EPO – Principal Directorate Business Services – Directorate Classification
Project: C471
Subject: Medicinal preparations
characterised by the non-active
ingredients used
Comments
Ref.:
IPC: A61K 47/00
15-07-2015
Annex 43-47 of project file
1. EP thanks Rapporteur once more for all the effort put into this project.
2. In order to advance the project and to support the Rapporteur, EP has modified the scheme
from Annex 43 instead of only commenting on it.
2.a. EP has tried to compromise in the outstanding points as much as possible.
We merely maintain our position with regard to A61K47/06.
We have reconsidered the issue with mineral oil and petrolatum and discussed this
extensively with examiners/scientists in the field. However, we cannot agree with the place
they are put in in the version of annex 43.
This conclusion is based on the architecture of the A61K47 scheme and the definition of these
compounds in the Handbook of Pharmaceutical Excipients:
“Mineral oil is a mixture of refined liquid saturated aliphatic (C14–C18) and cyclic
hydrocarbons obtained from petroleum.” “Petrolatum is a purified mixture of semisolid
saturated hydrocarbons having the general formula CnH2n+2, and is obtained from
petroleum.”
The A61K47 scheme is built-up by trying to characterize compounds by their functionality.
Going down in the scheme, there is a variety in functional groups, atoms or structure
complexity.
Mineral oil and petrolatum only comprise hydrocarbons. They do not have functional groups
which the natural oils such as olive oil, castor oil, lanolin do have. These compounds all have
functional groups e.g. esters, alcohol, acids. Because classifying these compounds by giving
symbols for each of these functional groups would amount to structurally allocating at least 2
different symbols to one oil, the symbol A61K47/44 is present.
So although one could argue that mineral oil comes from nature it cannot be considered a
natural oil in the sense of A61K47/44.
2.b. At the same time EP has proposed a few additional examples in subgroups A61K47/16,
47/32 and 47/36 which do not change the scope of the subgroups.
2.c. EP has also proposed some modifications to the status indicators (U, M, C). If this is
accepted the RCL would need to be adapted accordingly.
3. Modifications are based on Annex 43 and EP modifications are shown in blue color.
Yellow – add to scheme as in Annex 43
added by EP, deleted by EP
Medicinal preparations characterised by the non-active ingredients used, e.g.,
carriers, inert additives; targeting or modifying agents chemically bound to the
active ingredient
M
47/00
C
47/02
・
Inorganic compounds (macromolecular inorganic compounds A61K 47/30)
U
47/04
・・
non metals; compounds thereof
M
47/06
・
Organic compounds, e.g., synthetic hydrocarbons, synthetic polyolefins,
mineral oil, petrolatum
M
47/08
・・
containing oxygen, e.g., ethers, acetals, ketones, quinones, aldehydes,
peroxides
C
47/10
・・・
Alcohols; Phenols; Salts thereof, e.g., glycerol; Polyethylene glycols ( PEG);
Poloxamers; PEG/POE alkyl ethers ( sugar alcohols A61K 47/26; copolymers
containing polyalkylene glycol or poloxamer A61K 47/34 )
U
47/12
・・・
Carboxylic acids; Salts or anhydrides thereof
M
47/14
・・・
Esters of carboxylic acids, e.g., fatty acid monoglycerides, medium-chain
triglycerides, parabens, PEG fatty acid esters
M
47/16
・・
containing nitrogen, e.g., nitro-, nitroso-, azo-compounds, nitriles, cyanates
C
47/18
・・・
Amines ; Quaternary ammonium compounds, e.g., amides, ureas; amino
acids, aminosulphonic acids, aliphatic amines, poloxamines; Oligopeptides
having up to 5 amino acids
M
47/20
・・
containing sulfur, e.g., DMSO, docusate, sodium lauryl sulfate
M
47/22
・・
Heterocyclic compounds, e.g., ascorbic acid, tocopherol, pyrrolidones
M
47/24
・・
containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or
sulfur, e.g., cyclomethicone, phospholipids
C
47/26
・・
Carbohydrates, e.g., mono-, di-, oligosaccharides, nucleic acids, sugar
alcohols, amino sugars; Derivatives thereof, e.g. polysorbates, sorbitan fatty
acid esters, glycyrrhizin
M
47/28
・・
Steroids, e.g., cholesterol, bile acids, glycyrrhetinic acid
M
47/30
.
