Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
1997-03-24
2001-07-10
MacMillan, Keith D. (Department: 1627)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C514S315000
Reexamination Certificate
active
06258807
ABSTRACT:
FIELD OF THE INVENTION
This invention provides a method for using 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine, (hereinafter referred as “olanzapine”) for the treatment of pain. The present invention provides a method which is especially useful for the treatment of acute pain, nociceptive, and neuropathic pain.
BACKGROUND OF THE INVENTION
The present invention provides a method for treating pain.
The present invention provides a method for treating acute self-limiting ailments, low-grade somatic-type acute pain, including for example, but not limited to headache, arthritis, simple muscle strain, and dysmenorrhea. The invention further provides a method for treating neuropathic pain. Additionally, this invention provides a method for treating nociceptive pain.
There is a demand for more active analgesic agents with diminished side effects and toxicity and which are non-addictive. The ideal analgesic would reduce the awareness of pain, produce analgesia over a wide range of pain types, act satisfactorily whether given orally or parenterally, produce minimal or no side effects, be free from tendency to produce tolerance and drug dependence.
Applicants have discovered that olanzapine can provide many of the characteristics of an ideal analgesic for the treatment of pain.
It is known that olanzapine can provide antipsychotic activity and is commercially available for the treatment of psychosis. Olanzapine is a known compound and described in U.S. Pat. No. 5,229,382 as being useful for the treatment of schizophrenia, schizophreniform disorder, acute mania, mild anxiety states, and psychosis. U.S. Pat. No. 5,229,382 is herein incorporated by reference in its entirety. Surprisingly, and in accordance with this invention, Applicants have discovered that olanzapine can be useful for the treatment of pain. Olanzapine could address a long felt need for a safe and effective treatment for acute pain.
SUMMARY OF THE INVENTION
The present invention provides a method for treating pain comprising administering an effective amount of olanzapine to an animal in need of such treatment.
The present invention provides a method for treating acute pain comprising administering to a patient in need thereof, an analgesic dosage of olanzapine or a pharmaceutically acceptable salt thereof.
It is preferred that the acute pain shall be selected from the group consisting of headache, arthritis, simple muscle strain, and dysmenorrhea.
The present invention provides a method for treating nociceptive pain comprising administering to a patient in need thereof, an analgesic dosage of olanzapine or a pharmaceutically acceptable salt thereof.
The present invention provides a method for treating neuropathic pain comprising administering to a patient in need thereof, an analgesic dosage of olanzapine or a pharmaceutically acceptable salt thereof.
It is preferred that the neuropathic pain is selected from the group consisting of chronic lower back pain, pain associated with arthritis, cancer-associated pain, herpes neuralgia, phantom limb pain, central pain, opioid resistant neuropathic pain, bone injury pain, and pain during labor and delivery.
It is preferred that the nociceptive pain is selected from the group consisting of post-operative pain, cluster headaches, dental pain, surgical pain, pain resulting from severe, for example third degree, burns, post partum pain, angina pain, genitourinary tract related pain, and including cystitis.
Finally, the present invention can provide a method for treating inflammation in an animal comprising administering an anti-inflammatory dose of olanzapine to an animal in need of such treatment.
DETAILED DESCRIPTION OF THE INVENTION
Olanzapine is of the formula
or an acid addition salt thereof.
It is especially preferred that olanzapine will be the Form II olanzapine polymorph having a typical x-ray powder diffraction pattern as represented by the following interplanar spacings:
d
10.2689
8.577
7.4721
7.125
6.1459
6.071
5.4849
5.2181
5.1251
4.9874
4.7665
4.7158
4.4787
4.3307
4.2294
4.141
3.9873
3.7206
3.5645
3.5366
3.3828
3.2516
3.134
3.0848
3.0638
3.0111
2.8739
2.8102
2.7217
2.6432
2.6007
A typical example of an x-ray diffraction pattern for Form II is as follows wherein d represents the interplanar spacing and I/I
1
represents the typical relative intensities:
d
I/I
1
10.2689
100.00
8.577
7.96
7.4721
1.41
7.125
6.50
6.1459
3.12
6.071
5.12
5.4849
0.52
5.2181
6.86
5.1251
2.47
4.9874
7.41
4.7665
4.03
4.7158
6.80
4.4787
14.72
4.3307
1.48
4.2294
23.19
4.141
11.28
3.9873
9.01
3.7206
14.04
3.5645
2.27
3.5366
4.85
3.3828
3.47
3.2516
1.25
3.134
0.81
3.0848
0.45
3.0638
1.34
3.0111
3.51
2.8739
0.79
2.8102
1.47
2.7217
0.20
2.6432
1.26
2.6007 0.77
The x-ray diffraction patterns set out herein were obtained using a Siemens D5000 x-ray powder diffractometer having a copper K
a
radiation source of wavelength, 1=1.541 Å.
