamidronate disodium, PN-401, QS-21, quazepam, R-1549, raloxifen, ranpirnas, 13-cis-retic acid, satraplatin, seocalcitol, T-138067, tarceva, taxoprexin, thymosin-alpha-1, tiazofurin, tipifarnib, tirapazamine, TLK-286, toremifen, transMID-107R, valspodar, vapreotide, vatalanib, verteporfin, vinflunin, Z-100, and zoledronic acid. 4. A pharmaceutical formulation comprising a compound according to claim 1 and a pharmaceutically acceptable excipient. 5. A method for the treatment of breast carcinomas, colorectal carcinomas, prostate carcinomas or non-small-cell bronchial carcinomas comprising administering to a human or other mammal in need thereof a therapeutically effective amount of a compound according to claim 1. 6. A method for the treatment of hormone receptor-positive breast carcinomas or androgen receptor-negative prostate carcinomas comprising administering to a human or other mammal in need thereof a therapeutically effective amount of a compound according to claim 1. 7. A method for the treatment of breast carcinomas, colorectal carcinomas, prostate carcinomas or non-small-cell bronchial carcinomas comprising administering to a human or other mammal in need thereof a therapeutically effective amount of a compound according to claim 2. 8. A method for the treatment of hormone receptor-positive breast carcinomas or androgen receptor-negative prostate carcinomas comprising administering to a human or other mammal in need thereof a therapeutically effective amount of a compound according to claim 2.

Details for Patent 9,278,925

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Merck Teknika Llc	TICE BCG	bcg live	For Injection	102821	06/21/1989		2031-08-04
Merck Sharp & Dohme Corp.	INTRON A	interferon alfa-2b	For Injection	103132	06/04/1986		2031-08-04
Merck Sharp & Dohme Corp.	INTRON A	interferon alfa-2b	For Injection	103132			2031-08-04