Macromolecular compounds, including both organic and inorganic
compounds, e.g., inorganic polyphosphate
M
47/32
・・
Macromolecular compounds obtained by reactions only involving carbon-tocarbon unsaturated bonds, e.g., carbomers, poly(meth)acrylates, polyvinyl
pyrrolidone
C
47/34
・・
Macromolecular compounds obtained otherwise than by reactions only
involving carbon-to-carbon unsaturated bonds, e.g., polyesters, polyamino
acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or
poloxamers ( PEG or poloxamers A61K 47/10)
M
47/36
・・
Polysaccharides ; Derivatives thereof, e.g., gums, starch, alginate, dextrin,
hyaluronic acid, chitosan, inulin, agar, pectin
U
47/38
・・・
Cellulose; Derivatives thereof
C
47/40
・・・
Cyclodextrins ; Derivatives thereof (cyclodextrin inclusion compounds A61K
47/48769 )
C
47/42
・・
Proteins ; Polypeptides ; Degradation products thereof ; Derivatives thereof
e.g., albumin, gelatin, zein (oligopeptides having up to 5 amino acids A61K
47/18 ; polyamino acids A61K 47/34 )
C
47/44
・
Oils, fats or waxes according to more than one of groups A61K 47/02 – A61K
47/42; Natural or modified natural oils, fats or waxes, e.g., mineral oil,
petrolatum, (polyethoxylated) castor oil, montan wax, ozokerite, lignite,
shellac, rosin, beeswax, lanolin ( synthetic glycerides, e.g., medium-chain
triglycerides A61K 47/14 )
M
47/46
・
Ingredients of undetermined constitution or reaction products thereof, e.g.,
skin, bone, milk, cotton fiber, eggshell, oxgall, plant extracts
C
47/48
・
The non-active ingredient being chemically bound to the active ingredient,
e.g., polymer-drug conjugates
N
47/48007
・・
the non-active ingredient being a modifying agent
N
47/48015
・・・
the modifying agent being an inorganic compound; e.g., an inorganic ion that
is complexed with the active ingredient
N
47/48023
・・・
the modifying agent being an organic compound
・・・・
the modifying agent being also a pharmacologically or therapeutically active
agent, i.e., the entire conjugate being a codrug, i.e., a dimer, oligomer or
polymer of pharmacologically or therapeutically active compounds, e.g., a
polymer of asprin
N
47/481
N
47/48169
・・・
the modifying agent being an organic macromolecular compound, i.e., an
oligomeric, polymeric, dendrimeric molecule
N
47/48176
・・・・
the organic macromolecular compound has been obtained by reactions only
involving carbon-to-carbon unsaturated bonds, e.g., poly(meth)acrylate,
polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol,
polystyrene sulfonic acid resin
N
47/48192
・・・・
the organic macromolecular compound has been obtained otherwise than by
reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas,
polyurethanes
N
47/48215
・・・・・
the organic macromolecular compound being a polyoxyalkylene
oligomer,polymer, dendrimer, e.g., PEG, PPG, PEO, polyglycerol
N
47/4823
・・・・
the organic macromolecular compound being a polysaccharide or a
derivative, e.g., starch, chitosan, chitin, cellulose, pectin, cyclodextrin with the
pharmacologically active agent being covalently linked to the external surface
of the ring structure, a bacterial polysaccharide or oligosaccharide antigen, a
glycosaminoglycan
N
47/48238
・・・
the modifying agent being a protein, peptide, polyamino acid
N
47/48246
・・・・
drug-peptide, protein or polyamino acid conjugates, i.e., the modifying agent
being a protein, peptide or polyamino acid which is covalently bonded or
complexed to a therapeutically active agent (peptidic linkers A61K 47/48338)
N
47/48338
・・・・
peptidic linker, binder, spacer, e.g., peptidic enzyme-labile linker
N
47/48346
・・・・
the modifying agent being a pre-targeting system involving a peptide or
protein
( not an antibody A61K 47/48369 ) for targeting specific cells
N
47/48369
・・・
the modifying agent being an antibody, an immunoglobulin or a fragment
thereof, e.g., a Fc-fragment
N
47/48769
・・
the conjugate being characterized by a special physical or galenical form,
e.g., cell, gel, colloid, dispersion, emulsion, particle, capsule, inclusion
complex, device or kit
4. With regard to Annex 44 EP would like to submit a modified proposal which is more
adapted to A61K47/48, which does not deal with radioactive substances:
Pre-targeting system
An example of this is an immuno-conjugate that has a part
that recognizes a target antigen and a part that recognizes a
further substance to which a therapeutic agent is
attached. When said conjugate is administered it binds to
target cells, furnishing said cells with binding sites for the
therapeutic agent
Petra van de Wetering, Anwyn Dullaart
Ingo Seelmann (iseelmann@epo.org)