Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1997-06-30
2003-09-23
Qazi, Sabiha (Department: 1616)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S256000, C514S277000, C514S299000, C546S133000, C546S137000
Reexamination Certificate
active
06624173
ABSTRACT:
BACKGROUND OF THE INVENTION
The present invention relates to pharmaceutical compositions, and particularly pharmaceutical compositions incorporating compounds which are capable of affecting nicotinic cholinergic receptors. The present invention also relates to methods for treating a wide variety of conditions and disorders, and particularly conditions and disorders associated with dysfunction of the central and autonomic nervous systems.
Nicotine has been proposed to have a number of pharmacological effects. See, for example, Pullan et al.
N. Engl. J. Med
. 330:811-815 (1994). Certain of those effects may be related to effects upon neurotransmitter release. See for example, Sjak-shie et al.,
Brain Res
. 624:295 (1993), where neuroprotective effects of nicotine are proposed. Release of acetylcholine and dopamine by neurons upon administration of nicotine has been reported by Rowell et al.,
J. Neurochem
. 43:1593 (1984); Rapier et al.,
J. Neurochem
. 50:1123 (1988); Sandor et al.,
Brain Res
. 567:313 (1991) and Vizi,
Br. J. Pharmacol
. 47:765 (1973). Release of norepinephrine by neurons upon administration of nicotine has been reported by Hall et al.,
Biochem. Pharmacol
. 21:1829 (1972). Release of serotonin by neurons upon administration of nicotine has been reported by Hery et al.,
Arch. Int. Pharmacodyn. Ther
. 296:91 (1977). Release of glutamate by neurons upon administration of nicotine has been reported by Toth et al.,
Neurochem Res
. 17:265 (1992). In addition, nicotine reportedly potentiates the pharmacological behavior of certain pharmaceutical compositions used for the treatment of certain CNS disorders. See, Sanberg et al.,
Pharmacol. Biochem. & Behavior
46:303 (1993); Harsing et al.,
J. Neurochem
. 59:48 (1993) and Hughes,
Proceedings from Intl. Symp. Nic
. S40 (1994). Furthermore, various other beneficial pharmacological effects of nicotine have been proposed. See, Decina et al.,
Biol. Psychiatry
28:502 (1990); Wagner et al.,
Pharmacopsychiatty
21:301 (1988); Pomerleau et al.,
Addictive Behaviors
9:265 (1984); Onaivi et al.,
Life Sci
. 54(3):193 (1994) and Hamon,
Trends in Pharmacol. Res
. 15:36.
Various nicotinic compounds have be-en reported as being useful for treating a wide variety of conditions and disorders. See, for example, Williams et al.
DN&P
7(4):205-227 (1994), Arneric et al., CNS
Drug Rev
. 1(1):1-26 (1995), Arneric et al., Exp. Opin. Invest.
Drugs
5(1):79-100 (1996), Bencherif et al.,
JPET
279:1413 (1996), Lippiello et al.,
JPET
279:1422 (1996), PCT WO 94/08992, PCT WO 96/31475, and U.S. Pat. No. 5,583,140 to Bencherif et al., U.S. Pat. No. 5,597,919 to Dull et al., and U.S. Pat. No. 5,604,231 to Smith et al. Nicotinic compounds are particularly useful for treating a wide variety of Central Nervous System (CNS) disorders.
CNS disorders are a type of neurological disorder. CNS disorders can be drug induced; can be attributed to genetic predisposition, infection or trauma; or can be of unknown etiology. CNS disorders comprise neuropsychiatric disorders, neurological diseases and mental illnesses; and include neurodegenerative diseases, behavioral disorders, cognitive disorders and cognitive affective disorders. There are several CNS disorders whose clinical manifestations have been attributed to CNS dysfunction (i.e., disorders resulting from inappropriate levels of neurotransmitter release, inappropriate properties of neurotransmitter receptors, and/or inappropriate interaction between neurotransmitters and neurotransmitter receptors). Several CNS disorders can be attributed to a cholinergic deficiency, a dopaminergic deficiency, an adrenergic deficiency and/or a serotonergic deficiency. CNS disorders of relatively common occurrence include presenile dementia (early onset Alzheimer's disease), senile dementia (dementia of the Alzheimer's type), Parkinsonism including Parkinson's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, attention deficit disorder, anxiety, dyslexia, schizophrenia and Tourette's syndrome.