It is further preferred that the Form II olanzapine polymorph will be administered as the substantially pure Form II olanzapine polymorph.
As used herein “substantially pure” refers to Form II associated with less than about 5% Form I, preferably less than about 2% Form I, and more preferably less than about 1% Form I. Further, “substantially pure” Form II should contain less than about 0.5% related substances, wherein “related substances” refers to undesired chemical impurities or residual solvent or water. In particular, “substantially pure” Form II should contain less than about 0.05% content of acetonitrile, more preferably, less than about 0.005% content of acetonitrile. Additionally, the polymorph of the invention should contain less than 0.5% of associated water.
The polymorph obtainable by the process taught in the '382 patent will be designated as Form I and has a typical x-ray powder diffraction pattern substantially as follows, obtained using a Siemens D5000 x-ray powder diffractometer, wherein d represents the interplanar spacing:
d
9.9463
8.5579
8.2445
6.8862
6.3787
6.2439
5.5895
5.3055
4.9815
4.8333
4.7255
4.6286
4.533
4.4624
4.2915
4.2346
4.0855
3.8254
3.7489
3.6983
3.5817
3.5064
3.3392
3.2806
3.2138
3.1118
3.0507
2.948
2.8172
2.7589
2.6597
2.6336
2.5956
A typical example of an x-ray diffraction pattern for Form I is as follows wherein d represents the interplanar spacing and I/I
1
represents the typical relative intensities:
d
I/I
1
9.9463
100.00
8.5579
15.18
8.2445
1.96
6.8862
14.73
6.3787
4.25
6.2439
5.21
5.5895
1.10
5.3055
0.95
4.9815
6.14
4.8333
68.37
4.7255
21.88
4.6286
3.82
4.533
17.83
4.4624
5.02
4.2915
9.19
4.2346
18.88
4.0855
17.29
3.8254
6.49
3.7489
10.64
3.6983
14.65
3.5817
3.04
3.5064
9.23
3.3392
4.67
3.2806
1.96
3.2138
2.52
3.1118
4.81
3.0507
1.96
2.948
2.40
2.8172
2.89
2.7589
2.27
2.6597
1.86
2.6336
1.10
2.5956
1.73
The x-ray powder diffraction patterns herein were obtained with a copper K
a
of wavelength l=1.541 Å. The interplanar spacings in the column marked “d” are in Angstroms. The typical relative intensities are in the column marked “I/I
1
”.
As used herein, “animal” refers to a vertebrate animal. The most preferred animal is a mammal. As used herein, the term “mammal” shall refer to the Mammalia class of higher vertebrates. The term “mammal” includes, but is not limited to, a human. The term “treating” as used herein includes prophylaxis of the named condition or amelioration or elimination of the condition once it has been established.
Olanzapine is effective over a wide dosage range; however, it is desirable to administer a dosage that is as low as possible. For example, dosages per day of the olanzapine will normally fall within the range of about 0.1 mg to about 30 mg per day. However, it will be understood that the amount of the compound actually administered will be determined by a physician, in the light of the relevant circumstances including the type of acute pain to be treated, the age, weight, and response of t
Helton David R.
Kallman Mary J.
Shannon Harlan E.
Womer Daniel E.
Eli Lilly and Company
Harrison Nancy
MacMillan Keith D.
Palmberg Arleen
Prasthofer Thomas
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