Claims for Patent: 9,512,130

Summary for Patent: 9,512,130

Title:	Substituted imidazopyridazines
Abstract:	The present invention relates to substituted imidazopyridazine compounds, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
Inventor(s):	Koppitz; Marcus (Berlin, DE), Klar; Ulrich (Berlin, DE), Wengner; Antje Margret (Berlin, DE), Neuhaus; Roland (Berlin, DE), Siemeister; Gerhard (Berlin, DE), Bruning; Michael (Berlin, DE)
Assignee:	BAYER PHARMA AKTIENGESELLSCHAFT (Berlin, DE)
Application Number:	14/771,648
Patent Claims:	1. A compound of formula (A), (B) or (C): ##STR00044## or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same. 2. A pharmaceutical composition comprising a compound according to claim 1, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, particularly a pharmaceutically acceptable salt thereof, or a mixture of same, and a pharmaceutically acceptable diluent or carrier. 3. A pharmaceutical combination comprising: a compound according to claim 1, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof, or a mixture of same; and one or more agents selected from: a taxane, Docetaxel, Paclitaxel, or Taxol; an epothilone, Ixabepilone, Patupilone, or Sagopilone; Mitoxantrone; Predinisolone; Dexamethasone; Estramustin; Vinblastin; Vincristin; Doxorubicin; Adriamycin; Idarubicin; Daunorubicin; Bleomycin; Etoposide; Cyclophosphamide; Ifosfamide; Procarbazine; Melphalan; 5-Fluorouracil; Capecitabine; Fludarabine; Cytarabine; Ara-C; 2-Chloro-2''-deoxyadenosine; Thioguanine; an anti-androgen, Flutamide, Cyproterone acetate, or Bicalutamide; Bortezomib; a platinum derivative, Cisplatin, or Carboplatin; Chlorambucil; Methotrexate; and Rituximab. 4. A method of preparing a compound according to claim 1, comprising reacting an intermediate compound of formula (A1), (B1) or (C1): ##STR00045## in which Z' represents a group selected from: --C(.dbd.O)OH and --C(.dbd.O)O--(C.sub.1-C.sub.6-alkyl); with a compound of formula Ib: ##STR00046## thereby giving, upon optional deprotection, a compound of formula (A), (B) or (C) as defined in claim 1. 5. A method of preparing a compound according to claim 1, comprising reacting an intermediate compound of formula (A2), (B2) or (C2): ##STR00047## in which Q.sup.2 is a leaving group; with a compound of formula IIa: ##STR00048## in which Y is a substituent which is displaced in a coupling reaction; thereby giving, upon optional deprotection, a compound of formula (A), (B) or (C), as defined in claim 1. 6. A method of preparing a compound according to claim 1, comprising reacting an intermediate compound of formula (A3), (B3) or (C3): ##STR00049## in which Q.sup.1 is a leaving group; with a compound of formula (A4), (B4) or (C4): ##STR00050## thereby giving, upon optional deprotection, a compound of formula (A), (B) or (C), as defined in claim 1. 7. A method of preparing a compound according to claim 1, comprising reacting an intermediate compound of formula (A5), (B5) or (C5): ##STR00051## in which Q.sup.3 is an optionally protected NH.sub.2-group; with a compound of formula (A6), (B6) or (C6): ##STR00052## thereby giving, after reduction of the imine, and upon optional deprotection, a compound of formula (A), (B) or (C), as defined in claim 1. 8. A method of preparing a compound according claim 1, comprising reacting an intermediate compound of formula (A7), (B7) or (C7): ##STR00053## in which R.sup.3' is a leaving group; with a compound of formula (A8), (B8) or (C8): ##STR00054## in which Y is a substituent which is displaced in a coupling reaction; thereby giving a compound of formula (A), (B) or (C), as defined in claim 1. 9. A compound according to claim 1, which is ##STR00055## 10. A compound according to claim 1, which is a salt of ##STR00056##

Details for Patent 9,512,130

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	RITUXAN	rituximab	Injection	103705	11/26/1997		2033-03-01
Idec Pharmaceuticals Corp.	RITUXAN	rituximab	Injection	103737	02/19/2002		2033-03-01
Genentech, Inc.	RITUXAN HYCELA	rituximab and hyaluronidase human	Injection	761064	06/22/2017		2033-03-01