Senile dementia of the Alzheimer's type (SDAT) is a debilitating neurodegenerative disease, mainly afflicting the elderly; characterized by a progressive intellectual and personality decline, as well as a loss of memory, perception, reasoning, orientation and judgment. One feature of the disease is an observed decline in the function of cholinergic systems, and specifically, a severe depletion of cholinergic neurons (i.e., neurons that release acetylcholine, which is believed to be a neurotransmitter involved in learning and memory mechanisms). See, Jones, et al.,
Intern. J. Neurosci
. 50:147 (1990); Perry,
Br. Med. Bull
. 42:63 (1986); and Sitaram, et al.,
Science
201:274 (1978). It has been observed that nicotinic acetylcholine receptors, which bind nicotine and other nicotinic agonists with high affinity, are depleted during the progression of SDAT. See, Giacobini,
J. Neurosci. Res
. 27:548 (1990); and Baron,
Neurology
36:1490 (1986). As such, it would seem desirable to provide therapeutic compounds which either directly activate nicotinic receptors in place of acetylcholine or act to minimize the loss of those nicotinic receptors.
Certain attempts have been made to treat SDAT. For example, nicotine has been suggested to possess an ability to activate nicotinic cholinergic receptors upon acute administration, and to elicit an increase in the number of such receptors upon chronic administration to animals. See, Rowell,
Adv. Behav. Biol
. 31:191 (1987); and Marks,
J. Pharmacol. Exp. Ther
. 226:817 (1983). It also has been proposed that nicotine can act directly to elicit the release of acetylcholine in brain tissue, to improve cognitive functions, and to enhance attention. See, Rowell, et al.,
J. Neurochem
. 43:1593 (1984); Sherwood, Human
Psychopharm
. 8:155 (1993); Hodges, et al.,
Bio. of Nic
. Edit. by Lippiello, et al., p. 157 (1991); Sahakian, et al.,
Br. J. Psych
. 154:797 (1989); and U.S. Pat. No. 4,965,074 to Leeson and U.S. Pat. No. 5,242,935 to Lippiello et al. Other methods for treating SDAT have been proposed, including U.S. Pat. No. 5,212,188 to Caldwell et al. and U.S. Pat. No. 5,227,391 to Caldwell et al., European Patent Application No. 588,917 and PCT WO 96/30372. Another proposed treatment for SDAT is COGNEX®, which is a capsule containing tacrine hydrochloride, available from Parke-Davis Division of Warner-Lambert Company, which reportedly preserves existing acetylcholine levels in patients treated therewith.
Parkinson's disease (PD) is a debilitating neurodegenerative disease, presently of unknown etiology, characterized by tremors and muscular rigidity. A feature of the disease appears to involve the degeneration of dopaminergic neurons (i.e., which secrete dopamine). One symptom of the disease has been observed to be a concomitant loss of nicotinic receptors which are associated with such dopaminergic neurons, and which are believed to modulate the process of dopamine secretion. See, Rinne, et al.,
Brain Res
. 54:167 (1991) and Clark, et al.,
Br. J. Pharm
. 85:827 (1985). It also has been proposed that nicotine can ameliorate the symptoms of PD. See, Smith et al.,
Rev. Neurosci
. 3(1):25 (1992).
Certain attempts have been made to treat PD. One proposed treatment for PD is SINEMET CR®, which is a sustained-release tablet containing a mixture of carbidopa and levodopa, available from The DuPont Merck Pharmaceutical Co. Another proposed treatment for PD is ELDEPRYL®, which is a tablet containing selefiline hydrochloride, available from Somerset Pharmaceuticals, Inc. Another proposed treatment for PD is PARLODEL®, which is a tablet containing bromocriptine mesylate, available from Sandoz Pharmaceuticals Corporation. Another method for treating PD and a variety of other neurodegenerative diseases has been proposed in U.S. Pat. No. 5,210,076 to Berliner et al.
Tourette's syndrome (TS) is an autosomal dominant neuropsychiatric disorder characterized by a range of neurological and behavioral symptoms. Typical symptoms inclu
Bhatti Balwinder Singh
Caldwell William Scott
Crooks Peter Anthony
Deo Niranjan Madhukar
Dull Gary Maurice
Qazi Sabiha
Targacept, Inc.
Womble Carlyle Sandridge & Rice PLLC
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