September 24, 2012

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The following patent record is from the CAplusSM database.


Patent Number: WO 2012093101
Title: Indole compounds or analogs thereof as complement factor D inhibitors useful for the
treatment of age-related macular degeneration and their preparation
Inventor(s): Altmann, Eva; Hommel, Ulrich; Lorthiois, Edwige Liliane Jeanne; Maibaum, Juergen Klaus; Ostermann, Nils; Quancard, Jean; Randl, Stefan Andreas; Simic, Oliver; Vulpetti, Anna; Rogel, Olivier
Patent Assignee(s): Novartis AG, Switz.
Source: PCT Int. Appl., 566pp. CODEN: PIXXD2
Language: English


The invention provides a compound of formula I: a method for manufacturing the compds. of the invention, and its therapeutic uses. The invention further provides a combination of pharmacol. active agents and a pharmaceutical composition  Compds. of formula I wherein Z1 is  C and N; Z2 is CR2 and N; C4 is CR4 and N; Z5 is CR5, N and N-oxide; Z6 is CR6, N and N- oxide; Z7 is CR7, N and N-oxide; each Z is independently C and N; L is NH, CH2 and CHR1; R1  is H, OH and amino; R2 is H and C1-6 alkyl; R3 is H, C1-4 alkyl, C1-4 hydroxyalkyl, etc.; R4 is H, halo and C1-6 alkyl; R5 and R6 are independently H, halo, OH, amino, etc.; R7 is H,  halo, C1-6 alkoxy, etc.; X1 is (un)substituted methylene and S; X2 is (un)substituted  methylene, S, O, NH, etc.; X1X2 may be taken together for form (un)substituted ethylene; X3  is (un)substituted C0-2 alkylene; X2X3 taken together to form N=CH, , N=C-C1-4 alkyl; G is  CONH, CH2NHSO2, CH2NHCO, etc.;R20is H and C1-6 alkyl; R21 is H, OH, halo, C1-6 alkyl, etc.;  R22 is H and C1-6 alkyl; Z is C1-6 alkyl, C1-6 haloalkyl, Ph, etc.; and with provisions; and  pharmaceutically acceptable salt thereof, are claimed.  Example compound II was prepared by  amidation of (2S,4R)-1-(1-carbamoyl-1H-indol-3-ylcarbamoyl)- 4-fluoropyrrolidine-2-carboxylic  acid with 3-chloro-2-fluorobenzylamine. All the invention compds. were evaluated for their  complement factor D inhibitory activity.  From the assay, it was determined that compound II  exhibited IC50 value of 7 nM.

Please note:  Titles and abstracts for patent records in CAplus are routinely enhanced to better describe the claimed invention. In this example, CAS enhanced both the abstract and title using additional information found in the patent. The original title of the PCT publication is Indole compounds or analogues thereof useful for the treatment of age-related macular degeneration (AMD). For the CAplus record, this title was enhanced to read Indole compounds or analogs thereof as complement factor D inhibitors useful for the treatment of age-related macular degeneration and their preparation.

 View the full-text here.

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